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Itraconazole

It is an antifungal medication used to treat a number of fungal infections. This includes aspergillosis, blastomycosis, coccidioidomycosis, histoplasmosis, and paracoccidioidomycosis. It may be given by mouth or intravenously. More

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Description

It is an antifungal medication used to treat a number of fungal infections. This includes aspergillosis, blastomycosis, coccidioidomycosis, histoplasmosis, and paracoccidioidomycosis. It may be given by mouth or intravenously.

Generic Name

Itraconazole

Chemical names

Itraconazole; 84625-61-6; Sporanox; Oriconazole; Itrizole (TN); Sporanox (TN)

Brand names

Aouazol, Biospore, Candistat Cap, Canditral, Fulcover, Fungicap, Itaspor, Itra, Itrazen, Itrocol, Itrole, Itrosac, Itzucia, Sporanox

IUPAC name

1-(butan-2-yl)-4-{4-[4-(4-{[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-4,5-dihydro-1H-1,2,4-triazol-5-one

Pharmacokinetics

NA

Actions

NA

Dosage/Dosage form

The recommended dose is 100 to 200 mg once daily (2 capsules) per oral.

Therapeutic uses

For the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: pulmonary and extrapulmonary blastomycosis, histoplasmosis, aspergillosis, and onychomycosis.

Adverse effects/Side effects

Liver failure; heart failure; pulmonary oedema; CV disease. Dyspepsia, abdominal pain, nausea, vomiting, diarrhoea; menstrual disorders; constipation, rash, pruritus, urticaria; angioedema, anaphylaxis. Increased liver enzyme values, jaundice, Stevens-Johnson syndrome, hypokalaemia.

Interaction

  • Itraconazole is an inhibitor of CYP3A4 and plasma concentrations of many drugs including ciclosporin, digoxin and warfarin may be increased.
  • Concentration increased by: erythromycin, clarithromycin, HIV protease inhibitors.
  • Capsule absorption may be decreased by antacids, H2-receptor antagonists, and proton pump inhibitors.
  • Concentration decreased by: carbamazepine, phenobarbital, phenytoin, isoniazid, rifabutin, rifampin, nevirapine. 

Contraindications

Hypersensitivity to azole antifungals; pregnancy and lactation; hepatic disease. IV: CrCl: <30 ml/minutes.

Storage

Store at 15-25°C.

Information

Molecular weight

705.633

Molecular formula

C35H38Cl2N8O4

CAS number

84625-61-6

Precautions

Renal insufficiency; CHF, history of CHF, COPD; monitor liver function.