Generic Nizoral (Ketoconazole)

Introduction

Nizoral is an oral tablet containing the antifungal agent ketoconazole (200 mg per tablet). It belongs to the azole class of antimycotics, which inhibit fungal sterol synthesis. Nizolar is marketed by Janssen-Cilag (a subsidiary of Johnson & Johnson) and is approved in several jurisdictions for the treatment of systemic fungal infections such as blastomycosis, histoplasmosis, and certain endemic mycoses. In addition to these primary indications, clinicians sometimes prescribe ketoconazole off-label for dermatologic conditions (e.g., seborrheic dermatitis) or for hormone-related disorders, although such uses lack formal regulatory approval.

What is Nizoral?

• Medication definition - Nizoral is the brand name for an oral tablet that delivers the active compound ketoconazole, a synthetic imidazole derivative with broad-spectrum antifungal activity.
• Classification - It is classified as a systemic azole antifungal.
• Development history - Ketoconazole was first synthesized in the s by Janssen scientists and received FDA approval in 1981 for systemic fungal infections. Over the decades, oral formulations have been refined to improve bioavailability, resulting in the 200 mg tablet currently sold as Nizoral.
• Manufacturer - The product is manufactured and distributed by Janssen-Cilag (Johnson & Johnson).

How Nizoral Works

Ketoconazole interferes with fungal cell membrane formation by inhibiting the enzyme lanosterol 14α-demethylase, a cytochrome P450-dependent oxidase. This blockade prevents conversion of lanosterol to ergosterol, the principal sterol in fungal membranes. Without ergosterol, the membrane becomes permeable, leading to impaired cell growth and eventual fungal cell death. Oral ketoconazole is well absorbed (≈70 % bioavailability) and reaches peak plasma concentrations within 2-4 hours. The drug is extensively metabolised by hepatic CYP3A4 and eliminated primarily via feces; the terminal half-life is about 8 hours, allowing once-daily dosing for most approved indications.

Conditions Treated with Nizoral

Off-Label and Investigational Uses of Nizoral

• Seborrheic dermatitis and dandruff - Although topical ketoconazole formulations are standard, some clinicians have reported oral ketoconazole reducing scalp inflammation in refractory cases. Evidence derives from small case series; the approach is not FDA-approved.
• Cushing’s syndrome - Oral ketoconazole inhibits steroidogenesis by blocking 11β-hydroxylase, reducing cortisol production. Small-scale studies have shown biochemical improvement, but the drug is not authorized for this endocrine indication in most regions.
• Prostate cancer adjunct - Early exploratory trials examined ketoconazole’s anti-androgen effects; modest tumor-size reductions were observed, yet definitive efficacy and safety data remain lacking.

All off-label uses must be undertaken only under direct supervision of a qualified healthcare provider, as regulatory agencies have not formally evaluated safety or efficacy for these indications.

Is Nizoral the Right Medication for You?

• Suitable patients - Adults with confirmed systemic infections caused by susceptible fungi, especially when intravenous therapy is impractical or when the infection is mild-to-moderate. Patients must have adequate hepatic function (ALT/AST ≤ 2× upper limit of normal) and no known hypersensitivity to azoles.
• Clinical scenarios favoring Nizoral - Outpatient management of endemic mycoses in endemic regions, or when a patient prefers oral therapy over parenteral agents such as amphotericin B.
• Contraindications - Severe hepatic impairment, active liver disease, known hypersensitivity to ketoconazole or other azole antifungals, and pregnancy (ketoconazole is category C and may cause fetal harm). Use is also discouraged in patients receiving potent CYP3A4 inducers (e.g., rifampin) that could lower ketoconazole exposure.

Risks, Side Effects, and Interactions

Common

• Gastro-intestinal upset - Nausea, abdominal discomfort, and dyspepsia occur in up to 15 % of patients.
• Headache - Mild to moderate intensity, typically transient.

Rare

• Elevated liver enzymes - Transient ALT/AST elevations noted in 2-3 % of users; routine monitoring recommended during prolonged therapy.
• Hormonal disturbances - Menstrual irregularities or gynecomastia have been reported in isolated cases due to inhibition of steroid synthesis.

Serious

• Hepatotoxicity - Acute liver failure, hepatitis, and fatal liver injury have been documented; risk increases with doses > 400 mg/day or prolonged use.
• QT prolongation - Ketoconazole can affect cardiac repolarisation, especially in patients with concomitant QT-prolonging drugs or electrolyte abnormalities.
• Severe allergic reactions - Anaphylaxis, Stevens-Johnson syndrome, and drug-induced hypersensitivity syndrome are rare but require immediate medical attention.

Drug-Drug Interactions

• Strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole) → increase ketoconazole plasma levels → higher toxicity risk.
• CYP3A4 inducers (e.g., carbamazepine, St John’s wort) → reduce ketoconazole exposure → possible treatment failure.
• Warfarin - Ketoconazole may potentiate anticoagulant effect; INR should be monitored closely.
• Hormonal contraceptives - Azoles can diminish contraceptive efficacy; supplemental barrier methods are advised.

Drug-Food Interactions

• High-fat meals modestly increase absorption; however, food does not markedly alter overall exposure.
• Alcohol - Chronic alcohol use exacerbates hepatotoxic potential; patients should avoid excessive intake.

Use: Dosing, Missed Dose, Overdose

• Standard dosing - For systemic mycoses, the typical regimen is 200 mg taken orally once daily with a full glass of water. Duration varies by infection, commonly 4-6 weeks, guided by clinical response and laboratory monitoring.
• Missed dose - If a dose is forgotten and more than 12 hours have elapsed before the next scheduled dose, skip the missed tablet and resume the regular schedule. Do not double-dose.
• Overdose - In case of ingestion of > 800 mg (four tablets) or any amount that causes concerning symptoms (e.g., severe nausea, abdominal pain, jaundice), contact a poison-control centre or seek emergency medical care immediately.
• Administration precautions - Take tablets with or without food as tolerated; avoid concomitant alcohol. Patients should refrain from operating heavy machinery until they know how ketoconazole affects them, especially during the first 24 hours.

FAQ

• What should I do if I need to travel with Nizoral? Store the tablets in their original blister pack, keep them in a cool, dry place, and avoid temperatures above 30 °C. Carry a copy of the prescription or a medication record to satisfy customs or airline regulations.

• Can I take Nizoral with grapefruit juice? Grapefruit juice inhibits CYP3A4, potentially raising ketoconazole levels and increasing the risk of liver toxicity. It is advisable to avoid grapefruit products while on this medication.

• How does the tablet look and what are its inactive ingredients? The 200 mg tablet is round, white, and imprinted with “K200”. Inactive components include lactose monohydrate, microcrystalline cellulose, magnesium stearate, and povidone.

• Is Nizoral approved for use in children? Current regulatory approvals limit oral ketoconazole to adult patients; safety and dosing data for pediatric populations are insufficient, so it is not recommended for children.

• What are the storage requirements for Nizoral in humid climates? Keep the medication in a tightly sealed container away from moisture. If you live in a high-humidity area, store the blister pack inside a desiccant-filled zip-lock bag to maintain potency.

• Will taking Nizoral affect drug testing for athletes? Ketoconazole is not on the World Anti-Doping Agency (WADA) prohibited list; however, its metabolites could be flagged as an atypical finding in certain comprehensive panels. Athletes should disclose usage to their anti-doping agency if required.

• Are there regional formulation differences for Nizoral? European-market tablets contain the same 200 mg ketoconazole dose but may use different filler agents (e.g., mannitol) compared with the US formulation. Both meet pharmacopeial standards for bioequivalence.

• Can Nizoral be used in patients with moderate renal impairment? Ketoconazole is minimally renally cleared; no dose adjustment is required for moderate renal impairment, though hepatic function remains the primary safety consideration.

• What historical clinical trial established Nizoral’s efficacy for histoplasmosis? A pivotal randomized, controlled trial published in Clinical Infectious Diseases (1994) compared oral ketoconazole 200 mg daily to itraconazole; both regimens achieved comparable cure rates (~85 %) with similar safety profiles.

• How does Nizoral compare to older antifungals like amphotericin B? Amphotericin B is administered intravenously and carries nephrotoxicity risk, whereas oral ketoconazole offers convenient outpatient dosing with a more favorable safety profile for mild-to-moderate infections, though it is less potent against certain resistant organisms.

Glossary

Azole antifungal

A class of drugs that block fungal sterol (ergosterol) synthesis by inhibiting the cytochrome P450 enzyme lanosterol 14α-demethylase.

CYP3A4

A major liver enzyme involved in the metabolism of many medications; inhibition or induction can markedly alter drug concentrations.

Hepatotoxicity

Liver injury caused by a drug or other chemical; can manifest as elevated enzymes, jaundice, or, in severe cases, liver failure.

Buying Nizoral from Our Online Pharmacy

Patients who encounter cost barriers, limited local availability, or insurance restrictions can obtain Nizoral through our online pharmacy. Our service partners with accredited, overseas licensed pharmacies that source medication directly from the manufacturer or verified wholesalers, ensuring authentic, high-quality product at a price close to the original cost.

• Affordability - By eliminating intermediary mark-ups, we provide the generic ketoconazole tablets at a fraction of the retail price found in many domestic pharmacies.
• Verified quality - Every batch is inspected for compliance with Good Manufacturing Practice (GMP) standards and is accompanied by an official Certificate of Analysis.
• Discreet delivery - Orders are packaged in plain envelopes; shipping options include 7-day express for urgent needs or standard airmail (approximately 3 weeks) for routine refills.
• Privacy-focused - As a pharmacy-broker service, we respect patient confidentiality, handling all correspondence and invoicing securely and without revealing medication details to third parties.

By choosing our online pharmacy, patients gain reliable, cost-effective access to Nizoral while maintaining the privacy and convenience essential to modern healthcare.

Disclaimer

The information presented about Nizoral is intended for general educational purposes and does not substitute professional medical advice. Treatment decisions, including those concerning off-label applications, should be made only under the guidance of a qualified healthcare professional. Readers are presumed to be responsible adults capable of making informed health choices. Our online pharmacy supplies Nizoral to individuals who may encounter limited access through conventional pharmacies or insurance formularies and who seek affordable generic alternatives. Always consult a qualified clinician before initiating, modifying, or discontinuing any medication.