Itraconazole is an antifungal medication used to treat a number of fungal infections. This includes aspergillosis, blastomycosis, coccidioidomycosis, histoplasmosis, and paracoccidioidomycosis. It may be given by mouth or intravenously.

Molecular Structure


Class of Drug

Antifungal agent.

Mechanism of Action

Inhibits fungal cytochrome P450 synthesis of ergosterol, resulting in decreased cell wall integrity and leakage of essential cellular components.

Susceptible organisms in vivo: Not for cryptococcosis (fluconazole is preferred). Blastomyces dermatidis, Candida, Histoplasma, Aspergillus flavus, Coccidioides immitis Sporotrichosis.

Indications / Dosage / Route

Routes of Administration: Oral only.

Condition: Blastomycosis or histoplasmosis

Dose: Adults: 200 mg once daily. If there is no improvement or the disease is progressive, the dose may be increased in 100-mg increments. Maximum: 400 mg/d.

Children: 3-16 years: 100 mg/d.

Condition: Aspergillosis

Dose: Adults: 400 mg daily.

Condition: Life-threatening infections

Dose: Adults: 200 mg t.i.d. for the first 3 days.

Condition: Onychomycosis

Dose: Adults: 200 mg once a day for 12 consecutive weeks.

Condition: Oral solution: oropharyngeal candidiasis

Dose: Adults: 200 mg/d for 1-2 weeks.

Condition: Oral solution: esophageal candidiasis

Dose: Adults: 100 mg/d, minimum 3 weeks.

Adjustment of Dosage

Kidney disease: None.

Liver disease: None.

Elderly: None

Pediatric: Safety and efficacy have not been established in children <3 years.

Food and Drug Interactions

Food: Should be taken with food.

Pregnancy: Category C.

Lactation: Appears in breast milk. Avoid breastfeeding.

Contraindications: Hypersensitivity to itraconazole and other azole antifungals, coadministration of astemizole, triazolam, midazolam, treatment of onchomycosis during pregnancy.

Warnings / Precautions

> Review drugs that patient is currently taking to avoid possible dangerous drug drug interactions.

Clinically Important Drug Interactions

> Itraconazole increases effects/toxicity of the following: astemizole, calcium blockers, cisapride, cyclosporine, digoxin, midazo¬lam, sulfonylureas, tacrolimus, triazolam, warfarin.

> The following drugs decrease effects/toxicity of the following: itraconzole: isoniazid, phenytoin, rifampin, phenobarbital.

Adverse Reactions

> Common: nausea, vomiting, diarrhea, abdominal pain, rash.

> Serious: hepatotoxicity (rare), exfoliative skin disorders (rare).

Parameters to Monitor

> Signs and symptoms of liver toxicity, particularly in patients receiving treatment longer than 1 month.

> Symptoms indicating reactivation of blastomycosis: rales, chest pain, cough, fever, rash, SOB, weight loss.

> Symptoms indicating reactivation of histoplasmosis: Chest pain, generalized pain, rales, SOB, weight loss.

Advice to Patient

> Report symptoms of possible liver dysfunction: jaundice, anorexia, dark urine, pale stools, nausea, vomiting.

> Avoid driving and other activities requiring mental alertness or that are potentially dangerous until response to drug is known.

> Avoid alcohol.

> To minimize possible photosensitivity reaction, apply adequate sunscreen and use proper covering when exposed to strong sunlight.

Further Useful Info

> Itraconazole is not used for cryptococcosis (fluconazole is preferred). It is a broad-spectrum antifungal agent and covers Aspergillus species.

> For severe infections, amphotericin B is preferred.

> Itraconazole is very effective against onycomycosis, Candida infections, Blastomyces, Histoplasma, coccidiomycosis, aspergillosis, and sporotrichosis. It is effective for CNS infections. In general, amphotericin B is used acutely, then itraconazole is given as long term therapy.

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