Alcatadine is an imidazolium benzazepine that is 6, 11-dihydro-5H-imidazepine [2, 1-b]  benzazepine, which is replaced by formyl at the third position and 1-methylpiperidine-4-methylene at the 11th position. An antihistamine used in the treatment of allergic conjunctivitis. It has the effect of H1 receptor antagonist and anti-allergic drug. It is an aldehyde, a piperidine, an imidazepine, and a tertiary amine. This drug was approved in July 2010.
For the prevention of itching associated with allergic conjunctivitis.
Conjunctivitis, Seasonal Allergic
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.
Mechanism of action
Alcaftadine is a H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.
TARGET: Histamine H1 receptor
Clinical Trial Information
|NCT02308501||4||Completed||2015-10-21||Allergic Conjunctivitis||ORA, Inc.|
|NCT00223951||3||Completed||2015-02-19||Allergic Conjunctivitis||Vistakon Pharmaceuticals|
|NCT00889330||3||Completed||2015-02-18||Allergic Conjunctivitis||Vistakon Pharmaceuticals|
|NCT01808768||4||Unknown status||2013-05-29||Allergic Conjunctivitis||Starx Research Center, LLC|
|NCT00241319||3||Completed||2011-09-26||Allergic Conjunctivitis||Vistakon Pharmaceuticals|
|2012-03-01||New drugs 2012 part I.||Nursing|
|2012-01-01||Alcaftadine for the prevention of itching associated with allergic conjunctivitis.||The Annals of pharmacotherapy|
|2011-12-01||Histamine and H1-antihistamines: celebrating a century of progress.||The Journal of allergy and clinical immunology|
|2011-12-01||Alcaftadine: a topical antihistamine for use in allergic conjunctivitis.||Drugs of today (Barcelona, Spain : 1998)|
|2011-04-01||Clinical pharmacology of alcaftadine, a novel antihistamine for the prevention of allergic conjunctivitis.||Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics|