Ketazole

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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 Ketazole

Property Description
Active ingredient Ketoconazole
Form Tablet, Cream, Shampoo, Foam, Gel
Pharmacological class Azole Antifungal (Imidazole derivative)
General purpose Control and inhibit fungal growth
Origin Synthetic

Ketazole is a brand name for a medicinal product containing the sole active compound Ketoconazole, which is chemically defined as a synthetic broad-spectrum antifungal agent. It belongs to the imidazole sub-group, which is part of the larger azole antifungal pharmacological class, positioning it as a recognized agent against various fungal pathogens.


What Type of Medicine is Ketazole (Ketoconazole)?

Ketazole is a medicine primarily used for its capability to control or eliminate different types of fungal organisms. The fundamental identity of the drug is defined by the Ketoconazole molecule, a synthetic compound with the established chemical structure C26H28Cl2N4O4. Ketoconazole is recognized for its anti-fungal efficacy against susceptible organisms.

As a single-ingredient product, its classification as an antifungal agent is critical, signifying its therapeutic function of interfering with the viability and replication of fungal cells. This core function serves to manage persistent fungal proliferation.


Composition and Available Forms of Ketoconazole

The medicine is composed of the sole active ingredient, Ketoconazole, and is manufactured in multiple dosage forms to accommodate different sites of infection, positioning it as a versatile antifungal solution. This synthetic agent is available as a tablet for systemic use (acting internally throughout the body) and in various topical preparations.

These topical use forms include cream, shampoo, foam, and gel, which use specialized bases to deliver the antifungal compound directly to external surfaces like the skin or scalp. Ketoconazole is available in formulations that permit both topical use and oral administration. This range of available forms is often leveraged to address fungal conditions by ensuring targeted delivery of the antifungal.


General Purpose of this Antifungal Agent

The general purpose of this medicine is to resolve issues stemming from fungal proliferation by stopping the growth and survival of the causative microorganism. The inherent ability of Ketoconazole to disrupt the integrity of the fungal structure enables it to act as a fungistatic agent, which means it limits the fungal organism's capacity to spread and proliferate. The core benefit is the control and inhibition of the infectious agent, facilitating the natural recovery of affected tissues.

What side effects are possible with Ketazole?

Ketazole (Ketoconazole) is associated with an officially documented safety profile, which varies significantly between its systemic (oral tablet) and topical forms. Regulatory authorities highlight that the oral tablet carries a risk of serious adverse reactions that are systemic in nature.

Serious Adverse Reactions and Systemic Risks

The primary systemic safety concerns documented in official labels involve the Hepatobiliary Disorders (risk of severe, sometimes fatal, liver injury) and Cardiac Disorders (risk of QTc prolongation potentially leading to life-threatening ventricular dysrhythmias). A risk of Adrenal Insufficiency is also documented, which is generally related to higher dosages.

Side effects are classified across several System-Organ Classes, including Gastrointestinal Disorders (e.g., nausea, vomiting) which are commonly reported for the oral form. Other categories include Nervous System Disorders (such as headache and dizziness) and Skin and Subcutaneous Tissue Disorders (including rash and pruritus). Topical preparations are primarily linked to localized application site reactions like irritation or a burning sensation.

Official Safety Constraints

The most significant safety restrictions are based on pre-existing conditions. The oral form is officially contraindicated in individuals with acute or chronic liver disease, as well as those with pre-existing QTc prolongation. Liver function must be monitored before and during treatment, as adverse hepatic events have been reported both at the start and during long-term use. Safety constraints are also explicitly documented for specific groups, as the oral tablet's use is generally contraindicated during pregnancy, and its safety in children under 12 years has not been established.

Overdose and Emergency Response

Overdose and when to seek help

Official regulatory documents define the overdose profile for systemic Ketoconazole (Ketazole) primarily around the risk of severe organ toxicity and life-threatening cardiac events. Manifestations of overdose may include signs of acute liver injury, such as jaundice, fatigue, and nausea, alongside potential signs of adrenal insufficiency, including hypotension and unusual weakness.

Overdose has been associated with serious and potentially fatal outcomes, including the risk of requiring liver transplantation. Of particular concern is the potential for QT prolongation leading to life-threatening ventricular dysrhythmias, such as Torsades de pointes, which constitutes a cardiac emergency.

