Independent of etozolin elimination of kidney function. Single dose experiments in patients with renal insufficiency

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.