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Tripelennamine is a first-generation antihistamine of the ethylenediamine class, primarily used to treat symptoms associated with allergies and the common cold, such as sneezing, runny nose, itching, watery eyes, hives, and rashes[1][2][3]. It acts as a selective histamine H1 receptor antagonist with low sedative action but can cause mild sedation and gastrointestinal irritation[2][3]. Tripelennamine competes with histamine for binding at H1 receptors on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. This antagonism blocks the effects of endogenous histamine—such as pruritus (itching), vasodilation, increased vascular permeability (leading to swelling), hypotension, flushing, headache, tachycardia (rapid heartbeat), bronchoconstriction (airway narrowing), and pain potentiation—thereby providing temporary relief from allergic symptoms[2][7]. It has little anticholinergic activity compared to other first-generation antihistamines but may act as a weak serotonin-norepinephrine-dopamine reuptake inhibitor[3]. Tripelennamine was originally marketed under the brand name Pyribenzamine by Novartis[3], is approved for both human and veterinary use[2], but has largely been replaced by newer antihistamines in clinical practice due to its side effect profile.
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