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  5. Label Information: Lastacaft

FDA Label for Lastacaft

View Indications, Usage & Precautions

Table of Contents

    1. 1 INDICATIONS AND USAGE
    2. 2 DOSAGE AND ADMINISTRATION
    3. 3 DOSAGE FORMS AND STRENGTHS
    4. 4 CONTRAINDICATIONS
    5. 5.1 POTENTIAL FOR EYE INJURY AND CONTAMINATION
    6. 5.2 CONTACT LENS USE
    7. 6 ADVERSE REACTIONS
    8. 6.1 CLINICAL STUDIES EXPERIENCE
    9. 6.2 NON-OCULAR ADVERSE REACTIONS
    10. 6.3 POSTMARKETING EXPERIENCE
    11. 8.1 PREGNANCY
    12. 8.3 NURSING MOTHERS
    13. 8.4 PEDIATRIC USE
    14. 8.5 GERIATRIC USE
    15. 11 DESCRIPTION
    16. 12.1 MECHANISM OF ACTION
    17. OTHER
    18. 13.1 CARCINOGENESIS, MUTAGENESIS, IMPAIRMENT OF FERTILITY
    19. 14 CLINICAL STUDIES
    20. 16 HOW SUPPLIED/STORAGE AND HANDLING
    21. STORAGE AND HANDLING
    22. PACKAGE LABEL.PRINCIPAL DISPLAY PANEL

Lastacaft Product Label

The following document was submitted to the FDA by the labeler of this product Allergan, Inc.. The document includes published materials associated whith this product with the essential scientific information about this product as well as other prescribing information. Product labels may durg indications and usage, generic names, contraindications, active ingredients, strength dosage, routes of administration, appearance, warnings, inactive ingredients, etc.

1 Indications And Usage



LASTACAFT® is an H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis.


2 Dosage And Administration



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.


3 Dosage Forms And Strengths



Topical ophthalmic solution containing alcaftadine, 0.25% (2.5 mg/mL).


4 Contraindications



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


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®.


6 Adverse Reactions



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.


6.1 Clinical Studies Experience



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.


6.2 Non-Ocular Adverse Reactions



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.


6.3 Postmarketing Experience



The following adverse reactions have been identified during postmarketing use of LASTACAFT® in clinical practice. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. These reactions include eye discharge, eye swelling, erythema of eyelid, eyelid edema, lacrimation increased, vision blurred, hypersensitivity reactions including swelling of the face or allergic dermatitis, and somnolence.


8.1 Pregnancy



Pregnancy Category B. Reproduction studies performed in rats and rabbits revealed no evidence of impaired female reproduction or harm to the fetus due to alcaftadine. Oral doses in rats and rabbits of 20 and 80 mg/kg/day, respectively, produced plasma exposure levels approximately 200 and 9000 times the plasma exposure at the recommended human ocular dose. There are however, no adequate and well controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.


8.3 Nursing Mothers



It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when LASTACAFT® is administered to a nursing woman.


8.4 Pediatric Use



Safety and effectiveness in pediatric patients below the age of 2 years have not been established.


8.5 Geriatric Use



No overall differences in safety or effectiveness were observed between elderly and younger subjects.


11 Description



LASTACAFT® is a sterile, topically administered H1 receptor antagonist containing alcaftadine for ophthalmic use.

Alcaftadine is a white to yellow powder with an empirical formula of C19H21N3O and a molecular weight of 307.39.

Contains:

Active: alcaftadine 0.25% (2.5 mg/mL)

Inactives: benzalkonium chloride 0.005% as a preservative; edetate disodium; sodium phosphate, monobasic; purified water; sodium chloride; sodium hydroxide and/or hydrochloric acid (to adjust pH)

Chemical Name: 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-imidazo[2,1-b] [3] benzazepine-3-carboxaldehyde

Structural Formula:

The drug product has a pH of approximately 7 and an osmolality of approximately 290 mOsm/kg.


12.1 Mechanism Of Action



Alcaftadine is an H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.


Other



Absorption

Following bilateral topical ocular administration of alcaftadine ophthalmic solution, 0.25%, the mean plasma Cmax of alcaftadine was approximately 60 pg/mL and the median Tmax occurred at 15 minutes. Plasma concentrations of alcaftadine were below the lower limit of quantification (10 pg/mL) by 3 hours after dosing. The mean Cmax of the active carboxylic acid metabolite was approximately 3 ng/mL and occurred at 1 hour after dosing. Plasma concentrations of the carboxylic acid metabolite were below the lower limit of quantification (100 pg/mL) by 12 hours after dosing. There was no indication of systemic accumulation or changes in plasma exposure of alcaftadine or the active metabolite following daily topical ocular administration.

Distribution

The protein binding of alcaftadine and the active metabolite are 39.2% and 62.7%, respectively.

Metabolism

The metabolism of alcaftadine is mediated by non-CYP450 cytosolic enzymes to the active carboxylic acid metabolite. In vitro studies showed that neither alcaftadine nor the carboxylic acid metabolite substantially inhibited reactions catalyzed by major CYP450 enzymes.

Excretion

The elimination half-life of the carboxylic acid metabolite is approximately 2 hours following topical ocular administration. Based on data following oral administration of alcaftadine, the carboxylic acid metabolite is primarily eliminated unchanged in the urine.

Potential for Eye Injury and Sterility of Dropper Tip

To minimize eye injury and contamination of the dropper tip and solution, patients should be advised to not touch the eyelids or surrounding areas with the dropper tip, as this may contaminate the contents.

Concomitant Use with other Ophthalmic Products or Contact Lenses

If more than one topical ophthalmic drug is being used, the drugs should be administered at least five minutes apart.

Patients should be advised not to wear a contact lens if their eye is red. Patients should be advised that LASTACAFT® should not be used to treat contact lens-related irritation. Patients should also be advised to 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®.


© 2016 Allergan. All rights reserved.
Irvine, CA 92612, U.S.A.
All trademarks are the property of their respective owners.
Made in the U.S.A.
Patented. See: www.allergan.com/products/patent_notices

72468US13


13.1 Carcinogenesis, Mutagenesis, Impairment Of Fertility



Alcaftadine was not mutagenic or genotoxic in the Ames test, the mouse lymphoma assay or the mouse micronucleus assay.

Alcaftadine was found to have no effect on fertility of male and female rats at oral doses up to 20 mg/kg/day (approximately 200 times the plasma exposure at the recommended human ocular dose).


14 Clinical Studies



Clinical efficacy was evaluated in conjunctival allergen challenge (CAC) studies.
LASTACAFT® was more effective than its vehicle in preventing ocular itching in patients with allergic conjunctivitis induced by an ocular allergen challenge, both at 3 minutes post-dosing and at 16 hours post-dosing of LASTACAFT®.

The safety of LASTACAFT® was evaluated in a randomized clinical study of 909 subjects over a period of 6 weeks.


16 How Supplied/Storage And Handling



LASTACAFT® (alcaftadine ophthalmic solution) 0.25% is supplied in an opaque, white low-density polyethylene bottle with a white polystyrene cap.

3 mL fill in 5 mL bottle        NDC 0023-4290-03


Storage And Handling



Storage: Store at 15°-25°C (59°-77°F).


Package Label.Principal Display Panel



NDC 0023-4290-03
LASTACAFT®
(alcaftadine ophthalmic
solution) 0.25%
3 mL Sterile
ALLERGAN


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