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Itraconazole

Itraconazole is a triazole group of anti fungal agent.The triazoles (fluconazole, itraconazole etc.) were developed in order to increase the spectrum of anti fungal activity  and reduce the side effects associated with the imidazoles

Mechanism of action:

Itraconazole acts by inhibiting the enzyme demethylase (Lanosterol 14 α-demethylase is a cytochrome P450 enzyme that converts lanosterol to cholesterol.) This blocks the demethylation of lanosterol to ergosterol, the principal sterol of fungal membranes. This leads to disruption of fungal cell membrane and inhibition of  fungal cell growth.

Pharmacology:

  1. Itraconazole is well-absorbed orally and the drug requires acid for complete dissolution. After absorption,the drug is extensively bound to plasma proteins and distributes well in the body. But, unlike ketoconazole , therapeutic concentrations are not attained in the CSF.
  2. Itraconazole is extensively metabolized by the liver, but unlike ketoconazole,it does not inhibit androgen synthesis.
  3. Major metabolite of itraconazole, hydroxyitraconazole, is biologically active and has a similar antifungal spectrum like itraconazole.
  4. Very minimal amount of the drug is excreted by the urine; so, there is no need of dose reduction in renal failure.
Topical

Subconjunctival

Intravitreal

Intravenous

Oral

2% suspension

NA

NA

NA

200 mg/ day

Itraconazole is now the drug of choice for the treatment of blastomycosis, sporotrichosis, paracoccidioidomycosis, and histoplasmosis. Unlike ketoconazole, it is effective in acquired immunodeficiency syndrome associated histoplasmosis.

Side effects:

Adverse effects include nausea and vomiting, rash, hypokalemia, hypertension, edema, and headache.

Caution:

Itraconazole should be avoided in pregnancy.

Drug Interaction:

Itraconazole interferes with the metabolism of many drugs, including oral anticoagulants, statins, and quinidine.

Statutory Warning

Materials / Informations provided here are for educational purpose only ; and not to be used for medical advice, diagnosis or treatment