Summary
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.
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Tarutani M, Sakuma H, Shiratsuchi K, Mieda M (1985) Histamine H2-receptor antagonistic action of N-{3-[3-(1-piperidinylmethyl)phenoxy]propyl}acetoxyacetamide hydrochloride (TZU-0460). Arzneimittelforsch 35: 703–706
Tarutani M, Sakuma H, Shiratsuchi K, Mieda M (1985) Effects of N-{3-[3-(1-piperidinyl-methyl)phenoxy]propyl}acetoxy acetamide hydrochloride (TZU-0460), a histamine H2-receptor antagonist, on gastric acid secretion and ulcer formation. Arzneimittelforsch 35: 844–848
Honma S, Akutsu R, Iwamura S, Kawabe Y, Tsukamoto K (1985) Metabolic fate of TZU-0460, a new H2-receptor antagonist (8): The metabolism in man. Ohyo Yakuri (Phamacometrics) 30: 555–563
Bennett WM, Muther RS, Parker RA, Feig P, Morrison G, Golper TA, Singer I (1980) Drug therapy in renal failure: Dosing guidelines for adults. Part II: Sedatives, hypnotics, and tranquilizers; cardiovascular, antihypertensive, and diuretic agents; miscellaneous agents. Ann Intern Med 93: 286–325
Takabatake T, Ohta H, Yamamoto Y, Ishida Y, Hara H, Nakamura S, Ushiogi Y, Kawabata M, Hashimoto N, Hattori N (1985) Pharmacokinetics of famotidine, a new H2-receptor antagonist, in relation to renal function. Eur J Clin Pharmacol 28: 327–331
Ueno K, Amagaya T, Sato J, Ishikawa M (1985) Effect of new H2-receptor antagonist TZU-0460 on intragastric acidity. Jpn Pharmacol Ther 13: 579–587
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Takabatake, T., Ohta, H., Yamamoto, Y. et al. Pharmacokinetics of TZU-0460, a new H2-receptor antagonist, in patients with impaired renal function. Eur J Clin Pharmacol 30, 709–712 (1986). https://doi.org/10.1007/BF00608220
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DOI: https://doi.org/10.1007/BF00608220