Pharmacokinetics of TZU-0460, a new H2-receptor antagonist, in patients with impaired renal function.

Abstract

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.

• Authors: T Takabatake, H Ohta, Y Yamamoto, Y Ishida, H Hara, S Nakamura, Y Ushiogi, S Satoh, N Hattori
• Journal: European journal of clinical pharmacology (Eur J Clin Pharmacol) Vol. 30 Issue 6 Pg. 709-12 ( 1986) ISSN: 0031-6970 [Print] Germany
• PMID: 2876900 (Publication Type: Journal Article)

Chemical References

• Histamine H2 Antagonists
• Piperidines
• desacetyl-TZU-0460
• TZU 0460
• Creatinine

Topics

• Adult
• Aged
• Aged, 80 and over
• Creatinine (metabolism)
• Dose-Response Relationship, Drug
• Half-Life
• Histamine H2 Antagonists (metabolism)
• Humans
• Kidney Diseases (metabolism)
• Kinetics
• Middle Aged
• Piperidines (metabolism)