Drug Reference
Bepotastine
Rx only
Fact box
- Action class
- Histamine-1 Receptor Antagonist
- Habit forming
- No
- Availability
- Prescription (Rx)
Brand names
Bepreve
Available as
15 MG/ML · Ophthalmic Solution
FDA label sections are from openFDA and may not reflect the most recent labeling — confirm against the current DailyMed label.
Uses
1 INDICATIONS AND USAGE BEPREVE ® (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. BEPREVE is a histamine H1 receptor antagonist indicated for the treatment of itching associated with allergic conjunctivitis. ( 1 )
How it works
12.1 Mechanism of Action Bepotastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells.
How to use / dosing
2 DOSAGE AND ADMINISTRATION Instill one drop of BEPREVE into the affected eye(s) twice a day. Remove contact lenses prior to instillation of BEPREVE. • Instill one drop into the affected eye(s) twice a day. ( 2 ) • Remove contact lenses prior to instillation of BEPREVE. ( 2 )
Side effects
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 Bausch & Lomb Incorporated at 1-800-553-5340 or 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 BEPREVE. 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.
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 BEPREVE. 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.
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 BEPREVE. 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.
Safety advice
Conservative summary derived from FDA labeling — defaults to “consult your doctor” unless the label is explicit. Not a substitute for your clinician’s advice.
PregnancyUnsafe
8.1 Pregnancy Risk Summary There are no available human data for the use of BEPREVE 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 times higher than the maximum RHOD, on a mg/m 2 basis), the concentration of radio-labeled bepotastine besilate was similar in fetal liver and maternal blood plasma. The concentration in other fetal tissues was one-third to one-tenth the concentration in maternal blood plasma. In a pre/postnatal development study, oral administration of bepotastine besilate to rats during the perinatal and lactation periods produced an increase in stillbirths and decreased growth and development in offspring at a maternal dose of 1,000 mg/kg/day (5
BreastfeedingConsult your doctor
…of bepotastine besilate to rats during the perinatal and lactation periods produced an increase in stillbirths and decreased growth and development in offspring at a maternal dose of 1,000 mg/kg/day (5,400 times higher than the maximum RHOD, on a mg/m 2…
AlcoholNo information
No specific information in the FDA label.
DrivingNo information
No specific information in the FDA label.
KidneyNo information
No specific information in the FDA label.
LiverConsult your doctor
…of radio-labeled bepotastine besilate was similar in fetal liver and maternal blood plasma.…
Warnings & precautions
5 WARNINGS AND PRECAUTIONS • Contamination of Solution: Do not touch the dropper tip to any surface. Keep bottle tightly closed when not in use. ( 5.1 ) • Contact Lens Wear: BEPREVE should not be used to treat contact lens-related irritation. ( 5.2 ) 5.1 Contamination of Tip and Solution To minimize contaminating the dropper tip and solution, advise the patient not to touch the eyelids or surrounding areas with the dropper tip of the bottle and to keep the bottle tightly closed when not in use. 5.2 Contact Lens Wear BEPREVE should not be used to treat contact lens-related irritation. BEPREVE should not be instilled while wearing contact lenses. Patient should remove contact lenses prior to instillation of BEPREVE, because benzalkonium chloride may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of BEPREVE.
5.1 Contamination of Tip and Solution To minimize contaminating the dropper tip and solution, advise the patient not to touch the eyelids or surrounding areas with the dropper tip of the bottle and to keep the bottle tightly closed when not in use.
5.2 Contact Lens Wear BEPREVE should not be used to treat contact lens-related irritation. BEPREVE should not be instilled while wearing contact lenses. Patient should remove contact lenses prior to instillation of BEPREVE, because benzalkonium chloride may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of BEPREVE.
5.1 Contamination of Tip and Solution To minimize contaminating the dropper tip and solution, advise the patient not to touch the eyelids or surrounding areas with the dropper tip of the bottle and to keep the bottle tightly closed when not in use.
5.2 Contact Lens Wear BEPREVE should not be used to treat contact lens-related irritation. BEPREVE should not be instilled while wearing contact lenses. Patient should remove contact lenses prior to instillation of BEPREVE, because benzalkonium chloride may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of BEPREVE.
Contraindications
4 CONTRAINDICATIONS BEPREVE 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. ( 4 )
Pediatric use
8.4 Pediatric Use Safety and efficacy of BEPREVE (bepotastine besilate ophthalmic solution) 1.5% have not been established in pediatric patients under 2 years of age. Efficacy in pediatric patients under 10 years of age was extrapolated from clinical trials conducted in pediatric patients greater than 10 years of age and from adults.
⚑ About half of pediatric medication use is off-label and not described in FDA labels — absence of pediatric information does not mean a medicine is unused or unsafe in children. Confirm with your clinician.
Current FDA labels (DailyMed)
- BEPOTASTINE BESILATE SOLUTION/ DROPS [MYLAN PHARMACEUTICALS INC.]
- BEPOTASTINE BESILATE SOLUTION [SOMERSET THERAPEUTICS, LLC]
- BEPOTASTINE BESILATE SOLUTION/ DROPS [BAUSCH & LOMB AMERICAS INC.]
- BEPOTASTINE BESILATE OPHTHALMIC SOLUTION 1.5% SOLUTION/ DROPS [ALEMBIC PHARMACEUTICALS LIMITED]
- BEPOTASTINE BESILATE OPHTHALMIC SOLUTION 1.5% SOLUTION/ DROPS [ALEMBIC PHARMACEUTICALS INC.]
Authoritative sources
Reference only — not clinical advice. Verify against current FDA labeling and consult a licensed provider. About half of pediatric drug use is off-label and is not reflected in FDA labels; absence of pediatric information does not mean a medicine is unused or unsafe in children.