Buy Ketoconazole
Ketoconazole

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Ketoconazole is a broad-spectrum antifungal medication used to treat various serious fungal infections. It belongs to the azole class of drugs and works by slowing the growth of fungi that cause infection. This treatment is typically used when other antifungal therapies are not tolerated or appropriate.


Ingredient
Category
Availability
In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
Product is shipped in a fully discreet envelope with no content disclosure, including all required documentation inside

Product Sheet

Active Ingredient(s)
Ketoconazole
Reference Brand
Nizoral
Manufacturer
Johnson & Johnson
Product Form
Cream, Shampoo, Tablet
Regulatory Classification
OTC
Primary Category
Antifungal
Product Category
Dermatologicals, Antifungals for topical use, Imidazole and triazole derivatives
Pharmacological Class
Azole antifungals
Manufacturer Description
Used to treat various fungal infections of the skin and scalp, including dandruff and athlete's foot.
Mechanism of Action
Ketoconazole works by interfering with the synthesis of ergosterol, a vital component of fungal cell membranes. This weakens the membrane, causing the fungal cells to leak and eventually die, clearing the infection.
Route of Administration
Topical
Onset Time
Few days (Topical)
Duration
Varies by condition
Contraindications
Known allergy to ketoconazole, Liver disease (for oral use), Skin infections caused by viruses
Severe Adverse Events
Severe liver damage (oral only), Severe skin burning, Swelling of the face or lips
Common Side Effects
Dry skin, Skin irritation, Mild itching
Uncommon Side Effects
Stinging sensation, Changes in hair texture, Contact dermatitis
Drug Interactions
Topical corticosteroids, Warfarin (if oral)
Pregnancy Safety Warnings
Topical forms are generally safe; oral forms should be avoided. Consult your GP.
Age Restrictions
Consult doctor for children under 12
Storage Guidelines
Store below 25°C.

Ketoconazole FAQ

Can I take ketoconazole with alcohol?

Alcohol adds extra strain on the liver, which already processes ketoconazole. While occasional moderate consumption may be tolerated, patients with existing liver disease or those on prolonged ketoconazole therapy should limit or avoid alcohol to reduce the risk of hepatotoxicity.

What does a ketoconazole tablet look like?

In the UK, the 200 mg oral tablet is typically round, white to off-white, and may bear an imprint code such as “K200” or the manufacturer’s logo. Inactive ingredients often include lactose, starch, and magnesium stearate.

Is ketoconazole used in sports drug testing?

Ketoconazole is not listed as a prohibited substance by major sporting bodies such as UK Anti-Doping (UKAD). However, athletes should disclose all prescription medications to their medical team to avoid inadvertent violations.

How long does treatment with ketoconazole usually last?

The duration depends on the infection site and severity. For uncomplicated dermatophytosis, therapy may continue for 2-4 weeks. More invasive systemic infections might require treatment for 6 weeks or longer, as directed by a clinician.

Can ketoconazole be a substitute for fluconazole?

Both belong to the azole class but have different safety and drug-interaction profiles. Ketoconazole carries a higher risk of liver toxicity and is generally reserved for cases where fluconazole is contraindicated or ineffective.

What should I do if I develop a rash while taking ketoconazole?

A mild rash may be a common side effect, but any skin reaction that spreads, becomes painful, or is accompanied by swelling should be reported to a healthcare professional promptly, as it could signal an allergic response.

Are there any travel considerations with ketoconazole?

When traveling to regions with limited medical facilities, carry a sufficient supply of medication and a copy of the prescription. Keep tablets in their original packaging to aid customs clearance and avoid exposure to extreme temperatures.

Does ketoconazole interact with hormonal contraceptives?

Ketoconazole can increase plasma levels of estrogen-containing contraceptives by inhibiting CYP3A4, potentially raising the risk of side effects. However, contraceptive efficacy is generally maintained; discuss any concerns with a healthcare provider.

Why is ketoconazole less commonly prescribed today?

Due to reports of serious liver injury, regulatory agencies have restricted its oral use to specific indications where benefits outweigh risks. Many clinicians now prefer newer azoles with improved safety profiles.

