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  • CLASSES

    Topical Dermatological Antifungals

    DEA CLASS

    Rx

    DESCRIPTION

    Topical azole antifungal solution
    Indicated for treatment of onychomycosis of the toenails in adults
    Onychocryptosis (ingrown toenail) was the most frequently reported adverse event during clinical trials

    COMMON BRAND NAMES

    JUBLIA

    HOW SUPPLIED

    JUBLIA Topical Sol: 10%

    DOSAGE & INDICATIONS

    For the treatment of onychomycosis of the toenail(s) caused by Trichophyton rubrum and Trichophyton mentagrophytes.
    Topical dosage
    Adults

    Apply solution, using the integrated brush applicator, topically to the affected toenail(s) once daily for 48 weeks. Ensure the entire toenail (toenail beds, folds, hyponychium, and undersurface of the toenail plate) is completely covered.

    MAXIMUM DOSAGE

    Adults

    Specific maximum dosage information not available.

    Geriatric

    Specific maximum dosage information not available.

    Adolescents

    Safety and efficacy have not been established.

    Children

    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

    Topical Administration

    For topical use on toenails only; not for ophthalmic, oral, or intravaginal use.
    Instruct patients to avoid pedicures, and use of nail polish or cosmetic nail products during treatment.
    Efinaconazole solution is flammable. Avoid heat, flame, and tobacco smoking during and immediately following application.

    Other Topical Formulations

    Topical Nail Solution:
    Clean and dry toenails prior to application. Instruct patients to wait at least 10 minutes after showering, bathing, or washing before applying.
    Hold the bottle upside down directly over the affected toenail. Lightly squeeze the bottle to release 1 drop onto the toenail. For the big toenail, squeeze a 2nd drop to the end of the toenail.
    Spread the drop(s) around the affected toenail(s) using the integrated brush applicator. Ensure the entire toenail (toenail bed, folds, hyponychium, and undersurface of the toenail plate) is completely covered.
    Allow solution to dry completely.
    Wash hands with soap and water after the application process.

    STORAGE

    JUBLIA:
    - Flammable, keep away from heat and flame
    - Protect from freezing
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F

    CONTRAINDICATIONS / PRECAUTIONS

    Ocular exposure, ophthalmic administration, vaginal administration

    Efinaconazole is only approved for external use on toenails; it is not for ophthalmic administration, oral administration, or vaginal administration. During topical application, take care to avoid accidental ocular exposure.

    Pregnancy

    Efinaconazole is classified as a FDA pregnancy category C drug. There are no adequate or well-controlled studies in pregnancy women. Animal studies involving rats revealed embryofetal toxicities (embryofetal deaths, decreased live fetuses, placental effects) following subcutaneous administration of doses 559-times the maximum recommended human dose. Of note, these embryofetal toxicities occurred in the presence of maternal toxicities. No fetal malformations have been observed. Administer during pregnancy only if the potential benefits justify the potential risks to the fetus.

    Breast-feeding

    Data are limited regarding use of efinaconazole during breast-feeding, and its' excretion into human milk is unknown. 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. 

    Azole antifungals hypersensitivity

    Efinaconazole is an azole antifungal; caution is advised when applying to patients with a history of azole antifungals hypersensitivity. Instruct patients to discontinue use of the drug and seek immediate medical attention if a hypersensitivity reaction develops during treatment.

    Tobacco smoking

    Efinaconazole solution is flammable. Avoid heat, flame, and tobacco smoking during and immediately following application.

    ADVERSE REACTIONS

    Moderate

    contact dermatitis / Delayed / 2.2-2.2

    DRUG INTERACTIONS

    There are no drug interactions associated with Efinaconazole products.

    PREGNANCY AND LACTATION

    Pregnancy

    Efinaconazole is classified as a FDA pregnancy category C drug. There are no adequate or well-controlled studies in pregnancy women. Animal studies involving rats revealed embryofetal toxicities (embryofetal deaths, decreased live fetuses, placental effects) following subcutaneous administration of doses 559-times the maximum recommended human dose. Of note, these embryofetal toxicities occurred in the presence of maternal toxicities. No fetal malformations have been observed. Administer during pregnancy only if the potential benefits justify the potential risks to the fetus.

    Data are limited regarding use of efinaconazole during breast-feeding, and its' excretion into human milk is unknown. 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

    Efinaconazole exerts its antifungal activity by inhibiting fungal lanosterol 14-alpha-demethylase, an enzyme necessary for the biosynthesis of ergosterol. Ergosterol is an essential component of fungal cell membranes. By decreasing ergosterol concentrations, the fungal cell membrane permeability is increased, resulting in leakage of cellular contents.

    PHARMACOKINETICS

    Efinaconazole is applied topically to toenails. In healthy volunteers, the plasma half-life of efinaconazole, following 7 daily applications to all 10 toenails, was 29.9 hours. Distribution, metabolism, and excretion data are not available.
     
    Affected cytochrome P450 isoenzymes: None
    Based on data from in vitro studies, therapeutic concentrations of efinaconazole do NOT inhibit CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2PE1, nor CYP3A4. In addition, the drug does NOT induce CYP1A2 or CYP3A4.

    Topical Route

    Pharmacokinetic parameters were evaluated in 18 patients with severe onychomycosis. The drug was administered topically once daily for 28 days to patients' 10 toenails and 0.5 cm of adjacent skin. On treatment day 28, the mean plasma Cmax was 0.67 +/- 0.37 ng/mL and the mean AUC was 12.15 +/- 6.91 ng x hour/mL. At steady state, plasma drug concentrations generally remain consistent over a 24-hour dosing interval.