General Description
Acrivastine is a second-generation, short-acting histamine H1 receptor antagonist belonging to the propylamine class, structurally related to triprolidine. Its structure features a pyridine ring, a propenyl group, and a carboxylic acid moiety, which confers zwitterionic properties.
Mechanism of Action
Acrivastine acts as a selective, competitive antagonist at peripheral H1 receptors, blocking histamine-induced vasodilation, increased vascular permeability, and sensory nerve stimulation. Its carboxylic acid group limits penetration across the blood-brain barrier, significantly reducing central nervous system effects. The drug has a rapid onset but a relatively short duration of action, requiring more frequent dosing compared to other second-generation antihistamines.
Application
Acrivastine is indicated for the symptomatic relief of seasonal allergic rhinitis and chronic idiopathic urticaria, effectively reducing sneezing, rhinorrhea, and pruritus. Its fast onset makes it suitable for on-demand use. The drug is approved in combination with pseudoephedrine and is generally well-tolerated, with drowsiness occurring at a slightly higher rate than with cetirizine or loratadine.