Takabatake T, Ohta H, Yamamoto Y, Ishida Y, Hara H, Nakamura S, Ushiogi Y, Satoh S, Hattori N
Eur J Clin Pharmacol. 1986;30(6):709-12. doi: 10.1007/BF00608220.
We have studied pharmacokinetics of a new H2-receptor antagonist, TZU-0460, in patients with varying degrees of renal impairment. The apparent volume of distribution at steady-state was 1.70 l/kg, and the plasma protein binding of TZU-0460 or its active metabolite, desacetyl TZU-0460 was less than 10% in normal subjects. These variables were not altered with renal impairment. Sixty percent of TZU-0460 given orally was excreted via the kidney, mainly by tubular secretion. The half-time of elimination was 3.94 h in normal subjects, and was prolonged to 12.13 h in severe renal failure (creatinine clearance below 30 ml/min/1.48 m2). Dosage adjustment of TZU-0460 is necessary in renal failure.
我们研究了新型H2受体拮抗剂TZU - 0460在不同程度肾功能损害患者中的药代动力学。稳态时的表观分布容积为1.70升/千克，在正常受试者中，TZU - 0460或其活性代谢物去乙酰基TZU - 0460的血浆蛋白结合率低于10%。这些变量在肾功能损害时未发生改变。口服给予的TZU - 0460有60%经肾脏排泄，主要通过肾小管分泌。正常受试者的消除半衰期为3.94小时，在严重肾衰竭（肌酐清除率低于30毫升/分钟/1.48平方米）时延长至12.13小时。肾功能衰竭时需要调整TZU - 0460的剂量。
