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.

All labels observed (2)

Label Occurrences
Sporanox 1
itraconazole canonical 1

How this entity was disambiguated

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 ⓘ
availableAs capsules ⓘ
intravenous formulation ⓘ
oral solution ⓘ
belongsTo World Health Organization Model List of Essential Medicines ⓘ
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 ⓘ
eliminatedVia bile ⓘ
feces ⓘ
hasActiveMetabolite hydroxy-itraconazole ⓘ
hasATCCode J02AC02 ⓘ
hasBioavailability variable and formulation-dependent ⓘ
hasBlackBoxWarning risk of congestive heart failure ⓘ
hasBrandName Sporanox ⓘ
linked to: itraconazole
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 ⓘ
isLipophilic true ⓘ
isSubstrateOf CYP3A4 ⓘ
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 ⓘ

How these facts were elicited

Referenced by (2)

Full triples — surface form annotated when it differs from this entity's canonical label.

CYP3A4 → inhibitedBy → itraconazole ⓘ
itraconazole → hasBrandName → Sporanox ⓘ
linked to: itraconazole