Ciclopirox Olamine Uses – Indications, Contraindications

Ciclopirox Olamine Uses/ciclopirox Olamine is the olamine salt form of ciclopirox, a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. Ciclopirox exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).

Mechanism of Action of Ciclopirox Olamine

Unlike antifungals such as itraconazole and terbinafine, which affect sterol synthesis, ciclopirox is thought to act through the chelation of polyvalent metal cations, such as Fe³⁺ and Al³⁺. These cations inhibit many enzymes, including cytochromes, thus disrupting cellular activities such as mitochondrial electron transport processes and energy production. Ciclopirox also appears to modify the plasma membrane of fungi, resulting in the disorganization of internal structures. The anti-inflammatory action of ciclopirox is most likely due to inhibition of 5-lipoxygenase and cyclooxygenase. ciclopirox may exert its effect by disrupting DNA repair, cell division signals, and structures (mitotic spindles) as well as some elements of intracellular transport.

Ciclopirox is a broad-spectrum antifungal medication that also has antibacterial and anti-inflammatory properties. Its main mode of action is thought to be its high affinity for trivalent cations, which inhibit essential co-factors in enzymes. Ciclopirox exhibits either fungistatic or fungicidal activity in vitro against a broad spectrum of fungal organisms, such as dermatophytes, yeasts, dimorphic fungi, eumycetes, and actinomycetes. In addition to its broad spectrum of action, ciclopirox also exerts antibacterial activity against many Gram-positive and Gram-negative bacteria. Furthermore, the anti-inflammatory effects of ciclopirox have been demonstrated in human polymorphonuclear cells, where ciclopirox has inhibited the synthesis of prostaglandin and leukotriene. Ciclopirox can also exhibit its anti-inflammatory effects by inhibiting the formation of 5-lipoxygenase and cyclooxygenase.

Ciclopirox Olamine Uses

• A cyclohexane and pyridine derivative that is used for the treatment of fungal infections of the skin and nails, and for treatment of VAGINAL YEAST INFECTIONS.
• Treatment of congenital erythropoietic porphyria
• Used as a topical treatment in immunocompetent patients with mild to moderate onychomycosis of fingernails and toenails without lunula involvement, due to Trichophyton rubrum.
• Candidiasis, Cutaneous
• Pityriasis Versicolor
• Seborrheic dermatitis of the scalp
• Tinea Corporis
• Tinea Cruris
• Tinea Pedis
• Mild Onychomycosis
• Moderate Onychomycosis
• Ciclopirox is indicated for the treatment of tinea pedis and tinea corporis due to Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum, as well as seborrheic dermatitis. It is not to be used in the eyes or vagina, and nursing women should consult their doctors before use since it is not known whether ciclopirox passes into human milk. A burning sensation may be felt when first applying ciclopirox on the skin.
• In addition to other formulations, ciclopirox is used in lacquers for topical treatment of onychomycosis (fungal infections of the nails). A meta-analysis of the six trials of nail infections available in 2009 concluded that they provided evidence that topical ciclopirox had poor cure rates and that amorolfine might be substantially more effective, but more research was required.

Contraindications of Ciclopirox Olamine Cream

• Data or Information not available

Dosage of Ciclopirox Olamine

Strengths: 0.77%; 8%; 1%; 0.77% with cleanser

Onychomycosis – Fingernail

• 8% topical solution – Apply once a day (preferably at bedtime or 8 hours before washing) to all affected nails with the applicator brush provided. Apply evenly over the entire nail plate and 5 mm of surrounding skin. If possible, the solution should be applied to the nail bed, hyponychium, and the undersurface of the nail plate when it is free of the nail bed.
• The product should not be removed on a daily basis. Daily applications should be made over the previous coat and removed with alcohol every 7 days. This cycle should be repeated throughout the duration of treatment.

Seborrheic Dermatitis

• 0.77% topical gel – Apply to affected scalp areas twice a day (in the morning and evening) for 4 weeks.
• 1% topical shampoo – Wet hair and apply approximately 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, then rinse off. Treatment should be repeated twice a week for 4 weeks, with at least 3 days between applications.

Cutaneous Candidiasis

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.

Tinea Cruris

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.

Tinea Versicolor

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.

Tinea Corporis

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.
• 0.77% topical gel – Gently massage the gel into affected areas and surrounding skin twice a day (in the morning and evening) immediately after cleaning or washing areas to be treated. Interdigital tinea pedis and tinea corporis should be treated for 4 weeks.

Tinea Pedis

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.
• 0.77% topical gel – Gently massage the gel into affected areas and surrounding skin twice a day (in the morning and evening) immediately after cleaning or washing areas to be treated. Interdigital tinea pedis and tinea corporis should be treated for 4 weeks.

Pediatric Dosage

Onychomycosis – Fingernail

12 years or older

• 8% topical solution – Apply once a day (preferably at bedtime or 8 hours before washing) to all affected nails with the applicator brush provided.
• Apply evenly over the entire nail plate and 5 mm of surrounding skin.
• If possible, the solution should be applied to the nail bed, hyponychium, and the undersurface of the nail plate when it is free of the nail bed.

Onychomycosis – Toenail

12 years or older

• 8% topical solution – Apply once a day (preferably at bedtime or 8 hours before washing) to all affected nails with the applicator brush provided.
• Apply evenly over the entire nail plate and 5 mm of surrounding skin. If possible, the solution should be applied to the nail bed, hyponychium, and the undersurface of the nail plate when it is free of the nail bed.
• The product should not be removed on a daily basis. Daily applications should be made over the previous coat and removed with alcohol every 7 days. This cycle should be repeated throughout the duration of treatment.

