Soni N, Kam P
Anaesth Intensive Care. 1982 May;10(2):120-6. doi: 10.1177/0310057X8201000205.
4-aminopyridine is the first of the aminopyridines to be used in clinical practice. It blocks potassium channels and thereby increases acetylcholine, and possibly noradrenaline, release at nerve terminals. In man the drug has a significant action at the neuromuscular junction, but has little effect on the autonomic nervous system or muscle (smooth, skeletal, or cardiac) although such actions have been demonstrated in animals. It may be clinically useful in the reversal of nondepolariser blockade and a role in antibiotic associated block has been proposed. It may be used effectively as an analeptic agent. It appears to be a useful therapeutic agent in myasthenia gravis and Eaton Lambert syndrome, although of limited use in botulism. It effects on the central nervous system are considerable. These account for the major side effects of the drug which include tremor, excitability and convulsions.
4-氨基吡啶是氨基吡啶类中首个用于临床实践的药物。它可阻断钾通道，从而增加乙酰胆碱的释放，可能还会增加去甲肾上腺素在神经末梢的释放。在人体中，该药物在神经肌肉接头处有显著作用，但对自主神经系统或肌肉（平滑肌、骨骼肌或心肌）几乎没有影响，尽管在动物实验中已证实有此类作用。它在临床上可能有助于逆转非去极化肌松阻滞，并且有人提出它在抗生素相关性阻滞中也有作用。它可有效地用作苏醒剂。在重症肌无力和伊顿-兰伯特综合征中，它似乎是一种有用的治疗药物，尽管在肉毒中毒中的用途有限。它对中枢神经系统的影响相当大。这些导致了该药物的主要副作用，包括震颤、兴奋性增高和惊厥。
