Effects of age and chronic renal failure on the urinary excretion kinetics of famotidine in man
Effects of age and chronic renal failure on the urinary excretion kinetics of famotidine in man
复制标题
年龄和慢性肾功能衰竭对男性法莫替丁尿排泄动力学的影响
DOI：
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复制
发表时间：
2004
影响因子：
2.9
通讯作者：
G. A. Hessey
中科院分区：
文献类型：
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作者：
J. Lin;A. Chremos;K. Yeh;J. Antonello;G. A. Hessey
摘要
在16名健康青年、8名健康老年人以及18名不同程度肾功能不全患者静脉给药后，对一种新型强效H₂受体拮抗剂法莫替丁的血浆和尿液浓度进行了测定。
法莫替丁的血浆清除率和肾排泄率在老年志愿者和肾病患者中均降低。正常青年志愿者中法莫替丁的肾清除率平均为4.43毫升/分钟/千克（310毫升/分钟），超过了平均肌酐清除率1.55毫升/分钟/千克（109毫升/分钟），这表明净分泌是法莫替丁消除的一个重要机制。
法莫替丁肾清除率与肌酐清除率的比值随着肌酐清除率的降低而降低；这些结果表明，分泌过程的恶化比肾小球滤过的恶化快得多，且与“健存肾单位假说”不符。然而，总体清除率和肾清除率都与肌酐清除率显著相关。
表观半衰期也与肌酐清除率显著相关。由于法莫替丁基本上没有剂量相关的不良反应，轻度肾功能不全患者和老年人不需要调整剂量；然而，对于重度肾功能不全患者，在长期治疗期间可以延长给药间隔或减少每日剂量，以避免药物蓄积和潜在的不良影响。
SummaryThe plasma and urine concentrations of famotidine, a new, potent H2-receptor antagonist, have been measured in 16 healthy young adults, 8 healthy elderly people and 18 patients with varying degrees of renal dysfunction after intravenous administration.Both the plasma elimination and renal excretion of famotidine were decreased in the elderly volunteers and renal patients. The renal clearance of famotidine averaged 4.43 ml/min/kg (310 ml/min) in normal young volunteers, which exceeded the mean creatinine clearance 1.55 ml/min/kg (109 ml/min), suggesting net secretion is a significant mechanism for elimination of famotidine.The ratio of famotidine renal clearance to creatinine clearance decreased as creatinine clearance decreased; these results suggest that the deterioration in the secretion process was much faster than that in glomerular filtration and are incompatible with the “intact nephron hypothesis”. Nevertheless, both total body clearance and renal clearance were significantly correlated with creatinine clearance.The apparent half-life was also significantly correlated with creatinine clearance. Since famotidine is essentially free of dose-related adverse effects, dose adjustment in patients with mild renal insufficiency and in elderly people is not required; however, either a prolonged dosing interval or a decrease in daily dose during long-term therapy may be adapted for the patients with severe renal insufficiency to avoid accumulation and the potential undesirable effects.