Approved September 8, 2009

BEPOTASTINE BESILATE
(FDA Category 1S)

BEPREVE(TM) (ISTA Pharmaceuticals) 1.5% ophthalmic solution is a piperidine butyric acid monobenzenesulfonate and is a histamine H1 receptor antagonist.

DOSING INFORMATION: Instill 1 drop to the affected eye(s) twice daily.

PHARMACOKINETICS: Following 1 drop of bepotastine 1% or 1.5% at a frequency of 4 times daily for 7 days, peak plasma concentrations were achieved in about 1 to 2 hours. Protein binding is approximately 55% regardless of bepotastine concentration. Bepotastine is minimally metabolized by CYP450 isoenzymes and has a low potential for drug interaction. The primary route of elimination is urinary excretion with 75% to 90% excreted unchanged in the urine.

CAUTIONS: No specific contraindications have been determined. Bepotastine is for topical ophthalmic use only and should not to be used to treat contact lens-related eye irritation. The most common adverse effect was a mild taste after administration.

FDA APPROVED INDICATIONS: Bepotastine besilate ophthalmic solution 1.5% is approved for the treatment of itching associated with signs and symptoms of allergic conjunctivitis.