Weinberger M, Hendeles L
J Allergy Clin Immunol. 1985 Aug;76(2 Pt 2):277-84. doi: 10.1016/0091-6749(85)90642-6.
Four critical issues related to theophylline are addressed: What is theophylline? Why use it? How should it be used? Who should receive it? Theophylline is a methylated xanthine with established clinical benefit as maintenance therapy for chronic asthma. In fact, evolution of our knowledge of the pharmacodynamics and pharmacokinetics of theophylline has made this drug the most effective nonsteroidal prophylactic used for chronic asthma. Theophylline has the potential for serious toxicity at excessive serum concentrations. Nonetheless, its major justification for use today, when so many other asthma medications have become available, is because of the high degree of efficacy that can be attained with appropriate use. The optimal likelihood of maximal safe effect is attained with maintenance of serum concentrations within the 10 to 20 micrograms/ml therapeutic range. Dosage should be individualized by clinical titration, guided by measurement of serum concentrations, and continued only if well tolerated; selection of appropriate products and dosing intervals permits maintenance of acceptably stable serum concentrations. Asthma in patients only intermittently symptomatic, regardless of severity, is probably best treated by intervention measures with inhaled bronchodilators, supplemented when necessary by short-term use of oral corticosteroids, rather than by long-term maintenance therapy. Theophylline therapy in patients with obstructive pulmonary disease other than asthma should generally be highly selective and based on clearly demonstrable clinical benefit.
什么是茶碱?为什么使用它?应该如何使用?谁应该使用它?茶碱是一种甲基化黄嘌呤,作为慢性哮喘的维持治疗药物,具有确切的临床疗效。事实上,我们对茶碱药效学和药代动力学认识的发展,使这种药物成为用于慢性哮喘最有效的非甾体类预防性药物。当血清浓度过高时,茶碱有产生严重毒性的可能。尽管如此,在如今有如此多其他哮喘药物可供使用的情况下,它目前使用的主要理由是,合理使用时可获得高度的疗效。通过将血清浓度维持在10至20微克/毫升的治疗范围内,可实现最大安全效果的最佳可能性。剂量应通过临床滴定个体化,以血清浓度测量为指导,只有在耐受性良好的情况下才继续用药;选择合适的产品和给药间隔可维持可接受的稳定血清浓度。对于仅有间歇性症状的哮喘患者,无论严重程度如何,可能最好通过吸入支气管扩张剂进行干预治疗,必要时辅以短期口服糖皮质激素,而非长期维持治疗。对于哮喘以外的阻塞性肺疾病患者,茶碱治疗通常应具有高度选择性,并基于明确可证的临床益处。