ketoconazole (Rx)

Brand and Other Names:Nizoral
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 200mg

Fungal Infections

Indicated for the treatment of the following systemic fungal infections in patients who have failed or who are intolerant to other therapies: blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis

200-400 mg/day PO

Dosage Modifications

Renal impairment: No dosage modifications provided in manufacturer’s labeling

Hepatic impairment

  • No dosage modifications provided in manufacturer’s labeling
  • If hepatotoxicity occurs during treatment (ALT levels above UNL or ALT 30% above baseline): Interrupt dosing and order a full set of liver tests

Dosing Considerations

Do not use tablets as first-line treatment; should be used only when other effective antifungal therapy is not available or tolerated and the potential benefits are considered to outweigh the potential of hepatotoxicity

Avoid prescribing tablets to treat skin and nail fungal infections owing to risk of serious liver damage, adrenal gland problems, and harmful interactions with other medicines that outweigh its benefit in treating these conditions, which are not approved uses of the drug (these indications were removed from labeling by the FDA in 2013)

Do not use for fungal meningitis because of poor penetration into the CSF

Cushing Syndrome (Off-label)

Used off-label to inhibit steroidogenesis in patients with Cushing syndrome

600-800 mg/day PO

Used rarely and often toxic at doses required to reduce cortisol secretion

Recurrent Tinea Versicolor (Off-label)

400 mg PO monthly

Dosage Forms & Strengths

tablet

  • 200mg

Fungal Infections

Indicated for the treatment of the following systemic fungal infections in patients who have failed or who are intolerant to other therapies: blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis

<2 years old: Safety and efficacy not established

≥2 years old: 3.3-6.6 mg/kg/day PO  

Dosage Modifications

Renal impairment: No dosage modifications provided in manufacturer’s labeling

Hepatic impairment

  • No dosage modifications provided in manufacturer’s labeling
  • If hepatotoxicity occurs during treatment (ALT levels above UNL or ALT 30% above baseline): Interrupt dosing and order a full set of liver tests

Dosing Considerations

Do not use tablets as first-line treatment; should be used only when other effective antifungal therapy is not available or tolerated and the potential benefits are considered to outweigh the potential of hepatotoxicity

Avoid prescribing tablets to treat skin and nail fungal infections owing to risk of serious liver damage, adrenal gland problems, and harmful interactions with other medicines that outweigh its benefit in treating these conditions, which are not approved uses of the drug (these indications were removed from labeling by the FDA in 2013)

Do not use for fungal meningitis because of poor penetration into the CSF

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Interactions

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            Adverse Effects

            1-10%

            Nausea and vomiting (3-10%)

            Pruritus (2%)

            Abdominal pain (1%)

            <1%

            Alopecia

            Headache

            Dizziness

            Hyperlipidemia

            Somnolence

            Fever

            Chills

            Bulging fontanelles

            Depression

            Gynecomastia

            Diarrhea

            Impotence

            Thrombocytopenia

            Leukopenia

            Hemolytic anemia

            Erythema multiforme

            Orthostatic hypotension

            Jaundice

            Dyspepsia

            Dysgeusia

            Hepatotoxicity

            Decreased platelet count

            Xeroderma

            Photophobia

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            Warnings

            Black Box Warnings

            Tablets should be used only when other effective antifungal therapy is not available or tolerated and the potential benefits are considered to outweigh the potential risks

            Hepatotoxicity has occurred with oral use, including some fatalities or requiring liver transplantation; reported with oral administration of drug; some patients had no obvious risk factors for liver disease

            May cause QT prolongation; coadministration with dofetilide, quinidine, pimozide, cisapride, methadone, disopyramide, dronedarone, and ranolazine is contraindicated; ketoconazole can cause elevated plasma concentrations of these drugs (by CYP3A4 inhibition) and may prolong QT intervals, sometimes resulting in life-threatening ventricular dysrhythmias such as torsades de pointes

            Contraindications

            Hypersensitivity

            Contraindicated with dofetilide, quinidine, pimozide, cisapride, methadone, disopyramide, dronedarone, and ranolazine; can cause elevated plasma concentrations of these drugs and may prolong QT intervals, sometimes resulting in life-threatening ventricular dysrhythmias (eg, torsades de pointes)

            Concurrent therapy with cisapride, ergot derivatives, or triazolam (fatal cardiac arrhythmias may occur)

            Acute or chronic liver disease

            CYP3A4 metabolized HMG-CoA reductase inhibitors (eg, simvastatin, lovastatin); ketoconazole inhibits CYP3A4 and may increase risk of myopathy associated with statins

            Cautions

            Do not use tablets as first-line treatment; should be used only when other effective antifungal therapy is not available or tolerated and the potential benefits are considered to outweigh the potential of hepatotoxicity (see Black Box Warnings)

