Active substancePegasaspragaPegasaspraga
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  • Onkaspar
    solution w / m in / in 
    medac GmbH     Germany
  • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    1 ml of the preparation contains:

    active substance: PEG-L-asparhinase 750 ME;

    Excipients: sodium dihydrophosphate 1.20 mg, sodium hydrogen phosphate 5.58 mg, sodium chloride 8.50 mg, water for injection up to 1.00 ml.

    Description:

    Colorless transparent or slightly opalescent liquid.

    Pharmacotherapeutic group:Antitumor agent
    ATX: & nbsp

    L.01.X.X   Other antineoplastic agents

    L.01.X.X.24   Pegasaspragase

    Pharmacodynamics:

    Pegasus is the result of covalent binding of native Lasparaginase synthesized by a microorganism E.Coli, with monomethoxypolyethylene glycol.

    The mechanism of action of pegasasprasis does not differ from that of native Lasparaginase and consists in the enzymatic destruction of the amino acid LAsparagine, located in the blood plasma. It is believed that for tumor lymphoblasts, unlike healthy cells, this amino acid is indispensable, since they are not able to synthesize LAsparagine, necessary for their normal life. Destruction of pheaspargazoy amino acids LAsparagine in blood plasma leads to deficiency Lasparagine in tumor lymphoblasts, causes a violation of protein synthesis and death of tumor cells.

    Pharmacokinetics:

    The peak of the concentration of pegaspargas in blood plasma after intravenous administration correlates with the administered dose. The volume of distribution is equivalent to the volume of the plasma. The half-life of pegaspargas in blood plasma is 5.73 ± 3.24 days and significantly longer than the half-life of native asparaginase - 1.28 ± 0.35 days. At the end of a one-hour intravenous infusion of pegasgas, the amino acid LAsparagine in the blood plasma is not detected, while available to determine the value LThe asparaginase is retained in the plasma for at least 15 days after the first administration of pegas gas.

    Indications:

    Onkaspar is used in combination with other antitumor drugs for re-induction therapy of acute lymphoblastic leukemia in children and adults with the development of their hypersensitivity to native forms L-asparhinase.

    Contraindications:

    - Pancreatitis at the time of initiation of treatment or in anamnesis;

    - serious hemorrhagic complications associated with therapy L-asparaginase, in the anamnesis;

    - severe allergic reactions to the active substance or the auxiliaries in the history (generalized urticaria, bronchospasm, laryngeal edema, lowering blood pressure) or other severe adverse reactions to Oncaspar;

    - Pregnancy and the period of breastfeeding.

    Pregnancy and lactation:

    The use of the drug is contraindicated during pregnancy and during lactation.

    It is not known whether Oncaspar penetrates into breast milk, so if it is necessary to administer the drug before the treatment, breastfeeding should be discontinued.

    Dosing and Administration:

    Usually Onkaspar is used in combination therapy in combination with other cytostatics. The drug can be administered as part of induction, consolidation and maintenance therapy.

    In the monotherapy regime, Onkaspar can be used induction only if it is not possible to use other chemotherapeutic drugs included in the combined treatment regimens (such as vincristine, methotrexate, cytarabine, daunorubicin, doxorubicin) due to toxicity or for any other reasons related to the characteristics of the patient.

    Treatment should be performed by a doctor who has experience in chemotherapy and has knowledge of the effects and risks associated with the treatment regimens used.

    When selecting an individual dose should be guided by the data of the medical literature.

    If the doctor is not assigned otherwise, the following dosage regimens and regimens for Oncaspar should be observed.

    Recommended dose is 2500 ME (about 3.3 ml of the drug) / m2 body surface every 14 days.

    Children with a body surface of more than 0.6 m2 2500 IU / m2 every 14 days.

    Children with a body surface less than 0.6 m2 82.5 ME (0.11 ml of the preparation) / kg of body weight. Upon achievement of remission, supportive therapy should be prescribed, while the use of Oncaspar in maintenance therapy should be considered.

    Onkaspar is used intravenously or intramuscularly.

    Intramuscular administration is preferred because of the reduced risk of hepatotoxicity, coagulopathy, digestive and renal disorders, compared with intravenous administration.

