Walan A
Clin Gastroenterol. 1984 May;13(2):473-99.
Anticholinergic agents are most often divided into tertiary and quaternary ammonium compounds. Tertiary ammonium agents are fully and rapidly absorbed. Quaternary ammonium agents are slowly and incompletely absorbed, but do not cross the blood-brain barrier, or do so to a very limited degree, and have a very low rate of central nervous system side-effects. There are probably subclasses of cholinergic receptors, and anticholinergic agents have different affinities for these. Anticholinergics can decrease the basal acid secretion as well as secretion stimulated by histamine, pentagastrin, insulin or food. Combined therapy with antacids and anticholinergics will give a more long-lasting decrease in acidity than with either drug alone. The reported controlled studies with anticholinergic agents suggest that they can induce healing of duodenal ulcer to the same degree as cimetidine but at the cost of more frequent side-effects. Except for the studies on pirenzepine there are, however, too few studies in which anticholinergics have been compared with histamine H2-receptor antagonists; thus the place of anticholinergics in the treatment of an active duodenal ulcer is not clear. In doses of not less than 100 mg daily, pirenzepine is a candidate-drug for the short-term treatment of duodenal ulcer. At these doses, side-effects of dry mouth and visual disturbance are, however, rather frequent, and more serious side-effects such as urinary retention do also occur. More studies with both the conventional anticholinergics and pirenzepine, with emphasis not only on the desired effects but also on side-effects, are needed before anticholinergics can be taken into consideration as alternatives to histamine H2-receptor antagonists for healing and maintenance treatment. There is some evidence that long-term treatment with anticholinergic agents can decrease recurrences and complications of peptic ulcer disease. Even if there are some encouraging reports on the combination of anticholinergics and antacids, we need more such studies with lower doses of antacids and lower doses of anticholinergics before this combination therapy can be regarded as an equally good alternative to histamine H2-receptor antagonists for ulcer healing and symptom relief.
抗胆碱能药物通常分为叔铵化合物和季铵化合物。叔铵类药物能被完全且快速吸收。季铵类药物吸收缓慢且不完全，但不会穿过血脑屏障，或者仅有极少量能穿过，其引起中枢神经系统副作用的发生率极低。胆碱能受体可能存在不同亚类，抗胆碱能药物对这些亚类具有不同的亲和力。抗胆碱能药物可减少基础胃酸分泌以及由组胺、五肽胃泌素、胰岛素或食物刺激引起的胃酸分泌。与单独使用任何一种药物相比，抗酸剂与抗胆碱能药物联合治疗能使胃酸度降低的持续时间更长。已报道的关于抗胆碱能药物的对照研究表明，它们能诱导十二指肠溃疡愈合，程度与西咪替丁相同，但副作用更频繁。然而，除了关于哌仑西平的研究外，将抗胆碱能药物与组胺H2受体拮抗剂进行比较的研究太少；因此，抗胆碱能药物在治疗活动性十二指肠溃疡中的地位尚不清楚。每日剂量不少于100毫克时，哌仑西平是短期治疗十二指肠溃疡的候选药物。然而，在这些剂量下，口干和视觉障碍等副作用相当常见，也会出现诸如尿潴留等更严重的副作用。在将抗胆碱能药物作为组胺H2受体拮抗剂的替代药物用于溃疡愈合和维持治疗之前，需要对传统抗胆碱能药物和哌仑西平进行更多研究，不仅要关注预期效果，还要关注副作用。有证据表明，抗胆碱能药物长期治疗可降低消化性溃疡疾病的复发率和并发症。即使有一些关于抗胆碱能药物与抗酸剂联合使用的令人鼓舞的报告，但在这种联合治疗可被视为与组胺H2受体拮抗剂在溃疡愈合和症状缓解方面同样好的替代方案之前，我们还需要更多使用更低剂量抗酸剂和更低剂量抗胆碱能药物的此类研究。
