Aprotinin (Aprotininum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Inhibitors of fibrinolysis

Included in the formulation
  • Aprotex
    solution d / infusion 
    LENS-PHARM, LLC     Russia
  • Aprotex
    lyophilizate in / in 
    LENS-PHARM, LLC     Russia
  • Aeros®
    aerosol d / inhal. 
    BINNOFARM, CJSC     Russia
  • Vero-Narcap®
    lyophilizate in / in 
    VEROPHARM SA     Russia
  • Gordox®
    solution in / in 
    GEDEON RICHTER, OJSC     Hungary
  • Ingridry
    lyophilizate in / in 
    MICROGEN FGUP Scientific and Production Association     Russia
  • Contracal®
    lyophilizate in / in in / of the abdomen. 
    Teva Pharmaceutical Enterprises Co., Ltd.     Israel
  • Trasilol® 500,000
    solution d / infusion 
    Bayer Pharma AG     Germany
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    ONLS

    АТХ:

    B.02.A.B   Inhibitors of plasma proteinases

    B.02.A.B.01   Aprotinin

    Pharmacodynamics:

    Inhibits proteolytic enzymes in the blood and tissues. Reduces fibrinolytic blood activity, inhibits proteases (plasmin, kallikrein, kinokinase, chymotrypsin). Has a hemostatic effect with coagulopathies.

    The activity of the drug is measured in kallikrein inactivating units (KIE) and antitrypsin (ATPE). Blockade of the kallikrein-kinin system allows the use of aprotinin drug for relief of states of shock of any genesis.

    Pharmacokinetics:

    After intravenous administration it is distributed in extracellular spaces.

    The half-life is 150 minutes, the terminal one is 10 hours.

    Metabolism in the kidney: under the action of lysosomal enzymes, the drug disintegrates and is excreted in the urine as inactive metabolites.

    Indications:

    It is used for the treatment of acute and chronic (at the stage of exacerbation) pancreatitis, with pancreatonecrosis, hyperfibrinolytic bleeding of any genesis, for arresting shock conditions.

    ICD-10

    IX.I70-I79.I74   Embolism and thrombosis of the arteries

    IX.I80-I89.I82   Embolism and thrombosis of other veins

    XI.K80-K87.K85   Acute pancreatitis

    XI.K80-K87.K86.1   Other chronic pancreatitis

    XV.O60-O75.O72   Postpartum hemorrhage

    XVIII.R50-R69.R57.1   Hypovolemic shock

    XVIII.R50-R69.R57.8   Other types of shock

    Contraindications:

    Syndrome disseminated intravascular coagulation, except for the coagulopathy phase.

    I trimester of pregnancy.

    Individual intolerance.

    Carefully:

    It is used with caution in patients with a history of allergic reactions. Before the introduction, a skin test is required.

    Pregnancy and lactation:Recommendations for Food and Drug Administration (US Food and Drug Administration) - Category B. V II-III trimester of pregnancy is used in cases of extreme necessity. There is no evidence of ingestion in breast milk. Contraindicated in lactation.
    Dosing and Administration:

    Intravenous drip or jet (slow).The dose is selected individually, depending on the diagnosis, the patient's condition and the operational situation.

    Pancreatitis: acute - 300 thousand - 10 thousand KIE per day for 2-6 days. With an exacerbation of chronic pancreatitis - 25-50 thousand KIE per day.

    Hyperfibrinolytic coagulopathy: the initial dose is 1 million, the maintenance dose is 50,000 KIU per hour.

    Heart surgery: 2 million KIU (280 mg) at the beginning of anesthesia for 30 minutes, then 500,000 KIU per hour before the end of the surgery.

    Use in children

    At the age of 1 month to 18 years, the following dosing regimen is used: intravenously drip in 200 KIE / kg, after 10 minutes - 10,000 KIU / kg for 20 minutes, after that - 3,000 KIE / kg for 1 hour before complete hemostasis.

    The highest daily dose: for adults - 5 million KIE per day; for children - 20 thousand KIE / kg day.

    The highest single dose: 400 thousand KIE, children - 3 thousand KIE.

    Side effects:

    Cardiovascular system: arterial hypotension, tachycardia.

    Central nervous system: confusion, hallucinations.

    Digestive system: nausea and vomiting with rapid administration.

    Local reaction: thrombophlebitis with prolonged infusion.

    Allergic reactions.

    Overdose:

    Not described.

    Interaction:

    It exhibits a mutual antagonistic effect with simultaneous application with anestreplase, alteplase, streptokinase and urokinase.

    Special instructions:

    In the treatment, the activity of pancreatic enzymes, kallikrein, plasmin and thrombin is monitored.

    When hyperfibrinolysis is used against the background of the introduction of heparin.

    Instructions
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