Comparative Pharmacology
Head-to-head clinical analysis: ITRACONAZOLE versus NIZORAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ITRACONAZOLE versus NIZORAL.
ITRACONAZOLE vs NIZORAL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Inhibits fungal cytochrome P450-dependent 14α-demethylase, thereby blocking the conversion of lanosterol to ergosterol, disrupting fungal cell membrane synthesis.
Inhibits fungal CYP51 (lanosterol 14α-demethylase), blocking ergosterol synthesis and disrupting fungal cell membrane integrity.
200 mg orally once daily; for life-threatening infections, can be increased to 200 mg three times daily for first 3 days then twice daily. IV: 200 mg IV every 12 hours for 2 days, then 200 mg IV once daily.
Ketoconazole 200 mg orally once daily with food. For severe infections, increase to 400 mg once daily. Duration depends on indication.
None Documented
None Documented
Clinical Note
moderateItraconazole + Tranilast
"The risk or severity of adverse effects can be increased when Itraconazole is combined with Tranilast."
Clinical Note
moderateItraconazole + Tolfenamic acid
"The risk or severity of adverse effects can be increased when Itraconazole is combined with Tolfenamic acid."
Clinical Note
moderateItraconazole + Nimesulide
"The risk or severity of adverse effects can be increased when Itraconazole is combined with Nimesulide."
Clinical Note
moderateTerminal elimination half-life of itraconazole is approximately 24-36 hours after a single dose, but upon chronic dosing, the half-life increases to 34-42 hours due to saturable metabolism. For the active metabolite hydroxyitraconazole, half-life is similar. This prolonged half-life supports once- or twice-daily dosing.
Biphasic elimination: initial half-life ~2 hours, terminal half-life 6–10 hours in adults with normal hepatic function; prolonged in hepatic impairment.
Itraconazole is extensively metabolized in the liver; the primary route of elimination is fecal (approximately 54% as metabolites, 18% as unchanged drug). Renal excretion accounts for about 35% of the dose, with <1% as unchanged drug. Bilary excretion also contributes.
Approximately 70% of the dose is excreted unchanged in feces via biliary elimination, and about 20–35% is excreted in urine, with less than 1% as unchanged drug in urine.
Category D/X
Category C
Azole Antifungal
Azole Antifungal
Itraconazole + Risedronic acid
"The risk or severity of adverse effects can be increased when Itraconazole is combined with Risedronic acid."