黴菌感染
Aspergillosis, Invasive: Treatment of pulmonary and extrapulmonary aspergillosis in immunocompromised and nonimmunocompromised patients who are intolerant of or refractory to amphotericin B therapy
Blastomycosis: Treatment of pulmonary and extrapulmonary blastomycosis in immunocompromised and nonimmunocompromised patients
Histoplasmosis:Including chronic cavitary pulmonary disease and disseminated, nonmeningeal histoplasmosis in immunocompromised and nonimmunocompromised patients.
Onychomycosis: Treatment of onychomycosis of the toenail, with or without fingernail involvement, and onychomycosis of the fingernail caused by dermatophytes (tinea unguium) in nonimmunocompromised patients.

Itraconazole is a synthetic triazole antifungal agent that exerts its effect by blocking the C-demethylation step of cytochrome P450-dependent synthesis of ergosterol, a vital component of the fungal cell membrane.

Absorption
1. Time to peak concentration: (fed) 4.6 h +/- 1.8 h; fasting decreases absorption
2. Bioavailability: 55%
Metabolism
1. Hepatic; P450 CYP3A4
2. Active metabolite: hydroxyitraconazole
3. Elimination Half Life: 64 h +/- 32 h
Excretion
1. Fecal: 3% to 18% unchanged
2. Renal: about 40%, less than 0.03% unchanged
3. Dialyzable: no (hemodialysis); no (peritoneal dialysis)

1. Concomitant use with CYP3A4 substrates
2. Concomitant use with eliglustat in patients that are poor or intermediate metabolizers of CYP2D6, or those taking concomitant strong or moderate CYP2D6 inhibitors
3. Concomitant use with the following drugs in patients with renal or hepatic impairment: colchicine, fesoterodine, telithromycin, and solifenacin
4. Hypersensitivity to itraconazole or any other component of the product
5. Pregnant women or women contemplating pregnancy; do not use for the treatment of onychomycosis.
6. Ventricular dysfunction (eg, CHF); except for life-threatening or serious infections; do not use for the treatment of onychomycosis

Fetal risk has been demonstrated.

Infant risk cannot be ruled out. [MDX]

1. Gastrointestinal: Diarrhea, nausea, vomiting, abdominal pain
2. Cardiovascular: Edema
3. Central nervous system: Headache
4. Dermatologic: Skin rash
5. Hepatic: Abnormal hepatic function tests, increased liver enzymes
6. Respiratory: Rhinitis, upper respiratory tract infection, sinusitis
7. Miscellaneous: Fever (2% to 7%)

Aspergillosis, Invasive, prophylaxis:
1. Usual dose: 200 mg PO Q12H
2. Allogeneic stem cell transplant recipients: duration is at least 75 days if tolerated
3. Graft-versus-host disease: 16 wks or until the daily steroid dose is less than 10 mg prednisolone equivalents
Aspergillosis, Invasive, salvage therapy:
1. Usual dose: 200 mg PO QD up to a MAX of 200 mg BID
2. Life-threatening situations: 200 mg PO TID for 3 days (loading dose), followed by 200 mg PO QD or BID; continue for at least 3 months and until evidence of improvement
Blastomycosis:
1. Usual dose: 200 mg PO QD up to a MAX of 200 mg BID (for progressive fungal disease); continue for at least 3 months and until evidence of improvement
2. Life-threatening situations: 200 mg PO TID for 3 days (loading dose), followed by 200 mg QD to BID (for progressive fungal disease); continue for at least 3 months and until evidence of clinical and laboratory improvement
3. Mild-to-moderate pulmonary or disseminated disease: 200 mg PO TID for 3 days (loading dose), followed by 200 mg PO QD or BID for 6-12 months
4. CNS disease, stepdown therapy (after initial treatment with a lipid formulation amphotericin B), 200 mg PO BID to TID for at least 1 year and until resolution of cerebrospinal fluid abnormalities
Histoplasmosis, Disseminated:
1. Mild to moderate disease: 200 mg PO TID for 3 days, followed by 200 mg BID for at least 12 months
2. Moderately severe to severe disease, stepdown therapy after initial therapy with amphotericin B (deoxycholate or lipid formulation): 200 mg PO TID for 3 days, followed by 200 mg BID for at least 12 months
3. Lifelong suppressive therapy: 200 mg PO QD
Onychomycosis due to dermatophyte
1. Fingernails only: 200 mg PO BID for 1 week, off drug for 3 weeks, repeat 200 mg BID for 1 week
2. Ttoenails with or without fingernail involvement: 200 mg PO QD for 12 weeks

Solution prepatation is recommended.

Dose adjustment is not required

Dose adjustment is not required