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  • pharmacokinetics  (96)
  • Lepidoptera  (62)
  • phosphorus  (43)
  • Springer  (201)
  • 2020-2024
  • 1990-1994  (201)
  • 1992  (201)
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  • 2020-2024
  • 1990-1994  (201)
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  • 1
    Electronic Resource
    Electronic Resource
    Response of the braconid parasitoid Cotesia (= Apanteles) glomerata to volatile infochemicals: effects of bioassay set-up, parasitoid age and experience and barometric flux (1992)
    Springer
    Entomologia experimentalis et applicata 63 (1992), S. 163-175 
    Details
    ISSN: 1570-7458
    Keywords: Hymenoptera ; Braconidae ; Lepidoptera ; Pieridae ; cabbage ; tritrophic interactions ; semiochemicals ; host-habitat location ; foraging behaviour
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Upon initiating a research project on the role of volatile infochemicals in the tritrophic system Cotesia (= Apanteles) glomerata (L.)-Pieris brassicae (L.)-cabbage, a bioassay was developed to investigate the response of C. glomerata. The bioassay should be effective in terms of high responsiveness and minimum variability and constructed through a comparative approach. Twenty seven treatments, organized in a factorial randomized block design, compared the effect of three bioassay set-ups (glasshouse flight chamber, wind-tunnel and Y-tube olfactometer), three parasitoid age groups (1–2, 4–5 and 8–9 days old females), three pre-treatment experiences (naive, damage experienced and oviposition experienced wasps) and the day-to-day effect on response of C. glomerata to clean cabbage (CC) and planthost complex (PHC) in a dual choice test. The best results with regard to the strength and consistency of response to the PHC were obtained in the glasshouse flight-chamber by 4–5 days old female wasps with either damage or oviposition experience (94 and 90%, respectively). It is therefore recommended as a suitable bioassay for studying the role of volatile infochemicals in host-habitat location by C. glomerata. A day-to-day variation in response was found in the glasshouse and wind-tunnel. It was correlated with the direction of change in barometric pressure within the time period of the experiment, showing that steadily increasing atmospheric pressure yields a significantly higher response than steadily decreasing or fluctuating barometric flux. To control for the day effect it is suggested to conduct further experiments in a block design, having day as a block. Several aspects of the infochemical ecology of C. glomerata are discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00343576
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  • 2
    Electronic Resource
    Electronic Resource
    Diet-induced food preference by Manduca sexta larvae: acceptable non-host plants elicit a stronger induction than host plants (1992)
    Springer
    Entomologia experimentalis et applicata 63 (1992), S. 3-12 
    Details
    ISSN: 1570-7458
    Keywords: Feeding ; behaviour ; food preference induction ; diets ; Manduca sexta ; Lepidoptera
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Diet-induced changes in food preference by fifth instar larvae of the tobacco hornworm, Manduca sexta (Johan.) (Lepidoptera, Sphingidae), were examined. Two groups of larvae with different diet experience were used: larvae reared on a host or on an acceptable non-host plant species. Each group of larvae was offered a choice between leaf discs from each rearing plant species (2-plant choice test) and food preference was measured as the consumption of one plant species relative to that of the other plant species. Diet-induced changes in preferences were larger with the host versus acceptable non-host plant pairs Solanum pseudocapsicum (L.) versus Raphanus sativus (L.), Lycopersicon esculentum (Mill.) versus Vigna sinensis (Savi), and Datura innoxia (L.) versus V. sinensis than with the host versus host plant pairs L. esculentum versus Capsicum annuum (L.) and L. esculentum versus D. innoxia. To examine how much the food preference had been altered for each test plant species alone, two other groups of larvae were offered a choice between leaf discs from a single plant species and filter paper discs laced with distilled water (1-plant choice test). Larvae preferred the dietary plant species more strongly than the non-dietary plant species in tests using the following plant species: for C. annuum with C. annuum and L. esculentum as diets, for V. sinensis with V. sinensis and L. esculentum or D. innoxia as diets, and for R. sativus with R. sativus and S. pseudocapsicum as diets. The preference for the hosts L. esculentum and D. innoxia did not change significantly after rearing larvae on different hosts or on an acceptable non-host. Thus, diet-induction by M. sexta larvae results in an enhancement of preference for the dietary plant species which is much stronger with acceptable non-hosts than with hosts.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00350341
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  • 3
    Electronic Resource
    Electronic Resource
    Gut contents in molting lepidopteran larvae: a source of error in nutritional studies (1992)
    Springer
    Entomologia experimentalis et applicata 62 (1992), S. 87-91 
    Details
    ISSN: 1570-7458
    Keywords: Molting ; Lepidoptera ; nutritional indices
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00185646
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  • 4
    Electronic Resource
    Electronic Resource
    Resistance in certain maize cultivars to first and third-instar Chilo partellus larvae (1992)
    Springer
    Entomologia experimentalis et applicata 65 (1992), S. 75-80 
    Details
    ISSN: 1570-7458
    Keywords: Pyralidae ; Lepidoptera ; Zea mays L. ; Chilo partellus ; susceptibility
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The resistance/susceptibility levels of ten maize (Zea mays L.) cultivars to neonates and 3rd-instar larvae of Chilo partellus (Swinhoe) (Lepidoptera: Pyralidae) were measured in the field and screenhouse experiments. The maize cultivars tested were: Inbred A, Mp 704, V-37, Population 10, Hybrid 511, Katumani Composite B, ER-29 SVR, Poza Rica 7832, ICZ2-CM, and MMV 400. Most cultivars were found susceptible to 3rd-instar larvae based on the incidence of dead heart symptoms, foliar feeding and stem tunnelling caused by stem borers in both the field and screenhouse experiments. However, the maize cultivars V-37, MMV 400 and Poza Rica 7832 sustained significantly lesser damage than the other cultivars when infested with neonates or 3rd instar larvae. The screenhouse experiments conducted with five maize cultivars, i.e. Inbred A, Mp 704, V-37, ER-29 SVR, and Poza Rica 7832 showed that neonates fed less on the resistant than the susceptible maize cultivars but feeding by the 3rd instars was equally high on all the maize cultivars except Mp 704 on which the larvae fed less than the others. In the cultivars infested with neonates, the mean period for 50% moth emergence P50 was longest on Mp 704 followed by Poza Rica 7832, ER-29 SVR, V-37 and Inbred A. In the cultivars infested with 3rd-instars, P50 was longest for Poza Rica 7832 followed equally by the remaining cultivars. On the basis of the evidence presented we here conclude that neonates of C. partellus are sensitive to the growth inhibiting effects of the resistant maize cultivars Mp 704, V-37, and Poza Rica 7832 but the older larvae are insensitive to these effects of Mp 704 and V-37 but not of Poza Rica 7832.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00189719
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  • 5
    Electronic Resource
    Electronic Resource
    Diel flight periodicity of Chilo partellus (1992)
    Springer
    Entomologia experimentalis et applicata 65 (1992), S. 165-170 
    Details
    ISSN: 1570-7458
    Keywords: Lepidoptera ; Pyralidae ; stem borer ; suction trap ; behaviour ; maize ; dispersal ; pheromones ; activity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The diel flight periodicity of the nocturnal moth Chilo partellus (Swinhoe) (Lepidoptera;Pyralidae) was measured in the laboratory using an actograph and in the field with suction traps. Females showed almost no flight activity on the night of eclosion. Flight activity of mated females peaked before midnight, the period of peak oviposition activity. Male peak activity occurred after midnight coinciding with female eclosion. Presence or absence of females did not affect when or how long males were active. Data on flight activity and reproductive behaviour are discussed in relation to the use of pheromones to protect maize.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00221367
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  • 6
    Electronic Resource
    Electronic Resource
    MaleHeliothis virescens maintain upwind flight in response to experimentally pulsed filaments of their sex pheromone (Lepidoptera: Noctuidae) (1992)
    Springer
    Journal of insect behavior 5 (1992), S. 669-687 
    Details
    ISSN: 1572-8889
    Keywords: Heliothis virescens ; Noctuidae ; Lepidoptera ; upwind flight ; sex pheromone ; filaments
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Aspects of the intermittent fine structure of an odor plume were mimicked and experimentally modified in the wind tunnel using an air-pulsing device. Filaments of a behaviorally active blend of six sex-pheromone components created by the device in a temporally regular fashion elicited sustained upwind flight and source location in male Heliothis virescens.Males did not exhibit sustained upwind flight in significant numbers until a frequency of 4 filaments/s was delivered, at a loading of 1 μg of the major component, Z11-16: Ald, with the other components loaded at their appropriate ratios. A loading of 10 μg Z11-16: Ald was found to be optimal at this filament delivery rate. Electroantennogram recordings to different filament delivery rates of the complete blend indicated that a stationary male antenna can respond to the pulse rates used in this study. Importantly, when a main component necessary for upwind flight, Z9-14:Ald, was isolated into its own filaments and pulsed alternately against filaments of the five other components (including the other component essential for upwind flight, Z11-16: Ald), upwind flight to the source was significantly reduced (9%) compared to upwind flight and source location in response to filaments composed of the entire blend (30%), indicating that the complete pheromone blend must arrive on the antenna simultaneously for optimal evocation of sustained upwind progress. Neurophysiological evidence from other studies suggests that higher-order interneurons whose phasic response is enhanced when the entire blend is presented simultaneously may be of importance in explaining this behavioral difference stemming from synchronous vsasynchronous arrival of the components.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01047979
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  • 7
    Electronic Resource
    Electronic Resource
    Factors influencing the landing of maleEpiphyas postvittana (Walker) exhibiting pheromone-mediated flight (Lepidoptera: Tortricidae) (1992)
    Springer
    Journal of insect behavior 5 (1992), S. 699-720 
    Details
    ISSN: 1572-8889
    Keywords: sex pheromone ; landing behavior ; visual cues ; Epiphyas postvittana ; Lepidoptera ; Tortricidae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The effects of changes in various visual and olfactory properties of a white card surface on the landing position of male Epiphyas postvittanaexhibiting pheromone-mediated flight were studied in a wind tunnel. Males landed predominantly at the most downwind position of a surface in line with the pheromone source, regardless of the strength of the source. The position on the surface that males landed was strongly influenced by visual factors. The landing position of males appeared to be influenced by visual cues along all three axes of the surface. Decreases in either the dimension horizontally perpendicular to the wind direction or the vertical dimension resulted in greater numbers of males landing farther upwind on the surface than the downwind edge. Visual changes in the axis along the wind direction also affected the position at which males landed. For example, when presented with two white card surfaces with a 4- cm gap between them, males tended to land on the downwind edge of the upwind surface (on which the source was located). When the gap was bridged with clear Mylar, the landing pattern was significantly different, with the greater proportion of males landing on the downwind surface. However, when Mylar was placed on the plexiglass floor of the tunnel (in addition to bridging the gap), the landing pattern on the surface was not significantly different from that on the two surfaces without the Mylar bridge. It is suggested that during the prelanding and landing phases of pheromone-mediated flight, male moths orient to visual features of the surface containing the pheromone source rather than to visual features of the source (conspecific female moth) itself.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01047981
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  • 8
    Electronic Resource
    Electronic Resource
    Measurement of total dissolved phosphorus in small volumes of iron rich interstitial water (1992)
    Springer
    Aquatic sciences 54 (1992), S. 1-9 
    Details
    ISSN: 1420-9055
    Keywords: Sediment ; interstitial water ; phosphorus ; iron ; persulfate digestion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract It is shown that sorption of orthophosphate to iron compounds, formed during persulfate digestion, can cause a significant underestimation of total dissolved phosphorus in interstitial waters rich in iron and poor in phosphorus. Labelling the samples with carrier free32PO4 before digestion allows to correct for these losses.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00877261
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  • 9
    Electronic Resource
    Electronic Resource
    The influence of nutritional and genetic factors on larval performance of the cinnabar moth, Tyria jacobaeae (1992)
    Springer
    Entomologia experimentalis et applicata 62 (1992), S. 29-36 
    Details
    ISSN: 1570-7458
    Keywords: Alkaloids ; cinnabar moth ; insect genetics ; larval performance ; Lepidoptera ; nutritional ecology ; nitrogen ; sugar ; Tyria jacobaeae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract In a laboratory experiment using full-sibs, 60% of the variation in pupal weight of the monophage Tyria jacobaeae L. (Lepidoptera, Arctiidae) could be explained by variation in the nitrogen concentration of the food plant, Senecio jacobaea L. and only 4% by variation in sugar concentration. Larval weight and growth rates of young and old larvae were also positively correlated with nitrogen and sugar concentration. Developmental time was negatively correlated with nitrogen concentration. In a second experiment full-sib families differed significantly in larval weight at day 7, mortality, growth rate and developmental time. Pupal weight did not differ significantly among families, but was positively correlated with nitrogen concentration of Senecio. Larval performance was not significantly influenced by concentrations of sugars or alkaloids. We conclude that larval performance of Tyria during most of the larval period is mainly determined by genetic factors, but pupal weights are primarily determined by nitrogen concentration of the food plant.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00185638
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  • 10
    Electronic Resource
    Electronic Resource
    Deterrence of feeding and oviposition responses of adult Heliothis virescens by some compounds bitter-tasting to humans (1992)
    Springer
    Entomologia experimentalis et applicata 65 (1992), S. 81-93 
    Details
    ISSN: 1570-7458
    Keywords: Heliothis virescens ; Lepidoptera ; Noctuidae ; feeding behavior ; oviposition behavior ; electrophysiology ; deterrence ; antifeedant ; quinine ; quinidine ; atropine ; caffeine ; denatonium benzoate ; naringin ; sucrose octaacetate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Some compounds that are bitter-tasting to humans, both alkaloidal (quinine, quinidine, atropine, caffeine) and non-alkaloidal (denatonium benzoate, sucrose octaacetate, naringin), deterred feeding and oviposition by Heliothis virescens (F.) in laboratory and field cage experiments. Preliminary electrophysiological studies of gustatory sensilla on the ovipositor of H. virescens provided evidence of 3 neurons, one of which is responsive to sucrose. Preliminary indications are that responses of this neuron may be inhibited by quinine and denatonium benzoate.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00189720
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  • 11
    Electronic Resource
    Electronic Resource
    Mating behaviour of the corn stalk borerSesamia nnonagrioides (1992)
    Springer
    Entomologia experimentalis et applicata 65 (1992), S. 199-204 
    Details
    ISSN: 1570-7458
    Keywords: Sesamia nonagrioides ; Lepidoptera ; Noctuidae ; calling behaviour ; mating behaviour ; circadian rhythm
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The mating behaviour of the corn stalk borerSesamia nonagrioides (Lef.) [Lepidoptera:Noctuidae] was studied under laboratory conditions at 25 ± 1 °C, 65 ± 5% r.h. and 16:8 (L:D) regime. The females began calling during the first scotophase following emergence, the peak of calling occurred during the second scotophase and thereafter decreased. Maximum calling was observed between the fourth and sixth hour of the scotophase. The calling pattern varied with age. During the first and second scotophase most of the females were calling continuously, while during the third and fourth scotophase periodic calling was observed. The mean onset of calling was advanced and the mean length of calling per day was increased slightly as the female became older. Females held for 72 h in continuous darkness exhibited an endogenous circadian rhythm of calling. Matings began during the first scotophase following emergence and the peak of mating was observed during the second scotophase. Mated females did not remate. Few males mated more than once during the following scotophases.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02343852
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  • 12
    Electronic Resource
    Electronic Resource
    Localization of spectral receptors in the ommatidium of butterfly compound eye determined by polarization sensitivity (1992)
    Springer
    Journal of comparative physiology 171 (1992), S. 289-297 
    Details
    ISSN: 1432-1351
    Keywords: Electrophysiology ; Lepidoptera ; Photoreceptor ; Spectral sensitivity ; Vision
