Triazole Antifungal — Dermatophytes / Aspergillus / Endemic Mycoses
Pregnancy: Contraindicated in 1st trimester — teratogenic in animal studies; use fluconazole (short course) or amphotericin as alternative; avoid throughout if possible
Itraconazole
Brand names: Sporanox
Adult dose
Dose: Oral capsules (with food): 100–200 mg once or twice daily; Oral solution (on empty stomach): 200 mg once daily; IV loading: 200 mg twice daily × 2 days, then 200 mg once daily
Route: Oral (capsule or solution) or IV
Frequency: Once or twice daily (formulation-dependent)
Max: 400 mg/day
IMPORTANT formulation difference: capsules require food and acid for absorption; oral solution (cyclodextrin vehicle) taken on empty stomach — 30% better bioavailability than capsules. Check plasma levels (trough) — significant intra-patient variability. Used for: dermatophytes (onychomycosis), aspergillosis (alternative), histoplasmosis, blastomycosis, sporotrichosis.
Paediatric dose
Dose: 5 mg/kg mg/kg
Route: Oral solution
Frequency: Once daily
Max: 200 mg/day
BNFc: oral solution preferred in children — better bioavailability; capsules not recommended under 12 years
Dose adjustments
Renal
IV formulation: avoid if CrCl <30 mL/min (cyclodextrin vehicle accumulates); oral — no dose adjustment needed
Hepatic
Use with caution — hepatically metabolised; monitor LFTs; avoid if decompensated liver disease
Paediatric weight-based calculator
BNFc: oral solution preferred in children — better bioavailability; capsules not recommended under 12 years
Clinical pearls
- Capsules vs solution: always check which formulation — oral solution on empty stomach is preferred for reliable absorption; capsule absorption requires gastric acid and food (PPIs reduce absorption significantly)
- Trough level monitoring essential: target trough 0.5–1 mg/L (prophylaxis) or >1 mg/L (treatment) — significant variability
- Negative inotropic effect: avoid in patients with cardiac disease or heart failure — itraconazole can precipitate HF decompensation; MHRA warning
- Aspergillosis: voriconazole is preferred first-line; itraconazole is alternative if voriconazole not tolerated or for step-down oral therapy
Contraindications
- Concurrent terfenadine, astemizole, cisapride, quinidine, pimozide (QT prolongation/torsades risk)
- Concurrent simvastatin/lovastatin (rhabdomyolysis)
- Pregnancy (1st trimester — teratogenic)
- Ventricular dysfunction/heart failure (negative inotrope)
- Concurrent rifampicin (reduces itraconazole to sub-therapeutic)
Side effects
- Nausea and GI disturbance
- Hepatotoxicity (elevated LFTs — check monthly)
- Peripheral oedema (negative inotropic effect)
- Cardiac failure (especially in pre-existing cardiac disease)
- QTc prolongation
- Peripheral neuropathy (prolonged use)
- Hypokalaemia
Interactions
- Strong CYP3A4 inhibitor — numerous interactions
- Rifampicin — reduces itraconazole levels to zero (contraindicated)
- Statins (simvastatin/lovastatin) — rhabdomyolysis
- Calcium channel blockers — increased levels (oedema, heart failure)
- Warfarin — enhanced INR
- Immunosuppressants (ciclosporin, tacrolimus, sirolimus) — increased levels
Monitoring
- Itraconazole trough levels (2 weeks after initiation or dose change)
- LFTs monthly
- ECG (QTc)
- Cardiac function (heart failure symptoms)
- Potassium
Reference: BNFc; BNF 90; ESCMID/ECMM Aspergillosis Guidelines; MHRA Itraconazole Cardiac Warning; NICE NG133; PHE Fungal Infection Guidelines. Verify against your local formulary and the latest BNF before prescribing.
Related
Curated clinical cross-links plus same-class fallbacks.
Pathways