Koutsoviti-Papadopoulou M, Nikolaidis E, Batzias G C, Kounenis G
Department of Pharmacology, Faculty of Veterinary Medicine, Aristotle University, Thessaloniki, Greece.
Pharmacol Res. 2001 Apr;43(4):329-34. doi: 10.1006/phrs.2000.0785.
The present study examines the pharmacodynamic interaction between the H(2)-receptor antagonist ranitidine and the prokinetic agent cisapride on the isolated rabbit intestine. Ranitidine produced a concentration-dependent contractile effect on the duodenal, ileal and ascending colon preparations, with EC(50)values of 1.35 x 10(-4)M for the duodenum, 1.2 x 10(-4)M for the ileum and 1.15 x 10(-4)M for the ascending colon. The effect of cisapride on the ranitidine contractile effect was dependent on the cisapride concentration used. Thus, cisapride, at concentrations from 10(-10)up to 5 x 10(-7)for the duodenum and the ascending colon and up to 10(-6)M for the ileum, potentiated the contractile responses of the preparations to ranitidine. However, at higher concentrations cisapride produced a non-competitive inhibition of the intestinal contractile responses to ranitidine with IC(50)values of 4.2 x 10(-5)M for the duodenum, 1.65 x 10(-5)M for the ileum and 3.2 x 10(-6)M for the ascending colon. These data show that cisapride may modify the contractile responses of the isolated rabbit intestine to ranitidine, having a potentiating effect up to a certain concentration and an antagonistic one at higher concentrations. In conclusion, co-administration of the above drugs may lead to enhanced or reduced intestinal motility.
本研究考察了H2受体拮抗剂雷尼替丁与促动力药西沙必利在离体兔肠上的药效学相互作用。雷尼替丁对十二指肠、回肠和升结肠制剂产生浓度依赖性的收缩效应,十二指肠的EC50值为1.35×10−4M,回肠为1.2×10−4M,升结肠为1.15×10−4M。西沙必利对雷尼替丁收缩效应的影响取决于所用西沙必利的浓度。因此,对于十二指肠和升结肠,西沙必利浓度在10−10至5×10−7之间,对于回肠浓度在10−6M以下时,可增强制剂对雷尼替丁的收缩反应。然而,在较高浓度时,西沙必利对肠道对雷尼替丁的收缩反应产生非竞争性抑制,十二指肠的IC50值为4.2×10−5M,回肠为1.65×10−5M,升结肠为3.2×10−6M。这些数据表明,西沙必利可能会改变离体兔肠对雷尼替丁的收缩反应,在一定浓度以下有增强作用,在较高浓度时有拮抗作用。总之,上述药物联合使用可能会导致肠道运动增强或减弱。