Itraconazole is a drug used in the treatment of fungal infections, such as aspergillosis, blastomycosis, histoplasmosis, and fungal infection localized to the toenails and fingernails (onychomycosis).
Itraconazole is available as capsules or as an oral solution. The dose is 200 mg once a day, to 400 mg in severe infection. There is an intravenous preparation available in the US, but not in the UK. In the UK, if an intravenous preparation is required, then an alternative antifungal drug should be used.
Itraconazole has relatively low bioavailability after oral administration, especially when given in capsule form on empty stomach. The oral solution is better absorbed.The cyclodextrin contained in the oral solution can cause an osmotic diarrhea, and if this is a problem, then half the dose can be given as oral solution and half as capsule in order to reduce the amount of cyclodextrin given. Itraconazole capsules should always be taken with food, as this improves absorption. Itraconazole oral solution should be taken an hour before food, or two hours after food (and likewise if a combination of capsules and oral solution are used). Itraconazole may be taken with orange juice or cola, as absorption is also improved by acid. Absorption of itraconazole is impaired when taken with an antacid, H2-blocker or proton pump inhibitor.
Some doctors give an oral loading dose of 200 mg three times a day for three days, before dropping down to the usual dose. Because itraconazole absorption is unreliable, blood levels should be monitored at least once a week in those patients who are being treated for life-threatening (or potentially life-threatening) fungal infections.
In intravenous dosing, four doses of itraconazole 200 mg are given 12 hours apart, before changing the dose to once daily. There is no safety data for giving the intravenous preparation for more than 14 days continuously.
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Stomach upset, diarrhea, headache, or dizziness may occur the first few days as your body adjusts to the medication. Other side effects reported include ringing in the ears, fever, sexual performance problems, depression, drowsiness, or trouble sleeping. If any of these effects persist or worsen, notify your doctor promptly. Notify your doctor immediately if you develop: severe nausea, yellowing eyes/skin, unusual weakness, dark urine, pale stools, numbness or tingling of the hands/feet. In the unlikely event you have a serious allergic reaction to this drug, seek medical attention immediately. Symptoms of a serious allergic reaction include: rash, itching, swelling, dizziness, trouble breathing.
Itraconazole was found to cause a dose-related increase in maternal toxicity, embryotoxicity, and teratogenicity in rats at dosage levels of approximately 40-160 mg/kg/day (5-20x MRHD), and in mice at dosage levels of approximately 80 mg/kg/day (10x MRHD). In rats, the teratogenicity consisted of major skeletal defects; in mice, it consisted of encephaloceles and/or macroglossia.
Itraconazole is not removed by dialysis. In the event of accidental overdosage, supportive measures, including gastric lavage with sodium bicarbonate, should be employed.
Limited data exist on the outcomes of patients ingesting high doses of itraconazole. In patients taking either 1000 mg of SPORANOX® (itraconazole) Oral Solution or up to 3000 mg of SPORANOX® (itraconazole) Capsules, the adverse event profile was similar to that observed at recommended doses.