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  • Coleoptera  (25)
  • healthy volunteers  (17)
  • Springer  (42)
  • American Meteorological Society
  • 1980-1984  (42)
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  • Springer  (42)
  • American Meteorological Society
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  • 1
    Electronic Resource
    Electronic Resource
    Studies of the different metabolic pathways of antipyrine in man (1982)
    Springer
    European journal of clinical pharmacology 21 (1982), S. 433-441 
    Details
    ISSN: 1432-1041
    Keywords: antipyrine ; antipyrine metabolites ; drug metabolism ; route of administration ; healthy volunteers ; urinary excretion ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of antipyrine in plasma and saliva, and urinary excretion of its major metabolites, were studied following i.v. and oral administration of antipyrine 500 mg to 6 healthy volunteers. Data from both plasma and saliva showed that the oral bioavailability of antipyrine given as an aqueous solution was complete. The saliva/plasma concentration ratio was constant with time from about 3 h onwards, with a mean value of 0.87 after oral and 0.91 after i.v. administration. It is concluded that the pharmacokinetic parameters of antipyrine can be satisfactorily established on the basis of salivary data, although the volume of distribution and clearance values are then slightly too high. After i.v. administration, 3.8±1.9% of the dose was excreted in urine as unchanged antipyrine in 48h, 24.9±6.3% as 4-hydroxyantipyrine, 16.5±3.2% as norantipyrine, 13.0±2.2% as 3-hydroxymethyl-antipyrine and 5.8±1.0% as 3-carboxy-antipyrine. No significant differences were observed following oral administration. The half-lives calculated from the linear part of the urinary excretion rate curves of the metabolites were about the same for oral and i.v. administration, and were of the same order of magnitude as the elimination half-life of parent drug in plasma and saliva. It is important for determination of the ultimate metabolite ratio that urine is collected for at least 36h, because there is a delay in the excretion of 3-hydroxymethyl-antipyrine in urine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542332
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  • 2
    Electronic Resource
    Electronic Resource
    Influence of alaproclate on antipyrine metabolite formation in man (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 447-452 
    Details
    ISSN: 1432-1041
    Keywords: alaproclate ; antipyrine clearance ; serotonin reuptake inhibitor ; healthy volunteers ; antipyrine metabolism ; metabolite clearance ; alaproclate kinetics ; inhibition of drug metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Alaproclate, a selective serotonin reuptake inhibitor, presently undergoing clinical trial for the treatment of major depressive disorders, has been shown to inhibit hexobarbital metabolism in mice. In the present study the influence of oral alaproclate on the total plasma clearance of antipyrine and on the formation of its metabolites was investigated in 10 healthy volunteers. The peak level of alaproclate was reached after about 1.5 h, and after a distribution phase, its plasma elimination half-life was between 3.0 and 3.5 h. Antipyrine tests were performed before treatment, during the first four doses and after the seventh dose of alaproclate 200 mg/day. During treatment, total plasma antipyrine clearance and the clearance for production of all antipyrine metabolites were reduced by 30%, indicating non-selective inhibition of oxidative drug-metabolizing enzyme activity in man by alaproclate. After the last dose of alaproclate, antipyrine plasma clearance and the clearance to its metabolites returned to control values. In order to allow more detailed evaluation of the results, the time course of the clearances for production of metabolites was investigated. This revealed that the extent of inhibition of metabolite formation by alaproclate was dependent on the plasma alaproclate level, indicating a rapidly reversible inhibition.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00549593
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  • 3
    Electronic Resource
    Electronic Resource
    Ecdysteroids during pupal development of female Xyleborus ferrugineus (1981)
    Springer
    Entomologia experimentalis et applicata 30 (1981), S. 151-156 
    Details
    ISSN: 1570-7458
    Keywords: Xyleborus ferrugineus ; pupae ; ecdysteroids ; pharate adult ; radioimmunoassay ; Coleoptera ; Scolytidae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Description / Table of Contents: Zusammenfassung Der Ecdysteroidtiter weiblicher Puppen von Xyleborus ferrugineus (Fabr.) wurde geschätzt, indem ganze Tiere homogenisiert und radioimmunologisch untersucht wurden. Ein ausgeprägtes Maximum an Ecdysteroiden wurde bei 36 Stunden Puppenent-wicklung beobachtet (743 pg/mg Körpergewicht). Der Titer nahm ab auf 299 pg/mg im Pharatstadium und auf 193 pg/mg unmittelbar vor Schlüpfen der Adulten. Qualitative Studien mit HPLC ergaben in frischen Puppen ein Verhältnis von 3:1 Ecdyson zu 20-Hydrooxyecdyson. Pharatstadien enthielten vor allem 20-Hydrooxyecdyson. Das beobachtete einzige Maximum im Titer stimmt überein mit den Resultaten bei andern untersuchten Coleopteren.