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary 1. A butterfly Papilio has 5 types of spectral receptors in the compound eye. The spectral sensitivity of each type peaks in the UV, violet, blue, green, and red wavelengths, respectively. The green type contains two subtypes with and without a UV secondary peak. Here we studied the localization of these spectral receptors within the ommatidium. 2. An ommatidium contains 9 photoreceptors (R1–9), each of which is one of the 5 spectral receptor types. The photoreceptors bear parallel microvilli to form a nontwisted rhabdom, and thereby the photoreceptors are polarization sensitive. 3. We first examined the microvillar orientation by electron microscopy. The microvilli of R1, 2, and 9 are oriented dorso-ventrally (0°), whereas those of R3 and 4 are parallel to the antero-posterior axis (90°). The R5–8 bear microvilli diagonally: 45° for R6 and R8, 135° for R5 and R7. 4. We then recorded spectral and polarization sensitivities from single photoreceptors. The peak angle of the polarization sensitivity (θmax) of the UV, violet, and blue receptors were around 0°, whereas that of the green receptors was around 90°. In the double-peaked green receptors, the θmax at UV was also around 90°. The red receptors showed a θmax at around 35°. The polarization sensitivity ratio (PSmax/PSmin) of the double-peaked green receptors measured at UV was around 4, whereas the ratio of other receptors was around 2. 5. We conclude that R1 and R2 are either UV, violet, or blue receptors whereas R3 and R4 are green receptors. Some R6 and R8 are red receptors. We also conclude that the UV secondary peak in the double-peaked green receptor is not simply attributable to the coupling with UV receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00223959
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  • 13
    Electronic Resource
    Electronic Resource
    High resolution measurement of atmospheric carbon dioxide concentration changes by the labial palp organ of the moth Heliothis armigera (Lepidoptera: Noctuidae) (1992)
    Springer
    Journal of comparative physiology 171 (1992), S. 317-324 
    Details
    ISSN: 1432-1351
    Keywords: Carbon dioxide ; Chemoreception ; Lepidoptera ; Microclimate ; Sensory transduction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary In recordings of single unit action potentials, the responses of CO2-receptors in the labial palp organ of the moth Heliothis armigera to modulation of CO2-density around a background of 350 ppm were investigated. Modulation of CO2-density by square wave changes in concentration at constant barometric pressure evokes modulation of the spike rate. Modulation of CO2-density by square wave changes in barometric pressure at constant CO2-concentration evokes responses similar to those evoked by concentration modulation. For modulation depths of less than 1.5%, the output modulation depth is linearly related to the input; at higher modulation depths the gain decreases progressively. Using sinusoidal pressure modulation, the frequency dependence of both gain and output noise was determined over a range of 0.05 to 12.8 Hz. With increasing frequency the gain progressively increases at a rate of 2.4 dB/octave up to a maximum of 63 at 3 Hz; at higher frequencies, it decreases rapidly. The threshold sensitivity of the receptors, using input noise amplitude density as a criterion, is broadly tuned, with a minimum of 1 % contrast Hz-0.5 between 0.3 and 3 Hz. Using these figures, it is concluded that the sensory organ is capable of detecting fluctuations in CO2-density of 0.14% or 0.5 ppm. The results are related to the fluctuations in CO2-density which occur in a natural environment.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00223962
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  • 14
    Electronic Resource
    Electronic Resource
    The determination of phosphonate base scale inhibitors in brines by plasma spectrometry (1992)
    Springer
    Microchimica acta 109 (1992), S. 201-209 
    Details
    ISSN: 1436-5073
    Keywords: phosphonate base scale inhibitor ; brine ; direct current plasma ; inductively coupled plasma atomic emission spectrometry ; phosphorus
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The determination of phosphonate base scale inhibitors in brines by direct current plasma (DCP) and inductively coupled plasma atomic emission spectrometry (ICP-AES) is described. The first method is based on a direct nebulization of the brine samples and plasma using the phosphorus line at 213.618 nm. The second method involves extraction of phosphorus as phospho-antimonyl molybdate complex into methylisobutyl ketone (MIBK) phase and analysis of the extract for molybdenum using the Mo 313.260 nm line. Comparison between the proposed methods and an established recommended method [1] shows excellent agreement between the results in addition to the sensitivity and ease of automation provided by AES.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01242475
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  • 15
    Electronic Resource
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    The interpretation of Olsen extractable P values in relation to recommendations for the fertilizer requirements of crops (1992)
    Springer
    Nutrient cycling in agroecosystems 32 (1992), S. 223-227 
    Details
    ISSN: 1573-0867
    Keywords: Soil testing ; phosphorus ; relative yield
    Source: Springer Online Journal Archives 1860-2000
    Topics: Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition
    Notes: Abstract A greenhouse experiment, with Okra (Abelmoschus esculentus L.) as the test crop, was conducted on twenty-one soils ranging in Olsen's extractable phosphorus from 1.8 to 15.5µg Pg−1 soil. The experiment was conducted at Punjab Agricultural University, Ludhiana, India. The soils were nonsaline with pH ranging from 7.7 to 8.6. A critical level of 2.55µg Pg−1 soil was predicted by Cate and Nelson's (1971) statistical procedure. Because of a wide range in relative yields, this value did not accurately predict response to applied P. An approach to compute minimum response to applied fertilizer, which is likely to be obtained at a particular Olsen P level, has been presented. It involves calculation of lower 60 percent confidence limits for relative yield and fitting loge-linear regression to the transformed data. The regression was tested on a published data set and was found to hold well.
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    URL: http://dx.doi.org/10.1007/BF01048784
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  • 16
    Electronic Resource
    Electronic Resource
    Two post thinning fertilizer trials inPinus radiata in New South Wales, Australia (1992)
    Springer
    Nutrient cycling in agroecosystems 32 (1992), S. 259-267 
    Details
    ISSN: 1573-0867
    Keywords: Nitrogen ; phosphorus ; timber increment ; fertilization ; Pinus radiata
    Source: Springer Online Journal Archives 1860-2000
    Topics: Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition
    Notes: Abstract Two trials inPinus radiata growing on different sites in N.S.W. allowed consideration of fertilizer applications after 2nd or 3rd thinning. The trials included factorial applications of N and P at a single thinning intensity plus a further treatment which allowed assessment of different thinning intensities. The most significant growth responses were obtained by application of N and P in combination. The largest response (additional productivity compared with the unfertilized control) occurred 4 years after application and after 7 years there was no additional absolute response for either of the two sites. The largest fertilizer response was 70 m3 ha−1 over 7 years on one site and 36 m3 ha−1 on the other, indicating differences in absolute responses between sites. It was concluded that in planning treatments the most responsive sites near the end of the rotation should be selected to maximise economic returns. Foliage analyses indicated differences between sites at the commencement of the study. It was concluded that either a single year of foliage analyses at study commencement is of value, or sampling every year of the study should be used to analyse responses, but a single year of analysis during or at the end of the study would not be of value.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01050363
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  • 17
    Electronic Resource
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    Antioxidant alteration ofGlycine max (Fabaceae) defensive chemistry: Analogy to herbivory elicitation (1992)
    Springer
    Chemoecology 3 (1992), S. 25-32 
    Details
    ISSN: 1423-0445
    Keywords: defensive chemistry ; alterable ; elicitation ; herbivory ; antioxidant ; Fabaceae ; Glycine max ; Lepidoptera ; Noctuidae ; Trichoplusia ni
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary The water-soluble antioxidant, L-ascorbic acid (vitamin C), proved elicitory to alterable anti-herbivory inGlycine max againstTrichoplusia ni larvae. Elicitation by vitamin C was influenced especially by dose, time after elicitation and space in the plant. Results allow an analogy between antioxidant and herbivory elicitation. Elicitation apparently involves a sulfhydryl-protein-dependent redox mechanism which can be significantly affected by antioxidants. Findings would also support a proposed common redox-based mechanism, involving the plasma membrane, for communication between plant and animal cells and their environments.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01261453
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  • 18
    Electronic Resource
    Electronic Resource
    Cardenolide content, emetic potency, and thin-layer chromatography profiles of monarch butterflies,Danaus plexippus, and their larval host-plant milkweed,Asclepias humistrata, in Florida (1992)
    Springer
    Chemoecology 3 (1992), S. 1-13 
    Details
    ISSN: 1423-0445
    Keywords: aposematism ; cardenolide fingerprint ; chemical defense ; emesis ; plant-insect interaction ; migration ; Asclepiadaceae ; Apocynales ; Asclepias humistrata ; milkweed ; Lepidoptera ; Danainae ; Danaus plexippus ; monarch butterfly
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary This paper is the fourth in a series on cardenolide fingerprints of monarch butterflies (Danaus plexippus, Danainae) and their host-plant milkweeds (Asclepiadaceae) in the eastern United States. Cardenolide concentrations ofAsclepias humistrata plants from north central Florida ranged from 71 to 710 µg/0.1 g dry weight, with a mean of 417 µg/0.1 g. Monarchs reared individually on these plants contained cardenolide concentrations ranging from 243 to 575 µg/0.1 g dry weight, with a mean of 385 µg/0.1 g. Cardenolide uptake by butterflies was independent of plant concentration, suggesting that sequestration saturation occurs in monarchs fed cardenolide-rich host plants. Thinlayer chromatography resolved 19 cardenolides in the plants and 15 in the butterflies. In addition to humistratin,A. humistrata plants contained several relatively non-polar cardenolides of the calotropagenin series which are metabolized to more polar derivatives in the butterflies. These produced a butterfly cardenolide fingerprint clearly distinct from those previously established for monarchs reared on otherAsclepias species. In emetic assays with the blue jay,Cyanocitta cristata, the 50% emetic dose (ED50) per jay was 57.1 µg, and the average number of ED50 units per butterfly was 13.8, establishing that this important south eastern milkweed produces highly emetic, chemically defended monarchs. Our data provide further support for the use of cardenolide fingerprints of wild-caught monarchs to make ecological predictions concerning defence against natural enemies, seasonal movement and larval host-plant utilization by monarch butterflies during their annual cycle of migration, breeding and overwintering.
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    URL: http://dx.doi.org/10.1007/BF01261450
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    Leaf surface chemicals stimulating oviposition byPieris rapae (Lepidoptera: Pieridae) on cabbage (1992)
    Springer
    Chemoecology 3 (1992), S. 33-38 
    Details
    ISSN: 1423-0445
    Keywords: oviposition ; 3-indolylmethyl glucosinolate ; sinigrin ; glucoiberin ; cabbage ; Cruciferae ; Brassica oleracea ; Lepidoptera ; Pieridae ; Pieris rapae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary The chemical stimulation of oviposition byPieris rapae on cabbage was investigated by leaf washing and extraction. Isolation of the stimulant by various chromatographic techniques was monitored by a bioassay using Sieva bean as a surrogate host plant. Cold water, chloroform, or chloroform followed by cold water washes failed to release the stimulant from leaf surfaces. Boiling water or chloroform followed by methanol was required. The most active stimulatory compound was identified as 3-indolylmethyl glucosinolate (glucobrassicin). Other glucosinolates were identified as sinigrin, which was only slightly active, and glucoiberin, which was completely inactive as a stimulant. The significance of the selective response ofP. rapae andP. brassicae to different glucosinolates and the implications of the binding of polar allelochemicals to leaf surfaces is discussed with respect to host utilization and perception mechanisms of pierids.
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    URL: http://dx.doi.org/10.1007/BF01261454
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    Survival of first instar larvae ofDanaus plexippus (Lepidoptera: Danainae) in relation to cardiac glycoside and latex content ofAsclepias humistrata (Asclepiadaceae) (1992)
    Springer
    Chemoecology 3 (1992), S. 81-93 
    Details
    ISSN: 1423-0445
    Keywords: first instar survival ; latex ; cardiac glycosides ; cardenolides ; Lepidoptera ; Danainae ; Danaus plexippus ; Asclepiadaceae ; Asclepias humistrata ; milkweed
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary Our paper addresses field survivorship of first instar monarch butterfly larvae (Danaus plexippus L., Lep.: Danainae) in relation to the dual cardenolide and latex chemical defenses of the sand hill milkweed plant,Asclepias humistrata (Asclepiadaceae) growing naturally in north central Florida. Survival of first instar larvae in the field was 11.5% in the first experiment (15–20 April 1990), and dropped to 3.4% in the second experiment (20–30 April). About 30% of the larvae were found glued to the leaf surface by the milkweed latex. Predator exclusion of non-flying inverte-brates by applying “tanglefoot” to the plant stems suggested that the balance of the mortality was due to volant inverte-brates, or to falling and/or moving off the plants. Regression analyses to isolate some of the other variables affecting survivorship indicated that first instar mortality was correlated with (1) increasing cardiac glycoside concentration of the leaves, (2) increasing age of the plants, and (3) the temporal increase in concentration of cardiac glycosides in the leaves. The study also provided confirmatory data of previous studies that wild monarch females tend to oviposit onA. humistrata plants containing intermediate concentrations of cardiac glycosides. Cardiac glycoside concentration in the leaves was not correlated with that in the latex. The concentration of cardenolide in the latex is extremely high, constituting an average of 1.2 and 9.5% of the mass of the wet and dry latex, respectively. The data suggest that an increase in water content of the latex is compensated for by an influx of cardenolide with the result that the cardenolide concentration remains constant in the latex systems of plants that are growing naturally. We also observed first instar larvae taking their first bite of milkweed leaves in the field. In addition to confirming other workers findings that monarch larvae possess elaborate “sabotaging” behaviour of the milkweed's latex system, we discovered that several larvae on their first bite involuntarily imbided a small globule of latex and instantly became cataleptic. This catalepsis, lasting up to 10 min, may have been in response to the high concentration of cardenolide present in the latex ofA. humistrata, more than 10 times that in the leaves. The results of the present study suggest that more attention should be directed to plant chemical defenses upon initial attack by first instar insect larvae, rather than attempting correlations of plant chemistry with older larvae that have already passed the early instar gauntlet. The first bite of neonate insects may be the most critical moment for coping with the chemical defenses of many plants and may play a much more important role in the evolution of insect herbivory than has previously been recognized.
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    URL: http://dx.doi.org/10.1007/BF01245886
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    Identification of an oviposition-regulating pheromone in the European grapevine moth,Lobesia botrana (Lepidoptera: Tortricidae) (1992)
    Springer
    Cellular and molecular life sciences 48 (1992), S. 697-699 
    Details
    ISSN: 1420-9071
    Keywords: Oviposition-deterring pheromone ; Lepidoptera ; Tortricidae ; Lobesia botrana ; eggs ; fatty acids ; esters of fatty acids
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract The oviposition of the European grapevine moth (EGVM)Lobesia botrana can be deterred by an extract of conspecific eggs corresponding to 20 egg equivalents. The reduction of the oviposition behavior is dose-dependent. Nine chemicals have been extracted from the eggs and identified as straight chain fatty acids and esters of fatty acids. A mixture of these rather simple molecules induces the same levels of deterrence as the total extract. It might be possible to use oviposition regulating pheromone in the future for the control of EGVM populations.
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    URL: http://dx.doi.org/10.1007/BF02118323
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    Nutrient-chlorophyll trajectories across trophic gradients (1992)
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    Aquatic sciences 54 (1992), S. 58-76 
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    ISSN: 1420-9055
    Keywords: Eutrophication ; lake management ; phosphorus ; nitrogen ; chlorophyll-a ; slope estimator
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract We estimate the response of chl-a (mg · m−3) to changes in concentrations of total phosphorus (TP) by calculating the slopeS = Δchl-a/ΔTP in chl-a =f(TP) graphs. Results show that in years where algae are P-limited oligotrophic lakes respond less (median slope 0.21) to changes in nutrient concentrations than eutrophic lakes, (median slope 0.31) and these again less than hypereutrophic lakes, (median slope 1.02). We find no saturation value for the slope within the TP range considered (6–480 mg · m−3). Chl-a in eutrophic lakes responds more frequently to non-nutrient factors than oligotrophic and hypereutrophic lakes. Results obtained by replacing TP with a new nutrient parameter, TP′ = 0.056 · TP · IN0.226, in which inorganic nitrogen, IN, is factored in, suggest that nitrogen has an influence on chl-a in oligotrophic lakes. Blue-green algae respond less to changes in TP than other algal species, e.g., diatoms.
