A comment on β2-agonists and their use in asthma
A comment on β2-agonists and their use in asthma
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关于 β2 激动剂及其在哮喘中的应用的评论
DOI：
10.1016/0165-6147(83)90290-0
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发表时间：
1983
影响因子：
13.8
通讯作者：
R. Goldie
中科院分区：
文献类型：
--
作者：
J. Paterson;K. Lulich;R. Goldie
Introduction A number of pathological changes contribute to the reduction of airflow in asthma. They include constriction of bronchial smooth muscle, intense oedema of the airways wall and obstruction of airways with mucous plugsL The use of bronchodilator drugs in asthma has recently been comprehensively reviewed./3-Adrenoceptor agonists (/3-agonists) are the most widely used group of bronchodilators. They may be given orally or by injection, but are most frequently taken by metered-dose aerosol./3-Agonists reduce airways obstruction by causing relaxation of bronchial smooth muscle and also stimulate mucociliary transport, reverse bronchial venoconstricdon and inhibit the allergic release of chemical mediators such as histamine from mast cellsL It is generally considered that the most important of these effects is relaxation of airways smooth muscle which is therefore the property most frequently studied in experimental animals a. In 1967, Lands and his colleagues proposed the existence of two distihct types of/3-adrenoceptors which they named/31 and/3~ and many studies have since supported this concept s. Some of the responses initiated by either/31-or/3~. adrenoceptors and the properties of these subtypes are summarized in Table I.In the mid 1960s there was considerable concern regarding the increased death rate in asthmatics and its correlation with increased use of isoprenaline aerosols. It is now believed that these deaths were most likely due to delays in the introduction of additional therapy in patients whose clinical state was deterioratingL However, at that time, these deaths were thought to have been principally caused by excessive cardiac stimulation (ill-effect) in susceptible individuals who used inordinate amounts of isoprenaline for its bronchodilator activity (/3~-effect). In an attempt to minimize the extent of such overflow cardiac stimulation, the pharmaceutical industry began to develop agonists that were selective for/3~-adrenoceptors.
