Nizoral, with its active ingredient ketoconazole, represents a cornerstone in the topical and systemic management of fungal infections. As a broad-spectrum imidazole antifungal agent, it operates primarily by inhibiting the synthesis of ergosterol, a critical component of fungal cell membranes, leading to increased cellular permeability and eventual cell death. Its efficacy against a wide range of dermatophytes, yeasts, and fungi has been well-documented in clinical practice for decades. This product card provides a comprehensive, evidence-based overview for healthcare professionals and informed patients, detailing its appropriate use, pharmacological profile, and safety considerations to ensure optimal therapeutic outcomes.

Features

• Active Ingredient: Ketoconazole 20 mg per gram (2% w/w) in topical formulations; 200 mg per tablet in oral formulations.
• Drug Class: Synthetic imidazole broad-spectrum antifungal agent.
• Mechanism of Action: Inhibition of the cytochrome P450-dependent 14α-demethylase, blocking the conversion of lanosterol to ergosterol, a vital sterol in fungal cell membranes.
• Formulations: Available as a medicated shampoo, cream, and oral tablets.
• Spectrum of Activity: Effective against dermatophytes (Trichophyton, Microsporum, Epidermophyton), yeasts (Malassezia spp., Candida spp.), and other fungi.

Benefits

• Targeted Fungal Eradication: Directly disrupts the integrity of fungal cell walls, leading to fungistatic and fungicidal effects against susceptible organisms.
• Rapid Symptom Relief: Clinical studies demonstrate significant reduction in scaling, itching, and erythema associated with fungal infections, often within the first week of use.
• Reduction in Recurrence: Effective treatment of the underlying infection helps prevent common recurrences, particularly in conditions like seborrheic dermatitis and tinea versicolor.
• Proven Clinical Efficacy: Supported by extensive clinical trial data and decades of post-market surveillance confirming its safety and effectiveness profile.
• Dual-Action Shampoo: The 2% ketoconazole shampoo not only treats fungal conditions of the scalp but also helps control flaking and scaling associated with dandruff.

Common use

Nizoral is indicated for the treatment of a variety of fungal infections. Topical formulations (shampoo, cream) are primarily used for cutaneous manifestations, while the oral tablet is reserved for severe systemic infections. Common indications include:

• Seborrheic Dermatitis: Of the scalp (using the shampoo) and the body (using the cream).
• Tinea Versicolor (Pityriasis Versicolor): A common fungal infection causing discolored patches on the skin.
• Cutaneous Candidiasis: Infections of the skin caused by Candida species.
• Dermatophytoses: Including athlete’s foot (tinea pedis), jock itch (tinea cruris), and ringworm (tinea corporis).
• Systemic Fungal Infections: Oral tablets are used for blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis, as well as candidiasis in patients who are refractory to or intolerant of first-line therapy.

Dosage and direction

Administration is route and indication-specific. Always follow a healthcare provider’s prescription.

• Nizoral Shampoo (2%): Apply to wet hair, lather, and leave in place for 3-5 minutes before rinsing thoroughly. For seborrheic dermatitis, use twice weekly for 4 weeks, spacing uses 3 days apart. For maintenance, use once every 1-2 weeks. For tinea versicolor, apply once daily for 5 days.
• Nizoral Cream (2%): Apply a sufficient amount to cover the affected and immediate surrounding area once or twice daily. Duration of treatment varies by condition but typically lasts 2-6 weeks until clinical clearing is achieved.
• Nizoral Tablets (200 mg): The typical adult dosage is 200 mg once daily. In severe infections or if clinical response is insufficient, the dose may be increased to 400 mg once daily. Administration with an acidic beverage (e.g., cola) may be necessary to ensure adequate absorption. Duration of treatment is based on clinical response and may require several months for deep mycoses.

Precautions

• Topical Use: For external use only. Avoid contact with eyes, nose, mouth, and other mucous membranes. If contact occurs, rinse thoroughly with water.
• Hepatic Function: Oral ketoconazole has been associated with serious hepatotoxicity, including fatal liver failure. Liver function tests should be performed prior to and during treatment with oral Nizoral.
• Adrenal Function: Oral ketoconazole inhibits adrenal steroidogenesis. Monitor for signs of adrenal insufficiency during treatment.
• Pregnancy and Lactation: Topical use is generally considered low risk. Oral ketoconazole is contraindicated during pregnancy due to potential toxicity and should not be used by nursing mothers.
• Sun Exposure: Patients using Nizoral should minimize exposure to natural and artificial sunlight (tanning beds) as ketoconazole may cause photosensitivity.