Required Emergency Action

If overdose is suspected, official guidance mandates that an individual seek immediate medical attention by contacting a poison control center or emergency room at once. Emergency services must be called immediately if the affected person has collapsed, experienced a seizure, or has trouble breathing.

Management and Antidote

No specific antidote is known for Ketoconazole overdose; therefore, management is symptomatic and supportive. Regulatory documents describe that procedures such as gastric lavage and administration of activated charcoal may be considered if ingestion occurred within one hour. Specific monitoring of blood pressure and fluid and electrolyte balance may be required.

Therapeutic Uses of Ketazole

What Ketazole Treats: Main Uses and Benefits

Ketazole, which contains the antifungal agent ketoconazole, is relevant across three distinct therapeutic domains. It is applied in addressing the symptoms related to fungal or yeast growth and the associated discomfort, contributing to improved comfort and assisting in maintaining general well-being. The medicine is utilized across several therapeutic contexts.

The medication is commonly used to help with localized skin infections, including ringworm (tinea corporis), jock itch (tinea cruris), athlete's foot (tinea pedis), and Tinea versicolor. It also supports the management of recurrent scalp and skin conditions like dandruff and seborrheic dermatitis. In its specialized systemic use, it plays a role in managing serious illnesses such as blastomycosis and histoplasmosis, and conditions of hormone overproduction like endogenous Cushing's syndrome.

Quick Fact: Relief for Flaking and Scaly Symptoms

Ketazole is relevant when supportive symptom management is appropriate for conditions characterized by periods of heightened symptoms, generally helping to ease visible, disruptive manifestations like scaly rashes and persistent scalp flaking.

Eligibility and Restrictions for Use

Eligibility Map: Who Can and Cannot Use Ketazole

Official regulatory documentation establishes distinct eligibility rules for the systemic (oral tablet) and topical (cream, shampoo) forms of Ketazole (Ketoconazole).

Populations for whom use is contraindicated (Must Not Use):

  • Patients with acute or chronic liver disease or hepatic impairment (for the oral systemic formulation).
  • Patients with known hypersensitivity to Ketoconazole or any of its excipients (all formulations).
  • Pregnant women (for the oral systemic formulation) and women taking oral tablets who are breastfeeding.
  • Patients taking specific drugs that are strong CYP3A4 substrates, which can lead to QTc interval prolongation (for the oral systemic formulation).

Age-related eligibility rules:

  • The oral systemic formulation is not recommended for children under 12 years of age, as safety and efficacy have not been established.
  • Topical formulations are generally approved for adults and adolescents aged 12 years and over.

Eligibility-related restrictions:

  • The oral systemic formulation is not a first-line treatment and should only be used when alternative antifungal therapies are not available or not tolerated.
  • Use in older adults (geriatric) requires caution due to potential decreased organ function.

The regulatory profile strictly contraindicates the oral tablets for populations with compromised liver function or specific cardiovascular risk factors, and for pregnant or nursing women. For the topical formulations, eligibility is broader, primarily excluding those with a known hypersensitivity.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory documents establish specific interaction patterns for oral Ketazole (Ketoconazole), primarily due to its role as a potent inhibitor of the metabolic enzyme CYP3A4 and the transporter P-glycoprotein (P-gp). This dual inhibition significantly increases the plasma concentration (exposure) of many co-administered medicines, resulting in numerous restrictions.

Contraindicated Combinations

Co-administration is officially prohibited for a large number of substances, including certain drugs for heart rhythm (e.g., dofetilide, quinidine), cholesterol (e.g., simvastatin, lovastatin), and specific benzodiazepines (e.g., oral midazolam, triazolam). These prohibitions are due to the heightened risk of serious adverse outcomes, such as QT interval prolongation, rhabdomyolysis, or ergotism.

Administration Constraints

Ketazole absorption requires an acidic environment, necessitating a timing constraint when taken with acid-reducing agents. Aluminum-containing antacids must be administered at least 1 hour before or 2 hours after oral Ketazole. Certain strong enzyme-inducing agents, like rifampin, officially decrease the plasma concentration of Ketazole. Regulatory labels also mandate avoidance of alcohol due to increased hepatotoxicity risk and the potential for a disulfiram-like reaction.

