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Mechanism of Action
Ciclopirox acts by chelation of polyvalent cations (Fe3+ or Al3+) resulting in the inhibition of the metal-dependent enzymes that are responsible for the degradation of peroxides within the fungal cell.
In vitro studies showed that ciclopirox inhibited the formation of 5-lipoxygenase inflammatory mediators (5-HETE and LTB4) and also inhibited PGE2 release in a cell culture model. In vivo, ciclopirox inhibited inflammation in an arachidonic acid-induced murine ear edema model. The clinical significance of these findings is unknown.
A comparative study of the pharmacokinetics of LOPROX® GeI and LOPROX® Cream (ciclopirox olamine) 0.77% in 18 healthy males indicated that systemic absorption of ciclopirox from LOPROX® Gel (ciclopirox gel) was higher than that of LOPROX® Cream. A 5 gm dose of LOPROX® Gel (ciclopirox gel) produced a mean (±SD) peak serum concentration of 25.02 (±20.6) ng/mL total ciclopirox and 5 gm of LOPROX® Cream produced 18.62 (±13.56) ng/mL total ciclopirox. Approximately 3% of the applied ciclopirox was excreted in the urine within 48 hours after application, with a renal elimination half-life of about 5.5 hours.
In a study of LOPROX® Gel (ciclopirox gel) , 16 men with moderate to severe tinea cruris applied approximately 15 grams/day of the gel for 14.5 days. The mean (±SD) dose-normalized values of Cmax for total ciclopirox in serum were 100 (±42) ng/mL on Day 1 and 238 (±144) ng/mL on Day 15. During the 10 hours after dosing on Day 1, approximately 10% of the administered dose was excreted in the urine.
Ciclopirox is a hydroxypyridinone antifungal agent that inhibits the growth of pathogenic dermatophytes. Ciclopirox has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section:
Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.
Last reviewed on RxList: 11/5/2008
This monograph has been modified to include the generic and brand name in many instances.
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