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Titolo:
Effect of itraconazole on the pharmacokinetics of prednisolone and methylprednisolone and cortisol secretion in healthy subjects
Autore:
Lebrun-Vignes, B; Archer, VC; Diquet, B; Levron, JC; Chosidow, O; Puech, AJ; Warot, D;
Indirizzi:
Assistance Publ Hop Paris, Dept Pharmacol, Paris, France Assistance Publ Hop Paris Paris France s, Dept Pharmacol, Paris, France Assistance Publ Hop Paris, Dept Internal Med, Paris, France Assistance Publ Hop Paris Paris France Dept Internal Med, Paris, France Janssen Labs, Val de Reuil, France Janssen Labs Val de Reuil FranceJanssen Labs, Val de Reuil, France
Titolo Testata:
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
fascicolo: 5, volume: 51, anno: 2001,
pagine: 443 - 450
SICI:
0306-5251(200105)51:5<443:EOIOTP>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
TORSADES-DE-POINTES; PLASMA-CONCENTRATIONS; ORAL METHYLPREDNISOLONE; TRANSPLANT RECIPIENTS; ADRENAL-RESPONSE; KETOCONAZOLE; THERAPY; PHARMACODYNAMICS; ERYTHROMYCIN; TERFENADINE;
Keywords:
corticosteroids; drug-drug interaction; itraconazole; pharmacokinetics;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
45
Recensione:
Indirizzi per estratti:
Indirizzo: Diquet, B Hop La Pitie Salpetriere, Dept Pharmacol, 47 Bd Hop, F-75651 Paris, France Hop La Pitie Salpetriere 47 Bd Hop Paris France F-75651 France
Citazione:
B. Lebrun-Vignes et al., "Effect of itraconazole on the pharmacokinetics of prednisolone and methylprednisolone and cortisol secretion in healthy subjects", BR J CL PH, 51(5), 2001, pp. 443-450

Abstract

Aims Itraconazole is a potent inhibitor of CYP3A4 activity and is often used in combination with corticosteroids. Since the latter are partly metabolized by CYP3A4, we studied the interaction between itraconazole, prednisoneand methylprednisolone in healthy male subjects. Methods The effects of 4 days administration of oral itraconazole (400 mg on the first day then 200 mg day(-1) for 3 days) on the pharmacokinetics ofprednisolone after a single oral dose of prednisone (60 mg) and the pharmacokinetics of methylprednisolone after single oral dose of methylprednisolone (48 mg) were studied in II healthy male subjects in a two-period cross-over trial. Plasma cortisol concentrations were determined as a pharmacodynamic index. Results Itraconazole increased the mean area under the methylprednisolone concentration-time curve from 2773 ng ml(-1) h to 7011 ng ml(-1) h (P<0.001) and the elimination half-life from 3.2 h to 5.5 h (P<0.001). The pharmacokinetics of prednisolone were unchanged. Cortisol concentrations at 24 h were lower after administration of methylprednisolone with itraconazole than after methylprednisolone alone (24 ng ml(-1) vs 109 ng ml(-1), P<0.001). Conclusions Itraconazole increased methylprednisolone concentrations markedly with enhanced suppression of endogenous cortisol secretion, but had no effect on prednisolone pharmacokinetics. The pharmacokinetic interaction between methylprednisolone and itraconazole is probably related to inhibitionof hepatic CYP3A4 activity by itraconazole.

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Documento generato il 03/04/20 alle ore 14:02:32