Longmore J, Szabadi E, Bradshaw C M
Br J Clin Pharmacol. 1985 Mar;19(3):295-300. doi: 10.1111/j.1365-2125.1985.tb02646.x.
Twelve healthy male volunteers participated in five experimental sessions separated by weekly intervals. At the beginning of each session the subjects received one single oral dose of the following drugs, according to a double-blind, balanced cross-over design: binodaline hydrochloride (50 mg or 100 mg); amitriptyline hydrochloride (50 mg or 100 mg); lactose placebo. Salivation and resting pupil diameter were assessed before and 2 h after the ingestion of the drugs; baseline sweating, carbachol- or phenylephrine-evoked sweating were measured 2 h following drug taking. Binodaline, like placebo, had little effect on salivary output, whereas amitriptyline caused a dose-dependent decrease in salivation. None of the drugs caused any significant change in resting pupil diameter or in baseline sweating. Carbachol-evoked sweating did not differ significantly following the ingestion of binodaline or placebo; on the other hand responses to carbachol were significantly reduced following amitriptyline. Phenylephrine-evoked sweating was reduced by both binodaline and amitriptyline. The lack of effect of binodaline on salivation, resting pupil diameter, baseline and carbachol-evoked sweating is in agreement with the results of animal experiments indicating the lack of an interaction of this drug with cholinergic mechanisms. The reduction in phenylephrine-evoked sweating would be indicative of an alpha-adrenoceptor blocking property of this drug.
12名健康男性志愿者参加了5次实验，每次实验间隔一周。在每次实验开始时，受试者按照双盲、平衡交叉设计接受以下药物的单次口服剂量：盐酸比诺达林（50毫克或100毫克）；盐酸阿米替林（50毫克或100毫克）；乳糖安慰剂。在服药前和服药后2小时评估唾液分泌和静息瞳孔直径；在服药后2小时测量基础出汗、卡巴胆碱或去氧肾上腺素诱发的出汗。与安慰剂一样，比诺达林对唾液分泌影响很小，而阿米替林导致唾液分泌呈剂量依赖性减少。这些药物均未引起静息瞳孔直径或基础出汗的任何显著变化。服用比诺达林或安慰剂后，卡巴胆碱诱发的出汗没有显著差异；另一方面，服用阿米替林后对卡巴胆碱的反应显著降低。比诺达林和阿米替林均降低了去氧肾上腺素诱发的出汗。比诺达林对唾液分泌、静息瞳孔直径、基础出汗和卡巴胆碱诱发的出汗缺乏影响，这与动物实验结果一致，表明该药物与胆碱能机制缺乏相互作用。去氧肾上腺素诱发的出汗减少表明该药物具有α-肾上腺素能受体阻断特性。
