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Titolo:
Effects of fluconazole and fluvoxamine on the pharmacokinetics and pharmacodynamics of glimepiride
Autore:
Niemi, M; Backman, JT; Neuvonen, M; Laitila, J; Neuvonen, PJ; Kivisto, KT;
Indirizzi:
Univ Helsinki, Cent Hosp, Dept Clin Pharmacol, Hus 00029, Finland Univ Helsinki Hus Finland 00029 Dept Clin Pharmacol, Hus 00029, Finland
Titolo Testata:
CLINICAL PHARMACOLOGY & THERAPEUTICS
fascicolo: 4, volume: 69, anno: 2001,
pagine: 194 - 200
SICI:
0009-9236(200104)69:4<194:EOFAFO>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
SEROTONIN REUPTAKE INHIBITORS; HUMAN-LIVER-MICROSOMES; PERFORMANCE LIQUID-CHROMATOGRAPHY; IN-VITRO; WARFARIN-FLUCONAZOLE; DRUG-INTERACTIONS; HUMAN SERUM; METABOLISM; ITRACONAZOLE; TOLBUTAMIDE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
33
Recensione:
Indirizzi per estratti:
Indirizzo: Kivisto, KT Univ Helsinki, Cent Hosp, Dept Clin Pharmacol, POB 340, Hus 00029, Finland Univ Helsinki POB 340 Hus Finland 00029 0, Hus 00029, Finland
Citazione:
M. Niemi et al., "Effects of fluconazole and fluvoxamine on the pharmacokinetics and pharmacodynamics of glimepiride", CLIN PHARM, 69(4), 2001, pp. 194-200

Abstract

Objective: Our objective was to study the effects of fluconazole and fluvoxamine on the pharmacokinetics and pharmacodynamics of glimepiride, a new sulfonylurea antidiabetic drug. Methods: In this randomized, double-blind, three-phase crossover study, 12healthy volunteers took 200 mg of fluconazole once daily (400 mg on day 1), 100 mg of fluvoxamine once daily, or placebo once daily for 4 days. On day 4, a single oral dose of 0.5 mg of glimepiride was administered. Plasma glimepiride and blood glucose concentrations were measured up to 12 hours. Results: In the fluconazole phase, the mean total area under the plasma concentration-time curve of glimepiride was 238% (P <.0001) and the peak plasma concentration was 151% (P <.0001) of the respective control value. The mean elimination half-life of glimepiride was prolonged from 2.0 to 3.3 hours (P <.0001) by fluconazole. In the fluvoxamine phase, the mean area under the plasma concentration-time curve of glimepiride was not significantly different from that in the placebo phase. However, the mean peak plasma concentration of glimepiride was 143% (P <.05) of the control and the elimination half-life was prolonged from 2.0 to 2.3 hours (P <.01) by fluvoxamine. Fluconazole and fluvoxamine did not cause statistically significant changes in the effects of glimepiride on blood glucose concentrations. Conclusions: Fluconazole considerably increased the area under the plasma concentration-time curve of glimepiride and prolonged its elimination half-life. This was probably caused by inhibition of the cytochrome P-450 2C9-mediated biotransformation of glimepiride by fluconazole. Concomitant use of fluconazole with glimepiride may increase the risk of hypoglycemia as much as would a 2- to 3-fold increase in the dose of glimepiride. Fluvoxamine moderately increased the plasma concentrations and slightly prolonged the elimination half-life of glimepiride.

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Documento generato il 16/07/20 alle ore 15:32:32