Clinical and pharmacological group: & nbsp

Fibrinolytics

Included in the formulation
  • Hemase®
    lyophilizate for injections 
    TECHNOGEN NPP, LLC     Russia
  • Puroolase®
    lyophilizate in / in 
  • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    B.01.A.D.   Enzyme preparations

    Pharmacodynamics:A fibrinolytic agent, single-chain urokinase-type plasminogen activator. Under the action of plasmin and other serine proteases prourokinase easily converted into a double-stranded form (urokinase), whose chains are connected by a single disulfide bond. Specifically stimulates the conversion of profibrinolysin (plasminogen) to fibrinolysin (plasmin), capable of lysing fibrin clots. It has high specificity with respect to fibrin-associated plasminogen.
    Pharmacokinetics:Half-life is 7.1 minutes (20 mg bolus + 60 mg / h intravenously drip); 8.8 min (80 mg bolus); 5.1 minutes (40 mg bolus + 40 mg bolus with an interval of 30 minutes).
    Indications:

    For intravenous administration: occlusion of coronary vessels (acute myocardial infarction).

    For the introduction of subconjunctival, parabulbar, in the anterior chamber of the eye, intravitreal: hyphema, hemophthalmus; preretinal, subretinal and intra-retinal hemorrhages; fibrinoid syndrome of different genesis; occlusion of the central artery of the retina and its branches; central thrombosisveins of the retina and its branches; prevention of adhesions in the postoperative period with antiglaucoma operations.

    VII.H15-H22.H21.0   Hyphema

    VII.H30-H36.H34   Vascular occlusion of the retina

    VII.H30-H36.H35.6   Retinal hemorrhage

    VII.H43-H45.H44.8   Other diseases of the eyeball

    IX.I20-I25.I21   Acute myocardial infarction

    Contraindications:

    General Contraindications: Hypersensitivity, the propensity to bleeding (including hemorrhagic vasculitis, hemophilia, thrombocytopenia, and others), bleeding from the gastrointestinal tract prescription of up to 4 weeks, bacterial endocarditis.

    In cardiology: major surgery or vast trauma prescription to 4 weeks, intracranial or vnutrispinnomozgovye interference prescription to 8 weeks, the prescription of head injury to 4 weeks resuscitation (including cardiopulmonary resuscitation over 10 min), liver disease with severe disorders of the hemostatic system , puncture of major vessels (e.g., the subclavian vein), diabetic retinopathy haemorrhagic condition after hemorrhagic stroke (including a history of), indicator sistolicheskog about blood pressure of 180 mm Hg. and above or a diastolic blood pressure of 110 mm Hg.and above, cardiogenic shock (class IV according to Killip), suspicion of aortic aneurysm stratification, pregnancy.

    In ophthalmology: active form of tuberculosis, proliferative diabetic retinopathy with gliosis of III-IV degree, arterial hypertension with diastolic pressure above 105 mmHg, hypertensive crisis (risk of recurrence of intraocular hemorrhage), chronic renal failure (serum creatinine concentration above 0 , 02 g / l, urea - above 0.5 g / l), severe hepatic insufficiency (albumin concentration in the blood below 3 g%).

    Carefully:In combination with other thrombolytic agents.
    Pregnancy and lactation:Category of recommendations FDA is not defined. Adequate and well-controlled studies in humans and animals have not been conducted. There is no information on the penetration into breast milk. Contraindicated in pregnancy and lactation ..
    Dosing and Administration:

    Introduce intravenously in cardiac practice; subconjunctival, parabulbar, as well as in the anterior chamber of the eye, intravitreal - in ophthalmic practice.

    Applied in appropriate dosage forms and according to special schemes.

    Occlusion of coronary vessels (myocardial infarction): only intravenously at a dose of 100 mg (20 mg bolus and 80 mg dropwise for 60 minutes) in a 0.9% solution of sodium chloride. To prepare an infusion solution, the contents of the vial are dissolved in 20 ml of water for injection. The solution is prepared immediately before use and is not stored.

