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  • CLASSES

    Topical Dermatological Antifungals
    Topical Scalp Antifungals

    DEA CLASS

    Rx

    DESCRIPTION

    Antifungal agent; 1% cream or lotion used topically for tinea infections; 8% nail solution used for onychomycosis; 1% shampoo for seborrheic dermatitis of the scalp.

    COMMON BRAND NAMES

    Ciclodan, Ciclodan Nail Solution, Loprox, Loprox TS, Penlac

    HOW SUPPLIED

    Ciclodan/Ciclopirox/Ciclopirox Olamine/Loprox Topical Cream: 0.77%
    Ciclodan/Ciclopirox/Ciclopirox Olamine/Penlac Topical Sol: 8%
    Ciclopirox/Ciclopirox Olamine/Loprox/Loprox TS Topical Susp: 0.77%
    Ciclopirox/Loprox Topical Gel: 0.77%
    Ciclopirox/Loprox Topical Shampoo: 1%

    DOSAGE & INDICATIONS

    For the treatment of mild to moderate onychomycosis of fingernails and toenails without lunula involvement.
    Topical dosage (nail lacquer)
    Adults

    Apply once daily (preferably at bedtime or 8 hours before washing nails) to affected nails for up to 48 weeks.

    Children and Adoelscents 12 to 17 years

    Apply once daily (preferably at bedtime or 8 hours before washing nails) to affected nails for up to 48 weeks.

    For the topical treatment of seborrheic dermatitis of the scalp.
    Topical dosage (1% shampoo)
    Adults and Adolescents >= 16 years

    Wet hair and apply roughly 1 teaspoon (5 ml) to the scalp. Up to 10 ml may be used for long hair. Lather and leave on hair and scalp for 3 minutes. Rinse off. Repeat treatment twice per week for a total of 4 weeks, with a minimum of 3 days between applications. If there is no improvement after 4 weeks of treatment, the diagnosis should be reviewed.

    Topical dosage (0.77% gel)
    Adults and Adolescents >= 16 years

    Apply to affected scalp areas twice daily for 4 weeks.

    For the treatment of tinea corporis, tinea cruris, tinea pedis, tinea versicolor, and cutaneous candidiasis.
    For the treatment of tinea corporis and tinea pedis.
    Topical dosage (gel)
    Adults

    Apply to affected area(s) twice daily for 4 weeks.

    Adolescents 16 to 17 years

    Apply to affected area(s) twice daily for 4 weeks.

    Topical dosage (cream and suspension)
    Adults

    Apply to affected area(s) twice daily for 4 weeks.

    Children and Adolescents 10 to 17 years

    Apply to affected area(s) twice daily for 4 weeks.

    For the treatment of tinea cruris and cutaneous candidiasis.
    Topical dosage (cream and suspension)
    Adults

    Apply to affected area(s) twice daily for 4 weeks.

    Children and Adolescents 10 to 17 years

    Apply to affected area(s) twice daily for 4 weeks.

    For the treatment of tinea versicolor.
    Topical dosage (cream and suspension)
    Adults

    Apply to affected area(s) twice daily for 2 weeks.

    Children and Adolescents 10 to 17 years

    Apply to affected area(s) twice daily for 2 weeks.

    MAXIMUM DOSAGE

    Adults

    Maximum dosage is product specific; consult specific product labeling.

    Elderly

    Maximum dosage is product specific; consult specific product labeling.

    Adolescents

    Maximum dosage is product specific. Safety and efficacy are product specific; consult specific product labeling.

    Children

    >= 10 years: Maximum dosage is product specific. Safety and efficacy are product specific; consult specific product labeling.
    < 10 years: Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    No dosage adjustment is needed.

    Renal Impairment

    No dosage adjustment is needed.

    ADMINISTRATION

    Topical Administration

    For topical use only as directed. Not for ophthalmic, oral, or intravaginal use.
    Applied to the skin as a lotion or cream.
    Applied to the scalp as a shampoo.
    Applied to the nails as a nail lacquer.

    Cream/Ointment/Lotion Formulations

    Cream, Gel, or Suspension
    Wash hands before and after application, except when treating the infections of the hand(s).
    Apply sparingly in a thin film and rub gently into affected area(s) of clean, dry skin. Restrict application to the affected areas and try to avoid normal surrounding skin.
    Avoid use with occlusive wrappings or dressings.
    Patients who fail to respond to topical treatment after 4 weeks should be re-evaluated.

    Other Topical Formulations

    Nail Lacquer
    For topical use on fingernails and toenails and immediately adjacent skin only.
    Ciclopirox should be used in conjunction with a comprehensive management program for onychomycosis which includes removal of the unattached, infected nails (as frequently as monthly) by a health care professional and weekly trimming of the nails by the patient.
    Apply evenly over the entire nail plate and 5 mm of surrounding skin.
    If possible, apply to the nail bed, hyponychium, and the under surface of the nail plate when it is free of the nail bed (e.g., onycholysis).
    Apply daily over the previous coat. Remove the nail lacquer coat every 7 days with alcohol.
    Patients should file away (with an emery board) loose nail material and trim nails, as required, every 7 days after ciclopirox is removed with alcohol.
    Repeat this cycle throughout the duration of therapy.
    To prevent the screw cap from sticking to the nail solution bottle, do not allow the solution to get into the bottle threads.
    Close the nail solution bottle tightly after every use.
    Storage: To protect from light, replace bottle into carton after each use.
     
