Gordox instructions for use, contraindications, side effects, reviews. Gordox will help with problems with the pancreas Gordox side effects

Country of origin

Product group

Fibrinolysis inhibitor - polyvalent inhibitor of plasma proteinases

Release forms

• 10 ml - colorless glass ampoules (5) - plastic cell packaging (5) - cardboard packs

Description of the dosage form

• Concentrate for preparing a solution for intravenous administration Concentrate for preparing a solution for intravenous administration Concentrate for preparing a solution for intravenous administration, colorless or slightly colored, pure

pharmachologic effect

Pharmacokinetics

Special conditions

Compound

• aprotinin 10 thousand KIU/ml Excipients: sodium chloride 85 mg, benzyl alcohol 100 mg, water for up to 10 ml

Gordox indications for use

• - therapy of primary hyperfibrinolytic bleeding (post-traumatic, postoperative / especially during surgical interventions on the prostate gland, lungs/); - open heart surgery to reduce the intensity of bleeding and to reduce the need for blood products; - acute pancreatitis, exacerbation chronic pancreatitis, necrosis of the pancreas; - surgical interventions (including diagnostic) performed on the pancreas and adjacent organs abdominal cavity(to prevent enzymatic autolysis of the pancreas); - shock (toxic, traumatic, burn, hemorrhagic); - extensive and affecting several layers of traumatic tissue damage; - massive bleeding (during thrombolytic therapy); - extracorporeal circulation; - prevention of postoperative pulmonary embolism and bleeding, fat embolism in multiple injuries

Gordox contraindications

• - I and III trimesters of pregnancy; - lactation period ( breastfeeding); - increased sensitivity to aprotinin. The drug may be used with caution during cardiopulmonary by-pass surgery, deep hypothermia, circulatory arrest (increased risk of renal failure and death), if there is a history of indications of the development of allergic reactions or previous therapy with aprotinin, disseminated intravascular coagulation (with the exception of the coagulopathy phase) .

Gordox dosage

• 10000 KIU/ml 100000 KIU/10ml 100 thousand KIU/10ml

Gordox side effects

• From the central nervous system: psychotic reactions, hallucinations, confusion. Allergic reactions: urticaria, itching, rhinitis, conjunctivitis, bronchospasm, anaphylaxis, anaphylactoid reactions ( skin rash, itching, shortness of breath, nausea, increased heart rate - these symptoms can progress to anaphylactic shock with symptoms of circulatory failure, in some cases with death). With repeated administration of the drug, the incidence of anaphylactic reactions is less than 0.5%. Even if the second dose is well tolerated, further administration of aprotinin may cause severe anaphylaxis, the danger of which continues to increase with repeated doses. In some cases, an anaphylactoid reaction is observed after the first dose. If hypersensitivity reactions develop during infusion, administration of the drug should be stopped immediately and, if necessary, standard emergency treatment measures should be taken (for example, administration of epinephrine, corticosteroids, rehydration of the body). At surgical operations on the heart and administration of aprotinin in high doses is possible (

Drug interactions

Storage conditions

• store in a dry place
• keep away from children
• store in a place protected from light

Synonyms

• Aprotex, Aprotimbin, Ingiprol, Ingitril, Kontrikal, Kontrikal 10000, Trasylol, Trasylol 500000, Traskolan

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If the doctor prescribed Gordox, instructions for use for pancreatitis this drug must be strictly observed. One of the pathologies of the pancreas, accompanied by its inflammation, is pancreatitis. The enzymes of the organ begin to behave aggressively, destroying the gland from the inside, causing severe pain. Main method conservative treatment of this disease is the use of antienzymes (substances that inhibit the action of enzymes). One of them is Gordox. It was first created in Hungary from animal raw materials.

Why is Gordox prescribed for pancreatitis?

Gordox contains aprotinin. This is the main active ingredient of Gordox. It is obtained from the organs of cattle. The activity of aprotinin, like the drug itself, is expressed in KIU (kallikrein inactivating unit). Additional components are:

• sodium chloride;
• benzyl alcohol;
• water for injection.

