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  • pharmacokinetics  (261)
  • Lepidoptera  (124)
  • Springer  (385)
  • American Chemical Society
  • Blackwell Publishing Ltd
  • Elsevier
  • 1985-1989  (385)
  • 1960-1964
  • 1955-1959
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  • Springer  (385)
  • American Chemical Society
  • Blackwell Publishing Ltd
  • Elsevier
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  • 1
    Electronic Resource
    Electronic Resource
    Renal excretion and pharmacokinetics of methotrexate and 7-hydroxy-methotrexate following a 24-h high dose infusion of methotrexate in children (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 231-238 
    Details
    ISSN: 1432-1041
    Keywords: methotrexate ; hydroxymethotrexate ; lymphoid malignancy ; renal excretion ; metabolism ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In children with lymphoid malignancies 18 courses of methotrexate (18–200 mg/kg) administered as a 24-h infusion were monitored. Plasma concentrations and renal excretion rates of methotrexate (MTX) and 7-hydroxymethotrexate (7-OHMTX) were determined. A low correlation was found between the administered dose of MTX and the body exposure to MTX or 7-OHMTX. Although 84% of the MTX eventually recovered from the urine was excreted during the 24 h of the infusion, the renal clearance of MTX was markedly lower during the time of the infusion than after it. There were courses with a low and others with a high renal clearance of MTX during the infusion, despite the same urine flow. A low MTX renal clearance was correlated with a high body exposure to MTX. As the same variations were also seen in the same patient during successive courses, pharmacokinetical characterization of patients appears questionable. The renal clearance of 7-OHMTX was significantly lower than the renal clearance of MTX, and the body exposure to 7-OHMTX ranged from 2–40% of the MTX body exposure. Treatment courses with a low or a high body exposure to 7-OHMTX were not associated with different urinary recoveries of the metabolite. Differences in MTX hydroxylation could not be substantiated. Because the concentration of 7-OHMTX is high soon after the end of an infusion, a specific method of MTX determination should be chosen for controlling treatment.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614310
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  • 2
    Electronic Resource
    Electronic Resource
    Alteration by burn injury of the pharmacokinetics and pharmacodynamics of cimetidine in children (1989)
    Springer
    European journal of clinical pharmacology 36 (1989), S. 361-367 
    Details
    ISSN: 1432-1041
    Keywords: cimetidine ; burned children ; stress ulceration ; pharmacokinetics ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have studied the mechanisms of the increased dosage requirements of the H2-receptor antagonist cimetidine in paediatric burned patients in a pharmacokinetic and pharmacodynamic study. Cimetidine (10–15 mg·kg−1) was given to 21 burned children and multiple blood samples were obtained for determination of plasma cimetidine concentrations and pharmacokinetic analysis. The relation of gastric pH to plasma cimetidine concentrations was studied in five of these children who had nasogastric tubes. In an additional four patients the effects of cimetidine on gastric pH were studied during a continuous infusion of cimetidine, which maintained steady-state plasma cimetidine concentrations above 0.5 µg·ml−1. The mean (SEM) clearance of cimetidine in burned children was 16.22 ml·kg−1 and cimetidine half-life was 1.06 h. The cimetidine clearance and half-life values were significantly higher in burned children compared with our previously reported values for normal adult patients, 8.2 ml·min·kg−1 and 2.21 h respectively. Endogenous creatinine clearance normalized to 70 kg in burned children was 190 ml·min−1. In burned children 41% of the dose of intact cimetidine was excreted during 8 h of the study compared with 45% excretion during 24 h in healthy adult controls previously reported. The correlation coefficient between creatinine and cimetidine clearances was 0.93 (r 2=0.85). The plasma concentration of cimetidine needed to increase gastric pH to ≥4.0 was ≥1.0 µg·ml−1, which contrasts with the value of 〉0.5 µg·ml−1 required for adult burned patients. These findings support the hypothesis that the higher dosage requirements of cimetidine in burned children is due both to enhanced elimination kinetics and to alterations in target organ sensitivity, requiring higher than normal plasma concentrations for the desired effect. In burned children Cimetidine should be given in higher doses and/or more frequently.