Cloperastine | 合法藥品大搜索

Cloperastine (INN) or cloperastin, also known as cloperastine hydrochloride (JAN) (brand names Hustazol, Nitossil, Seki) and cloperastine fendizoate (or hybenzoate), is an antitussive and antihistamine that is marketed as a cough suppressant in Japan, Hong Kong, and in some European countries.[1][2][3] It was first introduced in 1972 in Japan, and then in Italy in 1981.[4]

Adverse effects may include sedation, drowsiness, heartburn, and thickening of bronchial secretions.[5]

The precise mechanism of action of cloperastine is not fully clear, but several different biological activities have been identified for the drug, of which include: ligand of the σ1 receptor (Ki = 20 nM) (likely an agonist),[6] GIRK channel blocker (described as "potent"),[7][8][9][10] antihistamine (Ki = 3.8 nM for the H1 receptor),[3][6] and anticholinergic.[3][11] It is thought that the latter two properties contribute to side effects, such as sedation...