Aprotex - instructions for use, dose, side effects, contraindications

Polyvalent protease inhibitor, has antiproteolytic, antifibrinolytic, hemostatic effect. Inactivates plasma proteinases (plasmin, trypsin, chymotrypsin, kallikrein, incl. activating fibrinolysis), blood cells and tissues that play an important role in pathophysiological processes.The therapeutic effect of aprotinin is due, first of all, to the suppression of the proteolytic action of plasmin and the blockade of plasminogen activation by autogenous activators. The presence of antiprotease activity determines the effectiveness of pancreatic and other conditions accompanied by a high content of kallikrein and other proteinases in plasma and tissues. Reduces the fibrinolytic activity of the blood, inhibits fibrinolysis and exerts a haemostatic effect with coagulopathy. Blockade of kallikrein-kinin system allows to use aprotinin for the prevention and treatment of various forms of shock, with angioneurotic edema.

Pharmacokinetics:

After intravenous administration it is quickly distributed in the extracellular space, briefly accumulated in the liver. It is inactivated in the gastrointestinal tract, part is destroyed in the liver. Half-life (T_1/2) from the blood plasma - about 150 min. Terminal T_1/2 - 7-10 hours. Slowly destroyed by the action of lysosomal enzymes of the kidneys to inactive products and is excreted for 5-6 hours.

Indications:

Pancreatitis (acute, exacerbation of chronic), pancreatic necrosis, prophylaxis of postoperative pancreatitis.

Hyperfibrinolytic bleeding:

-Post-traumatic;

- Postoperative (especially with operations on the prostate gland, lungs);

- Bleeding before, during and after childbirth (including embolism with amniotic fluid), polymenorrhea;

complications of thrombolytic therapy;

Prevention of bleeding during open heart surgery using an artificial circulation device;

Treatment and prevention of various forms of shock (endotoxic, traumatic, hemolytic);

Coagulopathies characterizing secondary hyperfibrinolysis;

Prevention of embolism (postoperative, with polytrauma);

Prevention of postoperative mumps.

Contraindications:

Hypersensitivity to aprotinin, other components of the drug, the protein of cattle; syndrome of disseminated intravascular coagulation (DVS-syndrome) (with the exception of the coagulopathy phase); pregnancy (I and III trimesters); lactation period.

Carefully:

Cardiopulmonary shunting operations, deep hypothermia, circulatory arrest during the operation with the use of an artificial circulation device (the risk of developing renal failure and death),allergic reactions in the anamnesis; previous treatment with aprotinin, as well as patients who received muscle relaxants 2-3 days before.

Pregnancy and lactation:

Possible use in the II trimester of pregnancy only for life indications. The clinical experience of using aprotinin during lactation is not enough. If it is necessary to prescribe the drug, breastfeeding should be discontinued (at the time of application).

Dosing and Administration:

Aprothex is administered only in the "lying" position, intravenously struising slowly (maximum - 5 ml per minute) or drip.

The contents of 1 vial are dissolved in 2 ml (for a dosage of 10,000 ATPE) or 20 ml (for dosage 1000Q0 ATPE) isotonic sodium chloride solution.

Typically, the following dosage regimens are prescribed:

With bleeding

The initial dose is 300,000 ATPE (399,000 IUU), followed by 140,000 ATPE (186,200 IU) every 4 hours intravenously until the hemostasis normalizes.

With acute pancreatitis

200000-300000 ATRE (266000-399000 KIE) is intravenously sprayed slowly, then intravenously drip - 200000-300000 ATPE (266000-399000 KIE) per day. The treatment is carried out until the clinical picture of the disease is normalized and the indices of laboratory tests are normalized.

Prevention of postoperative pancreatitis

200,000 AtPE (266,000 IUI) per day intravenously struino.

In case of shock conditions

The initial dose is 200,000-300,000 ATPE (266,000-399,000 IUI), followed by 140,000 ATPE (186,000 IUI) intravenously stratified every 4 hours.

With coagulopathy, characterized by secondary hyperfibrinolysis

Assign a dose of 750,000 AtPE (1 million KIE) and more.

Prevention of fat embolism

Initially, slowly intravenously at a dose of 200,000 ATPE (266,000 IUI), then 200,000 ATPE (266,000 IUI) were injected slowly intravenously every day.

Possible local application

With prolonged minor bleeding, a gauze pad impregnated with a solution of the drug at a dose of 75,000 ATPE (100,000 KIU) is applied to the spot of bleeding.

Patients with pancreatic necrosis and exudate in the abdominal cavity, containing enzymes a solution of Aprotex can be administered intraperitoneally (in addition to intravenous application).

Children

In case of violations of hemostasis, 15,000 ATPE (20,000 KIE) per kg of body weight is administered at a daily dose.

Side effects:

Allergic reactions: bronchospasm, urticaria, pruritus, rhinitis, conjunctivitis, anaphylactic reactions (up to anaphylactic shock).

From the cardiovascular system: lowering of blood pressure, tachycardia. The use of large doses of aprotinin (6 million - 9 million ATPE, which corresponds to 8-12million KIE) during repeated operations of shunting on coronary vessels may lead to an increased risk of myocardial infarction.

From the central nervous system: psychotic reactions, hallucinations, confusion.

From the digestive system: transient nausea, vomiting (with rapid administration).

Local reactions: thrombophlebitis at the site of administration (with prolonged administration).

Other: myalgia.

Interaction:

Pharmaceutically incompatible with other drugs (except for solutions of electrolytes and dextrose).

Inhibits the effects of fibrinolytic agents, incl. streptokinase, urokinase, alteplase.

Enhances the effect of heparin (the addition to heparinized blood causes an increase in the coagulation time of whole blood).

Mutual enhancement of the effect is noted with the joint appointment of aprotinin and reomacrodex.

Special instructions:

Patients with an increased risk of developing allergic reactions before using aprotinin are administered antihistamines. In the case of an allergic reaction, the administration of aprotinin should be stopped immediately.

The risk of developing allergic reactions increases in patients with prior treatment with aprotinin (for 15 days and up to 6 months).

With DVS-syndrome, the drug can be used only after removing all manifestations of ICE and against the background of preventive action of heparin. Caution should be given to patients who received muscle relaxants 2-3 days before.

Form release / dosage:

Lyophilizate for the preparation of a solution for intravenous administration of 10,000 ATPE and 100,000 ATPE.

Packaging:

In the bottles. 1 bottle with instructions for use in a pack of cardboard.

For 5 or 10 bottles together with instructions for use in a pack with partitions or special cardboard sockets.

At 30, 50, 85, 100 vials with instructions for use, based on one instruction for ten bottles, in a box of cardboard (for hospitals).

Storage conditions:In a place protected from light and inaccessible to children, at a temperature of no higher than 25 ° C.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002505 / 01

Date of registration:16.10.2008 / 29.07.2016

Expiration Date:Unlimited

The owner of the registration certificate:LENS-PHARM, LLC LENS-PHARM, LLC Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp10.09.2017

Illustrated instructions

Instructions

Aprotex (Aprotex)