What is the best way to store ketoconazole tablets while traveling?

Place the bottle in a sealed plastic bag to protect against moisture, keep it in a carry-on bag away from direct sunlight, and avoid storing it in hot compartments such as near a laptop or in a vehicle on a sunny day.

Ketoconazole: Generic Antifungal Medication Overview

Ketoconazole is an oral antifungal medication classified within the antifungals therapeutic group. It is supplied as a 200 mg pill and is prescribed in the United Kingdom under the supervision of a qualified prescriber. The medicine is a synthetic imidazole derivative that works by interfering with fungal cell membrane synthesis. In the UK, ketoconazole tablets are regulated by the Medicines and Healthcare products Regulatory Agency (MHRA) and are available only with a prescription.

How Ketoconazole Works in the Body

Ketoconazole belongs to the azole class of antifungals. Its primary pharmacological action is the inhibition of the fungal enzyme lanosterol 14α-demethylase, a key component of the ergosterol biosynthesis pathway. By blocking this enzyme, ketoconazole reduces the production of ergosterol, an essential sterol for fungal cell membranes. The resulting disruption compromises membrane integrity, leading to impaired cell growth and ultimately fungal cell death.

  • Onset of action: Clinical improvement is usually observed within a few days of initiating therapy, although full eradication of infection may require several weeks.
  • Metabolism: After oral absorption, ketoconazole is extensively metabolised in the liver by cytochrome P450 enzymes, particularly CYP3A4.
  • Elimination: Metabolites are excreted primarily in the bile and, to a lesser extent, in the urine.

Conditions Treated by Ketoconazole

Ketoconazole tablets have been approved for the treatment of certain systemic fungal infections, notably:

  • Dermatophytosis (e.g., tinea corporis, tinea cruris) when topical therapy is insufficient.
  • Candidiasis affecting the oral cavity, esophagus, or systemic sites in patients who cannot tolerate other antifungals.

These indications are aligned with the MHRA’s approved labeling for oral ketoconazole in the United Kingdom. The medication is generally reserved for cases where alternative agents (such as fluconazole or itraconazole) are unsuitable, owing to ketoconazole’s hepatic safety profile.

Evidence-Based Off-Label Uses

Some clinical investigations have explored ketoconazole for conditions beyond its approved fungal indications:

  • Cushing’s syndrome: Ketoconazole can inhibit adrenal steroid synthesis by blocking enzymes like 11β-hydroxylase, offering a medical option for patients with hypercortisolism. This use is off-label in the UK and must be managed by an endocrinologist.
  • Seborrheic dermatitis: Low-dose oral ketoconazole has been trialled as an adjunct to topical therapy for severe scalp involvement.

Disclaimer: Off-label use of ketoconazole requires careful medical supervision, individualized risk assessment, and regular monitoring of liver function. It is not approved by the MHRA for these indications.

Who Should (and Should Not) Use Ketoconazole?

Ideal Patient Profile

  • Adults with confirmed systemic or extensive dermatophyte or Candida infections where first-line agents are contraindicated or ineffective.
  • Patients with normal liver function tests (LFTs) at baseline.

Absolute Contraindications

  • Known hypersensitivity to ketoconazole or any azole antifungal.
  • Pre-existing severe hepatic impairment (e.g., Child-Pugh class C).
  • Concomitant use of drugs that are strong CYP3A4 inhibitors (e.g., clarithromycin, ritonavir) where dose adjustment is not feasible.

Relative Contraindications

  • Mild to moderate liver disease - requires close LFT monitoring.
  • Pregnancy (Category C) - ketoconazole crossing the placenta may pose fetal risk; it should be avoided unless clearly justified.
  • Breastfeeding - the drug is excreted in breast milk; alternatives are preferred.

Special Populations

  • Elderly: May have reduced hepatic clearance; dosing adjustments are often needed.
  • Renal impairment: No dose reduction is required for mild to moderate dysfunction, but severe renal failure warrants clinical judgment.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Gastrointestinal upset (nausea, abdominal pain) - reported frequently.
  • Headache - generally mild and transient.
  • Skin rash or pruritus - may indicate a mild hypersensitivity reaction.

