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Wheeless' Textbook of Orthopaedics

Ketoconazole/Nizoral





- For treatment of systemic fungal infections; Candidiasis, chronic
    mucocutaneous candidiasis, oral thrush, Blastomycosis,
    coccidioidomycosis, histoplasmosis, and paracoccidioidomycosis;
- topical cream for localized fungal infections due to dermatophytes & yeast;
- Adult: 200mg PO qd; increase to 400mg PO qd for very serious infections;
- Associated with severe hepatotoxicity; monitor LFT's closely throughout
    course of therapy;
- Drug interaction with any agent increasing gastric pH preventing
    absorption of ketoconazole;
- Note that ketoconazole requires gastric acidity for absorption
    (if patient is receiving H2 blockers, antacids, or anticholinergics,
    they should be administered at least 2hrs after Ketoconazole
    administration);
- may enhance effects of oral anticoagulants;
- may react with alcohol to produce disulfiram like reaction;
- Contraindicated with: fungal meningitis (poor CNS penetration);
- Use with caution in patients with a h/o liver dz, patients receiving
    warfarin like drugs (increased prothrombintime), cyclosporin A
    (increased serum level), phenytoin (altered metabolism), oral
    hypoglycemic agents (increased risked hypoglycemia), rifampin (
    decreased serum level);
- Diffusion from Blood into CSF minimal even w/ Inflammation even with high
    dose >800mg/dl;
- Dosing Regimens for Patients with Renal Insufficiency: (Dose for 70 kg
    Adult {gm / dosing interval inhours}): CrCl:>80:0.2-0.4/12-24;
    CrCl:50-79:0.2-0.4/12-24; CrCl:30-49:0.2-0.4/12-24;
    CrCl:10-29:0.2-0.4/12-24;
    - 10% of drug will be excreted in to urine (w/ nl RF(x))
- Peds: >2yrs: 3.3-6.6 mg/kg/day as a single dose;
- Supplied: Tabs: 200 mg; topical cream 2%;
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Original Text by Clifford R. Wheeless, III, MD.