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    URL: http://dx.doi.org/10.1007/BF00877264
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    Possibilities and limitations of lake restoration: Conclusions for Lake Lugano (1992)
    Springer
    Aquatic sciences 54 (1992), S. 381-390 
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    ISSN: 1420-9055
    Keywords: Eutrophication ; phosphorus ; lake restoration ; internal restoration measures for lakes ; Swiss lakes ; Lake Lugano (Lago di Lugano)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract In most lakes eutrophication is linked to an excessive input of phosphorus. Lake restoration by reduction of P-input (external measure) has led to a considerable drop of the P-concentration in all major Swiss lakes as well as in many other lakes. Internal restoration measures such as artificial mixing, drainage of hypolimnetic water, flushing, aeration, biomanipulation and others serve to improve and accelerate the response of a lake to external measures. For the case of Lago di Lugano, a simple two-box model is employed to demonstrate that a reduction of the P-input to about 25% of the present values is necessary to reach the “P-criterion” (P-concentration below 30 µg/l). Internal measures could possibly accelerate the extremely slow response of the northern basin.
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    Leaf surface compound fromBrassica oleracea (Cruciferae) induces oviposition byPieris brassicae (Lepidoptera: Pieridae) (1992)
    Springer
    Chemoecology 3 (1992), S. 39-44 
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    ISSN: 1423-0445
    Keywords: oviposition ; kairomone ; host plant selection ; indole glucosinolates ; Cruciferae ; Brassica oleracea ; cabbage ; Lepidoptera ; Pieridae ; Pieris brassicae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary Chemicals present on the surface of cabbage (Brassica oleracea L.) leaves were extracted by dipping these leaves for 3 s in dichloromethane followed by a 3 s dip in methanol. When offered in dual choice bioassays using green paper cards as a substrate, the methanol extract stimulated oviposition activity byPieris brassicae L. (Lepidoptera: Pieridae) females. The oviposition stimulant was isolated using medium pressure liquid chromatography, reversed-phase HPLC, ion-pair HPLC and ion exchange chromatography. Using1H-NMR spectroscopy, the stimulant could be identified as glucobrassicin (3-indolyl-methyl-glucosinolate). When pure glucobrassicin was offered at a dose identical to that in the crude methanol extract, butterflies did not discriminate between these two substrates in a dual choice test. It is argued that a high sensitivity for indole glucosinolates as host recognition factors may confer an adaptive value for these specialist crucifer feeders. The nutritional significance of their precursor tryptophan and the non-volatile nature of the aglycones formed upon enzymic hydrolysis in damaged tissues are proposed as properties of indole glucosinolates that contribute to this possible adaptive advantage.
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    Chemical basis of pupal cannibalism in a caterpillar (Utetheisa ornatrix) (1992)
    Springer
    Cellular and molecular life sciences 48 (1992), S. 97-102 
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    ISSN: 1420-9071
    Keywords: Lepidoptera ; Arctiidae ; pyrrolizidine alkaloids ; cannibalism ; acquired defense ; phagostimulation ; specific hunger
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract The mothUtetheisa ornatrix derives protection against predation from systemic pyrrolizidine alkaloids (PAs) that it sequesters as a larva from its foodplants (Leguminosae,Crotalaria spp.). We here show, in laboratory tests, thatUtetheisa deficient in body PA can make up for the chemical shortfall by cannibalizing pupae. We present evidence indicating that cannibalism in larvae is elicited not by hunger, but possibly by PA deficiency itself, and that in making cannibalistic choices larvae prefer PA-containing over PA-free pupae. PAs themselves, either in crystalline form or as additives to food items, proved phagostimulatory to larvae. In natureUtetheisa tend to pupate away from their foodplant, essentially out of reach of larval attack. The threat of cannibalism may have contributed to the evolution of this pupation behavior.
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    Relative nutritional quality of C3 and C4 grasses for a graminivorous lepidopteran, Paratrytone melane (Hesperiidae) (1992)
    Springer
    Oecologia 92 (1992), S. 97-103 
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    ISSN: 1432-1939
    Keywords: C3 and C4 grasses ; Lepidoptera ; Hesperiidae ; Paratrytone melane ; Nutrients
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary We tested the hypothesis that C4 grasses are inferior to C3 grasses as host plants for herbivorous insects by measuring the relative performance of larvae of a graminivorous lepidopteran, Paratrytone melane (Hesperiidae), fed C3 and C4 grasses. Relative growth rates and final weights were higher in larvae fed a C3 grass in Experiment I. However, in two additional experiments, relative growth rates and final weights were not significantly different in larvae fed C3 and C4 grasses. We examined two factors which are believed to cause C4 grasses to be of lower nutritional value than C3 grasses: foliar nutrient levels and nutrient digestibility. In general, foliar nutrient levels were higher in C3 grasses. In Experiment I, protein and soluble carbohydrates were digested from a C3 and a C4 grass with equivalent efficiencies. Therefore, differences in larval performance are best explained by higher nutrient levels in the C3 grass in this experiment. In Experiment II, soluble carbohydrates were digested with similar efficiencies from C3 and C4 grasses but protein was digested with greater efficiency from the C3 grasses. We conclude (1) that the bundle sheath anatomy of C4 grasses is not a barrier to soluble carbohydrate digestion and does not have a nutritionally significant effect on protein digestion and (2) that P. melane may consume C4 grasses at compensatory rates.
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    Digestion of uncrushed leaf tissues by leaf-snipping larval Lepidoptera (1992)
    Springer
    Oecologia 89 (1992), S. 229-235 
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    ISSN: 1432-1939
    Keywords: Lepidoptera ; Digestion ; Larvae ; Mandible ; C4 grasses
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary Cynodon dactylon (Poaceae) leaf pieces recovered from the frass of final-instar Paratrytone melane larvae (Lepidoptera: Hesperiidae) were composed of 14–22 percent crushed cells and 78–86 percent uncrushed cells, yet approximate digestibilities of soluble carbohydrates and protein averaged 78 and 88 percent, respectively. Therefore, nutrients from uncrushed cells were extracted by P. melane. The ability of P. melane and another leaf-snipping lepidopteran, Pseudaletia unipuncta (Noctuidae), to digest the contents of uncrushed bundle sheath and mesophyll cells in C. dactylon was examined with transmission electron microscopy. Organelles and plasma membranes were digested in the foreguts and midguts of both species. These findings suggest that nutrients in uncrushed leaf cells may be extracted through plasmodesmata and cell wall pores after membranes are digested. The generality of leaf-snipping, vis-a-vis leaf crushing, among larval Lepidoptera was assessed by surveying the mandible morphologies of 202 species. In 82 percent of the species surveyed only incisor regions were present. I conclude that leaf-snipping is a common mode of feeding among phytophagous Lepidoptera and that the digestion of cell contents is efficient despite the fact that few of the cells of ingested plant tissues are crushed.
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    Pharmacokinetics of rufloxacin in healthy volunteers (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 101-105 
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    ISSN: 1432-1041
    Keywords: Rufloxacin ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma and urine kinetics of rufloxacin were assessed in healthy volunteers after single (100, 200, 400 and 800 mg) and multiple (300 mg followed by 150 mg daily, Group 1, and 400 mg followed by 200 mg daily, Group 2) oral doses. The kinetics of a single oral dose of 800 mg was assessed in fasting and non-fasting subjects to assess the influence of food intake on drug absorption. The AUCs were 134, 266 and 375 μg · h · ml−1 after 100, 200 and 400 mg, respectively. The AUC after 800 mg p. o. was 715 μg · h · ml −1 in fasting subjects and 614 μg · h · ml−1 in non-fasting subjects. The parameters of the model and the mean renal clearance values indicated some departure from linearity in rufloxacin kinetics. After multiple doses the plasma drug levels during the 6th treatment day were similar to those after the first dose in Group 1 and were about 30–40% higher after the first dose in Group 2. The half-lives after the last dose were much shorter than those estimated in the single dose studies (33–36 h and 50–80 h, respectively).
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    Pharmacokinetics of meropenem in subjects with renal insufficiency (1992)
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    European journal of clinical pharmacology 42 (1992), S. 535-538 
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    ISSN: 1432-1041
    Keywords: Meropenem ; Carbapenem ; pharmacokinetics ; uraemia ; haemodialysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of IV meropenem (500 mg over 30 min) has been studied in 6 healthy volunteers and 26 patients with various degrees of renal impairment. Blood samples were taken at different times over 24 h in healthy subjects and 36 to 48 h in uraemic patients, and four or five urine samples were collected over 24 or 48 h. Meropenem concentrations in plasma and urine were measured by a microbiological assay. The mean peak plasma concentration of meropenem ranged from 28 to 40 μg·ml−1 and was not affected by the degree of renal impairment. The terminal half-life of meropenem was approximately 1 h in subjects with normal kidney function and it was proportionately increased as renal function decreased. A significant linear relationship between total body clearance and creatinine clearance as well as between renal clearance and creatinine clearance was observed. The mean apparent volume of distribution at steady state was not significantly altered in uraemic patients. The mean cumulative urinary recovery of meropenem in healthy volunteers was 77% of the administered dose and it was significantly decreased in patients with renal impairment. Haemodialysis shortened the elimination half-life, from 9.7 h during the predialysis period to 1.4 h during the dialysis period. The dose of meropenem should be reduced in relation to the decrease in creatinine clearance.
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    Pharmacokinetics of mefloquine in the presence of primaquine (1992)
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    European journal of clinical pharmacology 42 (1992), S. 559-560 
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    ISSN: 1432-1041
    Keywords: Mefloquine ; Thai subjects ; pharmacokinetics ; Primaquine ; drug interaction ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
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    URL: http://dx.doi.org/10.1007/BF00314870
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    Pharmacokinetics of diphemanil methylsulphate in healthy subjects (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 689-691 
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    ISSN: 1432-1041
    Keywords: Diphemanil methylsulphate ; pharmacokinetics ; healthy subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic parameters of oral diphemanil methylsulphate have been evaluated in six healthy male volunteers. Absorption of the drug was slow (tmax=2 to 4 h), the mean half-life was 8.35 h, and the amount of the drug recovered in urine within 48 h ranged from 0.6 to 7.4% of the administered dose. The results suggest low bioavailability, assuming that the drug is poorly metabolized.
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    Dose proportionality study of loperamide following oral administration of loperamide oxide (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 693-694 
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    ISSN: 1432-1041
    Keywords: Loperamide ; loperamide oxide ; diarrhoea ; pharmacokinetics ; dose-proportionality
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of loperamide, after oral administration of increasing doses (1 to 16 mg) of loperamide oxide, has been investigated in 10 healthy male volunteers, using a randomised cross-over design. Comparison of the maximum plasma loperamide concentration and AUC demonstrated that the bioavailability of loperamide was proportional to the dose of loperamide oxide administered.
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    Evaluation of the accuracy of a pharmacokinetically-based patient-controlled analgesia system (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 67-75 
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    ISSN: 1432-1041
    Keywords: Morphine ; Patient-controlled analgesia ; opioids ; pharmacokinetics ; bolus-elimination-transfer ; computer-assisted continuous infusion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Bone marrow transplant patients having severe, prolonged oral mucositis pain (expected to last for one to three weeks) used a computer-controlled infusion system to self-administer morphine for pain control. Individual patient pharmacokinetic information, derived from a pretreatment bolus morphine dose, was used in a new bolus-elimination transfer algorithm to produce rapid adjustments of steady plasma morphine concentrations when the patient requested more or less drug. We evaluated the performance characteristics (bias and precision) of this pharmacokinetically based patient-controlled analgesic infusion system (PKPCA) in a group of 15 cancer patients over six to 14 days. Although we found a three- to fivefold pharmaco-kinetic variability in the tailoring morphine dose data, the PKPCA system was free of systematic bias (insignificant overall prediction error) during the patient-controlled infusions in this study population. The absolute prediction error was 19.9% for the group on the first study day and 25.6% over the entire study period (aggregate results; 6–14 days of continuous use). Two-thirds of the patients exhibited no bias throughout the study period, and individual bias in the others was symmetrically distributed (three patients with underpredictions and two overpredicted). Magnitude of prediction error during the patient-controlled morphine infusions was not related to the magnitude of pharmacokinetic deviation of individual subjects from group parameters. Our results indicate that this PKPCA system provides accurate control of plasma morphine concentration when used by patients to self-administer opioid for prolonged pain relief continuously over 1 to 2 weeks. Use of individual pharmacokinetic information, instead of population parameters, may account for superior performance characteristic of this computer-assisted continuous drug infusion system.
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    Steady state pharmacokinetic profile of indomethacin in elderly patients and young volunteers (1992)
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    European journal of clinical pharmacology 43 (1992), S. 77-80 
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    ISSN: 1432-1041
    Keywords: Indomethacin ; steady-state ; pharmacokinetics ; elderly
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The steady-state pharmacokinetic profile of indomethacin was examined in twelve healthy volunteers (4 m, 8 f; 20–34 y) and in 12 elderly subjects (7 m, 5 f; 70–88 y). Two formulations of indomethacin were examined, providing duplicate data for each subject group. The subjects received each formulation of indomethacin (25 mg tid) for 6 days in a single blind crossover fashion. On day 7, after an overnight fast, a final 25 mg dose of indomethacin was given and plasma concentrations measured over the following 12 h. Kinetic parameters Cpmin, tmx and AUC (0–12 h) were determined. There were no differences in the pharmacokinetic parameters between young and elderly subjects or between data for the two formulations of indomethacin. AUC values (μg · ml−1 · h), for example, for the two formulations in the young subjects were 5.85 and 6.85 while the values for the elderly subjects were 6.55 and 6.50 respectively. When each treatment period was considered independently there was a significant difference between young and elderly subjects with regard to compliance. The rates of non compliance (over and under compliance) using a capsule count technique were, however, low with a mean maximum value of 5.8% being recorded for the elderly subjects.
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    Pharmacokinetics and dialysability of isradipine in chronic haemodialysis patients (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 231-233 
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    ISSN: 1432-1041
    Keywords: Isradipine ; Haemodialysis ; pharmacokinetics ; dialysability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of isradipine, a calcium-channel blocker, have been studied in eight patients on chronic haemodialysis. A single oral dose of 5 mg was administered on both a non-haemodialysis and a haemodialysis day and the plasma concentrations of isradipine were analyzed. The mean cmax, tmax, AUC, and t1/2 in plasma on the non-haemodialysis day were 5.2 ng·ml−1, 1.4 h, 23.8 ng·h·ml−1, and 3.1 h, respectively. The dialysis clearance of isradipine was negligible (5.0 ml·min−1). The t1/2 values during haemodialysis were not significantly different from those observed during the same period post dose on the non-haemodialysis day. The study demonstrates that supplemental doses of isradipine are not necessary in these patients since isradipine is not significantly removed by haemodialysis.
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    Disposition of quinine in plasma, red blood cells and saliva after oral and intravenous administration to healthy adult Africans (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 171-174 
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    ISSN: 1432-1041
    Keywords: Quinine ; Malaria ; pharmacokinetics ; red blood cells ; plasma ; saliva ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of quinine has been studied in ten healthy adult Africans after intravenous infusion and oral ingestion of a 500 mg dose. Blood and saliva samples were collected over 48 h and quinine in plasma, red cells and saliva was determined by HPLC. Quinine was rapidly and almost completely absorbed after an oral dose, with absorption half-life of 0.53 h, a tmax of 1–3 h and a bioavailability of 88%. Analysis of the i. v. data gave an apparent volume of distribution of 3.6 1·kg−1 and a plasma clearance of 0.19 l·kg−1·h−1. The concentration-time curves for plasma, red cells and saliva had declining phases were approximately parallel, giving a similar half-life that in all three media. The half-lives after the i. v. infusion also did not different from those after oral administration. The dose was well tolerated by both methods of administration.