Mechanism of Action

Fungal Ergosterol Biosynthesis Inhibition

Ketazole acts by engaging the sterol biosynthesis pathway within the fungal cell. It inhibits the fungal enzyme lanosterol 14alpha-demethylase (a cytochrome P450 enzyme, CYP51A1). This interference alters the conversion of lanosterol to ergosterol, a sterol required for the fungal cell membrane. The resulting depletion of ergosterol and the accumulation of intermediate sterols alters the membrane's fluidity and integrity. This mechanistic cascade leads to fungal cell destabilization and death.


Human Steroidogenesis Modulation

At higher systemic concentrations, Ketazole acts within the human endocrine pathways, exhibiting an affinity for certain mammalian cytochrome P450 enzymes involved in steroid hormone production. Specifically, it inhibits enzymes like 17alpha-hydroxylase and 17,20-lyase, which are required for the synthesis of cortisol and androgens. This inhibition results in altered concentrations of circulating steroid hormones.

Dosage and Administration Information

Ketazole is administered using two primary routes depending on the infection site: oral for systemic use and topical for localized cutaneous application. The oral tablet is generally indicated to be taken with food to ensure optimal absorption. The dosing schedule for systemic antifungal treatment typically begins at 200 mg once daily, and may be increased to 400 mg once daily, with a typical treatment duration of 6 months. Special care is required for co-administration with antacids containing aluminum, which must be administered at least 1 hour before or 2 hours after the tablet intake.

For the management of endogenous Cushing's syndrome, a specialized regimen is followed, starting at 400 to 600 mg daily in divided doses. This treatment is constrained by the need for supervision by a medical specialist, as the dosage is subject to individualized dose titration involving periodic 200 mg increments up to a maximum of 1200 mg/ day.

The topical preparations (cream, shampoo, foam, gel) have variable frequency patterns and duration. Treating seborrheic dermatitis often requires the 2% cream to be applied twice daily for a course of 4 weeks, while some tinea infections require only once daily application for 2 weeks. For pediatric patients at least 2 years of age requiring systemic treatment, the oral dosing rules are weight-based, calculated at 3.3 to 6.6 mg/ kg once daily.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Ketazole

Evidence for Topical Use in Skin and Scalp Fungal Infections

Research examined the topical use of Ketazole formulations in studies involving common skin and scalp conditions, including ringworm (tinea corporis), athlete’s foot (tinea pedis), tinea versicolor, and seborrheic dermatitis (dandruff). Research in this area primarily involves short-term Randomized Controlled Trials (RCTs) and comparative studies. Researchers monitored outcomes related to physical discomfort, such as itching and scaling, and used specific laboratory tests to measure the presence or eradication of the fungal organism.

Studies conducted during periods of increased symptom activity reported that a certain proportion of the observed populations achieved measurements consistent with the pre-defined study goal of mycological clearance. Findings also described patterns where the measured clinical severity scores for signs like redness and scaling showed change during the short-term study period. Research provides insight into short-term changes that were observed when exploring topical formulations for these conditions.

Research on Systemic Use in Deep-Seated Fungal Infections

Studies monitored the oral use of Ketazole in research involving patients with serious internal fungal illnesses, such as blastomycosis and histoplasmosis. Due to the severe nature and lower incidence of these conditions, the evidence base is primarily derived from observational cohorts, historical data, and case series. Studies monitored outcomes related to systemic or functional imbalance, specifically tracking clinical status and, in some settings, measurements related to fungal eradication.

Evidence Related to Endocrine Regulation (Cushing's Syndrome)

Ketazole was studied for its specialized role in managing endogenous Cushing's syndrome, a condition marked by temporary physiological imbalance (excess cortisol). This research primarily used small, prospective clinical trials and patient registries. Research highlights changes measured during the study period, reporting that measured decreases in cortisol levels were observed in a proportion of the studied patients. Findings help contextualize how the agent was studied in relation to this systemic imbalance.

What Research Gaps and Uncertainties Exist

Comparative evidence is lacking in current research that looks at Ketazole against the newest or preferred treatments for both superficial and systemic infections. Furthermore, long-term effects are not fully established for many outcomes, and the certainty remains low regarding sustained, years-long maintenance of symptom control for recurrent conditions. The evidence quality varies across studies, and data for certain groups remain insufficient, meaning that some questions remain to be explored. Findings describe group patterns, not personal outcomes, and evidence highlights what is known — and what is still uncertain.

