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海索那林:对其药理特性及治疗效果的综述,尤其涉及哮喘方面

Hexoprenaline: a review of its pharmacological properties and therapeutic efficacy with particular reference to asthma.

作者信息

Pinder R M, Brogden R N, Speight T M, Avery G S

出版信息

Drugs. 1977 Jul;14(1):1-28. doi: 10.2165/00003495-197714010-00001.

Abstract

Hexoprenaline1, N,N-[2-(3,4-dihydroxyphenyl)-2-hydroxyethyl] hexamethyl-enediamine, sulphate is a selective beta2-adrenoreceptor agonist which is active in man as a bronchodilator by the oral or intravenous routes and by inhalation. It is indicated for use in the treatment of bronchospasm associated with obstructive airways diseases, including asthma, bronchitis and emphysema. Clinical experience and double-blind studies have established that hexoprenaline is an effective bronchodilator. It major advantage over many other many other brochodilators of equal efficacy is its generally low production of side-effects, particularly tremor, palptitations, and tachycardia. In comparative trials, it has generally been rated as superior to orciprenaline or trimetoquinol, but comparisons with salbutamol have provided equivocal results. Oral hexoprenaline was superior to fenoterol as long-term maintenance therapy is asthma, principally because its somewhat lesser bronchodilatory effects were more than compensated for by a lesser incidence of side-effects.

摘要

海索那林1,即N,N-[2-(3,4-二羟基苯基)-2-羟乙基]己二胺硫酸盐,是一种选择性β2肾上腺素能受体激动剂,通过口服、静脉注射和吸入途径对人体具有支气管扩张作用。它适用于治疗与阻塞性气道疾病相关的支气管痉挛,包括哮喘、支气管炎和肺气肿。临床经验和双盲研究已证实海索那林是一种有效的支气管扩张剂。与许多其他疗效相当的支气管扩张剂相比,它的主要优势在于其副作用通常较少,尤其是震颤、心悸和心动过速。在比较试验中,它通常被评为优于奥西那林或曲美托喹,但与沙丁胺醇的比较结果并不明确。在哮喘的长期维持治疗中,口服海索那林优于非诺特罗,主要是因为其支气管扩张作用稍弱,但副作用发生率较低,足以弥补这一不足。

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