Comparative Pharmacology
Head-to-head clinical analysis: ITRACONAZOLE versus TERAZOL 7.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ITRACONAZOLE versus TERAZOL 7.
ITRACONAZOLE vs TERAZOL 7
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.
Terconazole is an imidazole antifungal agent that inhibits the synthesis of ergosterol, a key component of fungal cell membranes, by inhibiting the enzyme lanosterol 14α-demethylase. This disruption increases membrane permeability and leads to fungal cell death.
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.
Intravaginal: One full applicator (approximately 5 g of cream containing 40 mg of terconazole) inserted vaginally once daily at bedtime for 7 consecutive days.
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.
Terminal elimination half-life is approximately 7-10 hours; clinically, it allows for once-daily vaginal application, but systemic accumulation is minimal with vaginal dosing.
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.
Primarily fecal (approximately 60%) as unchanged drug and metabolites; renal excretion accounts for about 20% (mostly metabolites).
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."