Gordox is available in the form of a solution for injection, colorless or slightly yellowish color without sediment. One ampoule contains 10 ml of the drug, the amount of active substance is 10 thousand KIU per 1 ml (100 thousand KIU per 1 ampoule).

Aprotinin, as the main active ingredient of the drug, finds and destroys enzymes that destroy the pancreas, entering the bloodstream and tissues, and has a hemostatic effect. When hitting gastrointestinal tract inactivated, excreted from the body by the kidneys with urine in a small amount (25-40% of the drug within 48 hours after the first injection).

Gordox for pancreatitis is effective for the prevention and treatment of shock conditions.

For inflammation of the pancreas, Gordox is prescribed in the following cases:

• acute and chronic pancreatitis;
• pancreatic necrosis;
• traumatic, toxic and hemorrhagic shock with pancreatitis.

Instructions for medical use

medicine

GORDOX®

Tradename

Gordox ®

International nonproprietary name

Aprotinin

Dosage form

Solution for injection, 100000 KIU, 10 ml

Compound

10 ml of solution contains

active substance - aprotinin, concentrated solution, 100,000 KIE,

Excipients : sodium chloride, benzyl alcohol, water for injection.

Description

Transparent, colorless or slightly colored solution.

Pharmacotherapeutic group

Hemostatics. Proteolysis inhibitors. Aprotinin

ATX code B02AB01

Pharmacological properties

Pharmacokinetics

After intravenous administration aprotinin is rapidly distributed throughout the extracellular compartment, which is accompanied by a rapid decrease in the concentration of aprotinin in plasma; the half-life ranges from 0.3 to 0.7 hours. Later, in particular, 5 hours after administration, the terminal elimination phase begins, during which the half-life ranges from 5 to 10 hours.

The placenta is probably not completely impermeable to aprotinin, but penetration appears to be extremely slow.

During surgery, mean steady-state plasma drug concentrations in patients receiving aprotinin during cardiac surgery ranged from 175 to 281 KIU/mL using the following regimen:

2 million KIU as the initial IV dose; 2 million KIU per pump initial fill solution and 500,000 KIU per hour as a continuous intravenous infusion throughout the operation. The average steady-state plasma concentration of the drug during surgery after administration of half this dose ranged from 110 to 164 KIU/ml.

Data from pharmacokinetic studies of aprotinin in healthy volunteers, in cardiac patients undergoing cardiopulmonary bypass surgery, and in women undergoing hysterectomy indicate that pharmacokinetic parameters in the dose range from 50,000 KIU to 2 million KIU are linear.

Plasma protein binding was studied ex vivo in rat plasma by ultracentrifugation. About 20% of the antifibrinolytic activity was due to the unbound form in the protein-free layer, and 80% of the drug was bound to serum proteins.

In the steady-state phase, the volume of distribution was about 20 liters, and the total body clearance in humans was about 40 ml per minute.

Aprotinin accumulated in the kidneys and, to a lesser extent, in cartilage tissue.

The accumulation of the drug in the kidneys is the result of the binding of aprotinin to the brush border of the epithelial cells of the proximal tubules, as well as accumulation in the phagolysosomes of these cells. Cumulation in cartilage is determined by the affinity of the basic aprotinin for acidic proteoglycans.

In other organs, the concentration of the drug was generally no different from the content in the serum. The lowest concentration of the drug was observed in the brain; aprotinin practically did not enter the cerebrospinal fluid.

Only a small amount of aprotinin penetrates the placental barrier. The placenta cannot be considered completely impermeable to aprotinin, but the penetration rate is extremely low.

The penetration of aprotinin into breast milk has not been studied. However, because aprotinin is not absorbed after oral administration, aprotinin present in breast milk is not likely to harm the nursing infant, regardless of the amount.

Metabolism, elimination and excretion

The aprotinin molecule in the kidneys is broken down into shorter peptides or amino acids by the action of lysosomal enzymes. In humans, less than 5% of the administered dose of aprotinin is excreted in the urine. Following intravenous administration of 131I-labeled aprotinin to healthy volunteers, 25% to 40% of the labeled substance was excreted within 48 hours in urine in the form of metabolites. These metabolites did not have any enzyme inhibitory activity.

