Quantitative correlations among CYP3A sensitive substrates and inhibitors: literature analysis.
Curr Drug Metab
; 8(8): 810-4, 2007 Dec.
Article
em En
| MEDLINE
| ID: mdl-18220561
ABSTRACT
As a follow-up to the new classification of CYP3A inhibitors, the present work was undertaken to search for quantitative correlations of AUC ratios between sensitive substrates and midazolam (reference). A large set of clinical studies was obtained utilizing the M&T Drug Interaction Database, and recent Product Labels. Linear relationships were found between midazolam and four CYP3A substrates simvastatin, buspirone, triazolam and eplerenone. Simvastatin and buspirone were consistently more sensitive than midazolam, independent of the inhibitor. Quantitative correlations of AUC ratios between four CYP3A inhibitors (fluconazole, erythromycin, verapamil, diltiazem) and ketoconazole (400 mg/day) were also uncovered. The average potencies of these inhibitors relative to ketoconazole were 27% for erythromycin, 17% for fluconazole and 19% for verapamil.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Interações Medicamentosas
/
Citocromo P-450 CYP3A
/
Inibidores do Citocromo P-450 CYP3A
Tipo de estudo:
Diagnostic_studies
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article