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Itraconazole

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Itraconazole, Sporanox, Tolsura

  • Indications
  1. Onychomycosis
  • Metabolism
  1. Hepatic Cytochrome P450
  • 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
  • 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)
  • 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
  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
  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
  • Directions
  1. Take with food (lower pH increases absorption)
  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)
  • 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]