Krishna D R, Klotz U
Dr Margarete Fischer-Bosch Institute of Clinical Pharmacology, Stuttgart, West Germany.
Clin Pharmacokinet. 1988 Oct;15(4):205-15. doi: 10.2165/00003088-198815040-00001.
Since H2-receptor antagonists are widely and successfully used in the treatment of peptic ulcer, several alternatives to the standard agents cimetidine and ranitidine have been developed. Promising 'new' candidates might be famotidine and nizatidine. For proper selection of the appropriate drug, its pharmacokinetic properties and interaction potential should be known. All 'old' and 'new' H2-receptor blockers are eliminated relatively rapidly (t 1/2 ranges from 1.5 to 4 hours), mainly by the renal route (glomerular filtration and tubular secretion). They exhibit a linear disposition and their distribution is similar. Absorption is most complete for nizatidine, whereas famotidine demonstrates the lowest effective plasma concentrations. Since etintidine shares the same imidazole ring structure as cimetidine, it can also impair oxidative drug metabolism in the liver. In this respect, the non-interacting famotidine and nizatidine (like ranitidine) offer a definite advantage. Based on their very similar pharmacokinetic and interaction profiles, these 2 H2-receptor antagonists might be regarded as alternatives to the older drugs in this group, and at least some economic benefits might result from the competition they will provide.
由于H2受体拮抗剂已广泛且成功地用于消化性溃疡的治疗，因此已开发出几种标准药物西咪替丁和雷尼替丁的替代药物。有前景的“新型”候选药物可能是法莫替丁和尼扎替丁。为了正确选择合适的药物，应该了解其药代动力学特性和相互作用潜力。所有“旧”的和“新”的H2受体阻滞剂相对较快地被消除（半衰期为1.5至4小时），主要通过肾脏途径（肾小球滤过和肾小管分泌）。它们呈现线性处置，并且它们的分布相似。尼扎替丁的吸收最完全，而法莫替丁的有效血浆浓度最低。由于依替替丁与西咪替丁具有相同的咪唑环结构，它也会损害肝脏中的氧化药物代谢。在这方面，非相互作用的法莫替丁和尼扎替丁（如雷尼替丁）具有明显优势。基于它们非常相似的药代动力学和相互作用特征，这两种H2受体拮抗剂可被视为该组中旧药物的替代品，并且它们之间的竞争至少可能带来一些经济效益。
