Clinical Pharmacology Details


Itraconazole


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Indications & Dose:

Blastomycosis, histoplasmosis, aspergillosis, oropharyngeal candidiasis (sol), esophageal candidiasis (sol), superficial mycoses (dermatophytoses. pityriasis versicolor, sebopsoriasis, candidiasis ), onychomycosis, systemic mycoses (candidiasis, cryptococcal infections, paracoccidioidomycosis, coccidioidomycosis. subcutaneous mycoses (sporotrichosis, chromomycosis), cutaneous leishmaniasis, fungal keratitis, alternariosis, zygomycosis


DOSE


Adult



• Oropharyngeal candidiasis PO 200 mg sol (20 ml) qd for 1-2 wk


• Oropharyngeal candidiasis refractory to fluconazole: PO 100 mg sol (10 ml) bid


• Esophageal candidiasis: PO 100 mg sol (10 ml) qd for 3 wk, treat for at least 2 wk past resolution of symptoms


• Blasromycosis/histoplasmosis: PO 200 mg qd; may increase if evidence of progressive disease to 300- 400 mg/day in 2 divided doses


• Aspergillosis: PO 200-400 mg/ day; doses >200 mg/day should be given in 2 divided doses


• Life-threatening situations: PO loading dose of 200 mg tid should be given for 1st 3 days


• Onychomycosis: PO 200 mg qd for at least 3 mo or 200 mg qd x 1 wk/mo


Vulvovaginal candidiasis: 200mg twice daily for 1 day.


Tinea pedis & tinea manuum: 100mg daily for 30 days.


Onchomycosis: Either 200mg daily for 3 months or course (‘pulse’) of 200mg twice daily for 7 days, subsequent courses repeated after 21-day interval; fingernails 2 courses, toenails 2 courses.


Alternative in systemic infections: 200mg once daily (candidiasis 100-200mg once daily) increased in invasive or disseminated disease and in cryptococcal meningitis to 200mg twice daily.


Maintenance in AIDS patients and prophylaxis in neutropenia: 200mg once daily, increased to 200mg twice daily if low plasma itraconazole concentrations.


Non meningeal crypttococcosis; 200mg once daily Cryptococeal menengitis; 200 mg twice daily Prophylaxis in Neutropenia; 200mg once daily increasing to 200mg twice daily if itraconazole blood levels are low


Elderly & Children Not recommended.

Contraindications:

Side Effects:

Cautions:

Precautions:

Hypersensitivity to other azole antifungals; preexisting hepatic function abnormalities, children, hypochlorhydria (reduces drug absorption)

Interaction:

Drugs


Alprazolam: Increased plasma


Aluminum: Reduced itraconazole absorption


Amprenavir: Increased plasma amprenavir concentration


Antacids: Reduced itraconazole absorption


Astemizole: QT prolongation and life-threatening dysrhythmia 


Atevirdine: Increased plasma at evirdine concentration


Atorvastatin: Increased plasma atorvastatin concentration with risk of rhabdomyolysis


Buspirone: Increased plasma buspirone concentration


Calcium: Reduced itraconazole absorption


Cerivastatin: Increased plasma cerivastatin concentration with risk of rhabdomyolysis


Chlordiazepoxide: Increased plasma chlordiazepoxide concentration


Cimetidine: Reduced itraconazole absorption


Cisapride: QT prolongation and life-threatening dysrhythmia


Clarithromycin: Increased plasma itraconazole concentration


Cyclosporine: Increased plasma cyclosporine concentration


Diazepam: Increased plasma diazepam concentration


Digoxin: Increased plasma digoxin concentration


Didanosine: Reduced itraconazole absorption


Erythromycin: Increased plasma itraconazole concentration


Ethanol: Disulfiram-like reaction possible


Famotidine: Reduced itraconazole absorption


Felodipine: Increased plasma felodipine concentration


Fluvastatin: Increased plasma fluvastatin concentration with risk of rhabdomyolysis


Food: Increased itraconazole absorption


Indinavir: Increased plasma indinavir concentration


Lansoprazole: Reduced itraconazole absorption


Lovastatin: Increased plasma lovastatin concentration with risk of rhabdomyolysis


Magnesium: Reduced itraconazole absorption


Methadone: Increased plasma methadone concentration


Methylprednisolone: Increased plasma methyl prednisolone concentration


Midazolam: Increased plasma midazolam concentration


Nelfinavir: Increased plasma nelfinavir concentration


Nizatidine: Reduced itraconazole absorption


Omeprazole: Reduced itraconazole absorption


Oral anticoagulants: Increased hypoprothrombinemic response


Phenytoin: Markedly reduced Plasma itraconazole concentration


Pimozide: Increased plasma pimozide concentration, QT prolongation and life-threatening dysrhythmia


Pravastatin: Increased plasma pravastatin concentration with risk of rhabdomyolysis


Quinidine: Increased plasma quinidine concentration, QT prolongation and life-threatening dysrhythmia 


Rifampin: Decreased plasma itraconazole concentration; decreased plasma rifampin concentration


Ritonavir: Increased plasma ritonavir concentration


Saquinavir: Increased plasma saquinavir concentration


Simvastatin: Increased plasma simvastatin concentration with risk of rhabdomyolysis


Sodium bicarbonate: Reduced itraconazole absorption


Sucralfate: Reduced itraconazole absorption


Tacrolimus: Increased plasma taerolimus concentration


Terfenadine: QT prolongation and life-threatening dysrhythmia


Tolbutamide: Increased plasma tolbutamide concentration


Triazolam: Increased plasma triazolam concentration


Warfarin: Increased hypoprothrombinemic response 

Warnings:

Adverse Effects:

Lactations:

Excreted into breast milk; do not administer to nursing mothers 

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

CNS: Decreased libido, depression, dizziness, fatigue, fever, headache, insomnia, malaise, somnolence


CV: Edema, hypertension


GI: Abdominal pain, anorexia, diarrhea, hepatitis, liver function test * abnormality, nausea, vomiting


GU: Albuminuria, impotence


METAB: Hypokalemia


SKIN: Pruritus, rash (more common a in patients receiving immunosuppressants)

Patient And Carer Advice: