LOPROX® Gel (ciclopirox) 0.77% contains a synthetic antifungal agent, ciclopirox. It is intended for topical dermatologic use only.

Each gram of LOPROX® Gel contains 7.70 mg of ciclopirox in a gel consisting of Purified Water USP, Isopropyl Alcohol USP, Octyldodecanol NF, Dimethicone Copolyol 190, Carbomer 980, Sodium Hydroxide NF, and Docusate Sodium USP.

LOPROX® Gel is a white, slightly fluid gel.

The chemical name for ciclopirox is 6-cyclohexyl-1-hydroxy-4-methyl-2(1H)- pyridinone, with the empirical formula C₁₂H₁₇NO₂ and a molecular weight of 207.27. The CAS Registry Number is [29342-05-0]. The chemical structure is:

Superficial Dermatophyte Infections

LOPROX® GeI is indicated for the topical treatment of interdigital tinea pedis and tinea corporis due to Trichophyton rubrum, Trichophyton mentagrophytes, or Epidermophyton floccosum.

Seborrheic Dermatitis

LOPROX® Gel is indicated for the topical treatment of seborrheic dermatitis of the scalp.

Superficial Dermatophyte Infections

Gently massage LOPROX® Gel into the affected areas and surrounding skin twice daily, in the morning and evening immediately after cleaning or washing the areas to be treated. Interdigital tinea pedis and tinea corporis should be treated for 4 weeks. If a patient shows no clinical improvement after 4 weeks of treatment, the diagnosis should be reviewed.

Seborrheic Dermatitis of the Scalp

Apply LOPROX Gel to affected scalp areas twice daily, in the morning and evening for 4 weeks. Clinical improvement usually occurs within the first week with continuing resolution of signs and symptoms through the fourth week of treatment. If a patient shows no clinical improvement after 4 weeks of treatment, the diagnosis should be reviewed.

LOPROX® Gel (ciclopirox) 0.77% is supplied in 30 g tubes (NDC 99207-013-30), and 45 g tubes (NDC 99207-013-45).

Store at 15° - 30°C (59° - 86°F).

Prescribing Information as of September 2001. Manufactured for: MEDICIS, The Dermatology Company® Scottsdale, AZ 85258. By: Aventis Pharma Deutschland GmbH, D-65926 Frankfurt am Main. Made in Germany. FDA Rev date: 3/26/2003

In clinical trials, 140 (39%) of 359 subjects treated with LOPROX® Gel reported adverse experiences, irrespective of relationship to test materials, which resulted in 8 subjects discontinuing treatment. The most frequent experience reported was skin burning sensation upon application, which occurred in approximately 34% of seborrheic dermatitis patients and 7% of tinea pedis patients. Adverse experiences occurring between 1% to 5% were contact dermatitis and pruritus. Other reactions that occurred in less than 1% included dry skin, acne, rash, alopecia, pain upon application, eye pain, and facial edema.

No information provided.

LOPROX® Gel is not for ophthalmic, oral, or intravaginal use.

Keep out of reach of children.

If a reaction suggesting sensitivity or chemical irritation should occur with the use of LOPROX® Gel, treatment should be discontinued and appropriate therapy instituted. A transient burning sensation may occur, especially after application to sensitive areas. Avoid contact with eyes. Efficacy of LOPROX® Gel in immunosuppressed individuals has not been studied. Seborrheic dermatitis in association with acne, atopic dermatitis, Parkinsonism, psoriasis and rosacea has not been studied with LOPROX® Gel. Efficacy in the treatment of plantar and vesicular types of tinea pedis has not been established.

Carcinogenesis, Mutagenesis, Impairment of Fertility

A carcinogenicity study of ciclopirox (1% and 5% solutions in polyethylene glycol 400) 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 battery of in vitro genotoxicity tests was conducted with ciclopirox: evaluation of gene mutation in the Ames Salmonella and E. coli assays (negative); chromosome aberration assays in V79 Chinese hamster cells, with and without metabolic activation (positive); gene mutation assays 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/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 5000 mg/kg.

Pregnancy

Teratogenic effects: Pregnancy Category B

Reproduction studies of ciclopirox revealed no significant evidence of impaired fertility in rats exposed orally up to 5 mg/kg body weight (approximately 5 times the maximum recommended topical human dose based on surface area). No fetotoxicity was shown due to ciclopirox in the mouse, rat, rabbit, and monkey at oral doses up to 100, 30, 30, and 50 mg/kg body weight, respectively (approximately 37.5, 30, 44, and 77 times the maximum recommended topical human dose based on surface area). By the dermal route of administration, no fetotoxicity was shown due to ciclopirox in the rat and rabbit at doses up to 120 and 100 mg/kg body weight, respectively (approximately 121 and 147 times, respectively, the maximum recommended topical human dose based on surface area).

There are no adequate or well-controlled studies of topically applied ciclopirox in pregnant women. LOPROX® Gel should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Since many drugs are excreted in human milk, caution should be exercised when LOPROX® Gel is administered to a nursing woman.

Pediatric Use

The efficacy and safety of LOPROX® Gel in pediatric patients below the age of 16 years have not been established.

