Londong W, Londong V, Meierl A, Voderholzer U
Chirurgische und Medizinische Kliniken Innenstadt, University of Munich, West Germany.
Gut. 1987 Jul;28(7):888-95. doi: 10.1136/gut.28.7.888.
Telenzepine is an analogue of pirenzepine with a higher potency and similar selectivity for M1-receptors in animals. In this placebo controlled, double blind, randomised study mean peptone stimulated gastric acid secretion (mean +/- SEM) of 10 male healthy subjects (58 +/- 6 mmol H+/3 h for placebo) was significantly and dose dependently inhibited by oral telenzepine (2 mg: 31 +/- 5, 3 mg: 23 +/- 5, 5 mg: 21 +/- 4 mmol H+/3 h). Telenzepine 3 and 5 mg were significantly stronger than pirenzepine 50 mg orally (37 +/- 8 mmol H+/3 h). Mean percentage acid inhibition was 37% for pirenzepine, and 48, 61, and 64% for 2, 3, and 5 mg telenzepine, respectively. Basal and peptone stimulated gastrin release was unaffected. Mean salivary output per three hours declined moderately from 156 +/- 45 g (placebo) to 136 +/- 45 g with pirenzepine and significantly to 88 +/- 28 g, 95 +/- 39 g and 39 +/- 13 g with telenzepine 2, 3, and 5 mg, respectively. There was a parallel effect on Na+, K+, Ca++ and amylase output in saliva. Near point vision was not altered by either drug. Pulse rates were lowered by both substances. Complaints of dry mouth were more frequent with telenzepine 5 mg. On a molar basis telenzepine proved to be a 25 and 50 times more potent inhibitor of gastric and salivary secretion, respectively.
替仑西平是哌仑西平的类似物，在动物体内对M1受体具有更高的效力和相似的选择性。在这项安慰剂对照、双盲、随机研究中，10名男性健康受试者（安慰剂组为58±6 mmol H⁺/3 h）经蛋白胨刺激后的胃酸分泌均值（均值±标准误），口服替仑西平后受到显著且剂量依赖性的抑制（2 mg：31±5，3 mg：23±5，5 mg：21±4 mmol H⁺/3 h）。替仑西平3 mg和5 mg口服时比哌仑西平50 mg（37±8 mmol H⁺/3 h）的抑制作用显著更强。哌仑西平的平均胃酸抑制率为37%，替仑西平2 mg、3 mg和5 mg的平均胃酸抑制率分别为48%、61%和64%。基础和蛋白胨刺激后的胃泌素释放未受影响。每三小时的平均唾液分泌量从安慰剂组的156±45 g适度下降至哌仑西平组的136±45 g，而替仑西平2 mg、3 mg和5 mg组则显著下降至88±28 g、95±39 g和39±13 g。对唾液中的Na⁺、K⁺、Ca⁺⁺和淀粉酶分泌也有类似影响。两种药物均未改变近点视力。两种物质均使脉搏率降低。服用替仑西平5 mg时口干的主诉更为常见。按摩尔计算，替仑西平对胃酸和唾液分泌的抑制效力分别是哌仑西平的25倍和50倍。
