Prourokinase
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Clinical Pharmacology
Gemaza is a thrombolytic agent that is a serine protease in the form of a single-stranded molecule with a molecular weight of 54,000 daltons, consisting of 2 polypeptide chains with masses of 20 and 34 thousand Da, which are connected by a disulfide bridge. It specifically stimulates the conversion of profibrinolysin (plasminogen) into fibrinolysin (plasmin), an enzyme capable of lysing fibrin clots.
Indications
The drug "Gemaza" is used in ophthalmology for the treatment of the following pathology:
Composition
1 amp contains recombinant prourokinase 5 thousand IU.
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Dosage and Administration
The contents of 1 ampoule of the drug "Gemaza" is diluted in 0.5 ml of 0.9% sodium chloride solution. The resulting solution contains a dose corresponding to 5000 ME. The drug is administered parabulbarno or subconjunctival up to 10 injections per course.
To flush the anterior chamber of the eye with massive fibrin effusion into the anterior chamber or hyphema, the lyophilized substance (5000 ME) is diluted in 1 ml of 0.9% sodium chloride solution, after which 0.2 ml (1000 ME) or 0.1 ml (500 ME) of the resulting solution and diluted with 0.5 ml of 0.9% sodium chloride solution.
Adverse reactions
There may be an allergic reaction, which is expressed in swelling and hyperemia of the skin of the face on the administration side of the drug, symptoms of allergic tenonitis (chemosis, conjunctival hyperemia, reduced mobility of the eyeball).
Contraindications
Tendency to bleeding (including hemorrhagic diathesis, hemophilia, thrombocytopenia, etc.), increased risk of bleeding development (gastrointestinal bleeding up to 4 weeks old, extensive surgical intervention or extensive trauma up to 4 weeks old, intracranial or intraspinal cerebral interventions up to 8 weeks, head injury up to 4 weeks), resuscitation (including cardiopulmonary resuscitation for more than 10 minutes), liver disease with severe hemostasis, puncture of large vessels (eg subclavian vein), diabetic hemorrhagic retinopathy, a state after a hemorrhagic stroke (including a history), an increase in systolic blood pressure up to 180 mm Hg. and higher or diastolic blood pressure up to 110 mm Hg. and above, cardiogenic shock (class IV according to Killip), suspicion of dissection of an aortic aneurysm, septic endocarditis, pregnancy, hypersensitivity to prourokinase.
Drug interactions
The combined use of the drug with proteolytic agents has shown that combining the drug "Gemaza®" with injections of collalisin is impractical. The combination of the drug "Gemaza" with other thrombolytics should be used with caution. Perhaps the combined use of solutions of the drug "Gemaza" and Emoxypine, as well as the drug "Gemaza" and dexamethasone.
Pregnancy and Lactation
Contraindicated in pregnancy.
Special instructions
With the development of arterial hypotension (systolic blood pressure less than 90 mm Hg) and bradycardia (heart rate less than 50 beats / min), it is recommended to suspend the administration of the drug until normalization of blood pressure and heart rate. Cross-reactions with streptazy-streptokinase and allergies with streptococcal allergization, as a rule, does not occur.
When conducting surgical interventions against the background of the action of prourokinase to reduce the risk of hemorrhage, intramustate administration of etamzilat is recommended in a dose of 250-500 mg.
With caution used in combination with other troboliticheskimi means.
Overdosage
With the local administration of the drug "Gemaza" in doses of 5000 ME, there is no risk of systemic bleeding.
- Brand name: Gemaza
- Active ingredient: Prourokinase
- Dosage form: Lyophilisate for preparation of solution for injections.
- Manufacturer: Technogen
- Country of Origin: Russia
- Continuous production of prourokinase in feed harvest and perfusion cultures
- A prourokinase-RGDS chimera
- Thrombolysis vs. bleeding from hemostatic sites by a prourokinase mutant compared with tissue plasminogen activator
- C1-inhibitor prevents non-specific plasminogen activation by a prourokinase mutant without impeding fibrin-specific fibrinolysis
- Chromatographic Processing Scheme for Continuous Harvesting of rec-Prourokinase from Serum Free Medium Cell Cultures
- Mutant Prourokinase with Adjunctive C1-Inhibitor Is an Effective and Safer Alternative to tPA in Rat Stroke
- Efficacy of intravenous prourokinase and a combination of prourokinase and urokinase in acute myocardial infarction
- Low dose urokinase preactivated natural prourokinase for thrombolysis in acute myocardial infarction
- The blockage of the high-affinity lysine binding sites of plasminogen by EACA significantly inhibits prourokinase-induced plasminogen activation
- High-level production of prourokinase-annexin V chimeras in the methylotrophic yeast Pichia pastoris
- Efficient renaturation and fibrinolytic properties of prourokinase and a deletion mutant expressed in Escherichia coli as inclusion bodies
- Intra-arterial Prourokinase for Acute Ischemic Stroke: The PROACT II Study: A Randomized Controlled Trial
- Glycosylation of Prourokinase Produced by Pichia pastoris Impairs Enzymatic Activity but Not Secretion
- Elastase released from human granulocytes stimulated with N-formyl-chemotactic peptide prevents activation of tumor cell prourokinase (pro-uPA)
- Effect of purified, soluble urokinase receptor on the plasminogen-prourokinase activation system
- Thrombin–thrombomodulin inhibits prourokinase-mediated pleural mesothelial cell-dependent fibrinolysis
- Commentary on: `Effect of purified soluble urokinase receptor on the plasminogen prourokinase activation system' by N. Behrendt and K. Dano, FEBS Letters, 393 (1996) 31–36
- Reply to comment on `Effect of purified, soluble urokinase receptor on the plasminogen-prourokinase activation system' (A. A-R. Higazi)
- AMYLOID β PEPTIDES STIMULATE TISSUE-TYPE PLASMINOGEN ACTIVATOR BUT NOT RECOMBINANT PROUROKINASE
- Intracoronary thrombolysis following failed intravenous thrombolysis with prourokinase in patients with acute myocardial infarction
- Enhancement of the thrombolytic efficacy of prourokinase by lys-plasminogen in a dog model of arterial thrombosis