Oropharyngeal candidiasis
Second line
Treats oropharyngeal candidiasis including fluconazole-resistant infections. AEMPS keeps fluconazole as first-line and reserves itraconazole for resistance or intolerance.
Antifungal, triazole
ATC code: J02AC02 (Itraconazole)
Brand names
Sporanox, Tolsura
Itraconazole inhibits fungal CYP51 (lanosterol 14-alpha-demethylase) and blocks ergosterol synthesis, the main component of fungal membranes. Its spectrum covers dermatophytes, Candida, Aspergillus, and endemic dimorphic fungi. In humans, itraconazole is one of the most potent inhibitors of CYP3A4 and P-glycoprotein: concentrations of dozens of substrates (statins, immunosuppressants, calcium channel blockers, ergotamine) rise several-fold. carries a boxed warning on heart failure because of a negative inotropic effect.
Second line
Treats oropharyngeal candidiasis including fluconazole-resistant infections. AEMPS keeps fluconazole as first-line and reserves itraconazole for resistance or intolerance.
Second line
Triazole for long-term maintenance therapy of invasive aspergillosis after successful induction with voriconazole or isavuconazole. SEIMC and ESCMID position itraconazole as second-line.
Third line
Treats recurrent vulvovaginal candidiasis and fluconazole-resistant cases. SEGO keeps fluconazole as first-line.
15 pairs found. Sorted from critical to minor.
Mechanism
Itraconazole is the strongest CYP3A4 inhibitor. Cabergoline rises 5-7 fold. Valvulopathy and pulmonary fibrosis risk.
Symptoms
Dyspnoea, cardiac murmurs, edema.
Management
Combination contraindicated.
Mechanism
Itraconazole is the strongest CYP3A4 inhibitor. Cisapride rises 10+ fold. Fatal torsades.
Symptoms
Torsades de pointes.
Management
Combination contraindicated.
Mechanism
Strongest CYP3A4 inhibitor – dihydroergotamine rises 20+ fold.
Symptoms
Fatal ergotism.
Management
Combination contraindicated.
Mechanism
Itraconazole is the strongest CYP3A4 inhibitor. Ergotamine rises 20+ fold, fatal ergotism with gangrene. Ergomar Section 4.
Symptoms
Digital ischaemia, gangrene, stroke within hours.
Management
Combination contraindicated.
Mechanism
Strong CYP3A4 inhibitor – everolimus rises 9-fold. Certican Section 4.3 strict contraindication.
Symptoms
Acute immunosuppression, pneumonitis.
Management
Combination contraindicated.
Mechanism
Strong CYP3A4 inhibitor – lovastatin rises 20+ fold. contraindication.
Symptoms
Myalgia, weakness, dark urine, rising CK within 5-10 days.
Management
Combination contraindicated.
Sources
Mechanism
Itraconazole is the strongest clinical CYP3A4 inhibitor. Pimozide concentration rises 10+ fold; torsades de pointes risk is maximal. Orap Section 4 strict contraindication.
Symptoms
QT prolongation by day 3, syncope, torsades de pointes.
Management
Combination contraindicated. Alternative antifungal: terbinafine for superficial infections. For systemic infections, hold pimozide one week before itraconazole and resume 2 weeks after.
Mechanism
Itraconazole is the strongest CYP3A4 inhibitor in clinical use. Simvastatin is a sensitive substrate; its concentration rises 10–20 fold. Risk of rhabdomyolysis with acute kidney injury is the highest among statin–azole combinations.
Symptoms
Rhabdomyolysis within 3–7 days: myalgia, weakness, dark urine. CK above 50× ULN, oliguria.
Management
Combination contraindicated. Stop simvastatin one week before starting itraconazole and resume 2 weeks after the last dose. Alternative: pravastatin or rosuvastatin.
Sources
Mechanism
Itraconazole is the strongest CYP3A4 inhibitor. Sirolimus rises 10+ fold. Rapamune Section 4 contraindication.
Symptoms
Acute nephrotoxicity, hepatotoxicity, cytopenia.
Management
Combination contraindicated.
Sources
Mechanism
Strong CYP3A4 inhibitor – ticagrelor rises 5-7 fold. Section 4.3.
Symptoms
Bleeding.
Management
Combination contraindicated.
Mechanism
Itraconazole inhibits CYP3A4 and P-gp. Vincristine rises 5+ fold – fatal neurotoxicity with motor deficit and autonomic neuropathy.
Symptoms
Severe peripheral neuropathy, paralytic ileus, autonomic disorders.
Management
Combination contraindicated. Alternative antifungal – micafungin or caspofungin.
Mechanism
Itraconazole inhibits CYP3A4 and P-glycoprotein. Atorvastatin concentration rises 3–4 fold. does not contraindicate the combination outright but caps atorvastatin at 20 mg/day and requires CK monitoring.
Symptoms
Myalgia and weakness within 1–3 weeks; CK above 5× ULN.
Management
Cap atorvastatin at 20 mg/day. For short itraconazole courses (up to 14 days) the safer option is to hold atorvastatin altogether.
Mechanism
Strong CYP3A4 inhibitor. Cyclosporine rises 5+ fold.
Symptoms
Nephrotoxicity.
Management
Reduce cyclosporine by 75%.
Mechanism
Strong CYP3A4 inhibitor. Methadone rises 2-3 fold.
Symptoms
Sedation, respiratory depression, QT prolongation.
Management
Reduce methadone by 25%, ECG monitoring.
Mechanism
Itraconazole is a strong CYP3A4 inhibitor. Tacrolimus rises 5+ fold – severe nephrotoxicity.
Symptoms
Rising creatinine, hypertension, tremor within 3-7 days.
Management
Reduce tacrolimus by 75% with frequent blood level monitoring. If possible, switch itraconazole to an echinocandin.
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FDA Category C. Systemic azoles in the first trimester carry malformation risk (especially at doses >400 mg/day – a syndrome similar to chronic high-dose fluconazole exposure). AEMPS contraindicates systemic itraconazole in pregnancy except for life-threatening invasive mycoses. Topical and nail-lacquer forms are safer.
Compatible with caution. Hale L3. Transfers into milk (RID about 0.2%) with minimal infant exposure, but has a long half-life. AEMPS advises interrupting breastfeeding for courses >14 days; short vaginal or onychomycosis courses are compatible.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Itraconazole is evaluated for the following indications with varying evidence strength: Oropharyngeal candidiasis (evidence tier A), Vulvovaginal candidiasis (evidence tier B), Invasive aspergillosis (evidence tier B). See the full indication matrix with dosing and citations above on this page.
Common side effects of Itraconazole (≥ 1 in 100): Nausea, vomiting, diarrhoea, Elevated transaminases, Headache, Rash. See the Safety section for uncommon and serious reactions.
FDA category C. FDA Category C. Systemic azoles in the first trimester carry malformation risk (especially at doses >400 mg/day – a syndrome similar to chronic high-dose fluconazole exposure). AEMPS contraindicates systemic itraconazole in pregnancy except for life-threatening invasive mycoses. Topical and nail-lacquer forms are safer.
Compatible with caution. Hale L3. Transfers into milk (RID about 0.2%) with minimal infant exposure, but has a long half-life. AEMPS advises interrupting breastfeeding for courses >14 days; short vaginal or onychomycosis courses are compatible.
Itraconazole is contraindicated in: Hypersensitivity to itraconazole; Heart failure and left ventricular dysfunction; Pregnancy (systemic use); Co-administration with CYP3A4 substrates prolonging QT (quinidine, dofetilide, cisapride, pimozide, lovastatin, simvastatin, ergotamine). Full list in the Safety section.