Bepotastine (besylate)

Bepotastine is an antagonist of the histamine H₁ receptor that is selective over H₃, α₁-, α₂-, and β-adrenergic, dopamine D_2long, serotonin 5-HT₂, muscarinic acetylcholine, and benzodiazepine receptors.¹ It reduces dye leakage from the nasal passages of rats acutely sensitized to an antigen (ED₅₀ = 0.03 mg/kg) and inhibits histamine-induced bronchoconstriction in the anesthetized dog (ED₅₀ = 3.2 µg/kg).^2,3 Bepotastine prevents conjunctival vascular hyperpermeability in a guinea pig model of conjunctivitis in a dose-dependent manner.⁴ Formulations containing bepotastine have been used in the treatment of itching associated with allergic conjunctivitis.

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1. Kato, M., Nishida, A., Aga, Y., et al. Pharmacokinetic and pharmacodynamic evaluation of central effect of the novel antiallergic agent betotastine besilate. Arzneimittelforschung. 47(10), 1116-1124 (1997).

2. Murata, T., Matsumoto, Y., Suzuki, T., et al. Effect of betotastine besilate (TAU-284), a novel anti-allergic agent, on experimental allergic rhinitis. Arerugi 46(7), 576-584 (1997).

3. Matsubara, S., Ono, C., Yamazaki, N., et al. Inhibitory effects of bepotastine, a novel anti-allergic drug on histamine-induced bronchoconstriction in anesthetized dogs. Yakuri to Chiryo 25(4), 895-900 (1997).

4. Kida, T., Fuji, A., Sakai, O., et al. Bepotastine besilate, a highly selective histamine H₁ receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in in vitro and in vivo experimental allergic conjunctivitis models. Exp. Eye Res. 91(1), 85-91 (2010).