Active substanceProtamine sulfateProtamine sulfate
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  • Dosage form: & nbspsolution for intravenous administration
    Composition:

    1 ml of the solution contains:

    active substance: protamine sulfate - 10 mg;

    Excipients: sulfuric acid 0.05 M solution - up to pH 4.0-6.0 water for injection - up to 1 ml.

    Description:

    Transparent colorless or with a yellowish tinge solution.

    Pharmacotherapeutic group:hemostatic agent
    ATX: & nbsp

    V.03.A.B   Antidotes

    Pharmacodynamics:

    Protamine sulfate is a specific heparin antagonist. 1 mg of protamine sulfate neutralizes 80-120 ME heparin in the blood. Complexation is due to the abundance of cationic groups (due to arginine), which bind to the anionic centers of heparin. The action of the drug after intravenous injection occurs instantaneously ("on the needle") and lasts for 2 hours. After intravenous administration, a protamine-heparin complex is formed, which can break down with the release of heparin.

    When an overdose can reduce blood clotting, since he himself Protamine sulfate shows anticoagulant activity.

    Indications:

    - Bleeding due to an overdose of heparin;

    - before surgery in patients who take heparin with a therapeutic purpose;

    - after operations on the heart and blood vessels with extracorporeal circulation;

    - Hyperheparinemia.

    Contraindications:

    - Hypersensitivity to the components of the drug;

    - idiopathic or congenital hyperheparinemia (in such cases, the drug is not effective and may increase bleeding);

    - severe arterial hypotension;

    - thrombocytopenia;

    - Insufficiency of the adrenal cortex;

    - taking patients with insulin containing Protamine sulfate, as well as other medicinal productscontaining Protamine sulfate;

    - allergic reactions to fish in the anamnesis.

    There are no data on the use of the drug in children.

    Pregnancy and lactation:

    In pregnant women, the drug should be used only if the expected Benefits for the mother exceed the potential risk to the fetus (in the experiment, adverse effects on the fetus have been identified) and / or the child.

    Dosing and Administration:

    A solution of protamine sulfate is injected slowly intravenously in a stream or drip.The rate of administration should not exceed 5 mg per minute (eg, 50 mg of the drug administered within 10 minutes), since a more rapid administration may cause an anaphylactoid reaction. The dose of the drug depends on the method of administration of heparin. The calculated dose is dissolved in 300-500 ml of 0.9% sodium chloride solution. Do not administer more than 150 mg of protamine sulfate for 1 hour.

    1. With bolus injections of heparin the dose of protamine sulfate decreases depending on the time elapsed from the administration of heparin, since the latter is continuously removed from the body.

    Time past after

    injections of heparin:

    The dose of protamine sulfate

    per 100 IU of heparin:

    15-30 minutes

    1-1.5 mg

    30-60 minutes

    0.5-0.75 mg

    Over 2 hours

    0.25-0.375 mg

    2. If heparin was injected intravenously, it is necessary to stop its infusion and introduce 25-30 mg of protamine sulfate.

    3. With subcutaneous injections of heparin, the dose of protamine sulfate is 1-1,5 mg for every 100 ME heparin. The first 25-50 mg of protamine sulphate should be administered intravenously slowly, and the remaining dose - intravenously drip during 8-16 hours. Probably fractional administration of protamine sulfate, which requires control of activated partial thromboplastin time (APTT). For example, if administered subcutaneously 20000 ME heparin, after 2 hours resorption of heparin from complexes with protamine to 3333 ME heparin, in this regard, the next dose of protamine sulfate is 33 mg.

    4. In the case of using extracorporeal circulation during surgery, the dose of protamine sulfate is 1.5 mg per 100 ME heparin. When determining the dose of protamine, it is necessary to take into account the route of administration of heparin.

    Side effects:

    From the cardiovascular system: lowering of blood pressure, bradycardia.

    From the digestive system: nausea, vomiting.

    From the immune system: skin rash, itching, the development of anaphylactoid reactions.

    Other: a feeling of heat, skin flushing, a feeling of lack of air (with an overly rapid introduction).

    Overdose:

    It can be accompanied by bleeding, since protamine has its own anticoagulant activity.

    Treatment is symptomatic.

    Interaction:

    Pharmaceutically incompatible with cephalosporins and penicillins.

    It is an antagonist of low molecular weight heparins.

    May increase the intensity and duration of action of nondepolarizing muscle relaxants.

    Special instructions:

    The administration is carried out under the control of blood coagulability.

    Before the introduction, you should make sure the adequacy of the blood volume of the patient (hypovolemia increases the risk of collapse).

    Form release / dosage:

    Solution for intravenous administration, 10 mg / ml.

    Packaging:

    5 ml of the drug into neutral glass ampoules.

    5 ampoules are placed in a contour plastic package (tray) made of a polyvinylchloride film or a polyethylene terephthalate film.

    Five ampoules are placed in a contour mesh box made of a polyvinylchloride film or a polyethylene terephthalate film and aluminum foil of a printed lacquered or packaging material.

    1.2 contour plastic packages (pallets) or contour mesh packages together with the instruction for use are placed in a pack of cardboard.

    Packing for hospitals

    20, 25, 50, 100, 200 contour plastic packages (pallets) or contour mesh packages together with instructions for use are placed in a cardboard box.

    Storage conditions:

    In the dark place at a temperature of 4 to 10 ° C, do not allow freezing.

    Keep out of the reach of children.

    Shelf life:

    3 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001025
    Date of registration:18.10.2011
    The owner of the registration certificate:BINERGIYA, CJSC BINERGIYA, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp08.09.2015
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