    Shampoo
    Wet hair.
    Apply to scalp as directed in dosage. Lather and leave on for 3 minutes; rinse.

    STORAGE

    Ciclodan:
    - Store at controlled room temperature (between 68 and 77 degrees F)
    Ciclodan Nail Solution:
    - Flammable, keep away from heat and flame
    - Protect from light
    - Store at room temperature (between 59 to 86 degrees F)
    - Store in outer carton when not in use
    Loprox:
    - Store between 41 to 77 degrees F
    Loprox TS:
    - Store between 41 to 77 degrees F
    Penlac:
    - Keep away from heat and flame
    - Protect from light
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
    - Store in carton

    CONTRAINDICATIONS / PRECAUTIONS

    Skin abrasion

    Ciclopirox products are contraindicated in individuals who have shown hypersensitivity to any of its components. If a reaction suggesting sensitivity or chemical irritation occurs during therapy, discontinue the use of ciclopirox treatment and institute appropriate therapy. Caution should be used in applying ciclopirox to patients with a skin abrasion; application to these areas could worsen skin irritation.

    Ocular exposure

    Avoid ocular exposure when applying ciclopirox. Ciclopirox is not for ophthalmic, oral, or intravaginal use. Loprox shampoo, cream or lotion is for topical dermal application only. Penlac is for use on nails and immediately adjacent skin only.

    Onychomycosis

    As with many other topical antifungal drugs, ciclopirox creams and lotions are not effective for onychomycosis. This condition usually requires treatment with ciclopirox nail lacquer (Penlac) or an oral (systemic) antifungal drug.

    Corticosteroid therapy, human immunodeficiency virus (HIV) infection, immunosuppression, organ transplant, seizure disorder

    Due to the lack of safety and efficacy data, ciclopirox is not recommended in patients with a history of a seizure disorder or immunosuppression, including patients receiving corticosteroid therapy (e.g., oral, topical or inhaled corticosteroids). The clinical trials of ciclopirox excluded patients who had a history of immunosuppression (e.g., extensive, persistent, or unusual distribution of dermatomycoses, extensive seborrheic dermatitis, recent or recurring herpes zoster, or persistent herpes simplex, human immunodeficiency virus (HIV) infection, or received an organ transplant). Patients who required medication to control epilepsy, or patients with severe plantar (moccasin) tinea pedis were also excluded.

    Diabetes mellitus, peripheral vascular disease

    There is no safety and efficacy data with ciclopirox nail solution in patients with insulin dependent diabetes mellitus, diabetic neuropathy, or peripheral vascular disease. The risk of removal of the unattached, infected nail, by the health care professional and trimming by the patient, should be carefully considered before prescribing ciclopirox (e.g., Penlac) nail solution to patients with a history of insulin dependent diabetes mellitus.

    Geriatric

    Clinical studies of ciclopirox did not include sufficient numbers of geriatric subjects to determine whether they respond differently from younger subjects.

    Pregnancy

    Ciclopirox is classified as an FDA pregnancy category B drug. There are no adequate or well-controlled studies in pregnant women. Animal studies involving mice, rats, rabbits, and monkeys revealed no embryotoxicity or teratogenicity effects following oral administration of doses ranging from 13—54 times the maximum recommended human dose. Ciclopirox should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

    Breast-feeding

    Data are limited regarding use of ciclopirox during breast-feeding and its' excretion into breast milk is unknown. Topical application is not expected to result in significant maternal absorption, and thus should not be of great risk to a breast-feeding infant. However, it is rapidly absorbed following oral administration; therefore, nursing mothers should be instructed to avoid application topically to the breast while breast-feeding. Terbinafine, clotrimazole, and miconazole may be potential alternatives to consider during breast-feeding. However, site of infection, local susceptibility patterns, and specific microbial susceptibility should be assessed before choosing an alternative agent. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested or administered drug, health care providers are encouraged to report the adverse effect to the FDA.

    Children, infants, neonates

    The safe and effective use of ciclopirox has not been established in neonates, infants, nor children < 10 years of age. However, the 0.77% topical cream and suspension are approved and may be administered to children starting at 10 years of age. Pediatric patients 12 years of age and older may receive treatment with the 8% nail solution, and adolescents greater or equal to 16 years of age may also receive the 0.77% gel or 1% shampoo years.

    ADVERSE REACTIONS

    Severe

    ventricular tachycardia / Early / Incidence not known

    Moderate

    erythema / Early / 1.0-46.0
    contact dermatitis / Delayed / 0-5.0

    Mild

    pruritus / Rapid / 0-5.0
    nail discoloration / Delayed / 1.0-2.0
    alopecia / Delayed / 0-1.0
    hair discoloration / Delayed / 0-1.0
    rash / Early / 0-1.0
    xerosis / Delayed / 0-1.0
    acneiform rash / Delayed / 0-1.0
    headache / Early / Incidence not known

    DRUG INTERACTIONS

    There are no drug interactions associated with Ciclopirox products.