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    Binding of a metabolite of triflusal (2-hydroxy-4-trifluoromethylbenzoic acid) to serum proteins in rat and man (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 175-179 
    Details
    ISSN: 1432-1041
    Keywords: 2-hydroxy-4-trifluoromethylbenzoic acid (HTB) ; Triflusal ; triflusal metabolite (HTB) ; pharmacokinetics ; protein binding ; ultrafiltration ; binding constant
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 2-hydroxy-4-trifluoromethylbenzoic acid (HTB) is the main active metabolite of the platelet anti-aggregant drug triflusal. Its binding to plasma proteins of rats and healthy volunteers in vitro and in vivo has been studied. Rats were given a single oral dose of 50 mg·kg−1 triflusal and the healthy volunteers received 300 mg as a single oral dose or a multiple dose regimen of 600 mg every 24 h and 300 mg every 8 h, both for 13 days. Protein-free HTB was obtained by ultrafiltration. Unbound and total HTB concentrations were determined by HPLC. HTB was primarily bound to albumin in plasma. The Scatchard plots suggested two types of binding sites for HTB on the albumin molecule. In rats, the binding constants (K=intrinsic affinity constant, n=number of binding sites) were K1=1.4×105 l·mol−1, n1=1.23, and K2=4.1×103 l·mol−1 and n2=3.77. The mean plasma concentration in rats after oral administration was 185 (37) μg·ml−1 (protein-free HTB: 2.44 (0.77)%). The binding constants in human plasma were K1=4.7×105 l·mol−1, n1=1.93, K2=4.3 l·mol−1 and n2=4.28. The plasma HTB concentration in man (n=8) was 35 μg·ml−1 (Cmax) after a single oral dose of triflusal 300 mg, 172.96 μg·ml−1 (Cmax·ss) during the multiple dosage regimen of 300 mg every 8 h, and 131 μg·ml−1 (Cmax·ss) during the multiple oral dose regimen of 600 mg every 24 h. Unbound HTB ranged from 0.27 to 0.43%, depending on dose. HTB had high affinity for plasma albumin, which was not saturable after therapeutic doses. It showed linear elimination.
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    Temporary reversal of serum to cerebrospinal fluid glycerol concentration gradient after intravenous infusion of glycerol (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 181-185 
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    ISSN: 1432-1041
    Keywords: Glycerol ; brain oedema ; serum ; cerebrospinal fluid ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Glycerol 50 g infused i. v. over 2 to 6 h is widely used to treat cerebral oedema in patients with acute stroke. Its transit through the blood-cerebrospinal fluid barrier in subjects with uninflamed meninges has now been examined. In 7 patients with an external ventriculostomy for occlusive hydrocephalus, each of whom was given 500 ml of a 10% solution IV over 4 h, serum and CSF were repeatedly sampled during and after the infusion and glycerol was measured enzymatically. The highest serum glycerol level of 191–923 mg/l was observed at the end of the infusion. The maximum CSF glycerol of 18.7–110.8 mg/l was attained 0–1 h after the end of the infusion. Elimination both from serum and CSF approximated a single-exponential decay; the elimination half-life from serum was 0.29–0.56 h compared to 1.03–3.68 h from CSF. In six of the seven cases there was a temporary reversal of the serum/CSF concentration gradient during glycerol elimination. The ratios of the AUCs of CSF and serum, which describe the overall penetration of glycerol into CSF, ranged from 0.09–0.31. In conclusion, the serum level of glycerol produced by giving 50 g IV glycerol over 4 h may not be sufficiently high reliably dehydrate to brain tissue in many patients, and the slow elimination of glycerol from the CSF may be related to the so-called rebound phenomenon.
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    Formation and excretion of dipyrone metabolites in man (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 187-191 
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    ISSN: 1432-1041
    Keywords: Dipyrone ; Acetylation phenotype ; metabolism ; pharmacokinetics ; urinary excretion ; metabolite clearance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The formation and urinary excretion of the dipyrone metabolites, methylaminoantipyrine (MAA), aminoantipyrine (AA), formylaminoantipyrine (FAA) and acetylaminoantipyrine (AAA) were determined following administration of a single oral 1.0 g dose of dipyrone to 12 healthy volunteers. The AAA/AA plasma ratio showed that 3 subjects were slow and 9 were rapid acetylators. Pharmacokinetic parameters were determined separately for each group. A good correlation was found between the plasma and urine AAA/AA ratios. The renal clearance of the four metabolites was similar for both phenotypes. A significant difference in the rate of formation of dipyrone metabolites was found for AA, 0.25 (slow) vs 0.1 ml·min−1·kg−1 (rapid), and for AAA 0.75 (slow) vs 7.53 ml·min−1·kg−1 (rapid). There were comparable differences between slow and rapid acetylators in the AUC and the urinary excretion extrapolated to infinity for AA and AAA. The present results show that the kinetics of dipyrone metabolites in plasma and urine can provide a useful measure of the activity of the enzymes involved in their production.
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    Effect of salbutamol on digoxin pharmacokinetics (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 197-201 
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    ISSN: 1432-1041
    Keywords: Digoxin ; Salbutamol ; serum ; skeletal muscle digoxin ; pharmacokinetics ; drug interaction ; serum potassium
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A single dose of the β2-adrenoceptor agonist salbutamol has previously been shown to decrease serum digoxin concentration in healthy volunteers. A possible explanation of the phenomenon is a β2-adrenoceptor-mediated increase in the specific binding of digoxin to skeletal muscle. The present study was undertaken to further elucidate the effect of salbutamol on the pharmacokinetics of digoxin in man. Nine volunteers were studied on two occasions during salbutamol or placebo treatment. On test days salbutamol, 4 μg·kg−1·h−1 or saline was infused for 10 h, preceded and followed by four and three days, respectively, of oral administration. A single i. v. injection of digoxin 15 μg·kg−1, was given 20 min after starting the infusion. At the end of the infusion a muscle biopsy was taken from the vastus lateralis. Blood samples for the analysis of serum digoxin and potassium were repeatedly taken over 72 h. Urine was collected over a period of 24 h for determination of the renal excretion of digoxin and potassium. The serum digoxin concentration, expressed as the AUC 0–6 h was 15% lower during salbutamol infusion than during saline infusion. Salbutamol caused significantly faster elimination of digoxin from the central volume of distribution to deeper compartments. Salbutamol had no effect on the renal clearance of digoxin. The skeletal muscle digoxin concentration tended to be higher (48%) during salbutamol compared to placebo treatment. The serum potassium concentration was significantly lower after salbutamol compared to placebo, as was the rate of renal excretion of potassium. The results support the hypothesis that the salbutamol-induced decrease in serum digoxin is caused by increased distribution of digoxin to skeletal muscle (and possibly other tissues), and that this may be secondary to a β2-adrenoceptor-mediated increase in Na-K-ATPase activity.
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    URL: http://dx.doi.org/10.1007/BF00278484
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    Pharmacokinetics of nicorandil in patients with normal and impaired renal function (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 203-207 
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    ISSN: 1432-1041
    Keywords: Nicorandil ; pharmacokinetics ; angina pectoris ; uraemia ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of oral nicorandil 20 mg 12 hourly for 9 doses was evaluated in 21 hospitalized patients with angina pectoris due to coronary heart disease and with normal and impaired renal function. Patients were divided into 3 groups based on creatinine clearance (CLCr): GROUP I (n=6) 〉 80 ml/min, GROUP II (n=8) 20–80 ml/min, and GROUP III (n=7) 〈 20 ml/min. After the first dose, the total clearance of nicorandil (CL) value did not change with increasing renal failure and so was not dependent on creatinine clearance. After the last dose CL was 51 l·h−1 in Group I, 44 l·h−1 in Group II and 56 l·h−1 in Group III, and it was not related to creatinine clearance. The percentage of the dose excreted in the urine was 0.4%. No significant difference was noted in any of the other pharmacokinetic parameters examined in the three groups, not even on comparing values obtained on the first and last days of treatment. The findings suggest that there is no need to change the dose of nicorandil in subjects with different degrees of renal failure.
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    The pharmacokinetics and pharmacodynamics of sublingual and oral alprazolam in the post-prandial state (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 439-443 
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    ISSN: 1432-1041
    Keywords: Alprazolam ; benzodiazepines ; pharmacokinetics ; pharmacodynamics ; sublingual dosage
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We gave 12 healthy male volunteers 1 mg of alprazolam or placebo on three occasions after a standard breakfast in a double-blind, randomized, single-dose, three-way crossover study. The three trials were: (a) oral alprazolam and sublingual placebo; (b) oral placebo and sublingual alprazolam; (c) placebo by both routes. Plasma alprazolam concentrations during 24 h after each dose were measured by electron-capture gas-liquid chromatography. Peak plasma concentrations were reached later after sublingual than oral dosage (2.8 vs 1.8 h, P〈0.01). Other kinetic variables were not significantly different: peak plasma concentration, 11.3 vs 12.0 ng·ml−1; elimination half-life, 12.5 vs 11.7 h; and total area under the plasma concentration versus time curve, 197 vs 186 h·ng·ml−1. Pharmacodynamic measures showed that sublingual and oral alprazolam both produced sedation, fatigue, impaired digit symbol substitution, slowing of reaction time, and impairment of the acquisition and recall of information. These changes were initially observed at 0.5 h after dosage and lasted up to 8 h. In general the two routes were significantly different from placebo but not from each other.
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    Pharmacokinetics of ethanol in plasma and whole blood: estimation of total body water by the dilution principle (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 445-448 
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    ISSN: 1432-1041
    Keywords: Ethanol ; whole blood ; plasma ; total body water ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of ethanol in plasma and whole blood have been investigated and the results used to estimate the volume of total body water (TBW) by means of the dilution principle. Fifteen men (mean age 62 y) were given 0.6 g ethanol/kg body weight as an intravenous infusion over 1 h. The peak concentration of ethanol in plasma was 120 mg·dl−1 compared to 108 mg·dl−1 for whole blood. The disappearance rate of ethanol from plasma was 18.6 mg·dl−1·h−1 compared to 17.0 mg·dl−1·h−1 for the whole blood concentration-time data. The apparent volume of distribution of ethanol (Vz) was 0.54 l·kg−1 according to plasma kinetics compared to 0.59 l·kg−1 for the kinetics derived from whole blood. The mean area under the curve (AUC) was 294 mg·dl−1×h for plasma kinetics compared to 266 mg·dl−1×h for whole blood. The TBW was 40.9 l or 50.9% of body weight for the plasma concentration-time data. This agreed well with the 40.3 l or 50.1% of body weight obtained using whole blood.
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    High dose oral methylprednisolone in patients with rheumatoid arthritis: pharmacokinetics and clinical response (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 85-88 
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    ISSN: 1432-1041
    Keywords: Methylprednisolone ; Rheumatoid arthritis ; bioavailability ; pharmacokinetics ; clinical response ; pulse steroid therapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A commercially available 1.0 g intravenous (i.v.) dosage formulation of methylprednisolone, as the sodium hemisuccinate salt (Solu MedrolR, Upjohn) was administered both parenterally and orally (pulse steroid therapy) on separate occasions, to eight elderly (mean 65 y) patients with active rheumatoid arthritis. The relative oral bioavailability of the sterol was 69.2%. Elimination of methylprednisolone was prolonged when given orally; the mean residence times were 7.23 h and 3.94 h for oral and i.v. administrations, respectively. Clinical response to pulse steroid therapy was no different with respect to route of administration. There were no significant differences in standard clinical and laboratory assessments of disease activity when the two therapies were compared. Oral administration of methylprednisolone in patients requiring high-dose pulse steroid therapy is convenient and avoids the discomfort and inconvenience associated with i.v. administration.
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    Pharmacokinetics of IV and oral acetyl-L-carnitine in a multiple dose regimen in patients with senile dementia of Alzheimer type (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 89-93 
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    ISSN: 1432-1041
    Keywords: Acetyl-L-carnitine ; Senile Dementia of Alzheimer Type ; pharmacokinetics ; plasma concentration ; cerebrospinal fluid concentration ; carnitine metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Acetyl-L-carnitine (ALC), a physiological component of the L-carnitine family, has been proposed for treating Alzheimer's disease in pharmacological doses. As this condition requires prolonged therapy, its kinetics has been examined after a multiple dose regimen, involving different routes of administration, in 11 patients suffering from Senile Dementia of Alzheimer Type. The study design comprised a 3-day basal observation period, sham treatment with repeated blood sampling; treatment with 30 mg·kg−1 i.v. given twice for 10 days (plasma kinetics was studied on the 7th day), and 50 days of 2.0 g/day p.o. given in three daily doses. Total acid soluble L-carnitine, L-carnitine and acetyl-L-carnitine in plasma and CSF were evaluated using an enantioselective radioenzyme assay. Short chain L-carnitine esters were calculated as the difference between total and free-L-carnitine. The plasma concentrations of individual components of the L-carnitine family did not change during the three days of the basal period, nor were they affected during the sham therapy period. Following the i.v. bolus injections, the plasma concentrations showed a biphasic curve, with average t1/2 of 0.073 h and 1.73 h, respectively. At the end of oral treatment, plasma acetyl-L-carnitine and L-carnitine short chain esters were significantly higher than during the run-in phase. The CSF concentrations paralleled those in plasma, suggesting that ALC easily crosses the blood-brain barrier. It is concluded that i.v. and oral administration of multiple doses of ALC can increase its plasma and CSF concentration in patients suffering from Alzheimer's disease.
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    Multiple dose kinetics of ofloxacin and ofloxacin metabolites in haemodialysis patients (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 95-99 
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    ISSN: 1432-1041
    Keywords: Ofloxacin ; Haemodialysis ; ofloxacin metabolites ; pharmacokinetics ; multiple doses ; dosage selection ; renal failure ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 7 patients with end-stage renal disease on regular haemodialysis were treated orally with a loading dose of 200 mg ofloxacin and multiple maintenance doses of 100 mg per 24 h for 10 days. The pharmacokinetics of ofloxacin and its metabolites were studied at the end of the treatment period. Plasma and dialysate concentrations of ofloxacin and ofloxacin metabolites were measured by HPLC. Peak (3.1 mg·1−1) and trough levels (1.6 mg·1−1) and the AUC of ofloxacin were comparable to the values in healthy volunteers given 300 to 400 mg ofloxacin p.o. The mean half-life, determined in the dialysis-free interval (t1/2β) and during the haemodialysis session (t1/2HD), was 38.5 h and 9.9 h, respectively. Extrarenal clearance (32.7 ml·min−1) was unchanged as compared to that reported in healthy volunteers after a single dose of ofloxacin. The fractional removal by haemodialysis amounted to 21.5%. Two metabolites, ofloxacin-N-oxide and demethyl-ofloxacin, were detected in plasma. Despite prolonged t1/2β of both metabolites (66.1 and 50.9 h) and multiple doses of ofloxacin the peak concentrations of the metabolites reached only 14% and 5% of that of the parent drug, respectively. It is concluded that in patients on regular haemodialysis treatment the dosage adjustment employed resulted in safe and therapeutically favourable plasma concentrations. The observed accumulation of ofloxacin metabolites does not appear to have any toxic or therapeutic significance.
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    The effects of a salicylate, ibuprofen, and naproxen on the disposition of methotrexate in patients with rheumatoid arthritis (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 121-125 
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    ISSN: 1432-1041
    Keywords: Methotrexate ; non-steroidal anti-inflammatory drugs (NSAIDs) ; interaction ; disposition ; adverse effects ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have studied the pharmacokinetics of methotrexate in patients with rheumatoid arthritis concurrently treated with choline magnesium trisalicylate, ibuprofen, naproxen, or a non-NSAID analgesic (control treatment). The apparent systemic clearance of methotrexate was significantly reduced by all three treatments. Trisalicylate and ibuprofen both significantly reduced methotrexate renal clearance, but only the trisalicylate significantly displaced methotrexate from protein, increasing the fraction unbound by 28%. These data show that NSAIDs can affect the disposition of methotrexate, possibly increasing the potential for toxicity and necessitating dosage adjustments. However, large inter-subject variability precludes specific dosage recommendations.
