Grainger S L, Smith S E
Br J Clin Pharmacol. 1983 Dec;16(6):623-6. doi: 10.1111/j.1365-2125.1983.tb02231.x.
Heart-rate responses to intravenous hyoscine butylbromide, atropine and physiological saline in cumulative dosage regimens have been recorded in six healthy subjects. Atropine sulphate induced bradycardia at low, and tachycardia at higher, dose levels whereas hyoscine butylbromide caused only tachycardia but with a flatter dose-response relationship. Exact potency ratios could not be calculated because of the differing dose-response curves. However, an approximate estimate from a comparison of equiactive doses at the upper part of the curve yielded a value less than one half that obtained from the drugs' affinity constants in guinea-pig ileum. The findings suggest that, in addition to its action as a muscarinic antagonist, hyoscine butylbromide is a ganglion blocker in man as it is in animals.
已记录了6名健康受试者对静脉注射累积剂量的丁溴东莨菪碱、阿托品和生理盐水的心率反应。硫酸阿托品在低剂量时引起心动过缓，在高剂量时引起心动过速，而丁溴东莨菪碱仅引起心动过速，但剂量-反应关系较平缓。由于剂量-反应曲线不同，无法计算确切的效价比。然而，通过比较曲线上部的等效活性剂量得出的近似估计值，其结果小于从豚鼠回肠中药物亲和力常数获得的值的一半。这些发现表明，丁溴东莨菪碱除了作为毒蕈碱拮抗剂起作用外，在人体中也是一种神经节阻滞剂，如同在动物中一样。
