Oxizole (Oxiconazole)

OXIZOLE®

Stiefel

Oxiconazole Nitrate

Topical Antifungal

Action And Clinical Pharmacology: Oxiconazole nitrate is a broad-spectrum imidazole derivative whose antifungal activity is derived primarily from the inhibition of ergosterol biosynthesis, which is critical for cellular membrane integrity. It has fungicidal or fungistatic activity in vitro against a number of pathogenic fungi including the following dermatophytes, and yeasts: T. rubrum, T. mentagrophytes, T. tonsurans, T. violaceum, E. floccosum, M. canis, M. audouini, M. gypseum, C. albicans, and M. furfur.

Five hours after application of 2.5 mg/cmof oxiconazole nitrate cream onto human skin, the concentration of oxiconazole nitrate was demonstrated to be 16.2 mol in the epidermis, 3.64 mol in the upper corium, and 1.29 mol in the deeper corium. Systemic absorption of oxiconazole nitrate appears to be low. Less than 0.3% of the applied dose was recovered in the urine of volunteer subjects up to 5 days after application. Feces were not analyzed for the drug, and it is not known whether the absorption is higher than that estimated by recovery of drug in urine.

Indications And Clinical Uses: For the topical treatment of athlete’s foot (tinea pedis) due to T. rubrum, T. mentagrophytes or E. floccosum.

Contra-Indications: In individuals who have shown hypersensitivity to oxiconazole or any of its components.

Manufacturers’ Warnings In Clinical States: For external use only, not for ophthalmic or intravaginal use.

Precautions: General: If skin sensitization occurs, discontinue topical administration and institute appropriate therapy as required.

Pregnancy: Reproduction studies have been performed in rabbits, rats and mice at oral doses up to 100, 150 and 200 mg/kg/day, respectively, and revealed no evidence of harm to the fetus due to oxiconazole nitrate. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, oxiconazole preparations should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: Since oxiconazole is excreted in human milk, caution should be exercised when the drug is administered to a nursing woman. Although human data relating concentrations of oxiconazole in milk were not obtained, after s.c. administration of 5 mg/kg to female rats, the milk: plasma ratio at 1.5 to 12 hours was in the range of 3.0 to 8.0.

Adverse Reactions: During clinical trials, 37 (4.2%) of 879 patients treated with oxiconazole cream reported drug-related adverse reactions, including pruritus (1.6%), burning (1.4%), irritation (0.5%), erythema, stinging and allergic contact dermatitis (0.2% each) and folliculitis, fissuring, maceration rash and nodules (0.1% each).

In a controlled, multicenter clinical trial, 7 (2.6%) of 269 patients treated with oxiconazole lotion reported drug-related adverse reactions, including burning and stinging (0.7% each), pruritus, scaling, tingling, pain, and dyshidrotic eczema (0.4% each).

Symptoms And Treatment Of Overdose: Acute overdosage of oxiconazole in humans has not been reported to date.Symptoms: Animal studies have shown oxiconazole to be a CNS depressant and tissue irritant when administered orally or by injection.

Treatment: In cases of accidental ingestion, gastric lavage should be considered, otherwise, the treatment should be symptomatic.

Dosage And Administration: In patients with tinea pedis, oxiconazole cream and lotion should be applied to cover affected and surrounding areas twice daily (in the morning and evening). Medication should be gently massaged into the skin. Tinea pedis should be treated for 1 month to reduce the possibility of recurrence. If a patient shows no clinical improvement after the treatment period, the diagnosis should be reviewed.

Availability And Storage: Cream: Each g of white to off-white, opaque cream base contains: oxiconazole 10 mg as oxiconazole nitrate. Nonmedicinal ingredients: benzoic acid, cetyl alcohol, polysorbate 60, propylene glycol, purified water, stearyl alcohol and white petrolatum. Tubes of 30 g. Store between 15 and 30°C.

Lotion: Each g of white to off-white, opaque lotion base contains: oxiconazole 10 mg as oxiconazole nitrate. Nonmedicinal ingredients: benzoic acid, cetyl alcohol, polysorbate 60, propylene glycol, purified water, stearyl alcohol and white petrolatum. Bottles of 30 mL. Store between 15 and 30°C. Protect from light.

OXIZOLE® Stiefel Oxiconazole Nitrate Topical Antifungal

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