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胍乙啶用于治疗高血压已有15年以上的历史,现在已有充分的最新资料,足以对此药的应用及其作用作适当评论。作用机理胍乙啶专门作用于外周交感神经系统。这是由于此药受转运去甲肾上腺素进入神经末梢的泵的作用。“去甲肾上腺素泵”把胍乙啶主动转运入神经原;抑制去甲肾上腺素泵亦就抑制胍乙啶的作用。胍乙啶进入肾上腺素能神经原后,与去甲肾上腺素贮存小泡结合,从神经末梢释放去甲肾上腺素。除耗竭去甲肾上腺素外,胍乙啶还阻断正常由神经兴奋引起的儿茶酚胺释放。静脉给予大量胍乙啶可使肾上腺素能神经原释放相当量的儿茶酚胺,引起高血压。但一次日服100毫克则无此作用。
Guanethidine has been used for more than 15 years in the treatment of hypertension and is now fully up-to-date on the adequacy of the drug’s application and its role in making appropriate comments. Guanethidine acts specifically on the peripheral sympathetic nervous system. This is due to the action of this drug by a pump that transports norepinephrine into the nerve endings. The “norepinephrine pump” actively transports guanethidine into the neurogen; inhibition of the norepinephrine pump also inhibits the action of guanethidine. After the guanethidine enters the adrenergic neurons, it binds to the norepinephrine storage vesicles and releases norepinephrine from the nerve endings. In addition to depleting norepinephrine, guanethidine also blocks the release of catecholamines normally caused by nerve excitability. Intravenous administration of a large number of guanethidine adrenergic neurons can release a considerable amount of catecholamines, causing hypertension. But once a day 100 mg is no such role.