 |
FOR DERMATOLOGIC USE ONLY.
NOT FOR USE IN EYES.
Rx Only
LOPROX® (ciclopirox) Cream 0.77% and LOPROX® (ciclopirox) Lotion 0.77% are for topical use.
Each gram of LOPROX Cream contains 7.70 mg of Ciclopirox (as Ciclopirox Olamine) in a water miscible vanishing cream base consisting of Purified Water USP, Octyldodecanol NF, Mineral Oil USP, Stearyl Alcohol NF, Cetyl Alcohol NF, Cocamide DEA, Polysorbate 60 NF, Myristyl Alcohol NF, Sorbitan Monostearate NF, Lactic Acid USP, and Benzyl Alcohol NF (1%) as preservative.
Each gram of LOPROX Lotion contains 7.70 mg of Ciclopirox (as Ciclopirox Olamine) in a water miscible lotion base consisting of Purified Water USP, Cocamide DEA, Octyldodecanol NF, Mineral Oil USP, Stearyl Alcohol NF, Cetyl Alcohol NF, Polysorbate 60 NF, Myristyl Alcohol NF, Sorbitan Monostearate NF, Lactic Acid USP, and Benzyl Alcohol NF (1%) as preservative.
LOPROX Cream and Lotion contain 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.
|
|
LOPROX Cream and Lotion have a pH of 7.
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 cm 2 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 LOPROX Cream 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 LOPROX Cream.
In vitro penetration studies in frozen or fresh excised human cadaver and pig skin indicated that the penetration of LOPROX Lotion is equivalent to that of LOPROX Cream. Therapeutic equivalence of cream and lotion formulations also was indicated by studies of experimentally induced guinea pig and human trichophytosis.
LOPROX Cream and Lotion are indicated for the topical treatment of the following dermal infections: tinea pedis, tinea cruris, and tinea corporis due to Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis ; cutaneous candidiasis (moniliasis) due to Candida albicans ; and tinea (pityriasis) versicolor due to Malassezia furfur.
LOPROX Cream and Lotion are contraindicated in individuals who have shown hypersensitivity to any of its components.
General: LOPROX Cream and Lotion are not for ophthalmic use. Keep out of reach of children.
If a reaction suggesting sensitivity or chemical irritation should occur with the use of LOPROX Cream or Lotion, treatment should be discontinued and appropriate therapy instituted.
The patient should be told to:
Carcinogenesis, Mutagenesis, Impairment of Fertility: A carcinogenicity study in female mice dosed cutaneously twice per week for 50 weeks followed by a 6-month drug-free observation period prior to necropsy revealed no evidence of tumors at the application site.
The following in vitro and in vivo genotoxicity tests have been conducted with ciclopirox olamine: studies to evaluate gene mutation in the Ames Salmonella /Mammalian Microsome Assay (negative) and Yeast Saccharomyces Cerevisiae Assay (negative) and studies to evaluate chromosome aberrations in vivo in the Mouse Dominant Lethal Assay and in the Mouse Micronucleus Assay at 500 mg/kg (negative).
The following battery of in vitro genotoxicity tests were conducted with ciclopirox: a chromosome aberration assay in V79 Chinese Hamster Cells, with and without metabolic activation (positive); a gene mutation assay in the HGPRT - test with V79 Chinese Hamster Cells (negative); and a primary DNA damage assay (i.e., unscheduled DNA Synthesis Assay in A549 Human Cells (negative)). An in vitro Cell Transformation Assay in BALB/C3T3 Cells was negative for cell transformation. In an in vivo Chinese Hamster Bone Marrow Cytogenetic Assay, ciclopirox was negative for chromosome aberrations at 5000 mg/kg.
Pregnancy Category B: Reproduction studies have been performed in the mouse, rat, rabbit, and monkey, (via various routes of administration) at doses 10 times or more the topical human dose and have revealed no significant evidence of impaired fertility or harm to the fetus due to ciclopirox. 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.
Nursing Mothers: 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 LOPROX Cream or Lotion is administered to a nursing woman.
Pediatric Use: Safety and effectiveness in pediatric patients below the age of 10 years have not been established.
In all controlled clinical studies with 514 patients using LOPROX Cream and in 296 patients using the vehicle cream, the incidence of adverse reactions was low. This included pruritus at the site of application in one patient and worsening of the clinical signs and symptoms in another patient using ciclopirox cream and burning in one patient and worsening of the clinical signs and symptoms in another patient using the vehicle cream.
In the controlled clinical trial with 89 patients using LOPROX Lotion and 89 patients using the vehicle, the incidence of adverse reactions was low. Those considered possibly related to treatment or occurring in more than one patient were pruritus, which occurred in two patients using ciclopirox lotion and one patient using the lotion vehicle, and burning, which occurred in one patient using ciclopirox lotion.
Gently massage LOPROX Cream or Lotion into the affected and surrounding skin areas twice daily, in the morning and evening. 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 four weeks of treatment with LOPROX Cream or Lotion, the diagnosis should be redetermined. Patients with tinea versicolor usually exhibit clinical and mycological clearing after two weeks of treatment.
LOPROX® (ciclopirox) Cream 0.77% is supplied in 15 gram (NDC 99207-009-15), 30 gram (NDC 99207-009-30), and 90 gram (NDC 99207-009-90) tubes.
Store at controlled room temperature 15°- 30°C (59°- 86°F).
LOPROX® (ciclopirox) Lotion 0.77% is supplied in 30 mL bottles (NDC 99207-008-30), and 60 mL bottles (NDC 99207-008-60).
Bottle space provided to allow for vigorous shaking before each use.
Store between 5° and 25°C (41° and 77°F).
REG TM THE AVENTIS GROUP
Manufactured for:
MEDICIS, The Dermatology Company®
Scottsdale, AZ 85258
LOPROX Cream by:
Hoechst Marion Roussel
Deutschland GmbH
D-65926 Frankfurt am Main
LOPROX Lotion by:
West Pharmaceutical Services Lakewood, Inc.
Lakewood, NJ 08701