Streptokinase
Streptokinase: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. In case of impaired renal function
- 11. For violations of liver function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Streptokinase
ATX code: B01AD01
Active ingredient: streptokinase (streptokinase)
Manufacturer: Belmedpreparaty RUE (Republic of Belarus)
Description and photo updated: 2019-27-08
Streptokinase is a fibrinolytic; activates tissue and systemic fibrinolysis, restores the patency of thrombosed blood vessels, helps to reduce blood pressure and reduce total peripheral vascular resistance, followed by a decrease in cardiac output, in chronic heart failure improves left ventricular function; reduces the rate of deaths as a result of pulmonary embolism and myocardial infarction, reduces the number of thrombotic complications due to diseases of the cardiovascular system, improves heart function.
Release form and composition
Dosage form - lyophilisate for the preparation of a solution for intravenous (iv) and intra-arterial (i / a) administration: porous, hygroscopic mass compacted into a tablet, white with a yellowish tinge (750,000 or 1,500,000 ME each in vials, in a cardboard box 1 bottle and instructions for use of Streptokinase).
1 bottle with lyophilisate contains:
- streptokinase - 750,000 or 1,500,000 ME;
- polygeline - 25 mg;
- sodium L-glutamate - 25 mg.
Pharmacological properties
Pharmacodynamics
Streptokinase is a fibrinolytic agent. Combining with profibrinolysin (plasminogen), streptokinase forms a complex that activates its transition in the blood / blood clot to fibrinolysin (plasmin) - a proteolytic enzyme that promotes the dissolution of fibrin fibers in thrombi and blood clots, causes degradation of fibrinogen and other factors of plasma proteins, including V and VII. The drug dissolves blood clots, affecting them both from the outside and from the inside.
Streptokinase is a streptococcal protein with antigenic properties, therefore it can be neutralized in the body with appropriate antibodies. In such situations, the acceleration of fibrinolysis can be achieved by the introduction of additional doses of the drug necessary to neutralize the corresponding antibodies.
Streptokinase restores the patency of blood vessels with blood clots. When administered intravenously, it decreases blood pressure and total peripheral vascular resistance, which leads to a subsequent decrease in cardiac output. In patients with chronic heart failure, streptokinase improves left ventricular function.
The drug reduces the number of thrombotic complications in diseases of the cardiovascular system, improves functional parameters of the heart, reduces the frequency of deaths in pulmonary embolism and myocardial infarction.
The maximum effect of the drug develops after 45 minutes. The effect persists for several hours after the end of the infusion. Prolongation of prothrombin time persists for a period of up to 24 hours, which is due to a simultaneous decrease in the level of fibrinogen and an increase in the amount of circulating degradation products of fibrin and fibrinogen. Streptokinase activates both tissue fibrinolysis (the action is aimed at thrombolysis - dissolution of the thrombus) and systemic fibrinolysis (cleavage of blood fibrinogen), which may lead to bleeding (due to hypofibrinogenemia).
The use of streptokinase is most effective with fresh fibrin clots (before their retraction).
With intracoronary administration of the drug, thrombolysis occurs after 1 hour.
Pharmacokinetics
The drug is metabolized by hydrolysis. After intravenous administration of a dose of 1,500,000 IU, the half-life of streptokinase is 1 hour, of the streptokinase-profibrinolysin complex - 23 minutes. The complex is partially inactivated by anti-streptococcal antibodies. The resulting fibrinolysin is inactivated by alpha-2-microglobulin and alpha-2-antiplasmin. It is excreted in small quantities by the kidneys. Clearance is slowed down in patients with kidney disease.
Indications for use
- thromboembolism of the pulmonary artery (PE) and its branches;
- acute myocardial infarction in the period up to 24 hours from the beginning;
- thrombosis and thromboembolism of arteries (chronic, acute, subacute thrombosis of peripheral arteries, obliteration of arteriovenous shunt, chronic obliterating endarteritis);
- occlusion (obstruction) of the central vessels of the retina up to 6–8 hours old (arteries), up to 10 days (veins);
- thrombosis of the hemodialysis shunt;
- arterial thrombosis in children after therapeutic or diagnostic procedures, vascular thrombosis in newborns due to catheterization;
- thrombosis of the veins of internal organs, arteries and deep veins of the extremities (less than 14 days old) and the pelvis;
- thrombosis due to prosthetic heart valves;
- retrombosis after vascular surgery;
- rest angina on the background of acute myocardial infarction (monotherapy or as part of complex treatment).
Streptokinase is also used to flush intravenous catheters, including hemodialysis.
