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Bepotastine

Class: Antiallergic Agents
- Histamine H1-receptor Antagonists
- Mast-cell Stabilizers
Chemical Name: 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-,benzene sulfonate (1:1); (2) (+)-4-{4-[(S)-(4-Chlorophenyl)(pyridin-2-yl)methoxy]piperidin-1-yl}butanoic acid monobenzenesulfonate.
Molecular Formula: C21H25ClN2O3.C6H6O3S.547.10
CAS Number: 190786-44-8
Brands: Bepreve

Medically reviewed by Drugs.com on Sep 21, 2021. Written by ASHP.

Introduction

Histamine H 1-receptor antagonist with mass-cell stabilizing activity.

Uses for Bepotastine

Allergic Conjunctivitis

Symptomatic treatment of ocular itching associated with allergic conjunctivitis.

Bepotastine Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic solution.

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.

Avoid contamination of the solution container.

Dosage

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

Pediatric Patients

Allergic Conjunctivitis
Ophthalmic

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

Adults

Allergic Conjunctivitis
Ophthalmic

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

Cautions for Bepotastine

Contraindications

  • Manufacturer states none known.

Warnings/Precautions

Administration

For topical ophthalmic use only.

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.

Close container tightly when not in use.

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. Not indicated for contact lens-related ocular irritation.

Specific Populations

Pregnancy

Category C.

Lactation

Distributed into milk in rats following oral administration.

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

Pediatric Use

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

Geriatric Use

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

Common Adverse Effects

Mild taste following instillation, ocular irritation, headache, nasopharyngitis.

Interactions for Bepotastine

Minimally metabolized by CYP isoenzymes.

Drugs Metabolized by Hepatic Microsomal Enzymes

Low potential for drug interactions via inhibition of CYP isoenzymes 3A4, 2C9, and 2C19.

Effect on metabolism of substrates of CYP isoenzymes 1A2, 2C8, and 2D6 not established.

Bepotastine Pharmacokinetics

Absorption

Bioavailability

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

Distribution

Plasma Protein Binding

Approximately 55%.

Elimination

Metabolism

Minimally metabolized by CYP isoenzymes.

Elimination Route

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

Stability

Storage

Ophthalmic

Solution

15–25°C.

Actions

  • Inhibits the release of histamine and other mediators (e.g., leukotrienes, platelet activating factor [PAF]) involved in allergic reactions.

  • Exhibits mast-cell stabilizing activity.

  • Inhibits eosinophil migration to and activation at inflammatory sites.

Advice to Patients

  • Importance of learning and adhering to proper administration techniques to avoid contamination of the solution.

  • Importance of removing contact lenses prior to administration of each ophthalmic dose, since benzalkonium chloride preservative may be absorbed by soft lenses; may reinsert contact lenses after 10 minutes following administration if eyes are not red; importance of not wearing contact lenses if eyes are red.

  • Not indicated for contact lens-related ocular irritation.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.

  • Importance of informing patients of other important precautionary information.

  • (See Cautions.)

Preparations

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.

Bepotastine Besilate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

1.5%

Bepreve

Ista

AHFS DI Essentials™. © Copyright 2022, Selected Revisions October 1, 2010. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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