Gordox solution 10000 KIE/ml 10ml ampoules, 25pcs

Composition

1 ampoule contains:

Active ingredient:

aprotinin 100000 KIU;

Auxiliary substances:

sodium chloride-85 mg;

benzyl alcohol-100 mg;

water for injection-up to 10 ml

Pharmacological action

It is a broad-spectrum proteolytic enzyme inhibitor with antifibrinolytic properties. Forming reversible stoichiometric complexes – enzyme inhibitors, aprotinin suppresses the activity of plasma and tissue kallikrein, trypsin, plasmin, as a result of which it reduces the fibrinolytic activity of blood.

Aprotinin activates the contact phase of coagulation activation, which initiates coagulation with simultaneous activation of fibrinolysis. Under conditions of using an artificial circulatory system (AIC) and activation of coagulation caused by blood contact with foreign surfaces, additional inhibition of plasma kallikrein will help minimize disorders in the coagulation and fibrinolysis systems.

Aprotinin modulates the systemic inflammatory response that occurs during operations with artificial blood circulation. The systemic inflammatory response leads to an interconnected activation of the hemostasis, fibrinolysis, and cellular and humoral response systems. Aprotinin, by inhibiting numerous mediators (including kallikrein, plasmin, trypsin), weakens the inflammatory response, reduces fibrinolysis and thrombin formation.

Aprotinin inhibits the release of inflammatory cytokines and supports glycoprotein homeostasis. Aprotinin reduces the loss of glycoproteins (GPIb, GPIIb, GPIIa) by platelets and interferes with the expression of anti-inflammatory adhesive glycoproteins (GPllb) by granulocytes.

The use of aprotinin in surgery using AIC reduces the inflammatory response, which is expressed in a decrease in the volume of blood loss and the need for blood transfusion, and a decrease in the frequency of repeated mediastinal revisions to search for the source of bleeding.

Indications

• bleeding and hemorrhage of various origins;
• acute pancreatitis;
• various shocks.

Use during pregnancy and lactation

Research on the use of the drug Gordox was not performed in pregnant women. During pregnancy, use is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus.

When assessing the benefit/risk ratio, one should take into account the negative impact on the fetus of severe adverse reactions possible with the use of the drug, such as anaphylactic reactions, cardiac arrest, etc., as well as therapeutic measures taken to eliminate these reactions.

Application of the drug Gordox during lactation has not been studied. The drug is potentially safe when ingested in breast milk, as it does not have bioavailability when taken orally.

For children under 18 years of age, efficacy and safety have not been established.

Contraindications

Hypersensitivity to the components of the drug.

Side effects

Allergic reactions:  rarely-allergic, anaphylactic, or anaphylactoid reactions; very rarely-anaphylactic shock (potentially life-threatening).

Patients receiving aprotinin for the first time are unlikely to develop allergic or anaphylactic reactions. With repeated use, the frequency of allergic (anaphylactic) reactions can increase up to 5%, especially with repeated use of aprotinin for 6 months. If aprotinin is used repeatedly after more than 6 months, the risk of allergic/anaphylactic reactions is 0.9%.

The risk of severe allergic/anaphylactic reactions increases if aprotinin has been used more than 2 times within 6 months. Even if the repeated use of aprotinin did not cause any symptoms of allergic reactions, subsequent use of the drug can lead to the development of severe allergic reactions or anaphylactic shock, in rare cases with a fatal outcome.

Symptoms of allergic/anaphylactic reactions are manifested by disorders of the cardiovascular system (hypotension), digestive system (nausea), respiratory system (asthma/bronchospasm), skin (pruritus, urticaria, rash).

In case of hypersensitivity reactions when using aprotinin, the drug use should be stopped immediately and standard emergency measures should be provided – infusion therapy, use of epinephrine/epinephrine, corticosteroids.

From the cardiovascular system:  infrequently-myocardial ischemia, coronary artery thrombosis/occlusion, myocardial infarction, pericardial effusion, thrombosis; rarely-arterial thrombosis (with possible manifestation of impaired function of vital organs such as kidneys, lungs, brain); very rarely – pulmonary embolism.

From the hematopoietic system:  very rarely – coagulopathies, including DIC-syndrome.

From the urinary system:  infrequently-impaired renal function, renal failure.

Local reactions:  very rarely – reactions in the area of injection/infusion, thrombophlebitis.

Interaction

With simultaneous use of the drug Gordox with streptokinase, urokinase, alteplase decreases the activity of these drugs.

