PDR MEMBER LOGIN:
  • PDR Search

    Required field
  • Advertisement
  • CLASSES

    Ocular Anti-Allergics, Antihistamines

    DEA CLASS

    Rx

    DESCRIPTION

    Ophthalmic H1-blocker for allergic conjunctivitis. Not intended to treat contact lens related irritation.

    COMMON BRAND NAMES

    Emadine

    HOW SUPPLIED

    Emadine Ophthalmic Sol: 0.05%

    DOSAGE & INDICATIONS

    For the temporary relief of the signs and symptoms (e.g., ocular pruritus) of allergic conjunctivitis.
    Ophthalmic dosage
    Adults, Adolescents, and Children >= 3 years

    1 drop in the affected eye(s) up to 4 times per day.

    MAXIMUM DOSAGE

    Adults

    4 drops/day ophthalmic solution in each affected eye.

    Elderly

    4 drops/day ophthalmic solution in each affected eye.

    Adolescents

    4 drops/day ophthalmic solution each affected eye.

    Children

     >= 3 years: 4 drops/day ophthalmic solution in each affected eye.
     < 3 years: 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

    Emedastine is administered topically to the eye.
    Wash hands before and after use. Tilt the head back slightly and pull the lower eyelid down with the index finger. Instill the prescribed number of drops into the conjunctival sac and gently close eyes for 1—2 minutes. Do not blink.
    Care should be taken to avoid contamination. Do not touch the tip of the dropper to the eye, fingertips, or other surface.
    Patients should wait at least ten minutes after instilling the ophthalmic solution before inserting contact lenses.
    Do not share ophthalmic drops between patients.

    STORAGE

    Emadine:
    - Do not use more than 30 days after opening
    - Store below 77 degrees F

    CONTRAINDICATIONS / PRECAUTIONS

    Contact lenses

    Emedastine is contraindicated for use in patients with a known history of hypersensitivity to emedastine or other product ingredients. Emedastine ophthalmic solution is formulated with the preservative benzalkonium chloride, which may be absorbed by soft contact lenses. Users of soft contact lenses should not administer emedastine while wearing contact lenses. Contact lens wearers should wait at least 10 minutes after using emedastine before inserting their lenses. Do not use emedastine to treat contact lens related ocular irritation.

    Children, infants, neonates

    The safety and effectiveness of emedastine in neonates, infants, and children less than 3 years of age have not been established.

    Pregnancy

    Emedastine is classified as FDA pregnancy risk category B. There are no adequate and well-controlled studies in pregnant women, and its ability to cause fetal harm or affect reproductive capacity is unknown. Animal studies have failed to revealed any teratogenic effects at concentrations 15,000-times the maximum recommended ocular human concentration. Because animal studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

    Breast-feeding

    Data are limited regarding use of emedastine during breast-feeding, and its excretion into human milk is unknown. The manufacturer advises caution when administering to lactating mothers; however, exposure of a nursing infant is considered unlikely because systemic absorption is generally below detectable limits (< 0.3 ng/ml) when administered via the ophthalmic route. To minimize the amount of drug that may reach systemic circulation and breast milk, instruct the patient to apply pressure over the tear duct by the corner of the eye for 1 minute after each administration. 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, health care providers are encouraged to report the adverse effect to the FDA.

    ADVERSE REACTIONS

    Severe

    keratitis / Delayed / 0-5.0

    Moderate

    corneal deposits / Delayed / 0-5.0
    hyperemia / Delayed / 0-5.0
    blurred vision / Early / 0-5.0

    Mild

    headache / Early / 11.0-11.0
    dysgeusia / Early / 0-5.0
    sinusitis / Delayed / 0-5.0
    lacrimation / Early / 0-5.0
    rhinitis / Early / 0-5.0
    foreign body sensation / Rapid / 0-5.0
    pruritus / Rapid / 0-5.0
    xerophthalmia / Early / 0-5.0
    ocular irritation / Rapid / 0-5.0
    asthenia / Delayed / 0-5.0

    DRUG INTERACTIONS

    There are no drug interactions associated with Emedastine products.

    PREGNANCY AND LACTATION

    Pregnancy

    Emedastine is classified as FDA pregnancy risk category B. There are no adequate and well-controlled studies in pregnant women, and its ability to cause fetal harm or affect reproductive capacity is unknown. Animal studies have failed to revealed any teratogenic effects at concentrations 15,000-times the maximum recommended ocular human concentration. Because animal studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

    Data are limited regarding use of emedastine during breast-feeding, and its excretion into human milk is unknown. The manufacturer advises caution when administering to lactating mothers; however, exposure of a nursing infant is considered unlikely because systemic absorption is generally below detectable limits (< 0.3 ng/ml) when administered via the ophthalmic route. To minimize the amount of drug that may reach systemic circulation and breast milk, instruct the patient to apply pressure over the tear duct by the corner of the eye for 1 minute after each administration. 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, health care providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    Emedastine is a relatively selective antagonist at H1-receptors. Following topical ocular administration, emedastine blocks H1-receptors and inhibits histamine-stimulated vascular permeability in the conjunctiva. As a result, emedastine relieves the ocular pruritus associated with allergic conjunctivitis. The drug appears to exert no effects on adrenergic, dopaminergic, or serotonergic receptors.

    PHARMACOKINETICS

    Emedastine is administered topically to the eye. In oral administration studies of emedastine, it was shown that approximately 44% of the oral dose is excreted in the urine over 24 hours with only 3.6% of the dose excreted as parent drug. Two primary metabolites, 5- and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. The 5'-oxoanalogs of 5- and 6-hydroxyemedastine and the N-oxide are also formed as minor metabolites. The plasma elimination half-life is approximately 3—4 hours.

    Other Route(s)

    Ophthalmic Route
    Following ocular administration of emedastine, there appears to be low systemic exposure; plasma concentrations were generally below the level of detection of the assay (< 0.3 ng/mL).