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Alcaftadine

Clinical data
Trade names	Lastacaft
AHFS/Drugs.com	Monograph
MedlinePlus	a611022
License data	US DailyMed: Alcaftadine
Routes of administration	Eye drops
ATC code	S01GX11 (WHO)
Legal status
Legal status	US: OTC
Pharmacokinetic data
Elimination half-life	~2 hrs
Identifiers
IUPAC name 2-(1-Methylpiperidin-4-ylidene)-4,7-diazatricyclotetradeca- 1(14),3,5,10,12-pentaene-6-carbaldehyde
CAS Number	147084-10-4
PubChem CID	19371515
IUPHAR/BPS	7587
DrugBank	DB06766
ChemSpider	14201635
UNII	7Z8O94ECSX
KEGG	D06552
ChEBI	CHEBI:71023
ChEMBL	ChEMBL1201747
CompTox Dashboard (EPA)	DTXSID80598455
Chemical and physical data
Formula	C19H21N3O
Molar mass	307.397 g·mol
3D model (JSmol)	Interactive image
SMILES CN1CCC(=C2c3ccccc3CCn4c(C=O)cnc24)CC1
InChI InChI=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 Key: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. It is available as a generic medication and as an over-the-counter medication.

Medical uses

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

Pharmacology

Alcaftadine is an antagonist of histamine receptor 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. 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.

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.

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. By March 2012, 139,000 prescriptions had been written for 104,000 unique patients, and alcaftadine exceeded the sales of epinastine (Elestat).

Legal status

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

References

1. ^ "Lastacaft- alcaftadine solution/ drops". DailyMed. 1 August 2015. Retrieved 10 June 2020.
2. "Lastacaft- alcaftadine solution/ drops". DailyMed. 10 August 2022. Retrieved 20 May 2024.
3. ^ "Drug Approval Package: Lastacaft (alcaftadine) Ophthalmic Solution NDA #022134". U.S. Food and Drug Administration (FDA). 24 December 1999. Retrieved 10 June 2020.
4. "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.
5. ^ 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.
6. 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.
7. "Alcaftadine" (PDF). Office of Clinical Pharmacology Review. U.S. Food and Drug Administration. 17 November 2009.
8. "Drug Approval Package: Lastacaft (alcaftadine) Ophthalmic Solution NDA #022134". U.S. Food and Drug Administration (FDA). 24 December 1999. Retrieved 10 June 2020.
9. "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.

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