    Notes: Abstract Ecdysteroid titers were estimated on the whole body homogenates of Xyleborus ferrugineus (Fabr.) female pupae during development by radioimmunoassay. A distinct peak of ecdysteroids was observed at 36-hr pupal development (743 pg/mg body wt). Titer declined to 299 pg/mg by the pharate adult stage and to 193 pg/mg body wt just before adult emergence. Qualitative studies by HPLC revealed a ratio of 3:1 ecdysone to 20-hydroxyecdysone in the initial pupal stage. Pharate adults had mainly 20-hydroxyecdysone. The observed single peak in ecdysteroid titer agrees with findings in other studied coleopteran species.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00300880
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  • 4
    Electronic Resource
    Electronic Resource
    Defensive adaptations of eggs and adults ofGastrophysa cyanea (Coleoptera: Chrysomelidae) (1982)
    Springer
    Journal of chemical ecology 8 (1982), S. 453-462 
    Details
    ISSN: 1573-1561
    Keywords: Defensive secretions ; oleic acid ; hydrocarbons ; terpenoids ; eggs ; deterrents ; ants ; predation ; Chrysomelidae ; Coleoptera ; Gastrophysa cyanea ; reflex bleeding ; elytral glands
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Egg clusters and adults ofGastrophysa cyanea are conspicuous and, like their larvae, are chemically protected. The eggs owe their bright yellow color primarily to β-carotene and, in addition, contain substantial quantities of oleic acid. At natural concentrations oleic acid effectively deters many species of ants from feeding. The use of fatty acids as deterrents against ants is discussed as a possible widespread phenomenon among insects. During defensive confrontations, adults ofG. cyanea exhibit avoidance behavior and may also feign death. In addition, the adults may autohemmorhage or secrete a fluid from elytral or pronotal pores in response to traumatic stimuli. The secretions are effective against ants and contain a mixture of hydrocarbons as well as terpenoid components. The pattern of ontogenetic modification in the defensive chemical repertoire ofG. cyanea is discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00987793
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  • 5
    Electronic Resource
    Electronic Resource
    Pheromone production by axenically rearedDendroctonus ponderosae andIps paraconfusus (Coleoptera: Scolytidae) (1984)
    Springer
    Journal of chemical ecology 10 (1984), S. 281-290 
    Details
    ISSN: 1573-1561
    Keywords: Dendroctonus ponderosae ; Ips paraconfusus ; Coleoptera ; Scolytidae ; axenic rearing ; monoterpenes ; aggregation pheromones ; trans-verbenol ; exo-brevicomin ; ipsenol ; ipsdienol
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Mountain pine beetles,Dendroctonus ponderosae Hopkins, and California five-spined ips,Ips paraconfusus Lanier, were reared axenically from surface-sterilized eggs on aseptic pine phloem. After 24 hr in host logs, axenip femaleD. ponderosae and maleI. paraconfusus produced the aggregation pheromones,trans-verbenol (D. ponderosae), and ipsenol and ipsdienol (I. paraconfusus). Emergent, axenically reared maleD. ponderosae contained normal amounts of the pheromoneexo-brevicomin. Axenic femaleD. ponderosae treated with juvenile hormone or exposed to vapors of α-pinene, produced the pheromonetrans-verbenol. By 25–35 days after eclosion, axenic females exposed to α-pinene vapors produced over six times as muchtrans-verbenol as wild females, suggesting that while microorganisms in wild females may producetrans-verbenol, they may also inhibit production of the pheromone or use it as a substrate.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00987856
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  • 6
    Electronic Resource
    Electronic Resource
    Effect of dose on bioavailability of oral digoxin (1981)
    Springer
    European journal of clinical pharmacology 19 (1981), S. 53-55 
    Details
    ISSN: 1432-1041
    Keywords: digoxin ; bioavailability ; dose-dependency ; urinary excretion ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Nine healthy volunteers received single 0.25, 0.5, 1.0, 1.5, and 2.0 mg doses of oral digoxin tablets in random sequence on five occasions separated by at least 4 weeks. Urinary excretion of immunoassayable digoxin was determined from 8 consecutive 24 h urine samples collected after each dose. Mean values of cumulative urinary excretion of digoxin at the 5 doses were: 40.9, 35.6, 36.4, 34.1, and 33.5% of the dose (F=0.64; d. f.=4.32; N. S.). Mean values of urinary excretion half-life were: 2.48, 2.03, 2.20, 2.07, and 1.87 days (F=2.87; d. f.=4.32;p=0.05). Thus, the bioavailability of orally administered digoxin tablets in healthy volunteers is dose-independent over an 8-fold range of doses.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558384
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  • 7
    Electronic Resource
    Electronic Resource
    Pharmacokinetics in man of a new antiarrhythmic drug, cibenzoline (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 509-515 
    Details
    ISSN: 1432-1041
