Ketone

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Ketone

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Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Ketone

Quick Facts

Property Description
Active ingredient Ketoconazole
Form Tablet (oral), Cream, Shampoo, Foam, Gel (topical)
Pharmacological class Azole Antifungal, Imidazole Derivative
Common use Management of fungal and yeast infections
Origin Synthetic (chemically manufactured)

What Kind of Medicine is Ketoconazole? (Identity and Classification)

The medicine potentially marketed as Ketone contains the single active substance, Ketoconazole, which is a synthetic, broad-spectrum antifungal agent. This compound is classified within the azole antifungal family, specifically recognized as an imidazole derivative applied against dermatological fungi and yeasts.

Ketoconazole’s core purpose is antimycotic, designed to inhibit the growth and spread of fungal organisms. Unlike some strictly topical alternatives, the availability of Ketoconazole as both an oral tablet and various topical preparations underscores its flexibility for managing infections ranging from simple skin conditions to more complex systemic fungal challenges.

Forms and Origin: Is Ketone a Topical or Systemic Product? (Composition and Type)

Ketoconazole is a chemically synthesized compound, confirming it is synthetic in origin and not extracted from a natural source. This active ingredient is incorporated into multiple dosage forms to treat infections, including the oral tablet for internal (systemic) therapy and, distinctively, specialized topical preparations such as shampoo and foam.

This range of pharmaceutical preparations allows the medicine to be used either locally—delivering the drug directly to the affected area of the skin or scalp—or systemically via the oral route, ensuring flexibility in addressing different types and locations of fungal disease.

Primary Purpose and Unique Action (General Benefit and Mechanism High-Level)

The primary purpose of Ketoconazole is the management of fungal infections, acting as a fungistatic agent to halt organism proliferation. Its pharmacological actions are used for addressing conditions like seborrheic dermatitis of the scalp. Beyond its main function, Ketoconazole is characterized by a unique secondary action on human enzyme systems. When used systemically, this compound acts as an antiglucocorticoid. This distinct, secondary pharmacological property is utilized for managing specific endocrine disorders, making Ketoconazole unique among common antifungals.

Regulatory References

  1. EMA: Ketoconazole Esteve (EPAR)

What side effects are possible with Ketone?

Possible Side Effects and Safety Information

The medicine Ketoconazole, marketed as Ketone, has a safety profile that is differentiated based on the administration route. The oral tablet form is associated with potential systemic adverse reactions, while topical formulations primarily lead to local effects on the application site.

The most serious documented adverse reactions for the oral tablet involve Hepatobiliary disorders and Endocrine disorders. Regulatory authorities classify the risk of severe hepatotoxicity (liver injury) as a serious adverse reaction, which can occur regardless of the dose or duration of use. Adrenal insufficiency is also noted as an official systemic safety concern, which may be more pronounced at the initiation of treatment or during dose escalation.

Adverse reactions are formally categorized by frequency. Common reactions for the oral form typically include gastrointestinal issues such as nausea, vomiting, and abdominal pain, along with nervous system effects like headache and dizziness. Uncommon systemic effects may include hypersensitivity and certain reproductive system disorders, such as decreased libido.

For the topical preparations, effects are generally confined to the application site, classified as Common reactions such as a burning sensation, erythema, or pruritus. Serious adverse reactions like anaphylaxis are listed in official documents, though classified as rare.

Regulatory safety constraints explicitly note that the oral tablet is contraindicated in individuals with pre-existing acute or chronic liver disease. The systemic form also carries specific constraints regarding concomitant use with numerous other medicines due to the risk of serious adverse reactions from drug-drug interactions, such as those affecting the heart rhythm.

Overdose and Emergency Response

The official regulatory profile for Ketoconazole overdose focuses on severe, life-threatening outcomes affecting major organ systems. Documented systemic manifestations of overdose or excessive exposure primarily involve the hepatic system and the cardiovascular system.

