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  • pharmacokinetics  (22)
  • Lepidoptera  (14)
  • Scolytidae
  • Springer  (37)
  • 2005-2009
  • 1990-1994  (37)
  • 1980-1984
  • 1965-1969
  • 1993  (37)
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  • Springer  (37)
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  • 2005-2009
  • 1990-1994  (37)
  • 1980-1984
  • 1965-1969
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  • 1
    ISSN: 1573-0646
    Keywords: menogaril ; phase I ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Thirty-five patients with advanced refractory cancer were enrolled on this phase I study of menogaril administered orally every 4 weeks at dosages ranging from 85 mg/m2 to 625 mg/m2. An additional 12 patients received alternating oral and IV doses of menogaril (250 mg/m2 IV; 250–500 mg/m2 oral) with accompanying blood and urine sampling for pharmacokinetics analysis. Nausea and vomiting were the dose-limiting toxicities at the 625 mg/m2 dosage level; vomiting was inadequately relieved by prophylactic antiemetics at this dosage level. Other toxicities included sporadic leukopenia at all dosage levels; at dosages of 500 mg/m2 and 625 mg/m2, leukopenia 〈 3000/μl occurred in 7 of 24 patients. Anemia and thrombocytopenia were much less frequent toxicities. Among the patients receiving IV menogaril, peripheral vein phlebitis, leukopenia and anemia were the predominant toxicities. No antitumor responses were observed, yet one patient with nonsmall cell lung cancer experienced a 30% reduction in metastatic tumor nodules. For the patients receiving alternating oral and IV menogaril, comparative pharmacokinetic analyses were performed by HPLC. After oral administration, maximum plasma concentrations were achieved in an average of 6 hours; maximum plasma concentrations were less than one-quarter of those achieved after intravenous administration. The harmonic mean (±SD) terminal disposition half-life after oral dosing was 29.3 ±9.2 hours; mean systemic bioavailability was 33.6±10.5% after oral dosing. Forty-eight hours after an oral dose, mean cumulative urinary excretions of menogaril and the primary metabolite, N-demethylmenogaril, were 4.00±0.96% and 0.44±0.16%, respectively. Because of the poor tolerance of oral menogaril and minimal evidence of biological activity, this schedule of drug administration is not recommended for phase II evaluation. Based on this and other published studies of oral menogaril, frequent chronic low-intermediate dosages of the drug may be given orally with potentially better tolerance and antitumor activity.
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 45 (1993), S. 431-436 
    ISSN: 1432-1041
    Keywords: Fosinopril ; ACE inhibitors ; haemodialysis ; pharmacokinetics ; pharmacokinetics-pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and pharmacodynamics of fosinoprilat, the diacid of fosinopril sodium (a new angiotensin-converting enzyme (ACE) inhibitor), were investigated in six haemodialysis patients. Intravenous 14C-fosinoprilat (7.5 mg), oral 14C-fosinopril sodium (10 mg) and oral fosinopril sodium (10 mg) were administered in an open-label, randomized study. Mean maximum concentration (Cmax), clearance (CL), volume of distribution at steady-state (Vss), mean residence time (MRTiv), and t1/2 values after IV administration of 14C-fosinoprilat were 2,042 μg·ml−1, 11.3 ml·min−1, 11.01, 16.3 h and 28.3 h, respectively. Following oral administration of 14C-fosinopril, mean Cmax, time to maximum plasma concentration (tmax), and fosinoprilat bioavailability values were 197 ng·ml−1, 5.2 h and 29.2 %. Para-hydroxy fosinoprilat and fosinoprilat glucuronide comprised approximately 15 % and 2 % of radioactivity recovered in faeces. Four hours of haemodialysis only cleared approximately 1.5 % of the administered dose. The maximum effect (Emax) model was fitted to the percentage inhibition of serum ACE activity vs. fosinoprilat concentration data in three patients. Emax ranged from 95.3 to 102.5 %, and IC50 (the fosinoprilat concentration required to produce 50 % of Emax) ranged from 2.6 to 4.2 ng·ml−1. Pharmacokinetic variables of the patients were similar to those in patients with moderate to severe renal dysfunction. Dosage modifications or supplemental dosing following dialysis are unnecessary.