Contraindications

Nizoral is contraindicated in patients with:

• Known hypersensitivity to ketoconazole, any other imidazoles, or any component of the formulation.
• Chronic liver disease or baseline liver enzyme abnormalities (for oral formulation).
• Concomitant use of drugs that are highly dependent on CYP3A4 metabolism and for which elevated plasma concentrations are associated with serious and/or life-threatening events (e.g., quinidine, dofetilide, pimozide, levacetylmethadol, cisapride, triazolam, oral midazolam, ergot alkaloids, HMG-CoA reductase inhibitors like simvastatin and lovastatin).
• Concomitant use with colchicine, fesoterodine, or solifenacin in patients with varying degrees of renal or hepatic impairment.

Possible side effect

Side effects vary by route of administration.

• Topical (Shampoo/Cream): Generally well-tolerated. The most common side effects are local and may include abnormal hair texture, scalp pustules, mild burning, irritation, pruritus, and oiliness/dryness of hair and scalp.
• Oral (Tablets): Side effects are more common and can be severe.
  • Common: Nausea, vomiting, abdominal pain, pruritus.
  • Serious: Hepatotoxicity (may be fatal), adrenal insufficiency, severe dermatologic reactions (e.g., Stevens-Johnson syndrome), thrombocytopenia, anaphylaxis.

Drug interaction

Oral ketoconazole is a potent inhibitor of the cytochrome P450 3A4 enzyme system and has numerous significant drug interactions. Topical application results in minimal systemic absorption and is unlikely to cause interactions.

• Contraindicated Concomitant Use: As listed in Contraindications.
• Other Significant Interactions: May increase levels of alfentanil, budesonide, buspirone, busulfan, carbamazepine, cyclosporine, digoxin, docetaxel, felodipine, fentanyl, indinavir, methylprednisolone, paclitaxel, ritonavir, saquinavir, sirolimus, tacrolimus, verapamil, warfarin, and many others.
• Agents Affecting Absorption: Drugs that reduce gastric acidity (e.g., antacids, H2-receptor antagonists, proton pump inhibitors) may significantly reduce the absorption of oral ketoconazole. Administer these drugs at least 2 hours after ketoconazole.
• Consult a full drug interaction database or a pharmacist before initiating oral Nizoral therapy.

Missed dose

• Topical: Apply the next dose as soon as remembered, then resume the regular schedule. Do not apply a double dose to make up for the missed one.
• Oral: Take the missed dose as soon as remembered. However, if it is almost time for the next scheduled dose, skip the missed dose and resume the usual dosing schedule. Do not take a double dose to make up for a missed one.

Overdose

• Topical: Overdose is unlikely due to minimal systemic absorption. Treatment should be symptomatic and supportive.
• Oral: In the event of an overdose, symptomatic supportive measures should be instituted. Gastric lavage may be indicated if performed soon after ingestion. As ketoconazole is highly protein-bound, it is not dialyzable. Monitor liver function and adrenal function closely.

Storage

• Store at room temperature between 20°C to 25°C (68°F to 77°F).
• Keep the container tightly closed and protect from light and moisture.
• Do not freeze.
• Keep all medications out of the reach of children and pets.

Disclaimer

This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

“Nizoral shampoo has been a game-changer in my dermatology practice for managing stubborn seborrheic dermatitis. Patients report rapid relief from itching and flaking, and the twice-weekly regimen is highly effective for long-term control.” – Dermatologist, 15 years of experience.

“As an infectious disease specialist, I reserve oral ketoconazole for specific, serious systemic fungal infections where other antifungals are not suitable. Its potency is undeniable, but the required vigilance for hepatotoxicity and its extensive drug interaction profile demand careful patient selection and monitoring.” – ID Specialist.

“For my patients with recurrent tinea versicolor, a short course of Nizoral cream consistently clears the eruption. It’s a reliable and effective first-line topical agent in my toolkit.” – General Practitioner.