Serious Adverse Events

  • Hepatotoxicity: Elevations in ALT, AST, and bilirubin can progress to clinically significant liver injury. Rare cases of fulminant hepatitis have been documented.
  • Adrenal suppression: Particularly at higher doses or prolonged use, ketoconazole may reduce cortisol production.
  • QT prolongation: May occur in patients with pre-existing cardiac conditions or when combined with other QT-prolonging agents.

Drug Interactions

  • Major interactions: Strong CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) can increase ketoconazole plasma levels, raising the risk of hepatotoxicity.
  • Moderate interactions: CYP3A4 inducers (e.g., rifampicin, carbamazepine) may lower ketoconazole concentrations, reducing antifungal efficacy.
  • Warfarin: Ketoconazole may enhance anticoagulant effect; INR should be monitored closely.

Food and Lifestyle Interactions

  • Grapefruit juice: Inhibits CYP3A4 and can raise ketoconazole levels; patients should avoid large quantities.
  • Alcohol: Combined hepatic stress may increase the likelihood of liver injury; moderation is advised.
  • Driving: No direct impairment, but patients experiencing dizziness or severe fatigue should exercise caution.

If specific interaction data for a concurrent medication is unavailable, patients should always inform their healthcare provider of all prescribed, over-the-counter, and herbal products before starting ketoconazole.

How to Take Ketoconazole

  • Standard dosing: The common regimen for systemic fungal infections is 200 mg once daily, taken with a full glass of water. In some cases, clinicians may prescribe 200 mg twice daily; the exact schedule must be confirmed by the prescriber.
  • With food: Ketoconazole tablets are better absorbed when taken with a meal that contains some fat.
  • Missed dose: Take the missed tablet as soon as remembered unless it is close to the time of the next scheduled dose. Do not double the dose.
  • Overdose: Symptoms may include severe nausea, vomiting, abdominal pain, and marked liver enzyme elevations. Seek emergency medical attention; activated charcoal may be considered if presentation is early.
  • Discontinuation: Abrupt cessation is generally safe, but long-term therapy should be tapered under medical guidance to avoid rebound fungal growth.

Monitoring and Follow-Up

  • Baseline liver function tests (LFTs) before initiating therapy.
  • Follow-up LFTs at 2 weeks, then monthly for the first 3 months, and periodically thereafter if treatment continues beyond 3 months.
  • Clinical assessment for signs of hepatotoxicity (e.g., jaundice, dark urine) should be performed at each visit.
  • Drug level monitoring is not routinely required but may be considered when using interacting medications.

Storage and Handling

  • Store tablets at room temperature (15-25 °C), protected from moisture and direct sunlight.
  • Keep the container tightly closed and out of reach of children.
  • Do not use tablets beyond the expiration date printed on the pack.
  • Dispose of unused medication via a local pharmacy take-back scheme or following MHRA waste guidelines.

Medication-Specific Glossary

Lanosterol 14α-demethylase
The fungal enzyme targeted by azole antifungals; inhibition disrupts ergosterol synthesis essential for cell membrane stability.
Ergosterol
The primary sterol component of fungal cell membranes; its depletion compromises cell integrity.
CYP3A4
A major liver enzyme responsible for metabolising many drugs, including ketoconazole; inhibition or induction of CYP3A4 can alter drug levels.
Hepatotoxicity
Liver injury caused by a medication, characterised by elevated liver enzymes or clinical jaundice.
QT prolongation
An elongation of the heart’s electrical repolarisation interval, which can predispose to arrhythmias.
Adrenal suppression
Reduced production of cortisol and other adrenal steroids, potentially leading to fatigue, hypotension, or electrolyte imbalances.

Medical Disclaimer

This article provides educational information about ketoconazole and is not a substitute for professional medical advice. Treatment decisions, including the use of unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Information for Ketoconazole is sourced from established medical standards and updated frequently. It is provided for general guidance and should be confirmed with a healthcare professional before use.
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