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  • 3
    ISSN: 1432-1041
    Keywords: Felodipine ; Nitrendipine ; Nifedipine ; pharmacokinetics ; stereoselectivity ; enantiomers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of racemic (rac) felodipine, rac-nitrendipine and nifedipine (all given as an oral dose of 20 mg in solution) have been investigated in a randomised cross-over study in 12 healthy male subjects using stereoselective assays. Both felodipine and nitrendipine exhibited stereoselective pharmacokinetics. On average, the AUCs of the active (S)-enantiomers of felodipine and nitrendipine were 139% and 104% higher than those of their optical antipodes, but the elimination half-lives of the enantiomers of each racemate were not different. The AUCs of nifedipine, rac-felodipine, rac-nitrendipine and of their enantiomers were highly correlated (all r〉0.83), suggesting closely related rate limiting steps in the in vivo first-pass metabolism of these high-clearance drugs. Stereoselectivity was only a minor contributor to inter-individual variability in the oral pharmacokinetics of these compounds in healthy subjects.
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  • 4
    ISSN: 1432-1041
    Keywords: Terfenadine metabolism ; cimetidine ; ranitidine ; antihistamines ; Torsades de Pointes ; pharmacokinetics ; drug interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Terfenadine is a widely prescribed non-sedating antihistamine which undergoes rapid and almost complete first pass biotransformation to an active carboxylic acid metabolite. It is unusual to find unmetabolised terfenadine in the plasma of patients taking the drug. Terfenadine in vitro is a potent blocker of the myocardial potassium channel. Overdose, hepatic compromise and the coadministration of ketoconazole and erythromycin result in the accumulation of terfenadine, which is thought to be responsible of QT prolongation and Torsades de Pointes ventricular arrhythmia in susceptible individuals. Cimetidine and ranitidine are two popular H2 antagonists which are often taken with terfenadine. The effects of cimetidine and ranitidine on terfenadine metabolism were studied in two cohorts of 6 normal volunteers given the recommended dose of terfenadine (60 mg every 12 h) for 1 week prior to initiation of cimetidine 600 mg every 12 h or ranitidine 150 mg every 12 h. Pharmacokinetic profiles and morning pre-dose electrocardiograms were obtained whilst the patients were on terfenadine alone and after the addition of cimetidine or rantidine. One of the subjects in each cohort had a detectable plasma level of parent compound after 1 week of terfenadine therapy alone; it did not accumulate further after addition of the H2 antagonist. The pharmacokinetics of the carboxylic acid metabolite of terfenadine (Cmax, tmax, AUC) were not significantly changed after co-administration of either H2 antagonist. None of the remaining 5 subjects in either cohort demonstrated accumulation of unmetabolised terfenadine after addition of the respective H2 antagonist and electrocardiographic QT intervals and T-U morphology in them was not changed during the course of the study. We conclude that cimetidine and ranitidine in the dosages used in this study did not affect the metabolism of terfenadine, and that patients exposed to these drug combinations are not at increased risk of altered cardiac repolarisation.
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  • 5
    ISSN: 1573-1561
    Keywords: Semiochemicals ; pheromones ; Dryocoetes confusus ; Dryocoetes affaber ; Coleoptera ; Scolytidae ; enantiomers ; diastereoisomers ; exo-brevicomin ; endo-brevicomin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract In a field-trapping experiment, western balsam bark beetles,Dryocoetes confusus Swaine, were highly attracted to a 5∶1 mixture of (±)-exo-and (±)-endo-brevicomin. Beetles in the sympatric speciesD. affaber (Mann.), were best attracted to a 1∶1 blend of these semiochemicals [either (±)∶(±) or (±)∶(±)], suggesting that both geometrical isomers are pheromone components in these species. In laboratory bioassays and further field experiments, attraction ofD. confusus was greatest when the (+) enantiomers of both geometrical isomers of brevicomin were presented in a 9∶1 ratio. Responses by maleD. confusus to attractive mixtures were reduced in the presence of (−)-exo-brevicomin. Exploitation of the complete range of variability in pheromone structure (both geometrical and optical isomerism) would allow for optimization and regulation of response levels within a species and also could maintain reproductive isolation among sympatric congeneric species primarily through production and response to species-specific blends.
