Matsumura T, Yada S, Miyoshi Y, Komi N
First Department of Surgery, School of Medicine, University of Tokushima.
Nihon Shokakibyo Gakkai Zasshi. 1991 Oct;88(10):2663-70.
Fundamental study in dogs have shown that the synthetic protease inhibitor has pharmaceutical properties characterized by effect on motility of the sphincter of Oddi. Synthetic protease inhibitors, gabexate mesilate and nafamostat mesilate have effects on motility of the sphincter of Oddi in dogs. The motor effect of synthetic protease inhibitor on the sphincter of Oddi has been investigated by manometric evaluation. Immediately after intravenous administration of gabexate mesilate (5, 10, 50, and 100 mg/kg/h) the motility of the sphincter of Oddi was inhibited dose-dependently, on the other hand after intravenous administration of nafamostat mesilate (0.5, 1, and 5 mg/kg/h) motility of the sphincter of Oddi was accelerated. Therefore it was suggested that these results shown some considerable problems in clinical use.
对狗的基础研究表明,合成蛋白酶抑制剂具有药物特性,其特点是对Oddi括约肌的运动有影响。合成蛋白酶抑制剂甲磺酸加贝酯和甲磺酸萘莫司他对狗的Oddi括约肌运动有影响。通过测压评估研究了合成蛋白酶抑制剂对Oddi括约肌的运动作用。静脉注射甲磺酸加贝酯(5、10、50和100毫克/千克/小时)后,Oddi括约肌的运动立即受到剂量依赖性抑制,另一方面,静脉注射甲磺酸萘莫司他(0.5、1和5毫克/千克/小时)后,Oddi括约肌的运动加速。因此,有人认为这些结果在临床应用中存在一些相当大的问题。