    Prourokinase in a dose of 20 mg bolus + 60 mg intravenously drip for 60 min exceeds streptokinase (1.5 million units intravenously drip for 60 min) in efficiency (the percentage of recanalization is higher) and safety (the concentration of fibrin degradation products is lower and less often causes bleeding) . However, the functional status and mortality were comparable one year after treatment (80 mg prourokinase and 1.5 million units streptokinase intravenously drip for 60 min) and after 5 years with a trend towards a decrease in the cases of repeated infarction in the prourokinase group.

    Prourokinase at a dose of 80 mg / h is comparable to alteplase (100 mg every 3 hours) in terms of effectiveness (percentage of recanalization, reocclusion above), safety (there are fewer side effects).

    Single bolus administration of 60 mg prourokinase is not effective because of a low percentage of recanalization; a double bolus injection of 40 mg at an interval of 30 minutes increases the death rate (13.5%).A single bolus administration at a dose of 80 mg prourokinase is comparable to the standard regimen (20 mg bolus + 60 mg / h intravenously drip).

    Hyphema - subconjunctival or parabulbar, as well as in the anterior chamber of the eye.

    Hemophthalm: intravitreal.

    Pre-, sub- and intra-retinal hemorrhages: parabulbar.

    Fibrinoid syndrome of different genesis: intravitreal.

    Prevention of adhesions in the postoperative period at antiglaukomatoznyh operations: bred for subconjunctival administration and injected into the filter pad in the early postoperative period of 1-3 injections.

    For parabulbar and subconjunctival administration, the contents of 1 ampoule are dissolved in 0.5 ml of a 0.9% solution of sodium chloride (the concentration of the resulting solution corresponds to 5000 IU). The course of treatment - up to 10 injections.

    For washing the anterior chamber when a massive effusion of fibrin in it or hyphema contents of the vial are dissolved in 1 ml of 0.9% sodium chloride solution, whereupon 0.2 (1000 ME) or 0.1 ml (500 ME) of the resulting solution was diluted to 0 , 5 ml with 0.9% sodium chloride solution.

    For intravitreal single administration, the contents of the ampoule are dissolved in 1 ml of a 0.9% solution of sodium chloride, then 0.1 ml (500 IU) of the solution is diluted with 0.1-0.2 ml of 0.9% sodium chloride solution.

    Acute ischemic stroke - thrombolysis (including prourokinase recombinant for 6-9 mg intraarterially through an angiographic catheter into thrombus + heparin 2000 IU intravenously bolus during angiography, then 500 IU / h intravenously for 4 hours) against control (placebo / acetylsalicylic acid / sodium heparin intravenously, heparin sodium 2000 IU intravenously bolus during angiography, followed by 500 IU / h intravenously for 4 hours).

    Side effects:

    Allergic reactions: skin manifestations, as well as edema and hyperemia of the facial skin on the side of drug administration, allergic tenonitis (chemosis, conjunctival hyperemia, decreased mobility of the eyeball).

    From the side of cardio-vascular system: a decrease in blood pressure.

    From the side blood coagulation system: bleeding of varying severity from puncture sites and surgical incisions.

    Overdose:

    Symptoms: hemorrhage.

    Treatment: small bleeding can be stopped without stopping the drug administration by temporarily stopping the infusion of sodium heparin with additional control of activated partial thromboplastin time; In life-threatening bleeding, the administration of the drug is stopped andprescribe plasma or whole blood; if necessary, to neutralize the prourokinase effect, antifibrinolytic agents are administered, aprotinin, aminocaproic or tranexamic acid.

    In ophthalmology.

    Symptoms: relapse of intraocular hemorrhage.

    Treatment: intramuscularly 250-500 mg etamzilate.

    Interaction:AcetylsalicylicI acid, thrombolytics and anticoagulants - increased risk of bleeding.
    Special instructions:

    With the development of arterial hypotension (systolic blood pressure less than 90 mm Hg) and bradycardia (heart rate less than 50 beats per minute), it is recommended to stop the administration of the drug before the normalization of blood pressure and heart rate. Cross reactions with streptoza-streptokinase and allergies in streptococcal allergies, as a rule, does not arise.

    When performing surgical interventions against the background of prourokinase to reduce the risk of hemorrhage, intramuscular injection of etamzilate in a dose of 250-500 mg is recommended.

    Use with caution in combination with other trobolitics.

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