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Alcaftadine

Pronunciation: al-KAF-ta-deen
Class: Ophthalmic Antihistamine

Trade Names

Lastacaft
- Solution, ophthalmic 0.25%

Pharmacology

Direct H 1 -receptor antagonist that inhibits release of histamine from the mast cell.

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Pharmacokinetics

Absorption

C max is approximately 60 pg/mL for alcaftadine and approximately 3 ng/mL for the active carboxylic acid metabolite. T max is 15 min. No systemic accumulation was identified.

Distribution

Plasma protein binding of alcaftadine and the active metabolite is 39.2% and 62.7%, respectively.

Metabolism

Metabolized to active carboxylic acid metabolite.

Elimination

Elimination half-life of carboxylic acid is approximately 2 h. Mainly excreted unchanged in urine (after oral administration).

Indications and Usage

Prevention of itching associated with allergic conjunctivitis.

Contraindications

None well documented.

Dosage and Administration

Adults and Children 2 y of age and older

Ophthalmic Instill 1 drop in each eye once daily.

General Advice

  • For topical ophthalmic use only.

Storage/Stability

Store at 59° to 77°F.

Drug Interactions

None well documented.

Adverse Reactions

CNS

Headache (less than 3%).

Ophthalmic

Burning and/or stinging upon instillation, irritation, pruritus, redness (less than 4%).

Miscellaneous

Influenza, nasopharyngitis (less than 3%).

Precautions

Monitor

Assess ophthalmic symptoms (eg, itching) before and periodically throughout therapy. Advise patient to notify health care provider if symptoms are not controlled with medication.


Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 2 y of age.

Contact lens use

Advise patient not to instill medication while wearing contact lenses; lenses may be reinserted 10 min after medication administration.

Patient Information

  • Advise patient that usual dose is 1 drop instilled into each eye once daily.
  • Teach patient proper technique for instilling eye drops: wash hands; do not allow dropper tip to touch eye. Tilt head back, look up; pull lower eyelid down; instill prescribed number of drops. Close eye for 1 to 2 min and apply gentle pressure to bridge of nose for 3 to 5 min. Do not rub eye.
  • Advise patient to use medication daily during the period of exposure to allergens in order to prevent symptoms from recurring.
  • Advise patient that if symptoms are not controlled not to increase the dose but to inform health care provider.
  • Advise patient who wears contact lenses to remove lenses before instilling this medicine and to wait at least 10 min after instilling eye drops before inserting lenses. Advise patients not to wear contact lenses if their eyes are red.
  • Inform patient that temporary redness, itching, burning, or stinging of the eye are the most common adverse effects and to contact health care provider if they occur and are bothersome.

Copyright © 2009 Wolters Kluwer Health.

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