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

Trade Names

- Solution, ophthalmic 0.25%


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

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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.


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


Metabolized to active carboxylic acid metabolite.


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.


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.


Store at 59° to 77°F.

Drug Interactions

None well documented.

Adverse Reactions


Headache (less than 3%).


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


Influenza, nasopharyngitis (less than 3%).



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


Category B .




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.

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