Luzu (luliconazole)

Luliconazole, an imidazole derivative, is a synthetic azole antifungal agent.

Luliconazole, a synthetic azole antifungal agent, is an imidazole derivative. Luliconazole, like lanoconazole (not commercially available in the US), contains a dithiolan structure and a chiral center. However, luliconazole contains only the active R-enantiomer of the optical isomer whereas lanoconazole is a racemic compound containing both the active R-enantiomer and inactive S-enantiomer.

The potential for in vitro interconversion between R- and S-enantiomers has not been assessed.

Although the exact mechanism of action of luliconazole has not been fully determined, the antifungal activity of the drug appears to result from interference with ergosterol synthesis via inhibition of C-14 demethylation of sterol intermediates (e.g., lanosterol). This results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and accumulation of lanosterol.

Luliconazole is active in vitro against many dermatophytes, including Epidermophyton floccosum, Trichophyton mentagrophytes, T. rubrum, T. tonsurans, T. verrucosum, T. violaceum, Microsporum canis, and M. gypseum. Luliconazole also has in vitro activity against some other fungi, including Candida albicans, Malassezia furfur, M. restricta, M. slooffiae, and M. sympodialis. There is some evidence that luliconazole may be more active than terbinafine against dermatophytes and C. albicans in vitro.

Following topical application of luliconazole 1% cream to skin, low concentrations of the drug are absorbed systemically. In a study in 8 adults with moderate to severe tinea cruris and 12 adults with moderate to severe tinea pedis, luliconazole 1% cream was applied to affected and surrounding areas of skin once daily (approximately 3.5 g daily) for 15 days. In those with tinea cruris, mean peak plasma concentrations of luliconazole were 4.91 ng/mL after the first dose and 7.36 ng/mL after the final dose; the time to peak plasma concentrations was 21 and 6.5 hours, respectively.

In those with tinea pedis, mean peak plasma concentrations of luliconazole were 0.4 ng/mL after the first dose and 0.93 ng/mL after the final dose; the time to peak plasma concentrations was 16.9 and 5.8 hours, respectively. On day 15, the mean plasma half-life of luliconazole was 21.1 hours in those with tinea cruris and 32.4 hours in those with tinea pedis. In vitro studies suggest that systemically absorbed luliconazole may be metabolized by cytochrome P-450 (CYP) isoenzymes 2D6 and 3A4.

USES: Luliconazole is used to treat skin infections such as athlete's foot, jock itch, and ringworm. Luliconazole is an azole antifungal that works by preventing the growth of the fungus.

Generic name: luliconazole
Pronunciation: (LOO-li-KON-a-zole)
Drug class: Topical Antifungals
Therapeutic class: Dermatological

The following indications are listed for Luzu:

• Tinea Corporis
• Tinea Cruris
• Tinea Pedis

Also known as: Corporeal Ringworm, Dermatomycosis Pedis, Dhobie Itch, Eczema Marginatum, Jock Itch, Tinea Circinata, Tinea Glabrosa, Tinea Inguinalis, Tinea Of The Foot.