Nasser S S, Rees P J
Guy's Hospital, London, England.
Drug Saf. 1993 Jan;8(1):12-8. doi: 10.2165/00002018-199308010-00003.
Theophylline and its derivatives have been used in the treatment of asthma for over 50 years, but since the advent of more potent bronchodilators their use has become cloaked in controversy. Their continued existence results from their undoubted usefulness in severe acute asthma, nocturnal asthma, childhood asthma and moderate to severe chronic airflow limitation, and because of habitual use by physicians in other situations. The precise mechanism of action of theophylline remains uncertain. The role of phosphodiesterase inhibition and adenosine antagonism has been reviewed and the clinical significance of the anti-inflammatory action of theophylline discussed. Theophylline has unpredictable metabolism when first administered, and continued monitoring of drug concentrations is essential. Commonly encountered adverse effects may occur at therapeutic serum concentrations, frequently necessitating drug withdrawal. The overlapping therapeutic and toxic theophylline serum ranges can lead to life-threatening adverse effects at the upper end of the therapeutic range, especially in the elderly in whom special precaution is required.
茶碱及其衍生物用于治疗哮喘已有50多年，但自从更有效的支气管扩张剂问世以来，它们的使用一直存在争议。它们仍在使用是因为其在严重急性哮喘、夜间哮喘、儿童哮喘以及中度至重度慢性气流受限中具有毋庸置疑的效用，还因为医生在其他情况下的习惯性使用。茶碱的确切作用机制仍不确定。磷酸二酯酶抑制和腺苷拮抗的作用已得到综述，茶碱抗炎作用的临床意义也已被讨论。首次给药时，茶碱的代谢不可预测，持续监测药物浓度至关重要。治疗性血清浓度时可能会出现常见的不良反应，常常需要停药。茶碱治疗和中毒血清浓度范围重叠，在治疗范围上限可能导致危及生命的不良反应，尤其是在老年人中，对此需要特别预防。
