Chemistry:Alcaftadine
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.[2] It is available as a generic medication and as an over-the-counter medication.[3]
Medical uses
Alcaftadine is indicated for the prevention of itching associated with allergic conjunctivitis.[1]
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.[4] 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.[5]
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.[4]
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.[6]
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.[4]
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.[7] By March 2012, 139,000 prescriptions had been written for 104,000 unique patients, and alcaftadine exceeded the sales of epinastine (Elestat).[8]
Legal status
Alcaftadine was approved for medical use in the United States in July 2010.[1][2]
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 "Lastacaft- alcaftadine solution/ drops". 1 August 2015. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=17d37e8d-7825-424b-b6ca-0a85d0bf4694.
- ↑ 2.0 2.1 "Drug Approval Package: Lastacaft (alcaftadine) Ophthalmic Solution NDA #022134". 24 December 1999. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022134s000TOC.cfm.
- ↑ "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.
- ↑ 4.0 4.1 4.2 "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. January 2011. doi:10.2147/OPTH.S15379. PMID 21339800.
- ↑ "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. February 2011. doi:10.2147/DDDT.S15788. PMID 21340041.
- ↑ "Alcaftadine". Office of Clinical Pharmacology Review. U.S. Food and Drug Administration. 28 November 2009. https://www.fda.gov/media/78803/download.
- ↑ "Drug Approval Package: Lastacaft (alcaftadine) Ophthalmic Solution NDA #022134". 24 December 1999. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022134s000TOC.cfm.
- ↑ "Lastacaft (alcaftadine ophthalmic solution 0.25%)". Drug Use Review. U.S. Food and Drug Administration (FDA). 21 June 2012. https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/PediatricAdvisoryCommittee/UCM317430.pdf.
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