II. Indications
III. Metabolism
- Hepatic cytochrome P450
IV. Preparations
- Intraconazole (standard formulation)
- Tolsura
- Higher bioavailable formulation (greater GI absorption) released in 2019
- Itraconazole 200 mg is equivalent to 130 mg Tolsura
- Indications
- Precautions
- Increased serum levels with acid suppression (e.g. Proton Pump Inhibitor)
- Five fold higher cost than Itraconazole ($70/day instead of $15/day)
- References
- (2019) Presc Lett 26(2): 9
V. Drug Interactions: Serious (Contraindicated)
- Serious arrhythmia with
- Astemizole
- Cisapride
- Quinidine
- Pimozide (Orap)
- Rhabdomyolysis Risk
- Significant sedation with Benzodiazepines
- Midazolam (Versed)
- Triazolam (Halcion)
- Avoid other Benzodiazepines also
- Avoid barbiturates (e.g. Phenobarbital)
VI. Drug Interactions: Other
- Medications raising gastric pH and lowering absorption
- H2 Blockers (e.g. Ranitidine)
- Proton Pump Inhibitors (e.g. Omeprazole)
-
Oral Hypoglycemics (e.g. Sulfonylureas)
- Risk of Hypoglycemia
- Increased bleeding risk with Warfarin
VII. Dosing: Onychomycosis
-
Fingernails
- Daily (continuous): 200 mg daily for 6 weeks
- Monthly (pulsed): 200 mg twice daily for one week/month for 2-3 months
-
Toenails
- Daily (continuous): 200 mg daily for 12 weeks
- Monthly (pulsed): 200 mg twice daily for one week/month for 3-4 months
VIII. Dosing: Tinea Capitis
- Daily
- Solution 3 mg/kg/day up to 500 mg/day for 4-6 weeks
- Capsules 5 mg/kg/day up to 500 mg/day for 4-6 weeks
- Monthly
- Solution 3 mg/kg/day up to 500 mg/day, daily for one week per month for 2-3 months
- Capsules 5 mg/kg/day up to 500 mg/day, daily for one week per month for 2-3 months
IX. Directions
- Take with food (lower pH increases absorption)
X. Monitoring: Onychomycosis
- Pulse therapy: no monitoring
- Continuous therapy: Labs at baseline (previously also recommended every 6 weeks)
XI. References
- Boogaerts (2001) Drugs 61(Suppl I):39-47 [PubMed]
- De Beule (2001) Drugs 61(Suppl I):27-37 [PubMed]
- De Doncker (1997) J Am Acad Dermatol 37:969-74 [PubMed]
- Ely (2014) Am Fam Physician 90(10): 702-10 [PubMed]
- Friedlander (1999) Pediatr Infect Dis J 18(2):205-10 [PubMed]
- Gupta (1998) Int J Dermatol 37:303-8 [PubMed]
- Gupta (1999) J Am Acad Dermatol 41:237-49 [PubMed]
- Gupta (2001) Eur J Dermatol 11(1):6-10 [PubMed]
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Related Studies (from Trip Database) Open in New Window
| 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 | |
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 |
Ontology: Sporanox (C0699614)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D017964 |
| English | Janssen Brand of Itraconazole, Itraconazole Janssen Brand, sporanox, Sporanox |
