itraconazole
E850011
Itraconazole is a triazole antifungal medication commonly used to treat systemic and superficial fungal infections and known for significant drug–drug interactions via CYP3A4 inhibition.
Statements (65)
| Predicate | Object |
|---|---|
| instanceOf |
azole antifungal
ⓘ
systemic antifungal agent ⓘ triazole antifungal drug ⓘ |
| accumulatesIn |
keratinous tissues
ⓘ
nails ⓘ skin ⓘ |
| approvedBy | U.S. Food and Drug Administration NERFINISHED ⓘ |
| availableAs |
capsules
ⓘ
intravenous formulation ⓘ oral solution ⓘ |
| belongsTo | World Health Organization Model List of Essential Medicines NERFINISHED ⓘ |
| boxedWarningIncludes | coadministration with certain CYP3A4-metabolized drugs can cause QT prolongation ⓘ |
| canCause |
congestive heart failure exacerbation
ⓘ
hepatotoxicity ⓘ |
| canProlong | QT interval when combined with susceptible drugs ⓘ |
| contraindicatedIn | patients with ventricular dysfunction or heart failure ⓘ |
| discoveredBy | Janssen Pharmaceutica NERFINISHED ⓘ |
| eliminatedVia |
bile
ⓘ
feces ⓘ |
| hasActiveMetabolite | hydroxy-itraconazole ⓘ |
| hasATCCode | J02AC02 ⓘ |
| hasBioavailability | variable and formulation-dependent ⓘ |
| hasBlackBoxWarning | risk of congestive heart failure ⓘ |
| hasBrandName | Sporanox NERFINISHED ⓘ |
| hasChemicalClass | triazole ⓘ |
| hasCommonAdverseEffect |
abdominal pain
ⓘ
diarrhea ⓘ elevated liver enzymes ⓘ headache ⓘ nausea ⓘ vomiting ⓘ |
| hasHalfLife | approximately 24–42 hours in adults ⓘ |
| hasMechanismOfAction | inhibition of fungal lanosterol 14α-demethylase ⓘ |
| hasMolecularFormula | C35H38Cl2N8O4 ⓘ |
| hasPharmacologicalEffect |
fungicidal activity at high concentrations
ⓘ
fungistatic activity ⓘ |
| hasPregnancyCategory | C (systemic use; varies by jurisdiction) ⓘ |
| hasRouteOfAdministration | oral ⓘ |
| hasSignificantDrugInteractionVia | CYP3A4 inhibition ⓘ |
| increasesPlasmaLevelsOf | many CYP3A4 substrates ⓘ |
| inhibits | CYP3A4 ⓘ |
| isHighlyProteinBound | true ⓘ |
| isInhibitorOf | P-glycoprotein NERFINISHED ⓘ |
| isLipophilic | true ⓘ |
| isSubstrateOf | CYP3A4 NERFINISHED ⓘ |
| isTeratogenicIn | animal studies ⓘ |
| metabolizedIn | liver ⓘ |
| requires | gastric acidity for optimal absorption of capsule formulation ⓘ |
| shouldBeUsedWithCautionIn |
hepatic impairment
ⓘ
renal impairment ⓘ |
| targets | fungal cytochrome P450 14α-demethylase (CYP51) ⓘ |
| usedFor |
aspergillosis
ⓘ
blastomycosis ⓘ dermatophytosis ⓘ esophageal candidiasis ⓘ histoplasmosis ⓘ onychomycosis ⓘ oral candidiasis ⓘ pityriasis versicolor ⓘ sporotrichosis ⓘ superficial fungal infections ⓘ systemic fungal infections ⓘ tinea corporis ⓘ tinea cruris ⓘ tinea pedis ⓘ |
Referenced by (1)
Full triples — surface form annotated when it differs from this entity's canonical label.