Oxiconazole

Oxiconazole is an antifungal agent belonging to the pharmacological class of Imidazoles.

Oxiconazole has been approved to relieve symptoms and also for the treatment and maintenance of Tinea Versicolor, Tinea corporis /Tinea cruris, Tinea pedis.

An in vitro study using human skin showed that after applying 2.5 mg/cm2 of oxiconazole nitrate cream, the drug penetrated the skin with concentrations of 16.2 μmol in the epidermis, 3.64 μmol in the upper corium, and 1.29 μmol in the deeper corium after five hours. The systemic absorption of oxiconazole nitrate was found to be low, with less than 0.3% of the applied dose being recovered in the urine of volunteer subjects

The common side effects involved in using Oxiconazole are Redness, Pimple-like bumps, Burning, Stinging, Swelling, Irritation, Tenderness, Flaking of the treated skin.

Oxiconazole is available in the form of Cream/Lotion.

Oxiconazole is approved in Germany, Japan, Malaysia, India, the U.K., the U.S., and China.

Oxiconazole belonging to the pharmacological class of Imidazoles, acts as an antifungal agent.

Oxiconazole works by blocking the biosynthesis of ergosterol, a vital component required for maintaining the integrity of the cytoplasmic membrane in fungi. It achieves this by destabilizing the fungal cytochrome P450 51 enzyme, also known as Lanosterol 14-alpha demethylase, which plays a crucial role in the cell membrane structure of the fungus. Inhibiting this enzyme leads to cell lysis, effectively killing the fungal cells. Additionally, oxiconazole has been observed to inhibit DNA synthesis and reduce intracellular levels of ATP (adenosine triphosphate). Similar to other imidazole antifungals, oxiconazole can enhance membrane permeability to zinc, thus increasing its cytotoxic effects on the fungus.

Oxiconazole has been approved to relieve symptoms and also for the treatment and maintenance of Tinea Versicolor, Tinea corporis /Tinea cruris, Tinea pedis.

Oxiconazole is found to be available in the form of Cream/Lotion.

Oxiconazole can be used in the following treatment:

• Tinea Versicolor
• Tinea corporis /Tinea cruris
• Tinea pedis

Oxiconazole can help to relieve symptoms and also for the treatment and maintenance of Tinea Versicolor, Tinea corporis /Tinea cruris, Tinea pedis.

Oxiconazole is approved for use in the following clinical indications:

• Tinea Versicolor
• Tinea corporis /Tinea cruris
• Tinea pedis

Cream/Lotion

Dosage Adjustments in Pediatric Patients:

Tinea corporis, tinea cruris, tinea pedis, and tinea versicolor can be treated with the same topical cream dosage as adults in children aged 12 years and above.

There are no specific dietary restrictions associated with the use of Oxiconazole. Oxiconazole can be administered with or without food, and no specific foods or beverages are known to interact with Oxiconazole. The dietary restriction should be individualized as per patient requirements.

Oxiconazole may be contraindicated under the following conditions:

• Oxiconazole should not be used in patients with a known hypersensitivity (such as anaphylaxis) or any other component present in the product.

The treating physician must closely monitor the patient and keep pharmacovigilance as follows:

• Oxiconazole Cream and Lotion should not be used in the eyes or inside the vagina.

Due to the excretion of oxiconazole in human milk, it is advisable to exercise caution when administering the drug to a nursing woman.

Pregnancy:

Pregnancy Category B

Studies on reproduction conducted in rabbits, rats, and mice have involved oral doses up to 100, 150, and 200 mg/kg/day (equivalent to 57, 40, and 27 times the human dose based on mg/m2), respectively. These studies did not show any evidence of harm to the fetus resulting from oxiconazole nitrate exposure. However, it is essential to note that there are no sufficient and well-controlled studies in pregnant women. Since animal studies may not always accurately predict human responses, the use of this drug during pregnancy should be considered only when clearly necessary.

No specific food restrictions or dietary modifications are required when using Oxiconazole. Oxiconazole can be administered with or without food.

