Ciclopirox Olamine

Approved Indications:

• Dermatomycoses (Tinea infections):
• Tinea pedis (athlete’s foot)
• Tinea cruris (jock itch)
• Tinea corporis (ringworm)
• Candidiasis:
• Cutaneous candidiasis caused by Candida albicans
• Seborrheic Dermatitis:
• Mild to moderate cases on the scalp and face
• Tinea versicolor (Pityriasis versicolor)
• Onychomycosis (fungal nail infections):
• Mild to moderate cases involving distal nail without matrix involvement (when used as a nail lacquer)

Off-Label / Clinically Accepted Uses:

• Intertrigo with secondary fungal infection
• Fungal superinfections in eczematous skin
• Pediatric superficial fungal infections (topical use only)

Formulations:

• Topical cream, lotion, or gel: 1% Ciclopirox olamine
• Shampoo (Scalp formulation): 1%
• Nail lacquer: 8%

Adults and Adolescents (≥16 years):

• Tinea infections (skin):
  Apply a thin layer once or twice daily for 2–4 weeks
  Continue for several days after symptoms resolve
• Seborrheic Dermatitis (Scalp):
  Shampoo: Apply to wet scalp twice weekly for 4 weeks, leaving on scalp for 3–5 minutes before rinsing
• Onychomycosis (Nail lacquer):
  Apply once daily at bedtime to affected nails and surrounding skin
  Remove with alcohol every 7 days and trim nails weekly
  Treatment duration: Up to 48 weeks

Pediatrics (≥10 years):

• Use is safe topically in children; dosage same as adults

Elderly:

• No dosage adjustment required; monitor for dryness or irritation

Renal/Hepatic Impairment:

• No adjustment needed (topical route)

Ciclopirox olamine is a broad-spectrum antifungal agent that chelates polyvalent cations (e.g., Fe³⁺, Al³⁺), inhibiting metal-dependent enzymes vital to the fungal cell membrane structure and function. This disrupts essential cellular processes such as DNA repair, mitochondrial activity, and cellular respiration. Unlike azoles, it does not inhibit ergosterol synthesis, reducing the risk of cross-resistance. It also demonstrates anti-inflammatory and antibacterial properties, enhancing its effectiveness in mixed infections and inflammatory fungal dermatoses.

• Absorption: Minimal systemic absorption with topical application
• Nail lacquer: <5% systemic absorption
• Cream/lotion: ~1.3–1.5% in intact skin
• Distribution: Confined to the epidermis, dermis, and nail plate
• Metabolism: Extensively metabolized via liver after systemic absorption (minor); not a substrate of CYP450 enzymes
• Elimination: Excreted primarily via urine as glucuronide conjugates
• Half-life: Not systemically relevant due to low absorption
• Onset of Action: Symptomatic relief typically within 1–2 weeks

• Pregnancy:
• FDA Pregnancy Category B (for topical forms)
• Animal studies show no fetal harm; no adequate human studies
• Safe for use in pregnancy if clearly needed; avoid nail lacquer unless essential
• Lactation:
• Minimal systemic absorption suggests low risk
• No known excretion in breast milk; can be used with caution
• Avoid application to breast area in nursing mothers

• Primary Class: Topical Antifungal
• Subclass: Hydroxypyridone derivative

• Known hypersensitivity to ciclopirox or any component of the formulation
• Application to open wounds or mucous membranes
• Use in ocular infections or intra-vaginally (form not designed for these uses)
• Use of nail lacquer in patients with diabetic neuropathy or peripheral vascular disease involving nails (relative contraindication)

• Avoid Contact with Eyes: May cause irritation; rinse immediately if exposure occurs
• Discontinue if Hypersensitivity or Irritation Occurs: Rash, burning, or allergic contact dermatitis
• Do Not Occlude Treated Area: Occlusion may increase systemic absorption
• Nail Lacquer Use: Avoid cosmetic nail polish or artificial nails during treatment
• Monitor Treatment Response: Lack of improvement within 4 weeks may require alternative therapy or diagnostic reassessment
• Not for Systemic or Intravaginal Use

Topical Skin Formulations:

Common (1–10%):

• Burning, itching, or stinging at application site
• Redness or irritation
• Dry skin or scaling

Less Common (<1%):

• Contact dermatitis
• Hypopigmentation or hyperpigmentation
• Urticaria

Nail Lacquer:

• Discoloration of nail
• Brittle nails or onycholysis
• Mild erythema or burning near cuticle

Serious/Rare:

• Allergic contact dermatitis
• Severe localized skin reactions

Timing: Most reactions occur within the first few days of use and are generally mild

• Minimal risk of drug-drug interactions due to negligible systemic absorption

Potential Considerations:

• Nail polish or occlusive coverings may reduce efficacy of nail lacquer
• Concurrent topical corticosteroids may mask treatment failure or infection

CYP450 Involvement: None significant

Food or Alcohol Interactions: Not applicable for topical products

• 2023 Mycoses Guidelines (Europe):
• Endorsed ciclopirox nail lacquer as a valid monotherapy for mild distal subungual onychomycosis
• 2024 Clinical Dermatology Review:
• Highlighted efficacy in seborrheic dermatitis as comparable to ketoconazole, with added anti-inflammatory effect
• FDA Advisory:
• No significant safety changes in recent years; continued recommendation for limited, superficial fungal infections only

• Topical Cream/Lotion/Gel:
• Store at 20°C to 25°C (68°F to 77°F)
• Keep container tightly closed; avoid excessive moisture
• Do not freeze
• Shampoo:
• Store at room temperature
• Use within the expiry date; protect from direct light
• Nail Lacquer:
• Store below 30°C; keep bottle tightly closed
• Avoid exposure to direct sunlight or high temperatures
• Flammable – keep away from open flame
• Discard after 6 months of opening