No information provided.

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

Mechanism of Action

Ciclopirox 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.

In vitro studies showed that ciclopirox inhibited the formation of 5-lipoxygenase inflammatory mediators (5-HETE and LTB₄) and also inhibited PGE₂ release in a cell culture model. In vivo, ciclopirox inhibited inflammation in an arachidonic acid-induced murine ear edema model. The clinical significance of these findings is unknown.

Pharmacokinetics

A comparative study of the pharmacokinetics of LOPROX® GeI and LOPROX® Cream (ciclopirox olamine) 0.77% in 18 healthy males indicated that systemic absorption of ciclopirox from LOPROX® Gel was higher than that of LOPROX® Cream. A 5 gm dose of LOPROX® Gel produced a mean (±SD) peak serum concentration of 25.02 (±20.6) ng/mL total ciclopirox and 5 gm of LOPROX® Cream produced 18.62 (±13.56) ng/mL total ciclopirox. Approximately 3% of the applied ciclopirox was excreted in the urine within 48 hours after application, with a renal elimination half-life of about 5.5 hours.

In a study of LOPROX® Gel, 16 men with moderate to severe tinea cruris applied approximately 15 grams/day of the gel for 14.5 days. The mean (±SD) dose-normalized values of Cmax for total ciclopirox in serum were 100 (±42) ng/mL on Day 1 and 238 (±144) ng/mL on Day 15. During the 10 hours after dosing on Day 1, approximately 10% of the administered dose was excreted in the urine.

Microbiology

Ciclopirox is a hydroxypyridinone antifungal agent that inhibits the growth of pathogenic dermatophytes. Ciclopirox has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section:

Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.

The patient should be told the following:

1. Use LOPROX® Gel as directed by the physician. Avoid contact with the eyes and mucous membranes. LOPROX® Gel is for external use only.
2. Use the medication for fungal infections for the full treatment time even though symptoms may have improved, and notify the physician if there is no improvement after 4 weeks.
3. A transient burning/stinging sensation may be felt. This may occur in approximately 15% to 20% of cases, when LOPROX® Gel is used to treat seborrheic dermatitis of the scalp.
4. Inform the physician if the area of application shows signs of increased irritation or possible sensitization (redness with itching, burning, blistering, swelling, and/or oozing).
5. Avoid the use of occlusive dressings.
6. Do not use this medication for any disorder other than that for which it is prescribed.

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

CICLOPIROX GEL - TOPICAL

(cyc-low-PIE-rocks)

COMMON BRAND NAME(S): Loprox

USES: This medication is used to treat minor fungal skin infections (e.g., athletes foot, ringworm). It is also used to treat a certain scalp condition (seborrheic dermatitis, a type of dandruff). This medication may not work well for infections on the nails, for areas of very thick skin (e.g., palms of hands or soles of feet), or for persistent or frequent infections. In those cases, you may need to take other drugs by mouth. Consult your doctor for more details.

Ciclopirox is an antifungal drug that works by stopping the growth of fungus.

HOW TO USE: Wash your hands, then clean and dry the affected area. Apply a small amount of the medication to the area and gently rub into the skin or scalp, usually twice daily or as directed by your doctor. Do not cover or bandage the area unless told to do so by your doctor. Wash your hands after applying the medication. Avoid getting the medicine in your eyes, nose or mouth. If you do, rinse with plenty of water.

Use this medication regularly in order to get the most benefit from it. To help you remember, use it at the same times each day.

It may take one to two weeks of treatment to notice an improvement. Continue to use this medication for the full amount of time prescribed, even if symptoms disappear after a few days. Stopping the medication too early may not cure the infection, allowing the fungus to return.

Inform your doctor if your condition persists or worsens after two to four weeks of treatment.

SIDE EFFECTS: Itching, burning, stinging, or redness may occur when this medication is first applied to the skin. These should disappear in a few days as your body adjusts to the medication. If any of these effects persist or worsen, notify your doctor or pharmacist promptly. Tell your doctor or pharmacist immediately if blistering, swelling, or oozing occurs.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using ciclopirox, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: persistent/frequent fungal skin infections, infections over a large area of skin, toenail/fingernail infections, immune system problems (e.g., due to organ transplant, HIV disease).

This medication should be used only when clearly needed during pregnancy. Discuss the risks and benefits with your doctor.

It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of any medicine before checking with them first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of other products applied to the skin. Do not start or stop any medicine without the approval of your doctor or pharmacist.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national poison hotline at 1-800-222-1222. Canadian residents should call their local poison control center directly. This medication may be harmful if swallowed.

NOTES: Do not share this medication with others.

This medication has been prescribed for your current condition only. Do not use it later for another infection or scalp problem unless told to do so by your doctor. A different medication may be necessary in those cases.

Keep the affected area as dry as possible. To help prevent the growth of fungus, wear cotton fabrics and avoid tight fitting clothes or shoes. Ask your doctor or pharmacist for more details.

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature between 59-86 degrees F (15-30 degrees C) away from moisture and light. Tightly replace the cap after each use. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.