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Alcaftadine (Monograph)

Brand name: Lastacaft
Drug class: Antiallergic Agents
- Histamine H1-receptor Antagonists
Chemical name: 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-imidazo[2,1-b] [3] benzazepine-3-carboxaldehyde
Molecular formula: C19H21N3O
CAS number: 147084-10-4

Introduction

Histamine H1-receptor antagonist.

Uses for Alcaftadine

Allergic Conjunctivitis

Prevention of ocular itching associated with allergic conjunctivitis.

Alcaftadine Dosage and Administration

Administration

Apply topically to the eye as an ophthalmic solution. For topical ophthalmic use only.

Ophthalmic Administration

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

Avoid contamination of the solution container.

Dosage

Pediatric Patients

Allergic Conjunctivitis
Ophthalmic

Children ≥2 years of age: 1 drop of a 0.25% solution in each eye once daily.

Adults

Allergic Conjunctivitis
Ophthalmic

1 drop of a 0.25% solution in each eye once daily.

Special Populations

No special population recommendations at this time.

Cautions for Alcaftadine

Contraindications

Warnings/Precautions

Specific Populations

Pregnancy

Category B.

Lactation

Not known whether alcaftadine is distributed into milk. Use with caution.

Pediatric Use

Safety and efficacy not established in children <2 years of age. Safety evaluated in children ≥3 years of age; efficacy in children 2–9 years of age extrapolated from demonstrated efficacy in adults and children ≥10 years of age.

Geriatric Use

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

Common Adverse Effects

Ocular effects: Irritation, burning, and/or stinging upon instillation; redness; pruritus.

Nonocular effects: Nasopharyngitis, headache, influenza.

Drug Interactions

No formal drug interaction studies to date.

Not metabolized by CYP enzymes; does not substantially inhibit major CYP enzymes in vitro.

Alcaftadine Pharmacokinetics

Absorption

Bioavailability

Appears rapidly in systemic circulation following topical application to eye. Peak plasma concentrations of alcaftadine and its active metabolite occur at a median of 15 minutes and at 1 hour, respectively, after administration.

Onset

Rapid; effect on ocular itching apparent at 3 minutes after conjunctival antigen challenge.

Duration

Effect on ocular itching shown to persist for 16 hours.

Distribution

Extent

Not known whether distributed into milk.

Plasma Protein Binding

Alcaftadine: About 39%.

Carboxylic acid metabolite: About 63%.

Elimination

Metabolism

Metabolized by cytosolic, non-CYP enzymes to an active carboxylic acid metabolite.

Elimination Route

Carboxylic acid metabolite is eliminated mainly in urine (based on data for oral alcaftadine).

Half-life

Carboxylic acid metabolite: About 2 hours.

Plasma concentrations of alcaftadine and carboxylic acid metabolite are below limit of quantitation by 3 and 12 hours, respectively, after administration of alcaftadine ophthalmic solution.

Stability

Storage

Ophthalmic

Solution

15–25°C.

Actions

Advice to Patients

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.

Alcaftadine

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.25%

Lastacaft

Allergan

AHFS DI Essentials™. © Copyright 2024, Selected Revisions May 6, 2011. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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