Alcaftadine
Chemical compound
From Wikipedia, the free encyclopedia
Alcaftadine, sold under the brand name Lastacaft, is an antihistamine used to help prevent itching of the eyes.[1] It is an H1 histamine receptor antagonist.[1] It is given as an drops in the eye.[1]
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| Trade names | Lastacaft |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a611022 |
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| Routes of administration | Eye drops |
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| Elimination half-life | ~2 hrs |
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| Formula | C19H21N3O |
| Molar mass | 307.397 g·mol−1 |
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It was approved for medical use in the United States in July 2010.[3] It is available as a generic medication and as an over-the-counter medication.[4]
Medical uses
Pharmacology
Alcaftadine is an antagonist of histamine receptor 1.[1] By blocking the receptor, alcaftadine has been shown to reduce itching and redness of the eyes, and to reduce recruitment of eosinophils after exposure to an allergen.[5] Alcaftadine reduces the number of eosinophils compared to olopatadine 0.1%, and in animal models, alcaftadine 0.25% decreased the expression of the epithelial protein E-cadhedrin-1 compared to placebo. Reducing E-cadherin decreases junctions that lead to the progression of allergic conjunctivitis.[6]
Adverse effects
In studies comparing the effectiveness of olopatadine to alcaftadine, there was not a dose-response increase of adverse effects as alcaftadine doses increases for 0.05% to 0.1% to 0.25%. The most common seen side effect of alcaftadine administration was irritation or a stinging sensation at the administration site.[5]
Pharmacokinetics
Because alcaftadine is administered at low concentrations and at a local site (the eye), it appears to have minimal systemic effects, and the low absorption of alcaftadine results in minimal systemic accumulation.[7]
History
When alcaftadine was tested against placebo and olopatadine, only alcaftadine 0.25% showed a clinically significant reduction in conjunctival redness scores 7 and 15 minutes after administration. Alcaftadine 0.05%, 0.1%, and 0.25% all reduced lid swelling, conjunctival redness, and ocular itching/tearing compared to placebo.[5]
Society and culture
Economics
Allergan, Inc. began selling alcaftadine under the trade name Lastacaft after it was approved by the US Food and Drug Administration in July 2010.[8] By March 2012, 139,000 prescriptions had been written for 104,000 unique patients, and alcaftadine exceeded the sales of epinastine (Elestat).[9]
Legal status
Alcaftadine was approved for medical use in the United States in July 2010.[1][3]
