Infectious Disease Book

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Itraconazole

Aka: Itraconazole, Sporanox
  1. Indications
    1. Onychomycosis
  2. Metabolism
    1. Hepatic cytochrome P450
  3. Drug Interactions: Serious (Contraindicated)
    1. Serious arrhythmia with
      1. Astemizole
      2. Cisapride
      3. Quinidine
      4. Pimozide (Orap)
    2. Rhabdomyolysis Risk
      1. HMG-CoA Reductase Inhibitors (e.g. Simvastatin)
    3. Significant Sedation with Benzodiazepines
      1. Midazolam (Versed)
      2. Triazolam (Halcion)
      3. Avoid other Benzodiazepines also
      4. Avoid barbiturates (e.g. Phenobarbital)
  4. Drug Interactions: Other
    1. Medications raising gastric pH and lowering absorption
      1. H2 Blockers (e.g. Ranitidine)
      2. Proton Pump Inhibitors (e.g. Omeprazole)
    2. Oral Hypoglycemics (e.g. Sulfonylureas)
      1. Risk of Hypoglycemia
    3. Increased bleeding risk with Warfarin
  5. Dosing: Onychomycosis
    1. Continuous Therapy Dosing (Adult)
      1. Fingernail: 200 mg PO qd for 6 weeks
      2. Toenail: 200 mg PO qd for 3 months
    2. Pulse Therapy (Adult dosing)
      1. 200 mg PO bid for 1 week per month
      2. Course
        1. Fingernail: 2-3 months
        2. Toenail: 3-4 months
  6. Cost
    1. Twelve week supply: $900
  7. Directions
    1. Take with food (lower pH increases absorption)
  8. Monitoring: Onychomycosis
    1. Pulse therapy: no monitoring
    2. Continuous therapy at baseline and every 4 to 6 weeks
      1. Aspartate Aminotransferase (AST)
      2. Alanine Aminotransferase (ALT)
  9. References
    1. Boogaerts (2001) Drugs 61(Suppl I):39-47
    2. De Beule (2001) Drugs 61(Suppl I):27-37
    3. De Doncker (1997) J Am Acad Dermatol 37:969-74
    4. Friedlander (1999) Pediatr Infect Dis J 18(2):205-10
    5. Gupta (1998) Int J Dermatol 37:303-8
    6. Gupta (1999) J Am Acad Dermatol 41:237-49
    7. Gupta (2001) Eur J Dermatol 11(1):6-10

Itraconazole (C0064113)

Definition (MSH) A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.
Definition (CSP) orally active antimycotic; structurally related to ketoconazole.
Definition (NCI) A synthetic triazole agent with antimycotic properties. Formulated for both topical and systemic use, itraconazole preferentially inhibits fugal cytochrome P450 enzymes, resulting in a decrease in fungal ergosterol synthesis. Because of its low toxicity profile, this agent can be used for long-term maintenance treatment of chronic fungal infections. (NCI04)
Definition (NCI) A drug used to prevent or treat fungal infections. It belongs to the family of drugs called antifungal agents.
Definition (PDQ) A synthetic triazole agent with antimycotic properties. Formulated for both topical and systemic use, itraconazole preferentially inhibits fugal cytochrome P450 enzymes, resulting in a decrease in fungal ergosterol synthesis. Because of its low toxicity profile, this agent can be used for long-term maintenance treatment of chronic fungal infections. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39106&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39106&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1138" NCI Thesaurus)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D017964
SnomedCT 387532006, 96038009
English Itraconazole, 3H-1,2,4-Triazol-3-one, 4-(4-(4-(4-((2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-1-piperazinyl)phenyl)-2,4-dihydro-2-(1-methylpropyl)-, itraconazole, itraconazole (medication), ITRACONAZOLE, Itraconazole [Chemical/Ingredient], Itraconazole (product), Itraconazole (substance), ICZ
Swedish Itrakonazol
Czech itrakonazol
Finnish Itrakonatsoli
Russian ITRAKONAZOL, ИТРАКОНАЗОЛ
Japanese イトリゾール, イトラコナゾール
Polish Itrakonazol
Spanish itraconazol (producto), itraconazol (sustancia), itraconazol, Itraconazol
French Itraconazole
German Itraconazol
Italian Itraconazolo
Portuguese Itraconazol
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Sporanox (C0699614)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D017964
English Janssen Brand of Itraconazole, Itraconazole Janssen Brand, sporanox, Sporanox
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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