Data on the use of the drug in patients with terminal stage there is no renal failure; however, no clinically significant pharmacokinetic changes or obvious side effects were observed in patients with renal impairment. In this regard, no special dose adjustment is required in such cases.

Pharmacodynamics

Aprotinin is a protease inhibitor molecule wide range, which has antifibrinolytic activity. Forming a reversible stoichiometric enzyme-inhibitor complex, aprotinin in humans inhibits trypsin, plasmin, kallikrein in plasma and tissues, which leads to inhibition of fibrinolysis. In addition, it inhibits the contact phase of blood coagulation activation, which is a factor in starting the coagulation process and stimulating fibrinolysis.

Aprotinin is used during operations under cardiopulmonary bypass because it reduces inflammatory reactions, which leads to a decrease in the need for allogeneic blood transfusion and blood loss, as well as a decrease in the need for repeat mediastinal exploration for bleeding.

Indications for use

Aprotinin is indicated for the prevention of intraoperative blood loss and reduction of blood transfusion in adult patients with high risk large blood losses during isolated cardiopulmonary bypass surgery (i.e. coronary artery bypass surgery not accompanied by other cardiovascular interventions).

Before using aprotinin, the benefit/risk ratio and alternative treatment options should be carefully assessed..

Directions for use and doses

All patients should be tested for IgG antibodies, specific to aprotinin.

Test dose

Due to the risk of an allergic (anaphylactic) reaction, all patients should be given 10,000 KIU (kallikrein inhibitory units) of aprotinin (1 ml) intravenously at least 10 minutes before the initial dosage. If the initial dosage of 1 ml does not cause an allergic reaction, then a therapeutic dosage can be administered.

H 1 and H 2 antagonists can be administered 15 minutes before the aprotinin test. Equipment should be available to provide standard emergency treatment for anaphylactic and allergic reactions.

During open heart surgery (with cardiopulmonary bypass) to reduce blood loss and the need for blood transfusion

Dosage

After induction of anesthesia (but before sternotomy), it is recommended to administer a loading dose of 1 to 2 million KIU by slowly intravenous injection or infusion over 20 - 30 minutes. The next 1 - 2 million KIU should be administered after turning on the heart-lung machine. To avoid physical incompatibility between aprotinin and heparin added to the pump prime solution, each drug should be added to the pump prime solution during recirculation to ensure sufficient dilution of both drugs before they are mixed with each other. After the initial bolus infusion into high dose 250,000 to 500,000 KIU per hour should be administered by continuous infusion until the end of the operation.

In general, the total amount of aprotinin administered during the treatment cycle should not exceed 6 million KIU, which is due to the benzyl alcohol content of the injection solution.

Aprotinin for intravenous administration should be administered through the central venous catheter, which should not be used to administer any other drug.

Gordox ® can only be administered to patients in a supine position; administration should be carried out slowly ( maximum speed- from 5 to 10 ml per minute) by intravenous injection or short-term infusion.

Patients with impaired renal function: According to the clinical experience accumulated to date, no dose adjustment is required.

Use in pediatrics : babies, children younger age, children and adolescents: the effectiveness and safety of the drug in this age group of patients has not been established.

Use in elderly patients : in accordance with currently available clinical experience, elderly patients do not experience any particular reaction to the drug.

Side effects

In patients receiving aprotinin for the first time, the development of allergic or anaphylactic reactions is unlikely. In case of repeated administration, the incidence of allergic (anaphylactic) reactions can reach 5%. In a retrospective analysis of allergic (anaphylactic) reactions, it was shown that their frequency increases if reintroduction takes place within 6 months after primary treatment(incidence is 5% for re-exposure within 6 months and 0.9% for re-exposure after 6 months). In addition, in a retrospective analysis, the incidence of severe anaphylactic reactions was shown to be further increased in patients who received aprotinin more than twice within a 6-month period. Even if the patient tolerated it well re-treatment aprotinin, subsequent administration may cause severe allergic reaction or, in extremely rare cases, fatal anaphylactic shock.

