Pharmacokinetics of cicletanine in patients with impaired renal function.
The pharmacokinetics of cicletanine were studied in 43 patients with chronic renal failure of various degrees, including six patients treated by maintenance haemodialysis, following single oral administration of either 300 or 200 mg. A repeated-dose study was performed at the start and at the end of daily oral administration of 200 mg for 30 days in six patients with moderate renal dysfunction. The pharmacokinetics of cicletanine were markedly altered in patients with severe impairment of renal function (i.e., creatinine clearance under 30 ml/min/1.73 m2 or treated by chronic haemodialysis) with a significant increase in elimination half-life and tissue accumulation of the drug. In contrast, only minor alterations in the pharmacokinetic parameters were observed in patients with mild or moderate renal failure, even after repeated administration of the drug. In conclusion, the use of cicletanine should be restricted, on the basis of these pharmacokinetic data, to chronic uremic patients whose creatinine clearance is 30 ml/min/1.73 m2 or more.
Department of Nephrology, Necker Hospital, Paris, France.
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D000328:Adult; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004232:Diuretics / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004334:Drug Administration Schedule; D006207:Half-Life; D006801:Humans; D007676:Kidney Failure, Chronic / Q000378:metabolism*; D008875:Middle Aged; D011725:Pyridines; D013997:Time Factors
D000959:Antihypertensive Agents; D004232:Diuretics; D011725:Pyridines; C038068:cicletanine