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    Effect of tetracycline on mefloquine pharmacokinetics in Thai males (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 567-569 
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    ISSN: 1432-1041
    Keywords: Mefloquine ; Tetracycline ; Thai subjects ; Thai subjects ; drug interaction ; pharmacokinetics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of a single oral dose of mefloquine given either alone or with tetracycline has been studied in 20 healthy Thai male volunteers. There was a significantly higher maximum whole blood mefloquine concentration after coadministration with tetracycline (1600 vs 1160 ng · ml−1), as well as a significantly reduced terminal half-life (14.4 vs 19.3 days), mean residence time (11.9 vs 16.0 days) and volume of distribution at steady state (13.3 vs 19.91 · kg−1). Although there was no significant change in the AUC from zero time to infinity, the AUC from zero time to 7 days was significantly increased by tetracycline (6.18 vs 4.76 μg · ml−1 · day). The changes in mefloquine disposition after tetracycline treatment are probably due to a reduction in enterohepatic recycling. The initial increase in mefloquine AUC without an apparent increase in side-effects suggests that this combination may have a place in the treatment of multi-drug resistant falciparum malaria.
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    Pharmacokinetics of cyclosporine in hyperlipidaemic long-term survivors of heart transplantation (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 161-165 
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    ISSN: 1432-1041
    Keywords: Cyclosporine ; Hyperlipidaemia ; heart transplantation ; fenofibrate ; fenofibric acid ; pharmacokinetics ; drug interaction ; nephrotoxicity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Cyclosporine (Cy) binds to lipoproteins in plasma. In order to test if its pharmacokinetics would be modified when efficient lipid-lowering treatment is introduced, a study has been done of Cy pharmacokinetics and any interaction with the lipid-lowering agent fenofibrate in hyperlipidaemic long-term, survivors of heart transplantation. Fenofibrate 200 mg once daily significantly reduced blood lipids (cholesterol 6.5 vs 7.7 mmol/l; apoprotein B 1.2 vs 1.6 g/l) but did not modify mean whole blood Cy trough levels (113 before fenofibrate vs 103 ng·ml−1), Cmax (812 ng·ml−1 by RIA and 757 ng·ml−1 by HPLC before fenofibrate versus 865 and 741 respectively, during fenofibrate); tmax (1.6 and 1.7 h before fenofibrate versus 1.4 and 1.4 h respectively), and t1/2 (13.9 and 11.1 h versus 9.5 and 10.7 h). The only adverse effect was an increase in creatinine (157 vs 145 mmol/l). Further studies are needed to investigate the mechanism of Cy-fenofibrate nephrotoxicity and to evaluate the long-term efficiency and safety of fenofibrate after heart transplantation.
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    Plasma thiamine concentrations after intramuscular and oral multiple dosage regimens in healthy men (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 219-222 
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    ISSN: 1432-1041
    Keywords: Thiamine ; pharmacokinetics ; analytical method ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A novel liquid chromatographic method for the determination of thiamine in plasma has been developed and has been used to study plasma thiamine concentrations after multiple dosage regimens for 11 days. The method involves purification, concentration and analytical separation of thiochrome on-line, using a switching column system. Ten healthy men were given 500 mg thiamine i.m. once a day (Group 1) and ten were given 250 mg p.o. every 12 h (Group 2). The times to reach steady state (7 and 5.6 days for Groups 1 and 2, respectively) were not different (P〉0.05). The mean elimination half-life was 1.8 days. The mean minimum steady-state concentration after the oral regimen (23 μg·l−1) was 78% of that after the intramuscular regime (29 μg·l−1).
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    Investigation of a possible pharmacokinetic interaction between ibopamine and isosorbide-5-mononitrate (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 549-552 
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    ISSN: 1432-1041
    Keywords: Ibopamine ; Isosorbide-5-mononitrate ; pharmacokinetics ; drug interaction ; healthy volunteers ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The possibility of a pharmacokinetic interaction between isosorbide-5-mononitrate (5-ISMN) and epinine, the active metabolite of ibopamine, has been investigated in 8 healthy male subjects given single doses of 200 mg ibopamine and 20 mg 5-ISMN, separately and together. The plasma 5-ISMN concentration-time profile was the same whether 5-ISMN was administered concomitantly with ibopamine or alone [AUC(o-t): 2.24 μg·ml−1·h after 5-ISMN alone, 2.16 μg·ml−1·h after 5-ISMN + ibopamine]. The plasma concentrations of total and free epinine and the urinary recovery of total epinine, homovanillic acid and dihydroxyphenylacetic acid, too, were not different when ibopamine was administered alone or concomitantly with 5-ISMN. The intake of ibopamine did not change the blood pressure and heart rate. The decrease in diastolic blood pressure induced by 5-ISMN was not influenced by concomitant intake of ibopamine. The observations suggest that in healthy volunteers there is no pharmacokinetic interaction between 5-ISMN and ibopamine.
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    Metamizole-furosemide interaction study in healthy volunteers (1992)
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    European journal of clinical pharmacology 42 (1992), S. 593-598 
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    ISSN: 1432-1041
    Keywords: Metamizole ; Furosemide ; prostaglandins ; drug interaction ; adverse effects ; pharmacokinetics ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic and pharmacodynamic interactions between metamizole (dipyrone) and furosemide were investigated in 9 of 12 healthy female subjects able to complete the study. They received oral metamizole 3×1 g for 3 days or placebo (cross-over) and on the last day of both study periods furosemide 20 mg IV. On the last two days a balanced sodium diet (120 mEq) and on Day 3 an oral water load (600 ml) were given. Metamizole significantly inhibited basal urine flow, whereas the fractional excretion of sodium and chloride and the 12 h-GFR remained unchanged. Metamizole significantly reduced furosemide clearance (175 vs 141 ml · min−1), furosemide-stimulated plasma renin activity (1.42 vs 0.79 ng AI · ml−1 · h−1) and the urinary excretion of prostacyclin metabolites and of prostaglandin F2α (by 70–81%). The renal clearance and terminal half-life of furosemide, peak renal chloride and volume excretion were unchanged. Thus, metamizole did not interact with the renal excretion and the diuretic effect of furosemide, although prostaglandin synthesis was significantly reduced.
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    Rectal bioavailability of 6-mercaptopurine in children with acute lymphoblastic leukaemia: partial avoidance of “first-pass” metabolism (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 619-622 
    Details
    ISSN: 1432-1041
    Keywords: 6-Mercaptopurine ; suppository ; bioavailability ; acute lymphoblastic leukaemia ; children ; interindividual variability ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma levels and the area under the plasma concentration-time curve (AUC) values of 6-mercaptopurine (6-MP) were determined in a balanced crossover study of oral (powder) and rectal (macrogol suppository) administration to 5 children with acute lymphoblastic leukaemia (ALL). The AUC (538.6 ng · h · ml−1) after the rectal dose of 30 mg/m2 was approximately 1.5-times of that (365.5 ng · h · ml−1) after the oral dose of 87.5 mg/m2. The coefficients of variation of interindividual variability of the AUCs were 21.5% and 32.3%, respectively. The relative bioavailability of the macrogol suppository compared to the powder was approximately 4.39. These findings indicate that rectal administration of 6-MP could avoid the first-pass effect of this drug in the alimentary canal and/or liver, resulting in a large AUC of 6-MP, and so could reduce interindividual variability in plasma 6-MP concentrations. Rectal administration of 6-MP may be more effective than empirical oral dosing for the treatment of children with ALL, especially for patients with nausea and/or vomiting.
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    Rebound of plasma vancomycin levels after haemodialysis with highly permeable membranes (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 635-639 
    Details
    ISSN: 1432-1041
    Keywords: Vancomycin ; Haemodialysis ; highflux membranes ; pharmacokinetics ; renal failure
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Vancomycin is usually given only once a week to haemodialysis (HD) patients. If highly permeable dialysis membranes are used, however, high clearance values have been reported, so the aim of the study was to determine whether high clearance of vancomycin resulted in sufficient drug elimination to induce subtherapeutic plasma levels after one week. In 18 chronic HD patients, treated with polysulfone dialyzers (1.2 m2), the pharmacokinetics of vancomycin were studied after administration of 1 g. Concentrations were determined by fluorescence polarisation immunoassay. At a blood flow of 219 ml·min−1, HD clearance of vancomycin was 62.3 ml·min−1. Immediately after dialysis plasma concentrations were 38% lower than predialysis levels. However, marked rebound in the vancomycin level was observed 5 h later, resulting in plasma levels only 16% lower than prior to dialysis. 3 HD treatments in 1 week removed about one third of the initial dose. After one week 15 of 18 patients still had a therapeutic plasma level (〉5 μg·ml−1). In conclusion, polysulfone membranes show high clearance of vancomycin. However, transfer of drug from blood to dialysate appears to be faster than from tissues to blood. Because of a marked rebound in plasma level after treatment, therapeutic drug concentrations will still be present in most patients after one week.
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    URL: http://dx.doi.org/10.1007/BF00265928
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    Effect of treatment at night with S-1452, a thromboxane A2 receptor antagonist, on the morning rise in platelet aggregation (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 501-505 
    Details
    ISSN: 1432-1041
    Keywords: S-1452 ; thromboxane A2 receptor antagonist ; nocturnal dosage ; platelet aggregation ; circadian rhythm ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary It is well known that platelet aggregation shows a morning rise, which may contribute to the increase in the onset of ischaemic heart diseases during the morning period. The present study was undertaken to determine whether nocturnal dosage with S-1452, a thromboxane AZ receptor antagonist, would blunt the morning rise in platelet aggregability. S-1452 50 mg or placebo were given orally to 8 healthy subjects at 10.00 h (day trial) or 22.00 h (night trial) according to a cross-over design. Plasma concentrations of S-1452 and its metabolites, bisnor-( + )-S-145 and tetranor-(+ )-S-145, and platelet aggregation were determined during the 12-hour period following the dose. Mean plasma concentrations of S-1452, bisnor-( + )-S-145 and tetranor-(+ )-S-145 during the absorption phase were lower after the nocturnal dose than after the morning dose. The maximum plasma concentration and area under the plasma concentration-time curve of the compounds were also lower and the time to the maximum concentration were delayed after the treatment at night. A morning rise in platelet aggregation was observed following placebo treatment. The inhibitory effect of S-1452 on platelet aggregation was observed at 3 hours and persisted for up to 9 h in both trials. The results suggest that S-1452 is absorbed more slowly after the nocturnal dose than after the morning dose. However nocturnal treatment with 50 mg S-1452 may blunt the morning rise in platelet aggregability.
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    URL: http://dx.doi.org/10.1007/BF02285091
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    Intracolonic bioavailability of human calcitonin in man (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 527-531 
    Details
    ISSN: 1432-1041
    Keywords: Calcitonin ; Colonic administration ; Bioavailability ; pharmacokinetics ; pharmacodynamics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Human calcitonin (hCT) injected into the lumen of the descending colon of normal human subjects was absorbed within minutes and could be recognized intact in plasma as shown by RIA in combination with reverse-phase HPLC. The absorption was low and variable, with bioavailabilities ranging from 0.01% to 2.7% relative to intravenously administered hCT (area under the concentrationtime curve). With intravenous hCT serum calcium was lowered and the fractional urinary excretion of calcium, phosphorus, sodium and chloride was significantly stimulated. With the intracolonic hCT, the fractional urinary excretions of calcium, sodium and chloride were also marginally stimulated relative to intracolonic vehicle (placebo). In conclusion, hCT is absorbed intact from the colon, but the bioavailability is low and highly variable.
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    URL: http://dx.doi.org/10.1007/BF02285096
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    Pharmacokinetic and blood pressure effects of carvedilol in patients with chronic renal failure (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 85-88 
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    ISSN: 1432-1041
    Keywords: Hypertension ; Carvedilol ; chronic renal failure ; pharmacokinetics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic and acute systemic haemodynamic effects of a single oral dose of 50 mg carvedilol has been studied in 24 hypertensive patients with chronic renal failure. The patients were stratified into 3 groups according to the creatinine clearance: I 51–90 ml · min−1; II 26–50 ml · min−1; III 4–25 ml · min−1. The area under plasma level time curve AUC, the elimination half-life t/12, the maximum plasma concentration Cmax, the time to peak concentration tmax were not significantly different between groups, whereas the amount of unchanged drug or metabolite excreted in urine Ae and the renal clearance CLR of carvedilol and its metabolites M2, M4, M5 were significantly decreased in Group III. Blood pressure and heart rate decreased in all 3 groups of patients after acute administration of 50 mg carvedilol. Mild adverse effects were reported in 6 patients. Despite a decrease in the renal clearance of carvedilol and of its metabolites with decreasing kidney function, its main pharmacokinetic parameters remained unchanged. The present results suggest that the dose of carvedilol need not be reduced in hypertensive patients with chronic renal failure.
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    URL: http://dx.doi.org/10.1007/BF02280760
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    The pharmacokinetics of tiopronin and its principal metabolite (2-mercaptopropionic acid) after oral administration to healthy volunteers (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 93-95 
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    ISSN: 1432-1041
    Keywords: Tiopronin ; 2-mercaptopropionic acid ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have studied the pharmacokinetics of tiopronin and its principal metabolite, 2-mercaptopropionic acid (2-MPA) in healthy volunteers after the oral administration of 500 mg (2 Acadione® tablets), followed by simultaneous assay of the two compounds in plasma over a period of 48 h using a new method (emission of fluorescence after HPLC and post-column derivatization by pyrene-maleimide). The absorption of tiopronin was slow (tmax between 4 and 6 h) and the plasma concentrations subsequently fell biexponentially. The principal metabolite 2-MPA appeared later in the plasma (tmax between 10 and 12 h after a lag-time of 3 h) then disappeared monoexponentially. About 15% of the tiopronin was metabolized to 2-MPA.
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    URL: http://dx.doi.org/10.1007/BF02280762
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    Lack of effect of omeprazole, cimetidine, and ranitidine on the pharmacokinetics of ethanol in fasting male volunteers (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 209-212 
    Details
    ISSN: 1432-1041
    Keywords: Ethanol ; gastric acid inhibition ; pharmacokinetics ; antisecretory drugs ; omeprazole ; ranitidine ; cimetidine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of three gastric antisecretory drugs on the pharmacokinetics of ethanol have been studied in a randomized crossover experiment. Male medical students (n=12) took ethanol 0.8 g/kg body weight at 08.00 h after an overnight fast. On seven successive days before drinking ethanol they were given omeprazole 20 mg, cimetidine 800 mg, ranitidine 300 mg, or no drug, with a period of at least 7 days between treatments. The peak blood ethanol concentration of 21.9 to 22.8 mmol·l−1 occurred at 64 to 70 min after the end of drinking. The rate of disappearance of ethanol from the blood ranged from 3.0 to 3.3 mmol·l−1·h−1 and the rate of removal from the whole body ranged from 8.0 to 8.5 g·h−1. The apparent volume of distribution of ethanol was almost the same for all four treatments: mean 0.68 l·kg−1, corresponding to a mean total body water of 441 (59% body weight). Mean areas under the concentration-time profiles of ethanol ranged from 83 to 87 mmol·l−1·h for the four treatments. It is concluded that omeprazole, cimetidine and ranitidine do not alter the kinetics of a moderate dose of ethanol.
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    URL: http://dx.doi.org/10.1007/BF00278486
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    Absence of interaction between tenoxicam and warfarin (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 227-229 
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    ISSN: 1432-1041
    Keywords: Tenoxicam ; Warfarin ; drug interaction ; pharmacokinetics ; anticoagulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of tenoxicam on plasma warfarin concentrations and on its anticoagulant effect has been studied in healthy volunteers. Tenoxicam did not alter the plasma warfarin concentration versus time profile. Treatment with it for 14 days had no effect on the average dose of warfarin required to maintain the prothrombin time within a specified range. The coumarin dose index, an indicator of warfarin sensitivity, remained unchanged during tenoxicam administration. The results demonstrate the lack of a clinically relevant effect of tenoxicam on warfarin-induced anticoagulation.
