Cazzola M, Matera M G, Liccardi G, Sacerdoti G, D'Amato G, Rossi F
Divisione di Pneumologia ed Allergologia, Ospedale A. Cardarelli, Napoli, Italy.
Pulm Pharmacol. 1994 Apr;7(2):91-7. doi: 10.1006/pulp.1994.1010.
Muscarinic M1-receptor antagonists can prevent the induction of a long-lasting excitatory postsynaptic potential in autonomic ganglia. As the prolonged occupation of M1-receptors is a possible protective mechanism against vagal overstimulation, M1-antagonists might prove to be effective in preventing nocturnal wheeze. The aim of the present study was to investigate whether telenzepine, an M1-selective muscarinic receptor antagonist, administered orally at different doses (1.5 mg, 3 mg, 5 mg) for one week, reduced airway obstruction in patients with nocturnal asthma in comparison with placebo. Peak expiratory flow rate (PEFR) difference between each study medication (arithmetic means from values on days 4, 5 and 6) and baseline at 6 a.m. and at midnight on day 5 did not differ significantly. Treatment with placebo nocte (at night, 9 p.m.), or telenzepine 1.5 mg nocte, telenzepine 3 mg nocte and telenzepine 5 mg nocte did not affect significantly the 24-h time course of PEFR. The results of this study indicate that the use of telenzepine via the oral route at a dose of up to 5 mg is not effective in preventing nocturnal asthma.
毒蕈碱M1受体拮抗剂可防止自主神经节中持久兴奋性突触后电位的诱导。由于M1受体的长期占据是一种可能的抗迷走神经过度刺激的保护机制，M1拮抗剂可能被证明在预防夜间喘息方面有效。本研究的目的是调查与安慰剂相比，连续一周口服不同剂量（1.5毫克、3毫克、5毫克）的M1选择性毒蕈碱受体拮抗剂替仑西平是否能减轻夜间哮喘患者的气道阻塞。每种研究药物（第4、5和6天数值的算术平均值）与第5天上午6点和午夜基线之间的呼气峰值流速（PEFR）差异无显著统计学意义。夜间服用安慰剂、夜间服用1.5毫克替仑西平、夜间服用3毫克替仑西平和夜间服用5毫克替仑西平对PEFR的24小时时间进程均无显著影响。本研究结果表明，口服剂量高达5毫克的替仑西平对预防夜间哮喘无效。
