STREPTOKINASA - BIOFARM

General characteristics. Structure:

Active ingredient: 1 bottle contains Streptokinasas of 1 500 000 ME.

excipients: albumine, solution of a poligelin.

Main physical and chemical properties: the powder lyophilized white or light yellow color.

Pharmacological properties:

Pharmacodynamics. Streptokinasa – the high cleaning enzyme received at cultivation of a strain of ß - a hemolitic streptococcus of group C. Represents protein with a molecular weight about 50 000 дальтон. Has fibrinolitic activity. At connection with plasminogen Streptokinasa forms the complex activating transition of plasminogen of blood or a blood clot to plasmin. The plasmin having proteolytic enzymatic activity causes a lysis of threads of fibrin of blood clots, degradation of fibrinogen and other proteins of plasma, including V (accelerin) and V ІІ (convertin) of factors of turning of blood. Dissolves blood clots, affecting as their surfaces, and from within. It is most effective at fresh clots of fibrin (to retraction); recovers passability of the thrombosed blood vessels. After the end of infusion the hyper fibrinolitic effect of Streptokinasa is observed only within several hours, however lengthening of thrombin time can remain to 24 h owing to simultaneous decrease in level of fibrinogen and increase in number of the circulating products of degradation of fibrin and fibrinogen.

Pharmacokinetics. The complex elimination half-life Streptokinasa – plasminogen makes about 23 min. As Streptokinasa is weak streptococcal antigen, it is partially inactivated by anti-streptococcal antibodies which are always present at blood. Sotoyaniye of a fibrinolysis is reached only at introduction of the excess quantity of Streptokinasa necessary for neutralization of antibodies and the subsequent penetration of active Streptokinasa into blood clot. Metabolites and the mechanism of removal of Streptokinasa are not known.

Indications to use:

Acute myocardial infarction (within the first 12 hours); deep vein thrombosis; acute massive thromboembolism of a pulmonary artery; acute occlusion of arteries embolus or blood clot; thrombosing of the hemodialysis shunt.

Route of administration and doses:

At a myocardial infarction (within the first 12 hours) appoint intravenously kapelno in the dose of 1 500 000 ME dissolved in 100 ml of 0,9% of solution of sodium of chloride or 5% of solution of glucose. Perhaps intracoronary introduction in a dose  of 250 000 - 300 000 ME within 30-60 min.

At a deep vein thrombosis, an embolism of a pulmonary artery and arterial occlusion – intravenously kapelno in a dose of 250 000 ME in 100-300 ml of solvent within 30 min. Right after introduction of a shock dose begin a maintenance therapy. Introduction on 100 000 ME of Streptokinasa each hour within 3 days is possible. It is possible to carry out 12-hour infusion in a dose of 1 200 000 ME to 500 ml of solvent. It is very important that the speed of infusion was a constant. It is desirable to conduct a control research of passability of vessels upon termination of infusion. If within 3 days the positive clinical effect is not noted, therapy should be stopped. If necessary treatment by Streptokinasa can be prolonged for 1-3 days.

For dissolution of blood clots in hemodialysis shunts of 100 000 ME Streptokinasas dissolve in 100 ml of isotonic solution of sodium of chloride. 10 000 - 25 000 ME (10-25 ml) enter into zatrombirovanny department of the shunt then its venous end is blocked a clip. Attach a sterile unit-dose syringe for formation of the air emptiness providing an artery pulsation to the arterial end of the shunt. If necessary introduction of Streptokinasa can be repeated in 30-45 min.

Features of use:

In all cases treatment by Streptokinasa should be begun as soon as possible as the best effect is observed at fresh blood clots. Treatment by Streptokinasa is carried out under control of thrombin time  and content in fibrinogen blood. Before administration of drug it is recommended to determine the content of fibrinogen, thrombin time and the activated partial tromboplastinovy time. It is necessary to observe special care at purpose of Streptokinasa to patients aged 75 years are more senior.

Use of heparin can be begun not earlier than in 4 h after the termination of infusion of Streptokinasa.

Do not recommend to appoint Streptokinasa during the entire period of pregnancy.

Side effects:

Not cardiogenic fluid lungs, thromboembolism in connection with a separation of blood clot or its fragments, increase in SOE. At reusable introduction – increase in the ALT, nuclear Heating Plant level, an alkaline phosphatase, decrease in the ABP, arthritises, vasculites, nephrites, polyneuropathy, muscle pain. Skin rash, a small tortoiseshell, bleeding from places of punctures and cuts are possible fervescence on 1-2 ^{° C} (during the first 5-8 h introduction); disturbances of a menstrual cycle, bleeding from internals, hemorrhage in internals, arrhythmia (at a myocardial infarction).

Interaction with other medicines:

At the co-administration of Streptokinasa and drugs influencing system of a blood coagulation (heparin, indirect anticoagulants, antiagregant) the risk of developing of bleedings increases.

If just before an initiation of treatment Streptokinasa the patient received heparin, its action is neutralized administration of protamin of sulfate. In case of preliminary treatment indirect anticoagulants recommend use of drugs of vitamin K. Prior to treatment carry out by Streptokinasa definition of a prothrombin time. Streptokinasa is incompatible with dextrans and gidroksiletilirovanny starch.

Contraindications:

 The operation postponed to the last 10 days, injury, biopsy, puncture of not falling down vessel (a subclavial or jugular vein), cardiac tamponade, endotracheal intubation;

- damage of arteries of a brain which can take place at heavy arterial hypertension, an azotemic or diabetic retinitis, recently (up to 2 months) the had stroke or other cerebrovascular pathology, aneurisms;

- bleeding or high risk of developing of bleeding (hemorrhagic diathesis, thrombocytopenia, a heavy renal and/or liver failure, erosive cankers of a digestive tract in the last 6 months – a round ulcer, nonspecific ulcer colitis, a diverticulitis, menstrual bleedings, the pregnancy period – especially the first 18 weeks, a state after the delivery, an active form of tuberculosis, tumor, acute pancreatitis;

- risk of a cardial embolism, for example at atrial fibrillation against the background of defeat of the mitral valve and a bacterial endocarditis;

- recent treatment by Streptokinasa (from 5 days to 6 months the previous definition of a high caption of neutralized antibodies).

- mitral heart diseases with atrial fibrillation, a septic endocarditis.

Overdose:

Symptoms: strengthening  of collateral effects, most often – bleedings. In case of developing of bleeding introduction of Streptokinasa  should be stopped.

Treatment. If it is necessary to recover quickly a condition of system of a blood coagulation, it is necessary to begin treatment with drugs of aminocapronic acid. In need of completion of volume of blood administration of plasma substitutes, a packed red cells or whole blood, purpose of anti-fibrinolitic means (traneksamovy acid, Aprotininum) is recommended.

Storage conditions:

To store at a temperature from 2 °C to 8 °C. Validity term - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 1 500 000 ME in 1 bottle. On 1 bottle in a cardboard box.