            Avoid prescribing tablets to treat skin and nail fungal infections owing to risk of serious liver damage, adrenal gland problems, and harmful interactions with other medicines that outweigh its benefit in treating these conditions, which are not approved uses of the drug (these indications were removed from labeling by the FDA in 2013)

            Use catuion in patients with hypersensitivity to other azoles

            Increased long bone fragility reported with high dose in animal studies; choose dose carefully in patients susceptible to bone fragility, including the elderly and postmenopausal women

            Absorption reduced in patients with achlorhydria, avoid coadministration with drugs that decrease gastric acidity

            Not for the treatment of fungal meningitis; has poor penetration into cerebral spinal fluid

            Hepatotoxicity reported, including fatalities or liver transplantation (see Black Box Warnings)

            Ketoconazole decreases metabolism of midazolam PO, triazolam PO, or alprazolam and may result in prolonged hypnotic and sedative effects

            Coadministration of CYP3A4 metabolized HMG-CoA reductase inhibitors (eg, simvastatin, lovastatin) increases risk for myopathy (see Contraindications)

            Potential for gynecomastia (drug has antiandrogenic activity)

            Adrenal insufficiency

            • Decreases adrenal corticosteroid secretion at doses ≥400 mg
            • This effect is not shared with other azoles
            • Do not exceed recommended dose of 200-400 mg/day
            • Monitor adrenal function in patients with adrenal insufficiency or with borderline adrenal function, and in patients under prolonged periods of stress (eg, major surgery, intensive care)
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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Drug enters breast milk

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Inhibits cytochrome P450-dependent synthesis of ergosterol, which in turn inhibits cell-membrane formation

            Cushing syndrome (off-label): Inhibition of P450 enzymes includes the first step in cortisol synthesis, cholesterol side-chain cleavage, and conversion of 11-deoxycortisol to cortisol

            Absorption

            Rapid (~75%)

            Bioavailability: Decreases as gastric pH increases

            Peak plasma time: 1-2 hr

            Distribution

            Well distributed into inflamed joint fluid, saliva, bile, urine, breast milk, sebum, cerumen, feces, tendons, skin and soft tissue, testes; crosses blood-brain barrier poorly, with only negligible amounts reaching CSF

            Protein bound: 93-96%

            Metabolism

            Partially metabolized in liver via CYP3A4 to inactive compounds

            Elimination

            Half-life: Biphasic: initial, 2 hr; terminal, 8 hr

            Excretion: Feces (57%), urine (13%)

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Nizoral A-D topical
            -
            1 % shampoo
            Xolegel topical
            -
            2 % gel
            Ketodan topical
            -
            2 % foam
            ketoconazole oral
            -
            200 mg tablet
            ketoconazole oral
            -
            200 mg tablet
            ketoconazole oral
            -
            200 mg tablet
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % shampoo
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % foam
            ketoconazole topical
            -
            2 % foam
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % cream
            ketoconazole topical
            -
            2 % shampoo
            ketoconazole topical
            -
            2 % foam
            ketoconazole topical
            -
            2 % foam
            ketoconazole topical
            -
            2 % cream

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Select a drug:
            Patient Education
            ketoconazole oral

            KETOCONAZOLE - ORAL

            (kee-toe-CON-uh-zole)

            COMMON BRAND NAME(S): Nizoral

            WARNING: Ketoconazole can cause serious (possibly fatal) side effects and drug interactions. It should only be used when other treatments have not worked, are not available, or cannot be taken by you. Discuss the risks and benefits of this medication, as well as other effective and possibly safer treatments for fungal infections, with your doctor.Ketoconazole has rarely caused very serious (possibly fatal) liver problems. Get medical help right away if you develop symptoms of liver problems, including nausea/vomiting that doesn't stop, stomach/abdominal pain, dark urine, yellowing eyes/skin, loss of appetite, or light colored stools. To reduce your risk for liver problems, your doctor should obtain liver function tests every week while you are taking this medication. Do not drink alcoholic beverages while taking ketoconazole because alcohol increases the risk of serious liver problems. See also Notes section.Ketoconazole must not be used with certain other medications because a serious, possibly fatal, drug interaction may occur. Ketoconazole interacts with drugs such as disopyramide, dofetilide, dronedarone, methadone, pimozide, quinidine, ranolazine, among others. These interactions may increase the risk of a certain condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away. Tell your doctor and pharmacist about all the medications and products you may be taking before you start ketoconazole treatment. See also Precautions section.

