alcaftadine

{{Infobox drug

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| verifiedrevid = 477316420

| image = Alcaftadine.svg

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| tradename = Lastacaft

| Drugs.com = {{drugs.com|monograph|alcaftadine}}

| MedlinePlus = a611022

| DailyMedID = Alcaftadine

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| routes_of_administration = Eye drops

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| ATC_prefix = S01

| ATC_suffix = GX11

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| legal_US = OTC

| legal_US_comment = {{cite web | title=Lastacaft- alcaftadine solution/ drops | website=DailyMed | date=10 August 2022 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a3002410-4bf1-4182-9d7c-8193eb7cd215 | access-date=20 May 2024}}

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| CAS_number_Ref = {{cascite|changed|??}}

| CAS_number = 147084-10-4

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| PubChem = 19371515

| IUPHAR_ligand = 7587

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| DrugBank = DB06766

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| ChemSpiderID = 14201635

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| UNII = 7Z8O94ECSX

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| KEGG = D06552

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| ChEBI = 71023

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| ChEMBL = 1201747

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| IUPAC_name = 2-(1-Methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0^(3,7)]tetradeca- 1(14),3,5,10,12-pentaene-6-carbaldehyde

| C=19 | H=21 | N=3 | O=1

| SMILES = CN1CCC(=C2c3ccccc3CCn4c(C=O)cnc24)CC1

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| StdInChI = 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

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| StdInChIKey = MWTBKTRZPHJQLH-UHFFFAOYSA-N

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Alcaftadine, sold under the brand name Lastacaft, is an antihistamine used to help prevent itching of the eyes. It is an H1 histamine receptor antagonist. It is given as an drops in the eye.

It was approved for medical use in the United States in July 2010.{{cite web | title=Drug Approval Package: Lastacaft (alcaftadine) Ophthalmic Solution NDA #022134 | website=U.S. Food and Drug Administration (FDA) | date=24 December 1999 | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022134s000TOC.cfm | archive-url=https://web.archive.org/web/20131203114538/http://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022134s000TOC.cfm | url-status=dead | archive-date=3 December 2013 | access-date=10 June 2020}} It is available as a generic medication and as an over-the-counter medication.{{cite press release | title=Now Available Over the Counter, Lastacaft Provides Eye Allergy Itch Relief in Minutes that Lasts Through 16 Hours | website=PR Newswire | date=15 March 2022 | url=https://www.prnewswire.com/news-releases/now-available-over-the-counter-lastacaft-provides-eye-allergy-itch-relief-in-minutes-that-lasts-through-16-hours-301501288.html | access-date=18 May 2024}}

Medical uses

Alcaftadine is indicated for the prevention of itching associated with allergic conjunctivitis.

Pharmacology

Alcaftadine is an antagonist of histamine receptor 1.{{cite web | title=Lastacaft- alcaftadine solution/ drops | website=DailyMed | date=1 August 2015 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=17d37e8d-7825-424b-b6ca-0a85d0bf4694 | access-date=10 June 2020}} 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.{{cite journal | vauthors = Greiner JV, Edwards-Swanson K, Ingerman A | title = 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% | journal = Clinical Ophthalmology | volume = 5 | pages = 87–93 | date = January 2011 | pmid = 21339800| pmc = 3037035 | doi = 10.2147/OPTH.S15379 | doi-access = free }} 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.{{cite journal | vauthors = Ono SJ, Lane K | title = Comparison of effects of alcaftadine and olopatadine on conjunctival epithelium and eosinophil recruitment in a murine model of allergic conjunctivitis | journal = Drug Design, Development and Therapy | volume = 5 | pages = 77–84 | date = February 2011 | pmid = 21340041 | pmc = 3038998 | doi = 10.2147/DDDT.S15788 | doi-access = free }}

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.

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.{{cite web | title = Alcaftadine |url= https://www.fda.gov/downloads/drugs/developmentapprovalprocess/developmentresources/ucm223817.pdf | work = Office of Clinical Pharmacology Review | publisher = U.S. Food and Drug Administration | date = 17 November 2009 }}{{dead link|date=May 2025|bot=medic}}{{cbignore|bot=medic}}

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.

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.{{cite web | title=Drug Approval Package: Lastacaft (alcaftadine) Ophthalmic Solution NDA #022134 | website=U.S. Food and Drug Administration (FDA) | date=24 December 1999 | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022134s000TOC.cfm | access-date=10 June 2020}} By March 2012, 139,000 prescriptions had been written for 104,000 unique patients, and alcaftadine exceeded the sales of epinastine (Elestat).{{cite web | title = Lastacaft (alcaftadine ophthalmic solution 0.25%) | url = https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/PediatricAdvisoryCommittee/UCM317430.pdf | archive-url = https://web.archive.org/web/20170215193100/https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/PediatricAdvisoryCommittee/UCM317430.pdf | archive-date = 15 February 2017 | work = Drug Use Review | publisher = U.S. Food and Drug Administration (FDA) | date = 21 June 2012 }}

= Legal status =

Alcaftadine was approved for medical use in the United States in July 2010.

References

Category:H1 receptor antagonists

Category:Mast cell stabilizers

Category:Drugs developed by AbbVie

Category:Ophthalmology drugs