Composition, form of production and packaging
Lyophilizate for the preparation of a solution for intravenous administration in the form of an amorphous powder or a porous mass of white color, odorless.
prourokinase recombinant 2 million MEU
Excipients: sodium chloride.
Glass bottles (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the print edition of 2007.
Thrombolytic. Recombinant fibrin-specific activator of urokinase-type plasminogen.
It is a single-stranded molecule with a molecular weight of 46,000 Da, consisting of two polypeptide chain-domains with molecular weights of 17,000 and 29,000 Da that contain the regulatory portion and the catalytic domain of the enzyme, respectively, and are connected by a disulfide bridge. Due to its regulatory part it specifically interacts with fibrin-bound plasminogen and catalyzes the transformation of plasminogen into a plasmin protease capable of lysing fibrin clots (thrombi).
Data on the pharmacokinetics of the drug Purolase is not provided.
- Acute myocardial infarction (as a thrombolytic agent in the first hours after the development of the disease).
The drug is only for IV introduction!
The drug is prescribed at the earliest possible date from the onset of clinical symptoms in a dose of 6 million IU (2 million ME bolus + 4 million ME in infusion over 60 minutes).
The drug is administered according to the following scheme: the contents of one bottle (2 million ME) are diluted in 20 ml of 0.9% sodium chloride solution and injected bolus. For the preparation of the infusion solution, the contents of two vials (4 million ME) are diluted in 0.9% sodium chloride solution (20 ml per each vial), then the total volume of the solution is brought to 100 ml and injected iv in 60 min.
The solution is prepared immediately before use and can not be stored!
From the coagulation system of the blood: bleeding of varying severity. With the development of local bleeding (including from the sites of punctures, gums), which are the most frequent side effect when using the drug, as a rule, no additional interventions are required. With the development of serious complications - internal bleeding (lowering the hemoglobin level by more than 3 g / dL) or hemorrhagic stroke, immediate stopping of the drug administration and, if necessary, transfusion of blood components, is required.
Administration of the drug in therapeutic doses, as a rule, does not lead to the occurrence of allergic reactions and to a decrease in blood pressure.
- diseases that show increased bleeding (including hemorrhagic diathesis - hemophilia, thrombocytopenia) or conditions associated with a high risk of bleeding;
- extensive surgical intervention or extensive trauma up to 4 weeks;
- resuscitation measures that required intensive indirect cardiac massage, including cardiopulmonary resuscitation for more than 10 minutes;
- cardiogenic shock (class IV according to Kiplip);
- liver disease with pronounced disturbances of the hemostasis system;
- puncture of uncompressed vessels (v. subclavia);
- diabetic hemorrhagic retinopathy;
- previous hemorrhagic stroke;
- systolic blood pressure> 180 mm Hg. or diastolic blood pressure> 110 mm Hg, refractory to treatment;
- Suspicion of aortic dissection;
- septic endocarditis;
- Hypersensitivity to the components of the drug.
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy. Data on the safety of the drug during lactation (breastfeeding) is not provided.
APPLICATION FOR FUNCTIONS OF THE LIVER
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug is contraindicated in liver diseases, accompanied by severe disturbances of the hemostasis system.
To increase the effectiveness of Purolase therapy, simultaneous use of acetylsalicylic acid and heparin is recommended, which should be administered immediately after the diagnosis of acute myocardial infarction. The recommended initial dose of acetylsalicylic acid is 250-325 mg. In this case, for a rapid onset of the drug, you need to use an acetylsalicylic acid tablet that is not coated with an enteric coating (if only dosage forms covered with an enteric coating are available, the first tablet must be chewed). In the following days, the dose of acetylsalicylic acid is 100 mg / day for a long time after the infarction. The dose of heparin is calculated depending on the body weight. The appointment of heparin is recommended starting with IV bolus administration at a rate of 60 units / kg, but not more than 4000 units, followed by infusion of heparin for 24-48 hours at a rate of 1000 U / h under the control of APTT every 3 hours before APTT in 2-2.5 times higher than the original values.
Symptoms: manifestations of hemorrhagic syndrome.
Treatment: a small amount of bleeding can be stopped without stopping the administration of Purolase by temporarily disabling heparin infusion with additional control of APTT.
If life-threatening bleeding occurs, the drug should be stopped and freshly frozen plasma or whole blood should be prescribed. If necessary, to neutralize the effect of Purolase, it is possible to introduce an antifibrinolytic agent (including aprotinin, aminocaproic or tranexamic acid).
With simultaneous administration of Purolase with antiplatelet agents, oral anticoagulants, overdose of heparin (more than 4000 units) and other drugs acting on the blood coagulation system, the risk of bleeding increases.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light, out of reach of children at a temperature of 2 to 20 В° C. Shelf life - 3 years. The drug should not be used after the expiry date indicated on the package.