Asparaginase (Asparaginasum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antineoplastic agents

Included in the formulation
  • L-Asparaginase
    lyophilizate w / m d / infusion 
    OMUTNINSK SCIENTIFIC EXPERIMENTAL-INDUSTRIAL BASE, OJSC     Russia
  • Asparaginase medak
    lyophilizate w / m in / in 
    medac GmbH     Germany
  • Vero-Asparaginase
    lyophilizate w / m in / in 
    LENS-PHARM, LLC     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    L.01.X.X   Other antineoplastic agents

    L.01.X.X.02   Asparaginase

    Pharmacodynamics:

    It causes the hydrolysis of extracellular asparagine to ammonia and aspartic acid, as a result of which protein synthesis in fast-growing tumor cells is disrupted. The cells are fragmented into particles surrounded by membranes, then subjected to phagocytosis.

    Operates on cells that are in G1phase of the cell cycle. Under the action of the drug, the number of blast cells of the bone marrow and peripheral blood is reduced.

    Pharmacokinetics:

    The maximum concentration in blood plasma after intravenous administration is achieved after 14-24 hours. Cumulated after repeated administration after 24 hours.

    The half-life is 8-30 hours with intravenous administration and 39-49 hours - with intramuscular injection; does not depend on the dose, body surface area, age, sex, liver and kidney function, and the duration of the disease. In a small amount (about 1%) it penetrates the blood-brain barrier.It is cleaved in the reticuloendothelial system. The volume of distribution of the drug in plasma is 70-80%. Eliminated by the kidneys.

    Indications:

    It is used for acute and chronic leukemia, T-cell sarcoma, reticulosarcoma and lymphosarcoma.

    ICD-10

    II.C81-C96.C81   Hodgkin's disease [lymphogranulomatosis]

    II.C81-C96.C82   Follicular [nodular] non-Hodgkin's lymphoma

    II.C81-C96.C83   Diffuse non-Hodgkin's lymphoma

    II.C81-C96.C92.1   Chronic myeloid leukemia

    II.C81-C96.C91.1   Chronic lymphocytic leukemia

    II.C81-C96.C91.0   Acute lymphoblastic leukemia

    Contraindications:

    Severe hepatic and renal insufficiency, pancreatic insufficiency, diseases of the central nervous system.

    Individual intolerance.

    Carefully:Inhibition of hematopoiesis after radiation or cytotoxic therapy. Bacterial, viral (chicken pox, herpes) and fungal infections.
    Pregnancy and lactation:

    Recommendations for FDA - Category C. When pregnancy is used in case of emergency. During lactation during treatment, it is recommended to stop breastfeeding. Women of reproductive age are recommended to use reliable contraceptives during treatment.

    Dosing and Administration:

    The dosage regimen is selected by a physician with experience in chemotherapy. The course of treatment is 3-4 weeks.

    The highest daily dose: 400 000 IU.

    The highest single dose: 10,000 IU / m2.

    Side effects:

    Central nervous system: headache, drowsiness, emotional lability, depressive and hallucinatory syndrome.

    Blood coagulation system: decrease in the level of fibrinogen, V and VII factors, rarely - hemorrhage and bleeding.

    Metabolism: hyperglycemia, azotemia, hyperuricemia, hypoalbuminuria.

    Digestive system: attacks of pancreatitis with acute pain and vomiting, loss of appetite, fatty liver hepatosis.

    Side effects develop more often and are more severe in adults than in children.

    Allergic reactions.

    Overdose:

    Collapse state, hemorrhage, extreme severity of side effects.

    Treatment is symptomatic. In severe conditions - transfusion of blood components.

    Interaction:

    Strengthens the action of cytostatics.

    With simultaneous administration with prednisolone and vincristine, the myelotoxic, hyperglycemic, neurotoxic effect of asparazinase increases.

    Special instructions:

    It is forbidden to mix asparaginase with other preparations in one solution.

    It is not recommended to use the drug as a monotherapy.

    When treating asparaginase, vaccination of all family members is not recommended.

    Before the initial introduction of the drug, and if more than 1 week has passed since the last injection, it is necessary to carry out a skin test with 0.1 ml of sodium chloride solution containing 2 IU / ml. The resulting solution is injected subcutaneously into the region of the forearm. The result is evaluated after 3 hours. The formation of a blister or erythema with a diameter of up to 1 cm or more indicates a positive test. In this case, the method of desantification is used, in which the drug at a dose of 1 IU is administered intravenously every 10 minutes to the amount of the required dose.

    With a single intramuscular injection of the drug, the volume of the solution should be at least 2 ml.

    Intravenous administration is recommended for 30 minutes or more.

    In order to prevent the development of nephropathy due to increased formation of uric acid, patients are advised to consume a sufficient amount of liquid.

    If you accidentally get on the skin of the drug should be washed off with running water for 15 minutes or more.

    Instructions
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