Label: LOPROX- ciclopirox olamine suspension
LOPROX- ciclopirox olamine kit

  • NDC Code(s): 43538-550-60, 43538-551-60
  • Packager: Medimetriks Pharmaceuticals, Inc.
  • Category: HUMAN PRESCRIPTION DRUG LABEL
  • DEA Schedule: None
  • Marketing Status: New Drug Application

Drug Label Information

Updated November 30, 2018

If you are a consumer or patient please visit this version.

  • SPL UNCLASSIFIED SECTION

    For Topical Use Only
    Not for use in eyes

    Rx Only

  • DESCRIPTION

    LOPROX® (ciclopirox) Topical Suspension, 0.77% is for topical use.

    Each gram of LOPROX® Topical Suspension contains 7.70 mg of ciclopirox (as ciclopirox olamine) in a water miscible suspension 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, lactic acid USP, sorbitan monostearate NF, and benzyl alcohol NF (1%) as preservative.

    LOPROX® Topical Suspension 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.

    LOPROX® Topical Suspension has a pH of 7.

    The chemical structure is:

    Chemical Structure
  • 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 radiolabeled 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. Autoradiographic studies with human cadaver 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.

    In vitro penetration studies in frozen or fresh excised human cadaver and pig skin indicated that the penetration of LOPROX® Topical Suspension is equivalent to that of LOPROX® (ciclopirox) Cream, 0.77%. Therapeutic equivalence of cream and suspension formulations also was indicated by studies of experimentally induced guinea pig and human trichophytosis.

  • INDICATIONS AND USAGE

    LOPROX® Topical Suspension 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; ; cutaneous candidiasis (moniliasis) due to Candida albicans; and tinea (pityriasis) versicolor due to Malassezia furfur.

  • CONTRAINDICATIONS

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

  • WARNINGS

    General

    LOPROX® Topical Suspension 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® Topical Suspension, treatment should be discontinued and appropriate therapy instituted.

    Information for Patients

    The patient should be told to:

    1. Use the medication for the full treatment time even though signs/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, oozing) indicative of possible sensitization.
    3. Avoid the use of occlusive wrappings or dressings

    Carcinogenesis, Mutagenesis, 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® Topical Suspension 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. Caution should be exercised when LOPROX® Topical Suspension 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 the controlled clinical trial with 89 patients using LOPROX® Topical Suspension 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 suspension and one patient using the suspension vehicle, and burning, which occurred in one patient using ciclopirox suspension.

  • DOSAGE AND ADMINISTRATION

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

  • HOW SUPPLIED

    LOPROX® (ciclopirox) Topical Suspension, 0.77% is supplied in

    60 mL bottles (NDC 43538-550-60)

    Bottle space provided to allow for vigorous shaking before each use.

    Store between 5° - 25°C (41° - 77°F).

    To report SUSPECTED ADVERSE REACTIONS, contact Medimetriks Pharmaceuticals, Inc., at 1-973-882-7512 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

  • SPL UNCLASSIFIED SECTION

    Manufactured for:
    MEDIMETRIKS
    PHARMACEUTICALS, INC.
    383 Route 46 West, Fairfield, NJ 07004-2402 USA
    www.medimetriks.com

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

    Rev. 03/2016
    IP043-R1

  • PRINCIPAL DISPLAY PANEL - 60 mL Bottle Carton

    NDC 43538-550-60

    For Topical Use Only
    Not for use in eyes

    60 mL

    LOPROX®
    (ciclopirox)
    Topical
    Suspension,
    0.77%

    Rx Only

    MEDIMETRIKS
    PHARMACEUTICALS, INC.

    PRINCIPAL DISPLAY PANEL - 60 mL Bottle Carton

    PRINCIPAL DISPLAY PANEL - Kit Carton

    NDC 43538-551-60

    For Topical Use Only
    Not for use in eyes

    60mL
    Rx Only

    LOPROX®
    (ciclopirox)
    Topical
    Suspension,
    0.77%
    KIT

    KIT CONTAINS:

    1 -
    LOPROX® (ciclopirox) Topical Suspension, 0.77%
    60 mL Bottle
    1 -
    Rehyla® Hair + Body Cleanser
    Net wt. 16 oz. (454 g) Bottle

    MEDIMETRIKS
    PHARMACEUTICALS, INC.

