Alcaftadine
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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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| Pharmacokinetic data | |
| Elimination half-life | ~2 hrs |
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| DrugBank | |
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| Chemical and physical data | |
| Formula | C19H21N3O |
| Molar mass | 307.397 g·mol−1 |
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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]
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[edit]
Alcaftadine is indicated for the prevention of itching associated with allergic conjunctivitis.[1]
Pharmacology[edit]
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[edit]
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[edit]
Alcaftadine is administered as an eye drop which limits its effects to the eye.[medical citation needed]
The half life of alcaftadine after ocular administration is two hours.[medical citation needed]
The main metabolite of alcaftadine is a carboxylic acid that has minimal systemic effects.[medical citation needed] The maximum concentration of that metabolite is 0.06 ng/ml at Tmax of 15 minutes.[medical citation needed] Except for the metabolite, alcaftadine is excreted unchanged.[medical citation needed]
Because alcaftadine is administered at low concentrations and at a local site (the eye), it appears to have minimal systemic effects,[7] and the low absorption of alcaftadine results in minimal systemic accumulation.[medical citation needed]
History[edit]
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[edit]
Economics[edit]
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[edit]
Alcaftadine was approved for medical use in the United States in July 2010.[1][3]
References[edit]
- ^ a b c d e f g "Lastacaft- alcaftadine solution/ drops". DailyMed. 1 August 2015. Retrieved 10 June 2020.
- ^ "Lastacaft- alcaftadine solution/ drops". DailyMed. 10 August 2022. Retrieved 20 May 2024.
- ^ a b "Drug Approval Package: Lastacaft (alcaftadine) Ophthalmic Solution NDA #022134". U.S. Food and Drug Administration (FDA). 24 December 1999. Retrieved 10 June 2020.
- ^ "Now Available Over the Counter, Lastacaft Provides Eye Allergy Itch Relief in Minutes that Lasts Through 16 Hours". PR Newswire (Press release). 15 March 2022. Retrieved 18 May 2024.
- ^ a b c Greiner JV, Edwards-Swanson K, Ingerman A (January 2011). "Evaluation of alcaftadine 0.25% ophthalmic solution in acute allergic conjunctivitis at 15 minutes and 16 hours after instillation versus placebo and olopatadine 0.1%". Clinical Ophthalmology. 5: 87–93. doi:10.2147/OPTH.S15379. PMC 3037035. PMID 21339800.
- ^ Ono SJ, Lane K (February 2011). "Comparison of effects of alcaftadine and olopatadine on conjunctival epithelium and eosinophil recruitment in a murine model of allergic conjunctivitis". Drug Design, Development and Therapy. 5: 77–84. doi:10.2147/DDDT.S15788. PMC 3038998. PMID 21340041.
- ^ "Alcaftadine" (PDF). Office of Clinical Pharmacology Review. U.S. Food and Drug Administration. 17 November 2009.
- ^ "Drug Approval Package: Lastacaft (alcaftadine) Ophthalmic Solution NDA #022134". U.S. Food and Drug Administration (FDA). 24 December 1999. Retrieved 10 June 2020.
- ^ "Lastacaft (alcaftadine ophthalmic solution 0.25%)" (PDF). Drug Use Review. U.S. Food and Drug Administration (FDA). 21 June 2012. Archived from the original (PDF) on 15 February 2017.
