Product Name

Alcaftadine

CAS Number

147084-10-4

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Product Name:
Alcaftadine
CAS Number:
147084-10-4
Indication:
For the prevention of itching associated with allergic conjunctivitis.
Mode 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.

Pharmacodynamics:

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.

IUPAC:
5H-Imidazo(2, 1-b)(3)benzazepine-3-carboxaldehyde, 6, 11-dihydro-11-(1-methyl-4- piperidinylidene)-
ATC:
S01GX11
PubChem:
19371515
DrugBank:
DB06766
Formula:
C19-H21-N3-O
Molecular Mass:
307.3949
Synonyms:
Alcaftadine, Lastacaft, R 89674, R89674, UNII-7Z8O94ECSX
SMILES:
C1(=C2CCN(CC2)C)c2c(CCn3c1ncc3C=O)cccc2
InChi:
1S/C19H21N3O/c1-21-9-6-15(7-10-21)18-17-5-3-2-4-14(17)8-11-22-16(13-23)12-20-19(18)22/h2-5,12-13H,6-11H2,1H3
General Reference:
General Reference:

 

  1. Mahvan TD, Buckley WA, Hornecker JR: Alcaftadine for the prevention of itching associated with allergic conjunctivitis. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1025-32. doi: 10.1345/aph.1Q755. Epub 2012 Jul 17. Pubmed
  2. Simons FE, Simons KJ: Histamine and H1-antihistamines: celebrating a century of progress. J Allergy Clin Immunol. 2011 Dec;128(6):1139-1150.e4. doi: 10.1016/j.jaci.2011.09.005. Epub 2011 Oct 27. Pubmed
  3. Hussar DA, Samuel J: Vilazodone hydrochloride, linagliptin, and alcaftadine. J Am Pharm Assoc (2003). 2011 Jul-Aug;51(4):557-9. doi: 10.1331/JAPhA.2011.11534. Pubmed
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