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  • 6
    ISSN: 1573-1561
    Keywords: Eldana saccharina ; Lepidoptera ; Pyralidae ; exocrine secretions ; sex pheromone ; aggregation pheromone ; electroantennograms ; electroantennographic detection ; NMR
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract In addition totrans-3,7-dimethyl-6-octen-4-olide (eldanolide), vanillin, and 4-hydroxybenzaldehyde, identified by French workers in the wing gland and abdominal hair pencil secretions of the male African sugarcane borer,Eldana saccharina, we have, in an earlier note, reported the presence of several other terpenoid, aromatic, and unbranched-chain compounds such as, (Z)-3,7-dimethylocta-2,6-dienoic acid, 6,10,14-trimethyl-2-pentadecanol, 4-hydroxy-3-methoxybenzyl alcohol, 1-octadecane thiol, 16-hexadecanolide, and 18-octadecanolide in these secretions. In the present paper experimental details and spectral evidence supporting the identification of these compounds, as well as the identification of (Z)-9-hexadecenal and cw-3,7-di-methyl-6-octen-4-olide (cis-eldanolide), are reported. Using electroantennography it was found that male and female antennae reacted approximately equally strongly to both secretions. This result was confirmed in analyses of the secretions using coupled gas chromatography-electroantennography and it was found that male as well as female antennae responded to eldanolide. Vanillin, substituted phenols related to vanillin, and some oxygenated monoterpenes elicited weak responses in male and female antennae. In some analyses 6,10,14-trimethyl-2-pentadecanol, present in the secretions of the insect, gave a strong antennal response. The results obtained in dynamic and static headspace determinations showed that several of the organic compounds present in the glandular secretions are released in detectable quantities and are present in widely varying quantitative ratios in the effluvia of individual calling male moths.
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  • 7
    ISSN: 1573-1561
    Keywords: Lepidoptera ; Pyralidae ; Phycitinae ; Hulstia undulatella ; sex pheromone ; (Z)-9-tetradecen-1-ol acetate ; (Z)-9-tetradecen-1-ol ; (Z)-11-hexa-decen-1-ol acetate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Electroantennogram profiles of saturated and monounsaturated 12-, 14-, and 16-carbon acetates, and 12- and 14-carbon alcohols implicated (Z)-9-tetradecen-1-ol acetate (Z9-14: Ac) as a component of the female sex pheromone ofHulstia undulatella (Clemens). Gas chromatography-mass spectrometric analysis of extract of the female sex pheromone glands showed the presence of Z9-14:Ac (8.5 ng/female), (Z)-9-tetradecen-1-ol (Z9-14:OH), and (Z)-11-hexadecen-1-ol acetate (Z11-16:Ac) in a ratio of 100∶4∶21, respectively. In tests in sugar beet fields, Z9-14:Ac alone produced some trap catch. Addition of Z9-14: OH did not increase catch while addition of Z11-16:Ac eliminated catch, but addition of both Z9-14:OH and Z11-16: Ac increased catch sevenfold. A combination of Z9-14: OH and Z11-16: Ac without Z9-14: Ac did not produce trap catch. A lure of 200 μg Z9-14:Ac+16 μg Z9-14:OH+42 μg Z11-16:Ac is suggested for use in monitoring traps.
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Entomologia experimentalis et applicata 67 (1993), S. 57-64 
    ISSN: 1570-7458
    Keywords: Cydia pomonella ; codling moth ; mating disruption ; (E,E)-8,10-dodecadien-1-ol ; pheromones ; apple ; Lepidoptera ; Tortricidae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Polyethylene dispensers (Shin Etsu) containing 172 ml of the sex pheromone, (E, E)-8,10-dodecadien-1-ol (63%), dodecenol (31%) and tetradecenol (6%), of codling moth (CM),Cydia pomonella (L.), were placed in apple orchards in Virginia. Two blocks of about 2 ha each were treated in 1989, and three in 1990. Dispensers were placed in trees at a density of 1000/ha shortly after apple bloom. Male orientation to pheromone traps was almost totally disrupted (a few males were captured at high population densities). In 1989, the Daleville pheromone-treated block had 0.9% and 0.8% CM-injured fruit in the center and edge, respectively; 0% and 39.5% injured fruit were found in the conventional control and abandoned blocks, respectively. The Criglersville orchard (‘organically’ managed, with high CM density) CM harvest injury was 16.0%, 16.5%, 34.5%, and 26.5% in the pheromone-treated center and edge, organic control and abandoned blocks, respectively. In 1990, the Daleville CM harvest injury was 4.7%, 7.3%, 1.1%, 0.3% and 58%, in the pheromone-treated center and edge, control center and edge, and abandoned blocks, respectively (possible reasons for the high injury in this block are discussed). Harvest injury in the Fincastle pheromone-treated and control blocks were 0.7% and 0%, respectively. The Criglersville orchard yielded 17%, 19% and 20% CM-injured fruit at harvest in the pheromone-treated, organic control and abandoned blocks, respectively. Pheromone release rate was calculated as 37 mg/ha/h in 1989.