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558296
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  • 3
    Electronic Resource
    Electronic Resource
    The effects of age and chronic liver disease on the elimination of temazepam (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 93-97 
    Details
    ISSN: 1432-1041
    Keywords: temazepam ; liver disease ; elimination ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of the newer 1, 4 benzodiazepine temazepam were evaluated in 16 healthy subjects aged 18–92 years and in 15 cirrhotic patients, to ascertain the effect of ageing and liver disease. The data were analysed both by classic two compartment and by non-compartmental methods. The mean elimination half-life in the control subjects was 15.5 h, considerably longer than previous estimates. No correlation was found between age and pharmacokinetic parameters. The cirrhotic group showed no statistically significant difference in the pharmacokinetic parameters nor in the urinary recovery of the dose from the control group. Temazepam plasma protein binding was assessed in a second group of 9 cirrhotics of similar severity to the main group and in matched controls. When these binding data were applied to the mean clearance data, a modest although not statistically significant, reduction in free drug clearance was observed in the cirrhotic group. This study adds further support to the observation that drugs which undergo ether glucuronidation have normal elimination patterns in patients with liver disease. Temazepam may prove to be a useful hypnotic sedative in patients with liver disease.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614203
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  • 4
    Electronic Resource
    Electronic Resource
    Antifeedant and insecticidal properties of azadirachtin to the European Corn Borer, Ostrinia nubilalis (1985)
    Springer
    Entomologia experimentalis et applicata 38 (1985), S. 29-34 
    Details
    ISSN: 1570-7458
    Keywords: European corn borer ; Ostrinia nubilalis ; Pyralidae ; Lepidoptera ; azadirachtin ; antifeedant ; botanical insecticide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Description / Table of Contents: Résumé On a examiné les propriétés anti-appétantes et insecticides de l'azadirachtine, une substance triterpénoïde provenant d'Azadirachta indica envers la pyrale du maïs Ostrinia nubilalis. La concentration effective pour causer 50% d'inhibition de l'alimentation larvaire (PC50) sur des disques foliaires a été de 3.5 ppm pour les larves de premier stade et de 24 μg/8 pour celle de troisième stade. L'azadirachtine a sévèrement réduit la croissance larvaire à des concentrations de 1 et 10 ppm dans une diète méridique et, éventuellement, a causé 100% de mortalité à 10 ppm et 90% à 1 ppm. A 0.1 ppm l'azadirachtine n'a pas eu d'effet significatif sur les larves maïs a modifié l'indice de masculinité en faveur des mâles au moment de l'émergence et a empêché l'oviposition chez les femelles. Les indices nutritionnels pour les larves naïves de troisième âge et celles ayant subi une accoutumance suggèrent que la réduction de croissance est le résultat d'une intoxication comme le démontre une efficacité réduite de transformation chez les groupes traités à l'azadirachtine, plutôt que des changements de digestibilité. Il n'y a pas d'évidence claire de tolérance dans le groupe ayant subi l'accoutumance. Les résultats suggèrent qu'à 10 ppm l'azadirachtine est un insecticide botanique efficace envers O. nubilalis.
