Clinical pharmacokinetics of cicletanine hydrochloride

Results of the different pharmacokinetic studies performed with cicletanine, the first derivative of a new class of antihypertensive drugs, the furopyridines, are reviewed in this article. Pharmacokinetic studies with healthy subjects have shown that this drug is rapidly absorbed (time to Cmax about 0.65 h). It is strongly bound to plasma proteins (90%), with a volume of distribution of 37 l. The elimination half-life is between 6 to 8 h and elimination itself is mixed: renal and hepatic. The parameters are unchanged in young hypertensives. Pharmacokinetic studies in hepatic failure have shown that the mean retention time is about 6 h; the pharmacokinetic parameters are only slightly modified except in the case of cirrhosis with ascites and extra hepatic obstruction. The modification of pharmacokinetics in patients with renal failure is related to the severity of the condition. Small changes appear with moderate failure whereas important variations occur in severe renal failure.