Bepotastine Besilate
FDA Drug Information • Also known as: Bepotastine Besilate, Bepreve
- Brand Names
- Bepotastine Besilate, Bepreve
- Dosage Form
- POWDER
- Product Type
- BULK INGREDIENT
Description
11 DESCRIPTION Bepotastine besilate ophthalmic solution 1.5% is a sterile, topically administered drug for ophthalmic use. Each mL of bepotastine besilate ophthalmic solution 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. Bepotastine besilate ophthalmic solution is supplied as a sterile, aqueous 1.5% solution, with a pH of 6.8. The osmolality of bepotastine besilate ophthalmic solution 1.5% is approximately 290 mOsm/kg. Each mL of bepotastine besilate ophthalmic solution 1.5% contains: Active: bepotastine besilate 15 mg (equivalent to 10.7 mg bepotastine) Preservative: benzalkonium chloride 0.005% Inactives: monobasic sodium phosphate dihydrate, sodium chloride, sodium hydroxide to adjust pH, and water for injection, USP. Image
What Is Bepotastine Besilate Used For?
1 INDICATIONS AND USAGE Bepotastine besilate ophthalmic solution 1.5% is a histamine H 1 receptor antagonist indicated for the treatment of itching associated with signs and symptoms of allergic conjunctivitis. Bepotastine besilate ophthalmic solution is a histamine H 1 receptor antagonist indicated for the treatment of itching associated with allergic conjunctivitis.
Dosage and Administration
2 DOSAGE AND ADMINISTRATION Instill one drop of bepotastine besilate ophthalmic solution into the affected eye(s) twice a day. Remove contact lenses prior to instillation of bepotastine besilate ophthalmic solution. Instill one drop into the affected eye(s) twice a day. Remove contact lenses prior to instillation of bepotastine besilate ophthalmic solution.
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS The most common adverse reaction occurring in approximately 25% of patients was a mild taste following instillation. Other adverse reactions which occurred in 2-5% of subjects were eye irritation, headache, and nasopharyngitis. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Somerset Therapeutics, LLC at 1-800-417-9175 or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. 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. 6.2 Post-Marketing Experience Hypersensitivity reactions have been reported rarely during the post-marketing use of bepotastine besilate ophthalmic solution. Because these reactions are reported voluntarily from a population of unknown size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. The hypersensitivity reactions may include itching, body rash, and swelling of lips, tongue and/or throat.
Contraindications
4 CONTRAINDICATIONS Bepotastine besilate ophthalmic solution is contraindicated in patients with a history of hypersensitivity reactions to bepotastine or any of the other ingredients [see Adverse Reactions ( 6.2 )] . Hypersensitivity to any component of this product.
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary There are no available human data for the use of bepotastine besilate ophthalmic solution during pregnancy to inform any drug-associated risks. Oral administration of bepotastine besilate to pregnant rats or rabbits during organogenesis or during the pre/postnatal period did not produce adverse embryofetal or offspring effects at clinically relevant systemic exposures. Maternal toxicity was observed in the rabbits at the lowest dose administered, 20 mg/kg/day (215 times the maximum recommended human ophthalmic dose, RHOD, on a mg/m 2 basis) [see Data] . The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4%, and of miscarriage is 15 to 20%, of clinically recognized pregnancies. Data Animal Data In embryofetal development studies, oral administration of bepotastine besilate to pregnant rabbits throughout organogenesis did not produce teratogenic effects at maternal doses up to 500 mg/kg/day (approximately 5.400 times the maximum RHOD, on a mg/m 2 basis). A maternal no observed adverse effect level (NOAEL) was not identified in this study due to spontaneous abortion observed at the lowest dose tested, 20 mg/kg/day (approximately 215 times higher than the maximum RHOD, on a mg/m 2 basis). Oral administration of bepotastine besilate to pregnant rats throughout organogenesis produced skeletal anomalies at 1,000 mg/kg/day (5,400 times higher than the maximum RHOD, on a mg/m 2 basis), a dose that also produced maternal toxicity and lethality. No teratogenic effects were observed in rats at maternal doses up to 200 mg/kg/day (corresponding to an estimated blood plasma concentration 3,300 times higher than that anticipated in humans at the maximum RHOD). A maternal NOAEL was observed at 10 mg/kg/day (54 times higher than the maximum RHOD, on a mg/m 2 basis). Following a single 3 mg/kg oral dose in rats (16...
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING Bepotastine besilate ophthalmic solution 1.5% is supplied in a white LDPE bottle with a white LDPE nozzle and a white HDPE cap in the following size: 5 mL – NDC 70069- 711 -01 10 mL – NDC 70069- 712 -01 STORAGE Store at 15°C to 25°C (59°F to 77°F).
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.