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Entomologia experimentalis et applicata 67 (1993), S. 47-56 
    ISSN: 1570-7458
    Keywords: Platynota flavedana ; variegated leafroller ; Platynota ideausalis ; tufted apple bud moth ; Argyrotaenia velutinana ; redbanded leafroller ; mating disruption ; pheromones ; apple ; Lepidoptera ; Tortricidae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Mating disruption for control of variegated leafroller (VLR),Platynota flavedana (Clemens), tufted apple bud moth (TBM),P. ideausalis Walker, and redbanded leafroller (RBL),Argyrotaenia velutinana (Walker), was studied in Virginia apple orchards in 1989 and 1990. In 1989, each dispenser (1000/ha) contained 190 mg of 67.2%E11–14:Ac, 28.8%Z11–14:Ac, 1.4%E11–14:OH, 0.6%Z11–14:OH, and 2%Z9–12:Ac (a putative generic leafroller disruption blend). Trap captures of VLR, TBM and RBL were reduced by 97%, 51% and 55%, respectively. Average leafroller injury in the interior and edge of the pheromone block was 3.8% and 2.7%, respectively. The conventional control and abandoned blocks had 0.05 and 27.5% injury, respectively. Dispensers containingE11–14:OH (70%) andZ11–14:OH (30%) (close to the natural blend of VLR), more effectively disrupted orientation to pheromone traps by bothPlatynota spp. than did the generic blend. In 1990, dispensers containing 150 mg ofE11–14:OH (70%) andZ11–14:OH (1000/ha) were placed in two 2-ha blocks and one 4-ha block. One pheromonetreated block was sprayed in August with phosmet for codling moth, not timed for leafrollers. Trap captures of VLR and TBM were reduced by almost 100% and 69%, respectively. RBL captures were not reduced by VLR pheromone permeation. Injury fromPlatynota spp. in pheromone block middles and edges ranged from 0.3–1.7% and 0.3–2.3%, respectively. Injury in conventional blocks ranged from 0–1.1%. RBL injury in pheromone block middles ranged from 0–6.1%, and in edges, 1.7–4.8%. Injury in control blocks ranged from 0–1.1%. Combined leafroller injury in an abandoned block was 18% (s.e. 0.3). Release rates averaged 30 and 32 mg/ha/h for the VLR and generic pheromone dispensers, respectively.
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 49 (1993), S. 998-1001 
    ISSN: 1420-9071
    Keywords: Lepidoptera ; Tortricidae ; synomone ; pheromone ; behavior ; oviposition ; Lobesia botrana ; Cydia pomonella ; Cydia molesta ; Eupoecilia ambiguella ; fatty acids ; esters of fatty acids
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Oviposition of four tortricid pests of vineyards (the European grapevine moth and the grape berry moth) and fruit orchards (the codling moth and the oriental fruit moth) is deterred by a blend of straight chain fatty acids and esters of fatty acids that have been identified in the eggs of one of them: the European grapevine moth (EGVM)Lobesia botrana. This is the first evidence of inter-specific recognition of an egg-like signal in moths. We demonstrate that oviposition site selection is influenced by population density, avoidance of deterrent being most important when females are isolated. Inter-specific egg recognition might be an important phenomenon, especially in species competing for a common food resource. We propose the term ‘oviposition regulating synomone’ for molecules and blends that affect the inter-specific spacing of eggs.
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