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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LOPROX (LOPROX).
| Breastfeeding | It is not known whether ciclopirox is excreted in human milk following topical application. Due to low systemic absorption, it is likely compatible with breastfeeding, but caution is advised. Apply to the smallest possible area and avoid application to the breast area to minimize infant exposure. M/P ratio is not available. |
| 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. |
■ 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). |
Loading safety data…
| 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. |