Signs of potential severe liver injury, which may result in a fatal outcome or require liver transplantation, include jaundice (yellowing of the skin or eyes), dark urine, pale stools, and pain in the upper right abdomen. Cardiovascular risks are severe, with warnings about QT interval prolongation and the potential for life-threatening ventricular dysrhythmias, such as Torsades de Pointes. Neurological events like seizure or loss of consciousness are also associated with severe toxicity.

In the event of potential overdose or severe reaction, immediate medical attention is required. Regulators mandate calling emergency services if the individual is collapsed, seizing, or cannot be awakened. Management is symptomatic and supportive, as no specific antidote is known. Notably, if certain liquid topical products are accidentally ingested, regulatory instructions advise against inducing vomiting to avoid the risk of aspiration. Monitoring of liver function and electrolytes is required due to the potential for adrenal insufficiency following high-dose exposure.

Therapeutic Uses of Ketone

Ketone (Ketoconazole) is used across distinct therapeutic domains, providing support for conditions driven by fungal organisms and, systemically, for specific severe fungal diseases and unique endocrine regulation. Oral ketoconazole is considered relevant for managing serious systemic fungal infections like blastomycosis and histoplasmosis in specific clinical scenarios, as part of a strategy for managing fungal skin conditions.


Main Uses and Therapeutic Benefits

This medication is relevant for managing conditions characterized by inflammatory or irritative states caused by fungal or yeast overgrowth, including seborrheic dermatitis, ringworm (tinea), cutaneous candidiasis, and pityriasis versicolor. It is commonly used to help with symptom clusters that may become intense or disruptive, such as scaling, flaking, redness, and persistent itching.

For the oral form, it is applied in clinical settings that involve acute or unstable symptom patterns related to widespread internal infection or, uniquely, in scenarios where the patient experiences symptoms related to systemic imbalance from excessive cortisol production (Endogenous Hypercortisolism). The overall benefit is fungal control and relief from symptomatic manifestations for skin issues, or biochemical regulation to assist with maintaining functional stability in endocrine conditions.

“This approach is relevant when supportive symptom management is appropriate, helping to ease the overall symptom burden caused by fungal overgrowth or hormonal imbalance.”


Quick Fact: Relief for Key Symptom Domains
Symptomatic Target Scaling, Itching, Flaking, and Hypercortisolism Manifestations
Core Conditions Superficial Mycoses, Severe Systemic Fungal Diseases, Cushing's Syndrome
Main Benefit Supports Fungal Control and Biochemical Stability

Eligibility and Restrictions for Use

Official Eligibility and Contraindications

The eligibility criteria for Ketone (Ketoconazole) are strictly governed by the dosage form, with the oral tablet being highly restricted by regulatory authorities (FDA, EMA) due to serious risks.

Dosage Form Primary Eligibility Criterion
Oral Tablet Adults and children 2 years for Systemic Fungal Infections only when alternative therapies are unavailable or not tolerated
Topical Forms Adults and adolescents 12 years for superficial fungal infections (e.g., seborrheic dermatitis)

Populations Prohibited from Use (Contraindications)

Absolute prohibition applies to patients with acute or chronic liver disease for the oral tablet. Additionally, the oral tablet is strictly contraindicated for any individual taking specific coadministered drugs, such as certain statins (simvastatin, lovastatin) or medicines that prolong the QT interval (e.g., dofetilide, quinidine), due to the risk of severe adverse reactions. The medicine is also contraindicated for any patient with known hypersensitivity to Ketoconazole or its components.

Age and Pregnancy Restrictions

The safety and effectiveness of the oral tablet are not established in pediatric patients younger than 2 years of age. For topical preparations (cream, shampoo), use is not established in children younger than 12 years of age. Oral use is not recommended during breastfeeding due to regulatory caution.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Ketoconazole (Ketone) has a strictly defined interaction profile documented in regulatory labeling, primarily due to its potent effect on drug metabolism. The medicine is classified as a potent inhibitor of the CYP3A4 enzyme and is documented to inhibit the P-glycoprotein and BCRP drug transporters. This action significantly increases the plasma concentration of co-administered medicines that are substrates for these systems.