Pharmaceutical incompatibilities

Gordox is compatible with 20% glucose solution, hydroxyethylated starch solution, Ringer’s lactate solution.

Gordox should not be mixed with other medications.

How to take, course of use and dosage

In/in, slowly.

The maximum rate of use is 5-10 ml/min. When the drug is administered, the patient should be in a supine position. Gordox® should be administered through the main veins and should not be used to administer other drugs.

Due to the high risk of allergic/anaphylactic reactions, all patients should be given a trial dose 1 ml (10 thousand KIU) 10 minutes before the main dose of Gordox®. In the absence of negative reactions, a therapeutic dose of the drug is administered. It is possible to use histamine_H1– and_H2-receptor blockers 15 minutes before the use of Gordox®. In any case, standard emergency measures aimed at treating an allergic/anaphylactic reaction should be provided.

Adults: The initial dose of 1-2 million KIU is administered intravenously slowly for 15-20 minutes after the start of anesthesia and before sternotomy. The next 1-2 million These are added to the primary volume of the heart-lung apparatus. Aprotinin should be added to the primary volume during the recirculation period to ensure sufficient dilution of the drug and prevent interaction with heparin.

After the end of bolus use, a constant infusion is established at a rate of 250-500 thousand KIU/h until the end of the operation. The total amount of aprotinin administered during the entire course should not exceed 7 million KIU.

Patients with impaired renal function: no dosage adjustment is required.

Children: the drug is contraindicated in children under 18 years of age (efficacy and safety have not been established).

Elderly patients: There is no need to change the dosage regimen in elderly patients.

Overdose

Currently, no cases of overdose with the drug have been reported.

There is no antidote to the drug.

Special instructions

When using aprotinin, especially with repeated use of the drug, allergic/anaphylactic reactions may develop. Therefore, before using the drug, it is necessary to carefully evaluate the benefit/risk ratio. 10 minutes before the main dose of Gordox is administered, a trial dose 1 ml (10 thousand mg) is administered. CUE cards).

Histamine H1-and H2-receptor blockers may be used 15 minutes before the introduction of the therapeutic dose of Gordox. However, allergic / anaphylactic reactions may also occur with the introduction of a therapeutic dose of the drug, even if no adverse reactions were observed during the use of the trial dose.

If hypersensitivity reactions occur with the use of aprotinin, the drug should be discontinued immediately and standard emergency measures should be taken to treat allergic/anaphylactic reactions.

When performing thoracic aortic surgery using AIC and deep cold cardioplegia, Gordox should be used with extreme caution against the background of adequate heparin therapy.

Determining the time of activated clotting is not a standardized test for determining the coagulation capacity of blood, and the use of aprotinin may affect different test methods. The Coagulation Measurement Test (ACT) is subject to various dilution and temperature effects. The ACT test with kaolin does not increase to the same extent in the presence of aprotinin as the ACT test with celitis. Due to the difference in protocols, it is recommended to take the minimum values of the ACT test-750 seconds and the ACT test with kaolin-480 seconds in the presence of aprotinin, regardless of the effects of hemodilution and hypothermia.

The standard dose of heparin administered prior to cardiac canulation and the amount of heparin added to the primary volume in the AIC should be at least 350 IU / kg. The additional dose of heparin is determined by the patient’s body weight and the duration of extracorporeal circulation.The method of titration of protamine is not affected by aprotinin. Additional doses of heparin are determined based on the concentrations of heparin calculated by this method.

The concentration of heparin during bypass surgery should not fall below 2.7 U / ml (0.2 mg / kg) or below the level determined before the use of aprotinin. In patients treated with Gordox, neutralization of heparin with protamine should be performed only after interruption of extracorporeal circulation, based on a fixed amount of heparin administered, or under the control of the protamine titration method.

Gordox contains benzyl alcohol. The daily dose of benzyl alcohol should not exceed 90 mg / kg of body weight.

Aprotinin is not a substitute for heparin.

Preparations for parenteral use should be visually monitored immediately before use. Do not use the remaining solution for subsequent use.

Use in pediatrics

Contraindicated in children and adolescents under 18 years of age(efficacy and safety have not been established).

Influence on the ability to drive motor vehicles and manage mechanisms

There are no data on the effect of the drug Gordox on the ability to drive vehicles and work with mechanisms.

Form of production

Solution for intravenous use

Storage conditions

In a dark place, at a temperature not exceeding 30 °C

Shelf life

5 years

Active ingredient

Aprotinin

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Purpose

Adult Doctor’s prescription