Allergic or anaphylactic reactions affecting individual organ systems manifest themselves in the following forms:

Cardiovascular system: hypotension

Digestive system: nausea

Respiratory system: asthma (bronchospasm)

Skin and its appendages: itching, urticaria, rash

If an allergic reaction develops during injection or infusion, the drug should be stopped immediately. Standard measures should be used emergency assistance, including epinephrine administration, volume replacement, and corticosteroids.

Often (> 1% to< 10%)

- myocardial infarction

Uncommon (>0.1% to< 1%)

Myocardial ischemia, occlusion/thrombosis coronary artery, pericardial effusion

Thrombosis

Renal dysfunction, renal failure, oliguria

Rarely (from > 0.01% to< 0,1%)

Arterial thrombosis (and its forms characteristic of life important organs, for example: kidneys, lungs, brain)

Allergic reactions, anaphylactic/anaphylactoid reactions

Very rarely (< 0,01%)

Reactions occurring at the injection or infusion site, (thrombo)-phlebitis at the site of venipuncture

Pulmonary embolism

Disseminated intravascular coagulation (DIC), coagulopathy

Anaphylactic shock (life-threatening)

Contraindications

Hypersensitivity to the active substance or to any of excipients drug

Children and teenagers up to 18 years of age

Patients who have aprotinin-specific IgG antibodies are at increased risk of anaphylaxis when treated with aprotinin

If testing for specific IgG antibodies against aprotinin before starting treatment is not possible, but it is assumed that the patient has received treatment with aprotinin within the previous 12 months, administration of aprotinin is contraindicated.

Drug interactions

Aprotinin inhibits the action of thrombolytic drugs, including streptokinase, urokinase and alteplase (r-TPA = recombinant tissue plasiminogen activator), and the effect of inhibition is dose dependent.

special instructions

Conducted in Lately Observational studies suggest that treatment with aprotinin may be associated with renal dysfunction, particularly in patients with pre-existing renal impairment. When analyzing the results of placebo-controlled studies carried out in patients undergoing coronary artery bypass surgery, it was shown that in the group receiving aprotinin, there was an increase in serum creatinine levels by 0.5 mg/dl compared with the normal value. Accordingly, before prescribing aprotinin to patients with impaired renal function or at risk of renal damage (for example, during concomitant treatment with aminoglycosides), a careful assessment of the benefit-risk ratio is necessary.

This medicine contains benzyl alcohol. According to European guidelines, daily dosage benzyl alcohol should not exceed 90 mg per kilogram of body weight. Thus, during the treatment cycle, the maximum dosage of aprotinin cannot exceed 6 million KIU.

When using aprotinin, a careful benefit-risk assessment is necessary, especially in patients who have previously used aprotinin (including fibrin filling materials containing aprotinin), as they may develop an allergic reaction. Although most cases of anaphylaxis develop after the resolving dose is administered within 12 months, there are isolated case reports of anaphylactic reactions occurring upon reexposure after 12 months. When conducting aprotinin therapy, it is necessary to have emergency supplies available to treat allergic and anaphylactic reactions.

All patients receiving treatment with aprotinin should first be administered a test dose in order to assess the presence of a tendency to allergic reactions. The test dose should be administered to the patient in the operating room.

H1 and H2 antagonists can be administered 15 minutes before the aprotinin test.

The test dose of aprotinin in all patients should be one milliliter (10,000 KIU), and the patient should be observed for at least 10 minutes before administering the loading dose. However, even despite the absence of complications in the period after the initial dose of 1 ml, a therapeutic dose of aprotinin can cause an anaphylactic reaction. If an anaphylactic reaction develops, the aprotinin infusion should be stopped and the necessary emergency measures taken.

Due to the possibility of developing hypersensitivity reactions, before starting the use of Gordox ® it is necessary to carefully evaluate the benefit-risk ratio in each patient who has already received treatment with aprotinin.