    PRINCIPAL DISPLAY PANEL - Kit Carton
  • INGREDIENTS AND APPEARANCE
    LOPROX 
    ciclopirox olamine suspension
    Product Information
    Product TypeHUMAN PRESCRIPTION DRUGItem Code (Source)NDC:43538-550
    Route of AdministrationTOPICAL
    Active Ingredient/Active Moiety
    Ingredient NameBasis of StrengthStrength
    ciclopirox olamine (UNII: 50MD4SB4AP) (ciclopirox - UNII:19W019ZDRJ) ciclopirox7.7 mg  in 1 mL
    Inactive Ingredients
    Ingredient NameStrength
    benzyl alcohol (UNII: LKG8494WBH)  
    cetyl alcohol (UNII: 936JST6JCN)  
    lactic acid, unspecified form (UNII: 33X04XA5AT)  
    mineral oil (UNII: T5L8T28FGP)  
    myristyl alcohol (UNII: V42034O9PU)  
    octyldodecanol (UNII: 461N1O614Y)  
    water (UNII: 059QF0KO0R)  
    polysorbate 60 (UNII: CAL22UVI4M)  
    sorbitan monostearate (UNII: NVZ4I0H58X)  
    stearyl alcohol (UNII: 2KR89I4H1Y)  
    Coco Diethanolamide (UNII: 92005F972D)  
    Product Characteristics
    ColorWHITEScore    
    ShapeSize
    FlavorImprint Code
    Contains    
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    1NDC:43538-550-601 in 1 CARTON10/14/2016
    160 mL in 1 BOTTLE; Type 0: Not a Combination Product
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    NDANDA01982410/14/2016
    LOPROX 
    ciclopirox olamine kit
    Product Information
    Product TypeHUMAN PRESCRIPTION DRUGItem Code (Source)NDC:43538-551
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    1NDC:43538-551-601 in 1 CARTON10/14/2016
    Quantity of Parts
    Part #Package QuantityTotal Product Quantity
    Part 11 BOTTLE 60 mL
    Part 21 BOTTLE, PUMP 454 g
    Part 1 of 2
    LOPROX 
    ciclopirox olamine suspension
    Product Information
    Item Code (Source)NDC:43538-550
    Route of AdministrationTOPICAL
    Active Ingredient/Active Moiety
    Ingredient NameBasis of StrengthStrength
    ciclopirox olamine (UNII: 50MD4SB4AP) (ciclopirox - UNII:19W019ZDRJ) ciclopirox7.7 mg  in 1 mL
    Inactive Ingredients
    Ingredient NameStrength
    benzyl alcohol (UNII: LKG8494WBH)  
    cetyl alcohol (UNII: 936JST6JCN)  
    lactic acid, unspecified form (UNII: 33X04XA5AT)  
    mineral oil (UNII: T5L8T28FGP)  
    myristyl alcohol (UNII: V42034O9PU)  
    octyldodecanol (UNII: 461N1O614Y)  
    polysorbate 60 (UNII: CAL22UVI4M)  
    water (UNII: 059QF0KO0R)  
    sorbitan monostearate (UNII: NVZ4I0H58X)  
    stearyl alcohol (UNII: 2KR89I4H1Y)  
    Coco Diethanolamide (UNII: 92005F972D)  
    Product Characteristics
    ColorWHITEScore    
    ShapeSize
    FlavorImprint Code
    Contains    
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    160 mL in 1 BOTTLE; Type 0: Not a Combination Product
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    NDANDA01982410/14/2016
    Part 2 of 2
    REHYLA HAIR AND BODY CLEANSER 
    cleansing (cold creams, cleansing lotions, liquids, and pads) lotion/shampoo
    Product Information
    Route of AdministrationTOPICAL
    Other Ingredients
    Ingredient KindIngredient NameQuantity
    INGRWater (UNII: 059QF0KO0R)  
    INGRglyceryl stearate SE (UNII: FCZ5MH785I)  
    INGRglycerin (UNII: PDC6A3C0OX)  
    INGRSHEA BUTTER (UNII: K49155WL9Y)  
    INGRcetyl alcohol (UNII: 936JST6JCN)  
    INGRcocamidopropyl betaine (UNII: 5OCF3O11KX)  
    INGRDISODIUM OLEAMIDO MIPA-SULFOSUCCINATE (UNII: 0MBZ20845F)  
    INGRsodium lauroyl sarcosinate (UNII: 632GS99618)  
    INGRsodium lauryl sulfoacetate (UNII: D0Y70F2B9J)  
    INGRSOY STEROL (UNII: PL360EPO9J)  
    INGRcaprylyl glycol (UNII: 00YIU5438U)  
    INGRphenoxyethanol (UNII: HIE492ZZ3T)  
    INGRsodium chloride (UNII: 451W47IQ8X)  
    INGRpropylene glycol (UNII: 6DC9Q167V3)  
    INGRPEG-8 dimethicone (UNII: GIA7T764OD)  
    INGRHYALURONATE SODIUM (UNII: YSE9PPT4TH)  
    INGRCARBOXYPOLYMETHYLENE (UNII: 0A5MM307FC)  
    INGRlaureth-12 succinate (UNII: 8W3F9H704N)  
    INGRsalicylic acid (UNII: O414PZ4LPZ)  
    INGRC13-14 ISOPARAFFIN (UNII: E4F12ROE70)  
    INGRCHAMAEMELUM NOBILE FLOWER (UNII: O2T154T6OG)  
    INGRhexylene glycol (UNII: KEH0A3F75J)  
    INGRlaureth-7 (UNII: Z95S6G8201)  
    INGRedetate disodium (UNII: 7FLD91C86K)  
    Product Characteristics
    colorWHITEC48325
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    1454 g in 1 BOTTLE, PUMP; Type 0: Not a Combination Product
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    Cosmetic07/01/2014
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    NDANDA01982410/14/2016
    Labeler - Medimetriks Pharmaceuticals, Inc. (019903816)
    Establishment
    NameAddressID/FEIBusiness Operations
    Teligent011036910MANUFACTURE(43538-550, 43538-551) , PACK(43538-550, 43538-551)