luliconazole (Rx)

<1%

Application site reactions

Postmarketing Reports

Contact dermatitis

Cellulitis

Contraindications

None

Cautions

For topical use only; not for ophthalmic or intravaginal administration

May inhibit CYP2C19 and CYP3A4 isoenzymes; particularly when treating large surface areas (ie, moderate-to-severe tinea cruris) that result in increased luliconazole systemic exposure

Pregnancy

There are no available data with use in pregnant women to inform a drug-associated risk for major birth defects and miscarriage; in animal reproduction studies with pregnant rats and rabbits, there were no adverse developmental effects observed with subcutaneous administration of luliconazole during organogenesis at doses up to 3 and 24 times, respectively, the maximum recommended human dose (MRHD)

Lactation

There is no information available on presence in human milk, effects of drug on breastfed infant, or effects of drug on milk production after topical application to women who are breastfeeding; lack of clinical data during lactation precludes a clear determination of risk to an infant during lactation; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from therapy or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Imidazole antifungal that alters the fungal cell membrane; interacts with 14-alpha demethylase (an enzyme necessary for conversion of lanosterol to ergosterol), inhibiting the synthesis of ergosterol which is an essential component of the membrane; increases cell permeability causing leakage of cellular contents

Absorption

Tinea pedis

• Peak plasma concentration: 0.4 ng/mL (first dose); 0.93 ng/mL (final dose)
• Peak plasma time: 16.9 hr (first dose); 5.8 hr (final dose)
• AUC: 6.88 ng•hr/mL (first dose); 18.74 ng•hr/mL (final dose)

Tinea cruris

• Peak plasma time: 21 hr (first dose); 6.5 hr (final dose)
• Peak plasma concentration: 4.91 ng/mL (first dose); 7.36 ng/mL (final dose)
• AUC: 85.1 ng•hr/mL (first dose); 121.74 ng•hr/mL (final dose)

Distribution

Protein bound: >99%