Gordoks - instructions for use, reviews, analogs and forms of release (injections in injectable ampoules and droppers in solution) of the drug for the treatment of bleeding, pancreatitis, shock in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Gordoks. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Gordox in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Gordox in the presence of existing structural analogs.Use to treat bleeding and massive blood loss, pancreatitis, shock in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Gordoks - the inhibitor of proteolytic enzymes of a wide spectrum of action, possesses antifibrinolytic properties. Forming reversible stoichiometric complexes - inhibitors of enzymes, aprotinin (the active substance of the drug Gordoks) suppresses the activity of plasma and tissue kallikrein, trypsin, plasmin, which reduces the fibrinolytic activity of the blood.

Gordox activates the contact phase of clotting activation, which initiates coagulation with simultaneous activation of fibrinolysis. In conditions of using the artificial circulation device (AIC) and activation of clotting caused by the contact of blood with foreign surfaces, the additional inhibition of plasma kallikrein will help minimize disorders in clotting and fibrinolysis systems. Aprotinin modulates the systemic inflammatory reaction that occurs during operations in conditions of artificial circulation.A systemic inflammatory reaction leads to interconnected activation of hemostasis systems, fibrinolysis, activation of cellular and humoral response. Aprotinin, by inhibiting numerous mediators (including kallikrein, plasmin, trypsin), weakens the inflammatory reaction, reduces fibrinolysis and thrombin formation.

Aprotinin inhibits the release of inflammatory cytokines and supports the homeostasis of glycoproteins. Aprotinin reduces the loss of glycoproteins (GP1b, GP2b, GP3a) by platelets and prevents the expression of anti-inflammatory adhesive glycoproteins (GP2b) by granulocytes.

The use of Gordox 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, reducing the frequency of repeated revisions of the mediastinum to find the source of bleeding.

Composition

Aprotinin + auxiliary substances.

Pharmacokinetics

After intravenous administration, the concentration of aprotinin in the plasma rapidly decreases due to the distribution in the intercellular space. Comparison of pharmacodynamic parameters of aprotinin in healthy volunteers,in patients with cardiac pathology with the use of the device of artificial circulation, and in women with hysterectomy, showed a linear pharmacokinetics of the drug when doses from 50 thousand to 2 million KIE were administered. 80% of aprotinin binds to plasma proteins and 20% of antifibrinolytic activity is carried out by the preparation in its free form. Aprotinin accumulates in the kidneys, and, to a lesser extent, in the cartilaginous tissue. Accumulation in the kidneys occurs due to binding to the brush border of epithelial cells of the proximal renal tubules and accumulation in phagolysosomes of these cells. Accumulation in the cartilaginous tissue occurs due to the affinity of aprotinin, which is the base, and acid proteoglycans of the cartilaginous tissue. Concentrations of aprotinin in other organs are comparable with the concentration of the drug in plasma. The lowest concentration of the drug is determined in the brain, aprotinin practically does not penetrate into the cerebrospinal fluid. A very limited amount of aprotinin penetrates the placental barrier. Aprotinin is metabolized by lysosomal enzymes in the kidneys to inactive metabolites - short peptide chains and amino acids.Active aprotinin is detected with urine in a small amount (less than 5% of the administered dose). Within 48 hours, 25-40% of aprotinin is defined as inactive metabolites in the urine.

In patients with terminal renal failure pharmacokinetics of aprotinin has not been studied. In the study of patients with impaired renal function, changes in the pharmacokinetic parameters of aprotinin were not detected; correction of the dosing regimen is not required.