    For intravenous administration Onkaspar should be injected drip for 1-2 hours in 100 ml of 0.9% solution of sodium chloride or 5% solution of dextrose.

    With intramuscular administration the volume of the drug must not exceed 2 ml for children and 3 ml for adults. If it is necessary to introduce a larger volume of the drug, it should be injected through several injections at different locations. If the solution is cloudy or there is a deposit, Oncaspar can not be used.

    Do not shake!

    Side effects:

    The drug contains a protein 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 Oncaspar is commonly used in combination with other medicines, it is often difficult to determine the causal relationship between drug use and any side effect.

    The side effects of pegaspargas are largely correlated with the side effects of asparaginase. In this regard, for security reasons, the following side effects include effects not observed to date with the use of Oncaspar, but with asparaginase.

    To indicate the frequency of the following side effects, the following grades are used: very often (> 1/10), often (> 1/100, <1/10) infrequently (> 1/1000, <1/100), rarely (> 1 / 10000, <1/1000), very rarely (<1/10000), the frequency can not be estimated (the frequency can not be determined based on the available data).

    Type of reactions

    Adverse reactions and frequency of their manifestation

    Change in laboratory indicators

    Often: increased concentration of amylase in the blood

    Disturbances from the circulatory and lymphatic systems, hemostasis systems

    Often: myelosuppression of all three hematopoietic germs from mild to moderate severity; disorders of blood clotting due to changes in the processes of protein synthesis; bleeding, disseminated intravascular coagulation (DVS syndrome), thrombosis. Approximately half of cases of serious bleeding and thrombosis occur in the vessels of the brain and can lead to the development of such disorders as stroke, convulsions, headache, loss of consciousness.

    Rarely: hemolytic anemia.

    From the nervous system

    Often: disorders of the central nervous system: agitation,depression, hallucinations, confusion, drowsiness (violations of consciousness of moderate severity); violation of the electroencephalogram (reduction in alpha-wave activity, increase in the activity of theta and delta waves), possibly due to hyperammonemia.

    Rarely: may develop seizures and severe disturbances of consciousness, including to whom; syndrome of posterior reversible leukoencephalopathy.

    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, weight loss.

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

    Infrequently: mumps.

    Rarely: hemorrhagic or necrotic pancreatitis.

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

    From the genitourinary system

    Rarely: acute renal failure.

    Disturbances from the skin and skin appendages

    Often: allergic 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, a decrease in the concentration of thyroxine-binding globulin, hypoparathyroidism.

    Violations

    metabolism

    Often: changes in the concentration of blood lipids (increased or decreased cholesterol concentration, increased triglyceride concentration, increased concentration of lipoproteins very low density (VLDL) and a decrease in the concentration of low density lipoprotein (LDL), an increase in the activity of lipoprotein lipase); in most cases, these metabolic disturbances are not accompanied by clinical manifestations.

    A dose-independent increase in the concentration of blood urea, almost always 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: increased body temperature, pain syndrome (pain in the back, joints, in the abdominal area).

    Rarely: life-threatening hyperpyrexia.

    Immune system disorders

    Often: allergic reactions (local erythema, urticaria, skin itching, angioedema, hyperthermia, myalgia, dyspnea), bronchospasm, tachycardia, lowering of blood pressure, anaphylactic shock.

    Disorders from the hepatobiliary system

    Often: changes in hepatic enzyme activity (including dose-dependent increase in activity of alkaline phosphatase, serum transaminases, lactate dehydrogenase, serum bilirubin concentration), fatty liver infiltration, hypoalbuminemia, which can lead to the development of a complex of symptoms including edema.

    Rarely: cholestasis, jaundice, necrosis of liver cells and liver failure with a potentially fatal outcome.

    Overdose:

    The antidote for Onkaspar is unknown. Anaphylactic reactions require immediate administration of epinephrine, glucocorticosteroids, antihistamines and the use of oxygen.

    3 patients received 10,000 IU / m2 Onkaspara intravenously drip. One of them showed a slight increase in serum liver transaminases, another developed a rash 10 minutes after the start of the infusion, which occurred after slowing the rate of infusion and prescribing antihistamines. The third patient had no side effects.

    Interaction:

    The reduction in the concentration of serum proteins by pegasus is likely to increase the toxicity of other drugs that bind to the whey protein.

