Active substanceAsparaginaseAsparaginase
Similar drugsTo uncover
  • L-Asparaginase
    lyophilizate w / m d / infusion 
  • Asparaginase medak
    lyophilizate w / m in / in 
    medac GmbH     Germany
  • Vero-Asparaginase
    lyophilizate w / m in / in 
    LENS-PHARM, LLC     Russia
  • Dosage form: & nbsplyophilizate for the preparation of solution for intravenous and intramuscular administration
    Composition:

    1 bottle contains:

    active substance: L- asparaginase 5000 ME or 10,000 ME

    Excipients: no.

    Description:

    White or almost white lyophilized mass or powder.

    Pharmacotherapeutic group:Antitumor agent - enzyme
    ATX: & nbsp

    L.01.X.X   Other antineoplastic agents

    L.01.X.X.02   Asparaginase

    Pharmacodynamics:Asparaginase is an enzyme that catalyzes the cleavage of the amino acid - asparagine, necessary for the vital activity of cells. The maximum of its activity in suppressing proliferation is noted in the postmitotic G1phase of the cell cycle. It is believed that the action of asparaginase is based on a decrease in the level of asparagine in leukemic tumor cells, which, unlike normal cells, are not able to synthesize their own asparagine. As a result, protein synthesis is destroyed, as well as DNA and RNA synthesis.
    Pharmacokinetics:

    The maximum concentration in blood plasma is achieved with intravenous administration in the first minutes, with intramuscular injection - after 14-24 hours. 30% of the drug binds to plasma proteins. Asparaginase penetrates into the reticulo-endothelial system and slowly decomposes to inactive substances. The half-life with intravenous administration varies from 8 to 30 hours, with intramuscular injection it is 39-49 hours.

    With daily use of the drug it is possible to maintain its sufficient level in the blood, and traces of the enzyme can be detected in the blood plasma for another 10 days after the end of the course of treatment. In cerebrospinal fluid, less than 1% of the administered dose is determined.

    The route of excretion of the drug is not established. In urine, the drug appears only in trace amounts.

    Indications:

    Acute lymphoblastic leukemia in children and adults;

    Non-Hodgkin's lymphomas in children.

    Contraindications:

    - Pancreatitis is currently or in anamnesis, as there are cases of development of acute hemorrhagic pancreatitis after the administration of asparaginase,

    - Allergic reactions to asparaginase, obtained from E. coli strains, in anamnesis,

    - Pregnancy and the period of breastfeeding.

    Carefully:CNS diseases, diabetes, acute infections (including varicella, herpes zoster), gout (history), nephrolithiasis, disorders of the hemostatic system.
    Dosing and Administration:

    Treatment with asparaginase medaka should be performed only by a doctor-oncohematologist who has experience in carrying out antitumoral chemotherapy.

    Before initiating or resuming therapy, a prik test or an intradermal test with the drug should be performed before the risk of an IgE mediated hypersensitivity reaction is reduced.

    Holding the needle (prick) test: 1 drop of the ready to use solution of the drug (. See "Preparation of drug solution") is applied zondoobraznym tool on the inner surface of the forearm and pierce the epidermis via sterile needle drop. Avoid the appearance of blood. After 3 minutes, remove the drug. The result of the reaction is evaluated after 20 minutes: in case of occurrence of hyperemia and / or urticaria from treatment with L-asparaginase should be discarded.

    Conducting an intradermal test: several intradermal injections of asparaginase are carried out in sequence,gradually increasing the concentration of the drug (by preparing a series of appropriate dilutions of the solution). Since hypersensitivity reactions mediated not only by IgE but also by IgG and IgM have been reported, an intravenous test (1000 IU intravenously as a short infusion 1 hour prior to the start of the main dose administration) is recommended before intravenous administration of the drug.

    In monotherapy, unless otherwise indicated, the daily dose for intravenous administration in adults and children is on average 200 IU / kg body weight or 6000 IU /m2 surface of the body. Depending on the individual clinical response, the daily dose can be increased to 1000 IU / kg or more. It is also possible to administer higher single doses (1500 IU / kg or 45000 IU /m2 and more), especially if the drug is not administered on a daily basis (for example, twice a week). When used in such doses, the drug must be administered only intravenously. Usually asparaginase medak is used in combination chemotherapy along with other cytostatics. The method of administration, dose and duration of treatment are determined by the appropriate protocol of therapy. When administered intramuscularly, daily doses are usually from 100 to 400 IU / kg body weight or 3000-12000 IU /m2 surface of the body. At the same time intramuscularly, no more than 5000 ME asparaginase in 2 ml of solution should be administered. If it is necessary to introduce a larger single dose, several injections should be carried out in different places.