    PREGNANCY AND LACTATION

    Pregnancy

    Ciclopirox is classified as an FDA pregnancy category B drug. There are no adequate or well-controlled studies in pregnant women. Animal studies involving mice, rats, rabbits, and monkeys revealed no embryotoxicity or teratogenicity effects following oral administration of doses ranging from 13—54 times the maximum recommended human dose. Ciclopirox should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

    Data are limited regarding use of ciclopirox during breast-feeding and its' excretion into breast milk is unknown. Topical application is not expected to result in significant maternal absorption, and thus should not be of great risk to a breast-feeding infant. However, it is rapidly absorbed following oral administration; therefore, nursing mothers should be instructed to avoid application topically to the breast while breast-feeding. Terbinafine, clotrimazole, and miconazole may be potential alternatives to consider during breast-feeding. However, site of infection, local susceptibility patterns, and specific microbial susceptibility should be assessed before choosing an alternative agent. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested or administered drug, health care providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    Ciclopirox is a substituted pyridone antimycotic with activity against a broad spectrum of dermatophytes, yeasts, actinomycetes, molds, other fungi and some gram-positive and gram-negative bacteria. Although the exact cellular mechanisms are unknown, ciclopirox is thought to exert its antifungal and antibacterial activity by blocking fungal transmembrane transport, causing intracellular depletion of essential substrates (e.g., amino acids) and/or ions (e.g., potassium). Ciclopirox interferes with the synthesis of RNA and DNA. At high ciclopirox concentrations, the fungal cell membrane permeability is altered, allowing leakage of intracellular material. Ciclopirox does not inhibit synthesis nor cause lysis of the fungal cell wall. One in vitro study suggested that ciclopirox acts by chelation of polyvalent cations (Fe+3 or Al+3) resulting in inhibition of the metal-dependent enzymes that are responsible for the degradation of peroxides within the fungal cell; the clinical significance of this observation is not known.
     
    Ciclopirox has fungicidal activity against in vitro isolates of Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis, and Candida albicans. Ciclopirox also inhibits the growth of pathogenic dermatophytes, yeasts, and Malassezia furfur. Although not used for its antibacterial properties, ciclopirox has some activity against Trichomonas vaginalis and Mycoplasma.
     
    In vitro susceptibility testing methods for determining ciclopirox MIC values against the dermatophytic molds, including Trichophyton rubrum species, have not been standardized or validated. Breakpoints to determine whether clinical isolates of Trichophyton rubrum are susceptible or resistant to ciclopirox have not been established. Due to variation in laboratory techniquies, Trichophyton rubrum and Trichophyton mentagrophytes species are associated with a broad range of ciclopirox MIC values (range 1-20 ug/mL).
     
    Studies have not been conducted to evaluate drug resistance development in Trichophyton rubrum species exposed to ciclopirox. Studies assessing cross-resistance to ciclopirox and other known antifungal agents have not been performed.
     
    The relevance of the antifungal properties of ciclopirox for the indication of seborrheic dermatitis is not known.

    PHARMACOKINETICS

    Ciclopirox olamine is administered topically and is distributed to the stratum corneum, epidermis, hair follicles, sebaceous glands, and dermis. Topical ciclopirox also penetrates into fingernails and toenails.

    Oral Route

    Studies investigating ciclopirox disposition after oral administration demonstrate that ciclopirox is primarily renally excreted as glucuronides (about 94%) or as unchanged drug. Fecal excretion is negligible.

    Topical Route

    Ciclopirox, when applied as a topical 1% solution is approximately 1.3% systemically absorbed when applied to 750 cm2 of back skin which is occluded for 6 hours. The drug half-live is 1.7 hours. Two days after application, only 0.01% of the dose is recovered in the urine. Penetration studies for Loprox 1% lotion in human cadaverous skin resulted in 0.8 to 1.6% of the dose in the stratum corneum 1.5 to 6 hours after application. Penetration studies demonstrate that the 1% cream has equivalent systemic absorption to the 1% lotion.
     
    Systemic absorption of ciclopirox nail solution was determined in five patients with dermatophytic onychomycosis, after once daily application to all 20 digits and adjacent 5 mm of skin for six months. In this study, ciclopirox serum levels ranged from 12-80 ng/mL. Based on urinary data, the mean absorption of ciclopirox was <5% of the applied dose. One month after discontinuing treatment, the serum and urine ciclopirox concentrations were below the detection limit. The in vitro penetration of the ciclopirox nail solution was evaluated by application of radiolabeled ciclopirox to onychomycotic toenails that were avulsed; the drug penetrated to a nail depth of approximately 0.4 mm. As expected, nail plate concentrations decreased with nail depth. The clinical significance of these findings is unknown.