Stacher G, Bauer P, Schmierer G, Steinringer H
Int J Clin Pharmacol Biopharm. 1979 Nov;17(11):442-8.
In two studies, each on 16 healthy volunteers, the effects of pirenzepine on esophageal and lower esophageal sphincter (LES) contractile activity were studied under double blind conditions. One study was carried out on subjects who had fasted, the other on subjects who had ingested a standard meal. Each subject underwent two experiments, one with i.m. injection of 0.2 mg/kg body weight pirenzepine, the other with an injection of solvent. Heart rate, respiratory rate, electroencephalogram, and reaction time to acoustical stimuli were recorded to control for cardiovascular, respiratory and central nervous effects respectively. Pirenzepine under both fasting and nonfasting conditions caused significant decreases in number, amplitude, and duration of swallow-contractions. LES pressures under both conditions were significantly lower after pirenzepine than after the solvent. Pirenzepine furthermore caused a significant heart rate deceleration and respiratory acceleration, as well as an increased power in the faster Beta- and decreased power in the Alpha-range of the EEG. In conclusion, pirenzepine inhibits esophageal and LES contractile activity and also affects the central nervous system by a direct or indirect mechanism. An application of pirenzepine in hypertensive states of the LES and the esophagus seems possible and deserves further investigation.
在两项研究中,每项研究均针对16名健康志愿者,在双盲条件下研究了哌仑西平对食管及食管下括约肌(LES)收缩活动的影响。一项研究针对禁食的受试者进行,另一项针对摄入标准餐食的受试者进行。每名受试者均接受两项实验,一项为肌肉注射0.2mg/kg体重的哌仑西平,另一项为注射溶剂。分别记录心率、呼吸频率、脑电图以及对听觉刺激的反应时间,以控制心血管、呼吸及中枢神经效应。在禁食和非禁食条件下,哌仑西平均导致吞咽收缩的次数、幅度及持续时间显著减少。在两种条件下,哌仑西平给药后LES压力均显著低于溶剂给药后。此外,哌仑西平导致显著的心率减慢和呼吸加速,以及脑电图中较快的β波功率增加和α波功率降低。总之,哌仑西平抑制食管及LES收缩活动,并且还通过直接或间接机制影响中枢神经系统。哌仑西平在LES和食管高血压状态中的应用似乎可行,值得进一步研究。