法莫替丁的临床药物动力学。

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Echizen H, Ishizaki T

法莫替丁的临床药物动力学。

Pharmacokinet。1991年9月,21 (3):178 - 94。doi: 10.2165 / 00003088-199121030-00003。

PubMed ID

1764869 (在PubMed

]

文摘

法莫替丁是一个有效的组胺H2-receptor拮抗剂广泛用于消化性溃疡疾病的治疗和预防。静脉注射后等离子体法莫替丁浓度时间剖面展品biexponential衰变,分布半衰期约为0.18 - 0.5 h和消除半衰期约2 - 4 h。的体积分布稳态药物的范围从1.0到1.3 L /公斤;血浆蛋白结合低(15 - 22%)。法莫替丁消除70%不变到尿液后静脉管理。法莫替丁总身体和肾许可与肌酐清除率显著相关。因为它的肾清除率(15 L / h)远远超过了肾小球滤过率,法莫替丁被认为是消除不仅通过肾小球滤过,而且通过肾小管分泌。以来间隙减少在肾功能不全患者和老年患者,维护剂量应减少在这些患者组。删除任何当前使用的血液净化过程法莫替丁(血液透析、腹膜透析和血液过滤)不发生临床很大程度上如此。肝硬化似乎并不影响法莫替丁,除非严重肾功能不全的性格共存。 After oral administration, peak plasma concentrations are attained within 2 to 4h; the oral bioavailability ranges from 40 to 50%, due mainly to incomplete absorption. The oral absorption of the drug is dose-independent within a range of 5 to 40 mg. There are 3 formulations available (tablet, capsule and suspension), which appear to be bioequivalent. Coadministration of potent antacids reduces the oral absorption of famotidine by 20 to 30%. On a weight-to-weight basis, the antisecretory effect of famotidine is about 20 and 7.5 times more potent than those of cimetidine and ranitidine, respectively. Plasma famotidine concentrations correlate with its antisecretory effect: values of about 13 and 20 micrograms/L produce a 50% reduction in the gastrin-stimulated gastric acid secretion and a fasting intragastric pH of greater than 4, respectively. Available data suggest that famotidine interacts neither with the hepatic oxidative drug metabolism nor with the tubular secretion of other commonly used therapeutic agents. However, further studies are required to evaluate a full spectrum of its drug interaction potential.

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药物

法莫替丁