Gordox
Gordox: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Gordox
ATX code: B02AV01
Active ingredient: aprotinin (aprotinin)
Producer: Gedeon Richter (Hungary)
Description and photo update: 2019-17-09
Prices in pharmacies: from 177 rubles.
Buy
Gordox is a drug with antifibrinolytic, antiprotease effect, used during coronary artery bypass grafting operations.
Release form and composition
Gordox is produced in the form of a solution for intravenous administration: slightly colored or colorless (in colorless glass ampoules of 10 ml, 5 ampoules in plastic trays, 5 trays in a cardboard box complete with two additional trays).
The composition of 1 ampoule includes:
- Active substance: aprotinin - 100,000 Kallikrein Inactivating Units (KIE);
- Auxiliary components: benzyl alcohol - 100 mg; sodium chloride - 85 mg; water for injection - up to 10 ml.
Pharmacological properties
Pharmacodynamics
Aprotinin is a broad-spectrum proteolytic enzyme inhibitor with antifibrinolytic properties. It forms reversible stoichiometric complexes that are enzyme inhibitors, which causes inhibition of the activity of tissue and plasma plasmin, trypsin, and kallikrein and a subsequent decrease in the fibrinolytic activity of the blood.
Aprotinin is an activator of the contact phase of coagulation activation, initiating coagulation with a simultaneous increase in fibrinolysis. If a heart-lung machine is used in the treatment of a patient, which activates coagulation (this effect is caused by the contact of blood with foreign surfaces), additional inhibition of the functions of plasma kallikrein will minimize the disturbances in the functioning of the coagulation and fibrinolysis systems.
Aprotinin is a modulator of the inflammatory response of a systemic nature, which occurs during cardiopulmonary bypass operations and leads to an interrelated intensification of the processes occurring in the systems of fibrinolysis, hemostasis, activation of humoral and cellular responses. The active component of Gordox inhibits numerous mediators (trypsin, plasmin, kallikrein, etc.), which ensures the formation of thrombin, a decrease in fibrinolysis and a weakening of the inflammatory response. The substance also inhibits the release of inflammatory cytokines and maintains glycoprotein homeostasis. It minimizes the loss of glycoproteins (GP Ib, GP IIb, GP IIIa) by platelets and prevents the expression of anti-inflammatory adherent glycoproteins (C IIb) by granulocytes.
The use of aprotinin in surgery together with a connected heart-lung machine reduces the inflammatory response, which leads to a decrease in the need for blood transfusion and the volume of blood loss, and also reduces the frequency of repeated revisions of the mediastinum in order to find the source of bleeding.
Pharmacokinetics
When administered intravenously, the content of aprotinin in plasma rapidly decreases due to the distribution of the substance in the intercellular space. The initial half-life is 0.3–0.7 hours, and the final half-life is 5–10 hours. Average equilibrium intraoperative plasma concentrations of aprotinin are 175281 CIU / ml in patients to whom the drug is administered in the following regimen: intravenous loading dose of 2,000,000 CIU, 2,000,000 CIU per initial infusion volume, 500,000 CIU every hour throughout the entire time operations in the form of continuous intravenous infusion. With the introduction of half doses, the average equilibrium intraoperative plasma concentrations of Gordox are 110‒164 KIE / ml.
Comparison of the pharmacokinetic parameters of aprotinin in studies conducted in groups of healthy volunteers, patients with diagnosed cardiac pathology, connected to a heart-lung machine, and women with hysterectomy surgery proves the linear pharmacokinetics of Gordox when it is used in the dose range of 50,000-2,000,000 KIE. The degree of binding of aprotinin to plasma proteins is 80%. The active component of Gordox in unchanged form is responsible for 20% of antifibrinolytic activity. The equilibrium volume of distribution reaches approximately 20 liters, and the total clearance is approximately 40 ml / min.
Aprotinin is accumulated in the kidneys and, to a lesser extent, in the cartilage tissue. Its accumulation in the kidneys is carried out due to the binding of epithelial cells localized in the proximal renal tubules with the brush border and accumulation in the phagolysosomes of these cells. Cumulation in cartilage tissue is associated with the affinity of aprotinin, which is a base, and acidic proteoglycans contained in cartilage tissue. The content of aprotinin in other organs is comparable to that in plasma. The lowest level of this substance is determined in the brain, and it practically does not penetrate into the cerebrospinal fluid.
Aprotinin crosses the placental barrier only in strictly limited amounts. This substance is metabolized by lysosomal enzymes in the kidneys, forming inactive metabolites - amino acids and short polypeptide chains. In active form, aprotinin is determined in urine in small concentrations (less than 5% of the administered dose). Within two days, 25-40% of aprotinin is found in the urine in the form of metabolites that do not have pharmacological activity.
In patients with end-stage renal failure, the pharmacokinetics of aprotinin has not been adequately studied. Studies conducted on patients with renal dysfunction have shown that the pharmacokinetic parameters of the drug practically do not change, so there is no need to adjust the dosage regimen.
Indications for use
According to the instructions, Gordox is prescribed for adult patients to prevent intraoperative blood loss and reduce the volume of blood transfusion during coronary artery bypass grafting operations using a heart-lung machine.
Contraindications
- Age up to 18 years (the safety and efficacy of the drug for this age group have not been established);
- Hypersensitivity to drug components.
Instructions for use of Gordoks: method and dosage
Gordox is administered intravenously slowly.
