Indications
Part of combination chemotherapy in the treatment of
acute lymphocytic leukemia (ALL) in patients who developed
hypersensitivity to E. coli-derived asparaginase.
Action
Catalyst in the conversion of asparagine (an amino
acid) to aspartic acid and ammonia. Depletes asparagine
in leukemic cells. Therapeutic Effects: Death
of leukemic cells.
Pharmacokinetics
Absorption: Bioavailability after IM administration
unknown; IV administration results in complete bioavailability.
Distribution: Remains in the intravascular space.
Poor penetration into the CSF.
Metabolism and Excretion: Slowly sequestered
in the reticuloendothelial system.
Half-life: IV: 8–30 hr; IM: 39–49 hr.
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
IM unknown unknown unknown
IV unknown unknown unknown
Contraindications/Precautions
Contraindicated in: Previous hypersensitivity; History
of pancreatitis with prior L-asparaginase; History of
serious thrombosis or hemorrhagic events with prior Lasparaginase;
Lactation: Lactation.
Use Cautiously in: OB: Use only if the potential
benefit justifies the potential risk to the fetus.
Adverse Reactions/Side Effects
GI: PANCREATITIS,qliver function tests, nausea, vomiting.
Endo: hyperglycemia. Hemat: hemorrhage,
thromboembolic events. Misc: hypersensitivity reactions
including ANAPHYLAXIS, fever.
Interactions
Drug-Drug: None known.
Route/Dosage
IM, IV (Adults and Children): Substitution for
E.coli-derived asparaginase—25,000 International
Units/m2 substituted for each dose of E.coli-derived asparaginase;
Substitution for pegasparagase—25,000
International Units/m2 3 times a wk (Mon/Wed/Fri) for
6 doses substituted for each dose of pegasparagase.
Availability A
Powder for injection: 10,000 International Units/vial.
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