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ketoconazole (Rx)Brand and Other Names:Nizoral

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 200mg
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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
more...

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

Interaction Checker

ketoconazole and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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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)

            Hypersensitivity to other azoles

            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

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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