McFadden E R
Am J Med. 1985 Dec 20;79(6A):1-4. doi: 10.1016/0002-9343(85)90079-8.
Theophylline is a medium-potency bronchodilator that is useful in the treatment of reversible airway obstruction from any cause. It also improves contraction of the diaphragm, accelerates mucociliary transport, lowers pulmonary artery pressures, and limits the release of the mediators of immediate hypersensitivity from mast cells. The pharmacologic effects correlate closely with the plasma concentration of this drug, and within the defined therapeutic limits, only minor adverse effects occur. The dose of theophylline required to achieve therapeutic plasma levels varies considerably between subjects, mainly because of differences in clearance. The latter varies with age, smoking, alterations in hepatic function, cardiac failure, viral infections, and concurrent administration of other drugs. For the treatment of acute symptoms, either intravenous administration or a rapidly absorbed compound such as uncoated tablets or liquids is required. For the long-term management of reversible airway obstruction, sustained-release theophyllines are available. These formulations maintain therapeutic serum theophylline concentrations for prolonged periods, permitting longer dosing intervals and improved patient compliance.
茶碱是一种中等强度的支气管扩张剂，可用于治疗任何原因引起的可逆性气道阻塞。它还能改善膈肌收缩，加速黏液纤毛运输，降低肺动脉压，并限制肥大细胞释放速发型超敏反应介质。该药物的药理作用与血浆浓度密切相关，在规定的治疗范围内，仅会出现轻微的不良反应。达到治疗性血浆水平所需的茶碱剂量在个体之间差异很大，主要是因为清除率不同。清除率会因年龄、吸烟、肝功能改变、心力衰竭、病毒感染以及同时使用其他药物而有所变化。对于急性症状的治疗，需要静脉给药或使用如未包衣片剂或液体等吸收迅速的化合物。对于可逆性气道阻塞的长期管理，有缓释茶碱制剂可供使用。这些制剂可长时间维持治疗性血清茶碱浓度，允许更长的给药间隔并提高患者的依从性。
