Bepotastine was approved in Japan for use in the treatment of allergic rhinitis and urticaria/pruritus in July 2000 and January 2002, respectively. The ophthalmic solution is FDA-approved since Sept 8, 2009.
Product Details
Molecular Formula
C27H31ClN2O6S
Molecular Weight
547.1
Standard
JP
Uses
(1) Bepotastine has a role as an H1-receptor antagonist and an anti-allergic agent. Bepotastine ophthalmic is used for the symptomatic treatment of itching of the eyes caused by allergic conjunctivitis (a condition in which the eyes become itchy, swollen, red, and teary when they are exposed to certain substances in the air). Basically, histamine (H1) receptor antagonist used (as its benzenesulfonate salt) for treatment of itching associated with allergic conjunctivitis. (2) Bepotastine besilate 1.5% ophthalmic solution is a safe and effective treatment option for allergic conjunctivitis-associated pruritus. Human clinical trials demonstrate the efficacy and safety of systemic and ophthalmic bepotastine for pruritus relief, limited penetration across the blood-brain barrier, and kinetics suitable for twice-daily administration. (3) Bepotastine may also have other immunoactivity properties, such as inhibition of eosinophil migration, interleukin-5 (IL-5), leukotrienes (e.g., LTB4), and platelet-activating factor (PAF).
Mechanism Of Action
In allergic conjunctivitis, allergen exposure is followed by conjunctival mast cell degranulation and histamine released as a result of the formation of complementary IgE cross-links on the conjunctiva. Due to the release of histamine, symptoms such as itching can be observed. Bepotastine works to relieve itchy eyes by three primary mechanisms of action. (1) It is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. It belongs to the second-generation piperidine chemical class. It works by blocking the action and preventing the release of histamine, a substance in the body that causes allergic symptoms. (S)-(4-chlorophenyl)(pyridin-2-yl)methanol of bepotastine in which the hydroxyl hydrogen is substituted by a 1-(3-carboxypropyl)piperidin-4-yl group. (2) It a mast cell stabilizer. (3) It suppresses the migration of eosinophils into inflamed tissues to prevent tissue damage and worsening of allergic inflammation of the conjunctiva.
We're glad to help you with your products and services demands. For any inquiry, question or recommendation, please send an email to or fill out the following form.
For product and service inquiries, please use our online system or send an email to .