Key Studies & References

  1. Treatment of Tinea Corporis and Tinea Cruris: A Systematic Review

Frequently Asked Questions (FAQ)

Common questions about Ketazole (FAQ)


Q: Why do official documents say Ketazole has a 'black box' warning?

The official prescribing information for the oral tablet includes a Boxed Warning. This warning is used to draw attention to risks of serious or sometimes fatal adverse effects. For Ketazole, this includes the risk of severe liver injury (hepatotoxicity) and the potential for serious heart rhythm problems that can result from dangerous drug interactions.


Q: Is Ketazole the same kind of drug as [Similar Drug Name]?

Ketazole belongs to the azole antifungal pharmacological class. Medicines within this class, such as fluconazole or itraconazole, share a similar mechanism of action against fungi. However, regulatory documents describe that each drug has its own specific indications (what it treats), available forms, and a distinct safety profile.


Q: What makes Ketazole different from other drugs that treat the same condition?

Official regulatory documents indicate that the oral systemic formulation of Ketazole is not a first-line treatment for fungal infections. Due to the documented risk of serious systemic side effects, its use is generally reserved for specific severe or life-threatening infections when alternative antifungal therapies are unavailable or not tolerated.


Q: Does Ketazole need to be taken long-term?

The required duration of treatment can vary widely depending on the condition. For some serious systemic fungal infections, treatment may last for several months. For the specialized use of managing Cushing's syndrome, treatment may be prolonged and is managed under the supervision of a medical specialist.


Q: Is it safe to use Ketazole with birth control pills?

Official information indicates that Ketazole is a strong inhibitor of the CYP3A4 enzyme, which processes many other medications, including hormonal contraceptives (birth control pills). This combination could potentially alter the levels of the contraceptive in the body. Detailed information can be reviewed in the official drug interaction sections.


Q: What happens if I miss a dose of Ketazole?

For topical preparations (like cream or shampoo), official guidelines generally describe a procedure where a missed dose is applied when remembered, unless it conflicts with the next dose, which may then require skipping the missed dose. Policies for the oral tablet may be different, and the goal remains to follow the prescribed schedule.


Q: Is Ketazole safe for older adults (seniors)?

Regulatory documents state that caution is required when prescribing the oral form for older adults. This is generally due to the greater likelihood of pre-existing conditions and the potential for reduced kidney, liver, or heart function, as well as the common use of other concurrent medications.


Q: What should a person do if they notice unusual side effects from Ketazole?

Official guidance highlights that patients taking the oral tablet should be aware of and report any signs or symptoms that may suggest liver problems. These symptoms include unusual fatigue, loss of appetite, vomiting, jaundice (yellowing of skin or eyes), or dark urine. Such reporting allows a healthcare professional to review the situation and determine if necessary testing is indicated.


Q: Can Ketazole be used by children?

For the oral tablet, official prescribing information states that safety and effectiveness have not been established in children under 12 years of age, and it is generally not recommended for this age group. Some topical formulations may have different age restrictions that permit use in adolescents or older children.


Q: How soon after stopping Ketazole does it completely leave the body?

The elimination of Ketazole from the body is described as biphasic, meaning it occurs in two distinct phases. The drug is extensively processed (metabolized) in the liver, and most of it is then excreted through the bile, with a smaller amount being excreted by the kidneys.


Q: Can men and women use Ketazole with the same expected outcome?

Official documents describe that Ketazole can influence hormone synthesis, particularly at higher systemic concentrations. Studies have reported that in men, the drug may cause a dose-related and reversible decrease in serum testosterone levels. The potential for different systemic impacts is recognized in official documents.


Q: Does Ketazole cause any changes in mood or anxiety levels?

The official side effect listings for the oral tablet include rare reports of psychiatric or nervous system disorders. These infrequent effects have been described as confusion, insomnia, nervousness, and paranoid delusions. Official documentation describes that the drug's influence on endocrine pathways may relate to some reported effects.


Q: Do people gain weight while taking Ketazole?

Official regulatory documents describe infrequent metabolic and endocrine effects, including changes in appetite and transient changes in lipid (fat) profiles. However, weight gain itself is not always explicitly listed as a common reported side effect of the oral tablet.


