LOPROX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LOPROX (LOPROX).
Ciclopirox is a hydroxypyridone antifungal agent that inhibits metal-dependent enzymes, including cytochromes, by chelating polyvalent cations (Fe3+, Al3+). It disrupts fungal cell membrane integrity and mitochondrial electron transport, leading to fungicidal activity. It also has anti-inflammatory properties by inhibiting prostaglandin and leukotriene synthesis.
| Metabolism | Ciclopirox is primarily metabolized via glucuronidation and oxidation to inactive metabolites. The main enzyme involved is not fully characterized; it is not a major substrate or inhibitor of CYP450 enzymes. |
| Excretion | Less than 1% of topically applied ciclopirox is absorbed; absorbed drug is conjugated and excreted renally as glucuronides, with minor fecal elimination. |
| Half-life | Terminal elimination half-life is approximately 1.7 hours for the absorbed fraction, reflecting rapid renal clearance. |
| Protein binding | Approximately 98% bound to serum proteins, primarily albumin. |
| Volume of Distribution | 0.3 L/kg, indicating distribution primarily within extracellular fluid; limited tissue penetration due to high protein binding. |
| Bioavailability | Topical: negligible systemic bioavailability (<1%) due to minimal percutaneous absorption. |
| Onset of Action | Topical: clinical improvement may be seen within 1 week of regular application, with full effect over 2-4 weeks. |
| Duration of Action | Duration of action corresponds to drug presence at application site; continued application for 2-4 weeks is required for mycological cure, with longer treatment for nail infections. |
| Molecular Weight | 268.35 |
Ciclopirox 1% cream or lotion: apply to affected area twice daily. Nail lacquer (8%): apply to affected nails daily. Shampoo (1%): apply 5-10 mL to wet scalp, lather, leave for 3 minutes, rinse; use twice weekly.
| Dosage form | CREAM |
| Renal impairment | No dose adjustment required for topical use; systemic absorption is minimal. |
| Liver impairment | No dose adjustment required for topical use; systemic absorption is minimal. |
| Pediatric use | Safety and efficacy in children <10 years not established; for age ≥10 years, same as adult dosing. |
| Geriatric use | No specific dose adjustment; use caution if extensive topical application to compromised skin due to potential increased absorption. |
| 1st trimester | Avoid unless clearly needed; limited human data, animal studies suggest risk. |
| 2nd trimester | Avoid unless clearly needed; limited human data. |
| 3rd trimester | Avoid unless clearly needed; limited human data. |
Clinical note
Comprehensive clinical and safety monograph for LOPROX (LOPROX).
| Placental transfer | Unknown; molecular weight suggests minimal transfer, but no data. |
| Breastfeeding | Minimal systemic absorption after topical application; unlikely to be excreted into breast milk in significant amounts. Use with caution. |
| Lactation Rating | L3 |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to ciclopirox or any component of the formulation
| Precautions | For external use only. Avoid contact with eyes. If irritation or sensitization occurs, discontinue use. In nail polish formulation, avoid use in patients with underlying nail disease or immunosuppression. Use in pregnancy only if clearly needed (Category B). |
| Food/Dietary | None known. No dietary restrictions required with topical or nail lacquer use. |
| Clinical Pearls | LOPROX (ciclopirox) is a broad-spectrum antifungal with anti-inflammatory activity. It is available as a cream, gel, and nail lacquer. For nail lacquer, apply daily over entire nail plate and 5 mm of surrounding skin; remove with alcohol every 7 days. Avoid concurrent use of occlusive dressings unless directed. Ciclopirox is effective against dermatophytes, Candida, and Malassezia. In tinea pedis, treatment duration is 2 weeks for cream; for onychomycosis, up to 48 weeks may be needed. |
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| Teratogenic Risk | Ciclopirox olamine (LOPROX) is classified as FDA Pregnancy Category B. Animal studies have not shown teratogenic effects, but there are no adequate and well-controlled studies in pregnant women. Topical application results in minimal systemic absorption; therefore, risk to the fetus is considered low. No specific fetal risks have been identified for any trimester. |
| Fetal Monitoring | No specific monitoring is required beyond routine prenatal care, as systemic exposure is negligible with topical use. Monitor for local skin reactions or hypersensitivity. |
| Fertility Effects | No studies on fertility in humans. In animal studies, no impairment of fertility was observed. |
| Patient Advice | Apply exactly as prescribed; do not use more often or longer than directed. · For nail lacquer, apply daily to affected nails and surrounding skin; remove with alcohol swab every 7 days. · Do not use on open wounds or in eyes, mouth, or vagina. · Wash hands after application unless treating hands. · Continue treatment for full duration even if symptoms improve. · Report any signs of skin irritation, blistering, or worsening rash. · Avoid covering treated area with bandages unless instructed. |