Bepotastine (Monograph)

Brand name: Bepreve
Drug 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

Introduction

Histamine H ₁-receptor antagonist with mass-cell stabilizing activity.^{1 2 3 5}

Uses for Bepotastine

Allergic Conjunctivitis

Symptomatic treatment of ocular itching associated with allergic conjunctivitis.^{1 3 7 8 9 10}

Bepotastine Dosage and Administration

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

Allergic Conjunctivitis

Ophthalmic

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

Adults

Allergic Conjunctivitis

Ophthalmic

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

Related/similar drugs

prednisone, cetirizine ophthalmic, dexamethasone ophthalmic, azelastine ophthalmic, prednisolone ophthalmic, doxylamine

Cautions for Bepotastine

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

Pregnancy

Category C.^{1 5}

Lactation

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

Pediatric Use

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

Geriatric Use

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}

Drug Interactions

Minimally metabolized by CYP isoenzymes.¹

Drugs Metabolized by Hepatic Microsomal Enzymes

Low potential for drug interactions via inhibition of CYP isoenzymes 3A4, 2C9, and 2C19.¹

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

Bepotastine Pharmacokinetics

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

Stability

Storage

Ophthalmic

Solution

15–25°C.¹

Actions

• Inhibits the release of histamine and other mediators (e.g., leukotrienes, platelet activating factor [PAF]) involved in allergic reactions.^{1 2 3 5}

• Exhibits mast-cell stabilizing activity.^{1 2 3 5}

• Inhibits eosinophil migration to and activation at inflammatory sites.²

Advice to Patients

• Importance of learning and adhering to proper administration techniques to avoid contamination of the solution.^{1 5}

• 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.^{1 5}

• Not indicated for contact lens-related ocular irritation.^{1 5}

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.¹

• Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.¹

• Importance of informing patients of other important precautionary information.

• (See Cautions.)¹

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.

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