    Preparation of the solution

    To prepare the solution of the drug in a vial with a syringe, a 2.0 ml (5000 ME) bottle or 4.0 ml (10000 ME bottle) of water for injection is poured on the inner wall in an orderly manner. Do not direct the water jet directly onto the lyophilizate! To dissolve the contents, slowly rotate the bottle, not shaking, to avoid the formation of foam. The resulting solution may slightly opalescent. The solution prepared in this way is ready for use for intramuscular administration and does not require further dilution in this case. For continuous drip infusion, the calculated amount of Asparaginase honey is diluted in 250-500 ml of 0.9% sodium chloride solution or 5% glucose solution and administered intravenously for several hours. Duration of treatment The duration of treatment is determined individually according to the protocol of chemotherapy.However, in the event of serious side effects or severe organ damage, consideration should be given to the need for interruption of therapy.

    Side effects:

    Asparaginase is an organism that is foreign to the body and can cause immunological reactions. In addition, the use of asparaginase can lead to disorders in the organs and systems of the body, in which intensive protein synthesis is carried out (especially in the liver and pancreas). Because the asparaginase usually used in combination with other drugs, it is often difficult to determine the causal relationship between drug use and any side effect.

    The frequency of occurrence of side effects, used in the following table: very often (1/10), often (1/100, <1/10) infrequently (1/1000, <1/100), rarely (1/10000, <1/1000), very rarely (<1/10000, including individual messages), the frequency is not can be estimated (the frequency can not be determined from the available data).

    Within each group of effects combined according to the frequency of manifestation, side effects are presented depending on the degree of their severity in descending order.

    Type of reactions

    Adverse reactions and their frequency


    manifestations

    Change

    Often: increase in concentration

    laboratory indicators

    amylases in serum

    Violations

    Often: Myelosuppression of all three hematopoiesis germs

    from the blood and

    from mild to moderate severity. Violations of blood clotting due to changes in the processes of protein synthesis; bleeding, disseminated intravascular coagulation (DVS-syndrome), thrombosis.

    lymphatic system, hemostasis system

    Approximately half of cases of severe bleeding and thrombosis are observed in the vessels of the brain and can lead to the development of such disorders as stroke, convulsions, loss of consciousness.

    Rarely: hemolytic anemia.











    Disturbances from the nervous system

    Often: disorders of the central nervous system: excitation, depression, hallucinations, confusion and drowsiness (violations of moderate-level consciousness), violations of the electroencephalogram (decrease in alpha-wave activity, increase in theta and delta wave activity); may be hyperammonemia.

    Rarely: may develop cramps and severe impairment of consciousness,including to whom; reversible delayed leukoencephalopathic syndrome.

    Rarely: tremor of fingers.

    Disorders from the gastrointestinal tract

    Often: gastrointestinal disorders from mild to moderate severity, such as anorexia, nausea, vomiting, abdominal cramps, diarrhea and weight loss.

    Often: acute pancreatitis, disorders of the exocrine function of the pancreas, accompanied by diarrhea.

    Infrequently: mumps.

    Rarely: hemorrhagic or

    necrotic pancreatitis.

    Rarely: pseudocystosis of the pancreas, pancreatitis with fatal outcome, pancreatitis with concomitant acute mumps.

    Disorders from the genitourinary system

    Rarely: acute renal failure.

    Disturbances from the skin and skin appendages

    Often: hypersensitivity reactions.

    Rarely: toxic epidermal necrolysis (Lyell's syndrome).

    Disorders from the endocrine system

    Often: a violation of the endocrine function of the pancreas, accompanied by diabetic ketoacidosis; hyperosmolar hyperglycemia.

    Rarely: transitional secondary hypothyroidism, decrease in the concentration of thyroxine-binding globulin, hypoparathyroidism.

    Metabolic disorders

    Often: changes in blood lipid levels (increase or decrease in cholesterol concentration, increase in triglyceride concentration, increase in the concentration of very low density lipoproteins (VLDL) and decrease in the concentration of low density lipoprotein (LDL), increase in lipoprotein lipase activity). In most cases, these metabolic disturbances are not accompanied by clinical manifestations. Increase in the concentration of blood urea nitrogen due to extrarenal metabolic disorders.

    Infrequently: hyperuricemia. Hyperammonemia.

    Infections and invasions

    The frequency can not be estimated:

    development of infections.

    General disorders and reactions at the site of administration

    Often: pain at the injection site, swelling.

    Often: fever, pain syndrome (pain in the back, joints, in the abdominal area). Very rarely: life-threatening hyperpyrexia.

    Immune system disorders

    Often: allergic reactions: local erythema, urticaria, difficulty breathing.

    Often: anaphylactic shock, bronchospasm.