    Notes: Abstract Azadirachtin, a triterpenoid substance from the neem tree, Azadirachta indica A. Juss., Meliaceae, was evaluated for its antifeedant and insecticidal properties to the European corn borer Ostrinia nubilalis Hübner. The 50% protective concentration for larval feeding on treated corn disks (PC50) was 3.5 ppm for neonate larvae and 24 ppm for third instar larvae. Azadirachtin severely reduced larval growth at 1 and 10 ppm in a meridic diet and eventually caused 100% mortality at 10 ppm and 90% at 1 ppm. At 0.1 ppm azadirachtin showed no significant effect on larvae but altered the sex ratio in favor of male moths during adult emergence and arrested oviposition of female moths. Nutritional indices for naive and habituated third instar larvae suggested that reduction of growth was due to toxicity as shown by a lowered efficiency of conversion in the azadirachtin treated groups, rather than changes in digestibility. No clear evidence of tolerance was observed in the habituated group. The data suggest that at 10 ppm azadirachtin is an effective botanical insecticide for control of O. nubilalis.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00163349
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  • 5
    Electronic Resource
    Electronic Resource
    Discovery of novel avermectins with unprecedented insecticidal activity (1989)
    Springer
    Cellular and molecular life sciences 45 (1989), S. 315-316 
    Details
    ISSN: 1420-9071
    Keywords: 4″-Amino-4″-deoxyavermectins ; avermectin ; insecticide ; Lepidoptera
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary A new class of insecticidal and antiparasitic agents, 4″-amino-4′-deoxy avermectins, has been developed by chemical modification of avermectin B1. The most effective of these compounds are 1500-fold more potent than avermectin B1 (abamectin) against the beet armywormSpodoptera exigua and show similar potency against other lepidopteran larvae.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01951823
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  • 6
    Electronic Resource
    Electronic Resource
    Doxazosin in patients with hypertension (1988)
    Springer
    European journal of clinical pharmacology 35 (1988), S. 21-24 
    Details
    ISSN: 1432-1041
    Keywords: doxazosin ; hypertension ; alpha-adrenergic blockade ; bioavailability ; pharmacokinetics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The antihypertensive effects and steady-state pharmacokinetics of doxazosin, as well as the bioequivalence of four dosage forms, were studied in 25 hypertensive patients. For an 8 mg daily dose mean Cmax at steady-state for all patients was 108 ng/ml; the mean tmax was 1.8 h. The mean terminal elimination half-life was 22 h. The four tablets containing 1, 2, 4, or 8 mg of doxazosin were bioequivalent in delivering the 8 mg dose. In patients with mild to moderate hypertension, 26-day treatment with doxazosin resulted in blood pressure reduction of 10/7 mm Hg in the supine and 13/18 mm Hg in the standing position. Adverse effects were generally mild and of brief duration.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00555502
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  • 7
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of phenylethylmalonamide (PEMA) in elderly men (1987)
    Springer
    European journal of clinical pharmacology 33 (1987), S. 431-434 
    Details
    ISSN: 1432-1041
    Keywords: phenylethylmalonamide ; pharmacokinetics ; elderly
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of phenylethylmalonamide (PEMA) were studied in 6 elderly men after oral administration of a single 400 mg dose. Peak PEMA serum levels were obtained within 4 h of intake, half-life values ranged from 30.7–57.9 h in these elderly men. The elimination half-life was twice as long when compared to a study previously performed in young volunteers.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00637644
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  • 8
    Electronic Resource
    Electronic Resource
    Paracetamol disposition and metabolite kinetics in patients with chronic renal failure (1989)
    Springer
    European journal of clinical pharmacology 36 (1989), S. 291-297 
    Details
    ISSN: 1432-1041
