• Histoplasmosis. • Blastomycosis. • Aspergillosis. • Dermatophyte infection of fingernails or toenails in nonimmunocompromised patients (oral capsules only). • Oropharyngeal esophageal candidiasis.
Aspergillosis, Blastomycosis, Histoplasmosis
Adults: PO 200 to 400 mg/day. Give doses higher than 200 mg in 2 divided doses. An inadequate treatment period may lead to recurrence.
Adults: PO 100 mg/day (10 mL) for a minimum of 3 wk. Continue treatment for 2 wk following resolution of symptoms. Doses up to 200 mg/day may be used based on medical judgment of the patient’s response. Vigorously swish solution in mouth (10 mL at a time) for several seconds and swallow.
Capsules: Loading dose of 200 mg 3 times daily for 3 days. Continue treatment for a minimum of 3 mo and until clinical parameters and laboratory tests indicate the active fungal infection has subsided.
Onychomycosis, Fingernails Only
Adults: PO 2 treatment pulses separated by a 3-wk period without itraconazole. Each pulse consisting of 200 mg twice daily for 1 wk.
Onychomycosis, Toenails With or Without Fingernail Involvement
Adults: PO 200 mg/day for 12 wk.
Adults: PO 200 mg (20 mL)/day of oral solution for 1 to 2 wk. Vigorously swish solution in mouth (10 mL at a time) for several seconds and swallow. For patients with oropharyngeal candidiasis unresponsive/refractory to treatment with fluconazole tablets, the recommended dose is 100 mg (10 mL) twice daily.
|•||Inhibits enzymes necessary for integrity of the fungal cell membrane.|
|•||Fungistatic effects against susceptible organisms.|
|•||Active against Histoplasma capsulatum, Blastomyces dermatitidis, Cryptococcus neoformans, Aspergillus fumigatus, Trichophyton spp., Candida, and tinea unguium.|
Coadministration with cisapride, dofetilide, ergot derivatives (eg, ergotamine), nisoldipine, pimozide, quinidine, triazolam, levacetylmethadol (levomethadyl), oral midazolam, or HMG-CoA reductase inhibitors metabolized by the CYP-450 3A enzyme system (eg, lovastatin, simvastatin); not for treatment of onychomycosis in pregnant women or women contemplating pregnancy; ventricular dysfunction such as CHF or history of CHF; hypersensitivity to any component of the product.
The incidence and type of adverse reaction vary depending on usage and route of administration.CV: Hypertension (3%); hypotension, orthostatic hypotension, tachycardia, vasculitis (1%); CHF (postmarketing).
CNS: Headache (4%); fatigue (3%); depression, dizziness (2%); decreased libido, malaise, somnolence, vertigo (1%); hypoesthesia, paresthesia, peripheral neuropathy (postmarketing).
DERM: Rash (9%); increased sweating (4%); pruritus (3%); skin disorder (2%); hypotension (1%); alopecia, erythema multiforme, exfoliative dermatitis, leukocytoclastic vasculitis, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria (postmarketing).
EENT: Ophthalmic malformations, tinnitus, visual disturbances including blurred vision and diplopia (postmarketing).
GI: Diarrhea, nausea (11%); vomiting (7%); abdominal pain (6%); GI disorders (4%); constipation (2%); anorexia (1%); dysgeusia, dyspepsia (postmarketing).
GU: Abnormal renal function, albuminuria, impotence (1%); erectile dysfunction, menstrual disorder, pollakiuria, urinary incontinence (postmarketing).
HEMA/LYMPH: Leukopenia, neutropenia, thrombocytopenia (postmarketing).
HEPA: Bilirubinemia (6%); elevated liver enzymes (4%); abnormal hepatic function, ALT increased (3%); AST increased, jaundice (2%); hepatitis, hepatotoxicity (some fatal), reversible increases in hepatic enzymes (postmarketing).
M/N: Hypokalemia (9%); hypertriglyceridemia, increased serum creatinine (3%); hypomagnesemia, increased alkaline phosphatase, increased LDH (2%); fluid overload, hypocalcemia, increased BUN (1%).
MUSC: Myalgia, rigors (1%); arthralgia (postmarketing).
RESP: Coughing (4%); increased sputum, dyspnea, pneumonia, sinusitis (2%); pulmonary edema (postmarketing).
OTHER: Fever (7%); edema (4%); chest pain (3%); pain, Pneumocystis carinii infection (2%); anaphylactic, anaphylactoid, and allergic reactions, anaphylaxis, angioneurotic edema, chromosomal and multiple malformations, peripheral edema, serum sickness (postmarketing).
Alfentanil, alfuzosin, almotriptan, alprazolam, aripiprazole, atorvastatin, bosentan, buspirone, busulfan, carbamazepine, cerivastatin, cilostazol, cinacalcet, conivaptan, cyclophosphamide, cyclosporine, diazepam, digoxin, disopyramide, docetaxel, eletriptan, fentanyl, gefitinib, halofantrine, haloperidol, protease inhibitors, quetiapine, risperidone, sildenafil, sirolimus, tacrolimus, tadalafil, tolterodine, trimetrexate, vardenafil, venlafaxine, warfarin, zolpidem
Levels may be elevated by itraconazole, increasing the risk of adverse reactions.
Antacids, carbamazepine, grapefruit juice, H2 -receptor antagonists (eg, cimetidine), isoniazid, orange juice, phenobarbital, phenytoin, proton pump inhibitors
Plasma levels of itraconazole may be decreased.
Calcium blockers (eg, amlodipine, felodipine, nifedipine, verapamil)
Edema has occurred with concomitant dihydropyridine calcium blockers.
Cisapride, dofetilide, eplerenone, ergot alkaloids, levacetylmethadol, lovastatin, nisoldapine, oral midazolam, pimozide, quinidine, ranolazine, simvastatin, triazolam
Serious CV events may occur. Coadministration is contraindicated.
Corticosteroids (eg, budesonide, dexamethasone, methylprednisolone)
The metabolism of these corticosteroids may be inhibited, resulting in increased toxicity.
May decrease therapeutic effects of itraconazole. Administer itraconazole 2 h or more before didanosine.
HMG-CoA reductase inhibitors
Coadministration may increase risk of rhabdomyolysis. Lovastatin and simvastatin coadministration is contraindicated.
Hypoglycemia may occur. Monitor blood glucose.
Macrolide antibiotics (eg, clarithromycin, erythromycin), protease inhibitors (eg, indinavir, ritonavir)
Plasma levels of itraconazole may be increased.
Nevirapine, phenytoin, rifamycins
Reduced plasma levels of itraconazole may occur. Avoid use if possible.
Phenytoin, rifamycins, vinca alkaloids
Levels may be elevated by itraconazole, increasing the risk of adverse reactions. Avoid use if possible.
Therapeutic Classification: antifungals (systemic)
Absorption: Oral absorption is enhanced by food.
Distribution: Tissue concentrations are higher than plasma concentrations. Does not enter CSF; enters breast milk.
Protein Binding: Itraconazole —99.8%; hydroxyitraconazole — 99.5%.
Metabolism/Excretion: Mostly metabolized by the liver and excreted in feces. Hydroxyitraconazole, the major metabolite, has antifungal activity.
Half-life: 21 hr.
|ORAL||RAPID||4 HOUR||12-24 HOUR|
|INTRAVENOUS||UNKNOWN||END OF INFUSION||12-24 HOUR|