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The issues (aspects) of bronchodilator and tocolytic actions of β₂-adrenoceptor agonists are reviewed. The data on short-acting and new long-acting β₂-agonists are presented. It is marked that it is necessary to use long-acting β₂-agonists and glucocorticosteroids concomitantly. Examples of clinical efficacy of locally produced β₂-adrenoceptor agonist salbutamol hemisuccinate in various dosage forms used as a bronchodilator for treatment of bronchopulmonary diseases, and also as a tocolytic for habitual noncarrying of pregnancy are given.