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[茶碱疗法的复兴]

[The renaissance of theophylline therapy].

作者信息

Ahrens J

出版信息

Fortschr Med. 1982 Jun 17;100(23):1120-4.

PMID:6286438
Abstract

Deeper insight into the pharmacodynamics and pharmacokinetics of theophylline during the past 10 years led to the wide-spread use of the substance in the treatment of obstructive airway diseases. The effect of theophylline can be explained by different mechanisms of action, namely increase in cAMP and prostaglandins, redistribution of calcium, and blockade of purinergic receptors. Besides the known antiobstructive activity of theophylline ethylenediamine, its influence on the respiratory muscles is an essential clinical quality. The results of pharmacokinetic studies and routine determination of theophylline levels contributed to greatly improve the efficacy of theophylline therapy. At adequate doses, theophylline or theophylline ethylenediamine in sustained-release form constitutes the most effective long-term treatment of chronic asthma today. The pharmacological properties of ethylenediamine reinforce some of the more important effects of theophylline and improve tolerance. Combining the substance with beta-sympathomimetics elicits additive effects, while side effects are kept low.

摘要

在过去十年中,对茶碱的药效学和药代动力学有了更深入的了解,这使得该物质在阻塞性气道疾病的治疗中得到了广泛应用。茶碱的作用可通过不同的作用机制来解释,即增加环磷酸腺苷(cAMP)和前列腺素、钙的重新分布以及嘌呤能受体的阻断。除了已知的氨茶碱的抗阻塞活性外,其对呼吸肌的影响是一项重要的临床特性。药代动力学研究结果和茶碱水平的常规测定极大地提高了茶碱治疗的疗效。在适当剂量下,缓释形式的茶碱或氨茶碱是当今治疗慢性哮喘最有效的长期疗法。乙二胺的药理特性增强了茶碱的一些更重要的作用,并提高了耐受性。将该物质与β-拟交感神经药联合使用可产生相加作用,同时副作用保持在较低水平。

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