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    URL: http://dx.doi.org/10.1007/BF00278491
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    The influence of hydrochlorothiazide on the pharmacokinetics of enalapril in elderly patients (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 173-177 
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    ISSN: 1432-1041
    Keywords: Enalapril ; Hydrochlorothiazide ; pharmacokinetics ; renal impairment ; old patients
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a randomized, cross-over, single-dose study of 19 elderly hypertensive patients (aged 62–84 y, SBP 〉 160 mm Hg, DBP 〉 100 mm Hg, creatinine clearance 11–93 ml·min−1) we have studied the pharmacokinetics of the angiotensin converting enzyme (ACE) inhibitor enalapril after a single oral dose of either 10 mg enalapril or 10 mg enalapril + 25 mg hydrochlorothiazide. The pharmacokinetics of enalapril were unaffected by hydrochlorothiazide, but there was a significant reduction in renal clearance and a significant increase in AUC(0–24 h) of enalaprilat after hydrochlorothiazide, resulting in higher serum concentrations of the active drug. This was independent of the individual degree of renal impairment and might be due either to an initial reduction of GFR by hydrochlorothiazide or to interference with the tubular secretion of enalaprilat. The relationships between serum enalaprilat and serum ACE activity were similar after both treatments, both consistent with a value for Ki of enalaprilat of about 0.1 nmol·l−1. Thus, serum ACE activity was not affected by hydrochlorothiazide but completely reflected the pharmacokinetics of enalaprilat in both treatments.
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    Lack of pharmacodynamic and pharmacokinetic interactions of the antihistamine ebastine with ethanol in healthy subjects (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 179-184 
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    ISSN: 1432-1041
    Keywords: Ebastine ; Ethanol interaction ; carebastine ; psychomotor performance ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have given 12 healthy subjects the H1-antihistamine ebastine (20 mg) or placebo in a double-blind, crossover study for one week each. The subjects were tested for drug effects on Day 6 of each period, and for interactions of ebastine with ethanol (0.8 g·kg−1) on Day 7. On both days, the testing runs were done at baseline and at 2, 4, and 6 h after the drug. Performance was evaluated both objectively (digit symbol substitution, flicker fusion, Maddox wing, nystagmus, simulated driving, body balance) and subjectively (visual analogue scales) and with questionnaires. Venous blood samples were taken daily during maintenance and during each test run for assay of plasma carebastine. Blood ethanol concentrations were assayed with an Alcolmeter in the breath and directly in the blood. Plasma carebastine concentration reached a steady-state from Day 3 on; the mean concentrations in the morning were 92 µg·l−1 on Day 6 and 104 µg·l−1 on Day 7. The rise in plasma carebastine after an extra 20 mg of ebastine was accelerated but not increased by ethanol. Ebastine did not impair performance objectively or subjectively. It slightly improved body balance and reduced errors during simple tracking at 4 h. Blood ethanol concentrations peaked (mean 0.76 g·l−1) at 1.5 h after ethanol intake. Ethanol impaired performance in most objective tests and produced clumsiness, muzziness, and mental slowness, but little drowsiness. Ebastine neither modified the blood ethanol concentrations nor increased the effects of ethanol. We conclude that treatment with 20 mg ebastine once daily for one week provides steady concentrations of carebastine in plasma without impairment of skilled performance or important interactions with alcohol.
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    Lack of interaction ofβ-methyldigoxin with ranitidine in patients with chronic congestive heart failure (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 205-206 
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    ISSN: 1432-1041
    Keywords: β-Methyldigoxin ; Ranitidine ; pharmacokinetics ; drug interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
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    URL: http://dx.doi.org/10.1007/BF01740673
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    The effect of haemodialysis on the pharmacokinetics of tenoxicam in patients with end-stage renal disease (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 197-199 
    Details
    ISSN: 1432-1041
    Keywords: Tenoxicam ; pharmacokinetics ; haemodialysis ; end-stage renal disease
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have studied the pharmacokinetics of tenoxicam after single and multiple oral doses of 20 mg in five patients (2 men and 3 women) with end-stage renal disease undergoing haemodialysis. After a single dose, tenoxicam had a half-life (t1/2) of 33 h, an apparent clearance (CL·f−1) of 4.3 ml·min−1, and an apparent volume of distribution (Vz·f−1) of 11.8 l. The maximum tenoxicam concentration (Cmax) was 4.3 mg·l−1 at a median tmax of 1.7 h. There were no significant differences between the values calculated from the pre- or post-dialyser port plasma samples. Tenoxicam plasma concentrations measured during once daily dosing before and after haemodialysis showed that tenoxicam does not accumulate. Our findings suggest that dosage adjustment may not be required in patients with end-stage renal disease on haemodialysis taking tenoxicam.
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    Relationship between arterial and peripheral venous catecholamine plasma catecholamine concentrations during infusion of noradrenaline and adrenaline in healthy volunteers (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 245-249 
    Details
    ISSN: 1432-1041
    Keywords: Noradrenaline ; Adrenaline ; catecholamines ; pharmacokinetics ; healthy volunteers ; IV infusion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Noradrenaline and adrenaline were infused IV at 5 different rates (0.01–0.2 μg · kg · min− for 30 min to volunteers. The plasma catecholamine concentrations were determined by HPLC and electro-chemical detection. At the highest infusion rate, the arterial and venous plasma concentrations of noradrenaline increased from 1.18 to 44.1 nmol · l−1and from 1.14 to 31.9 nmol · l−1, respectively, and of adrenaline from 0.29 to 23.9 nmol · l−1 and from 0.28 to 19.3 nmol · l−1 respectively. The peripheral venous plasma concentration of noradrenaline averaged 76% of the arterial concentration, and of adrenaline it was 73%. There was a linear relationship between the peripheral venous and arterial plasma noradrenaline and adrenaline concentrations at therapeutic doses.
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    Pharmacokinetic profile of a novel slow release preparation of molsidomine (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 273-276 
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    ISSN: 1432-1041
    Keywords: Molsidomine ; slow release ; pharmacokinetics ; in vitro/in vivo correlation ; pharmacokinetics ; healthy volunteers ; dissolution profile
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A novel slow release preparation containing 24 mg molsidomine has been investigated in 6 healthy subjects. Individual concentration/time-profiles after the tablet showed two separate concentration peaks at 2.2 h and 15.0 h. The relative bioavailability of the slow release preparation in comparison to an aqueous solution of molsidomine was 0.67. The in vivo dissolution profile revealed either a progressive decrease in dissolution velocity caused by altered physico-chemical conditions in the ileum and the colon or a progressive reduction in the absorption constant. In all subjects deconvolution revealed a punctual increase in absorption about 15 h post-dose, coinciding with the second peak of the concentration/time-profile. Therapeutic plasma levels of molsidomine (〉 5 ng · ml−1 were not maintained over 24 h by this slow release formulation.
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    Captopril does not interact with the pharmacodynamics and pharmacokinetics of digitoxin in healthy man (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 445-447 
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    ISSN: 1432-1041
    Keywords: Captopril ; Digitoxin ; impedance cardiography ; drug interaction ; healthy volunteers ; pharmacodynamics ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The chronic oral administration of 0.07 mg digitoxin o. d. for up to 58 days to 12 healthy volunteers caused a small drop in mean heart rate HR (95 % CI: −7.9 to −1.6 beats · min−1), in mean diastolic blood pressure (95 % CI: −8.3 to −0.4 mm Hg), shortening of the QTc-interval (95 % CI: −42 to −19 ms), shortening of the HR-corrected pre-ejection period PEPc (95 % CI: −16 to −1 ms) and electromechanical systole QS2c (95 % CI: −25 to −1 ms), and an increase in the impedance cardiographic Heather index (dZ/dtmax/RZ, 95 % CI: 0.3 to 4.3) relative to the baseline measurements before digitalisation. The concomitant administration of 25 mg oral captopril b. d. did not significantly alter these responses relative to the concomitant double-blind administration of placebo, nor did it alter the pharmacokinetic characteristics of plasma digitoxin at steady state. Thus, no relevant change in the pharmacokinetic and pharmacodynamic characteristics of chronically administered digitoxin were induced by concomitant treatment with captopril.
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    Enantioselective pharmacodynamics and pharmacokinetics of chiral non-steroidal anti-inflammatory drugs (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 237-256 
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    ISSN: 1432-1041
    Keywords: Non-steroidal anti-inflammatory drugs ; Enantioselective ; Enantiomers ; pharmacodynamics ; pharmacokinetics ; stereoselective
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
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    URL: http://dx.doi.org/10.1007/BF00266343
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    Acute effects of drinking grapefruit juice on the pharmacokinetics and dynamics on felodipine — and its potential clinical relevance (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 313-317 
    Details
    ISSN: 1432-1041
    Keywords: Dihydropyridine ; Felodipine ; availability ; flavonoids ; dietary interaction ; pharmacokinetics ; pharmacodynamics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of drinking grapefruit juice on the acute pharmacokinetic and haemodynamic actions of the dihydropyridine calcium antagonist felodipine given as a 5 mg plain tablet has been studied in nine, healthy, middle-aged males. Compared to water, grapefruit juice caused an increase in Cmax from mean 6 to 16 nmol · l−1, and in the AUC from 23 to 65 nmol · h · l−1. The change in AUC corresponded to an increase in the systemic availability of felodipine from 15 to 45%, assuming no change in its clearance. This change was probably caused by inhibition of the oxidation of felodipine to the inactive dehydrofelodipine by flavonoids in grapefruit juice. The interaction with grapefruit juice is believed to be a class effect for the dihydropyridines, as oxidation of the dihydropyridine ring to the corresponding pyridine derivative is a major metabolic route for all these drugs. The higher plasma concentrations of felodipine taken with grapefruit juice resulted in a greater change in blood pressure measured in the morning 3 h after dosing (−9%) than did water (0%).
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    Pharmacokinetics of midazolam during continuous infusion in critically ill neonates (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 329-332 
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    ISSN: 1432-1041
    Keywords: Midazolam ; Fentanyl ; Neonates ; pharmacokinetics ; sedation drug interaction ; hypotension
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Midazolam is a water soluble benzodiazepine, with a short elimination half-life in adults and children. An IV bolus (0.2 mg·kg−1) immediately followed by continuous infusion of 0.06 mg·kg−1·h−1 was administered to 15 critically ill neonates at a gestational age of 32.8 weeks, who required sedation for mechanical ventilation. Heart rate and blood pressure were closely monitored. Hypotension occurred in 4 patients after the bolus dose or during the continuous infusion. Three of them had also been given fentanyl. Individual pharmacokinetic parameters were calculated: plasma clearance was 3.9 ml·min−1, elimination half-life was 12.0 h. Because of its short half-life compared to diazepam, midazolam may be used during the neonatal period to achieve rapid, brief sedation. However, it should be administered cautiously to neonates, particularly in premature infants, or if fentanyl is also given.
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    Theophylline steady state pharmacokinetics is not altered by omeprazole (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 343-345 
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    ISSN: 1432-1041
    Keywords: Omeprazole ; Theophylline ; pharmacokinetics ; drug interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of omeprazole treatment on theophylline pharmacokinetics was studied in eight, non-smoking healthy male volunteers during repeated administration of a slow release formulation of theophylline. In a randomized double-blind cross-over study, the subjects received theophylline 5 mg·kg−1 per day with omeprazole 20 mg per day or identical placebo during two periods, each of 7 days, separated by a washout period of 7 days. The oral clearance of theophylline remained unchanged whether it was administered alone or with omeprazole (54.2 ml·min−1). The average urinary excretion of theophylline and its metabolites, 1,3 dimethyluric acid (1,3-DMU), 3-methylxanthine (3-MX), 1-methyluric acid (1-MU) amounted to 9%, 32%, 12% and 22% of the administered dose, respectively, and no significant change occured during concomitant treatment with omeprazole. Thus, the formation and clearance of the metabolites was not altered by omeprazole. Consequently, omeprazole in the recommended dose of 20 mg daily can safely be administered to patients on theophylline therapy.
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    Disposition kinetics and concentration-effect relationship of metipranolol in patients with cirrhosis and healthy subjects (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 337-340 
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    ISSN: 1432-1041
    Keywords: Metipranolol ; Liver cirrhosis ; pharmacokinetics ; pharmacodynamics ; beta-adrenoreceptor blockade
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The disposition kinetics and heart rate reducing effect of deacetylmetipranolol (DMP), the active form of the β-adrenoreceptor blocking agent metipranolol (MP), administered as a single 40 mg oral dose have been compared in 6 patients with cirrhosis and 6 healthy volunteers. The mean maximal DMP concentration was significantly higher and the time to reach the peak level shorter in the patients compared to the healthy subjects. There was also a significantly higher AUC of DMP, a shorter half-life of the rapid phase of the decline in DMP concentrations, a smaller central compartment and lower apparent DMP clearance in patients. A correlation with the albumin level was observed in cirrhotics for individual values of apparent DMP clearance (r=0.92) and AUC (r=-0.89). The maximal reduction in heart rate was recorded in patients at plasma DMP levels which were already significantly lower than the peak levels. Median inhibitory concentrations (IC50) and maximum possible heart rate reductions (Δ HRmax), obtained by fitting individual plots of the plasma DMP concentration-effect relationship to the inhibitory Emax model in the postdistributional phase of DMP disposition were significantly higher in cirrhotics than in healthy subjects. It is conjectured that down-regulation of adrenoreceptors due to chronic sympathetic activation in hepatic cirrhosis contributes to decreased sensitivity to the reduction in heart rate following a single dose of the beta-blocker.
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    Influence of food on serum ambenonium concentration in patients with myasthenia gravis (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 371-374 
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    ISSN: 1432-1041
    Keywords: Ambenonium chloride ; Myasthenia gravis ; dietary effect ; serum concentration ; adverse effects ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Influence of food on the serum concentration and kinetics ambenonium chloride (AMBC) has been examined in thirteen patients with myasthenia gravis (MG). Mean serum concentrations and Cmax during fasting were higher than those in the non-fasting state. The AUC (0–3 h) was also about four-times larger. The drug effects versus the serum concentration were observed to be anti-clockwise or clockwise. The effective range of the Cmax varied between patients. The unexpected increase in Cmax led to adverse muscarinic actions of AMBC, when the condition was changed from the non-fasting to the fasting state. It is recommended that the dose be changed during non-fasting treatment when adjusting the optimum regimen for patients myasthenia gravis. Patients must be advised to keep to the dosing and dietary schedule in order to avoid unexpected adverse actions to AMBC.
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    Stereoselective pharmacokinetics of oral nitrendipine in elderly hypertensive patients with normal and impaired renal function (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 423-427 
    Details
    ISSN: 1432-1041
    Keywords: Nitrendipine ; enantiomers ; stereoselectivity ; Renal failure ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of the enantiomers of nitrendipine has been studied in seven elderly patients with chronic renal failure (CRF) and in six control subjects (mean creatinine clearance 30 and 97 ml·min−1 respectively). Racemic nitrendipine 20 mg was given once daily for seven days and the pharmacokinetics of the enantiomers over the last dosage interval were determined using a stereospecific assay. In both groups nitrendipine exhibited stereoselective pharmacokinetics (AUC, Cmax), but the half-lives of the enantiomers did not differ in individual subjects. As an index of stereoselectivity, the mean S/R ratio of AUCs in control subjects (2.07) was not significantly different from the ratio in patients with CRF (2.68). The mean AUCs of (S)- and (R)-nitrendipine during the last dosage interval were increased in CRF by 132% and 85%, respectively. The observed doubling of the half-lives and the increases in Cmax did not reach significance because of the large variability in each group. Thus, the pharmacokinetics of oral nitrendipine is altered in CRF, but there was no change in the stereoselectivity of its pharmacokinetics.
