Purolase lyophilizate 2mlIU 50ml vial 1pc, 50ml vial 1pc

Composition

Recombinant prourokinase (contains 180 mg sodium chloride) 2,000,000 ME. Excipients: sodium chloride-180 mg

Pharmacological action

Pharmacological action is a thrombolytic. Recombinant fibrin is a specific plasminogen activator of the urokinase type.

It is a single-stranded molecule with a molecular weight of 46,000 Da, consisting of two polypeptide chains-domains with molecular weights of 17,000 and 29,000 Da, which contain the regulatory part 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 conversion of plasminogen into a plasmin protease capable of lysing fibrin clots (blood clots).

Pharmacokinetics

Data on the pharmacokinetics of Purolase were not provided.

Indications

Acute myocardial infarction in the first 6 hours after the onset of the disease (as a thrombolytic agent).

Contraindications

of the Disease, manifested an increased risk of bleeding (haemorrhagic diathesis — hemophilia, thrombocytopenia, etc. ) or condition with a high risk of bleeding;

– Hypersensitivity to the drug;

– Extensive surgery or extensive trauma, previous to 4 weeks;

– Resuscitation, intensive requiring chest compressions, including CPR for more than 10 min;

– Cardiogenic shock (class IV by Killip);

– liver Disease with severe disorders of hemostasis;

– Needling compressively vessels (v. subclavia);

– Diabetic hemorrhagic retinopathy;

– Prior hemorrhagic stroke;

– Systolic blood pressure (BP) 3 180 mm. RT. article or diastolic blood pressure of 110 mm. 3 RT. article refractory to treatment;

– Suspected aortic dissection;

Septic endocarditis;

– Pregnancy and lactation period;

– Children’s age up to 18 years since the efficacy and safety of the drug in this group of individuals has not been studied.

Side effects

Bleeding of varying severity. With the development of local bleeding (for example, from puncture sites, gums, etc. ), which are the most common side effect when using the drug, as a rule, additional interventions are not required. With the development of serious complications — internal bleeding (a decrease in hemoglobin by more than 3 g/dl), an immediate stop of the drug use and, if necessary, blood transfusion is required.

If a hemorrhagic stroke is suspected, urgent consultation with a neurologist and appropriate examination (computed tomography, etc. ) and treatment are required.

Effective coronary thrombolysis may be accompanied by the occurrence of reperfusion arrhythmia, which may require the use of conventional antiarrhythmic therapy.

use of the drug in therapeutic doses, as a rule, does not lead to a decrease in blood pressure.

Allergic reactions with the introduction of the drug, usually, are not observed or expressed very weakly. With the development of allergic reactions, conventional anti-allergic therapy is used. Anaphylactic reactions (i. e., IgE-related) were not observed even with repeated use of the drug.

Interaction

The risk of bleeding may increase with the simultaneous use of antiplatelet agents, indirect anticoagulants, with an overdose of heparin (more than 4000 units) and other drugs acting on the blood coagulation system.

How to take, course of use and dosage

For intravenous use only!

The drug should be administered as early as possible in the first 6 hours after the onset of clinical symptoms. It is permissible to administer the drug in the period from 6 to 12 hours from the moment of development of the disease, if there are appropriate indications for thrombolytic therapy. It should be borne in mind that the effectiveness of thrombolytic therapy may decrease during this period.

The recommended total dose of the drug should not exceed 100,000 IU / kg of body weight.

The drug can be administered according to the “double bolus” scheme or according to the “bolus plus infusion”scheme.

use of the drug according to the “double bolus” scheme.

The drug is administered intravenously according to the “double bolus” scheme: the first bolus is 4,000,000IU + the second bolus (0 4,000,000) ME, at a dose of 4,000,000 8,000,000 ME, depending on the patient’s body weight according to Table 1.

The dose of the first bolus should not exceed 4,000,000 IU.

Drug use scheme:

The contents of two vials of the drug (4,000,000 IU) are thoroughly dissolved in 40 ml of 0.9% sodium chloride solution (20 ml for each bottle) and the entire volume (40 ml) is administered intravenously as the first bolus jet. If the patient’s weight exceeds 60 kg, then a second additional bolus is administered at a dose according to Table 1. To do this, the contents of the additional vial(s) of the drug are dissolved in 20 ml of 0.9% sodium chloride solution and 10-40 ml (1,000,000-4,000,000 IU) of the total volume is administered 25 minutes after the first bolus intravenously in the form of a second bolus jet.

