Loprox Cream (Ciclopirox Olamine)

LOPROX®

Hoechst Marion Roussel

Ciclopirox Olamine

Topical Antifungal

Action And Clinical Pharmacology: Ciclopirox is a synthetic broad spectrum antifungal agent that inhibits the growth of pathogenic dermatophytes, yeasts, and M. furfur. It exhibits fungicidal activity in vitro against isolates of T. rubrum, T. mentagrophytes, E. floccosum, M. canis and C. albicans.

The mode of action of ciclopirox olamine was studied mainly in C. albicans. It is presumed that ciclopirox mediated growth inhibition or death of fungal cells is primarily caused by in vitro cellular depletion of some essential substrates and/or ions and that such effects are brought about through blockage of their uptake from the medium.

No data on mechanism of action are available for dermatophytes.

Penetration studies in human cadaverous skin with tagged ciclopirox cream 1% showed the presence of 0.8 and 1.6% of the dose in 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 through the epidermis, hair follicles, into the dermis, hair and the sebaceous gland with a depot or reservoir in the stratum corneum.

Pharmacokinetic studies in males with tagged ciclopirox cream 1% showed an average of 1.3% absorption of the dose. The cream was applied topically under occlusion to the back, with a total penetration time of 6 hours. Excretion occurred via the kidney, with biological half-life of 1.7 hours. Two days after application only 0.01% of the dose applied could be found in the urine.

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 1%. The ingredients of ciclopirox lotion 1% are qualitatively the same as those of ciclopirox cream 1%.

Microbiology: Ciclopirox can be best described as a broad spectrum antimycotic agent with significant antibacterial activity. It is also effective against several protozoa.

Indications And Clinical Uses: For the topical treatment of the following dermal infections; tinea pedis, tinea cruris and tinea corporis due to T. rubrum, T. mentagrophytes, E. floccosum, M. canis; cutaneous candidiasis (moniliasis) due to C. albicans; and tinea (pityriasis) versicolor due to M. furfur.

It is not proposed for vaginal application.

Contra-Indications: In individuals who have shown hypersensitivity to any of the product components.

Manufacturers’ Warnings In Clinical States: Not for ophthalmic use.

Precautions: If a reaction suggesting sensitivity or chemical irritation should occur with the use of ciclopirox, treatment should be discontinued and appropriate therapy instituted.

Pregnancy: Reproduction studies have been performed in the mouse, rat, rabbit and monkey (via various routes of administration) at doses 10 times or greater than the topical human dose. No significant evidence of impaired fertility or harm to the fetus due to the use of ciclopirox has been revealed. However, a higher incidence of systemic absorption of ciclopirox in the rat was noted in the group given 30 mg/kg orally as compared to controls. There are, however, no adequate or well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Lactation: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when ciclopirox is administered to nursing women.

Children: Safety and effectiveness in children below the age of 10 years have not been established.

Adverse Reactions: Ciclopirox is well tolerated with a low incidence of adverse reactions reported in clinical trials. Ciclopirox cream had a 0.4% incidence of adverse reactions in controlled clinical trials. These included pruritus at the site of application, worsening of clinical signs and symptoms and mild to severe burning reported in a few cases.

In a controlled clinical trial with 89 patients using ciclopirox lotion and 89 patients using the vehicle, the incidence of adverse reactions was low. The side effects included pruritus occurring in 3 patients and burning, which occurred in 1 patient.

Symptoms And Treatment Of Overdose: Symptoms and Treatment: There have been no clinical reports of acute overdosage with ciclopirox cream or lotion by any route of administration.

From acute toxicity studies of ciclopirox cream 1% in adult rats, oral doses of 36 g/kg produced no evidence of toxic signs.

Dosage: Gently massage into the affected and surrounding skin areas twice daily, in the morning and evening, for a minimum of 4 weeks. Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment. If a patient shows no clinical improvement after 2 weeks of treatment with ciclopirox the diagnosis should be redetermined. Patients with tinea versicolor usually exhibit clinical and mycological clearing after 2 weeks of treatment.

Availability And Storage: Cream: Each tube contains: ciclopirox olamine USP 1%. Nonmedicinal ingredients: benzyl alcohol, cetyl alcohol, cocamide DEA, lactic acid, mineral oil, myristyl alcohol, octyldodecanol, polysorbate 60, sorbitan monostearate, stearyl alcohol, and purified water. Tubes of 15 and 30 g.

Lotion: Each bottle contains: ciclopirox olamine USP 1%. Nonmedicinal ingredients: benzyl alcohol, cetyl alcohol, cocamide DEA, lactic acid, mineral oil, myristyl alcohol, octyldodecanol, polysorbate 60, sorbitan monostearate, stearyl alcohol, and purified water. Bottles of 30 mL.

Store at room temperature below 25°C.

LOPROX® Hoechst Marion Roussel Ciclopirox Olamine Topical Antifungal

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