Lönnerholm G, Widerlöv E
Eur J Clin Pharmacol. 1975 Apr 4;8(3-4):233-40. doi: 10.1007/BF00567121.
Intravenous atropine sulphate (0.25, 0.40, 0.75 and 1.50 mg), atropine methylnitrate (0.08, 0.13 and 0.25 mg) and saline were given to 72 healthy medical students. The effects on heart rate and rhythm, systolic and diastolic blood pressure and salivary secretion were studied. Salivation was inhibited by all the doses of the two drugs. There was a clear dose-response relationship and methylatropine was about 3 times as potent as atropine. Heart rate was accelerated by 0.75 and 1.50 mg atropine, and 0.25 mg methylatropine, whereas 0.25 mg atropine and 0.08 and 0.13 mg methylatropine induced bradycardia, which was considered to be due to a peripheral action. It is suggested that the drugs act as partial agonists at muscarinic receptors. No clear effect on blood pressure was seen, except for the highest dose of atropine, after which the diastolic pressure was increased. 20 out of 59 subjects who received anticholinergics developed supra-ventricular arrhythmias; with both drugs periods of nodal rhythm were most common. They appeared shortly after the injection and usually lasted for a few minutes.
向72名健康医学生静脉注射硫酸阿托品(0.25、0.40、0.75和1.50毫克)、硝酸甲基阿托品(0.08、0.13和0.25毫克)和生理盐水。研究了这些药物对心率和心律、收缩压和舒张压以及唾液分泌的影响。两种药物的所有剂量均能抑制唾液分泌。存在明显的剂量反应关系,甲基阿托品的效力约为阿托品的3倍。0.75和1.50毫克阿托品以及0.25毫克甲基阿托品可使心率加快,而0.25毫克阿托品以及0.08和0.13毫克甲基阿托品可诱发心动过缓,这被认为是由外周作用引起的。提示这些药物在毒蕈碱受体上起部分激动剂的作用。除了最高剂量的阿托品使舒张压升高外,未观察到对血压有明显影响。59名接受抗胆碱能药物治疗的受试者中有20人出现室上性心律失常;两种药物引起的结性心律最为常见。它们在注射后不久出现,通常持续几分钟。