Itraconazole
- Atc Codes:J02AC02
- CAS Codes:84625-61-6
- PHARMGKB ID:84625-61-6
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Itrabene, Itraconazol, Sporanox; Belgium: Itraconazole, Sporanox; Bulgaria: Itraconazole, Orungal; Cyprus: Etrel, Sporal; Czech Republic: Cladostad, Itrakonazol, Prokanazol, Sporanox; Denmark: Itroconazol, Niddazol, Sporanox; Estonia: Cladosol, Itraconazol, Orungal, Prokanazol; Finland: Sporanox; France: Itraconazole, Sporanox; Germany: Canifug-Itra, Itracol, Itraconazol, Itraconbeta, Intraderm, Intrafungol, Itrazol, Sempera, Siros, Sporanox; Greece: Assosept-S, Bevonazole, Brovicton, Deratil, Etrel, Fansidol, Flunol, Fungonazol, Fungospor, Idranox, Inrozol, Isoflon, Itrabest, Itracon, Itraconal, Itralfa, Itrapron, Itraspor, Itraviron, Itrazol, Laverio, Lorenzol, Mesmor, Micronazol, Mycodrox, Neo Candimyck, Prominox, Soprazon, Sporanox, Sporizole, Sterginox; Hungary: Cladostad, Itraconazol, Itraconep, Itragen, Omicral, Orungal; Ireland: Sporanox; Italy: Itraconaz, Sporanox, Tranizolo, Trazer, Triasporin; Latvia: Cladosol, Itraconazol, Itranols, Orungal; Lithuania: Itraconazol; Luxembourg: Sporanox; Malta: Itraconazol, Sporal, Sporanox; Netherlands: Itraconazol, Trisporal; Poland: Cladostad, Fungitrac, IntraGen, IntraLek, Orungal, Trioxal; Portugal: Itraconazol, Sporanox; Romania: Itraconazol, Micogal, Omicral, Orungal, Sporilin; Slovakia: Cladostad, Itrakonazol, Sporanox; Slovenia: Itrasporin, Sporanox; Spain: Canadiol, Hongoseril, Itraconazol, Sporanox; Sweden: Itrakonazol, Sporanox; UK: Itraconazole, Sporanox.
North America
Canada: Sporanox; USA: Itraconazole, Sporanox.
Latin America
Argentina: Itrac, Micotenk, Nitridazol, Panastat, Salimidin, Sporanox; Brazil: Estiranox, Fungonax, Itraconazol, Itraconol, Itracotan, Itralex, Itraspor, Itrazol, Neo-Itrax, Sporanox, Spozol, Traconal, Tracozon; Mexico: Carexan, Conamed, Congox, Derusil, Fitocyd, Fuzoltec, Iqcona, Isoporum, Isox, Itraconazol, Itracosid, Itranax, Lozartil, Rixtal, Seritral, Silicsan, Sinozol, Solmavin, Sporanox, Steitraz, Trax-100, Z-Fin, Zolken, Zotril.
Asia
Japan: Iconazon, Idenolart, ITCZ, Itorat, Itracon, Itraconazole, Itraconet, Itrareel, Itrizole, Toracona.
Drug combinations
Chemistry
Itraconazole: C~35~H~38~Cl~2~N~8~O~4~. Mw: 705.63. (1) 3H-1,2,4-Triazol-3-one, 4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl)-; (2)(±)-1-sec-Butyl-4-[p-[4-[p-[[(2R*,4S*)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-D2-1,2,4-triazolin-5-one. CAS-84625-61-6 (1984).
Pharmacologic Category
Antifungals; Azoles. (ATC-Code: J02AC02).
Mechanism of action
Interferes with cytochrome P450 activity, decreasing ergosterol synthesis (principal sterol in fungal cell membrane) and inhibiting cell membrane formation.
Therapeutic use
Treatment of susceptible fungal infections in immunocompromised and immunocompetent patients including blastomycosis and histoplasmosis. Aspergillosis, and onychomycosis of toenail. Treatment of onychomycosis of fingernail without concomitant toenail infection via a pulse-type dosing regimen. Active against Aspergillus, Candida, Coccidioides, Cryptococcus, Sporothrix, tinea unguium.
Pregnancy and lactiation implications
Should not be used to treat onychomycosis during pregnancy. Use not recommended during lactation.
Unlabeled use
Contraindications
Hypersensitivity to itraconazole, any component of the formulation, or to other azoles. Concurrent administration with cisapride, dofetilide, ergot derivatives, levomethadyl, lovastatin, midazolam, pimozide, quinidine, simvastatin, or triazolam. Treatment of onychomycosis in evidence of left ventricular dysfunction, CHF, or history of CHF.
Warnings and precautions
Heart failure, or neuropathy might occur. Not recommended for use in active liver disease, elevated liver enzymes, or prior hepatotoxic reactions to other drugs. Not recommended for treatment of onychomycosis in left ventricular dysfunction or history of CHF. I.V. formulation should not be used in renal impairment (i.e. CrCl <30 mL/minute). Initiation of treatment with oral solution not recommended in immediate risk for systemic candidiasis (e.g. patients with severe neutropenia). Oral capsules and oral solution cannot be used interchangeably. CHF, peripheral edema, and pulmonary edema reported in immunocompromised or immunocompetent patients. Life-threatening cardiac dysrhythmias and/or sudden death occurred in patients receiving cisapride, pimozide, or quinidine concomitantly with itraconazole or other CYP3A4 inhibitors. Anaphylaxis and Stevens-Johnson syndrome reported rarely. Itraconazole should be used with caution in individuals hypersensitive to other azoles. Overgrowth of nonsusceptible fungi may occur. Toenail infections generally require more prolonged antifungal therapy than fingernail infections.