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Cloperastine is a centrally acting antitussive (cough suppressant) and antihistamine. It is used primarily for the relief of cough associated with upper respiratory tract infections and other conditions. The drug acts on the central nervous system, specifically affecting the cough center in the brainstem without depressing respiratory function or causing significant cardiocirculatory effects[1][2][3][5]. Its mechanism of action includes antagonism at histamine H1 receptor (antihistaminic), blockade of G protein-coupled inwardly rectifying potassium (GIRK) channels, sigma receptor agonism, and anticholinergic activity[3][5][6]. These combined actions contribute to its efficacy as an antitussive and its side effect profile, which may include sedation and thickening of bronchial secretions. Cloperastine was first introduced in Japan in 1972 and later marketed in several European countries[5]. It is available as various salts including hydrochloride and fendizoate.
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