Pharmacokinetics and metabolism of C-tinidazole in humans.

Autor: Wood, S. G., John, B. A., Chasseaud, L. F., Brodie, R. R., Baker, J. M., Faulkner, J. K., Wood, B. A., Darragh, A., Lambe, R. F.
Zdroj: Journal of Antimicrobial Chemotherapy (JAC); Jul1986, Vol. 17 Issue 6, p801-809, 9p
Abstrakt: Following intravenous infusion of 800 mg of C-tinidazole during 30 min to two human subjects, a mean of 44% of the dose was excreted in urine during the first 24 h, increasing to 63% of the dose during five days: 12% of the dose was excreted in the faeces, indicating the possible involvement of biliary excretion and other secretory processes in the disposition of tinidazole. At 6 min after the end of the infusion, the mean plasma tinidazole concentration was 12 mg/l. Tinidazole was a major component in 0–120 h urine (about 32% of urinary C): the major metabolite in the 0–120 h urine examined was ethyl 2-(5-hydroxy-2-methyl-4-nitro-1-imidazolyl)ethyl sulphone (about 30% urinary C), the product of hydroxylation and nitro-group migration. These compounds were also present in the faeces. A minor urinary metabolite was 2-hydroxymethyltinidazole (about 9% urinary C), which was also present in plasma. The mean pharmacokinetic parameters obtained for tinidazole were similar to those reported in the literature; total clearance 51 ml/min, renal clearance 10 ml/min, volume of distribution 501 and half-life 11.6 h. [ABSTRACT FROM PUBLISHER]
Databáze: Complementary Index