Contraindications
- hemorrhagic diathesis;
- bleeding;
- inflammation of the colon;
- erosive and ulcerative lesions of the gastrointestinal tract (gastrointestinal tract);
- multiple recent injuries;
- aneurysm;
- diabetic retinopathy;
- tumors and metastases of the spinal cord and brain;
- tumors with a tendency to bleeding;
- arterial hypertension with arterial pressure (BP) ≥200/110 mm Hg. Art.;
- acute pancreatitis;
- endocarditis, pericarditis, mitral heart defects with atrial fibrillation;
- active form of tuberculosis, cavernous pulmonary tuberculosis;
- septic thrombosis, sepsis;
- period after surgery: 8–12 days after surgery, 3–6 weeks after major surgery, 8 weeks after neurosurgery;
- recent biopsy of internal organs;
- translumbar arteriography and 4 weeks after it;
- acute hemorrhagic stroke and 3 months after it;
- the first 18 weeks of pregnancy;
- pathological course of pregnancy associated with an increased likelihood of bleeding;
- childbirth or abortion (within 10 days after the procedure);
- continuous (long-term) catheterization;
- hypersensitivity to the drug.
With caution, Streptokinase is used for hepatic / renal failure, bronchial asthma, streptococcal infection (including rheumatism), bronchiectasis with hemoptysis, dilated esophageal veins, recent prescription of anticoagulants, conditions after cardiopulmonary resuscitation (including chest compressions after chest compressions)), artificial ventilation, nephrolithiasis, menorrhagia, in the menstrual period, with previous treatment with streptokinase (within 5 days - 1 year) and in the elderly ≥75 years.
Streptokinase, instructions for use: method and dosage
Streptokinase is administered intra-arterially (i.v.), intravenous (i.v.) drip and intracoronary.
Treatment regimens depending on the disease / condition:
- thrombosis of peripheral arteries or veins in adult patients. For short-term thrombolysis: initial dose - 250,000 IU intravenously (for half an hour), then maintenance doses (for 6 hours, 1 time per hour) - 1,500,000 ME; the maximum dose for the entire cycle is 9,000,000 ME (repetition of the 6-hour course of administration can be carried out no later than the 5th day from the first therapy). For long-term thrombolytic therapy: initial dose - 250,000 IU intravenously drip (for half an hour), then intravenous infusion lasting from 12 hours to 3-5 days (no more) - 100,000 IU per hour; if necessary, you can continue therapy after a break with the replacement of streptokinase with another homologous thrombolytic;
- thrombosis of the coronary vessels. For short-term thrombolysis: intravenous drip of 1 500 000 ME (for an hour), then the introduction of heparin at a dose of 1000 IU per hour; efficacy control is carried out by determining thrombin or partially thromboplastin time. For long-term thrombolytic therapy of peripheral vascular thrombosis: the initial dose is 250,000 IU (for half an hour), then the maintenance dose is 100,000 IU per hour (until a 2-4 fold increase in thrombin time is reached 6–8 hours after the onset of lysis); the fibrinogen index in blood plasma should not fall below 1 g / l. In the case of an increase in thrombin time after a few hours more than 4 times, the maintenance dose should be reduced by 2 times and applied until the thrombin time is stabilized in the above interval;
- intracoronary thrombus. For short-term thrombolysis: intracoronary (using a catheter) 20,000 ME, then 2,000-4,000 IU per minute, the total dose is 140,000 ME in 30-40 minutes or 250,000-300,000 ME in 30-60 minutes. Streptokinase is administered for at least 1 hour, but recanalization may develop faster;
- acute, subacute, chronic peripheral thrombosis and embolism. At a dose of 1000–2000 IU, intra-arterial solution is injected into the affected area every 3-5 minutes; the duration of the procedure and the number of injections depend on the depth of occlusion and the location of the vessel; the maximum dose is 120,000 IU in 3 hours; simultaneous angioplasty is allowed;
- deep vein thrombosis and pulmonary embolism. 250,000 IU IV drip for half an hour, then 100,000 IU per hour for 1-3 days (depending on the nature of the disease);
- restoration of the patency of the cannula. 100,000-250,000 IU per 2 ml of isotonic sodium chloride solution is slowly introduced into each clogged end of the tube. The duration of the procedure is 2 hours, after which the contents are sucked off.
The recommended dosing regimen for children: at a dose of 1000-10,000 IU / kg IV drip for 20-30 minutes, then long-term infusion of 1000 IU / kg / hour until significant bleeding appears at the injection site. Heparin is used to prevent retrombosis. The duration of the course of therapy should not exceed 5 days.
For intravenous administration, the lyophilisate is carefully dissolved, avoiding foaming, in 5 ml of 0.9% sodium chloride solution, water for injection or Ringer's solution.
