Blair D A, Glover W E, Kidd B S, Roddie I C
Br J Pharmacol Chemother. 1960 Sep;15(3):466-75. doi: 10.1111/j.1476-5381.1960.tb01274.x.
After intra-arterial infusion of bretylium tosylate (12.5 mg.), the reflex changes in vasoconstrictor tone which normally occur in the forearm with body cooling, positive pressure breathing, the Valsalva manoeuvre and postural change were greatly reduced or abolished. Reflex vasodilatation mediated by cholinergic fibres in response to body heating or to emotional stress was little affected. It was concluded that bretylium can selectively block the activity of sympathetic noradrenergic fibres without causing a similar block of sympathetic cholinergic fibres. As the responses to intravenous or intra-arterial infusions of adrenaline or noradrenaline were not reduced after bretylium, it was concluded that bretylium interferes with the activity of noradrenergic fibres rather than with the activity of the noradrenaline released at the nerve ending. After bretylium infusion, forearm and hand blood flow did not often rise to levels characteristic of full release of vasoconstrictor tone. As infusion of bretylium into a nerve-blocked forearm resulted in a pronounced reduction in flow, it is concluded that bretylium also has a constrictor effect on blood vessels. The state of the vessels following an infusion of bretylium appears to depend on the balance between this constrictor action and the longer-acting sympathetic blocking effect.
静脉内输注甲苯磺酸溴苄铵(12.5毫克)后,通常在身体降温、正压呼吸、瓦尔萨尔瓦动作和体位改变时在前臂出现的血管收缩张力反射性变化大为减少或消失。由胆碱能纤维介导的对身体发热或情绪应激的反射性血管舒张几乎未受影响。得出的结论是,溴苄铵可选择性阻断交感去甲肾上腺素能纤维的活性,而不会对交感胆碱能纤维产生类似的阻断作用。由于在输注溴苄铵后,对静脉内或动脉内输注肾上腺素或去甲肾上腺素的反应并未减弱,因此得出结论,溴苄铵干扰的是去甲肾上腺素能纤维的活性,而非神经末梢释放的去甲肾上腺素的活性。输注溴苄铵后,前臂和手部血流量通常不会升高至血管收缩张力完全解除时的特征性水平。由于将溴苄铵输注到神经阻滞的前臂中会导致血流量明显减少,因此得出结论,溴苄铵对血管也有收缩作用。输注溴苄铵后血管的状态似乎取决于这种收缩作用与长效交感神经阻滞作用之间的平衡。