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Titolo:
Effect of fluconazole on plasma fluvastatin and pravastatin concentrations
Autore:
Kantola, T; Backman, JT; Niemi, M; Kivisto, KT; Neuvonen, PJ;
Indirizzi:
Univ Helsinki, Dept Clin Pharmacol, FIN-00290 Helsinki, Finland Univ Helsinki Helsinki Finland FIN-00290 ol, FIN-00290 Helsinki, Finland Univ Helsinki, Cent Hosp, FIN-00290 Helsinki, Finland Univ Helsinki Helsinki Finland FIN-00290 sp, FIN-00290 Helsinki, Finland
Titolo Testata:
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
fascicolo: 3, volume: 56, anno: 2000,
pagine: 225 - 229
SICI:
0031-6970(200006)56:3<225:EOFOPF>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
PERFORMANCE LIQUID-CHROMATOGRAPHY; EXPANDED CLINICAL-EVALUATION; DRUG-INTERACTIONS; SYSTEMIC ANTIMYCOTICS; WARFARIN-FLUCONAZOLE; REDUCTASE INHIBITORS; LOVASTATIN EXCEL; HUMAN-LIVER; IN-VITRO; ITRACONAZOLE;
Keywords:
fluvastatin; pravastatin; fluconazole;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
36
Recensione:
Indirizzi per estratti:
Indirizzo: Neuvonen, PJ Univ Helsinki, Dept Clin Pharmacol, Haartmanink 4, FIN-00290 Helsinki, Finland Univ Helsinki Haartmanink 4 Helsinki Finland FIN-00290 nland
Citazione:
T. Kantola et al., "Effect of fluconazole on plasma fluvastatin and pravastatin concentrations", EUR J CL PH, 56(3), 2000, pp. 225-229

Abstract

Objective: To study the effects of fluconazole on the pharmacokinetics of fluvastatin and pravastatin, two inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. Methods: Two separate randomised, double-blind, two-phase, crossover studies with identical study design were carried out. In each study, 12 healthy volunteers were given a 4-day pretreatment with oral fluconazole (400 mg onday 1 and 200 mg on days 2-4) or placebo, according to a randomisation schedule. On day 4, a single oral dose of 40 mg fluvastatin (study I) or 40 mgpravastatin (study II) was administered orally. Plasma concentrations of fluvastatin, pravastatin and fluconazole were measured over 24 h. Results: In study I, fluconazole increased the mean area under the plasma fluvastatin concentration-time curve (AUC(0-infinity)) by 84% (P < 0.01), the mean elimination half-life (t(1/2)) of fluvastatin by 80% (P < 0.01) andits mean peak plasma concentration (C-max) by 44% (P < 0.05). In study II,fluconazole had no significant effect on the pharmacokinetics of pravastatin. Conclusions: Fluconazole has a significant interaction with fluvastatin. The mechanism of the increased plasma concentrations and prolonged elimination of fluvastatin is probably inhibition of the CYP2C9-mediated metabolism of fluvastatin by fluconazole. Care should be taken if fluconazole or otherpotent inhibitors of CYP2C9 are prescribed to patients using fluvastatin. However, pravastatin is not susceptible to interactions with fluconazole orother potent CYP2C9 inhibitors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/07/20 alle ore 07:49:02