Davis W J, Feldman B R
Cutis. 1976 Jun;17(6):1091-8.
The understanding of the properties of adrenergic receptors and modification of ring and the N-alkyl side chain constituents have resulted in adrenergic agents with a high degree of specificity for the lung and few cardiac and central nervous system stimulating problems. These agents are useful by aerosol and oral routes, alone and in addition to theophylline for asthma. Theophylline, which acts to increase cyclic AMP by inhibition of phosphodiesterase and beta 2 adrenergic agents which increase cyclic AMP by stimulating adenylate cyclase, are the mainstays of asthma therapy. Therapy is usually begun with theophylline. Persistent symptoms with adequate theophylline levels (10-20 mug/ml) indicates the need for a beta 2 adrenergic agent by aerosol or orally as a supplement. Occasional patients will not tolerate theophylline in any preparation and can be treated with beta 2 adrenergic agents with success. The future holds great promise for improved and safer beta 2 adrenergic agents which will offer the physician a more effective means of treating asthma.
对肾上腺素能受体特性的了解以及对环和N-烷基侧链成分的修饰,已产生了对肺部具有高度特异性且几乎没有心脏和中枢神经系统刺激问题的肾上腺素能药物。这些药物通过气雾剂和口服途径单独使用或与茶碱联合用于治疗哮喘均有效。茶碱通过抑制磷酸二酯酶来增加环磷酸腺苷(cAMP),而β2肾上腺素能药物则通过刺激腺苷酸环化酶来增加cAMP,它们是哮喘治疗的主要药物。治疗通常从使用茶碱开始。在茶碱水平充足(10 - 20微克/毫升)的情况下仍有持续症状,表明需要通过气雾剂或口服补充β2肾上腺素能药物。偶尔有患者无法耐受任何制剂中的茶碱,可用β2肾上腺素能药物成功治疗。未来有望研发出更优质、更安全的β2肾上腺素能药物,为医生提供更有效的哮喘治疗手段。