I. See Also

  1. Imidazole
  2. Topical Antifungal

II. Precautions

  1. Hepatotoxicity risk (FDA black box warning)
    1. Oral forumulation indicated only for severe, refractory systemic fungal infections due to Ketoconazole hepatotoxicity
    2. No longer indicated in Skin Infections
    3. If Ketoconazole is used, requires Liver Function Tests at baseline and again weekly

III. Adverse Effects: Oral (systemic formulation)

IV. Drug Interactions: Oral (systemic formulation)

  1. Serious cardiac arrhythmia with Hismanal or Seldane (off market in U.S.)
  2. Multiple other drug interactions
    1. CYP2C9 Inhibitor
    2. CYP3A3 Inhibitor and CYP3A4 Inhibitor

V. Lab monitoring: Oral (systemic formulation)

  1. Follow Liver Function Tests at baseline and weekly

VI. Directions

  1. Taking with food decreases gastric irritation

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Cost: Medications

ketoconazole (on 1/21/2015 at Medicaid.Gov Survey of pharmacy drug pricing)
KETOCONAZOLE 2% CREAM Generic $0.98 per gram
KETOCONAZOLE 2% SHAMPOO Generic $0.07 per ml
KETOCONAZOLE 200 MG TABLET Generic $1.66 each
nizoral (on 1/6/2015 at Medicaid.Gov Survey of pharmacy drug pricing)
NIZORAL 2% SHAMPOO Generic $0.07 per ml

Ontology: Ketoconazole (C0022625)

Definition (NCI_NCI-GLOSS) A drug that treats infection caused by a fungus. It is also used as a treatment for prostate cancer because it can block the production of male sex hormones.
Definition (NCI) A synthetic derivative of phenylpiperazine with broad antifungal properties and potential antineoplastic activity. Ketoconazole inhibits sterol 14-a-dimethylase, a microsomal cytochrome P450-dependent enzyme, thereby disrupting synthesis of ergosterol, an important component of the fungal cell wall. (NCI04)
Definition (MSH) Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients.
Definition (CSP) 1-acetyl-4-(2,4-dichlorophenyl-2-imidazolylmethyl- 1,3- dioxolanylmethoxyphenyl) piperazine; broad spectrum, oral antifungal.
Definition (PDQ) A synthetic derivative of phenylpiperazine with broad antifungal properties and potential antineoplastic activity. Ketoconazole inhibits sterol 14-a-dimethylase, a microsomal cytochrome P450-dependent enzyme, thereby disrupting synthesis of ergosterol, an important component of the fungal cell wall. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39488&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39488&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C605" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D007654
SnomedCT 326240002, 332902002, 324673001, 387216007, 40232005
LNC LP15862-3, MTHU002299
English Ketoconazole, Piperazine, 1-acetyl-4-(4-((2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-, cis-, Ketoconazole [gyn], Ketoconazole [infections], Ketoconazole [skin], Cis-1-Acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazole-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazine, ketoconazole, Ketoconazole [gynaecological use], Ketoconazole [gynecological use], ketoconazole (medication), KETOCONAZOLE, Ketoconazole [Chemical/Ingredient], Ketoconazole [skin] (product), Ketoconazole [infections] (product), Ketoconazole [gynecological use] (product), Ketoconazole (product), Ketoconazole (substance), KCZ, Ketoconazole [gynecological use] (substance), Ketoconazole [infections] (substance), Ketoconazole [skin] (substance)
Swedish Ketokonazol
Spanish ketoconazol [infecciones], ketoconazol (piel), Cetoconazol, cetoconazol (uso dermatológico), ketoconazol [antiinfeccioso], ketoconazol [antiinfeccioso] (producto), ketoconazol (uso dermatológico) (producto), cetoconazol [uso ginecológico], ketoconazol (uso dermatológico), cetoconazol (uso dermatológico) (producto), ketoconazol [uso ginecológico] (producto), ketoconazol [uso ginecológico], cetoconazol [antiinfeccioso], Ketoconazol, cetoconazol (producto), cetoconazol (sustancia), cetoconazol, ketoconazol (piel) (producto), ketoconazol (producto), ketoconazol (sustancia), ketoconazol [infecciones] (producto), ketoconazol
Czech ketokonazol
Finnish Ketokonatsoli
Russian KETOKONAZOL, КЕТОКОНАЗОЛ
Japanese ケトコナゾール, ニゾラール, ニトラゼン, ケトパミン, プルナ
Croatian KETOKONAZOL
Polish Ketokonazol
Portuguese Cetoconazol, Ketoconazol
French Kétoconazole
German Ketoconazol
Italian Ketoconazolo

Ontology: Nizoral (C0699439)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D007654
English Janssen Brand of Ketoconazole, Ketoconazole Janssen Brand, nizoral, Nizoral