The efficacy and selectivity of pirenzepine. Review and commentary.
The efficacy and selectivity of pirenzepine. Review and commentary.
复制标题
哌仑西平的功效和选择性。
DOI：
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发表时间：
1982
期刊：
影响因子：
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通讯作者：
P. Reilly
中科院分区：
文献类型：
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作者：
E. Texter;P. Reilly
哌仑西平是一种选择性结合胃粘膜M受体的新型抗胆碱能药物。我们回顾了溃疡患者的双盲治疗研究和临床药理学证据的愈合和选择性。在718例十二指肠溃疡患者和630例胃溃疡患者的试验中，100-150 mg/天剂量的溃疡愈合率在54-84%之间变化。这些试验的总副作用发生率为18.1%。在150 mg/天剂量下，口干发生率为13.5%，视力障碍发生率为6.3%，便秘发生率为2.6%。在临床药理学试验中，哌仑西平在100 mg/天剂量下中度抑制胃分泌，对唾液分泌和食管运动有轻微抑制作用。较高剂量产生预期的副交感神经阻滞特征，但不存在心脏加速。我们的结论是，哌仑西平在低剂量下，与经典的抗毒蕈碱药物相比，是相对选择性的胃分泌不足。在100-150 mg/天剂量的治疗试验中，它可能与副作用频率较低有关。口干和视觉障碍是最常见的副作用。选择性受剂量限制，迄今为止仅在每日100 mg分2次给药时得到证实。
Pirenzepine is a new anticholinergic agent which selectively binds to gastric mucosal muscarinic receptors. We reviewed the double-blind, therapeutic studies on ulcer patients and the clinical pharmacology for evidence of healing and selectivity. Healing rates of ulcer at doses of 100-150 mg/day varied between 54-84% in trials with 718 duodenal ulcer patients and 630 patients with gastric ulcer. Total side effects incidence in these trials was 18.1%. At 150 mg/day, there was 13.5% incidence of dry mouth, 6.3% incidence of visual disturbance and 2.6% incidence of constipation. In clinical pharmacology trials, pirenzepine moderately inhibited gastric secretion with a slight inhibition of salivary secretion and esophageal motility at 100 mg/day. Higher doses produced the expected parasympatholytic profile, except for the absence of cardioacceleration. We conclude that pirenzepine in low doses, compared to classical antimuscarinic drugs, is relatively selective for gastric hyposecretion. It may be associated with a lower frequency of side effects in therapeutic trials at doses of 100-150 mg/day. Dry mouth and visual disturbance are the most common side effects. Selectivity is dose limited and has so far been demonstrated only at a daily dosage of 100 mg, in 2 divided doses.