    Disorders from the hepatobiliary system

    Often: changes in hepatic enzyme activity (a dose-independent increase in the concentration of alkaline phosphatase, serum transaminases, lactate dehydrogenase, serum bilirubin), hyperammonemia, fatty liver infiltration, hypoalbuminemia, which in combination with other factors can lead to the development of edema.

    Rarely: cholestasis, jaundice, necrosis of liver cells and hepatic insufficiency with possible fatal outcome.

    Overdose:

    To date, no cases of an overdose of asparaginase have been reported.

    The specific antidote is not known.

    Treatment: hospitalization, monitoring of vital functions, symptomatic therapy.

    Interaction:

    General patterns: Asparaginase can increase the toxicity of other drugs, affecting liver function.

    Vincristine: increased toxicity and an increased risk of anaphylactic reactions may be associated with the use of vincristine simultaneously or immediately prior to the administration of asparaginase.

    Prednisolone: the use of prednisolone in conjunction with asparaginase may increase the risk of disorders in the blood coagulation system (including a decrease in the concentration of fibrinogen and antithrombin III).

    Methotrexate and cytarabine: can interact with asparaginase in various ways: the previous administration of these drugs may synergistically enhance the effect of asparaginase; the administration of methotrexate and cytarabine after asparaginase may antagonize its effect.

    Anticoagulants: the use of asparaginase may provoke the development of bleeding and / or thrombosis. Therefore, caution should be exercised when using the drug simultaneously with anticoagulants such as coumarin, heparin, dipyridamole, as well as acetylsalicylic acid, other non-steroidal anti-inflammatory drugs.

    Vaccination: as a result of the effects of combined chemotherapy, as well as the impact of the disease itself, concomitant vaccination with live vaccines increases the risk of developing serious infections. Therefore, immunization with live vaccines should be carried out no earlier than 3 months after the completion of the course of antitumor treatment.

    Special instructions:

    Against the background of treatment with asparaginase, the following life threatening complications may occur: anaphylaxis; Hyperglycemic conditions that can be treated with insulin; bleeding disorders requiring replacement therapy with fresh frozen plasma to reduce the risk of bleeding.

    Recommended follow-up examinations and precautions

    Before the start of treatment, it is necessary to conduct a study of kidney function and determine the concentration of electrolytes, transaminases, glucose and protein in the blood.

    After the initiation of treatment with asparaginase, regular blood testing with blood counting, control of electrolytes, urinary excretion, glucose in the blood and urine, hemostasis parameters (activated partial thromboplastin time (APTT), prothrombin time, antithrombin concentration and D- dimer), amylase and lipase of blood, alkaline phosphatase, bilirubin, ammonia, triglycerides, cholesterol, if necessary - very low density lipoproteins (VLDL) and lipoproteins low (LDL) from the start of therapy to the complete normalization of these indicators.

    Control of blood form factors and physical examination should be performed every 4 weeks during the first year after completion of therapy, quarterly for the 2nd and 3rd year, then every six months.

    The risk of developing hypersensitivity reactions increases with the increase in the number of doses administered. However, in rare cases, allergic reactions can occur with the first administration of asparaginase.

    In some patients, the formation of antibodies to asparaginase, which neutralizes its effect, can occur without clinical manifestations of hypersensitivity. However, the presence of such antibodies can lead to accelerated inactivation and accelerated elimination of asparaginase from the body ("silent inactivation" of asparaginase). To detect hypersensitivity or reduce the effectiveness of therapy due to "silent inactivation" during treatment, it is recommended to periodically perform a determination of the concentration of asparaginase in the blood, for example, using the MAAT test system (medac Asparaginase Activity Test). Negative results of the intradermal tests performed before the start of treatment do not exclude the possibility of the development of anaphylactic reactions.

    Depending on the clinical course of the disease, additional studies may be required.

    Immune system disorders

    In case of appearance during the therapy with Asparaginase medak symptoms of allergic reactions treatment with the drug should be stopped immediately. Depending on the severity of the developed allergic reactions, it is necessary to conduct appropriate therapeutic measures: administration of antihistamines, glucocorticosteroids and, if necessary, drugs that stabilize hemodynamics. In most cases, treatment can be continued by switching to another asparaginase preparation.

    Effect on hemopoiesis

    Asparaginase can cause from mild to moderate severity myelosuppression of all three hematopoiesis germs; in general, it does not have any clinical significance for the treatment.

    Blood clotting disorders

    The risk of thrombosis increases with increasing time after completion of treatment. It should be borne in mind that the cause of the above disorders in the blood clotting system, in addition to asparaginase, may be concomitant treatment with other myelosuppressive drugs, as well as the disease itself.

