Streptokinasa

General characteristics. Structure:

Active ingredient: 750000 or 1500000 ME Streptokinasas.

Pharmacological properties:

Pharmacodynamics. Streptokinasa — the fermental drug received from culture of a β-hemolitic streptococcus of group C. Drug has fibrinolitic activity that is caused by ability to interact with blood plasminogen. Streptokinasa complex with plasminogen has proteolytic activity and catalyzes transformation of plasminogen into plasmin. The last is capable to cause a lysis of fibrin in clots, to inactivate fibrinogen, and also factors V and VII blood coagulations.

Activity of Streptokinasa is determined by ability of drug to lyse in certain conditions the fibrin clot formed by mix of solutions of fibrinogen and thrombin and expressed in international (international) units (IE or ME).

Apply Streptokinasa to recovery of passability of the thrombosed blood vessels; drug causes a lysis of blood clots, acting on them not only from a surface, but also getting in blood clot (especially at fresh blood clots).

Pharmacokinetics. An elimination half-life after intravenous administration 1500000 ME Streptokinasas — 1 hour, a complex Streptokinasa plasminogen — about 23 min. Biotransformiruyetsya in a liver by hydrolysis. It is removed in a small amount by kidneys. At liver diseases the clearance is slowed down, the renal failure does not influence clearance.

Indications to use:

Indications to use of Streptokinasa are: an embolism of a pulmonary artery and its branches, fibrinferments and an embolism of peripheral arteries, fibrinferments of superficial and deep veins (extremities, a basin), an acute myocardial infarction (during the first 12 h), thrombosis of vessels of a mesh cover of an eye and other states proceeding with acute embolisms and fibrinferments or with threat of formation of blood clots.

Route of administration and doses:

Enter Streptokinasa intravenously kapelno, and in necessary cases — vnutriarterialno.

Intravenously enter usually in an initial dose 250000 ME into 50 ml of isotonic solution of sodium of chloride within 30 min. (30 drops a minute). This dose usually causes the beginning of a lysis of blood clot. Then continue introduction of Streptokinasa in a dose 100000 ME in an hour. The general duration of introduction makes, as a rule, 16 — 18 h. The subsequent treatment is carried out by heparin and anticoagulants of indirect action.

At extensive arterial and venous fibrinferments long administration of drug sometimes is necessary.

Intra arterial introduction of Streptokinasa is applied in the acute period of a myocardial infarction (an initial dose 20000 ME; supporting — 2000 — 4000 ME a minute within 30 — 90 min.).

In all cases introduction of 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.

Features of use:

System use at a myocardial infarction after 24 h is not recommended and more, at a deep vein thrombosis — 14 days and more, at fibrinferment of vessels of a retina: arterial occlusions — 6 — 8 h and more, venous — 10 days and more, at chronic occlusions of arteries, including an obliterating endarteritis — 6 weeks and more.

Precautionary measures. Treatment is carried out under control of indicators of thrombin or partial tromboplastinovy time. With extra care apply at the expressed abnormal liver functions and kidneys, a diabetes mellitus, bronchial asthma, the postponed streptococcal infection, including rheumatism, a bronchietasia with a pneumorrhagia, a gullet phlebectasia, recent purpose of anticoagulants, states after cardiopulmonary resuscitation, IVL, the bleedings accompanying urological diseases, including at an urolithiasis, and also at chronic gastrointestinal diseases, menorrhagias, menstrual bleedings, earlier (from 5 days to 1 year) treated with Streptokinasa, at senile age (over 75 years).

Drug is used in the conditions of a hospital.

Side effects:

When using Streptokinasa nonspecific reactions to protein can develop: a headache, nausea, a fever, allergic reactions (at the expressed allergic reactions use of corticosteroids is recommended).

At bystry intravenous administration development of hypotension, disturbance of a cordial rhythm are possible. It is necessary to consider a possibility of emergence of embolisms (in connection with mobilization of elements of blood clot).

Interaction with other medicines:

Heparin, coumarin derivatives, Dipiridamolum, NPVS, including acetylsalicylic acid, dextrans, valproic acid strengthen anticoagulative effect and increase risk of bleedings.

It is incompatible with plasma substituting solutions — hydroxyethylated starch and a dextran.

Contraindications:

Drug is contraindicated at acute bleedings, hemorrhagic diathesis, fresh ulcers of digestive tract, after recently undergone operations, at the expressed hypertensia, a septic endocarditis, disturbances of cerebral circulation, a pulmonary tuberculosis (cavernous forms), in the first trimester of pregnancy.

Overdose:

Symptoms: strengthening of side effect (it is the most frequent — bleedings)

Treatment: a bleeding stop (whenever possible), purpose of anti-fibrinolitic means (traneksamovy acid, the paraaminomethylbenzoic acid, inhibitors of kallikrein or protease, including Aprotininum, aminocapronic acid — 5 g/h, then on 1 g/h within 4 — 8 hours before achievement of effect), substitution of blood loss (except a dextran and hydroxyethylated starch), a symptomatic treatment.

Issue conditions:

According to the recipe

Packaging:

The powder lyophilized for preparation of solution for injections 750000 and 1500000 ME.