    Keywords: cibenzoline ; pharmacokinetics ; bioavailability ; urinary excretion ; antiarrhythmic drug ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of cibenzoline (UP 339.01), a new antiarrhythmic drug, was studied after i.v. and oral administration to 5 healthy subjects. Cibenzoline levels in plasma and urine cibenzoline were measured by a GLC method. After i.v. administration, the total clearance was 826 ml · min−1. The fraction of cibenzoline excreted unchanged in the urine was 0.602 and it was correlated with the creatinine clearance. After i.v. and oral administration, the renal clearances were 499 ml · min−1 and 439 ml · min−1, and the half-lives were 4 h 01 min and 3 h 24 min, respectively. The differences were not significant. Availability by the oral route was 0.92, the maximum plasma concentration being observed at 1 h 36 min. The results were compared with those for other antiarrhythmic drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609894
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  • 8
    Electronic Resource
    Electronic Resource
    Effects of acute administration of zetidoline, a new antidopaminergic drug, on plasma prolactin and aldosterone levels in man (1984)
    Springer
    European journal of clinical pharmacology 26 (1984), S. 29-32 
    Details
    ISSN: 1432-1041
    Keywords: zetidoline ; prolactin ; aldosterone ; dopamine ; healthy volunteers ; pharmacodynamic effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The neuroendocrinological effects of acute oral administration of 20 mg zetidoline, a new antipsychotic drug with antidopaminergic properties, were evaluated in 8 healthy volunteers, by a double-blind, crossover comparison with placebo. Zetidoline significantly increased serum prolactin (p〈0.01 at 1–3 h; p〈0.05 at 4–6 h). No significant change was observed in blood levels of aldosterone, renin, cortisol, growth hormone and electrolytes, or in blood pressure and heart rate. The data suggest that the drug increases prolactin through blockade of dopaminergic receptors. The lack of change in the aldosterone levels may be evidence against the hypothesis of dopaminergic control of aldosterone secretion.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00546704
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  • 9
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of canrenone and metabolites after base hydrolysis following single and multiple dose oral administration of spironolactone (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 441-446 
    Details
    ISSN: 1432-1041
    Keywords: spironolactone ; canrenone ; metabolites ; pharmacokinetics ; single/multiple oral doses ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of canrenone and ‘total metabolites’ after base hydrolysis was studied in eight young volunteers following single and multiple dose oral administration of spironolactone. The plasma levels of canrenone and ‘total metabolites’ were fitted to a two-compartment open model with a first-order absorption process. From our eight normal subjects studied, the harmonic mean of the distributive half-life (t1/2α) of canrenone was found to be 1.66 h, and the harmonic mean of the terminal elimination half-life (t1/2β) to be 22.6 h. Harmonic means of the distributive and elimination half-lives of ‘total metabolites’ after base hydrolysis were 2.48 h and 28.8 h respectively. The accumulation ratio of canrenone was 2.53, whereas that of ‘total metabolites’ was 1.89. Despite the fact that spironolactone has been shown to induce hepatic metabolism of other drugs, no evidence of autoinduction was noted in the present study, as plasma levels of canrenone and ‘total metabolites’ were found to obey a linear two-compartment model with reproducible absorption and disposition after single and multiple doses.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00549592
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  • 10
    Electronic Resource
    Electronic Resource
    Evaluation of a radioreceptor assay for beta-adrenoceptor antagonists in plasma (1980)
    Springer
    European journal of clinical pharmacology 17 (1980), S. 349-354 
    Details
    ISSN: 1432-1041
    Keywords: propranolol ; radioreceptor assay ; beta-adrenoceptor antagonists ; lung membranes ; plasma level ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A radioreceptor assay (RRA) recently developed in this laboratory for beta-adrenoceptor antagonists in plasma was evaluated in normal volunteers and compared with a radioimmunoassay (RIA) for propranolol. The RRA depends upon the ability of beta-adrenoceptor antagonists to compete with a radiolabelled ligand for beta-adrenoceptor binding sites on lung membranes. Unlike other assays, it measures biologically active drugs including active metabolites of the parent compound. In volunteers given a single oral dose of (±)-propranolol, considerable differences between the two assay methods were demonstrated. In other experiments this difference was shown to relate to the RIA's sensitivity to the inactive (+)-isomer of propranolol and possibly to inactive metabolites. The facility of the RRA in measuring plasma levels of several other non-selective beta-adrenoceptor antagonists was also demonstrated. By employing (−)-propranolol as the standard in the RRA, all of these drugs can be directly compared with a single and relatively simple assay technique.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558447
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