Label: LASTACAFT- alcaftadine solution/ drops

  • Category: HUMAN PRESCRIPTION DRUG LABEL
  • DEA Schedule: None
  • Marketing Status: New Drug Application

Drug Label Information

Updated September 30, 2010

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  • HIGHLIGHTS OF PRESCRIBING INFORMATION
    These highlights do not include all the information needed to use LASTACAFT™ safely and effectively. See full prescribing information for LASTACAFT™.

    LASTACAFT™ (alcaftadine ophthalmic solution) 0.25%
    Initial U.S. Approval: 2010

    INDICATIONS AND USAGE

    LASTACAFT™ is an H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. (1)

    DOSAGE AND ADMINISTRATION

    Instill one drop in each eye once daily. (2)

    DOSAGE FORMS AND STRENGTHS

    Ophthalmic solution containing alcaftadine, 0.25% (2.5 mg/mL) (3)

    WARNINGS AND PRECAUTIONS

    • To minimize the risk of contamination, do not touch dropper tip to any surface. Keep bottle tightly closed when not in use. (5.1)
    • LASTACAFT™ should not be used to treat contact lens-related irritation. (5.2)
    • Remove contact lenses prior to instillation of LASTACAFT™. (5.2)

    ADVERSE REACTIONS

    The most common ocular adverse reactions, occurring in < 4% of LASTACAFT™-treated eyes, were eye irritation, burning and/or stinging on instillation, eye redness, and eye pruritus. (6.1)

    The most common non-ocular adverse reactions, occurring in < 3% of subjects with LASTACAFT™-treated eyes, were nasopharyngitis, headache and influenza. (6.2)

    To report SUSPECTED ADVERSE REACTIONS, contact Allergan at 1-800-433-8871 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

    See 17 for PATIENT COUNSELING INFORMATION.

    Revised: 8/2011

  • Table of Contents

    FULL PRESCRIBING INFORMATION: CONTENTS*

    1 INDICATIONS AND USAGE

    2 DOSAGE AND ADMINISTRATION

    3 DOSAGE FORMS AND STRENGTHS

    4 CONTRAINDICATIONS

    5 WARNINGS AND PRECAUTIONS

    5.1 Contamination of Tip and Solution

    5.2 Contact Lens Use

    5.3 Topical Ophthalmic Use Only

    6 ADVERSE REACTIONS

    6.1 Ocular Adverse Reactions

    6.2 Non-ocular Adverse Reactions

    8 USE IN SPECIFIC POPULATIONS

    8.1 Pregnancy

    8.3 Nursing Mothers

    8.4 Pediatric Use

    8.5 Geriatric Use

    11 DESCRIPTION

    12 CLINICAL PHARMACOLOGY

    12.1 Mechanism of Action

    12.3 Pharmacokinetics

    13 NONCLINICAL TOXICOLOGY

    13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

    14 CLINICAL STUDIES

    16 HOW SUPPLIED/STORAGE AND HANDLING

    17 PATIENT COUNSELING INFORMATION

    17.1 Sterility of Dropper Tip

    17.2 Concomitant Use of Contact Lenses

    17.3 Topical Ophthalmic Use only

    *
    Sections or subsections omitted from the full prescribing information are not listed.
  • 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.

  • 3 DOSAGE FORMS AND STRENGTHS

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

  • 4 CONTRAINDICATIONS

    None.

  • 5 WARNINGS AND PRECAUTIONS

    5.1 Contamination of Tip and Solution

    To minimize contaminating 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™.

    5.3 Topical Ophthalmic Use Only

    LASTACAFT™ is for topical ophthalmic use only.

  • 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 Ocular Adverse Reactions

    The most frequent ocular adverse reactions, occurring in < 4% of LASTACAFT™-treated eyes, 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 < 3% of subjects with LASTACAFT™-treated eyes, were nasopharyngitis, headache and influenza. Some of these events were similar to the underlying disease being studied.

  • 8 USE IN SPECIFIC POPULATIONS

    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). Preservative: benzalkonium chloride 0.005%. Inactives: edetate disodium, monobasic sodium phosphate, 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:

    Structural Formula

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

  • 12 CLINICAL PHARMACOLOGY

    12.1 Mechanism of Action

    Alcaftadine is a 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.

    12.3 Pharmacokinetics

    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.

    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.

    In vitro studies showed that neither alcaftadine nor the carboxylic acid metabolite substantially inhibited reactions catalyzed by major CYP450 enzymes.

  • 13 NONCLINICAL TOXICOLOGY

    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 polypropylene cap.

    3 mL fill in 5 mL bottle      NDC 54868-6294-0

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

  • 17 PATIENT COUNSELING INFORMATION

    17.1 Sterility of Dropper Tip

    Patients should be advised to not touch dropper tip to any surface, as this may contaminate the contents.

    17.2 Concomitant Use of Contact Lenses

    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™.

    17.3 Topical Ophthalmic Use only

    For topical ophthalmic administration only.

    ALLERGAN
    Manufactured for Allergan, Inc., Irvine, CA 92612, U.S.A.
    © 2010 Allergan, Inc.
    ® and ™ marks owned by Allergan, Inc.
    Manufactured in the U.S.A. by JHP Pharmaceuticals, LLC

    72409US10B

    Relabeling and Repackaging by:
    Physicians Total Care, Inc., Tulsa, OK 74146

  • PRINCIPAL DISPLAY PANEL


    NDC 54868-6294-0

    image of package label

    LASTACAFT™

    (alcaftadine ophthalmic

    solution) 0.25%

    3 mL Sterile



  • INGREDIENTS AND APPEARANCE
    LASTACAFT 
    alcaftadine solution/ drops
    Product Information
    Product TypeHUMAN PRESCRIPTION DRUGItem Code (Source)NDC:54868-6294(NDC:0023-4290)
    Route of AdministrationOPHTHALMIC
    Active Ingredient/Active Moiety
    Ingredient NameBasis of StrengthStrength
    alcaftadine (UNII: 7Z8O94ECSX) (alcaftadine - UNII:7Z8O94ECSX) alcaftadine2.5 mg  in 1 mL
    Inactive Ingredients
    Ingredient NameStrength
    benzalkonium chloride (UNII: F5UM2KM3W7)  
    edetate disodium (UNII: 7FLD91C86K)  
    sodium phosphate, monobasic (UNII: 3980JIH2SW)  
    water (UNII: 059QF0KO0R)  
    sodium chloride (UNII: 451W47IQ8X)  
    sodium hydroxide (UNII: 55X04QC32I)  
    hydrochloric acid (UNII: QTT17582CB)  
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    1NDC:54868-6294-01 in 1 CARTON
    13 mL in 1 BOTTLE, PLASTIC
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    NDANDA02213408/19/2011
    Labeler - Physicians Total Care, Inc. (194123980)
    Establishment
    NameAddressID/FEIBusiness Operations
    Physicians Total Care, Inc.194123980relabel, repack
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