Bepotastine besilate is an H1-receptor antagonist and mast cell stabilizer. It is indicated for the treatment of ocular pruritus associated with allergic conjunctivitis in adults and pediatric patients age 2 years or older. Bepotastine besilate is administered twice daily. The products contain benzalkonium chloride which may be absorbed by soft contact lenses.
Administration
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Ophthalmic Administration
-Bepotastine besilate is for topical ophthalmic use only.
-Wash hands before and after use. Tilt the head back slightly and pull the lower eyelid down with the index finger. Squeeze the prescribed number of drops into the conjunctival sac and gently close eyes for 1 to 2 minutes. Do not blink.
-Care should be taken to avoid contamination. Do not touch the tip of the dropper to the eye, fingertips, or other surface.
-Remove contact lenses prior to instilling the drops. Instruct patients to wait at least 10 minutes before reinserting contact lenses. NOTE: Patients should be advised not to wear contact lenses if their eye is red.
-Do not share ophthalmic drops between patients.
Ocular irritation was reported in 2 to 5% of patients who received bepotastine besilate ophthalmic solution during pre-marketing pre-marketing clinical trials.
Headache was reported in 2 to 5% of patients who received bepotastine besilate ophthalmic solution during pre-marketing clinical trials.
Nasopharyngitis/pharyngitis was reported in 2 to 5% of patients who received bepotastine besilate ophthalmic solution during pre-marketing clinical trials.
Approximately 25% of patients who received bepotastine besilate ophthalmic solution during pre-marketing clinical trials reported a mild taste (dysgeusia) after administration.
Hypersensitivity reactions, including pruritus, rash (unspecified), and swelling of lips, tongue and/or throat have been reported rarely during the post-marketing use of bepotastine. A causal relationship has not been established.
Remove contact lenses prior to the ophthalmic administration of bepotastine besilate. The preservative benzalkonium chloride may be absorbed by soft contact lenses. Contact lens wearers should wait at least 10 minutes after administration before inserting their lenses. Bepotastine besilate should not be used to treat contact lens-related irritation. Advise patients not to wear their contact lens if their eye is red.
Safe and effective use of bepotastine besilate in neonates, infants, and children below the age of 2 years has not been established. Efficacy in pediatric patients between 2 and 10 years was extrapolated from clinical trials conducted in pediatric patients older than 10 years and adults.
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.
For the treatment of itching (ocular pruritus) associated with signs and symptoms of allergic conjunctivitis:
Ophthalmic dosage:
Adults: Instill 1 drop into the affected eye(s) twice daily.
Adolescents and Children 2 to 17 years: Instill 1 drop into the affected eye(s) twice daily.
Maximum Dosage Limits:
-Adults
2 drops/day per eye.
-Geriatric
2 drops/day per eye.
-Adolescents
2 drops/day per eye.
-Children
2 years and older: 2 drops/day per eye.
younger than 2 years: Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
There are no drug interactions associated with Bepotastine products.
Bepotastine besilate is a topically active, direct H1- receptor antagonist and an inhibitor of the release of histamine from mast cells or a 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. The extent of protein binding of bepotastine is approximately 55% and independent of bepotastine concentration. The main route of elimination of bepotastine besilate is urinary excretion, with approximately 75 to 90% excreted unchanged in urine.
Affected cytochrome P450 isoenzymes and drug transporters: None
In vitro metabolism studies with human liver microsomes demonstrated that bepotastine is minimally metabolized by CYP450 isozymes. Bepotastine besilate does not inhibit the metabolism of various cytochrome P450 substrates via inhibition of CYP3A4, CYP2C9, and CYP2C19. The effect of bepotastine besilate on the metabolism of substrates of CYP1A2, CYP2C8 and CYP2D6 was not studied. Bepotastine besilate has a low potential for drug interactions via inhibition of CYP3A4, CYP2C9, and CYP2C19.
-Route-Specific Pharmacokinetics
Other Route(s)
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 (2 ng/mL) in 11 of 12 subjects.