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Chloropyramine is a first-generation antihistamine of the ethylenediamine class, primarily used in several Eastern European countries for the treatment of allergic conditions such as allergic conjunctivitis, allergic rhinitis, bronchial asthma, angioedema (Quincke's edema), urticaria, and other atopic reactions. It is also indicated for allergic reactions to insect bites, food and drug allergies, and anaphylactic shock. Chloropyramine acts as a competitive reversible antagonist (or inverse agonist) at the histamine H1 receptor. By blocking this receptor, it inhibits vasodilation, increased vascular permeability, and tissue edema associated with histamine release. The drug also exhibits anticholinergic properties due to its ability to cross the blood-brain barrier; these effects contribute to side effects such as drowsiness and dry mouth[1][2][3][5][6]. In addition to its antihistaminic action in allergy management, preclinical data suggest that chloropyramine can inhibit Vascular endothelial growth factor receptor 3 and Focal adhesion kinase activity in vitro and reduce tumor growth in vivo[7].
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