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Loprox Cream

Generic Name: ciclopirox olamine
Dosage Form: cream

FOR DERMATOLOGIC USE ONLY.
NOT FOR USE IN EYES.

Rx Only

Loprox Cream Description

LOPROX® Cream (ciclopirox) 0.77% is 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, 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.

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

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

Loprox Cream - Clinical Pharmacology

Mechanism of Action

Ciclopirox is a hydroxypyridone antifungal agent that 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.

Pharmacokinetics

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 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.

Indications and Usage for Loprox Cream

LOPROX® Cream is 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; candidiasis (moniliasis) due to Candida albicans; and tinea (pityriasis) versicolor due to Malassezia furfur.

Contraindications

LOPROX® Cream is contraindicated in individuals who have shown hypersensitivity to any of its components.

Warnings

LOPROX® Cream is not for ophthalmic use.

Keep out of reach of children.

Precautions

If a reaction suggesting sensitivity or chemical irritation should occur with the use of LOPROX® Cream, treatment should be discontinued and appropriate therapy instituted.

Information for Patientss

The patient should be told to:

  1. Use the medication for the full treatment time even though symptoms may have improved and notify the physician if there is no improvement after four weeks.
  2. Inform the physician if the area of application shows signs of increased irritation (redness, itching, burning, blistering, swelling, or oozing) indicative of possible sensitization.
  3. Avoid the use of occlusive wrappings or dressings

Carcinogenesis, Mutagenesis, and Impairment of Fertility

A 104-week dermal carcinogenicity study in mice was conducted with ciclopirox cream applied at doses up to 1.93% (100 mg/kg/day or 300 mg/m2/day). No increase in drug related neoplasms was noted when compared to control.

The following in vitro genotoxicity tests have been conducted with ciclopirox: evaluation of gene mutation in the Ames Salmonella and E. coli assays (negative); chromosome aberration assays in V79 Chinese hamster lung fibroblast cells, with and without metabolic activation (positive); chromosome aberration assays in V79 Chinese hamster lung fibroblast cells in the presence of supplemental Fe3+, with and without metabolic activation (negative); gene mutation assays in the HGPRT-test with V79 Chinese hamster lung fibroblast 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/c 3T3 cells was negative for cell transformation. In an in vivo Chinese hamster bone marrow cytogenetic assay, ciclopirox was negative for chromosome aberrations at a dosage of 5000 mg/kg body weight.

A combined oral fertility and embryofetal developmental study was conducted in rats with ciclopirox olamine. No effect on fertility or reproductive performance was noted at the highest dose tested of 3.85 mg/kg/day ciclopirox (approximately 1.2 times the maximum recommended human dose based on body surface area comparisons).

Pregnancy

Teratogenic Effects

Pregnancy Category B

There are no adequate or well-controlled studies in pregnant women. Therefore, LOPROX® Cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Oral embryofetal developmental studies were conducted in mice, rats, rabbits and monkeys. Ciclopirox or ciclopirox olamine was orally administered during the period of organogenesis. No maternal toxicity, embryotoxicity or teratogenicity were noted at the highest doses of 77, 125, 80 and 38.5 mg/kg/day ciclopirox in mice, rats, rabbits and monkeys, respectively (approximately 11, 37, 51 and 24 times the maximum recommended human dose based on body surface area comparisons, respectively).

Dermal embryofetal developmental studies were conducted in rats and rabbits with ciclopirox olamine dissolved in PEG 400. Ciclopirox olamine was topically administered during the period of organogenesis. No maternal toxicity, embryotoxicity or teratogenicity were noted at the highest doses of 92 mg/kg/day and 77 mg/kg/day ciclopirox in rats and rabbits, respectively (approximately 27 and 49 times the maximum recommended human dose based on body surface area comparisons, respectively).

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 is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients below the age of 10 years have not been established.

Adverse Reactions

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.

Loprox Cream Dosage and Administration

Gently massage LOPROX® Cream 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, the diagnosis should be redetermined. Patients with tinea versicolor usually exhibit clinical and mycological clearing after two weeks of treatment.

How is Loprox Cream Supplied

LOPROX® Cream (ciclopirox) 0.77% is supplied in

90 gram (NDC 43538-540-90)

STORAGE

Store at 15º - 30ºC (59º - 86ºF).

To report SUSPECTED ADVERSE REACTIONS, contact Medimetriks Pharmaceuticals, Inc., at 1-973-882-8812 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Manufactured for:

MEDIMETRIKS
PHARMACEUTICALS, INC.

