Itraconazole

Aka: Itraconazole, Sporanox, Tolsura

II. Indications

  1. Onychomycosis

III. Metabolism

  1. Hepatic Cytochrome P450

IV. Preparations

  1. Intraconazole (standard formulation)
  2. Tolsura
    1. Higher bioavailable formulation (greater GI absorption) released in 2019
    2. Itraconazole 200 mg is equivalent to 130 mg Tolsura
    3. Indications
      1. Blastomycosis
      2. Histoplasmosis
      3. Aspergillosis
    4. Precautions
      1. Increased serum levels with acid suppression (e.g. Proton Pump Inhibitor)
      2. Five fold higher cost than Itraconazole ($70/day instead of $15/day)
    5. References
      1. (2019) Presc Lett 26(2): 9

V. 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)

VI. 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

VII. Dosing: Onychomycosis

  1. Fingernails
    1. Daily (continuous): 200 mg daily for 6 weeks
    2. Monthly (pulsed): 200 mg twice daily for one week/month for 2-3 months
  2. Toenails
    1. Daily (continuous): 200 mg daily for 12 weeks
    2. Monthly (pulsed): 200 mg twice daily for one week/month for 3-4 months

VIII. Dosing: Tinea Capitis

  1. Daily
    1. Solution 3 mg/kg/day up to 500 mg/day for 4-6 weeks
    2. Capsules 5 mg/kg/day up to 500 mg/day for 4-6 weeks
  2. Monthly
    1. Solution 3 mg/kg/day up to 500 mg/day, daily for one week per month for 2-3 months
    2. Capsules 5 mg/kg/day up to 500 mg/day, daily for one week per month for 2-3 months

IX. Directions

  1. Take with food (lower pH increases absorption)

X. Monitoring: Onychomycosis

  1. Pulse therapy: no monitoring
  2. Continuous therapy: Labs at baseline (previously also recommended every 6 weeks)
    1. Aspartate Aminotransferase (AST)
    2. Alanine Aminotransferase (ALT)

XI. References

  1. Boogaerts (2001) Drugs 61(Suppl I):39-47 [PubMed]
  2. De Beule (2001) Drugs 61(Suppl I):27-37 [PubMed]
  3. De Doncker (1997) J Am Acad Dermatol 37:969-74 [PubMed]
  4. Ely (2014) Am Fam Physician 90(10): 702-10 [PubMed]
  5. Friedlander (1999) Pediatr Infect Dis J 18(2):205-10 [PubMed]
  6. Gupta (1998) Int J Dermatol 37:303-8 [PubMed]
  7. Gupta (1999) J Am Acad Dermatol 41:237-49 [PubMed]
  8. Gupta (2001) Eur J Dermatol 11(1):6-10 [PubMed]

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Related Studies

Cost: Medications

itraconazole (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
ITRACONAZOLE 100 MG CAPSULE Generic $4.24 each
sporanox (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
SPORANOX 10 MG/ML SOLUTION $1.89 per ml
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Ontology: Itraconazole (C0064113)

Definition (MSH) A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.
Definition (NCI_NCI-GLOSS) A drug used to prevent or treat fungal infections. It belongs to the family of drugs called antifungal agents.
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 (CSP) orally active antimycotic; structurally related to ketoconazole.
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 Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D017964
SnomedCT 387532006, 96038009
LNC LP14995-2, MTHU002298
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], Oriconazole, (+-)-1-sec-Butyl-4-(p-(4-(p-(((2R*,4S*)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-1-piperazinyl)phenyl)-delta(sup 2)-1,2,4-triazolin-5-one, 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
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Sporanox (C0699614)

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

Related Topics in Pharmacology

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