Effect of ketoconazole on the pharmacokinetics of ornidazole--a possible role of p-glycoprotein and CYP3A.
Drug Metabol Drug Interact
; 22(1): 67-77, 2006.
Article
en En
| MEDLINE
| ID: mdl-17152348
ABSTRACT
The influence of ketoconazole, a modulator of P-glycoprotein (P-gp), on the exsorption of ornidazole from everted sacs of rat intestine (duodenum, jejunum and ileum) was investigated. The effect of ketoconazole pretreatment on the pharmacokinetics of ornidazole was also studied in eight healthy human volunteers. After overnight fasting ornidazole 500 mg was administered before and after pretreatment with ketoconazole 200 mg once daily for 7 days. Serum samples were analyzed by reversed phase HPLC. Significant differences were observed in pharmacokinetic parameters C(max), AUC(0-t), AUC(0-infinity), T(max) and clearance. Ornidazole is believed to be metabolized through CYP3A and it has considerable intestinal efflux, which was observed from the in vitro study. The altered pharmacokinetic parameters can be attributed to ornidazole efflux from the blood to the intestine and its metabolism by CYP3A in the intestine.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Ornidazol
/
Citocromo P-450 CYP3A
/
Amebicidas
/
Mucosa Intestinal
/
Cetoconazol
/
Antifúngicos
Límite:
Adult
/
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Drug Metabol Drug Interact
Asunto de la revista:
FARMACOLOGIA
Año:
2006
Tipo del documento:
Article
País de afiliación:
India