383 Route 46 West, Fairfield, NJ 07004-2402 USA
www.medimetriks.com

Manufactured by: Teligent, Inc., Buena, NJ 08310

Rev. 01/2016
IP042-R1

PRINCIPAL DISPLAY PANEL - 90 g Tube Carton

NDC 43538-540-90

For Topical Use Only
Not for use in eyes

90 g
Rx Only

LOPROX® (ciclopirox)
Cream, 0.77%

MEDIMETRIKS
PHARMACEUTICALS, INC.

PRINCIPAL DISPLAY PANEL - Kit Carton

NDC 43538-541-90

For Topical Use Only
Not for use in eyes

90 g
Rx Only

LOPROX®
(ciclopirox)
Cream, 0.77%
KIT

KIT CONTAINS:

1 -
LOPROX® (ciclopirox) Cream, 0.77%
90 g Tube
1 -
Rehyla® Hair + Body Cleanser
Net wt. 16 oz. (454 g) Bottle

MEDIMETRIKS
PHARMACEUTICALS, INC.

Established Pharmacological Class
Substance Pharmacological Class
Rehyla Hair and Body Cleanser CLEANSING (COLD CREAMS, CLEANSING LOTIONS, LIQUIDS, AND PADS)
LOPROX 
ciclopirox olamine cream
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:43538-540
Route of Administration TOPICAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
ciclopirox olamine (ciclopirox) ciclopirox 7.7 mg  in 1 g
Inactive Ingredients
Ingredient Name Strength
benzyl alcohol  
cetyl alcohol  
lactic acid, unspecified form  
light mineral oil  
myristyl alcohol  
octyldodecanol  
polysorbate 60  
water  
sorbitan monostearate  
stearyl alcohol  
Product Characteristics
Color WHITE Score     
Shape Size
Flavor Imprint Code
Contains         
Packaging
# Item Code Package Description
1 NDC:43538-540-90 1 TUBE in 1 CARTON
1 90 g in 1 TUBE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA018748 01/14/2016
LOPROX 
ciclopirox olamine kit
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:43538-541
Packaging
# Item Code Package Description
1 NDC:43538-541-90 1 KIT in 1 CARTON
Quantity of Parts
Part # Package Quantity Total Product Quantity
Part 1 1 TUBE 90 g
Part 2 1 BOTTLE, PUMP 454 g
Part 1 of 2
LOPROX 
ciclopirox olamine cream
Product Information
     
Route of Administration TOPICAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Ciclopirox Olamine (ciclopirox) ciclopirox 7.7 mg  in 1 g
Inactive Ingredients
Ingredient Name Strength
benzyl alcohol  
cetyl alcohol  
lactic acid, unspecified form  
light mineral oil  
myristyl alcohol  
octyldodecanol  
polysorbate 60  
water  
sorbitan monostearate  
stearyl alcohol  
Product Characteristics
Color WHITE Score     
Shape Size
Flavor Imprint Code
Contains         
Packaging
# Item Code Package Description
1 90 g in 1 TUBE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA018748 01/14/2016
Part 2 of 2
REHYLA HAIR AND BODY CLEANSER 
lotion/shampoo
Product Information
     
Route of Administration TOPICAL DEA Schedule     
Ingredients
Ingredient Name Quantity
Water  
glyceryl stearate SE  
glycerin  
shea butter  
cetyl alcohol  
cocamidopropyl betaine  
disodium oleamido mipa-sulfosuccinate  
sodium lauroyl sarcosinate  
sodium lauryl sulfoacetate  
soy sterol  
caprylyl glycol  
phenoxyethanol  
sodium chloride  
propylene glycol  
PEG-8 dimethicone  
hyaluronate sodium  
carboxypolymethylene  
laureth-12 succinate  
salicylic acid  
C13-14 isoparaffin  
chamaemelum nobile flower  
hexylene glycol  
laureth-7  
edetate disodium  
Product Characteristics
color WHITE C48325
Packaging
# Item Code Package Description
1 454 g in 1 BOTTLE, PUMP
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
COSMETIC 07/01/2014
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA018748 06/13/2016
Labeler - Medimetriks Pharmaceuticals, Inc. (019903816)
Establishment
Name Address ID/FEI Operations
Teligent, Inc 011036910 MANUFACTURE(43538-540, 43538-541), PACK(43538-541)
Revised: 06/2016
 
Medimetriks Pharmaceuticals, Inc.
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