Parry M, Heathcote B V
Life Sci. 1982 Oct 4;31(14):1465-71. doi: 10.1016/0024-3205(82)90008-x.
The ability of pirenzepine and atropine, given i.v., to inhibit gastric acid and salivary secretion and increase pupil diameter has been assessed in the rat. Pirenzepine had a similar potency against acid secretion, ED 50 0.71 (0.41 to 1.1) mg.kg-1, and salivary secretion, ED 50 (0.43 to .59) mg.kg-1, whilst its potency was less in the eye, ED 50 1.8 (1.6 to 2.1) mg.kg-1. Atropine however, was more potent in reducing salivary secretion, ED 50 0.012 (0.010 to 0.016) mg.kg-1 and increasing pupil diameter, ED 50 0.028 (0.025 to 0.031) mg.kg-1 than in inhibiting gastric acid secretion, ED 50 0.056 (0.037 to 0.083) mg.kg-1. Therefore, that quantity of pirenzepine which inhibits gastric acid secretion by 50% will have only a slight effect on the eye and will inhibit salivary secretion by a similar magnitude. In contrast, the amount of atropine required to inhibit acid secretion by 50% will significantly increase pupil diameter and abolish salivary secretion.
已在大鼠中评估了静脉注射哌仑西平和阿托品抑制胃酸和唾液分泌以及扩大瞳孔直径的能力。哌仑西平对胃酸分泌的效力相似,半数有效剂量(ED50)为0.71(0.41至1.1)mg·kg-1,对唾液分泌的ED50为(0.43至0.59)mg·kg-1,而其在眼部的效力较低,ED50为1.8(1.6至2.1)mg·kg-1。然而,阿托品在减少唾液分泌(ED50为0.012(0.010至0.016)mg·kg-1)和扩大瞳孔直径(ED50为0.028(0.025至0.031)mg·kg-1)方面比抑制胃酸分泌(ED50为0.056(0.037至0.083)mg·kg-1)更有效。因此,能抑制50%胃酸分泌的哌仑西平剂量对眼睛只有轻微影响,且对唾液分泌的抑制程度相似。相比之下,抑制50%胃酸分泌所需的阿托品剂量会显著扩大瞳孔直径并消除唾液分泌。