Pharmacokinetics of TZU-0460, a new H2-receptor antagonist, in patients with impaired renal function.
We have studied pharmacokinetics of a new H2-receptor antagonist, TZU-0460, in patients with varying degrees of renal impairment. The apparent volume of distribution at steady-state was 1.70 l/kg, and the plasma protein binding of TZU-0460 or its active metabolite, desacetyl TZU-0460 was less than 10% in normal subjects. These variables were not altered with renal impairment. Sixty percent of TZU-0460 given orally was excreted via the kidney, mainly by tubular secretion. The half-time of elimination was 3.94 h in normal subjects, and was prolonged to 12.13 h in severe renal failure (creatinine clearance below 30 ml/min/1.48 m2). Dosage adjustment of TZU-0460 is necessary in renal failure.
D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D003404:Creatinine / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006207:Half-Life; D006635:Histamine H2 Antagonists / Q000378:metabolism*; D006801:Humans; D007674:Kidney Diseases / Q000378:metabolism*; D007700:Kinetics; D008875:Middle Aged; D010880:Piperidines / Q000378:metabolism*
D006635:Histamine H2 Antagonists; D010880:Piperidines; C050717:desacetyl-TZU-0460; C045914:TZU 0460; D003404:Creatinine