Indications

• pancreatitis (acute, exacerbation of chronic), pancreatic necrosis;
• performance of diagnostic studies and operations on the pancreas (prophylaxis of enzymatic autolysis of the pancreas during surgery on it and a number of located organs of the abdominal cavity);
• prevention of acute nonspecific postoperative mumps;
• bleeding on the background of hyperfibrinolysis: post-traumatic, postoperative (especially with operations on the prostate gland, lungs), before, after and during labor (including embolism with amniotic fluid);
• polymenorea;
• angioedema (edema of Quincke);
• shock (toxic, traumatic, burn, hemorrhagic);
• extensive and deep traumatic tissue damage;
• as an auxiliary therapy - coagulopathy, characterized by secondary hyperfibrinolysis (in the initial phase, before the onset of the effect after the use of heparin and the replacement of clotting factors);
• massive bleeding (during thrombolytic therapy), during extracorporeal circulation;
• prevention of postoperative pulmonary embolism and bleeding, fat embolism with polytrauma, especially with fractures of the lower extremities and bones of the skull.

Forms of release

Solution for intravenous administration (injections in ampoules for injections and droppers).

Other dosage forms, be it tablets or capsules, do not exist.

Instructions for use and dosage

Gordoks enter intravenously, slowly (in the form of droppers). The maximum rate of administration is 5-10 ml / min. When the drug is administered, the patient should be in the supine position. Gudox should be injected through the trunk veins, do not use them for the administration of other drugs.

In connection with the high risk of allergic / anaphylactic reactions, a trial dose of 1 ml (10,000 IUI) should be administered to all patients 10 minutes before the introduction of the main dose of Gordox.In the absence of negative reactions, a therapeutic dose of the drug is administered. It is possible to use blockers of histamine H1 and H2 receptors 15 minutes prior to the administration of the drug Gordoks. In any case, standard emergency measures should be provided to treat an allergic / anaphylactic reaction.

Adults should be given an initial dose of 1-2 million KIU; administered intravenously slowly within 15-20 minutes after the onset of anesthesia and before sternotomy. The next 1-2 million KIEs are added to the primary volume of the heart-lung device. Aprotinin should be added to the primary volume during the recycling period to ensure sufficient dilution of the drug and prevent interaction with heparin.

After the end of the bolus injection, 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 KIE.

Patients with impaired renal function, elderly patients do not need dose adjustment.

Side effect

• allergic, anaphylactic, anaphylactoid reactions;
• anaphylactic shock (potentially life-threatening);
• myocardial ischemia;
• thrombosis / occlusion of the coronary arteries;
• myocardial infarction;
• pericardial effusion;
• thromboses;
• arterial thrombosis (with a possible manifestation of impaired function of vital organs such as the kidneys, lungs, brain);
• pulmonary embolism;
• coagulopathy, incl. DIC-syndrome;
• impaired renal function;
• kidney failure;
• reactions in the field of injection / infusion;
• thrombophlebitis.

In patients receiving aprotinin for the first time, the development of allergic or anaphylactic reactions is unlikely. With repeated administration, the incidence of allergic (anaphylactic) reactions may increase to 5%, especially with repeated use of aprotinin for 6 months. With repeated use of aprotinin after more than 6 months, the risk of allergic / anaphylactic reactions is 0.9%. The risk of severe allergic / anaphylactic reactions increases if within 6 months aprotinin was applied more than 2 times. Even in cases when repeated use of aprotinin did not observe symptoms of allergic reactions,the subsequent use of the drug may 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 cardiovascular disorders (arterial hypotension), digestive system (nausea), respiratory system (asthma / bronchospasm), skin (itching, urticaria, rash). If hypersensitivity reactions develop with aprotinin, the drug should be discontinued immediately and standard emergency measures should be taken - infusion therapy, adrenaline / epinephrine, corticosteroids.

Contraindications

• age under 18 years (effectiveness and safety not established);
• hypersensitivity to aprotinin or any of the excipients.

Application in pregnancy and lactation

Studies on the use of the drug Gordox in pregnant women have not been conducted. In pregnancy, use is only possible 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 adverse effect on the fetus of severe adverse reactions that may occur with the use of the drug, such as anaphylactic reactions, cardiac arrest, etc., and the therapeutic measures taken to eliminate these reactions.

The use of the drug Gordoks in the lactation period has not been studied. The drug is potentially safe when ingested with a baby with breast milk, because it does not have bioavailability when taken orally.

