| Item |
Information |
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Drug Groups
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approved |
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Description
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Alcaftadine is a H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. This drug was approved in July 2010. |
| Indication |
For the prevention of itching associated with allergic conjunctivitis. |
| Pharmacology |
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. |
| Biotransformation |
The metabolism of alcaftadine is mediated by non-CYP450 cytosolic enzymes to the active carboxylic acid metabolite. |
| Half Life |
The elimination half-life of the carboxylic acid metabolite is approximately 2 hours following topical ocular administration. |
| Protein Binding |
The protein binding of alcaftadine and the active metabolite are 39.2% and 62.7% respectively. |
| Elimination |
Based on data following oral administration of alcaftadine, the carboxylic acid metabolite is primarily eliminated unchanged in the urine. |
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