Indications
Invasive aspergillosis refractory to, or intolerant of,
other therapies. Candidemia and associated serious infections
(intra-abdominal abscesses, peritonitis, pleural
space infections). Esophageal candidiasis. Suspected
fungal infections in febrile neutropenic patients.
Action
Inhibits the synthesis of (1, 3)-D-glucan, a necessary
component of the fungal cell wall. Therapeutic Effects:
Death of susceptible fungi.
Pharmacokinetics
Absorption: IV administration results in complete
bioavailability.
Distribution: Widely distributed to tissues.
Protein Binding: 97%.
Metabolism and Excretion: Slowly and extensively
metabolized; 1.5% excreted unchanged in
urine.
Half-life: Polyphasic: phase—9–11 hr;
phase—40–50 hr.
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
IV unknown end of infusion
24 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Concurrent
use with cyclosporine.
Use Cautiously in: Moderate hepatic impairment
(pmaintenance dose recommended).
Adverse Reactions/Side Effects
CNS: headache, chills. GI: diarrhea,qliver enzymes,
nausea, vomiting. Resp: bronchospasm. GU:qserum
creatinine. Derm: STEVENS-JOHNSON SYNDROME, TOXIC
EPIDERMAL NECROLYSIS, flushing, pruritis, rash. Local:
venous irritation at injection site. Misc: allergic reactions
including ANAPHYLAXIS, ANGIOEDEMA, fever.
Interactions
Drug-Drug: Concurrent use with cyclosporine is
not recommended due toqrisk of hepatic toxicity. May
pblood levels and effects of tacrolimus. Blood levels
and effectiveness may bepby rifampin; maintenance
dose should beqto 70 mg (in patients with normal
liver function). Blood levels and effectiveness also may
bepby efavirenz, nelfinavir, nevirapine, phenytoin,
dexamethasone, or carbamazepine; anqin
the maintenance dose to 70 mg should be considered
in patients who are not clinically responding.
Route/Dosage
IV (Adults): 70 mg initially followed by 50 mg daily,
duration determined by clinical situation and response;
Esophageal candidiasis—50 mg daily, duration determined
by clinical situation and response.
IV (Children 3mo): 70 mg/m2 (max: 70 mg) initially
followed by 50 mg/m2 daily (max: 70 mg/day),
duration determined by clinical situation and response.
IV (Infants 1 to 3 mo and Neonates): 25 mg/m2/
dose once daily.
Hepatic Impairment
IV (Adults): Moderate hepatic impairment—70 mg
initially followed by 35 mg daily, duration determined
by clinical situation and response.
Availability (generic available)
Powder for injection: 50 mg/vial, 70 mg/vial.
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