Bepreve (Bepotastine besilate) ™ (bepotastine besilate ophthalmic solution) 1.5% is a histamine H receptor antagonist indicated for the treatment of itching associated with signs and symptoms of allergic conjunctivitis.

Instill one drop of Bepreve (Bepotastine besilate) ™ into the affected eye(s) twice a day (BID).

Topical ophthalmic solution containing bepotastine besilate 1.5%.

Patients should be advised not to wear a contact lens if their eye is red. Bepreve (Bepotastine besilate) ™ should not be used to treat contact lens-related irritation.

Bepreve (Bepotastine besilate) ™ should not be instilled while wearing contact lenses. Remove contact lenses prior to instillation of Bepreve (Bepotastine besilate) ™. The preservative in Bepreve (Bepotastine besilate) ™, benzalkonium chloride, may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of Bepreve (Bepotastine besilate) ™.

The most common reported adverse reaction occurring in approximately 25% of subjects was a mild taste following instillation. Other adverse reactions occurring in 2-5% of subjects were eye irritation, headache, and nasopharyngitis.

Pregnancy Category C: Teratogenicity studies have been performed in animals. Bepotastine besilate was not found to be teratogenic in rats during organogenesis and fetal development at oral doses up to 200 mg/kg/day (representing a systemic concentration approximately 3,300 times that anticipated for topical ocular use in humans), but did show some potential for causing skeletal abnormalities at 1,000 mg/kg/day. There were no teratogenic effects seen in rabbits at oral doses up to 500 mg/kg/day given during organogenesis and fetal development (>13,000 times the dose in humans on a mg/kg basis). Evidence of infertility was seen in rats given oral bepotastine besilate 1,000 mg/kg/day however, no evidence of infertility was observed in rats given 200 mg/kg/day (approximately 3,300 times the topical ocular use in humans). The concentration of radiolabeled bepotastine besilate was similar in fetal liver and maternal blood plasma following a single 3 mg/kg oral dose. The concentration in other fetal tissues was one-third to one-tenth the concentration in maternal blood plasma.

An increase in stillborns and decreased growth and development were observed in pups born from rats given oral doses of 1,000 mg/kg/day during perinatal and lactation periods. There were no observed effects in rats treated with 100 mg/kg/day.

There are no adequate and well-controlled studies of bepotastine besilate in pregnant women. Because animal reproduction studies are not always predictive of human response, Bepreve (Bepotastine besilate) ™ (bepotastine besilate ophthalmic solution) 1.5% should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Following a single 3 mg/kg oral dose of radiolabeled bepotastine besilate to nursing rats 11 days after delivery, the maximum concentration of radioactivity in milk was 0.40 μg eq/mL 1 hour after administration; at 48 hours after administration the concentration was below detection limits. The milk concentration was higher than the maternal blood plasma concentration at each time of measurement.

It is not known if bepotastine besilate is excreted in human milk. Caution should be exercised when Bepreve (Bepotastine besilate) ™ (bepotastine besilate ophthalmic solution) 1.5% is administered to a nursing woman.

Bepreve (Bepotastine besilate) ™ (bepotastine besilate ophthalmic solution) 1.5% is a sterile, topically administered drug for ophthalmic use. Each mL of Bepreve (Bepotastine besilate) ™ contains 15 mg bepotastine besilate.

Bepotastine besilate is designated chemically as (+) -4-[[(S)-p-chloro-alpha -2-pyridylbenzyl]oxy]-1-piperidine butyric acid monobenzenesulfonate. The chemical structure for bepotastine besilate is:

Bepotastine besilate is a white or pale yellowish crystalline powder. The molecular weight of bepotastine besilate is 547.06 daltons. Bepreve (Bepotastine besilate) ™ ophthalmic solution is supplied as a sterile, aqueous 1.5% solution, with a pH of 6.8.

The osmolality of Bepreve (Bepotastine besilate) ™ (bepotastine besilate ophthalmic solution) 1.5% is approximately 290 mOsm/kg.

Absorption:
Dtistribution:
In vitro
Excretion:

Clinical efficacy was evaluated in 2 conjunctival allergen challenge (CAC) studies (237 patients). Bepreve (Bepotastine besilate) ™ (bepotastine besilate ophthalmic solution) 1.5% was more effective than its vehicle for relieving ocular itching induced by an ocular allergen challenge, both at a CAC 15 minutes post-dosing and a CAC 8 hours post dosing of Bepreve (Bepotastine besilate) ™.

The safety of Bepreve (Bepotastine besilate) ™ was evaluated in a randomized clinical study of 861 subjects over a period of 6 weeks.

Bepreve (Bepotastine besilate) ™ (bepotastine besilate ophthalmic solution) 1.5% is supplied in a white low density polyethylene plastic squeeze bottle with a white controlled dropper tip and a white polypropylene cap in the following size:10 mL (NDC 67425-007-75)

Patients should be advised not to wear a contact lens if their eye is red. Patients should be advised that Bepreve (Bepotastine besilate) ™ should not be used to treat contact lens-related irritation.

Patients should also be advised to remove contact lenses prior to instillation of Bepreve (Bepotastine besilate) ™. The preservative in Bepreve (Bepotastine besilate) ™, benzalkonium chloride, may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of Bepreve (Bepotastine besilate) ™.

Bepreve (Bepotastine besilate) ™ (bepotastine besilate ophthalmic solution) 1.5%

Sterile 10 mL          NDC 67425-007-75

For topical application in the eye.

Store at 15-25C (59-77F)

Rx only

Bepreve (Bepotastine besilate) ™ (bepotastine besilate ophthalmic solution) 1.5%

Sterile 10 mL          NDC 67425-007-75

Rx only

Each mL Contains:
Active:
Preservative:
Inactives:
This product is sterile when manufactured and should be dispensed in the original unopened container. Instruct patient on precautions to avoid contamination.

Usual dosage:
Instill one drop into the affected eye(s) twice a day.

See accompanying prescribing information.

Store at 15º –25ºC (59º–77ºF)