Ingitril

General characteristics. Structure:

Active ingredient: 15 PIECES of Aprotininum from lungs of cattle.

Pharmacological properties:

Pharmacodynamics. Polyvalent inhibitor of proteases, has anti-proteolytic, anti-fibrinolitic and haemo static effect. Inactivates the major proteases (trypsin, chymotrypsin, the kininogenaza, kallikrein including activating a fibrinolysis). Brakes both total proteolytic activity, and activity of separate proteolitiyochesky enzymes.

Existence of anti-protease activity defines efficiency of Aprotininum at the porazheyoniya of a pancreas and other states which are followed high soderzhayoniy kallikrein and other proteases in plasma and fabrics.

Reduces fibrinolitic activity of blood, brakes a fibrinolysis and has gemosyotatichesky effect at coagulopathies.

Blockade of kallikrein-kinin system allows to use it for prevention and treatment of various forms of shock.

Pharmacokinetics. After intravenous administration it is quickly distributed in extracellular space, quickly collects in a liver.

It is inactivated in digestive tract, a part collapses in a liver. An elimination half-life (T1/2) - 150 min., terminal - 7-10 h. It is removed by kidneys during 5-6 h in the form of inactive decomposition products.

Indications to use:

Pancreatitis (acute, aggravation of chronic), pancreatonecrosis. Performance of diagnostiyochesky researches and pancreas operations (prevention of a fermentativyony autolysis of a pancreas at operations on it and nearby the located oreganos of an abdominal cavity).

Bleeding against the background of a hyper fibrinolysis: posttraumatic, postoperative (osoyobenno at prostate gland, lungs operations), to, later and at the time of delivery (including at an embolism amniotic waters); polymenorrhea.

Quincke's disease.

Shock (toxic, traumatic, burn, hemorrhagic).

Extensive and deep traumatic damages of fabrics.

As auxiliary therapy - the coagulopathies which are characterized by a secondary hyper fibrinolysis (in an initial phase, before effect after use of a gepayorin and substitution of factors of coagulation); massive bleeding (during tromboliyotichesky therapy).

Carrying out extracorporal blood circulation.

Prevention of postoperative pulmonary embolisms and bleedings; a fatty embolism at polyinjuries, especially at fractures of the lower extremities and bones of a skull.

Use for treatment of children is not studied.

Route of administration and doses:

Enter intravenously slowly, only in situation "lying" struyno (with a speed no more than 5 ml/min.) or kapelno.

At acute pancreatitis preferably drop introduction in a dose of 200 PIECES a day. The necessary dose dissolve 0,9% of isotonic solution of sodium of chloride in 500-1000 ml. At the complicated pancreatitis before purpose of the specified dose the drug is administered vnutyorivenno struyno (slowly) in a dose of 100 PIECES in 10-20 ml of 0,9% of isotonic solution of sodium of chloride. In this case the daily dose makes 300 PIECES.

In such dose drug is appointed within 2-6 days before emergence of signs of terapevtiyochesky effect. Then it is possible to reduce a daily dose to 100-150 PIECES.
After stopping of pain, vomiting, elimination of the peritoneal phenomena, paresis of intestines, the termination of tachycardia, normalization of content of amylase in blood and urine the drug is administered intravenously kapelno by 60 PIECES a day within 3-4 days. Stop treatment in process of achievement of permanent improvement.

The course dose at treatment of acute pancreatitis varies from 600 to 5000 PIECES.

For prevention of postoperative pancreatitis and bleedings (including at the patients operated in the conditions of artificial circulation) Aprotininum is entered struyno slowly in a dose of 100-200 PIECES (into 10-20 ml of 0,9% of isotonic solution of sodium of chloride), then enter intravenously kapelno in a daily dose 200 PIECES during the first three days of the postoperative period.

At the bleedings which are followed by a fibrinolysis, Aprotininum is appointed vnutrivenyono kapelno in a dose of 300 PIECES a day to a stop of bleeding or normalization of fibriyonolitichesky activity.

At depressed cases the initial dose makes 200-300 PIECES, then to 150 PIECES vnutriyovenno struyno every 4 hour. At patients with burn shock and an acute burn toxaemia the drug is administered within 5-7 days on 140-200 PIECES daily intravenously kapelno with a speed of 40-60 thaws a minute.

Dissolution of the necessary dose of Aprotininum in 200 ml of solution of Procainum of 1 mg/ml is allowed.

At pancreatic and high enteric fistulas drug is used locally in a dose of 100 PIECES. Drug is dissolved in this case in the volume of 0,9% of an isotonic rastvoyor of sodium of chloride or other solvents (solution of Procainum of 5 mg/ml, Dextrosums of 40 mg/ml), sufficient for the round-the-clock slow introduction to fistula (3-4 l).

Features of use:

Pregnancy and lactation. Contraindicated in I and III trimesters of pregnancy (in the II trimester of pregnancy only in urgent cases). For the period of treatment it is necessary to stop breastfeeding.

To patients with the increased risk of development of allergic reactions before use of Aprotininum administer the antihistaminic drugs. The risk of development of allergic reactions increases at patients with the previous treatment by Aprotininum (within 15 days and up to 6 months).

At a hyper fibrinolysis and a syndrome of the disseminated intravascular coagulation purpose of Aprotininum is possible only after elimination of all manifestations of disseminiyorovanny intravascular coagulation and against the background of preventive administration of heparin.

Especially carefully it is necessary to appoint the patient whom in the previous 2-3 days naznayochat muscle relaxants for prevention of thrombosis of small peripheral vessels. At development of anaphylactic reactions introduction is immediately stopped and carry out sootyovetstvuyushchy therapy.

Influence on ability to manage vehicles and mechanisms. Considering possible side effects, it is not necessary to use drug at control of vehicles and to be engaged in other potentially dangerous types of activity demanding concentration of attention and speed of psychomotor reactions.

Side effects:

From cardiovascular system, a lowering of arterial pressure, a takhikaryodiya, risk of development of a myocardial infarction at use of high doses of Aprotininum during repeated operations of shunting on coronary vessels.

From the central nervous system: psychotic reactions, hallucinations, consciousness spuyotannost.

Allergic reactions: urticaria, a skin itch, rhinitis, conjunctivitis, anaphylactic reactions (up to an acute anaphylaxis).

From the alimentary system: nausea, vomiting (at bystry introduction).

Local reactions: thrombophlebitis in an injection site (at long introduction).

Others: bronchospasm, mialgiya.

Interaction with other medicines:

Aprotininum pharmaceutical is incompatible with other medicines (except for solutions of electrolytes and a dextrose).

Inhibits effects of Streptokinasa, urokinase and alteplaza; strengthens action of a gepariyon (addition to a heparinized blood causes increase in time of coagulation of whole blood).

Contraindications:

Hypersensitivity, sharply expressed allergic reactions (including on protein of cattle), a syndrome of the disseminated intravascular coagulation (except for a coagulopathy phase); pregnancy (I and III trimesters), lactation period.

With care. A deep hypothermia, a blood circulation stop, during operation with use of the device for artificial circulation (risk of development of a renal failure and a lethal outcome), allergic reactions in the anamnesis; the previous treatment by Aprotininum.

Storage conditions:

In the place protected from light at a temperature from 2 to 20 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Lyophilisate for preparation of solution for intravenous administration of 15 PIECES in ampoules or glass bottles from neutral glass. On 10 ampoules or bottles with the application instruction place in a pack from a cardboard. Put a knife in each pack ampoule or the scarificator. When packaging the ampoules having a ring of a break or a point for opening the knife ampoule or the scarificator is not put.