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直接作用的胆碱能激动剂在各个医学领域有许多治疗用途。胆碱酯类药物,包括乙酰胆碱,由于非选择性和短效作用而具有有限的临床实用性。尽管如此,乙酰胆碱和卡巴胆酯在眼科手术中以局部应用,用于诱导瞳孔缩小。毛果芸香碱,一种肌能受体和节后神经刺激剂,能有效治疗开角型青光眼,缓解放射治疗或干燥综合征引起的干燥口腔和干燥嘴巴。塞维替明,一种选择性M3受体激动剂,由于副作用较少,被优先选用作为唾液诱导剂。倍他乐克用于术后或产后尿潴留,神经源性膀胱问题,先天性大肠,以及胃食管反流症状。甲胆碱通过吸入途径用于识别非哮喘患者的支气管高反应性。
胆碱类生物碱,如亚碱乐因,对骨骼肌和血小板具有肌能受体和烟碱作用。尽管其对中枢神经系统有影响,亚碱乐因既不增强认知功能,也没有提供治疗效益。总之,直接作用的胆碱能激动剂在治疗特定医学状况中是至关重要的。然而,其有益使用是根据对选择性和潜在副作用的权衡来决定的。
直接作用的胆碱能激动剂包括胆碱酯(如乙酰胆碱、乙酰甲胆碱和氨甲胆碱)和生物碱(如毛果芸香碱和西维美林)。它们有多种治疗应用。
在眼科手术期间,乙酰胆碱用于收缩瞳孔。然而,其应用受到其非选择性和临时效应的限制。
乙酰甲胆碱刺激气道中的毒蕈碱受体。其吸入用于诊断支气管气道高反应性。气道狭窄的程度有助于诊断哮喘及其严重程度。
另一种毒蕈碱刺激剂 Bethanechol 可改善胃肠道和尿路收缩,缓解便秘和无法排尿。
含有毛果芸香碱(一种毒蕈碱和神经节刺激剂)的滴眼液用于降低眼压和治疗青光眼。
Cevimeline 是一种选择性的 M3 激动剂。它用于通过增加流涎和泪液分泌来帮助口干或眼睛干燥的患者。
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