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单次静脉注射替考拉宁在不同程度肾功能损害受试者中的药代动力学。

Pharmacokinetics of a single intravenous dose of teicoplanin in subjects with various degrees of renal impairment.

作者信息

Bonati M, Traina G L, Rosina R, Buniva G

机构信息

Laboratory of Clinical Pharmacology, Instituto di Ricerche Farmacologiche Mario Negri, Milano, Italy.

出版信息

J Antimicrob Chemother. 1988 Jan;21 Suppl A:29-37. doi: 10.1093/jac/21.suppl_a.29.

Abstract

The pharmacokinetic profile of teicoplanin after single 3 mg/kg doses in adults with different degrees of renal failure was reviewed. The disposition of teicoplanin was adequately described by a three-compartment open pharmacokinetic model and it appears to be primarily related to the degree of renal function. Teicoplanin total body clearance was less and the terminal elimination half-life progressively prolonged in association with renal failure, but the volume of distribution at steady-state did not change. Highly significant relationships between teicoplanin total body and renal clearance and creatinine clearance have been reported and serve as a basis for adjusting dosage in patients with renal failure. In patients on continuous ambulatory peritoneal dialysis teicoplanin, administered either intravenously or intraperitoneally, showed bidirectional exchange characteristics through the peritoneal membrane, although transfer from the systemic circulation to peritoneal fluid was consistently low. Haemodialysis made no significant contribution to total body clearance of teicoplanin. Guidelines for administration of teicoplanin in patients with renal failure are discussed.

摘要

回顾了替考拉宁在不同程度肾功能衰竭的成人中单次给予3mg/kg剂量后的药代动力学特征。替考拉宁的处置可用三室开放药代动力学模型充分描述,且其似乎主要与肾功能程度有关。随着肾功能衰竭,替考拉宁的全身清除率降低,终末消除半衰期逐渐延长,但稳态分布容积未改变。已有报道称替考拉宁的全身清除率和肾清除率与肌酐清除率之间存在高度显著的关系,这为调整肾功能衰竭患者的剂量提供了依据。在持续非卧床腹膜透析患者中,静脉内或腹腔内给予替考拉宁后,其通过腹膜表现出双向交换特征,尽管从体循环向腹膜液的转运一直较低。血液透析对替考拉宁的全身清除率无显著贡献。讨论了肾功能衰竭患者使用替考拉宁的给药指南。

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