Side effects
- blood coagulation system: bleeding from the injection sites, from the gums, hemorrhage in the pericardium / myocardium, in the skin, in the brain, hematomas, internal bleeding (including retroperitoneal, urogenital, from the gastrointestinal tract);
- cardiovascular system: noncardiogenic pulmonary edema (intracoronary administration), reperfusion arrhythmia, embolic stroke, thromboembolism (with mobilization of a thrombus or its fragmentation), including pulmonary embolism (deep vein thrombosis therapy) and distal artery (cholesterol embolism) local thrombosis; Shenlein-Henoch syndrome (capillary toxicosis), increased ESR (erythrocyte sedimentation rate);
- hypersensitivity reactions (mainly with subsequent administrations): dyspnoea, urticaria, skin flushing, generalized exanthema, hyperthermia, chills, pain in the spine, myalgia, headache, decreased blood pressure, tachycardia or bradycardia, vasculitis (including hemorrhagic), arthritis, polyneuropathy, nephritis, bronchospasm, angioedema, anaphylactic shock;
- laboratory parameters (repeated administration): increased activity of hepatic transaminases and alkaline phosphatase, gamma-glutamyltransferase and creatine phosphokinase, decreased cholinesterase activity, hyperbilirubinemia;
- other reactions: rupture of the spleen.
Overdose
Overdose symptom is massive bleeding.
For the treatment of the condition: they cancel streptokinase, stop bleeding using antifibrinolytics (paraaminomethylbenzoic or tranexamic acids, inhibitors of kallikrein and other proteases), restore blood loss (except for hydroxyethylated starch and dextran), carry out symptomatic treatment.
special instructions
Streptokinase is allowed to be used only in a hospital setting.
The solution prepared from the lyophilisate should be used within 12 hours.
In the course of therapy, it is required to monitor blood coagulation indicators once every 4 hours: thrombin or partial thromboplastin time. To avoid vascular reocclusion, it is necessary to increase the thrombin time by 2–4 times, the partial thromboplastin time by 1.5–2.5 times, for which the required amount of heparin is first introduced - 500–1000 IU / h, and then oral forms of derivatives are used coumarin.
Before the administration of the solution to children and patients with a history of elevated antistreptokinase antibody titers, a streptokinase sensitivity test is performed.
At the beginning of therapy, infusion is performed at a low rate for newborns, for prophylaxis 10 minutes before the procedure, 100-200 mg of methylprednisolone with antihistamines is allowed. Repeated administration of the drug increases the risk of developing hypersensitivity reactions. Before the start of streptokinase use, newborns undergo an ultrasound examination of the skull.
In case of deep vein thrombosis during therapy, patients are not recommended to interrupt the use of contraceptives in order to avoid menorrhagia.
After 5 days from the start of treatment and within 1 year after its end after a streptococcal infection, the risk of developing resistance is increased as a result of an increase in the titer of antistreptococcal antibodies. If necessary, other fibrinolytics (for example, urokinase) should be used for thrombolytic therapy in such patients.
Intravenous streptokinase is preferably administered into the vessels of the upper extremities; after the procedure, it is required to apply a pressure bandage for half an hour with monitoring of its condition in the future due to possible bleeding; cannot be administered within 10 days after intramuscular (i / m) injections and arterial punctures.
Application during pregnancy and lactation
The use of streptokinase is contraindicated in the first 18 weeks of pregnancy, if a pregnant woman has pathology associated with an increased risk of bleeding, as well as within 10 days after childbirth or abortion.
With impaired renal function
With caution, streptokinase should be used in patients with renal insufficiency.
For violations of liver function
With caution, streptokinase should be used in patients with hepatic impairment.
Use in the elderly
In patients over the age of 75, Streptokinase should be used with extreme caution.
Drug interactions
- valproic acid, heparin, dipyridamole, dextrans, coumarin derivatives, acetylsalicylic acid: enhance the action of streptokinase and increase the risk of bleeding;
- antifibrinolytic drugs: weaken the effect of fibrinolytics;
- dextran and hydroxyethyl starch (plasma substitutes): incompatible with streptokinase, their use as a solvent is unacceptable.
Analogs
Streptokinase analogs are: Gemaza, Metalize, Purolaza, Trombovazim, Thromboflux, Urokinase Medak, Fibrinolysin, Eberkinase (Recombinant streptokinase).
Terms and conditions of storage
Store out of the reach of children at temperatures up to 25 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about streptokinase
The drug is used in a hospital setting and often as part of a combination therapy, therefore, there are no reviews of Streptokinase on specialized medical sites and forums. Doctors point out that this fibrinolytic agent is effective only with fresh blood clots, so the result is achieved only with timely treatment. Also, doctors note: the drug has a large list of contraindications and can cause side effects, and therefore it is always used with caution and under close control.
The price of Streptokinase in pharmacies
Approximate prices for Streptokinase: lyophilisate for preparation of a solution for intravenous and intravenous administration in a dose of 750,000 IU - 2689–3436 rubles. for 1 bottle, in a dose of 1,500,000 IU - 2,895–3,989 rubles. for 1 bottle.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