If it is known that the patient has already received or could receive repeated treatment with aprotinin, it is recommended to comply with the following measures precautions. All patients should be administered a test dose of Gordox ® in a volume of 1 milliliter (10,000 KIU) at least 10 minutes before the initial dose. In addition, an H1 antagonist (eg, clemastine) and an H2 antagonist (eg, cimetidine) may be administered 15 minutes before the test dose of Gordox® is administered. If necessary, standard emergency measures should be used to treat an allergic (anaphylactic) reaction.

It should not be forgotten, however, that a therapeutic dose may cause an allergic reaction, even if the patient tolerated the initial 1-mL test dose well without experiencing any undesirable symptoms. If this occurs, the aprotinin infusion should be stopped immediately and standard emergency management measures to treat anaphylactic reactions should be initiated.

Patients treated with Gordox ® had an increased incidence of renal failure and mortality compared with an age-matched control group that had a similar medical history and also underwent kidney surgery. thoracic region aorta under conditions of artificial circulation with circulatory arrest against the background of deep hypothermia. In such cases, Gordox ® can be prescribed only with extreme caution. Appropriate anticoagulant treatment with heparin is necessary.

Additional notes on the use of the drug under conditions of artificial circulation

To maintain adequate anticoagulant activity against the background of artificial circulation during simultaneous use Gordoxa ® , the use of any of the following methods is recommended:

1. a activated clotting time (ABC): ABC cannot be considered a standard coagulation test; interpretation of the results of this test depends on the presence of aprotinin. In addition, the test results are influenced by differences due to dilution and the temperature used under cardiopulmonary bypass conditions. It has been shown that the effect of aprotinin is expressed to a lesser extent in relation to kaolin ABC, in comparison with ABC using diatomaceous earth (celite). Despite the variety of protocols, it is recommended to perform the 750-second ABC test using diatomaceous earth or the 480-second ABC test using kaolin in the presence of aprotinin, regardless of the degree of hemodilution and hypothermia. For advice regarding the interpretation of test results in the presence of Gordox ®, you should contact the manufacturer of the ABC test reagents.

2.administration of constant dosages of heparin: The standard loading dose of heparin that is administered before cardiac catheterization, as well as the amount of heparin that is added to the primary filling solution of the heart-lung machine, should be at least 350 IU/kg. The additional dose of heparin is determined taking into account the patient's body weight and the duration of the intervention under artificial circulation.

3.heparin/protamine titration: The results of this method are not affected by the presence of aprotinin and are therefore acceptable for measuring heparin levels. The relationship between heparin dose and response should be assessed by titrating protamine before administering aprotinin (to determine the heparin loading dose).

Additional heparin can be administered based on the heparin concentration measured by titration with protamine. Heparin concentrations during cardiopulmonary bypass should not fall below 2.7 U/mL (2.0 mg/kg) or below the dose determined in the heparin dose-response test performed prior to administration of aprotinin.

After completion of cardiopulmonary bypass, if the patient received Gordox ® injections, heparin should be neutralized by administering protamine. The amount of protamine should be calculated based on a fixed ratio, which is determined from the amount of heparin administered or calculated using the protamine titration method.

Important:the use of Gordox ® does not mean that the need for heparin is reduced.

Pregnancy and lactation

There are no adequate and well-controlled studies in pregnant women.

Aprotinin should not be used during pregnancy unless the potential benefit outweighs the expected risk. In the event of serious adverse reactions (such as anaphylactic reaction, cardiac arrest, etc.) and during their treatment, the potential risk of harm to the fetus should be taken into account when assessing the risks and benefits.

The ability of aprotinin to be excreted in human breast milk has not been studied.

There is no information on the use of Gordox ® injections during breastfeeding. Given that aprotinin is not absorbed when taken orally, no amount of it present in breast milk is likely to harm a nursing baby.

Features of the effect of the drug on the ability to drive vehicle or potentially dangerous mechanisms

Given the scope of use of the drug, consideration of these effects is irrelevant.

Overdose

Symptoms: manifestations of overdose or intoxication have not been described.

Treatment:there is no specific antidote. Symptomatic treatment is recommended.

Release form and packaging

10 ml in colorless glass ampoules with a breaking point. 5 ampoules are placed in a plastic blister pack.

