ELIMINATION KINETICS OF CAPTOPRIL IN PATIENTS WITH RENAL-FAILURE
ELIMINATION KINETICS OF CAPTOPRIL IN PATIENTS WITH RENAL-FAILURE
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DOI：
10.1038/ki.1984.114
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发表时间：
1984-01-01
影响因子：
19.6
通讯作者：
ROMMEL, AJ
中科院分区：
文献类型：
--
作者：
DUCHIN, KL;PIERIDES, AM;ROMMEL, AJ
对21例不同程度肾损害患者口服100 mg 14C-卡托普利后，测定了卡托普利的动力学。卡托普利的消除动力学采用非模型方法进行评价。卡托普利的体内清除率(CLB)在透析间期随着肌酐清除量(CLcr)从轻度肾功能衰竭患者的5.2ml/min/kg降至血液透析患者的1.6ml/min/kg而稳步下降。在轻度肾损害患者中，卡托普利的肾和非肾清除分别平均为2.2ml/分钟/kg和3.0ml/分钟/公斤，而在严重肾损害患者中，卡托普利的肾和非肾清除分别降至0.2ml/分钟/公斤和1.5ml/分钟/公斤(P<；0.001)。在轻度、中度和重度肾损害患者之间，96-120小时内总累积放射性排泄量(粪便加尿液)的程度没有显著差异。在轻度、中度和重度肾损害组中，卡托普利48h的肾脏排泄量平均为剂量的29%、21%和8%。在另外5名血液透析患者中，卡托普利的平均透析器清除量平均为120毫升/分钟。剂量，.apprx。在4h透析液中回收率为35%。肾功能衰竭患者可能需要减少卡托普利的剂量。
Captopril kinetics were determined after a 100-mg oral dose of 14C-captopril in 21 patients with various degrees of renal impairment. Elimination kinetics of captopril were evaluated by model-independent methods. The body clearance (ClB) of captopril decreased steadily with decreasing creatinine clearance (ClCR) from 5.2 ml/min/kg for mild renal failure patients to 1.6 ml/min/kg for hemodialysis patients during an interdialytic period. In patients with mild renal impairment, renal and nonrenal clearances of captopril averaged 2.2 and 3.0 ml/min/kg, respectively, and fell (P < 0.001) to 0.2 and 1.5 ml/min/kg in patients with severe renal impairment. There were no significant differences in the extent of total cumulative excretion (fecal plus urinary) of radioactivity over a 96 to 120 h period between the patients with mild, moderate, and severe renal impairment. The 48 h renal excretion of captopril averaged 29, 21, and 8% of the dose in the mild, moderate, and severe renally impaired groups. In five additional hemodialysis patients, the mean dialyzer clearance of captopril averaged 120 ml/min. Of the dose, .apprx. 35% was recovered in the 4 h dialysate. A reduction in the dose of captopril may be necessary in patients with renal failure.