Formal Prohibitions

Co-administration with numerous CYP3A4-metabolized drugs is formally contraindicated by health authorities due to the high risk of serious or life-threatening adverse reactions. Prohibited combinations include specific antiarrhythmics (e.g., dofetilide, quinidine), certain HMG-CoA reductase inhibitors (e.g., simvastatin, lovastatin), and ergot alkaloids (e.g., ergotamine).

Administration Constraints

The product's oral absorption is dependent on gastric acidity. Acid-reducing agents, such as antacids and proton pump inhibitors, reduce the oral absorption of Ketoconazole. To avoid impaired absorption, administration of acid-neutralizing medicines must be separated by at least two hours from oral Ketoconazole intake. Consumption of alcohol is restricted during treatment due to the increased risk of hepatotoxicity.

Population-Specific Notes

The medicine is formally contraindicated in patients with acute or chronic liver disease, as this patient condition heightens the overall risk of interaction-related toxicity.

Mechanism of Action

Fungal Cell Membrane Synthesis Blockade

This domain covers the drug's core action as an inhibitor of the fungal enzyme Lanosterol 14-alpha demethylase (LADM). This inhibition arrests the synthesis of ergosterol , a sterol essential for the structural integrity and function of the fungal cell membrane. The molecular cascade leads to compromised fungal cell integrity, which results in a fungistatic cellular state.


️ Systemic Hormone Pathway Modulation

This secondary domain involves the compound acting as an inhibitor and antagonist within human endocrine systems, an effect primarily observed at higher systemic concentrations. The mechanism includes inhibiting key adrenal P450 enzymes responsible for cortisol synthesis and competitively blocking the Glucocorticoid Receptor (GR). This targeted interference with the steroidogenesis pathway leads to an anti-glucocorticoid physiological consequence.

Dosage and Administration Information

The administration of Ketoconazole, marketed as Ketone, is defined by its dosage form, which mandates distinct usage procedures for the oral tablet (systemic use) and topical preparations (localized use). All instructions should be followed according to the specific requirements for each form.

Administration Routes and Dosing

Administration Route Standard Adult Dosing (Starting Dose) Frequency and Duration (Typical)
Oral Tablet (200 mg) 200 mg once daily Single daily administration for a minimum of 6 months.
Topical Shampoo (2%) Wash affected areas Twice weekly for 2–4 weeks; prophylaxis is typically once every 1–2 weeks.

Conditions for Proper Use

Oral Administration Conditions:

  • With Food Requirement: The oral tablet must be taken with a meal to facilitate proper absorption.
  • Acidity Management: The drug requires an acidic environment for dissolution. If a patient is taking acid-reducing medications (e.g., antacids or H2-blockers), those medications should be taken at least 2 hours after the oral tablet.

Topical Administration Procedure:

  • Contact Time: When using the topical 2% shampoo, the product must be lathered and left on the affected skin or scalp area for 3 to 5 minutes before being rinsed off with water.

Use in Specific Populations:

  • For children 2 years of age and older, the oral dosage is based on body weight, typically administered as 3.3 to 6.6 mg/kg/day as a single dose. Safety and efficacy are not established for children under 2 years of age.

Recent Clinical Evidence

Research evidence / Overview of studies for Ketone

Evidence for Use in Fungal Skin and Scalp Conditions (Superficial Mycoses)

The research foundation for the topical forms of Ketoconazole is characterized by a body of short-term Randomized Controlled Trials (RCTs) and subsequent systematic reviews, as referenced in scientific databases. These trials were primarily applied in studies examining patient-reported experiences and outcomes related to physical discomfort for conditions characterized by inflammatory or irritative states like seborrheic dermatitis. Research examined endpoints such as mycological clearance (fungal culture status) and changes in symptom intensity or variability (e.g., scaling and itching) over defined time intervals. Studies tracked and reported the rates of clearance (mycological endpoints) and research explored measured changes in symptom scores over short-term periods. The differences in the formulations studied may introduce inconsistency, and data for certain groups remain insufficient.