5-blister packaging along with instructions for medical use in the state and Russian languages ​​are placed in a cardboard box.

Storage conditions

Store in original packaging, protected from light at a temperature not exceeding 30 0 C.

Keep out of the reach of children!

Shelf life

5 years

Do not use after expiration date.

Conditions for dispensing from pharmacies

On prescription

Available for stationary use only

Name and country of the manufacturing organization

JSC "Gedeon Richter"

1103 Budapest, st. Dymroyi 19-21, Hungary

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Treatment of gastrointestinal diseases in cats is not always successful, especially if your pet has developed such an unpleasant disease as pancreatitis. This condition causes the animal severe pain and interferes with the digestion of food. Pancreatitis can lead to severe exhaustion or even death of the animal. Therefore, the problem should be solved immediately with the help of the drug “Gordox” for cats. How to use this medicine and give it to your pet? This article will tell you in more detail.

Composition of the drug

The active component of Gordox is aprotinin, a special substance that helps to weaken inflammatory reactions in the pancreas and also helps to activate greater blood clotting, which is especially important for postoperative bleeding.

In veterinary medicine it is used after various surgical interventions However, unauthorized treatment of cats with this drug can lead to many side effects, including death. Instructions for use of Gordox for cats and kittens are the very first thing you should read when handling this drug.

Release form

The maximum effect in the treatment of gastrointestinal diseases can be achieved only in one case - the subcutaneous administration of Gordox to a cat. Therefore, this medicine is available in the form of a solution, poured into ampoules of 10 ml each. One package of Gordox contains 25 injection ampoules. This drug has no analogues.

Indications for use

You can give Gordox to a cat for the following diagnoses::

• acute and chronic pancreatitis;
• pancreatic necrosis (death of gastrointestinal tissue);
• bleeding that occurs for the first time, as a reaction to surgery, or after giving birth to a cat;
• angioedema;
• state of shock, for example, after injury or poisoning;
• with extensive deep injuries to the soft tissues of the cat’s body. Especially if there is a large loss of blood.

The only contraindication for use is pregnancy and lactation in a cat, as well as the pet’s hypersensitivity to active substances drug, resulting in allergic reactions.

Dosage

The dosage of "Gordox" for a cat is prescribed by a veterinarian after an examination - ultrasound of the abdominal cavity, and an appropriate diagnosis.

The administration of this drug is carried out using a catheter, or using a syringe subcutaneously, in the area of ​​the scruff of the neck. For acute attacks of pancreatitis, Gordox is administered intravenously for the first two days, and then, if vomiting is not observed, this medication can be prescribed subcutaneously once a day for 5-7 days.

As a rule, cats and kittens up to 5 kg are administered 0.5 ml of Gordox, and the same animals whose weight ranges from 5 to 15 kg are given 1 ml of the drug. For larger cats or cats, the dosage is calculated separately after consultation with a veterinarian.

Side effects

"Gordox" is always prescribed with caution, since despite its high effectiveness, this medicine has a large amount adverse reactions. The most important of which is the development of an allergy to the main active ingredient of the drug - aprotinin.

Animals exposed to Gordox for the first time tend to be less susceptible to side effects, which include the following:

• allergies leading to anaphylactic shock;
• disturbances in the functioning of the cardiovascular system;
• severe arrest of hematopoiesis, up to DIC syndrome (formation of blood clots);
• disorders of the kidneys;
• liver failure.

If any deviations in the animal’s condition occur, you should immediately contact a specialist.

Thus, the use of “Gordox” for cats becomes a real salvation if the animal has received deep wounds and urgently needs to increase blood clotting. This medicine also helps greatly with pancreatitis, especially during acute attacks of the disease. On the other hand, Gordox has a huge number of side effects, and its administration to a cat can only be done by a specialist in a laboratory setting. Therefore, it is more important than ever to consult a veterinarian who will prescribe correct treatment and make an accurate diagnosis.

VETERINARIAN CONSULTATION REQUIRED. INFORMATION FOR INFORMATION ONLY.