Itraconazol Sandoz (Itraconazole)

Itraconazole is an azole antifungal that interferes with fungal cell membrane synthesis, and it is indicated for several serious mycotic infections.

• Invasive aspergillosis: treatment of life‑threatening lung infection caused by Aspergillus species.
• Blastomycosis: therapy for systemic infection caused by Blastomyces dermatitidis.
• Histoplasmosis: management of disseminated disease due to Histoplasma capsulatum.
• Candidiasis: eradication of oral, esophageal and systemic Candida infections.
• Dermatophyte infections: cure of skin and nail fungal infections.
• Sporotrichosis: treatment of subcutaneous infection caused by Sporothrix species.

• Itraconazole inhibits the fungal enzyme lanosterol 14α‑demethylase, a cytochrome P450 isoform responsible for converting lanosterol to ergosterol. By blocking this step, the drug reduces ergosterol synthesis, compromising fungal cell membrane integrity and leading to growth inhibition and cell death. The inhibition is concentration‑dependent and persists after drug removal due to high affinity for the enzyme. Itraconazole’s activity covers a broad spectrum of yeasts and molds, making it effective against both systemic and superficial infections.

Itraconazole may cause a variety of adverse reactions, ranging from mild to severe.

Common Side Effects

• Nausea: mild gastrointestinal upset.
• Headache: transient cranial discomfort.
• Abdominal pain: discomfort in the stomach area.
• Diarrhea: loose stools.
• Rash: mild skin eruption.
• Elevated liver enzymes: mild increase in hepatic transaminases.
• Taste alteration: temporary change in flavor perception.
• Fatigue: feeling of tiredness or lack of energy.

Serious or Rare Side Effects

• Hepatotoxicity: severe liver injury or failure.
• Congestive heart failure: worsening of pre‑existing cardiac conditions.
• Severe skin reactions: Stevens‑Johnson syndrome or toxic epidermal necrolysis.
• Visual disturbances: blurred vision or photopsia.
• Anaphylaxis: life‑threatening allergic reaction.

When prescribing itraconazole, several precautions should be observed to ensure patient safety.

• Liver function monitoring: assess hepatic enzymes before and during therapy.
• Drug interactions: review concomitant medications that affect CYP3A4.
• Cardiac status: avoid in patients with heart failure.
• Pregnancy: contraindicated in pregnancy due to fetal risk.
• Breastfeeding: not recommended while nursing.
• Store at ambient temperature: keep below 25°C in original packaging, protect from moisture.

Itraconazole interacts with several drugs through CYP3A4 inhibition and other mechanisms.

Major Interactions (Avoid)

• Certain statins (e.g., simvastatin, lovastatin): risk of rhabdomyolysis.
• Ergot derivatives (e.g., ergotamine): risk of severe vasospasm.
• Pimozide: increased plasma levels leading to cardiac toxicity.
• Cisapride: risk of QT prolongation.
• Certain benzodiazepines (e.g., midazolam): enhanced sedation.

Moderate Interactions (Monitor Closely)

• Anticoagulants (e.g., warfarin): may increase INR.
• Anticonvulsants (e.g., carbamazepine): may reduce itraconazole levels.
• HIV protease inhibitors (e.g., ritonavir): may increase itraconazole exposure.
• Oral contraceptives: may reduce efficacy.
• Rifampin: may markedly decrease itraconazole concentrations.