            USES: See also Warning section.Ketoconazole is used to treat certain serious fungal infections in the body. Ketoconazole belongs to the class of drugs called azole antifungals. It works by stopping the growth of the fungus.Ketoconazole should not be used to treat fungal infections on the skin and nails due to the risk of serious side effects and drug interactions. Talk to your doctor about other medications you can use to treat these types of infection.

            HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking ketoconazole and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth as directed by your doctor, usually once a day. This medication may be taken with or without food, but taking it with food helps to reduce stomach upset.If you are taking an antacid, take ketoconazole at least 2 hours before or 1 hour after taking the antacid, otherwise ketoconazole may not be absorbed into the body. See also Drug Interactions for more information.The dosage and length of treatment is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). In children, the dosage is also based on weight. It may take from several days to several months to complete treatment.This medication works best when the amount of medicine in your body is kept at a constant level. Take this drug at evenly spaced intervals. To help you remember, take it at the same time each day.Continue to take this medication until the full prescribed amount is finished, even if symptoms disappear after a few days. Stopping the medication too early may result in a return of the infection.Tell your doctor if your condition lasts or gets worse.

            SIDE EFFECTS: See also Warning section.Nausea and vomiting may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: headache, vision changes, mental/mood changes (such as depression, thoughts of suicide).Although unlikely, when ketoconazole is used at high doses, it may cause an adrenal gland problem (adrenal insufficiency), a decrease in testosterone levels, and a decrease in sperm production. Ketoconazole can also worsen existing adrenal gland function problems (See also Precautions section). The adrenal gland problem may make it more difficult for your body to respond to physical stress. Before having surgery or emergency treatment, or if you get a serious illness/injury, tell your doctor or dentist that you are using this medication. Your doctor may order a blood test to monitor your adrenal gland function while you are taking ketoconazole. These effects usually go away after ketoconazole treatment is stopped. Tell your doctor right away if you have any serious side effects, including: unusual tiredness, weakness, dizziness upon standing, diarrhea, weight loss, menstrual period changes, decreased sexual interest or ability, enlarged/tender breasts in men.Get medical help right away if you have any very serious side effects, including: fast/irregular heartbeat, severe dizziness, fainting.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: See also Side Effects section.Before taking ketoconazole, tell your doctor or pharmacist if you are allergic to it; or to levoketoconazole; or to other azole antifungal drugs (such as fluconazole, itraconazole); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver problems, alcohol use, low testosterone levels, decreased adrenal gland function problems (such as low cortisol levels, Addison's disease, adrenal insufficiency), little or no stomach acid production (achlorhydria).Ketoconazole may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using ketoconazole, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using ketoconazole safely.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Do not drink alcoholic beverages while taking this medication because alcohol increases the risk of serious liver problems. Avoiding alcoholic beverages will also decrease the risk of a rare reaction with ketoconazole that may result in flushing, headache, and nausea.Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.This medication passes into breast milk. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: See also Warning and How to Use sections.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Ketoconazole interacts with many prescription and nonprescription drugs. While you are taking ketoconazole, it is very important to tell your doctor or pharmacist of any changes in medications that you are taking.Some products that may interact with this drug include: other drugs that can cause liver problems (such as acetaminophen).Other medications can affect the removal of ketoconazole from your body, which may affect how ketoconazole works. Examples include isoniazid, nevirapine, rifamycins (such as rifabutin, rifampin), St. John's wort, among others.This medication can slow down the removal of many other medications from your body, which may affect how they work. Examples of affected drugs include some benzodiazepines (such as alprazolam, midazolam, triazolam), domperidone, eletriptan, eplerenone, ergot drugs (such as ergotamine), nisoldipine, drugs used to treat erectile dysfunction-ED or pulmonary hypertension (such as sildenafil, tadalafil), some drugs used to treat seizures (such as phenytoin), some statin drugs (such as lovastatin, simvastatin), among others.Ketoconazole requires acid in the stomach to be well absorbed. If you are taking drugs that decrease the amount of stomach acid including antacids, heartburn/ulcer drugs (H2 blockers such as cimetidine, famotidine, ranitidine), sucralfate, or if you are taking drugs that slow down gut movement (anticholinergics such as dicyclomine, propantheline), take ketoconazole at least 2 hours before any of these drugs. If you are taking proton pump inhibitors (PPIs such as lansoprazole, omeprazole), ask your doctor or pharmacist for advice on how to reduce or avoid this interaction.Ketoconazole is very similar to levoketoconazole. Do not use medications containing levoketoconazole while using ketoconazole.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: Do not share this medication with others.This medication has been prescribed for your current condition only. Do not use it later for another infection unless your doctor tells you to.Lab and/or medical tests (such as liver function, INR) must be done before you start taking this medication and while you are taking it. Keep all medical and lab appointments. Consult your doctor for more details.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            Information last revised December 2022. Copyright(c) 2022 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.