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  • CLASSES

    Ocular Anti-Allergics, Antihistamines

    DEA CLASS

    Rx

    DESCRIPTION

    Topical ophthalmic H1-antagonist
    Used for the prevention of ocular pruritus associated with allergic conjunctivitis
    Once daily administration

    COMMON BRAND NAMES

    LASTACAFT

    HOW SUPPLIED

    LASTACAFT Ophthalmic Sol: 0.25%

    DOSAGE & INDICATIONS

    For the prevention of ocular pruritus associated with allergic conjunctivitis.
    Ophthalmic dosage
    Adults, Adolescents, and Children >= 2 years

    Instill 1 drop topically in each eye once daily. Duration of treatment has not been defined by the manufacturer; however, the safety of administering alcaftadine over a 6-week period was evaluated in a clinical study.

    MAXIMUM DOSAGE

    Adults

    1 drop/day ophthalmic solution in each eye.

    Geriatric

    1 drop/day ophthalmic solution in each eye.

    Adolescents

    1 drop/day ophthalmic solution in each eye.

    Children

    >= 2 years: 1 drop/day ophthalmic solution in each eye.
    < 2 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    Renal Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Ophthalmic Administration

    For topical administration to the eyes only.
    Wash hands prior to and after use. Tilt the head back slightly and pull the lower eyelid down with the index finger. Squeeze one drop into the conjunctival sac of each eye and gently close eyes for 1—2 minutes. Do not blink.
    Take care to avoid contamination. Do not touch the tip of the dropper to the eye, fingertips, or other surface.
    Instruct patients to remove contact lenses prior to instilling the ophthalmic solution; contact lenses may be reinserted 10 minutes after administration of the ophthalmic solution.
    If more than 1 topical ophthalmic medication is being used, separate administration by at least 5 minutes.
    Do not share ophthalmic drops between patients.

    STORAGE

    LASTACAFT :
    - Store between 59 to 77 degrees F

    CONTRAINDICATIONS / PRECAUTIONS

    General Information

    Alcaftadine is contraindicated in patients with a history of hypersensitivity to any component of the product.

    Contact lenses

    The manufacturer recommends removing contact lenses prior to and for 10 minutes after administration of alcaftadine ophthalmic solution. Alcaftadine ophthalmic solution is formulated with the preservative benzalkonium chloride 0.005%, which may be absorbed by soft contact lenses. Alcaftadine is not indicated for treatment of contact lens-related irritation. Further, advise patients to avoid wearing contact lenses if their eyes become red.

    Children, infants, neonates

    The safety and efficacy of alcaftadine have not been established in neonates, infants, or children < 2 years of age.

    Pregnancy

    Alcaftadine is classified as pregnancy risk category B. No adequate, well controlled studies in pregnant women are available. Animal studies involving rats (20 mg/kg/day alcaftadine PO) and rabbits (80 mg/kg/day alcaftadine PO) did not result in any harm to the fetus or the female reproductive system. The plasma exposures in the pregnant rats and rabbits were 200 and 9,000 times higher then the plasma exposure after a recommended human ocular dose. Because animal reproductive studies are not always predictive of human response, only administer alcaftadine during pregnancy if clearly needed.

    Breast-feeding

    It is not known whether alcaftadine is excreted into human milk. Because many drugs are excreted in human milk, the manufacturer recommends using caution when administering alcaftadine to women who are breast-feeding. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    ADVERSE REACTIONS

    Severe

    angioedema / Rapid / Incidence not known

    Moderate

    ocular inflammation / Early / Incidence not known
    blurred vision / Early / Incidence not known

    Mild

    ocular irritation / Rapid / 0-4.0
    ocular pain / Early / 0-4.0
    ocular pruritus / Rapid / 0-4.0
    pharyngitis / Delayed / 0-3.0
    headache / Early / 0-3.0
    lacrimation / Early / Incidence not known
    ocular discharge / Delayed / Incidence not known
    drowsiness / Early / Incidence not known

    DRUG INTERACTIONS

    There are no drug interactions associated with Alcaftadine products.

    PREGNANCY AND LACTATION

    Pregnancy

    Alcaftadine is classified as pregnancy risk category B. No adequate, well controlled studies in pregnant women are available. Animal studies involving rats (20 mg/kg/day alcaftadine PO) and rabbits (80 mg/kg/day alcaftadine PO) did not result in any harm to the fetus or the female reproductive system. The plasma exposures in the pregnant rats and rabbits were 200 and 9,000 times higher then the plasma exposure after a recommended human ocular dose. Because animal reproductive studies are not always predictive of human response, only administer alcaftadine during pregnancy if clearly needed.

    It is not known whether alcaftadine is excreted into human milk. Because many drugs are excreted in human milk, the manufacturer recommends using caution when administering alcaftadine to women who are breast-feeding. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    Alcaftadine is a topically active, H1-receptor antagonist and an inhibitor of histamine release from mast cells. After topical ocular administration, alcaftadine inhibits histamine-stimulated vascular permeability in the conjunctiva, thereby preventing the formation of ocular edema and wheal. Alcaftadine has also been shown to decrease chemotaxis and activation of eosinophils. As a result of these pharmacologic actions, alcaftadine relieves ocular pruritus associated with allergic conjunctivitis.

    PHARMACOKINETICS

    Alcaftadine is administered topically to the eyes. Once absorbed, alcaftadine is metabolized by non-CYP450 enzymes to an active metabolite, carboxylic acid. The protein binding of alcaftadine and carboxylic acid are 39.2% and 62.7%, respectively. Carboxylic acid has a half-life of approximately 2 hours and is primarily eliminated unchanged in the urine.

    Other Route(s)

    Ophthalmic Route
    Systemic absorption is limited after ophthalmic administration of alcaftadine. Instilling alcaftadine into both eyes results in a mean peak plasma concentrations (Cmax) of approximately 60 pg/mL. The median time to reach peak plasma concentration (Tmax) is 15 minutes, and the plasma concentrations fall below the limits of quantification (10 pg/mL) by 3 hours post-dose. The Cmax for carboxylic acid is approximately 3 ng/mL and occurs about 1 hour after dosing. The plasma concentrations of carboxylic acid are detectable for up to 12 hours after dosing. According to the manufacturer, there appears to be no systemic accumulation of alcaftadine or the active metabolite after daily topical ocular administration.