Bukowskyj M, Nakatsu K, Munt P W
Ann Intern Med. 1984 Jul;101(1):63-73. doi: 10.7326/0003-4819-101-1-63.
Advances have recently been made in understanding the pharmacokinetics of theophylline. To correlate the new knowledge of theophylline pharmacokinetics with the drug's current status in therapy, we have critically reviewed the relevant investigations of the last 5 years. We consider data on its presumed mechanisms of action, factors affecting its clearance, its use in pregnancy, treatment of overdoses, and important drug interactions. Theophylline clearance is decreased by concomitant use of erythromycin, cimetidine, high-dose allopurinol, oral contraceptives, and caffeine. Clearance is increased by concomitant use of phenobarbital and phenytoin. Newly discovered actions of theophylline include dose-dependent improvement of diaphragmatic contractility, augmentation of ventilatory response to hypoxia, and sleep disturbances (especially with high-dose treatments). Points clinically relevant to the daily use of theophylline derivatives and the importance of sustained-release preparations are discussed. Theophylline continues to play a major role in therapy for reactive airways disease.
最近在了解茶碱的药代动力学方面取得了进展。为了将茶碱药代动力学的新知识与该药物目前的治疗现状联系起来，我们对过去5年的相关研究进行了严格审查。我们考虑了关于其假定作用机制、影响其清除率的因素、在妊娠期的使用、过量用药的治疗以及重要药物相互作用的数据。同时使用红霉素、西咪替丁、高剂量别嘌醇、口服避孕药和咖啡因会降低茶碱的清除率。同时使用苯巴比妥和苯妥英会增加清除率。茶碱新发现的作用包括剂量依赖性改善膈肌收缩力、增强对低氧的通气反应以及睡眠障碍（尤其是高剂量治疗时）。讨论了与茶碱衍生物日常使用临床相关的要点以及缓释制剂的重要性。茶碱在反应性气道疾病的治疗中继续发挥重要作用。
