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
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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