    An increased risk of thrombosis has been reported in children with clotting factor V mutations, resistance to activated protein C, or a decreased concentration of protein S, antithrombin III, or protein C in serum. In such patients, central venous catheters should be avoided whenever possible, as this may increase the risk of thromboembolic complications. When conducting induction therapy in patients with acute lymphoblastic leukemia, the central venous catheter, if possible, should be established after asparaginase treatment is completed.

    When laboratory monitoring of blood coagulability is performed, it is possible to detect signs of disturbance of the blood coagulation system and fibrinolysis, for example, reduction of fibrinogen concentration, coagulation factors IX, XI, antithrombin III, protein C and plasminogen, as well as an increase in the concentration of von Willebrand factor, inhibitor of plasminogen activator type 1 , fragments 1 and 2 of prothrombin, and fibrinogen cleavage products (D-dimers). Fibrinogen can be considered as an indicator of control of the pro- and anticoagulant system.If the concentration of fibrinogen or antithrombin III is significantly reduced, the need for selective substitution therapy should be assessed. Antithrombin III Assign in the form of infusion at a dose of 100% minus the current concentration in the blood serum, measured in percent, multiplied by the body weight in kg. Fibrinogen is introduced in the form of fresh-frozen plasma at a dose of 10-15 ml / kg body weight.

    Thrombocytopenia and sepsis increase the risk of bleeding.

    Influence on the nervous system

    In rare cases, it is possible to develop a reversible leukoencephalopathy syndrome. Symptoms of leukoencephalopathy syndrome are mainly manifested in the form of increased blood pressure, seizures, headache, changes in mental state and acute visual impairment (mainly cortical blindness or cortical hemianopia). Treatment of leukoencephalopathy syndrome is symptomatic. The main measures in these cases are antihypertensive therapy and arresting seizures with antiepileptic drugs. It is also recommended to reduce the dose or interrupt immunosuppressive drug therapy.

    Disorders from the gastrointestinal tract

    There are separate reports on the formation of pseudocyst pseudocysts (for up to 4 months after the end of treatment). In this regard, patients need to conduct appropriate examinations (eg, ultrasound) within 4 months after the last injection of asparaginase. Since the exact pathogenesis of pseudocyst formation is not known, in such cases only symptomatic treatment can be recommended.

    In the literature, 2 cases of mumps not associated with pancreatitis were reported; After stopping the injection of asparaginase, mumps symptoms resolved within a few days.

    Disorders from the endocrine system

    Often observed changes in the endocrine function of the pancreas are manifested mainly in the form of violations of glucose metabolism. In this case, both diabetic ketoacidosis and hyperosmolar hyperglycemia can develop, which are usually amenable to treatment with insulin preparations. Risk factors for developing hyperglycemia include age over 10 years, overweight, Down's syndrome. Violation of the exocrine function of the pancreas can cause diarrhea.

    Metabolic disorders

    The change in the concentration of serum lipids can be caused by the concomitant administration of glucocorticoids.

    With a significant increase in these indicators (for example, at a triglyceride concentration> 2000 mg / dL), careful monitoring is recommended because of the increased risk of developing pancreatitis.

    Common violations

    A rise in body temperature, in most cases passing spontaneously, can be observed after 2-5 hours after the administration of asparaginase. Often observed pain in the joints, back, in the abdomen, is usually associated with allergic reactions and pancreatitis. In very rare life-threatening hyperpyrexia.

    Disorders from the hepatobiliary system

    Violation of protein synthesis can lead to a decrease in the concentration of whey proteins. In the majority of patients, the development of a dose-dependent decrease in serum albumin concentration is possible during treatment. Most violations affect the α2 and β fractions of albumin, while the α1 fraction remains unchanged. Since the concentration of serum albumin is essential for the binding and transport of certain drugs,Serum albumin control is necessary, especially in combination chemotherapy. As a result of hypoalbuminemia, edema can develop. During or after the treatment with asparaginase, the serum amylase concentration may increase. In such cases, further treatment with asparaginase should be suspended. During therapy with the drug and within 3 months after its completion, patients should abstain from sexual activity or use reliable contraceptive measures.

    Effect on the ability to drive transp. cf. and fur:During drug treatment it is necessary to avoid driving and other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Liofilizate for solution for intravenous and intramuscular injection of 5000 ME or 10,000 ME.

    Packaging:

    In a glass bottle. 1 bottle with instructions for use packed in a cardboard box.

    5 cardboard packs containing each 1 bottle and instructions for use are packed in a transparent polymer film.
    Storage conditions:

    In the dark place at a temperature of 2-8 ° C in the original packaging.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012317 / 01
    Date of registration:25.04.2007 / 20.01.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:medac GmbHmedac GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspTIRUFARM, LLCTIRUFARM, LLCRussia
    Information update date: & nbsp27.09.2017
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