    In addition, due to the inhibition of protein synthesis and cell replication pegasgas can influence the action of such drugs as methotrexate, the pharmacotherapeutic effect of which is associated with cellular replication.

    Pegasus is able to increase the toxicity of other drugs, affecting liver function.

    Pegaspargas can affect the metabolism of other drugs, especially in the liver.

    The use of pehaspargase can cause a change in the concentration of clotting factors, which in turn can lead to an increased risk of bleeding and / or thrombosis. Therefore, caution should be exercised when using Oncaspar together with medicinal productsdrugs that affect blood clotting and platelet aggregation, such as coumarin, heparin, dipyridamole, acetylsalicylic acid, non-steroidal anti-inflammatory drugs.

    The use of vincristine at the same time or immediately prior to the administration of pegaspargasis can lead to an increase in toxicity and increases the risk of anaphylactic reactions.

    The use of prednisolone in conjunction with pegas gas may increase the risk of disorders in the blood coagulation system (including a decrease in the concentration of fibrinogen and antithrombin III in the blood serum).

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

    Vaccination with live vaccines when it is performed against a background of combined chemotherapy increases the risk of developing serious infections, including because of the influence of the disease itself. Therefore, immunization with live vaccines should be carried out no earlier than 3 months after the completion of the course of antitumor treatment.

    During the treatment with Oncaspar, alcohol should be avoided.

    Special instructions:

    Possible hypersensitivity reactions, including life-threatening anaphylactic reactions, are more common in patients with known hypersensitivity to other forms L-asparhinase. The risk of developing hypersensitivity reactions increases with the increase in the number of doses administered. However, in rare cases, allergic reactions can develop with the first administration of pegasasprasis.

    The routine rule should be compulsory observation of the patient within 1 hour after the end of the drug administration and availability of available resuscitative equipment and drugs for the treatment of anaphylaxis (epinephrine, oxygen, glucocorticosteroid preparations, etc.). In case of allergic reactions, the drug should be discontinued immediately and the necessary medical measures taken.

    Patients should be informed of possible hypersensitivity reactions to Oncaspar, including the possible rapid development of anaphylactic reactions.

    In some patients, the formation of antibodies to pegasparas, which is a foreign protein, can occur without clinical manifestations of hypersensitivity. However, the presence of such antibodies can lead to accelerated inactivation and accelerated elimination of pegasus from the body ("silent inactivation" of pegaspargas). Therefore, during the treatment it is recommended to periodically measure the concentration of the drug 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.

    Within 2-5 hours after the administration of the drug, there may be an increase in body temperature, which in most cases passes spontaneously. Often observed pain in the joints, back, in the abdomen, is usually associated with allergic reactions and pancreatitis.

    Pegaspargas 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.

    When assigning pegasas, you should consider the increased risk of bleeding, especially when combined with drugs that reduce blood clotting (such as acetylsalicylic acid and other non-steroidal anti-inflammatory drugs). Patients should be warned about the inadmissibility of simultaneous use of drugs that also increase the risk of bleeding.

    With an increase in the time after completion of treatment, the risk of thrombosis begins to dominate among coagulation disorders. It should be borne in mind that the cause of disorders in the blood clotting system, in addition to pegasasprasis, may be concomitant treatment with other myelosuppressive drugs, as well as the disease itself.

    An increased risk of thrombosis has been described in children with mutations of the clotting factor V, resistance to activated protein C or a reduced protein concentration S, antithrombin III or protein C in the blood serum, during asparaginase treatment. 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 installed after the end of the treatment with pegas gas.

    Because the pegasgas affects the plasma proteins, it is necessary to carry out regular monitoring of the fibrinogen, prothrombin time and partial thromboplastin time.

    In carrying out laboratory monitoring parameters of blood clotting is possible to detect signs of disorders of blood clotting and fibrinolysis, for example, reducing the concentration of fibrinogen, clotting factor IX, XI, antithrombin III, protein C and plasminogen, as well as increase the concentration of von Willebrand factor, plasminogen activator inhibitor 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 administered by infusion at a dose of 100 minus the current concentration in the serum, measured in percent, a value 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.

    When combined therapy with Oncaspar is used, the risk of hepatotoxicity must be considered.

