ELSPAR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ELSPAR (ELSPAR).
Asparaginase (ELSPAR) catalyzes the deamination of asparagine to aspartic acid and ammonia, depleting circulating asparagine. Leukemic cells with low asparagine synthetase activity rely on exogenous asparagine; depletion inhibits protein synthesis and induces apoptosis.
| Metabolism | Degraded by proteolysis to smaller peptides and amino acids; not significantly metabolized by hepatic enzymes. |
| Excretion | Primarily cleared by the reticuloendothelial system; negligible renal excretion (<5%). Biliary excretion accounts for <1%. |
| Half-life | Terminal elimination half-life is approximately 1.1–1.7 days (26–41 hours) in patients with normal hepatic function; prolonged in hepatic impairment. |
| Protein binding | Minimal protein binding (<5%); not extensively bound to albumin. |
| Volume of Distribution | Vd is approximately 2.2–4.5 L/kg, indicating extensive extravascular distribution, primarily in plasma and interstitial fluid. |
| Bioavailability | Intramuscular: approximately 45–60%; Intravenous: 100%. |
| Onset of Action | Intravenous: 24–48 hours; Intramuscular: 48–72 hours. |
| Duration of Action | Duration of asparagine depletion lasts 14–21 days after a single dose; clinical effects persist accordingly. |
Adult: 200 IU/kg/day IV or IM for 28 days for induction; 50 IU/kg/week IV or IM for maintenance.
| Dosage form | VIAL |
| Renal impairment | No specific dose adjustment; use with caution in severe impairment (CrCl <30 mL/min). |
| Liver impairment | Contraindicated in Child-Pugh class C; reduce dose by 50% in Child-Pugh class B. |
| Pediatric use | Children: 200 IU/kg/day IV or IM for 28 days for induction; 50 IU/kg/week IV or IM for maintenance. |
| Geriatric use | No specific adjustment; monitor for hepatic and renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ELSPAR (ELSPAR).
| Breastfeeding | No data on presence in human milk; M/P ratio unknown. Due to potential for serious adverse reactions in the breastfed infant, advise to discontinue breastfeeding during therapy and for at least 3 months after the last dose. |
| Teratogenic Risk | ELSPAR (asparaginase) is contraindicated in pregnancy. First trimester: high risk of fetal malformations; second and third trimesters: risk of fetal growth restriction and developmental toxicity. |
| Fetal Monitoring |
■ FDA Black Box Warning
Risk of anaphylaxis and serious allergic reactions, including angioedema and urticaria, especially upon repeated administration.
| Serious Effects |
["History of anaphylaxis to asparaginase products","History of pancreatitis during prior asparaginase therapy","Severe hepatic impairment"]
| Precautions | ["Anaphylaxis and hypersensitivity reactions (may require pretreatment and emergency equipment)","Pancreatitis (monitor lipase/amylase; discontinue if pancreatitis develops)","Hepatotoxicity (liver function monitoring)","Thrombosis and hemorrhage (coagulation factor abnormalities, especially decreased fibrinogen and antithrombin III)","Hyperglycemia (glucose monitoring)","Neurotoxicity (including seizures and altered mental status)"] |
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| Monitor complete blood counts, liver function tests, pancreatic enzymes, coagulation parameters, and glucose levels. Fetal monitoring with serial ultrasounds to assess growth and amniotic fluid volume. |
| Fertility Effects | May impair female fertility due to ovarian failure; effects on male fertility unknown. Use effective contraception during treatment and for at least 3 months after. |