Q: Are there different strengths of Ketazole tablets available?

According to the official prescribing information for the systemic formulation, the Ketazole tablet is available as a 200 mg tablet.


Q: Why is Ketazole sometimes given in combination with another medicine?

Ketazole has been studied and used alongside other agents, particularly when managing complex conditions where the goal is to address temporary physiological imbalances. For example, it is sometimes used in specialized regimens related to the management of Cushing's syndrome.


Q: Does Ketazole work better if taken in the morning or at night?

Official instructions for the oral tablet mandate that it must be taken with food to ensure the best possible absorption into the body. While the dosing is typically once daily, specific timing (morning or night) is not universally mandated and is typically left to the discretion of the prescribing professional.


Q: Is Ketazole effective for mild cases of the condition, or just severe ones?

The oral tablet is explicitly indicated for use only in the case of severe or life-threatening systemic fungal infections where alternative treatments are unavailable or not tolerated. The topical forms (cream, shampoo), however, are used for common, localized, and superficial fungal conditions.


Q: Do researchers know exactly why Ketazole helps some people but not others?

Official research summaries and regulatory documents acknowledge that the evidence quality varies across available studies. Data for certain patient groups may remain insufficient, indicating that some open questions regarding variability in individual effectiveness still exist and require further exploration.


Q: Can people with kidney problems use Ketazole?

While the primary contraindication is for patients with acute or chronic liver disease, official documents on the drug's path through the body (pharmacokinetics) note that it is partially excreted by the kidneys. Official documents suggest that caution may be indicated in patients with decreased overall organ function, including renal (kidney) function.


Q: Is Ketazole the first drug tried for this condition?

The oral systemic formulation of Ketazole is explicitly not a first-line treatment. Its use is only considered when alternative, preferred antifungal therapies are either unavailable or have been shown to be not tolerated by the patient.


Q: Does Ketazole interact with herbal supplements like St. John's wort?

Official interaction sections list strong enzyme-inducing agents that can decrease the blood level of Ketazole. St. John’s wort is known to affect the same metabolic pathway (CYP3A4), and as this interaction could potentially reduce Ketazole's effectiveness, official guidance on drug interaction should be reviewed.


Q: Is the purpose of Ketazole mainly to treat symptoms or the underlying cause?

The fundamental purpose of Ketazole, as described in regulatory documents, is to resolve issues stemming from fungal proliferation by stopping the growth and survival of the causative microorganism. This classification means it acts on the underlying cause of the fungal infection rather than just addressing the symptoms.


Q: Does Ketazole affect fertility?

Due to its mechanism of influencing steroid hormone synthesis, the potential for an adverse effect on puberty and/or fertility must be carefully considered when long-term therapy is being discussed, particularly in children.


Q: How does taking Ketazole affect blood sugar levels?

Ketazole is known to affect human endocrine pathways and, at high doses, can inhibit the synthesis of certain hormones like cortisol. In some endocrine-related studies, rare reports of hypoglycemia (low blood sugar) have been described as a potential effect.


Q: Are there any long-term monitoring tests required while on Ketazole?

Yes, official safety constraints mandate frequent monitoring of liver function tests. These tests must be performed before starting treatment, at regular intervals during the initial weeks (e.g., at week 2 and week 4), and then typically monthly while the patient continues treatment to check for any adverse hepatic events.

How should Ketazole be stored and disposed of?

Official Storage and Disposal Requirements for Ketoconazole

Ketoconazole (Ketazole) must be stored under specific regulatory conditions to maintain stability, with requirements varying by product form (tablet, cream, shampoo, foam).

Mandatory Storage Conditions

Item Requirement
Temperature Store most forms at 20° to 25°C (68° to 77°F) (Controlled Room Temperature); Tablets at 15° to 30°C (59° to 86°F).
Protection Tablets must be protected from moisture and stored in a light-resistant container.
Child Safety All formulations must be stored out of the sight and reach of children.
Handling Flammable foam must not be exposed to heat and should be kept from freezing; fire/flame must be avoided during application.

Disposal: Unused or expired medicine must not be disposed of via wastewater or household waste. Patients should consult a pharmacist or healthcare professional for proper disposal according to local and national regulations.

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

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