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Titolo:
The effect of ketoconazole on the pharmacokinetics, pharmacodynamics and safety of nisoldipine
Autore:
Heinig, R; Adelmann, HG; Ahr, G;
Indirizzi:
Bayer AG, Inst Clin Pharmacol, D-42096 Wuppertal, Germany Bayer AG Wuppertal Germany D-42096 Pharmacol, D-42096 Wuppertal, Germany
Titolo Testata:
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
fascicolo: 1, volume: 55, anno: 1999,
pagine: 57 - 60
SICI:
0031-6970(199903)55:1<57:TEOKOT>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
INCREASES PLASMA-CONCENTRATIONS; THERAPEUTIC EFFICACY; COAT-CORE; HYPERTENSION;
Keywords:
enzyme inhibition; cytochrome P450 3A4; first-pass metabolism; bioavailability;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
22
Recensione:
Indirizzi per estratti:
Indirizzo: Heinig, R Bayer AG, Inst Clin Pharmacol, Bldg 405,Aprather Weg 18, D-42096Wuppertal, Bayer AG Bldg 405,Aprather Weg 18 Wuppertal Germany D-42096 al,
Citazione:
R. Heinig et al., "The effect of ketoconazole on the pharmacokinetics, pharmacodynamics and safety of nisoldipine", EUR J CL PH, 55(1), 1999, pp. 57-60

Abstract

Objective: The primary aim of the present study was to investigate the effect of ketoconazole on the pharmacokinetics of nisoldipine. Methods: A single dose of nisoldipine 5 mg immediaterelease tablet was administered eitheralone or in combination with ketoconazole 200 mg (4 days pretreatment and concomitant administration) in a randomized crossover trial in seven healthy male Caucasian volunteers. Plasma concentration-versus-time profiles of nisoldipine and its metabolite M9 were determined. Results: Pre-treatment with and concomitant administration of ketoconazole resulted in a 24-fold and11-fold, increase in mean AUC and C-max of nisoldipine, respectively, compared with treatment with nisoldipine 5 mg alone. The ketoconazole-induced increase in plasma concentration of the metabolite M9 was of similar magnitude. Conclusion: The interaction is attributed to inhibition of cytochrome 3A4-mediated first-pass metabolism. Keto-conazole and other antifungal drugsof the substituted imidazole type as well as other potent inhibitors of cytochrome 3A4 should not be used concomitantly with nisoldipine.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 10:53:01