Use in children

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

Application in elderly patients

Older patients do not need a dose adjustment.

special instructions

When using aprotinin, especially with repeated use of the drug, it is possible to develop allergic / anaphylactic reactions. Therefore, before using the drug, you should carefully evaluate the benefit / risk ratio. 10 minutes before the introduction of the main dose of Gordoks, a trial dose of 1 ml (10 thousand KIE) is administered. 15 minutes before the introduction of a therapeutic dose of Gordox, it is possible to use blockers of histamine H1 and H2 receptors.However, allergic / anaphylactic reactions may also develop with the administration of a therapeutic dose of the drug, even if no adverse reactions were noted during the administration of the trial dose. If hypersensitivity reactions develop with aprotinin, the drug should be discontinued immediately and standard emergency measures aimed at treating allergic / anaphylactic reactions should be carried out.

When performing an operation on the thoracic aorta using AIC and using deep cold cardioplegia, Gordox should be used very carefully with adequate Heparin therapy.

Determination of the activated clotting time is not a standardized test for determining the coagulation ability of blood, and the use of aprotinin can influence various test methods. The measurement of the degree of coagulation (ACT) is influenced by various effects during dilution and exposure to temperature. The ACT test with kaolin does not increase so much with aprotinin as an ACT test with Celite. Because of 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 sec in the presence of aprotinin, regardless of the effects of hemodilution and hypothermia. The standard dose of heparin administered before cancellation of the heart 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 the extracorporeal circulation period. The method of titration of protamine is not influenced by aprotinin. Additional doses of heparin are determined based on the concentration of heparin, calculated by this method. Concentration of heparin during shunting should not fall below 2.7 U / ml (0.2 mg / kg) or below the level determined prior to the use of aprotinin. In patients treated with Gordox, neutralization of heparin with protamine should be performed only after interrupting the extracorporeal circulation, based on a fixed amount of heparin administered or under the control of the protamine titration method.

Gordoks 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 administration should be visualized immediately before use. Do not use remnants of the solution for later use.

Impact on the ability to drive vehicles and manage mechanisms

Data on the effect of the drug Gordoks on the ability to drive vehicles and work with mechanisms are absent.

Drug Interactions

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

Pharmaceutical incompatibility

Gordoks is compatible with 20% glucose solution, hydroxyethyl starch solution, lactated Ringer's solution.

Gordoks should not be confused with other drugs.

Analogues of the drug Gordoks

Structural analogs for the active substance:

• Aprotex;
• Aeros;
• Inhistril;
• Contrikal;
• Trasilol 500,000;
• Traskolan.

Analogues on the pharmacological group (enzymes and antiferments):

• Abomin;
• Aprotex;
• Acetazolamide;
• Gastenorm forte;
• Hemicellulase;
• Hyaluronidase;
• Diakarb;
• Digestal;
• Digestal forte;
• Dorzolamide hydrochloride;
• Dorzopt;
• Dorzopt Plus;
• Inhistril;
• Iruksol;
• Caripazim;
• Collagenase KK;
• Contrikal;
• Kosopt;
• Creon;
• Lidase;
• Lidase (for injection);
• Longidase;
• Mezim;
• Mezim forte;
• Mikrazim;
• Eyes;
• Normoenzyme;
• Pangrol;
• Panzim Forte;
• Panzinorm;
• Panzinorm forte;
• Pancreatym;
• Pancreatin;
• Pancreatin forte;
• Pankurmen;
• Pantcitrate;
• Papain;
• Penzital;
• Pepphysis;
• Procaripazim;
• Ribonuclease;
• Ronidase;
• Trasilol 500,000;
• Traskolan;
• Trypsin crystalline;
• Trusopt;
• Fabrazim;
• Festal;
• Phlogenzyme;
• Himopsin;
• Chymotrypsin;
• Ceresim;
• Elapraza;
• Enzistal;
• Enterosan;
• Hermitage;
• Unienzym with MPS.

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