Seborrheic Dermatitis

16 years or older

• 0.77% topical gel – Apply to affected scalp areas twice a day (in the morning and evening) for 4 weeks.
• 1% topical shampoo – Wet hair and apply approximately 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, then rinse off. Treatment should be repeated twice a week for 4 weeks, with at least 3 days between applications.

Cutaneous Candidiasis

10 years or older

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.
• Patients with tinea versicolor usually exhibit clinical and mycological clearing after 2 weeks of treatment.

Tinea Cruris

10 years or older

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.
• Patients with tinea versicolor usually exhibit clinical and mycological clearing after 2 weeks of treatment.

Tinea Versicolor

10 years or older

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.
• Patients with tinea versicolor usually exhibit clinical and mycological clearing after 2 weeks of treatment.

Tinea Corporis

10 years or older

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.

16 years or older

• 0.77% topical gel – Gently massage the gel into affected areas and surrounding skin twice a day (in the morning and evening) immediately after cleaning or washing areas to be treated. Interdigital tinea pedis and tinea corporis should be treated for 4 weeks.

Tinea Pedis

10 years or older

• 0.77% topical cream, suspension (lotion) – Gently massage into affected and surrounding skin areas twice a day (in the morning and evening). Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment.

16 years or older

• 0.77% topical gel – Gently massage the gel into affected areas and surrounding skin twice a day (in the morning and evening) immediately after cleaning or washing areas to be treated. Interdigital tinea pedis and tinea corporis should be treated for 4 weeks.

Side Effects of Ciclopirox Olamine Cream

More common

• Burning, itching, redness, swelling, or other signs of irritation not present before use of this medicine
• Burning, dryness, irritation, itching, or redness of skin (usually mild and temporary)
• Eye pain (if certain products have been used near the eye)
• Headache
• Increased redness or scaling of skin sores (usually mild and temporary)
• Skin color changes
• Skin infection
• Skin rash (usually mild and temporary)
• Softening and tearing of the skin
• Thinning of the skin with easy bruising

Less common

• Burning sensation of the skin
• Dry skin
• flushing or redness of the skin
• itching, scaling, severe redness, soreness, or swelling of the skin
• skin irritation
• skin rash, encrusted, scaly and oozing
• thinning of the skin with easy bruising, especially when used on the face or where the skin folds together (eg, between the fingers)
• Dandruff
• headache
• itching skin or scalp
• oily skin
• rash
• skin disorder

Rare

• Thinning, weakness, or wasting away of the skin
• Acne or pimples
• burning and itching of the skin with pinhead-sized red blisters
• increased hair growth on the forehead, back, arms, and legs
• lightening of normal skin color
• lightening of treated areas of dark skin
• reddish purple lines on the arms, face, legs, trunk, or groin
• softening of the skin

Drug Interactions of Ciclopirox Olamine

may interact with following drugs, supplements & may change the efficacy of drugs

• Acenocoumarol
• Clorindione
• Coumarin
• Dicoumarol
• Diphenadione
• Ethyl biscoumacetate
• Fluindione
• hydroxycoumarin
• Phenindione
• Phenprocoumon
• Tioclomaro
• Warfarin

Pregnancy Category of Ciclopirox Olamine Cream

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if ciclopirox passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of this medication have not been established for children. The cream and lotion may be used for children 10 years and older.

How should I use this medication?

• Nail lacquer – Ciclopirox lacquer is usually applied to the affected nails once daily at bedtime or at least 8 hours before washing the affected area. Before using this medication for the first time and once a week while using this medication, remove any loose nail or nail pieces using nail clippers or nail files. Then, using the applicator brush provided, apply lacquer evenly over the entire nail, the skin right around the nail, and on the bottom side of the nail and the skin beneath it. Let the lacquer dry (about 30 seconds) before putting socks or stockings on. Apply daily over the previous coat. Once a week, remove the lacquer with rubbing alcohol. You should file away (with an emery board) loose nail material and trim nails, as required, or as directed by your doctor. Avoid contact with the eyes and mucous membranes (e.g., mouth) and avoid contact with skin other than the skin surrounding the nail(s) being treated. Do not use nail polish on treated nails. Ciclopirox lacquer should be stored at room temperature. Protect this medication from light by storing the bottle in its carton after each use. Keep away from heat and flame.
• Cream or lotion – Gently massage the medication into the affected and surrounding skin areas twice daily, in the morning and evening, for a minimum of 4 weeks. If within 2 weeks there is no improvement in symptoms such as itching, call your doctor. Do not use this medication in the eyes or in the vagina. Store the cream or lotion at room temperature and keep it out of the reach of children.
• Shampoo – Ciclopirox shampoo is generally used 2 or 3 times a week, or as often as recommended by your doctor. Wet hair and apply enough shampoo to work up an abundant lather. Massage the scalp with your fingertips for 2 to 3 minutes, then rinse the hair well. Repeat lathering and rinsing. Keep ciclopirox shampoo out of the eyes and away from the eyelids. If you get this medication in your eyes, flush well with clean water. Ciclopirox shampoo may cause discoloration of grey, white, or chemically damaged hair. Store the shampoo at room temperature and keep it out of reach of children.

References