The drug should be administered through the main veins, which cannot be used with the introduction of other drugs. The maximum speed is 5-10 ml per minute. With the introduction of Gordoks, the patient should be in a horizontal position (lying on his back).
Due to the high risk of allergic / anaphylactic reactions, all patients 10 minutes before the administration of the main dose of Gordox need to enter a test dose of 1 ml (10 thousand KIE). In the absence of negative reactions, a therapeutic dose of the drug can be administered. 15 minutes before the administration of Gordox, it is possible to use blockers of histamine H1 and H2 receptors. In any case, it is necessary to provide standard emergency measures that are aimed at treating allergic / anaphylactic reactions.
Gordox is recommended to be used in an initial dose of 1-2 million CIU. The drug should be administered within 15-20 minutes after the onset of anesthesia and before the sternotomy. The next dose of 1-2 million CIU must be added to the primary volume of the heart-lung apparatus. To avoid interaction with heparin and to ensure sufficient dilution of the drug, aprotinin is added to the primary volume during the recirculation period.
After the end of the bolus injection and until the end of the operation, you need to establish a constant infusion with an injection rate of 250-500 thousand KIE per hour. The total amount of the injected drug during the entire course should not exceed 7 million KIU.
Patients with functional impairment of the kidneys, as well as elderly patients, do not need to adjust the dose.
Side effects
During therapy, the following side effects may develop:
- Hematopoietic system: very rarely - coagulopathy, including disseminated intravascular coagulation syndrome;
- Cardiovascular system: infrequently - myocardial infarction, myocardial ischemia, thrombosis / occlusion of coronary arteries, thrombosis, pericardial effusion; rarely - arterial thrombosis (possible manifestation of dysfunctions of such vital organs as the brain, lungs, kidneys); very rarely - pulmonary embolism;
- Urinary system: infrequently - functional disorders of the kidneys, renal failure;
- Local reactions: very rarely - thrombophlebitis, reactions in the area of infusion / injection;
- Allergic reactions: rarely - anaphylactic, allergic, anaphylactoid reactions; very rarely - potentially life-threatening anaphylactic shock.
In patients who receive aprotinin for the first time, the development of anaphylactic or allergic reactions is unlikely. With repeated administration of Gordox, especially with repeated use within 6 months, the incidence of allergic (anaphylactic) reactions can increase up to 5%. The risk of their development increases if the drug has been used more than 2 times within 6 months. Symptoms are usually manifested by disorders of the digestive (nausea), cardiovascular (arterial hypotension), respiratory (bronchospasm / asthma) systems, as well as skin disorders (urticaria, itching, rash). With the development of hypersensitivity reactions during the use of aprotinin, it is necessary to immediately stop its administration and carry out standard emergency measures: infusion therapy, administration of corticosteroids and epinephrine / adrenaline.
Overdose
At the moment, no cases of Gordox overdose have been registered. There is no specific antidote to the drug.
special instructions
During operations on the thoracic aorta using deep cold cardioplegia and the use of a heart-lung machine, Gordox should be used very carefully against the background of adequate heparin therapy.
Aprotinin is not a substitute for heparin.
The use of Gordox can affect various methods of conducting tests that determine the coagulation ability of blood.
The preparation contains benzyl alcohol, the daily dose of which should not exceed 90 mg / kg of body weight.
Immediately before use, Gordox's solution must be visually inspected. Do not use the remains of the drug for subsequent use.
Influence on the ability to drive vehicles and complex mechanisms
There is no information about the effect of Gordox on the ability to drive vehicles and work with complex mechanisms.
Application during pregnancy and lactation
Studies on the effects of the drug on the body of pregnant women have not been conducted. During pregnancy, the appointment of Gordox is permissible only if the potential benefits of therapy for the mother significantly outweigh the possible risks to the fetus. When assessing the benefit / risk ratio, it is necessary to take into account the negative effects on the fetus of severe adverse reactions, sometimes manifested with the introduction of a drug, which include cardiac arrest, anaphylactic reactions, etc., as well as the treatment procedures that are carried out to eliminate these reactions.
The effect of Gordox on lactation is not well understood. The drug is considered potentially safe when it enters the body of a child with breast milk, since the oral bioavailability of aprotinin is minimal.
Drug interactions
Gordox is compatible with 20% hydroxyethylated starch solution, glucose solution and Ringer's lactate solution.
With the simultaneous use of Gordox with urokinase, streptokinase and alteplase, the activity of these drugs decreases.
Gordox should not be mixed with other drugs.
Analogs
Analogs of Gordox are: Aprotex, Aerus, Aprotinin, Ingitril, Trasilol 500,000, Traxolan.
Terms and conditions of storage
Store in a dark place, out of reach of children, at temperatures up to 30 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Gordox
According to reviews, Gordox has established itself as an effective drug in the treatment of acute pancreatitis. There are reports that in patients with such a diagnosis, acute symptoms of the disease disappear after 2-3 days of using the drug. They also claim that Gordox is also suitable for treating children, but this requires strict supervision of a specialist.
Price for Gordox in pharmacies
The approximate price for Gordox in pharmacy chains is 4,700-5,700 rubles (the package includes 25 ampoules).
Gordoks: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Gordox 10000 KIE / ml solution for intravenous administration 10 ml 25 pcs. 177 r Buy |
|
Gordox 10000 KIE / ml concentrate for preparation of solution for intravenous administration 10 ml 5 pcs. RUB 955 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
