van Zwieten P A
Arch Int Pharmacodyn Ther. 1975 Mar;214(1):12-30.
From clinical experience it is known that the hypotensive action of clonidine and alpha-methyl-DOPA is antagonized by desipramine. This antagonism was investigated in detail in chloralose-anaesthetized cats. Both the centrally acting hypotensive agents and the tricyclic antidepressants where infused into the left vertebral artery. (1) The central hypotensive action clonidine was antagonized by desipramine, imipramine, amitriptyline, protriptyline and mianserine. For the inhibition of the hypotensive action of clonidine by protriptyline a parallel shift of the dose-response curve was obtained, indicating the possibility of a competitive antagonism. The central hypotensive action of alpha-methyl-DOPA was antagonized by desipramine and imipramine and that of amphetamine by imipramine. (2) The modest central hypotensive action of tricyclic antidepressants themselves and that of cocaine is explained by means of the inhibition of noradrenaline re-uptake in the CNS, brought about by these compounds. (3) It seems likely that the antagonism occurs at the level of central alpha-adrenoreceptors in the brain stem. (4) The antagonism probably reflects a general interaction between centrally acting hypotensive drugs and tricylclic antidepressants. The alpha-sympatholytic properties of the tricyclic antidepressants probably give rise to a blockade of the central alpha-adrenoreceptors, stimulated by clonidine, noradrenaline (via amphetamine) and alpha-methylnoradrenaline (from alpha-methyl-DOPA). The cocaine-like activity of antidepressants does not play a part.
从临床经验可知,地昔帕明可拮抗可乐定和α-甲基多巴的降压作用。在水合氯醛麻醉的猫身上对这种拮抗作用进行了详细研究。将中枢性降压药和三环类抗抑郁药都注入左椎动脉。(1)地昔帕明、丙咪嗪、阿米替林、普罗替林和米安色林可拮抗可乐定的中枢降压作用。对于普罗替林抑制可乐定的降压作用,得到了剂量-反应曲线的平行移动,表明存在竞争性拮抗的可能性。地昔帕明和丙咪嗪可拮抗α-甲基多巴的中枢降压作用,丙咪嗪可拮抗苯丙胺的中枢降压作用。(2)三环类抗抑郁药本身适度的中枢降压作用以及可卡因的中枢降压作用是通过这些化合物对中枢神经系统中去甲肾上腺素再摄取的抑制来解释的。(3)这种拮抗作用似乎发生在脑干中枢α-肾上腺素能受体水平。(4)这种拮抗作用可能反映了中枢性降压药与三环类抗抑郁药之间的一般相互作用。三环类抗抑郁药的α-交感神经阻滞特性可能导致对可乐定、去甲肾上腺素(通过苯丙胺)和α-甲基去甲肾上腺素(来自α-甲基多巴)刺激的中枢α-肾上腺素能受体的阻滞。抗抑郁药的可卡因样活性不起作用。