Davies R J, Bennett J, Osman J
J Asthma. 1984;21(6):443-50. doi: 10.3109/02770908409083225.
The inhalation of drugs that are active in the respiratory tract offers the ideal route of administration, since it results in the rapid delivery of appropriate concentrations with a much reduced risk of systemic adverse effects: Problems with regard to poor absorption from the gastrointestinal tract (sodium cromoglycate) or substantial effect on liver metabolism (verapamil) can be avoided. Certain drugs such as antihistamines and ketotifen may be more effective administered by inhalation since high concentrations with reduced unwanted effects can be achieved on the bronchial surface where, in allergic asthma, the critical initial interaction between sensitized mast cells (mucosal?) and allergen with subsequent mediator release occurs. Indeed inhaled verapamil has been shown to be effective in animal models of asthma but not in man. Systemically administered nifedipine gives partial and variable protection against induced asthma in man and its efficacy (with reduced cardiovascular effects) may well be improved by inhalation.
吸入作用于呼吸道的药物提供了理想的给药途径，因为它能迅速输送适当的浓度，同时大大降低全身不良反应的风险：可以避免胃肠道吸收不良（色甘酸钠）或对肝脏代谢有重大影响（维拉帕米）等问题。某些药物，如抗组胺药和酮替芬，通过吸入给药可能更有效，因为在支气管表面可以达到高浓度且副作用减少，在过敏性哮喘中，致敏肥大细胞（黏膜？）与变应原之间关键的初始相互作用以及随后的介质释放就发生在支气管表面。事实上，吸入维拉帕米已被证明在哮喘动物模型中有效，但在人体中无效。全身给药的硝苯地平对人体诱发的哮喘有部分且可变的保护作用，其疗效（同时降低心血管效应）通过吸入给药很可能会得到改善。
