Knauf H, Hasenfuss G, Wais U, Schollmeyer P, Mutschler E
Arzneimittelforschung. 1980;30(10):1791-3.
Following a single oral dose of the novel diuretic ethyl (Z)-(3-methyl-4-oxo-5-piperidino-thiazolidin-2-ylidene) acetate (etozolin, Elkapin), the plasma levels of the parent drug and its active metabolite (Z)-(3-methyl-4-oxo-5-piperidino-thiazolidin-2-ylidene) acetic acid (ozolinone) were determined by means of HPLC. In order to learn whether or not impairment of renal function influences the plasma levels of the diuretics and their elimination rate 19 patients with various degrees of reduced glomerular filtration rate were investigated. The lack of correlation between elimination half-life (HL) and creatinine clearance showed that there is no influence of kidney disease on the pharmacokinetic parameters of etozolin and ozolinone. Even in severe renal insufficiency the HL of etozolin and ozolinone did not differ from normal values, the mean HL of etozolin being 2.8 +/- 0.4 h and of ozolinone being 10.2 +/- 1.5 h. Also impairment of liver function did not signficantly alter the pharmacokinetic parameters of these diuretic agents. It is concluded that in the single dose experiments renal insufficiency does not significantly influence the metabolization of etozolin and ozolinone.
单次口服新型利尿剂乙（Z）-（3-甲基-4-氧代-5-哌啶基-噻唑烷-2-亚基）乙酸酯（依托唑啉，Elkapin）后，采用高效液相色谱法测定母体药物及其活性代谢物（Z）-（3-甲基-4-氧代-5-哌啶基-噻唑烷-2-亚基）乙酸（奥唑啉酮）的血浆水平。为了了解肾功能损害是否会影响利尿剂的血浆水平及其消除率，对19例肾小球滤过率不同程度降低的患者进行了研究。消除半衰期（HL）与肌酐清除率之间缺乏相关性表明，肾脏疾病对依托唑啉和奥唑啉酮的药代动力学参数没有影响。即使在严重肾功能不全的情况下，依托唑啉和奥唑啉酮的HL与正常值也没有差异，依托唑啉的平均HL为2.8±0.4小时，奥唑啉酮的平均HL为10.2±1.5小时。肝功能损害也未显著改变这些利尿剂的药代动力学参数。得出的结论是，在单剂量实验中，肾功能不全不会显著影响依托唑啉和奥唑啉酮的代谢。
