Alcaftadine

Alcaftadine is an H 1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.

• LASTACAFT ® is an H 1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. LASTACAFT ® is an H 1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis.ICD-10: H10.9

• LASTACAFT ® is contraindicated in patients with hypersensitivity to any component in the product.contraindicated

Instill one drop in each eye once daily. If more than 1 topical ophthalmic medicinal product is being used, each one should be administered at least 5 minutes apart. Instill one drop in each eye once daily. ( 2 )

• Potential for Eye Injury and Contamination : To minimize the risk of eye injury and contamination, do not touch dropper tip to eyelids and surrounding areas, or any other surface. Keep bottle tightly closed when not in use. ( 5.1 ) • Contact Lens Wear: LASTACAFT ® should not be used to treat contact lens-related irritation. Remove contact lenses prior to instillation of LASTACAFT ® . ( 5.2 ) 5.1 Potential for Eye Injury and Contamination To minimize eye injury and contamination of the dropper tip and solution, care should be taken not to touch the eyelids or surrounding areas with the dropper tip of the bottle. Keep bottle tightly closed when not in use. 5.2 Contact Lens Use Patients should be advised not to wear a contact lens if their eye is red. LASTACAFT ® should not be used to treat contact lens-related irritation. LASTACAFT ® should not be instilled while wearing contact lenses. Remove contact lenses prior to instillation of LASTACAFT ® . The preservative in LASTACAFT ® , benzalkonium chloride, may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of LASTACAFT ® .

The most common ocular adverse reactions, occurring in less than 4% of eyes treated with LASTACAFT ® , were eye irritation, burning and/or stinging on instillation, eye redness, and eye pruritus. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Allergan at 1-800-678-1605 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The most frequent ocular adverse reactions, occurring in less than 4% of eyes treated with LASTACAFT ® , were eye irritation, burning and/or stinging upon instillation, eye redness and eye pruritus. The most frequent non-ocular adverse reactions, occurring in less than 3% of subjects with eyes treated with LASTACAFT ® , were nasopharyngitis and headache. Some of these events were similar to the underlying disease being studied. 6. 2 Postmarketing Experience The following adverse reactions have been identified during post-approval use of LASTACAFT ® . Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies with LASTACAFT® in pregnant women to inform a drug associated risk. There are limited data with the use of alcaftadine eye drops in pregnant women. In embryofetal studies in rats and rabbits, oral administration of alcaftadine during the period of organogenesis did not produce maternal or embryofetal toxicity at clinically relevant doses. Advise pregnant women of a potential risk to the fetus and mother. LASTACAFT® should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus and mother. The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4%, and of miscarriage is 15 to 20%, of clinically recognized pregnancies. Data Animal Data In rats, oral administration of 5, 20 or 40 mg/kg/day alcaftadine during the period of organogenesis (gestational days 6 – 16) caused maternal lethality at doses of 40 mg/kg. The no observed adverse effect level (NOAEL) for maternal toxicity was 20 mg/kg/day (an exposure 230-times higher than that at the maximum recommended human ophthalmic dose [MRHOD], based on AUC). There were no adverse embryofetal effects up to a dose of 20 mg/kg.

Metabolism

Absorption Following bilateral topical ocular administration of alcaftadine ophthalmic solution, 0.25%, the mean plasma C max of alcaftadine was approximately 60 pg/mL and the median T max occurred at 15 minutes. Plasma concentrations of alcaftadine were below the lower limit of quantification (10 pg/mL) by 3 hours after dosing.

• Jul 28, 2010NDANDA022134Abbvie
• Jun 23, 2023ANDAANDA210659Eugia Pharma
• Mar 1, 2024ANDAANDA209706Gland
• Oct 2, 2024ANDAANDA209290Alembic

1. 1Ocular Hyperaemia29533%
2. 2Eye Irritation16819%
3. 3Eye Pruritus10211%
4. 4Eye Pain10111%
5. 5Eye Swelling819.1%
6. 6Drug Ineffective657.3%
7. 7Hypersensitivity637.1%
8. 8Lacrimation Increased566.3%
9. 9Eye Discharge455.1%
10. 10Eyelid Oedema424.7%
11. 11Erythema Of Eyelid394.4%
12. 12Conjunctivitis384.3%
13. 13Headache364.0%
14. 14Scleral Hyperaemia364.0%
15. 15Vision Blurred364.0%

The 8 most recently updated of 8 ClinicalTrials.gov registrations naming Alcaftadine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Single-Center Evaluation of the Anti-Inflammatory Effects of Lastacaft as Measured by In-Vivo Confocal Microscopy
  Completed · Phase 4 · Interventional · 25 enrolled · ORA, Inc.
  NCT02308501updated 2021-03-18
• Safety and Efficacy of Lastacaft® for the Prevention of Itching Associated With Allergic Conjunctivitis in Korea
  Completed · Observational · 3,423 enrolled · Allergan
  NCT02555761updated 2019-07-05
• A Patient Reported Ocular Comfort Assessment Comparing Bepreve to Lastacaft
  Completed · Observational · 25 enrolled · Cunningham, Derek N., O.D., P.A.
  NCT01339507updated 2016-01-27
• Safety and Efficacy Study of a Eye Drop for Eye Allergy
  Completed · Phase 3 · Interventional · 60 enrolled · Vistakon Pharmaceuticals
  NCT00889330updated 2015-03-06
• A Study to Evaluate the Efficacy of Lastacaft® Compared to Pataday™ and Placebo in Patients With Acute Allergic Conjunctivitis
  Completed · Phase 4 · Interventional · 157 enrolled · Allergan
  NCT01732757updated 2014-01-14
• Ocular Allergy Treatment Practical Impact Trial
  Unknown · Phase 4 · Interventional · 50 enrolled · Starx Research Center, LLC
  NCT01808768updated 2013-05-30
• A Study to Evaluate the Duration of LASTACAFT® in Acute Allergic Conjunctivitis
  Completed · Phase 4 · Interventional · 127 enrolled · Allergan
  NCT01470118updated 2013-02-21
• Comparison of Tolerability Between Two Allergy Drops
  Unknown · Phase 4 · Interventional · 48 enrolled · Hom, Milton M., OD, FAAO
  NCT01390961updated 2011-07-11

Frequently asked questions

How does Alcaftadine work?

Alcaftadine is an H 1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.

What is Alcaftadine used for?

According to FDA labeling, Alcaftadine carries indications including: LASTACAFT ® is an H 1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. LASTACAFT ® is an H 1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Alcaftadine?

Alcaftadine is classified as Other antiallergics, Histamine-1 Receptor Antagonist, Histamine H1 Receptor Antagonists, Antipruritic Activity.

What are the brand names for Alcaftadine?

Alcaftadine is marketed under brand names including Lastacaft.

What are the contraindications for Alcaftadine?

Alcaftadine labeling lists contraindications including: LASTACAFT ® is contraindicated in patients with hypersensitivity to any component in the product.. Always consult the full prescribing information and a clinician.