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]

Related Research Articles

H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines; other agents may have antihistaminergic action but are not true antihistamines.

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<span class="mw-page-title-main">Allergic conjunctivitis</span> Medical condition

Allergic conjunctivitis (AC) is inflammation of the conjunctiva due to allergy. Although allergens differ among patients, the most common cause is hay fever. Symptoms consist of redness, edema (swelling) of the conjunctiva, itching, and increased lacrimation. If this is combined with rhinitis, the condition is termed allergic rhinoconjunctivitis (ARC).

<span class="mw-page-title-main">Eye drop</span> Liquid applied directly to the eye

Eye drops or eyedrops are liquid drops applied directly to the surface of the eye usually in small amounts such as a single drop or a few drops. Eye drops usually contain saline to match the salinity of the eye. Drops containing only saline and sometimes a lubricant are often used as artificial tears to treat dry eyes or simple eye irritation such as itching or redness. Eye drops may also contain one or more medications to treat a wide variety of eye diseases. Depending on the condition being treated, they may contain steroids, antihistamines, sympathomimetics, beta receptor blockers, parasympathomimetics, parasympatholytics, prostaglandins, nonsteroidal anti-inflammatory drugs (NSAIDs), antibiotics, antifungals, or topical anesthetics.

<span class="mw-page-title-main">Olopatadine</span> Chemical compound

Olopatadine, sold under the brand name Patanol among others, is an antihistamine medication used to decrease the symptoms of allergic conjunctivitis and allergic rhinitis. It is used as eye drops or as a nasal spray. The eye drops generally result in an improvement within half an hour.

<span class="mw-page-title-main">Ketotifen</span> Antihistamine medication

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<span class="mw-page-title-main">Emedastine</span> Chemical compound

Emedastine (trade name Emadine) is a second generation antihistamine used in eye drops to alleviate the symptoms of allergic conjunctivitis. It acts as a H1 receptor antagonist. It works by blocking the action of histamine that causes allergic symptoms. It is used in form of the difumarate. The emedastine difumarate is a white, crystalline, water-soluble fine powder. Emedastine eye drops is usually applied twice a day to the affected eye. When the patients with allergic conjunctivitis were treated with 0.05% emedastine difumarate ophthalmic solution for six weeks, the signs and symptoms such as redness, itching and swelling of the eyes were relieved. Emedastine appears to be devoid of effects on adrenergic, dopaminergic and serotonin receptors. This drug was developed by Alcon, which is global medical company specializing in eye care products.

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Bimatoprost, sold under the brand name Lumigan among others, is a medication used to treat high pressure inside the eye including glaucoma. Specifically it is used for open angle glaucoma when other agents are not sufficient. It may also be used to increase the size of the eyelashes. It is used as an eye drop and effects generally occur within four hours.

<span class="mw-page-title-main">Loteprednol</span> Pharmaceutical drug

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Naphazoline/pheniramine, sold under the brand name Naphcon-A among others, is a combination eye drop used to help the symptoms of allergic conjunctivitis such as from hay fever. It contains naphazoline and pheniramine. It is used as an eye drop. Use is not recommended for more than three days.

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<span class="mw-page-title-main">Bilastine</span> Antihistamine medication

Bilastine is an antihistamine medication used to treat hives (urticaria), allergic rhinitis and itchy inflamed eyes (allergic conjunctivitis) caused by an allergy. It is a second-generation antihistamine and takes effect by selectively inhibiting the histamine H1 receptor, preventing these allergic reactions. Bilastine has an effectiveness similar to cetirizine, fexofenadine, and desloratadine.

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<span class="mw-page-title-main">Netarsudil</span> Chemical compound

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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. 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.
  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.