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Pronunciation |
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(am
foe TER i sin bee LIP id KOM
pleks) |
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U.S. Brand
Names |
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Abelcet™ |
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Generic
Available |
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No |
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Synonyms |
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ABLC |
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Pharmacological Index |
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Antifungal Agent, Parenteral |
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Use |
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Treatment of aspergillosis or any type of progressive fungal infection in
patients who are refractory to or intolerant of conventional amphotericin B
therapy |
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Pregnancy Risk
Factor |
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B |
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Pregnancy/Breast-Feeding
Implications |
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Breast-feeding/lactation: Due to limited data, consider discontinuing nursing
during therapy |
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Contraindications |
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Hypersensitivity to amphotericin or any component in the
formulation |
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Warnings/Precautions |
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Anaphylaxis has been reported with other amphotericin B-containing drugs.
Facilities for cardiopulmonary resuscitation should be available during
administration due to the possibility of anaphylactic reaction. If severe
respiratory distress occurs, the infusion should be immediately discontinued.
During the initial dosing, the drug should be administered under close clinical
observation. Acute reactions (including fever and chills) may occur 1-2 hours
after starting an intravenous infusion. These reactions are usually more common
with the first few doses and generally diminish with subsequent doses. Pulmonary
reactions may occur in neutropenic patients receiving leukocyte transfusions;
separation of the infusions as much as possible is advised. |
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Adverse
Reactions |
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>10%:
Central nervous system: Chills, fever
Renal: Increased serum creatinine
1% to 10%:
Cardiovascular: Hypotension, cardiac arrest
Central nervous system: Headache, pain
Dermatologic: Rash
Endocrine & metabolic: Bilirubinemia, hypokalemia, acidosis
Gastrointestinal: Nausea, vomiting, diarrhea, gastrointestinal hemorrhage,
abdominal pain
Renal: Renal failure
Respiratory: Respiratory failure, dyspnea, pneumonia |
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Drug
Interactions |
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Increased nephrotoxicity: Aminoglycosides, cyclosporine, other nephrotoxic
drugs
Potentiation of hypokalemia: Corticosteroids, corticotropin
Increased digitalis and neuromuscular-blocking agent toxicity due to
hypokalemia
Decreased effect: Pharmacologic antagonism may occur with azole antifungal
agents (eg, miconazole, ketoconazole)
Pulmonary toxicity has occurred with concomitant administration of
amphotericin B and leukocyte transfusions |
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Stability |
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100 mg vials in 20 mL of suspension in single-use vials (no preservative is
present). Intact vials should be stored at 2°C to
8°C (35°F to
46°F) and protected from exposure to light; do not freeze
intact vials. Shake the vial gently until there is no evidence of any yellow
sediment at the bottom. Withdraw the appropriate dose and filter the contents (5
micron filter) prior to dilution. Dilute into D5W to a final
concentration of 1 mg/mL. For pediatric patients and patients with
cardiovascular disease, the drug may be diluted with D5W to a final
concentration of 2 mg/mL.
Do not use an in-line filter <5 microns
Diluted solution is stable for up to 15 hours at 2°C to
8°C (38°F to
46°F) and an additional 6 hours at room temperature
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Mechanism of
Action |
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Binds to ergosterol altering cell membrane permeability in susceptible fungi
and causing leakage of cell components with subsequent cell
death |
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Pharmacodynamics/Kinetics |
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Distribution: Vd: Increases with increasing doses; reflects
increased uptake by tissues (131 L/kg with 5 mg/kg/day)
Half-life: ~24 hours
Clearance: Increases with increasing doses [400 mL/hour/kg (with 5
mg/kg/day)] |
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Usual Dosage |
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Children and Adults: I.V.:
Range: 2.5-5 mg/kg/day as a single infusion
Dosing adjustment in renal impairment: None necessary; effects of
renal impairment are not currently known
Hemodialysis: No supplemental dosage necessary
Peritoneal dialysis: No supplemental dosage necessary
Continuous arteriovenous or venovenous hemofiltration (CAVH/CAVHD): No
supplemental dosage necessary |
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Monitoring
Parameters |
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Renal function (monitor frequently during therapy), electrolytes (especially
potassium and magnesium), liver function tests, temperature, PT/PTT, CBC;
monitor input and output; monitor for signs of hypokalemia (muscle weakness,
cramping, drowsiness, EKG changes, etc) |
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Mental Health: Effects
on Mental Status |
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Sedation is common; may cause delirium |
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Mental Health:
Effects on Psychiatric
Treatment |
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May cause bone marrow suppression; use caution with clozapine and
carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Infusion therapy may take several months. Maintain good personal hygiene to
reduce spread and recurrence of lesions. Maintain adequate hydration (2-3 L/day
of fluids unless instructed to restrict fluid intake). You may experience
postural hypotension (use caution when changing from lying or sitting position
to standing or when climbing stairs); nausea or vomiting (small frequent meals,
frequent mouth care, sucking lozenges, or chewing gum may help). Report chest
pain or palpitations, chills or fever, skin rash, muscle cramping or weakness,
alteration in voiding patterns, CNS disturbances, pain at injection site,
persistent GI disturbance, or other adverse reactions. Breast-feeding
precautions: Do not breast-feed. |
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Nursing
Implications |
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I.V. therapy may take several months; personal hygiene is very important to
help reduce the spread and recurrence of lesions; most skin lesions require 1-3
weeks of therapy; report any hearing loss |
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Dosage Forms |
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Injection: 5 mg/mL (20 mL) |
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References |
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De Marie S,
"Clinical Use of Liposomal and Lipid-Complexed Amphotericin B," J Antimicrob
Chemother, 1994, 33(5):907-16.
Hiemenz JW and Walsh TJ,
"Lipid Formulations of Amphotericin B: Recent Progress and Future Directions,"
Clin Infect Dis, 1996, 22 Suppl 2:S133-44.
Kline S, Larsen TA, Fieber L, et al,
"Limited Toxicity of Prolonged Therapy With High Doses of Amphotericin B Lipid Complex,"
Clin Infect Dis, 1995, 21(5):1154-8.
Patel R,
"Antifungal Agents. Part I. Amphotericin B Preparations and Flucytosine,"
Mayo Clin Proc, 1998, 73(12):1205-25.
Rapp RP, Gubbins PO, and Evans ME, "Amphotericin B Lipid Complex," Ann
Pharmacother, 1997, 31(10):1174-86.
Slain D,
"Lipid-Based Amphotericin B for the Treatment of Fungal Infections,"
Pharmacotherapy, 1999, 19(3):306-23.
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