Robson R A, Bailey R R, Sharman J R
Clin Pharmacokinet. 1984 Jan-Feb;9(1):88-94. doi: 10.2165/00003088-198409010-00005.
The single-dose pharmacokinetics of intravenously and orally administered tinidazole were studied in normal subjects and patients with severe chronic renal failure. The clearance of tinidazole was also measured in patients on regular haemodialysis. After intravenous administration the mean elimination half-life of tinidazole was 17.1 +/- 2.3 (SD) hours in the normal subjects and 16.9 +/- 4.9 hours in patients with renal failure; the mean apparent volumes of distribution were 0.80 +/- 0.09 L/kg and 0.69 +/- 0.09 L/kg, respectively. Following oral administration the mean elimination half-life was 15.6 +/- 1.6 hours in the normal subjects and 18.4 +/- 3.5 hours in patients with renal failure; there were no statistically significant differences in these pharmacokinetic parameters. There was no accumulation of the major metabolite (hydroxymethyl tinidazole) in normal subjects or in patients with renal failure. Tinidazole clearance during haemodialysis was 71 +/- 7.7 ml/min. In the presence of renal failure no modification of tinidazole dosage would appear to be necessary. Tinidazole should be administered in full dosage following haemodialysis.
在正常受试者和严重慢性肾衰竭患者中研究了静脉注射和口服替硝唑的单剂量药代动力学。还对定期进行血液透析的患者测定了替硝唑的清除率。静脉给药后,替硝唑在正常受试者中的平均消除半衰期为17.1±2.3(标准差)小时,在肾衰竭患者中为16.9±4.9小时;平均表观分布容积分别为0.80±0.09L/kg和0.69±0.09L/kg。口服给药后,正常受试者的平均消除半衰期为15.6±1.6小时,肾衰竭患者为18.4±3.5小时;这些药代动力学参数无统计学显著差异。在正常受试者或肾衰竭患者中,主要代谢产物(羟甲基替硝唑)均无蓄积。血液透析期间替硝唑的清除率为71±7.7ml/min。在肾衰竭情况下,似乎无需调整替硝唑剂量。血液透析后应给予替硝唑全剂量。