Active substanceCoagulation factor VIIICoagulation factor VIII
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  • Emoklot D.I.
    lyophilizate d / infusion 
    Kedrion SpA     Italy
  • Dosage form: & nbsplyophilizate for solution for infusion
    Composition:

    EMOKLOT D.I. (bottles)

    250 ME

    500 ME

    1000 ME

    Active substance:
    The activity of the human factor of coagulation of VIII complex with von Willebrand factor

    Specific activity (in the final product)

    250 ME

    500 ME

    1000 ME

    At least 80 IU / mg protein

    Excipients:

    Sodium Citrate

    14.7 mg

    29.4 mg

    29.4 mg

    Sodium chloride

    33.0 mg

    66.0 mg

    66.0 mg

    Glycine

    45.0 mg

    90.0 mg

    90.0 mg

    Calcium chloride

    0.73 mg

    1.47 mg

    1.47 mg

    SOLVENT

    Water for injections

    5 ml

    10 ml

    10 ml

    Description:

    Lyophilizate white or light yellow color.

    After dissolution, a clear or slightly opalescent colorless or light yellowth solution.

    Pharmacotherapeutic group:hemostatic agent
    ATX: & nbsp

    B.02.B.D.02   Coagulation factor VIII

    Pharmacodynamics:

    The complex of factors VIII (VIII) and Willebrand consists of two molecules with different physiological functions. Activated factor fVIII acts as a cofactor activating coagulation factor IX accelerating conversion of the coagulation factor X into the active form. Activated coagulation factor X converts prothrombin into thrombin. Then thrombin converts fibrinogen into fibrin and forms a thrombus. Decreased level of FVIII leads to the development of hemophilia A. Substitution therapy increases the level of fVIII in plasma, which temporarily corrects the deficiency of the factor in the blood plasma and prevents bleeding. Willebrand factor stabilizes the FVIII molecule, promotes adhesion of platelets to the site of vascular injury, participates in platelet aggregation and is necessary in the substitution therapy of patients with Willebrand disease.

    FVIII derived from human plasma is an ordinary constituent of human plasma and acts as an endogenous factor. It is not possible to determine the toxicity of single injections, while high doses lead to an overdose. The determination of the toxicity of repeated doses in animals is not possible due to the appearance of antibodies to a foreign protein. Clinical studies have shown the absence of oncogenic and mutagenic effects of FVIII, obtained from human plasma, experimental studies in this case are inexpedient.

    Pharmacokinetics:After the administration, the activity FVIII in the blood plasma reaches 80-120% of the required (calculated) activity level of this factor. Activity FVIII in blood plasma decreases by a two-phase eexponential curve. In the initial phase, the distribution between the vascular bed and tissues occurs with a half-life of plasma from 3 to 6 hours; approximately 2 / 3-3 / 4 FVIII remains in the bloodstream. In the subsequent slow phase (which probably reflects consumption FVIII) the half-life period varies from 8 to 20 hours (an average of 12 hours). This reflects the true biological half-life.
    Indications:

    Treatment and prevention of bleeding caused by a hereditary and acute deficiency of the blood coagulation factor VIII (hemophilia A, hemophilia A with a coagulation factor inhibitor VIII, acute deficiency of the coagulation factor VIII due to the spontaneous appearance of a factor inhibitor).

    Von Willebrand's disease.

    Contraindications:

    Hypersensitivity to the components of the drug.

    Pregnancy and lactation:

    When using the drug by pregnant women during clinical studies, complications are not established. Experimental studies in animals are not sufficient to assess the effect on reproductive function, the development of the embryo or fetus, the course of pregnancy, peri- and postnatal development of the child.Therefore, the drug can be used only if the expected benefit for a woman exceeds the possible risk to the fetus and infant.

    Dosing and Administration:

    Treatment should begin under the strict supervision of a doctor who has experience in the therapy of hemophilia.

    Doses and duration of substitution therapy depends on the severity of the deficiency of the coagulation factor VIII, the localization and volume of bleeding, and the severity of the clinical condition of the patient.

    Calculation of the required dose of coagulation factor VIII (FVIII) is based on empirical data: 1 IU FVIII / kg of body weight increases the activity of the clotting factor in plasma by 1.5-2%.

    Given the initial activity of the coagulation factor VIII in the patient's plasma, the calculation of the required dose of the drug is carried out according to the formula:

    The required dose (ME FVIII) = body weight of the patient (kg) x required increase in activity FVIII (%) x 0.5.

    The total dose and frequency of drug administration should always be correlated with clinical efficacy in each case.

    The following table reflects the level of FVIII required to stop bleeding or prevent bleeding during surgical interventions, as well as the duration of maintenance of the necessary activity of FVIII in the blood plasma of the patient.

    Severity of bleeding /

    volume of surgical intervention

    Required level of fVIII in blood plasma

    (% from the norm)

    Multiplicity of administration /

    duration of therapy

    Minor bleeding

    Hemorrhages in the joints

    30

    At least 1 day, until the bleeding stops

    Significant bleeding

    40-50

    Repeat infusions every 12-24 hours for 3-4 days or more until the bleeding stops completely, the wound is healed, or the pain stops and the joint movements recovered.

    Pronounced hemarthrosis, muscle hemorrhage, tooth extraction, slight head injury, mild surgical interventions, bleeding from the oral cavity

    Life-threatening bleeding

    Severe surgery, gastrointestinal bleeding, intra-abdominal, intracranial or pleural bleeding, fractures

    60-100

    Within 7 days, then maintenance therapy for the next 7 days (activity FVIII 30-60%)

    In some cases, more than calculated amounts of the drug may be needed, especially at the start of therapy.

