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Epinastine
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  • AHFS Monographs

Epinastine

Class: Antiallergic Agents
- Histamine H1-receptor Antagonists
Chemical Name: 3-Amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine
Molecular Formula: C16H15N3
CAS Number: 80012-43-7
Brands: Elestat

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

Introduction

Relatively selective histamine H1-receptor antagonist with mast-cell stabilizing properties.

Uses for Epinastine

Allergic Conjunctivitis

Prevention of ocular itching associated with allergic conjunctivitis.

Epinastine Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic solution. Not for injection or oral use.

Dosage

Available as epinastine hydrochloride; dosage expressed in terms of the salt.

Pediatric Patients

Allergic Conjunctivitis
Ophthalmic

Children ≥3 years of age: 1 drop of a 0.05% solution in each eye twice daily for up to 8 weeks.

Continue therapy throughout period of exposure (i.e., until pollen season is over or until exposure to offending allergen is terminated), even in absence of symptoms.

Adults

Allergic Conjunctivitis
Ophthalmic

1 drop of a 0.05% solution in each eye twice daily for up to 8 weeks.

Continue therapy throughout period of exposure (i.e., until pollen season is over or until exposure to offending allergen is terminated), even in absence of symptoms.

Cautions for Epinastine

Contraindications

  • Known hypersensitivity to epinastine or any ingredient in the formulation.

Warnings/Precautions

Specific Populations

Pregnancy

Category C.

Lactation

Distributed into milk in rats; not known whether distributed into human milk. Use with caution.

Pediatric Use

Safety and efficacy not established in children <3 years of age.

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.

Common Adverse Effects

Ocular discomfort (e.g., burning, folliculosis, hyperemia, pruritus), infection (e.g., cold symptoms, upper respiratory infections).

Interactions for Epinastine

No formal drug interaction studies to date.

Epinastine Pharmacokinetics

Absorption

Bioavailability

Limited systemic exposure following topical application to the eye. No increase in systemic absorption following multiple dosing.

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