Sagrada A, Schiavone A, Cefalá A, Trespi P, Giachetti A
Arch Int Pharmacodyn Ther. 1987 Jun;287(2):237-47.
The spasmolytic activity of N-Butyl Hyoscine (NBH) (1) has been investigated in conscious dogs provided with ileal or colonic Thiry fistulas in which motility was stimulated by intraluminal distension. In ileal motility experiments, phasic motility index (PMI), intestinal tonus, contraction frequency and heart rate were monitored. Intravenous administration of NBH (10 to 100 micrograms/kg) depressed PMI (ED50 35.1 micrograms/kg) and the other motility parameters. Heart rate increases were observed at 100 micrograms/kg. Application of NBH directly into the fistula (300 to 3000 micrograms/kg) caused a long-lasting, potent inhibition (31-72%) of PMI; tonus and contraction frequency were only slightly affected, while heart rate was not altered. When NBH was administered into an ileal fistula adjacent to the one from which motility was recorded, changes of PMI and other parameters were observed only after a massive dose of the drug (10000 micrograms/kg). In colonic fistula experiments, intraluminal NBH administration (300 to 3000 micrograms/kg) depressed colonic motility (39-59%), without affecting heart rate. It is concluded that NBH present in the intestine, although poorly absorbed, exerts local spasmolytic action.
已在装有回肠或结肠蒂里氏瘘管的清醒犬中研究了丁溴东莨菪碱(NBH)(1)的解痉活性,其中通过腔内扩张刺激运动。在回肠蠕动实验中,监测了相运动指数(PMI)、肠张力、收缩频率和心率。静脉注射NBH(10至100微克/千克)可降低PMI(ED50为35.1微克/千克)及其他运动参数。在100微克/千克时观察到心率增加。将NBH直接注入瘘管(300至3000微克/千克)可对PMI产生持久、强效的抑制作用(31%-72%);张力和收缩频率仅受到轻微影响,而心率未改变。当将NBH注入与记录运动的瘘管相邻的回肠瘘管时,仅在大剂量给药(10000微克/千克)后才观察到PMI和其他参数的变化。在结肠瘘管实验中,腔内给予NBH(300至3000微克/千克)可降低结肠运动(39%-59%),而不影响心率。得出的结论是,肠道内的NBH尽管吸收不良,但仍发挥局部解痉作用。