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

Images: Related links to external sites (from Google)

Cost: Medications

Ketoconazole (on 2/9/2012 at DrugStore.com)
Ketoconazole 2% Shampoo 120ml Bottle #1 for $27.99 ($27.99/unit)
Ketoconazole 2% Foam 50gm Can #1 for $175.99 ($175.99/unit)
Ketoconazole 2% Foam 100gm Can #1 for $326.00 ($326.00/unit)
Ketoconazole 2% Cream 15gm Tube #1 for $19.99 ($19.99/unit)
Ketoconazole 2% Cream 30gm Tube #1 for $26.99 ($26.99/unit)
Ketoconazole 2% Cream 60gm Tube #1 for $35.99 ($35.99/unit)
Ketoconazole 200mg Tablets #14 for $30.99 ($2.21/unit)
Nizoral (on 2/9/2012 at DrugStore.com)
Nizoral 200mg Tablets #30 for $129.99 ($4.33/unit)
Nizoral 2% Shampoo 120ml Bottle #1 for $53.99 ($53.99/unit)

Ontology: Ketoconazole (C0022625)

Definition (MSH) Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients.
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 (CSP) 1-acetyl-4-(2,4-dichlorophenyl-2-imidazolylmethyl- 1,3- dioxolanylmethoxyphenyl) piperazine; broad spectrum, oral antifungal.
Definition (NCI) 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 (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 Organic Chemical (T109) , Pharmacologic Substance(T121)
MSH D007654
SnomedCT 332902002, 324673001, 326240002, 387216007, 40232005
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 [infections] (product), Ketoconazole [skin] (product), Ketoconazole [gynecological use] (product), ketoconazole (medication), KETOCONAZOLE, Ketoconazole [Chemical/Ingredient], Ketoconazole (product), Ketoconazole (substance), KCZ, Ketoconazole [gynecological use] (substance), Ketoconazole [infections] (substance), Ketoconazole [skin] (substance)
Swedish Ketokonazol
Spanish ketoconazol [infecciones], ketoconazol (piel), cetoconazol (uso dermatológico) (producto), ketoconazol [antiinfeccioso] (producto), ketoconazol [uso ginecológico], ketoconazol [uso ginecológico] (producto), ketoconazol [antiinfeccioso], cetoconazol [antiinfeccioso], ketoconazol (uso dermatológico) (producto), cetoconazol (uso dermatológico), ketoconazol (uso dermatológico), cetoconazol [uso ginecológico], cetoconazol (producto), cetoconazol (sustancia), cetoconazol, ketoconazol (piel) (producto), ketoconazol (producto), ketoconazol (sustancia), ketoconazol [infecciones] (producto), ketoconazol, 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
French Kétoconazole
German Ketoconazol
Italian Ketoconazolo
Portuguese Ketoconazol

Ontology: Nizoral (C0699439)

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