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

    1 ml of the preparation contains: Protamine sulfate - 10 mg; water for injection up to 1 ml.

    Description:Transparent colorless or with a yellowish tinge of liquid.
    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 units of 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 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, tk. himself Protamine sulfate shows anticoagulant activity.

    Pharmacokinetics:

    No pharmacokinetics studies have been performed.

    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;

    - hypergeparinemia.

    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;

    - patients with insulin containing Protamine sulfate, as well as other medicines containing Protamine sulfate;

    - allergic reactions to fish in the anamnesis.

    The experience of medical use in children is limited.

    Pregnancy and lactation:

    Perhaps, if the expected effect of therapy exceeds the potential risk to the fetus.

    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 can 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 elapsed since

    injections of heparin

    The dose of protamine sulfate at

    calculation 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 is administered intravenously drip, 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 per 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.

    The maximum duration of treatment is 3 days.

    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:

    Can be accompanied by bleeding, tk. Protamine has its own anticoagulant activity.

    Treatment is symptomatic.

    Interaction:

    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:

    2 ml or 5 ml in ampoules.

    5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film.

    1 or 2 contour mesh packages together with the instruction for use and the ampoule ampoule or ampoule scarifier are placed in a pack of cardboard.

    5 or 10 ampoules, together with an instruction for use and a scarifier ampoule or a knife ampoule, are placed in a box of cardboard with a corrugated liner.

    When using ampoules with a point or a ring of fracture, the scriber or ampoule knife is not inserted.

    Storage conditions:

    In the dark place at a temperature of 4 ° C to 25 ° C.

    Do not freeze. Keep out of the reach of children.

    Shelf life:

    4 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-004846/10
    Date of registration:27.05.2010
    The owner of the registration certificate:ELLARA, LTD. ELLARA, LTD. Russia
    Manufacturer: & nbsp
    Information update date: & nbsp08.09.2015
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