API: Itraconazole

What Is Itraconazole and How Does It Work?

Itraconazole belongs to a class of antifungals called triazoles and can be administered orally or intravenously to treat a broad spectrum of fungal infections, particularly those for which Fluconazole or other antifungals are ineffective. Itraconazole works by inhibiting the synthesis of ergosterol (a key component of fungal cell membranes) via the cytochrome P450.1 As the drug essentially works by slowing the growth of the fungus causing the infection, itraconazole may be effective in preventing fungal infections in immunocompromised patients. Itraconazole has a broad spectrum of activity, making it the drug of choice in treating resistant fungi.

For more information, including a MSDS sheet, please see PNA’s Itraconazole page.

Approved Indications2

  • Blastomycosis: Itraconazole is used to treat blastomycosis of the skin and internal organs.
  • Histoplasmosis: Itraconazole is used to treat histoplasmosis in the lungs and other organs and for chronic cavitary pulmonary disease.
  • Aspergillosis: Itraconazole is effective for treating aspergillosis, particularly in patients who don’t respond to amphotericin B therapy.
  • Onychomycosis: In non-immunocompromised patients, itraconazole may be used to treat onychomycosis of the fingers and toenails.
  • Other conditions: Itraconazole may also be effective in treating other infections of resistant fungi, such as Candida and Cryptococcus.

Side Effects and Drug Interactions3

Common side effects in patients taking itraconazole include:

  • Nausea and vomiting
  • Diarrhea or constipation
  • Bloating
  • Itching or Rash
  • Edema
  • Dizziness and fatigue
  • Headache
  • Hypertension
  • Increased blood triglycerides

Patients who suffer from severity of these common side effects should contact their pharmacist or physician right away. Patients who experience fever, shortness of breath, swelling or rapid weight gain, tinnitus or other problems with hearing, numbness or tingling, blurred or double vision, burning when urinating or loss of bladder control, pain in upper stomach spreading to back, or congestive heart failure symptoms should inform their physician immediately.4
Note: It is important to report any signs or symptoms that suggest liver dysfunction, such as:

  • Unusual fatigue
  • Poor appetite
  • Nausea and vomiting
  • Jaundice
  • Dark urine or pale stool

Patients who are allergic to itraconazole should not take this drug. Itraconazole should not be used for treatment of onychomycosis in patients with a history of heart failure.5

Itraconazole reduces the liver metabolism of certain drugs that caused increased blood levels and side effects from those drugs. This list includes: cisapride, pimozide, quinidine, dofetilide, levomethadyl, warfarin, tolbutamide, glyburide, glipizide, protease inhibitors, midazolam, and triazolam.

Use of calcium channel blockers may increase the risk of heart failure. Risk of serious adverse effects has also been noted when itraconazole has been used in patients taking statins such as simvastatin and lovastatin.

Latest News and Research

Itraconazole was developed in 1984 as a broad spectrum antifungal drug that can be used in cases where species resistance is widespread. The drug is available as both a capsule and in liquid form, and can be compounded into a topical cream. It is currently effective against Aspergillus, Blastomyces Candida (all species including many fluconazole resistant isolates), Coccidioides, Cryptococcus, Histoplasma, Paracoccidioides, Scedosporium apiospermum, and Sporothrix schenckii.6 The drug is also active against all skin fungi and is the best agent against black molds, including Bipolaris and Exserohilum. Resistance to itraconazole is sometimes reported in Aspergillus and in Candida, but not as widely as resistance is seen with fluconazole. Activity against different fungi changes constantly depending on prescription patterns and resistance activity in the area.

New research shows promise for the use of itraconazole, possibly in conjunction with another agent (such as arsenic trioxide) for treatment of medulloblastoma and basal cell carcinoma.7 Itraconazole also shows promise in treating invasive fungal diseases during a high risk period of recovery in patients with acute myeloid leukemia/myelodysplastic syndrome undergoing remission-induction chemotherapy.8

Buying Guide

PNA is a recommended bulk supplier of Itraconazole and other APIs. You can learn more about Itraconazole here.

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Resources

Show 8 footnotes

  1. “Itraconazole,” December 1, 2015, http://www.drugs.com/pro/itraconazole.html
  2. “Neurontin,” 2016, http://www.rxlist.com/neurontin-drug/consumer-uses.htm
  3. “itraconazole, Sporanox,” December 31, 2014, http://www.medicinenet.com/itraconazole/article.htm
  4. “Sporanox, 2016, http://www.rxlist.com/sporanox-side-effects-drug-center.htm
  5. “Itraconazole, 2016, http://reference.medscape.com/drug/sporanox-omnel-itraconazole-342591#5
  6. “itraconazole,” http://www.fungalinfectiontrust.org/itracon.html
  7. “Itraconazole and Arsenic Trioxide Inhibit Hedgehog Pathway Activation and Tumor Growth Associated with Acquired Resistance to Smoothened Antagonists,” January 14, 2013, http://www.sciencedirect.com/science/article/pii/S1535610812004953
  8. “Comparative Clinical Effectiveness Of Prophylactic Voriconazole/Posaconazole To Fluconazole/Itraconazole In Patients With Acute Myeloid Leukemia/Myelodysplastic Syndrome Undergoing Cytotoxic Chemotherapy Over A 12-Year Period,” March 2012, http://www.haematologica.org/content/97/3/459