To ensure reliable solubility of the drug, dissolve each vial in 20 ml of 0.9% sodium chloride solution, and not in a smaller volume. The concentration of the drug solution in 0.9% sodium chloride solution should not exceed 100,000 IU / ml. The solution of the drug is prepared immediately before use and is not subject to storage.

use of the drug according to the “bolus + infusion” scheme.

In patients with a body weight of 60 to 85 kg, the drug is administered intravenously at a total dose of 6,000,000 IU (2,000,000 IU bolus, then 4,000,000 IU as an infusion for 60 minutes).

In patients with a body weight of more than 85 kg, the drug is administered intravenously at a total dose of 8,000,000 IU (2,000,000 IU bolus, then 6,000,000 IU as an infusion for 60 minutes).

In patients with a body weight of less than 60 kg, the drug is administered intravenously according to the scheme: 2,000,000 IU bolus, then as an infusion for 60 minutes, the dose of which is calculated by the formula:

100,000 IU / kg × [body weight in kg] minus 2,000,000 IU.

Drug use scheme:

The contents of one vial (2,000,000 IU) are dissolved in 20 ml of 0.9% sodium chloride solution and administered by bolus. To prepare the infusion solution, the contents of two (4,000,000 IU) or three (6,000,000 IU) vials are dissolved in 0.9% sodium chloride solution (20 ml for each bottle), then the total volume of the solution is adjusted to 100 ml and administered intravenously for 60 minutes.

To ensure reliable solubility of the drug, dissolve each vial in 20 ml of 0.9% sodium chloride solution, and not in a smaller volume. The concentration of the drug solution in 0.9% sodium chloride solution should not exceed 100,000 IU / ml. The solution of the drug is prepared immediately before use and is not subject to storage.

Overdose

Symptoms: hemorrhagic complications.

Treatment: minor bleeding can be stopped without stopping the drug use by temporarily stopping the heparin infusion with additional monitoring of APTT (activated partial thromboplastin time).

If life-threatening bleeding occurs, the drug use should be stopped and fresh frozen plasma or whole blood should be prescribed. If necessary, an antifibrinolytic agent, such as aminocaproic acid or tranexamic acid, can be administered to neutralize the effect of the drug.

Description

Amorphous powder or porous mass of white color, odorless.

Special instructions

Treatment of myocardial infarction should be carried out by qualified specialists in accordance with the standards of medical care for patients with acute myocardial infarction, with the mandatory use of anticoagulant and antiplatelet therapy.

Additional recommendations for the use of anticoagulant and antiplatelet therapy to increase the effectiveness of Purolase therapy.

Concomitant use of acetylsalicylic acid, clopidogrel, and heparin is recommended, and should be administered immediately after the diagnosis of acute myocardial infarction. The recommended starting dose of acetylsalicylic acid is 160-250 mg. In this case, for a quick start of the drug’s action, it is necessary to use an acetylsalicylic acid tablet that is not covered with an enteric coating.

The first dose must be chewed and wait for its absorption from the oral cavity. Subsequently, it is recommended to take acetylsalicylic acid at a dose of 75-100 mg per day indefinitely after a heart attack.

Clopidogrel is used in a loading dose of 300 mg with a transition to a maintenance dose of 75 mg per day for the first 12 months after a myocardial infarction. The dose of heparin is calculated depending on body weight. use of heparin is recommended to start with an intravenous bolus at the rate of 60 U / kg, but not more than 4000 U, followed by infusion of heparin for 24-48 hours at a rate of 1000 U / h under the control of APTT every 3 hours until the APTT increases 2-2.5 times higher than the initial values.

Form of production

Lyophilizate for the preparation of a solution for intravenous use of 2,000,000 IU in vials of 50 ml. 1 bottle with instructions for use in a cardboard pack.

Storage conditions

Store in a dry place protected from light at a temperature of 2 to 20 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Prourokinase

Conditions of release from pharmacies

By prescription

Dosage form

lyophilizate for solution preparation