OXICONAZOLE NITRATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OXICONAZOLE NITRATE (OXICONAZOLE NITRATE).
Oxiconazole nitrate is an azole antifungal agent that inhibits the synthesis of ergosterol, a key component of fungal cell membranes, by inhibiting the enzyme lanosterol 14α-demethylase. This leads to increased membrane permeability and cell death.
| Metabolism | Following topical application, systemic absorption is minimal. Any absorbed drug is likely metabolized via hepatic cytochrome P450 enzymes, though specific pathways are not well characterized. |
| Excretion | Primarily biliary/fecal: >75% of dose excreted unchanged and as metabolites in feces via bile; renal excretion accounts for <10% (mostly inactive metabolites). |
| Half-life | Terminal elimination half-life is approximately 20-30 hours, allowing once-daily or twice-daily topical application. |
| Protein binding | Highly protein-bound (>95%), primarily to albumin. |
| Volume of Distribution | Following topical application, systemic absorption is minimal (<1%), so Vd is not clinically applicable. For systemic (IV) data in animals, Vd is approximately 2-3 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Topical: Systemic bioavailability is <1% due to minimal percutaneous absorption. Not available in oral or parenteral formulations for systemic use. |
| Onset of Action | Topical: Onset of antifungal effect within 24-48 hours after first application; clinical improvement often seen within 1 week. |
| Duration of Action | Duration of antifungal activity persists for at least 24 hours after a single topical application, supporting once-daily dosing. Treatment typically continues for 2-4 weeks depending on infection. |
Apply a thin layer to affected skin once daily for 2 weeks for tinea pedis, tinea cruris, and tinea corporis.
| Dosage form | CREAM |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Approved for children ≥2 years: apply to affected area once daily for 2 weeks. |
| Geriatric use | No specific dose adjustment; use caution due to potential skin thinning or reduced barrier function in elderly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OXICONAZOLE NITRATE (OXICONAZOLE NITRATE).
| Breastfeeding | Unknown if oxiconazole nitrate is excreted in human breast milk. Due to minimal systemic absorption after topical application, it is considered likely safe during breastfeeding. M/P ratio not available. Use caution if applied to breast area to avoid infant ingestion. |
| Teratogenic Risk | Oxiconazole nitrate is a topical antifungal. Systemic absorption is minimal (<1% in animal studies), thus no known fetal risk from topical use. However, oral administration in animal studies at high doses has shown embryotoxicity and fetotoxicity, but no teratogenicity. First trimester: no known risk with topical use. Second and third trimesters: no known risk with topical use. Overall, topical use during pregnancy is considered low risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to oxiconazole or any component of the formulation.","Use in eyes, mouth, or vagina."]
| Precautions | ["For external use only; avoid contact with eyes and mucous membranes.","Discontinue use if irritation or hypersensitivity occurs.","Not recommended in pregnant women unless potential benefit outweighs risk; use with caution during lactation."] |
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| Fetal Monitoring | No specific maternal or fetal monitoring required for topical use. Monitor for local adverse effects. Systemic absorption is negligible, so no routine monitoring for systemic effects is needed. |
| Fertility Effects | No studies on human fertility. In animal studies, no impairment of fertility observed at topical doses. Systemic absorption is minimal, so effects on human fertility are unlikely. |