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    URL: http://dx.doi.org/10.1007/BF00280129
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    Chloroquine levels in blood during chronic treatment of patients with rheumatoid arthritis (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 429-433 
    Details
    ISSN: 1432-1041
    Keywords: Chloroquine ; Rheumatoid arthritis ; desethylchloroquine ; bisdesethylchloroquine ; blood levels ; toxicity ; therapeutic activity ; dose-effect relationship ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Blood levels of racemic chloroquine and its main metabolites desethylchloroquine and bisdesethylchloroquine were measured in 29 patients treated chronically for rheumatoid arthritis. In six patients, the concentrations were followed during a one day dosage interval. There was considerable intersubject variability in the steady state blood concentrations of chloroquine (range 36.6 to 3895 ng·ml−1) and its two main biotransformation products; the latter represented, respectively, 47.7% and 12.9% of the concentration of chloroquine. This finding shows the need for further studies in view of the known toxic effects of chloroquine and the inevitable accumulation due to the exceptionally long residence time of the compound and its metabolites. The main requirement, which has not yet been met, for adding chloroquine to the list of drugs for which therapeutic drug monitoring is useful, is the lack of information about its mechanism of action, and consequently the dose-effect relationships of its therapeutic and toxic actions. Regular ophthalmic examination, in particular, is strongly recommended. The relatively high concentrations of desethylchloroquine and bisdesethylchloroquine found during chronic treatment show the need for more information about the therapeutic value and adverse effects of the metabolites.
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    URL: http://dx.doi.org/10.1007/BF00280130
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    Elevated plasma nilvadipine concentration after single and chronic oral administration to patients with chronic liver disease (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 475-479 
    Details
    ISSN: 1432-1041
    Keywords: Calcium channel blocker ; Nilvadipine ; blood pressure ; liver disease ; pharmacokinetics ; pharmacodynamics ; cirrhosis ; hepatitis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Fourteen normotensive patients with liver disease (6 with cirrhosis and 8 with chronic hepatitis) and 7 healthy volunteers were given a single oral dose of nilvadipine 2 mg. In addition, nilvadipine 4 mg was administered orally twice daily for several months to 6 hypertensive patients with mild liver dysfunction and 18 hypertensives with normal liver function. A significant increase in plasma nilvadipine was found in the patients with cirrhosis as compared both to the normal and chronic hepatitis subjects; the time to peak concentration was similar among the three groups. The peak plasma nilvadipine concentration was closely correlated both with the serum albumin level and the retention of indocyanine green. Changes in blood pressure, pulse rate and various vasoactive hormones following a single oral dose of nilvadipine did not differ between the groups. Thus, an increase in plasma nilvadipine relative to the level in normal subjects was demonstrated in patients with cirrhosis following a single oral dose, as well as in patients with slight liver dysfunction following long-term oral administration.
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    URL: http://dx.doi.org/10.1007/BF00314853
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    Digoxin-interactions in man: Spironolactone reduces renal but not biliary digoxin clearance (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 481-485 
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    ISSN: 1432-1041
    Keywords: Digoxin ; Spironolactone ; drug interaction ; biliary clearance ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The possibility of an inhibitory effect of spironolactone on the biliary clearance of digoxin has been investigated in 6 healthy subjects. Plasma clearance and the renal and biliary clearance of digoxin were determined twice at steady state (digoxin 0.5 to 1 mg·d−1 p.o. for 6 days), alone or in combination with spironolactone 200 mg daily, after an intravenous dose of digoxin (0.7 × oral dose) on Day 7. Plasma and urine were collected for 48 h. Biliary clearance of digoxin was determined on Day 8 by a duodenal perfusion technique. During spironolactone treatment plasma digoxin clearance tended to be lower (255 vs 224 ml/min; P=0.057) and renal clearance significantly lower (166 vs 144 ml/min), while the biliary clearance of digoxin remained unchanged (106 vs 103 ml/min). Thus, spironolactone reduced the renal clearance of digoxin by an average of 13%, without affecting its biliary clearance.
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    URL: http://dx.doi.org/10.1007/BF00314854
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    Pharmacokinetics of vinorelbine in man (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 545-547 
    Details
    ISSN: 1432-1041
    Keywords: Vinorelbine ; anti-neoplastic agents ; vinca alkaloids ; pharmacokinetics ; lung neoplasms ; HPLC ; assay method
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of vinorelbine has been investigated by a new HPLC method in 8 cancer patients receiving 8 weekly doses (30 mg·m−2) administered by brief infusion (15 min). The plasma concentration-time curves showed a tri-exponential decay with a long terminal half-life (44.7 h) and a high volume of distribution (Vz=75.61·kg−1). The concentrations after the 8th infusion were significantly lower than after the 1st infusion, but without significant modification of CL (1.28 l·h−1·kg−1) or AUC (0.80 mg·l−1·h). The pharmacokinetic parameters exhibited wide inter-individual variations. The results are consistent with those of previous RIA studies, although the HPLC method appears to be more specific and more precise.
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    URL: http://dx.doi.org/10.1007/BF00314866
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    The postoperative pharmacokinetics of codeine (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 663-666 
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    ISSN: 1432-1041
    Keywords: Morphine ; Codeine ; drug metabolism ; pharmacokinetics ; systemic availability ; individual variability ; post-operative state
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The metabolism and systemic availability of codeine have been studied in 12 patients after cholecystectomy. They were given 20 mg codeine as an IV bolus dose on the first day after surgery and 50 mg codeine as a single oral on the fourth day after surgery. Codeine had a medium to high extraction ratio and a total plasma clearance of 10.8 (4.3) ml·min−1·kg−1. The clearance varied fourfold between subjects. All the patients were extensive metabolizers with regard to the debrisoquine/sparteine polymorphism, as tested using dextromethorphan as the probe drug. Nevertheless, the formation of morphine from codeine was very small and plasma morphine concentrations were below the detection limit of 3.3 nmol·1−1 (1 ng·ml−1). As a corollary, the morphine/codeine ratio in the the concentration-time curves was less than 3% in all the patients. The systemic availability of codeine varied extensively between subjects (range 12–84%). This might partly explain differences in the dose of codeine required as an analgesic.
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    URL: http://dx.doi.org/10.1007/BF00265933
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    The pharmacokinetics of nifurtimox in chronic renal failure (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 671-673 
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    ISSN: 1432-1041
    Keywords: Nifurtimox ; Changas' disease ; renal failure ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of nifurtimox, a drug used in the treatment of Trypanosoma cruzi infections, has been studied in seven patients with chronic renal failure undergoing haemodialysis, and in seven healthy subjects. Each subject took nifurtimox 15 mg·kg−1 orally and blood samples were obtained for 10 h after administration. Nifurtimox in serum was analyzed by HPLC. The patients with chronic renal failure had a higher Cmax than the control subjects due to a change in systemic availability. An alternative explanation would be that both the distribution volume and the clearance had changed. The mean half-life in the patients with chronic renal failure was similar to that in the healthy subjects.
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    URL: http://dx.doi.org/10.1007/BF00265935
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    Lack of pharmacokinetic interaction between moxonidine and hydrochlorothiazide (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 209-210 
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    ISSN: 1432-1041
    Keywords: Moxonidine ; Hydrochlorothiazide ; pharmacokinetics ; drug interaction ; steady-state ; healthy volunteers ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01740675
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    Altered pharmacokinetics of lignocaine after epidural injection in Type II diabetics (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 269-271 
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    ISSN: 1432-1041
    Keywords: Lignocaine ; diabetes mellitus ; pharmacokinetics ; epidural anaesthesia
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of lignocaine has been compared after epidural anaesthesia in diabetics and nondiabetic patients. Epidural lignocaine 8 mg · kg−1 was given to 8 well controlled Type II diabetic and 8 nondiabetic patients and the plasma drug concentration in serial blood samples were measured by HPLC. The plasma level of lignocaine was lower in diabetics compared to non-diabetics. The peak level was attained at 20 min in both groups. The clearance of the drug was significantly higher, (39,9 vs 16,7 ml · min− · kg−) associated with a decreased elimination half-life and mean residence time. The study suggests that the rate of absorption of lignocaine is not altered after epidural administration and that its hepatic metabolism is increased in diabetics compared to non-diabetics.
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    URL: http://dx.doi.org/10.1007/BF02333021
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    Pharmacokinetic estimations from microdialysis data (1992)
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    European journal of clinical pharmacology 43 (1992), S. 289-294 
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    ISSN: 1432-1041
    Keywords: Microdialysis ; Drug concentration ; parameter estimation ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Microdialysis has recently been adapted for sampling the extracellular fluid of various organs in order to measure drug concentrations, and the first clinical application has been published. My aim here is to provide simple rules about how to analyse pharmacokinetic data from such studies. The plotting of data on a time scale and the estimation of C (0) and slopes is not a trivial problem when multicompartmental models are assumed or sampling intervals are unequal. I have developed formulae and algorithms to solve the problem. A simple rule of thumb is given, suggesting when these formulae need to be applied. It is shown that the calculations of half-life and slopes is similar to standard methods for equal sample intervals and that calculation of AUC and clearance may be even more accurate for microdialysis data than for ordinary blood sampling, because of the time-integral character of the dialysis method. I have dealt with both zero-order and first-order kinetics.
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    Pharmacokinetics of pirmenol in young and elderly subjects (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 437-439 
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    ISSN: 1432-1041
    Keywords: Pirmenol ; pharmacokinetics ; elderly subjects ; age effect ; adverse effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The steady state pharmacokinetics of pirmenol was compared in twelve healthy young (aged 18 to 45 y) and 11 elderly subjects (over 65 y) subjects given pirmenol HCl 100 mg every 12 h for a total of 14 doses. In addition, the single-dose pharmacokinetics of pirmenol was determined following a 100 mg oral dose in the young subject group for comparison with the results of repeated administration. In the young subjects, the mean single-dose and steady-state CLR of pirmenol were similar; however, Ae was 29 % higher and CL/f was 22 % lower at steady state than after the single dose. Steady-state (fourteenth dose) Cmin, Cmax, tmax, λz, Ae, CL/f, CLR and V values were similar in the young and elderly subjects. Based on pharmacokinetic considerations, the dosage of pirmenol is unlikely to differ in young and elderly subjects.
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    URL: http://dx.doi.org/10.1007/BF02220624
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    The effect of a low dose of quinidine on the disposition of flecainide in healthy volunteers (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 441-443 
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    ISSN: 1432-1041
    Keywords: Flecainide ; quinidine ; pharmacokinetics ; metabolism inhibition ; drug interaction ; renal transport
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have studied the effects of quinidine on ECG intervals and on the pharmacokinetics of flecainide and its two metabolites in 6 healthy men in an open randomized crossover study. Flecainide acetate (150 mg) was given as a constant rate i. v. infusion over 30 min. Quinidine (50 mg orally), given the previous evening, did not change the volume of distribution of flecainide (7.9 vs 7.41·kg−1), but significantly increased its half-life (8.8 vs 10.7 h). This was attributable to a reduction in total clearance (10.6 vs 8.1 ml·min−1·kg−1), most of it being accounted for by a reduction in non-renal clearance (7.2 vs 5.2 ml·min−1·kg−1). The excretion of the metabolites of flecainide over 48 h was significantly reduced. These findings suggest that quinidine inhibits the first step of flecainide metabolism, although it may also reduce its renal clearance, but to a lesser extent (3.5 vs 2.9 ml·min−1·kg−1). The effects of flecainide on ECG intervals were not altered by quinidine. Thus, quinidine tends to shift extensive metabolizer status for flecainide towards poor metabolizer status and may also alter its renal excretion.
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    Capture of gypsy moth,Lymantria dispar (L.), andLymantria mathura (L.) males in traps baited with disparlure enantiomers and olefin precursor in the People's Republic of China (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 2153-2159 
    Details
    ISSN: 1573-1561
    Keywords: Lymantria dispar ; gypsy moth ; Lymantria mathura ; Lepidoptera ; Lymantriidae ; pheromone ; disparlure ; cis-7,8-epoxy-2-methyocta-decane
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Pheromone traps baited with (+)-disparlure,cis-7,8-epoxy-2methyocta-decane, captured males ofLymantria dispar, L. monacha, andL. mathura in northeastern People's Republic of China.L. dispar responded to the addition of olefin to (+)-disparlure-baited traps in a negative doseresponse manner. Observations on site and seasonal capture ofL. dispar andL. mathura are discussed.
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    Behavioral and electrophysiological activity of (Z,E)-7,9,11-dodecatrienyl formate, a mimic of the major sex pheromone component of carob moth,Ectomyelois ceratoniae (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 2331-2352 
    Details
    ISSN: 1573-1561
    Keywords: Lepidoptera ; Pyralidae ; sex pheromone ; (Z,E)-9,11,13-tetradecatrienal ; mimic ; (Z,E)-7,9,11-dodecatrienyl formate ; wind tunnel ; attractant ; electrophysiology ; receptor cell
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract The behavioral and electrophysiological activity of a mimic [(Z,E)7,9,11-dodecatrienyl formate] of the major sex pheromone component [(Z,E) 9,11,13-tetradecatrienal] of carob moth was assessed. Wind-tunnel bioassays demonstrated that the formate was as effective as natural gland extracts, and significantly more effective than the trienal alone or than the trienal blended with two minor pheromone components, in evoking source contact. Dispensers containing the formate were as effective as trienal-containing blend lures in attracting males when placed at the same dosage in traps in date gardens. Single-cell recordings showed that at least two olfactory neurons, differentiated by spike amplitude, are located in the long trichoid hairs on male carob moth antennae. Dose-response relationships indicated that puffs from cartridges loaded with at least 0.1 μg of the formate or of the trienal were necessary to elicit spiking by either the small or the large-spiking cell within a sensillum. Cross-adaptation studies demonstrated that both compounds stimulated the same large-spiking cell. The frequencies of spikes evoked from the large cell when stimulated by emissions from 0.1-μg, 1-μg, or 10-μg cartridges of either the formate or the trienal were not significantly different, suggesting that the formate is an effective mimic of the trienal at the antennal receptor cell level.
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    Evaluation of flavonoids inGossypium arboreum (L.) cottons as potential source of resistance to tobacco budworm (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 105-114 
    Details
    ISSN: 1573-1561
    Keywords: Cotton ; Gossypium arboreum ; tobacco budworm ; Heliothis virescens ; Lepidoptera ; Noctuidae ; resistance ; allelochemicals ; flavonoids ; gossypetin 8-0-rhamnoside ; gossypetin 8-0-glucoside
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Asiatic cottons [Gossypium arboreum (L.)] have been investigated as a source of resistance to the tobacco budworm [Heliothis virescens (Fab.)] because their diversely colored petals have been presumed to contain various allelochemicals. However, we found that larvae fedG. arboreum squares (buds) grew about equally compared with those fed squares from commercialG. hirsutum lines. The best source of resistance was found in severalG. hirsutum double-haploid (DH) lines. In our investigation of allelochemicals, G.arboreum lines were found to contain much less gossypol in leaves, squares (buds), and petals thanG. hirsutum L. lines. Flavonoids were significantly higher inG. arboreum lines only in petals. Of 22G. arboreum lines from which squares were gathered and fed to tobacco budworm (TBW) larvae in the laboratory, larval growth was not significantly decreased on any, but larval survival was decreased on six. When the square flavonoids were isolated and incorporated in laboratory diets for the TBW, moderate toxicity was observed. However, the estimated toxicities were not greater than those of the same flavonoid isolates fromG. hirsutum lines. The most prevalent flavonoids, all previously found in G.arboreum plant tissues, were gossypetin 8-0-glucoside and gossypetin 8-0-rhamnoside, neither of which were present inG. hirsutum tissue. Quercetin 3-0-glucoside, quercetin-3′-0-glucoside, and quercetin 7-0-glucoside were also present in significant amounts in both species. Gossypetin 8-0-rhamnoside and gossypetin 8-0-glucoside were the most toxic flavonoids tested (the ED50% was estimated to be 0.007 and 0.024) and therefore may prove to be contributing factors of resistance to TBW feeding.