Evidence for Use in Managing Specific Endocrine Conditions (Endogenous Hypercortisolism)

The research foundation for the management of endogenous hypercortisolism is composed mainly of retrospective observational studies, case series, and small prospective cohorts. Large, randomized controlled trials are scarce for this specific condition. This research was studied for its use in a specific endocrine disorder, often in patients whose condition involves periods of heightened symptoms related to cortisol excess.

Studies monitored outcomes related to systemic or functional imbalance, with the primary focus on biochemical endpoints such as changes in 24-hour urinary free cortisol (UFC) levels. Studies report how symptoms evolved in the observed populations, noting that levels of cortisol were observed to change in the measured cohorts. The lack of large, blinded, randomized controlled trials means the evidence for this highly specific use is less certain than for the topical indications, and long-term effects are not fully established.

Key Studies & References PubMed: Biomedical Literature Database (Search for Ketoconazole RCTs and Reviews)

Frequently Asked Questions (FAQ)

Common questions about Ketone (FAQ)

Q: Is it common to experience headache or dizziness when first starting Ketone?

A: Regulatory documents indicate that headache and dizziness are listed as Common adverse reactions for the oral form of Ketone. Official product information notes that the serious risk of Adrenal Insufficiency may be more noticeable at the initiation of treatment or when the dosage is increased.

Q: What are some signs of a more serious side effect of Ketone mentioned in regulatory warnings?

A: The official patient information for the oral tablet advises reporting specific signs related to the serious risk of liver injury (hepatotoxicity). These signs include unusual fatigue, loss of appetite (anorexia), vomiting, jaundice (yellowing of the skin), dark urine, or pale stools. These signs are listed in patient information as symptoms that warrant contacting a healthcare provider immediately.

Q: Are there any long-term safety concerns documented for Ketone?

A: Regulatory authorities have reported serious liver injury (hepatotoxicity), including cases with fatal outcomes, in patients taking the drug for long durations. This is why the oral tablet is strictly restricted for use only when other effective therapies are not available or tolerated, regardless of the treatment length.

Q: Does Ketone need to be monitored with regular blood tests or check-ups?

A: For the oral tablet, regulatory guidelines require the monitoring of specific laboratory tests, such as liver function tests (e.g., ALT levels), by the healthcare provider throughout the duration of treatment. These tests are typically obtained at baseline and then monitored weekly.

Q: Is the effectiveness of Ketone supported by large-scale clinical trials?

A: The regulatory status of the oral tablet reflects that it is reserved for severe systemic fungal infections and only indicated when other effective therapies are unavailable or not tolerated. This limitation is based on the regulatory assessment that the potential benefits must clearly outweigh the potential risks for this specific group of patients.

Q: Does Ketone affect the ability to drive or operate machinery?

A: Regulatory documentation for the topical forms states they are generally not likely to affect the ability to drive. However, the oral tablet lists dizziness as a Common adverse reaction. Due to the listed adverse reactions, individuals may need to assess their response to the medication before driving or operating machinery.

Q: What is the recommended action if a scheduled intake of Ketone is missed?

A: Patient instructions typically advise that if a dose is missed, it should be applied or taken as soon as it is remembered. However, if it is nearly time for the next scheduled dose, the missed dose should be skipped entirely, and the regular schedule should be resumed. Regulatory patient instructions generally advise resuming the regular schedule and avoiding taking extra doses.

Q: Are there specific vitamins or supplements that should not be taken with Ketone?

A: Official drug information sources and patient-facing materials advise that products containing Grapefruit and the herbal supplement St. John’s Wort may interact with Ketoconazole. Information indicates that such products warrant review by a healthcare provider.

Q: Does Ketone treat other conditions besides the main one listed in the official labeling?

A: Official documents explicitly state that the safety and effectiveness of the medicine have not been established for uses outside of the specified fungal infections. Regulatory bodies do not approve its use for unlisted indications.

