Alcaftadine

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Alcaftadine
Alcaftadine.svg
Clinical data
Trade names Lastacaft
AHFS/Drugs.com Monograph
MedlinePlus a611022
License data
Routes of
administration 		Eye drops
ATC code
Legal status
Legal status
Pharmacokinetic data
Elimination half-life ~2 hrs
Identifiers
  • 2-(1-Methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0(3,7)]tetradeca- 1(14),3,5,10,12-pentaene-6-carbaldehyde
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C19H21N3O
Molar mass 307.397 g·mol−1
3D model (JSmol)
  • CN1CCC(=C2c3ccccc3CCn4c(C=O)cnc24)CC1
  • 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 Yes check.svgY
  • Key:MWTBKTRZPHJQLH-UHFFFAOYSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

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]

Contents

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

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. [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]

Alcaftadine was approved for medical use in the United States in July 2010. [1] [3]

References

  1. 1 2 3 4 5 6 7 "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. 1 2 "Drug Approval Package: Lastacaft (alcaftadine) Ophthalmic Solution NDA #022134". U.S. Food and Drug Administration (FDA). 24 December 1999. Archived from the original on 3 December 2013. 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. 1 2 3 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.[ dead link ]
  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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