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    Attraction ofHeliothis virescens (F.) (Lepidoptera: Noctuidae) to volatiles from extracts of cotton flowers (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 907-914 
    Details
    ISSN: 1573-1561
    Keywords: Tobacco budworm ; Heliothis virescens ; Lepidoptera ; Noctuidae ; cotton ; gossypium hirsutum ; oviposition ; attractant ; floral extracts
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Mated and virgin female and virgin male tobacco budworm moths,Heliothis virescens (F.), responded via directed upwind flight in wind-tunnel bioassays to volatiles from floral extracts of cotton,Gossypium hirsutum L. Significantly more male and female moths landed on cloth dispensers treated with a methylene chloride extract of debracted flowers than on control dispensers treated only with methylene chloride. Only mated females landed in significant numbers on the dispensers treated with extract of cotton squares, flowers (including bracts), or flower petals. After landing, most of the moths examined the dispensers by probing with their antennae, proboscis, and/or ovipositor.
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    Influence of cabbage proteinase inhibitorsin situ on the growth of larvalTrichoplusia ni andPieris rapae (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 1009-1024 
    Details
    ISSN: 1573-1561
    Keywords: Pieris rapae ; Artogeia rapae ; Trichoplusia ni ; Lepidoptera ; Noctuidae ; Pieridae ; trypsin inhibitors ; chymotrypsin inhibitors ; serine proteinase inhibitors ; cabbage ; Cruciferae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Trypsin and chymotrypsin inhibitors are proteins that are developmentally regulated in foliage of cabbage plants, appearing at high concentrations in young foliage on mature plants. This temporal and spacial regulation of foliar proteinase inhibitors is synchronized with the appearance and distribution of foliar feeding Lepidoptera. When insects were allowed to select their feeding sites, larvalPieris rapae fed on the young foliage of cabbage plants, while larvalTrichoplusia ni fed on the mature foliage on cabbage plants. LarvalP. rapae that fed on mature plants were significantly smaller than larvae feeding on young plants, while there was no significant difference between larvalT. ni feeding on mature plants and those feeding on young plants. Thus, there was a significant inverse correlation between the level of proteinase inhibitory activity in cabbage foliage and larval growth. WhenP. rapae andT. ni were provided with an artificial diet containing total protein (including significant levels of proteinase inhibitors) that was extracted from cabbage foliage, there was a significant reduction in growth and development of both species of Lepidoptera.
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    Qualitative and quantitative analyses of volatiles and pheromone gland extracts collected fromGalleria mellonella (L.) (Lepidoptera: Pyralidae) (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 1255-1268 
    Details
    ISSN: 1573-1561
    Keywords: Lepidoptera ; Pyralidae ; Gallerinae ; Galleria mellonella ; greater wax moth ; sex pheromone gland ; nonanoic acid ; undecanoic acid ; 1-nonanol ; 1-undecanol
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Chemical analyses of pheromone-gland extracts and volatiles released by maleGalleria mellonella (L.), the greater wax moth, resulted in the identification and quantification of the aldehydes, primary alcohols, and fatty acids of nonane and undecane. Adult females released none of these six compounds. Mean percentages of the aldehydes and alcohols in the gland extracts were 19.0% undecanal, 3.9% nonanal, 48.3% 1-undecanol, and 28.8% 1-nonanol. Mean percentages of the aldehydes and alcohols in volatiles collected during the first hour of scotophase from moths 1 to 9 days old were 77.4% undecanal, 20.8% nonanal, 1.46% 1-undecanol, and 0.36% 1-nonanol. Age did not significantly affect the amount of each compound collected. The collection of volatiles from moths 3 to 5 days old during a 12-hr scotophase indicated that production was greatest during the first and third quarters of the period. Methylation of group volatile samples allowed the quantification of the fatty acids.
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    Abraxas grossulariata L. (Lepidoptera: Geometridae): Identification of (3Z,6Z,9Z)-3,6,9-heptadecatriene and (6Z,9Z)-6,9-cis-3,4-epoxyheptadecadiene in the female sex pheromone (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 13-25 
    Details
    ISSN: 1573-1561
    Keywords: Pheromone identification ; (6Z,9Z)-6,9-cis-3,4-epoxyhepta-decadiene ; (3Z,6Z,9Z)-3,6,9-heptadecatriene ; Abraxas grossulariata ; Lepidoptera ; Geometridae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract (3Z,6Z,9Z)-3,6,9-Heptadecatriene and (6Z,9Z)-6,9-cis-3,4-epoxyheptadecadiene have been identified in female sex pheromone gland extracts ofAbraxas grossulariata L. (Lepidoptera: Geometridae). The compounds were detected by gas chromatography with electroantennographic detection (GC-EAD) and identified by GC-mass spectrometry (GC-MS). The amounts of hydrocarbon and epoxide were 0.13 and 0.42 ng/female, respectively. These identifications were confirmed by synthesis; the absolute configuration of the epoxide remains to be determined. Another isomeric epoxide, (3Z,6Z)-3,6-cis-9,10-epoxyheptadecadiene, was tentatively identified in small amounts (0.04 ng/female). Racemic (6Z,9Z)-6,9-cis-3,4-epoxyheptadecadiene elicited the largest electroantennogram response within a series of heptadecadiene and nonadecadiene monoepoxides and the corresponding trienic hydrocarbons and, in field tests, attracted maleA. grossulariata into traps. Addition of 10% (3Z,6Z,9Z)-3,6,9-heptadecatriene to this epoxide enhanced attractiveness; addition of (3Z,6Z)-3,6-cis-9,10-epoxyheptadecadiene had no effect at low proportions while higher proportions caused a reduction in the numbers of males caught.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00997161
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  • 93
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    Multicomponent sex pheromone inMacrocentrus grandii Goidanich (Hymenoptera: Braconidae) (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 1901-1912 
    Details
    ISSN: 1573-1561
    Keywords: Parasitoid ; pheromone ; bioassay ; wind-tunnel ; Hymenoptera ; Braconidae ; Macrocentrus grandii ; Lepidoptera ; Pyralidae ; Ostrinia nubil-alis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract A multicomponent sex pheromone inMacrocentms grandii Goidanich (Hymenoptera: Braconidae) was demonstrated using wind-tunnel and field bioassays. In wind-tunnel bioassays, three Florisii fractions from female wasps (hexane, 5%, and 50% ether in hexane) and one from male wasps (50% ether in hexane) were attractive to males. The hexane and 5% ether in hexane fractions each elicited similar male behavioral responses. These included upwind anemotaxis, casting, landing on the source, wing fanning, and mating attempts between males. The 50% ether in hexane fraction, whether male- or female-derived, initiated a strong flight response by males but few landings on the source. In addition, the 50% ether in hexane fraction was found to synergize strongly the hexane fraction. All females tested in the wind tunnel gave no responses to male- or female-derived extracts. Field tests generally supported the wind-tunnel results, although no field attraction was observed for the 5% ether in hexane fraction.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981915
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  • 94
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    Sex pheromone components of the giant looper,Boarmia selenaria schiff. (Lepidoptera: Geometridae): Identification, synthesis, electrophysiological evaluation, and behavioral activity (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 165-181 
    Details
    ISSN: 1573-1561
    Keywords: Boarmia selenaria ; giant looper ; sex pheromones ; Lepidoptera ; Geometridae ; (Z,Z)-6,9-cis-(3S,4R)-epoxynonadecadiene ; (Z,Z)-6,9-cis-(3R,4S)-epoxynonadecadiene ; (Z,Z,Z)-3,6,9-nonadecatriene, anantiomers ; enantioselective synthesis ; EAG ; wind tunnel ; field tests ; precursor
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract (Z,Z)-6,9-cis-(3S,4R)-Epoxynonadecadiene9a and (Z,Z,Z)-3,6,9-nonadecatriene have been identified as sex pheromone components in female ovipositor extracts and effluvia of the geometridBoarmia selenaria. The identification was based on relative retention times on gas chromatographic columns, GC-MS, chemical enantioselective syntheses, EAG, wind-tunnel behavioral experiments, and field tests. A single female ovipositor extract contained an average of 42 ng of (Z,Z)-6,9-cis-3,4-epoxynonadecadiene and 2 ng of (Z,Z,Z)-3,6,9-nonadecatriene.EAG, wind-tunnel behavioral studies, and field tests demonstrated that maleB. selenaria exhibit preferential attraction for the (3S,4R)-enantiomer of (Z,Z)-6,9-cis-3,4-epoxynonadecadiene. Only in effluvia and ovipositor extracts of calling females was (Z,Z)-6,9-cis- 3,4-epoxynonadecadiene detected, whereas relatively high amounts of (Z,Z,Z)-3,6,9-nonadecatriene were found in noncalling females. Wind-tunnel behavioral studies showed that (Z,Z,Z)-3,6,9-nonadecatriene did not elicit any response in the males, and when tested in combination with a mixture of monoepoxynonadecadienes, (Z,Z,Z)-3,6,9-nonadecatriene decreased the observed behavioral responses. A possible precursor role for (Z,Z,Z)-3,6,9-nonadecatriene in the pheromonal system is discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00993751
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  • 95
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    Biological activity and in vivo degradation of tritiated female sex pheromone in the male European corn borer (1992)
    Springer
    Journal of chemical ecology 18 (1992), S. 283-298 
    Details
    ISSN: 1573-1561
    Keywords: Lepidoptera ; Pyralidae ; Ostrinia nubilalis ; European corn borer ; tritiated pheromone ; 11-tetradecenyl acetate ; sensory biochemistry ; catabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Isomers of [11,12-3H2]-11-tetradecenyl acetate (57 Ci/mM) were synthesized. Behavioral assay of the two compounds using Z- and E-type European corn borer (ECB) males showed that introduction of tritons into the double bond of the pheromone caused a significant isotope effect in the E-type ECB but not in the Z-type ECB. Measurements of tritium associated with the male antennae after a 3-min exposure showed that radioactivity equivalent to 10−7 mol pheromone was adsorbed onto male antennae. Time-course in vivo metabolic studies with picogram amounts of compound applied topically to antennae of E- and Z-type males and Z-type females showed that they metabolized pheromone similarly but females degraded pheromone more slowly than males. Pheromone was hydrolyzed, and the only other major radiolabeled metabolite observed by combined high-pressure liquid chromatography-radiodetection was tritiated water. Capillary gas chromatography and radiomonitoring permitted detection of a trace amount of 11-tetradecenoic acid, which indicated alcohol oxidase activity is associated with the antennae. Evidence shows that clearing of pheromone from the ECB male antennae involves hydrolysis and oxidation of the alcohol to fatty acid, which in turn is degraded, probably via β-oxidation, to carbon dioxide and water.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00994232
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  • 96
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    An EPR and molecular mechanics study of radical adducts of phosphonyl radicals with 2-hydroperfluoro-4-methyl-and 4,4-dimethyl-2-pentene (1992)
    Springer
    Russian chemical bulletin 41 (1992), S. 2008-2011 
    Details
    ISSN: 1573-9171
    Keywords: EPR ; radical ; fluorine ; conformation ; phosphorus
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract EPR spectra of radical adducts of phosphonyl radicals with 2-hydroperfluoro-4-methyl- and 4,4-dimethyl-2-pentene have been studied. The molecular mechanics method has been used to determine the preferred conformation of the (CF3)2CF-CF-HCF3P(O)(OMe)2 radical. The eclipsed conformation of the C–P bond and 2p z -orbital of an unpaired electron is stabilized due to steric factor and hyperconjugation.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00863364
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  • 97
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    Pharmacokinetics and cytotoxicity of B.3839, a molecular combination of 5-fluorouracil and N-(2-chloroethyl)-N-nitrosourea, in a mouse model (1992)
    Springer
    Investigational new drugs 10 (1992), S. 149-158 
    Details
    ISSN: 1573-0646
    Keywords: pharmacokinetics ; cytotoxicity ; molecular combination ; fluorouracil ; nitrosourea
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary B.3839 is the prototype compound in a series of novel molecular combinations of chloroethylnitrosoureas and 5-fluorouracil(5-FU) and has been tested against MAC tumours in mice. Previous studies have shown it is moderately active against MAC15A and highly active against MAC13 though this activity is dependent on route of administration. The aim of this study was to determine whether bioavailability could explain this difference in anti-tumour activity. Plasma levels of B.3839 and 5-FU after i.p. and oral administration were measured using HPLC. Non tumour-bearing and MAC26 bearing mice gave almost identical plasma profiles after i.p. administration with the Cmax being 29.8 and 30.4μ gml−1 and t1/2 16 and 15 min. The AUCs were 15.3 and 13.9μg h ml−1 suggesting tumour load had no influence over plasma levels. Oral administration gave a much lower Cmax of 8.0μg ml−1 but an AUC of 15.2μg h ml−1 due to a longer terminal t1/2 (94 min) giving 99% bioavailability. Levels of 5-FU release from B.3839 by either route were considered too small to influence anti-tumour activity. Cytotoxicity assaysin vitro against the MAC lines gave IC70 values of 5.3, 13.8 and 8.6μg ml−1 for MAC 26,13 and 15A respectively after a one hour exposure. Bone marrow toxicity was shown to be less severe than that of TCNU which is currently in clinical trials. The results show bioavailability alone is not enough to explain tumour response. There appears to be a need for a threshold concentration (C) to be maintained for a period of time (t).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00877239
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  • 98
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    Physiological pharmacokinetic parameters for cis-dichlorodiammineplatinum(II) (DDP) in the mouse (1992)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 20 (1992), S. 95-99 
    Details
    ISSN: 1573-8744
    Keywords: pharmacokinetics ; physiological model ; cisplatin ; DDP ; cis-dichlorodiammineplatinum(II)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01143187
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  • 99
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    Evaluation of dose-related pharmacokinetics and pharmacodynamics of prednisolone in man (1992)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 20 (1992), S. 567-589 
    Details
    ISSN: 1573-8744
    Keywords: prednisolone ; pharmacokinetics ; pharmacodynamics ; corticosteroids ; protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics and pharmacodynamics of prednisolone were evaluated in normal male volunteers. Seven subjects completed 3 phases: 16.4−and 49.2−mg iv prednisolone, and a phase with no drug to assess baseline responses. Plasma concentrations of prednisolone and urine concentrations of prednisolone and 5 metabolites were assayed by HPLC. Protein binding of prednisolone was measured by ultrafiltration. The polyexponential disposition of free and total plasma prednisolone were evaluated and apparent parameters were compared between doses. Suppression of plasma cortisol and alterations in blood basophil and helper-T cell trafficking were used as pharmacodynamic indices. Pharmacodynamic models were used to relate total or free plasma prednisolone concentrations to each of these effects generating response parameters and IC50 (50% inhibitory) concentrations common to both doses. The pharmacokinetics of total drug were comparable to previous findings with CLand Vss increasing with dose. Free prednisolone exhibited slight capacitylimited elimination and distribution as CLand Vss decreased with the larger dose. Pharmacodynamic models jointly fitting all three phases characterized the suppression/trafficking phenomena equally well with use of total or free drug concentrations. In each case the models provided realistic values of parameters relating to steroid sensitivity-in particular IC50-and to the underlying physiology of the affected systems. This study comprehensively elucidates the complexities of prednisolone pharmacokinetics and demonstrates how plasma concentration-time profiles of total or free prednisolone can be utilized for evaluation of prednisolone pharmacodynamics.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01064420
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  • 100
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    Algorithms to rapidly achieve and maintain stable drug concentrations at the site of drug effect with a computer-controlled infusion pump (1992)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 20 (1992), S. 147-169 
    Details
    ISSN: 1573-8744
    Keywords: computers ; pharmacokinetics ; pharmacodynamics ; infusions ; drug delivery ; computer driven ; effect site
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Computer-controlled infusion pumps incorporating an internal model of drug pharmacokinetics can rapidly achieve and maintain constant drug concentrations in the plasma. Although these pumps offer more accurate titration of intravenous drugs than is possible with simple boluses or constant rate infusions, the choice of the plasma as the target site is arbitrary. The plasma is not the site of drug effect for most drugs. This manuscript describes two algorithms for calculation of the infusion rates necessary for a computer-controlled infusion pump to rapidly achieve, and then maintain, the desired target concentration at the site of drug effect rather than in the plasma.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01070999
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