    In combination with hepatotoxic drugs, Onkaspar should be used with caution, while carefully monitoring the liver function. Particular caution should be shown when prescribing the drug to patients with a history of liver failure.

    Violation of protein synthesis can lead to a decrease in the concentration of serum proteins. In most patients, the development of a dose-independent decrease in serum albumin concentration is observed during treatment. Most often violations affect α2 and β fraction of albumin, while the fraction α1 remains unchanged. Since the concentration of serum albumin is essential for the binding and transport of certain drugs, control of serum albumin is necessary, especially in combination chemotherapy. As a result of hypoalbuminemia, edema can develop.

    Due to the presence of separate reports on the formation of pancreatic pseudocysts (during the timeup to 4 months after the end of treatment), patients should undergo appropriate examinations (eg, ultrasound) within 4 months after the last injection of pegas gas. Since the exact pathogenesis of pseudocyst formation is not known, in such cases only supportive treatment can be recommended.

    In the case of significant changes in the concentration of serum lipids, which may be associated, including the simultaneous administration of glucocorticosteroids (eg triglyceride concentrations greater than 2000 mg / 100 ml), careful clinical observation and standard treatment are recommended in view of the increased risk of pancreatitis.

    For early detection of pancreatitis, it is necessary to regularly determine the concentration of amylase in the blood, which can increase during and after the treatment with pegasas. If signs of pancreatitis develop, including an increase in the concentration of amylase, treatment with Oncaspar should be discontinued.

    In the treatment with asparaginase preparations, it is possible to develop mumps that are not associated with pancreatitis, the symptoms of which are resolved within a few days after discontinuation of the asparaginase preparation.

    Violation of the exocrine function of the pancreas can lead to diarrhea.

    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. Possible causes of glucose metabolism disturbances are, on the one hand, a decrease in insulin production due to a violation of protein synthesis under the influence of pegaspargase, on the other hand - a violation of the secretion of insulin or a decrease in the number of insulin receptors. In this regard, in the treatment of pegasasgas, regular monitoring of glucose in the blood and urine should be carried out.

    Risk factors for developing hyperglycemia include age over 10 years, overweight, Down's syndrome.

    To assess the therapeutic effect, you should constantly monitor the parameters of peripheral blood (with the counting of the formed elements) and the function of the bone marrow.

    When combined therapy with Oncaspar is used, it is necessary to take into account the risk of toxicity from the central nervous system.

    In rare cases, it is possible to develop a syndrome of reversible leukoencephalopathy. Symptoms of this 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 the syndrome of the posterior reversible leukoencephalopathy is symptomatic. Priority 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.

    In the course of laboratory studies, in the first days after the initiation of therapy, often a significant decrease in the number of circulating tumor cells (lymphoblasts) is observed, the concentration of leukocytes can be from normal to significantly reduced. In this case, the concentration of uric acid in the blood serum can significantly increase, which is accompanied by a risk of developing uremic nephropathy.

    When prescribing Onkaspar, one should take into account the ability of pegasasprogs to provide immunosuppressive action,which can increase the risk of infection.

    Patients should use reliable contraceptive methods during Oncaspar treatment.

    When dealing with drug Oncaspar care must be taken to avoid contact with skin and mucous membranes, especially getting it in your eyes and inhalation of vapors, as the drug can cause irritation in contact. In case of accidental contact with the skin or mucous membranes, a thorough rinsing of the contact area with a large amount of water should be performed for at least 15 minutes.

    After the treatment, the unused preparation, as well as the used materials, must be disposed of in accordance with the rules adopted in the medical institution.

    Effect on the ability to drive transp. cf. and fur:

    During treatment to avoid traffic management tools and training other potentially hazardous activities that require high concentration and psychomotor speed reactions.

    Form release / dosage:Solution for intravenous and intramuscular injection.
    Packaging:

    At 3750 IU / 5 ml in neutral glass vials, sealed with a rubber stopper with aluminum rolling and a plastic protective cover.

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

    Storage conditions:

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

    Do not freeze!

    Keep out of the reach of children!

    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:П N012651 / 01
    Date of registration:25.04.2007 / 19.01.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:medac GmbHmedac GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspTIRUFARM, LLCTIRUFARM, LLCRussia
    Information update date: & nbsp07.06.2017
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