JUBLIA

Topical Dermatological Antifungals

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

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 second 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.

contact dermatitis / Delayed / 2.2-2.2
erythema / Early / Incidence not known
Onychomadesis / Delayed / Incidence not known

nail discoloration / Delayed / Incidence not known

JUBLIA

Rx

Topical azole antifungal solution
Used for the treatment of onychomycosis of the toenails in adults and pediatric patients 6 years and older
Onychocryptosis (ingrown toenail) was the most frequently reported adverse event during clinical trials

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.

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.[57382]

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

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

There are no drug interactions associated with Efinaconazole products.

JUBLIA Topical Sol: 10%

Specific maximum dosage information not available.

Specific maximum dosage information not available.

Specific maximum dosage information not available.

6 to 12 years: Specific maximum dosage information not available.
1 to 5 years: Safety and efficacy have not been established.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

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.

Efinaconazole is applied topically to toenails. In healthy volunteers, the plasma half-life of efinaconazole, after 7 daily applications to all 10 toenails, was 29.9 hours. Distribution, metabolism, and excretion data are not available.[57382]
 
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.[57382]

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.

There are no adequate or well-controlled studies of efinaconazole use during human pregnancy to inform any drug-associated risks of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies, efinaconazole did not cause any fetal malformations when administered to pregnant rabbits and rats during the period of organogenesis at subcutaneous doses up to 112 and 154 times, respectively, the maximum recommended human dose (MRHD) based on AUC comparisons. Embryofetal toxicities (embryofetal deaths, decreased live fetuses, placental effects) were observed only in rats in the presence of maternal toxicity at systemic exposures 559 times the MRHD based on AUC comparisons. Subcutaneous efinaconazole administration to pregnant rats from the beginning of organogenesis through the end of lactation did not cause embryofetal toxicity or developmental effects at systemic exposures 17 times the MRHD based on AUC comparisons.[57382]

It is unknown if efinaconazole is excreted in human milk. After repeated subcutaneous injection, efinaconazole was detected in the milk of nursing rats. 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.[57382]