Ciclopirox Olamine (Ciclopirox Olamine Topical) - Description and Clinical Pharmacology

FOR DERMATOLOGIC USE ONLY.

NOT FOR USE IN EYES.

Rx only

DESCRIPTION

Ciclopirox Olamine Cream 0.77% is for topical use.

Each gram of Ciclopirox Olamine Cream 0.77% contains 7.70 mg of ciclopirox (as ciclopirox olamine) in a water miscible vanishing cream base consisting of Purified Water USP, Cetyl Alcohol NF, Light Mineral Oil NF, Octyldodecanol NF, Stearyl Alcohol NF, Polysorbate 60 NF, Myristyl Alcohol, Sorbitan Monostearate NF, Lactic Acid USP, and Benzyl Alcohol NF (1%) as preservative.

Ciclopirox Olamine Cream 0.77% contains a synthetic, broad-spectrum, antifungal agent ciclopirox (as ciclopirox olamine). The chemical name is 6-cyclohexyl-1-hydroxy-4-methyl-2(1 H)-pyridone, 2-aminoethanol salt.

The CAS Registry Number is 41621-49-2. The chemical structure is:

CLINICAL PHARMACOLOGY

Ciclopirox is a broad-spectrum, antifungal agent that inhibits the growth of pathogenic dermatophytes, yeasts, and Malassezia furfur. Ciclopirox exhibits fungicidal activity in vitro against isolates of Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis, and Candida albicans.

Pharmacokinetic studies in men with tagged ciclopirox solution in polyethylene glycol 400 showed an average of 1.3% absorption of the dose when it was applied topically to 750 cm² on the back followed by occlusion for 6 hours. The biological half-life was 1.7 hours and excretion occurred via the kidney. Two days after application only 0.01% of the dose applied could be found in the urine. Fecal excretion was negligible.

Penetration studies in human cadaverous skin from the back, with Ciclopirox Olamine Cream 0.77% with tagged ciclopirox showed the presence of 0.8 to 1.6% of the dose in the stratum corneum 1.5 to 6 hours after application. The levels in the dermis were still 10 to 15 times above the minimum inhibitory concentrations.

Autoradiographic studies with human cadaverous skin showed that ciclopirox penetrates into the hair and through the epidermis and hair follicles into the sebaceous glands and dermis, while a portion of the drug remains in the stratum corneum.

Draize Human Sensitization Assay, 21-Day Cumulative Irritancy study, Phototoxicity study, and Photo-Draize study conducted in a total of 142 healthy male subjects showed no contact sensitization of the delayed hypersensitivity type, no irritation, no phototoxicity, and no photo-contact sensitization due to Ciclopirox Olamine Cream 0.77%.