Stacher G, Havlik E, Bergmann H, Schmierer G, Winklehner S
Scand J Gastroenterol Suppl. 1982;72:153-8.
Pirenzepine (PIR), in contrast to classical antimuscarinic drugs, shows heterogeneity of binding that corresponds with the pharmacological activity: gastric secretion is inhibited by low doses, whereas higher doses are needed to inhibit gastrointestinal motility. This study investigated the effects of oral PIR on gastric emptying and antral motor activity. 20 healthy men (mean age 24.9 yr) participated in two experimental sessions, one week apart. According to a cross-over double blind design they received, three and a half days prior to the studies, either 50 mg PIR twice daily or placebo (PLA). A semisolid test meal labelled with 150 MBq 99mTc hSA was administered. A gamma camera coupled to a computer monitored modulation depth (MD), frequency (FR), and propagation velocity (PV) of antral contractions together with gastric emptying rate (GE) according to a modification of Akkerman's technique. PIR decreased MD (PLA: 21.2 +/- 1.7 SEM%; PIR: 17.2 +/- 1.5%; P less than 0.005) and increased FR (PLA: 3.12 +/- 0.05 cycles/min; PIR: 3.29 +/- 0.07 c/min; P less than 0.005) significantly whereas PV was accelerated (PLA: 2.9 +/- 0.2 mm/sec; PIR: 3.1 +/- 0.3 mm/sec; n.s.) and GE delayed only slightly (PLA: 50.4 +/- 8.5 kcpm; PIR: 35.5 +/- 6.0 kcpm; n.s.). PIR produced more frequent stools in three and accommodation difficulties and a dry mouth in each two subjects. PLA caused no side effects.
PIR delays GE insignificantly despite of considerable effects on antral motility.
与传统抗毒蕈碱药物不同,哌仑西平(PIR)显示出与药理活性相对应的结合异质性:低剂量可抑制胃酸分泌,而抑制胃肠动力则需要更高剂量。本研究调查了口服PIR对胃排空和胃窦运动活性的影响。20名健康男性(平均年龄24.9岁)参加了两个实验阶段,间隔一周。根据交叉双盲设计,在研究前三天半,他们每天两次接受50mg PIR或安慰剂(PLA)。给予标记有150MBq 99mTc hSA的半固体试验餐。根据Akkerman技术的改进,用与计算机相连的γ相机监测胃窦收缩的调制深度(MD)、频率(FR)和传播速度(PV)以及胃排空率(GE)。PIR显著降低MD(PLA:21.2±1.7 SEM%;PIR:17.2±1.5%;P<0.005)并增加FR(PLA:3.