Baunack A R, Weihrauch T R
Department of Medicine and Development, Bayer AG. Wuppertal Fed. Rep. of Germany.
Arzneimittelforschung. 1991 Jun;41(6):595-602.
In this paper the pharmacodynamic effects of calcium channel blockers (verapamil, nifedipine, diltiazem, fendiline, nitrendipine, nimodipine, and nisoldipine) on esophageal motility in man and their clinical effects in patients with various forms of primary esophageal motility disorders are critically analysed and summarized. The evaluation of efficacy and safety is mainly focused on nifedipine (Bay a 1040, Adalat; CAS 21829-25-4), since it has been best documented clinical pharmacologically and therapeutically in this field. Nifedipine and--with varying potency--the other calcium antagonists reduce effectively the increased lower esophageal sphincter pressure (LESP) and abnormally high and prolonged peristaltic and nonperistaltic contractions in the esophageal body in patients with achalasia, diffuse esophageal spasm (DES), and other disorders which may cause angina-like chest pain and/or dysphagia. Pharmacodynamic effects on esophageal motility are closely correlated with the plasma concentration of nifedipine in healthy volunteers and in patients. However, a final judgement on the therapeutic value of these compounds in esophageal motor abnormalities cannot be given due to conflicting results from clinical studies with fairly small numbers of patients and varying study designs. Among the different calcium antagonists investigated nifedipine represents the best investigated and the most suitable compound for the treatment of primary hypertensive esophageal motor disorders.
本文对钙通道阻滞剂(维拉帕米、硝苯地平、地尔硫䓬、芬地林、尼群地平、尼莫地平和尼索地平)对人体食管动力的药效学作用及其在各种原发性食管动力障碍患者中的临床效果进行了批判性分析和总结。疗效和安全性评估主要集中在硝苯地平(拜耳a 1040,心痛定;CAS 21829-25-4),因为它在该领域的临床药理学和治疗方面有最充分的文献记载。硝苯地平以及其他钙拮抗剂(效力各异)能有效降低贲门失弛缓症、弥漫性食管痉挛(DES)和其他可能导致心绞痛样胸痛和/或吞咽困难的疾病患者食管下括约肌压力(LESP)升高以及食管体部异常高且持续的蠕动和非蠕动收缩。在健康志愿者和患者中,对食管动力的药效学作用与硝苯地平的血浆浓度密切相关。然而,由于患者数量相对较少且研究设计各异的临床研究结果相互矛盾,无法对这些化合物在食管运动异常中的治疗价值做出最终判断。在所研究的不同钙拮抗剂中,硝苯地平是研究最充分且最适合治疗原发性高血压性食管动力障碍的化合物。