Bepreve

Ocular Anti-Allergics, Antihistamines

dysgeusia / Early / 25.0-25.0
ocular irritation / Rapid / 2.0-5.0
headache / Early / 2.0-5.0
pharyngitis / Delayed / 2.0-5.0
rash / Early / 0-1.0
pruritus / Rapid / 0-1.0

Bepreve

Rx

Ophthalmic antihistamine and mast cell stabilizer
For treatment of itching due to allergic conjunctivitis
Remove contact lenses before and for 10 minutes after the dose

Instill 1 drop into the affected eye(s) twice daily.

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

There are no drug interactions associated with Bepotastine products.

Bepotastine/Bepreve/Betotastine besilate Ophthalmic Sol: 1.5%

2 drops/day per eye.

2 drops/day per eye.

2 drops/day per eye.

>= 2 years: 2 drops/day per eye.
< 2 years: Safety and efficacy have not been established.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Bepotastine besilate is a topically active, direct H1- receptor antagonist and mast cell stabilizer. By reducing these inflammatory mediators, topical ocular administration relieves the ocular pruritus associated with allergic conjunctivitis.

Bepotastine besilate is administered topically to the eye.
 
Bepotastine besilate is approximately 55% protein bound. Protein binding is independent of bepotastine besilate concentrations.
 
In vitro studies have shown that bepotastine besilate is minimally metabolized by the CYP450 enzyme system. Bepotastine besilate does not inhibit the CYP3A4, CYP2C9, or CYP2C19 isoenzymes in vitro. The effects of bepotastine besilate on the CYP1A2, CYP2C8, and CYP2D6 isoenzymes were not studied.
 
Bepotastine besilate is eliminated via urinary excretion with approximately 75 to 90% of the drug excreted unchanged in the urine.

Ophthalmic Route
After ophthalmic administration, bepotastine besilate results in minimal systemic exposure. Administration of one drop of 1% or 1.5% bepotastine besilate to each eye four times daily for seven days in 12 healthy adults resulted in maximum plasma concentrations of 5.1 +/- 2.5 ng/mL and 7.3 +/- 1.9 ng/mL, respectively, 1 to 2 hours after instillation. Plasma concentrations 24 hours after administration were below the quantifiable limit in 11 of 12 subjects.

No adequate and well-controlled studies of bepotastine besilate in pregnant women have been performed. Animal data reveal no harmful embryofetal or offspring effects following oral administration of the drug to rats and rabbits during pregnancy.

According to the manufacturer, bepotastine besilate should be used with caution during breast-feeding. It is not known if bepotastine besilate is excreted in human milk or if the drug has an adverse effect on milk production. Ophthalmic administration results in minimal systemic exposure; therefore, it is unlikely that nursing infants would be exposed to clinically significant amounts via breast milk. To minimize the amount of drug that reaches the systemic circulation and breast milk, apply pressure over the tear duct by the corner of the eye for 1 minute after ophthalmic administration. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.