ALCAFTADINE

Description

Alcaftadine, a histamine H₁/H₂ receptor antagonist, was approved in the United States in 2010 for the prevention of itching and redness associated with allergic conjunctivitis. Seasonal and perennial allergic conjunctivitis affects up to 40% of the population worldwide. There are numerous treatment options, with topical antihistamines being an effective therapy. Some of the primary symptoms and signs of allergic conjunctivitis are ocular itching and conjunctival redness. The pharmaceutical market for conjunctivitis is substantial and steadily increasing.

The Uses of ALCAFTADINE

Alcaftadine is a H1 histamine receptor antagonist. Alcaftadine is used to prevent eye irritation and treat the signs and symptoms of allergic conjunctivitis.

Background

Alcaftadine is a H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. This drug was approved in July 2010.

Indications

For the prevention of itching associated with allergic conjunctivitis.

Pharmacokinetics

Following bilateral topical ocular administration of alcaftadine ophthalmic solution, 0.25%, the mean plasma Cmax of alcaftadine was approximately 60 pg/mL and the median Tmax occurred at 15 minutes. Plasma concentrations of alcaftadine were below the lower limit of quantification (10 pg/mL) by 3 hours after dosing. The mean Cmax of the active carboxylic acid metabolite was approximately 3 ng/mL and occurred at 1 hour after dosing. Plasma concentrations of the carboxylic acid metabolite were below the lower limit of quantification (100 pg/mL) by 12 hours after dosing.

Metabolism

The metabolism of alcaftadine is mediated by non-CYP450 cytosolic enzymes to the active carboxylic acid metabolite.