Bilastine is a non-sedating, long-acting H1 receptor selective antagonist. Its effects are mediated via selective inhibition of peripheral H1-receptors. It shows moderate to high affinity for histamine H1-receptors and no affinity for muscarinic, serotonergic, dopaminergic and noradrenergic receptors.
Bilastine inhibits histamine induced flare skin reactions for 24 hours following single doses. Therefore, it shows very good efficacy and safety profile in treating allergic conditions.