The adverse reactions related to Oxiconazole can be categorized as follows:

Common:

• Itching
• Burning

• Burning, itching, and pain in hairy areas
• Blistering, crusting, dryness, or flaking of the skin
• Scaling
• Severe redness, soreness, or swelling of the skin
• Pus at the root of hair

There is no sufficient scientific evidence traceable regarding drug interactions related to the drug Oxiconazole.

The following are the side effects involving Oxiconazole:

The use of molecule oxiconazole should be prudent in the following group of special populations:

Pregnancy:

Pregnancy Category B

Studies on reproduction conducted in rabbits, rats, and mice have involved oral doses up to 100, 150, and 200 mg/kg/day (equivalent to 57, 40, and 27 times the human dose based on mg/m2), respectively. These studies did not show any evidence of harm to the fetus resulting from oxiconazole nitrate exposure. However, it is essential to note that there are no sufficient and well-controlled studies on pregnant women. Since animal studies may not always accurately predict human responses, the use of this drug during pregnancy should be considered only when clearly necessary.

Lactation:

Due to the excretion of oxiconazole in human milk, it is advisable to exercise caution when administering the drug to a nursing woman.

Pediatric:

Oxiconazole cream is found to be suitable for treating tinea corporis, tinea cruris, tinea pedis, and tinea (pityriasis) versicolor in the pediatric patients. However, these conditions, which Oxiconazole cream had been demonstrated to effectively treat, are found to be uncommon among children under the age of 12.

Geriatric Use:

A relatively small group of patients aged 60 years and above (approximately 396 individuals) received treatment with Oxiconazole Cream in both US and non-US clinical trials. Additionally, a limited number of geriatric patients (n = 43) were treated with Oxiconazole Lotion in US clinical trials. Due to the small sample size, it is not feasible to conduct separate analyses regarding the effectiveness and safety of the treatments in this specific age group. Nevertheless, it is noteworthy that no adverse events were reported with Oxiconazole Lotion in the geriatric patients, and the adverse reactions observed with Oxiconazole Cream in this age group were similar to those reported by younger patients. Considering the available data, there is no need for dosage adjustments of Oxiconazole Cream and Lotion in geriatric patients.

The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Oxiconazole.

In an animal study, researchers applied a 5% concentration of oxiconazole cream (which is five times stronger than the regular product) to about 10% of the body surface area of 40 male and female rats for 35 days. Tragically, three rats died, and severe inflammation of the skin was observed. It is essential to note that there have been no reported incidents of overdoses in humans using oxiconazole nitrate cream or lotion.

Pharmacodynamics:

Oxiconazole is an imidazole derivative with broad-spectrum antifungal properties. Its main mode of action involves inhibiting the biosynthesis of ergosterol, a crucial component of fungal cell membranes. This inhibition either kills the fungi (fungicidal) or prevents their growth (fungistatic) in laboratory settings.

Pharmacokinetics:

An in vitro permeation technique using human skin was used to evaluate the skin penetration of oxiconazole nitrate. After applying 2.5 mg/cm2 of oxiconazole nitrate cream to human skin, the concentrations of the drug were found to be 16.2 μmol in the epidermis, 3.64 μmol in the upper corium, and 1.29 μmol in the deeper corium five hours post-application. The systemic absorption of oxiconazole nitrate was found to be low. When using radiolabeled drug, less than 0.3% of the applied dose of oxiconazole nitrate was recovered in the urine of volunteer subjects up to 5 days after applying the cream formulation.

1. https://www.goodrx.com/oxiconazole/what-is
2. https://medlineplus.gov/druginfo/meds/a689004.html
3. https://my.clevelandclinic.org/health/drugs/18461-oxiconazole-skin-cream
4. https://go.drugbank.com/drugs/DB00239
5. https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/19828slr009,20209slr005_Oxiconazole_lbl.pdf
6. https://www.rxlist.com/Oxiconazole-drug.htm
7. https://pdf.hres.ca/dpd_pm/00003160.PDF
8. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/205076Orig1s000lbl.pdf
9. https://reference.medscape.com/drug/Oxiconazole-oxiconazole-topical-343492
10. https://www.clinicalkey.com/#!/content/drug_monograph/6-s2.0-1487