RP64305 Ebastine

Ebastine, is a H1 antihistamine with low potential for causing drowsiness. It does not penetrate the blood–brain barrier to a significant amount and thus combines an effective block of the H1 receptor in peripheral tissue with a low incidence of central side effects, i.e. seldom causing sedation or drowsiness. After oral administration, ebastine undergoes extensive first-pass metabolism by hepatic cytochrome P450 3A4 into its active carboxylic acid metabolite, carebastine. This conversion is practically complete. Ebastine is a second-generation H1 receptor antagonist that is indicated mainly for allergic rhinitis and chronic idiopathic urticaria.

Histamine Receptor Inhibitors Related Products:

Pitolisant; Pitolisant oxalate; Loratadine; Bepotastine; Ciproxifan; Ciproxifan Maleate; Fexofenadine hydrochloride; Hydroxyzine dihydrochloride; Azatadine maleate; Betahistine dihydrochloride; Pitolisant hydrochloride

[1]. Tagawa, M., et al., Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-chlorpheniramine, a classical antihistamine. Br J Clin Pharmacol, 2001. 52(5): p. 501-9.

[2]. Bousquet, J., et al., A 12-week, placebo-controlled study of the efficacy and safety of ebastine, 10 and 20 mg once daily, in the treatment of perennial allergic rhinitis. Multicentre Study Group. Allergy, 1999. 54(6): p. 562-8.