Q: Is Ketone considered a long-term treatment option?

A: The systemic form’s minimum required duration is often a minimum of 6 months. However, the oral tablet is only authorized for limited use due to the risk of serious side effects, meaning it is not considered a general, first-line long-term option.

Q: Can Ketone affect a person's mood or energy levels?

A: Yes, the medicine carries a serious risk of Adrenal Insufficiency, which is a condition that impacts hormone and energy balance and can influence mood. Furthermore, official patient warnings for liver injury include reporting symptoms such as unusual fatigue.

Q: Can Ketone be taken at the same time as common over-the-counter pain relievers?

A: Regulatory warnings indicate that taking Ketoconazole alongside other medicines that can also affect the liver, such as certain over-the-counter pain relievers (NSAIDs), may increase the overall risk of liver injury (hepatotoxicity). The official guidance indicates that co-administration warrants review by a healthcare provider.

Q: How long has the drug Ketone been on the market in the US or Europe?

A: Ketoconazole is considered one of the earliest synthetic azole antifungal agents. It was initially developed and introduced for clinical use during the late 1970s and early 1980s.

Q: Are generic versions of Ketone currently available for purchase?

A: Yes, regulatory records from bodies like the FDA confirm that generic versions of both the oral tablet and various topical formulations of Ketoconazole are available for prescription.

Q: How long does Ketone stay present in the body after the last dose?

A: The elimination of the active ingredient is described as biphasic. After oral intake, the half-life is approximately 2 hours during the initial 10 hours and then extends to about 8 hours thereafter.

Q: Can Ketone be stopped abruptly, or does it require gradual cessation?

A: Due to the potential risk of developing Adrenal Insufficiency while taking the oral tablet, Official guidance emphasizes that any change to the treatment plan warrants discussion with a qualified healthcare professional.

Q: How is Ketone classified by regulatory bodies (e.g., controlled substance)?

A: The medicine is designated as a prescription-only medicine by regulatory bodies. It is not currently classified or scheduled as a controlled substance.

Q: Does Ketone interact with herbal remedies like St. John's Wort?

A: Yes, patient information sources specifically mention that herbal products like St. John’s Wort may interact with Ketoconazole. Information indicates that these potential interactions warrant review by a healthcare professional.

Q: Can Ketone affect the results of routine lab tests?

A: Yes, due to the drug’s known effects on the liver and adrenal system, official regulatory guidelines require the monitoring of specific lab tests, such as liver enzyme levels (like ALT), both before and during treatment.

Q: Is Ketone used to manage pain?

A: No. The official indications for the oral tablet are limited to the management of systemic fungal infections. Pain management is not an approved use according to official regulatory documentation.

Q: Why do official documents emphasize a certain lifestyle change alongside Ketone use?

A: Official patient instructions, particularly for the topical form, include advice on concurrent clothing or hygiene (e.g., wearing loose-fitting cotton underwear). This is intended to support the treatment and help clear the fungal infection completely.

Q: Is Ketone typically taken in the morning or at night?

A: Regulatory patient information does not mandate a specific time (morning or night) for intake. However, it emphasizes that the medicine must be taken at the same time every day to ensure consistent drug levels in the body.

How should Ketone be stored and disposed of?

How to Store and Dispose of Ketone

Official regulatory guidelines define specific requirements for the storage, handling, and disposal of this product, focusing on safety and environmental protection.

Storage Requirements

Ketone must be stored in a cool, dry, and well-ventilated area, typically maintained at room temperature. It is critical to keep the container tightly closed and to store the product away from heat, sparks, open flames, and any ignition sources. The product must be handled using non-sparking tools and in a grounded container.

Disposal Instructions

Disposal of unused or expired Ketone must be performed through an approved waste disposal plant in compliance with all local and national hazardous waste regulations. Do not dispose of the product in household trash, wastewater, or release it into the environment. Regulatory bodies often classify this substance as a controlled or hazardous waste, requiring specialized collection and destruction.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

Equivalent of Ketone found in:

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