    Keywords: paracetamol ; renal failure ; drug disposition ; polar metabolites ; cumulation ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The disposition of paracetamol following an oral dose of 1.0 g was compared in 10 healthy volunteers, 7 patients with moderate chronic renal failure and 6 patients with end stage renal failure on maintenance haemodialysis. Paracetamol absorption was normal in the patients with renal failure. The mean plasma half-life of paracetamol from 2 to 8 h was similar in the 3 groups (2.1 to 2.3 h) but from 8 to 24 h it disappeared much more slowly in the renal failure patients (half-life 11.7 compared with 4.9 h in the healthy volunteers). Plasma concentrations of paracetamol glucuronide and sulphate conjugates were greatly increased in the patients with moderate renal failure and the mean plasma half-lives were 30.5 and 21.8 h respectively compared with about 3 h in the healthy volunteers. Plasma concentrations of these metabolites were even higher in the dialysis patients and there was no significant fall over 24 h. The cysteine and mercapturic acid conjugates of paracetamol could only be measured in plasma in the patients with renal failure and concentrations were very low. The fractional urinary recovery of paracetamol and its glucuronide, sulphate, cysteine and mercapturic acid conjugates was similar in healthy volunteers and patients with moderate renal failure. The mean renal clearances of paracetamol and its glucuronide and sulphate conjugates in the healthy volunteers and patients with moderate renal failure were 15.7, 137 and 172, and 5.9, 14.5 and 14.8 ml/min respectively. In the latter patients the mean renal clearances of the cysteine and mercapturic acid conjugates were much greater at 35.4 and 80.2 ml/min. In the patients with moderate renal failure the AUC's of the glucuronide and sulphate conjugates were related to the plasma creatinine and there were significant negative correlations with the renal clearances of these metabolites and total urinary recovery. Marked cumulation of the polar glucuronide and sulphate conjugates of paracetamol would seem inevitable in patients with renal failure and the parent drug is apparently regenerated to a limited extent from retained metabolites.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558162
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  • 9
    Electronic Resource
    Electronic Resource
    Almitrine bismesylate disposition in the human digestive tract (1989)
    Springer
    European journal of clinical pharmacology 37 (1989), S. 487-491 
    Details
    ISSN: 1432-1041
    Keywords: almitrine ; drug absorption ; liver metabolism ; pharmacokinetics ; biliary excretion ; metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The absorption of almitrine from the upper gastrointestinal tract has been evaluated in 6 healthy volunteers by an intubation technique. Almitrine bismesylate dissolved in malic acid was introduced into the stomach after homogenization with a meal containing the marker14C-polyethylene glycol (PEG) 4000. Unlabeled PEG 4000 was infused into the second part of duodenum throughout the experiment. Samples of the luminal content were collected every 15 min for four hours from the stomach and at the ligament of Treitz. Blood was also collected. Almitrine was neither absorbed from nor metabolized in the stomach. About 37% of the quantity of drug emptied from the stomach was absorbed from the duodenum. Almitrine was detected in plasma 50 min after ingestion of the meal and its plasma concentration-time profile reflected the cumulative gastric emptying rate. The metabolite tetrahydroxy almitrine was found in intestinal samples as soon as unchanged drug was detected in plasma. The intraluminal rate of formation of the metabolite increased with time. The results suggest hepatic metabolism of almitrine followed by rapid excretion of the metabolite in the bile.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558129
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  • 10
    Electronic Resource
    Electronic Resource
    Lack of effect of ponsinomycin on the plasma pharmacokinetics of theophylline (1989)
    Springer
    European journal of clinical pharmacology 37 (1989), S. 101-104 
    Details
    ISSN: 1432-1041
    Keywords: theophylline ; ponsinomycin ; pharmacokinetics ; drug interactions ; macrolide antibiotic
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of ponsinomycin on the pharmacokinetics of theophylline has been studied in 12 young healthy volunteers. They received 10 doses of theophylline 200 mg every 8 h p.o., successively in the absence and then in the presence of ponsinomycin. This new macrolide, structurally related to midecamycin, was given in the therapeutic dose of 800 mg b.d. for 5 days, starting 2 days before the second phase of treatment with theophylline. The pharmacokinetic parameters of theophylline, calculated from its plasma concentration at steady-state, were not affected by the co-treatment. In particular, there was no significant difference between the peak and trough plasma levels, apparent clearance or apparent elimination half-life of theophylline in the absence and the presence of ponsinomycin. Only renal clearance was slightly (27%) but significantly increased by the co-treatment. The results suggest that ponsinomycin would be a good choice if a macrolide antibiotic were needed in patients being treated with theophylline.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609435
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