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.