Bepotastine Besilate

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic solution.1 2 3 5 6

Remove soft contact lenses prior to administration of each dose (since benzalkonium chloride may be absorbed by the lenses); may reinsert lenses after 10 minutes following administration if eyes are not red.1 5

Avoid contamination of the solution container.1 5

Dosage

Available as bepotastine besilate; dosage expressed in terms of the salt.1

Pediatric Patients

Children ≥2 years of age: 1 drop of a 1.5% solution in the affected eye(s) twice daily.1

Adults

1 drop of a 1.5% solution in the affected eye(s) twice daily.1 5

Contraindications

• Manufacturer states none known.1

Warnings/Precautions

Administration

For topical ophthalmic use only.1

Proper Handling to Avoid Contamination

To avoid contamination of the dropper tip and solution, do not to touch the eyelids or surrounding areas with the dropper tip.1

Close container tightly when not in use.1

Contact Lenses

Remove contact lenses prior to administration of each dose, since benzalkonium chloride preservative may be absorbed by soft contact lenses; lenses may be reinserted after 10 minutes following administration if eyes are not red; patient should not wear contact lenses if eyes are red.1 5 Not indicated for contact lens-related ocular irritation.1 5

Specific Populations

Category C.1 5

Distributed into milk in rats following oral administration.1

Not known whether bepotastine besilate distributes into human milk following topical application to the eye.1 Use caution.1

Safety and efficacy not established in pediatric patients <2 years of age.1 Efficacy in pediatric patients <10 years of age was extrapolated from clinical trials conducted in pediatric patients >10 years of age and adults.1

No overall differences in efficacy or safety observed between geriatric and younger patients.1

Common Adverse Effects

Mild taste following instillation,1 3 6 ocular irritation, headache, nasopharyngitis.1 2 3 10

Absorption

Bioavailability

Peak plasma concentrations achieved approximately 1–2 hours after instillation.1

Distribution

Plasma Protein Binding

Approximately 55%.1

Elimination

Metabolism

Minimally metabolized by CYP isoenzymes.1

Elimination Route

Excreted principally in urine as unchanged drug (75–90%).1

Storage

Ophthalmic

15–25°C.1

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.