Takabatake T, Ohta H, Maekawa M, Yamamoto Y, Ishida Y, Hara H, Nakamura S, Ushiogi Y, Kawabata M, Hashimoto N
Eur J Clin Pharmacol. 1985;28(3):327-31. doi: 10.1007/BF00543332.
The pharmacokinetics of a new, potent H2-receptor antagonist, famotidine, 20 mg i.v. was studied in 7 subjects with normal renal function and in 24 patients with varying degrees of renal impairment. The volume of distribution at steady state was 1.141/kg in normal subjects and was not altered in renal failure. The half-life of elimination was 2.59 h in normal subjects and was unchanged in mild renal failure (creatinine clearance, CLCR 90-60 ml/min/1.48 m2) but was increased to 4.72 h in moderate renal failure (CLCR 60-30 ml/min/1.48 m2), and to 12.07 h in severe renal failure (CLCR below 30 ml/min/1.48 m2). The cumulative urinary excretion and renal clearance of famotidine were correspondingly reduced in patients with impaired kidney function. In normal subjects and in patients with mild to moderate renal failure, about 70% of famotidine was excreted through the kidney, mainly by tubular secretion. In patients with a CLCR above 60 ml/min/1.48 m2 the normal daily dose of famotidine can be employed, but in those with a CLCR between 60 and 30 ml/min/1.48 m2 the dose should be reduced by half, and in patients with a CLCR below 30 ml/min/1.48 m2 a reduction by three quarters of the normal dose is recommended.
对7名肾功能正常的受试者和24名不同程度肾功能损害的患者，研究了静脉注射20毫克新型强效H2受体拮抗剂法莫替丁的药代动力学。正常受试者稳态分布容积为1.14升/千克，肾衰竭时未改变。正常受试者消除半衰期为2.59小时，轻度肾衰竭（肌酐清除率，CLCR 90 - 60毫升/分钟/1.48平方米）时不变，但中度肾衰竭（CLCR 60 - 30毫升/分钟/1.48平方米）时增至4.72小时，重度肾衰竭（CLCR低于30毫升/分钟/1.48平方米）时增至12.07小时。法莫替丁的累积尿排泄量和肾清除率在肾功能损害患者中相应降低。在正常受试者和轻度至中度肾衰竭患者中，约70%的法莫替丁通过肾脏排泄，主要通过肾小管分泌。CLCR高于60毫升/分钟/1.48平方米的患者可采用法莫替丁正常日剂量，但CLCR在60至30毫升/分钟/1.48平方米之间的患者剂量应减半，CLCR低于30毫升/分钟/1.48平方米的患者建议剂量减少至正常剂量的四分之一。
