论文部分内容阅读
治疗消化性溃疡的新药不断问世,有些已投用于临床。大部分是以前使用之药品的第二代。常用的抗胆硷药因其副作用而在应用上受到限制,所以人们始终未放弃寻觅新抗胆硷药的努力。有人观察一组16例十二指肠溃疡病患者夜间服用anisotrpine methylbromide 80毫克,白天服制酸剂。在2、4、6周后各治愈11、13和14例。而服安慰剂的14例患者在同期内各治愈6、8和11例。pirenzepine为首选的抗胆硷药,无明显的H_2—受体阻滞活性,系3环状的、纯抗毒蕈硷药物。但与3环状的镇静剂不同,pirenzepine亲水性强,不易透过血脑屏障,对中枢神经系统几无影响。常规剂量对瞳孔、膀胱、肠道及心脏的影响甚微,提示pirenzepine可能有选择性抗毒蕈硷的性质。亚细胞研究提示毒蕈硷受体有不同的亚纲(subclass)。这些亚纲的密度在器官分布上有差异。因此结合pirenzepine的能力亦有强弱之分。平滑肌及心脏亲和力低,而外分泌腺亲和力高。
New drugs for the treatment of peptic ulcer continue to come out, some have been put into clinical use. Most are the second generation of previously used drugs. Commonly used anticholinergic drugs are limited in their application due to their side effects, so people have not given up their efforts to find new anticholinergics. It was observed in a group of 16 patients with duodenal ulcer patients taking anisotrpine methylbromide 80 mg at night during the day antacid. In 2, 4, 6 weeks after the treatment of 11,13 and 14 cases. In the same period, 14 patients who took placebo cured 6, 8 and 11 patients respectively. Pirenzepine is the preferred anticholinergic drug, with no apparent H 2 -receptor blocker activity, a 3-ring, pure anti-muscarinic drug. But unlike the 3-ring sedatives, pirenzepine is highly hydrophilic and difficult to penetrate the blood-brain barrier and has little effect on the central nervous system. Routine doses have little effect on pupils, bladder, gut and heart, suggesting that pirenzepine may have selective anti-muscarinic properties. Subcellular studies suggest that muscarinic receptors have different subclasses. The density of these subclasses varies in organ distribution. Therefore, the ability to combine pirenzepine also has the strength of the points. Smooth muscle and cardiac affinity low, while the high affinity of exocrine glands.