Itraconazole

DEA Class; Rx

Common Brand Names; Sporanox, Onmel, Tolsura

• Antifungals, Systemic; 

Oral, azole antifungal agent
Used for blastomycosis, histoplasmosis, aspergillosis, onychomycosis, and oropharyngeal or esophageal candidiasis
Dosage forms not interchangeable

Hypersensitivity

Contraindicated with certain CYP3A4 substrate drugs (see Black Box Warnings)

Coadministration with colchicine, fesoterodine, and solifenacin in patients with varying degrees of renal or hepatic impairment

Coadministration with eliglustat in patients who are poor or intermediated CYP2D6 metabolizers, or if coadministered with strong or moderate CYP2D6 inhibitors

Increased plasma concentrations resulting from coadministration with itraconazole of some of the aforementioned drugs can lead to QT prolongation and ventricular tachyarrhythmias

Treatment of onychomycosis in women who are pregnant or plan to become pregnant

Coadministration with venetoclax in patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) during dose initiation and ramp-up phase of venetoclax

Systemic fungal infections

• Nausea (11%)
• Rash (9%)
• Vomiting (5%)
• Edema (4%)
• Headache (4%)
• Abnormal liver function test results (3%)
• Diarrhea (3%)
• Fever (3%)
• Fatigue (3%)
• Hypertension (3%)
• Pruritus (3%)
• Abdominal pain (2%)
• Dizziness (2%)
• Hypertriglyceridemia (2%)
• Hypokalemia (2%)
• Albuminuria (1%)
• Anorexia (1%)
• Decreased libido (1%)
• Somnolence (1%)
• Anorexia (1%)
• Impotence (1%)

1-10% (Toenail infections)

• Headache (10%)
• Rhinitis (9%)
• Upper respiratory tract infection (8%)
• Sinusitis, injury (7%)
• Diarrhea (4%)
• Dyspepsia (4%)
• Flatulence (4%)
• Abdominal pain (4%)
• Dizziness (4%)
• Rash (4%)
• Elevated liver enzymes (4%)
• Gastrointestinal disorders (4%)
• Rash (3%)
• Cystitis (3%)
• Urinary tract infection (3%)
• Liver function abnormality (3%)
• Myalgia (3%)
• Nausea (3%)
• Hypertension (2%)
• Appetite increased (2%)
• Constipation (2%)
• Gastritis, gastroenteritis (2%)
• Pharyngitis (2%)

Cases of serious hepatotoxicity, including liver failure and death, reported; discontinue if liver disease develops, and perform liver function tests; readministration discouraged

Prolongs QT interval; caution with concurrent QT-prolonging drugs or congenital long QT (see Black Box Warnings for drugs contraindicated for use with itraconazole)

Can cause or exacerbated CHF; not for the treatment of other indications in patients with evidence of ventricular dysfunction unless benefit clearly outweighs risks; risk factors include cardiac disease such as ischemic and valvular disease; significant pulmonary disease such as chronic obstructive pulmonary disease; and renal failure and other edematous disorders; monitor for signs and symptoms of CHF during treatment; if signs or symptoms of CHF appear or worsen during administration, reassess benefit-risk of continuing treatment

Calcium channel blockers can have negative inotropic effects which may be additive to those of itraconazole. when co-administering itraconazole and calcium channel blockers, monitor carefully for signs and symptoms of CHF during treatment due to an increased risk of CHF

Life-threatening cardiac arrhythmias and/or sudden death reported when coadministered with drugs that are CYP3A4 substrates and are associated with arrhythmias with increased systemic exposure (eg, pimozide, methadone, quinidine)

May cause CNS depression, which may impair mental alertness and subsequently impair ability to operate heavy machinery or performing hazardous tasks

Oral capsule and oral solution are not bioequivalent; do not use interchangeably

Parenteral form is incompatible with most aqueous solutions; use dedicated line, and do not mix with other drugs in any way

If peripheral neuropathy occurs that may be attributable to itraconazole, discontinue treatment

If cystic fibrosis patient does not respond to itraconazole, consider switching to alternative therapy; large differences in itraconazole pharmacokinetic parameters observed in cystic fibrosis patients

Transient or permanent hearing loss reported in patients receiving treatment with itraconazole; several reports included concurrent administration of quinidine, which is contraindicated; the hearing loss usually resolves when treatment is stopped but can persist in some patients

Caution with renal impairment; data are limited

There are no data on exposure to itraconazole during pregnancy

Itraconazole is excreted in human milk

No data on the amount of itraconazole in human milk, the effects on the breastfed child, or the effects on milk production

Itraconazole

capsule

• 65mg (Tolsura)
• 100mg (Sporanox, generic)

oral solution

• 10mg/mL (Sporanox, generic)

tablet

• 200mg (Onmel)