Del Soldato P, Ghiorzi A, Cereda E, Donetti A
Pharmacology. 1985;30(1):45-51. doi: 10.1159/000138049.
The protective effect of cimetidine, ranitidine and a newer H2-receptor antagonist, mifentidine (proposed INN), on models of gastric and duodenal damage, caused by activation of H2 receptors, was studied. Gastric erosions were induced in rats by intravenous dimaprit (100 mg/kg) while duodenal damage was investigated in guinea pigs following subcutaneous administration of dimaprit (2 mg/kg, 6 doses). All the compounds reduced or abolished gastric and duodenal damage in rats and guinea pigs, mifentidine being more potent than both cimetidine and ranitidine. The antiulcer effect of the H2-receptor antagonists was related to the dose and to their ability to inhibit dimaprit-induced gastric acid secretion. The duration of action proved to be different for the three compounds. According to the two dosing schedules adopted to evaluate the duration of action, mifentidine, compared to cimetidine and ranitidine, required considerably lower oral dosages to display its protective effect.
研究了西咪替丁、雷尼替丁以及一种更新的H2受体拮抗剂米芬替丁（建议使用的国际非专利名称）对由H2受体激活引起的胃和十二指肠损伤模型的保护作用。通过静脉注射地马普明（100mg/kg）在大鼠中诱导胃糜烂，而在豚鼠皮下注射地马普明（2mg/kg，6剂）后研究十二指肠损伤。所有化合物均减轻或消除了大鼠和豚鼠的胃和十二指肠损伤，米芬替丁比西咪替丁和雷尼替丁更有效。H2受体拮抗剂的抗溃疡作用与剂量及其抑制地马普明诱导的胃酸分泌的能力有关。事实证明，这三种化合物的作用持续时间不同。根据用于评估作用持续时间的两种给药方案，与西咪替丁和雷尼替丁相比，米芬替丁显示其保护作用所需的口服剂量要低得多。