    During the course of treatment it is recommended to determine the activity of FVIII for correcting the dose of the drug and the frequency of its administration. In the case of extensive surgical interventions, accurate monitoring of substitution therapy is particularly needed, which implies the determination of the activity of FVIII in blood plasma.Patients may have a different response to the administration of FVIII, giving different levels in vivo release of the factor and its half-life.

    Patients should be checked for the appearance of inhibitors of FVIII. If the expected increase in the activity of the factor in the blood plasma is not achieved, or the bleeding is not controlled by the appropriate dose, then it is necessary to conduct a test for the presence of inhibitors of vWIII activity. If the inhibitor is present in an amount of less than 10BE (BetaZedEnits) in ml, the administration of an additional amount of the human coagulation factor VIII can neutralize the inhibitor. Patients with an inhibitor level of more than 10 BY or a high history of an anesthetic are recommended to administer a concentrate of the prothrombin complex.

    In patients with von Willebrand's disease, substitution therapy is carried out empirically and depends on the level of fVIII in the blood plasma, which is measured daily (before and after the administration of the drug EHIKLOT DI). Monitoring of bleeding time is mandatory in cases of bleeding from mucous and non-stop, despite adequate level VIII: C in blood plasma. In these patients, the dose of EMOKLOT D.I. it is necessary to increase.

    Cooking method

    EMOKLOT D.I.must be dissolved immediately before administration. Do not use the solution in the presence of flaky and other mechanical inclusions in it. The drug is administered intravenously for 3-5 minutes under the control of the patient's pulse.

    Add the solvent to the lyophilized substance through a double needle and rotate the vial with the concentrate until completely dissolved. The lyophilized substance can be dissolved more quickly if the solvent is heated in a water bath to a temperature of no higher than 37 ° C. With incomplete dissolution of the drug, it will be difficult to filter through the filter needle. To avoid foaming, the solvent must be slowly poured onto the wall of the vial with the lyophilized preparation. After the preparation of the solution, it must be dialed into the syringe using a filter needle, after which the needle is changed and, using the injection equipment from the supplied kit, enter the drug intravenously at the indicated rate.

    Side effects:

    Rarely, hypersensitivity reactions, fever.

    In patients with hemophilia A, antibodies (inhibitors) may appear to the coagulation factor VIII, which manifests itself as an ineffective clinical response.In this case it is recommended to contact a specialized hemophilic center.

    Overdose:

    There is no evidence of symptoms of an overdose of the human coagulation factor VIII.

    Interaction:

    The interaction of the human coagulation factor VIII with other drugs is unknown.

    For the introduction, only the tested injection kits from the enclosed kit can be used.

    Special instructions:

    In the case of the development of a hypersensitivity reaction in the appointment of EMOKLOT D.I. the drug should be discontinued.

    The preparation time of the concentrate should not exceed 3 minutes. After the preparation of the solution, it must be used immediately. The contents of one bottle should be used completely in one introduction. The solution remaining unused, is subject to destruction in the established order.

    EMOKLOT D.I. is prepared from human plasma. When using plasma or products made from human plasma, the transmission of infectious agents, including those not yet known, can not be completely ruled out. To reduce the risk of transmission, careful selection of donors and harvested plasma is carried out by special testing (monitoring of each portion of plasma,used to produce the drug, the absence of HIV type 1 and type 2, HbsAg, antibodies to HCV and ALT level). In addition, everyone is tested pool of plasma polymerase chain reaction to detect the genome of viral hepatitis C. In addition to testing in the production process, double viral inactivation is used (solvent-detergent method and heat treatment at 100 ° C for 30 minutes).

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

    The drug has no effect on the ability to manage vehicles and machinery.

    Form release / dosage:Lyophilizate for the preparation of a solution for infusions, 250 IU, 500 IU or 1000 IU.
    Packaging:

    EMOKLOT D.I. 250 ME - a vial of clear glass with a lyophilizate containing 250 ME factor VIII, a 5 ml solvent bottle, and a sterile pyrogen-free system (10 ml syringe, needle-catheter needle, needle-adapter, needle-filter, aseptic adhesive) for intravenous infusion of the drug. *

    EMOKLOT D.I. 500 ME - a vial of clear glass with a lyophilizate containing 500 ME factor VIII, a 10 ml solvent bottle, and a sterile, pyrogen-free system (20 ml syringe, needle-catheter needle, needle-adapter, needle-filter, aseptic adhesive plaster) for intravenous infusion of the drug. *

    EMokluot D.I. 1000 ME - a vial of clear glass with lyophilizate containing 1000 ME factor VIII, a 10 ml solvent bottle, and a sterile pyrogen-free system (syringe ml, needle-catheter butterfly, needle-adapter, needle-filter, aseptic adhesive plaster) for intravenous infusion of the drug. *

    * Box with lyophilizate, box with solvent and system in a common cardboard box.

    Storage conditions:At a temperature 2 ° С-8 ° С, in a place protected from light and inaccessible to children.
    The prepared solution should be used immediately.
    Shelf life:If the packaging has not been breached and storage conditions are fully respected, the shelf life is 2 years from the date of manufacture.
    Can not be used after the expiration date.
    Can not use a turbid solution or in the presence of a flocculent deposit in it.
    Terms of leave from pharmacies:On prescription
    Registration number:P N015035 / 01-2003
    Date of registration:07.10.2008
    The owner of the registration certificate:Kedrion SpAKedrion SpA Italy
    Manufacturer: & nbsp
    Representation: & nbspPHARMONYX PHARMONYX Russia
    Information update date: & nbsp14.09.2015
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