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JoVE Core
Pharmacology
肾上腺素激动剂:混合作用药物
肾上腺素激动剂:混合作用药物
JoVE Core
Pharmacology
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JoVE Core Pharmacology
Adrenergic Agonists: Mixed-Action Agents

6.7: 肾上腺素激动剂:混合作用药物

1,372 Views
01:28 min
September 22, 2023
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Please note that some of the translations on this page are AI generated. Click here for the English version.

Overview

混合作用肾上腺素激动剂,如麻黄碱和假麻黄碱,对肾上腺素受体直接和间接产生影响。这些药物刺激肾上腺素受体,并间接释放储存的神经递质,增强肾上腺素反应。

麻黄碱和假麻黄碱缺乏儿茶酚胺基团,使它们不容易被代谢酶降解。它们具有更高的口服生物利用度和亲脂性,从而延长作用时间。它们的反应会受到儿茶酚胺耗竭剂(如胍乙啶或利血平)的先前治疗的影响从而减弱。

麻黄碱,第一种口服活性的交感神经兴奋剂,用于治疗哮喘和鼻塞。然而,它有潜在的滥用风险,并且有更安全的替代品可供选择,因此使用受限。假麻黄碱主要用作鼻腔解充血剂,但由于潜在的非法合成甲基苯丙胺的风险,受到严格管制。

Transcript

混合作用肾上腺素能激动剂通过刺激肾上腺素能受体直接起作用,并通过从神经末梢释放储存的儿茶酚胺间接起作用。

与内源性儿茶酚胺不同,混合作用激动剂缺乏儿茶酚部分,使它们成为代谢酶的不良底物,从而延长其作用持续时间。

麻黄碱和伪麻黄碱都表现出极好的口服生物利用度和 CNS 渗透性,但效果不如儿茶酚胺。

麻黄碱 - 从麻黄植物中分离 - 已被用作治疗哮喘的口服活性拟交感神经药。

由于麻黄碱会引起心脏刺激和血管收缩,因此用于治疗麻醉引起的低血压。然而,它是一种比异丙肾上腺素或肾上腺素效果较差的支气管扩张剂。

此外,它的中枢刺激作用是其作为性能增强剂被滥用的原因。

伪麻黄碱是一种具有更多间接作用的麻黄碱异构体,口服有效且对 CNS 的影响较小。它主要用作减充血剂。

由于它通常用作非法甲基苯丙胺生产的前体,因此其销售受到严格监管。

Explore More Videos

肾上腺素能激动剂 混合作用剂 麻黄碱 伪麻黄碱 肾上腺素能受体 神经递质 口服生物利用度 亲脂性 作用持续时间 拟交感神经 哮喘治疗 鼻塞 继发性滥用 鼻减充血剂 甲基苯丙胺合成

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