Test Catalog

Test ID: ITCON    
Itraconazole, Serum

Useful For Suggests clinical disorders or settings where the test may be helpful

Verifying systemic absorption of orally administered itraconazole


Patients with life-threatening fungal infections


Patients considered at risk for poor absorption or rapid clearance of itraconazole

Clinical Information Discusses physiology, pathophysiology, and general clinical aspects, as they relate to a laboratory test

Itraconazole is a synthetic triazole antifungal drug approved for treatment and prophylaxis of a variety of fungal infections. Its activity results from inhibition of fungal synthesis of ergosterol, an integral component of fungal cell membranes.


Concerns about adequate absorption and drug interactions are some of the major indications for therapeutic drug monitoring. Mean oral bioavailability approximates 55% but is highly variable; absorption can be enhanced by food or acidic drinks. Hepatic enzyme inducers can cause low serum itraconazole levels, and coadministration of these drugs has been associated with itraconazole therapeutic failure.


Itraconazole therapeutic efficacy is greatest when serum concentrations exceed 0.5 mcg/mL for localized infections, or 1.0 mcg/mL for systemic infections. An active metabolite, hydroxyitraconazole, is present in serum at roughly twice the level of the parent drug. These concentrations refer to analysis by high-performance liquid chromatography; quantitation by bioassay results in considerably higher apparent drug measurements due to reactivity with the active metabolite.

Reference Values Describes reference intervals and additional information for interpretation of test results. May include intervals based on age and sex when appropriate. Intervals are Mayo-derived, unless otherwise designated. If an interpretive report is provided, the reference value field will state this.


>0.5 mcg/mL (localized infection)

>1 mcg/mL (systemic infection)



No therapeutic range established; activity and serum concentration are similar to parent drug.

Interpretation Provides information to assist in interpretation of the test results

A lower cutoff concentration has not been defined that applies in all cases. The serum concentration must be interpreted in association with other variables, such as the nature of the infection, the specific microorganism, and minimal inhibitory concentration (MIC) results, if available. Localized infections are more likely to respond when serum itraconazole is more than 0.5 mcg/mL (by high-performance liquid chromatography); systemic infections generally require drug concentrations more than 1.0 mcg/mL. Consider target of more than 1.5 mcg/mL for itraconazole plus hydroxyitraconazole.

Cautions Discusses conditions that may cause diagnostic confusion, including improper specimen collection and handling, inappropriate test selection, and interfering substances

Enteropathy, H2-histamine receptor blockers, hepatic enzyme inducers, and other variables can result in low to non-detectable serum levels with concomitant high risk of therapeutic failure.


AIDS patients and organ transplant patients receiving immunosuppressive therapy tend to have lower serum itraconazole levels on standard doses and are thus at high risk of therapeutic failure.

Clinical Reference Recommendations for in-depth reading of a clinical nature

1. Andes D, Pascual A, Marchetti O: Antifungal therapeutic drug monitoring: established and emerging indications. Antimicrob Agents Chemother. 2009 Jan;53(1):24-34

2. Hope WW, Billaud EM, Lestner J, Denning DW: Therapeutic drug monitoring for triazoles. Curr Opin Infect Dis. 2008 Dec;21(6):580-586

3. Rifai N, Horvath AR, Wittwer CT, eds: Tietz Textbook of Clinical Chemistry and Molecular Diagnostics. 6th ed. Elsevier. 2018