Purolaza

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Purolaza: 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. Use in childhood
11. For violations of liver function
12. Drug interactions
13. Analogs
14. Terms and conditions of storage
15. Terms of dispensing from pharmacies
16. Reviews
17. Price in pharmacies

Latin name: Purolase

ATX code: B01AD

Active ingredient: prourokinase (Prourokinase)

Manufacturer: Federal State Budgetary Institution "National Medical Research Center of Cardiology" of the Ministry of Health of the Russian Federation (Russia)

Description and photo update: 2019-03-12

Lyophilisate for preparation of solution for intravenous administration of Purolaz

Purolaza is an enzymatic thrombolytic drug, tissue plasminogen activator.

Release form and composition

Dosage form - lyophilisate for the preparation of a solution for intravenous (i / v) administration: white porous mass or odorless amorphous powder (in a cardboard box 1 bottle containing 50 ml of lyophilisate, and instructions for use of Purolase).

The active substance in the composition of 50 ml of lyophilisate: recombinant prourokinase - 2,000,000 international units (ME) (contains sodium chloride - 180 mg).

Pharmacological properties

Pharmacodynamics

Purolase belongs to the recombinant fibrin-specific plasminogen activators of the urokinase type. The active principle of the drug is the recombinant prourokinase enzyme, a single-chain molecule with a molecular weight of 46,000 Da. This molecule contains two polypeptide chain-domains with molecular weights of 17,000 and 29,000 Da, which are connected by a disulfide bridge and consist, respectively, of the regulatory part and the catalytic domain of the enzyme.

Recombinant prourokinase, through its regulatory part, specifically interacts with fibrin-bound plasminogen and catalyzes the conversion of plasminogen into plasmin (protease), which can lyse thrombi (fibrin clots).

Pharmacokinetics

No data provided.

Indications for use

Purolazu is prescribed as a thrombolytic agent for acute myocardial infarction in the first 6 hours after its development.

Contraindications

Absolute contraindications to Purolaza:

conditions with a high probability of bleeding or pathology accompanied by increased bleeding (hemorrhagic diathesis, including thrombocytopenia, hemophilia, and others);
extensive surgery or extensive trauma up to 28 days old;
resuscitation measures that required intensive chest compressions, including cardiopulmonary resuscitation for more than 10 minutes;
cardiogenic shock (according to Killip's classification - IV class);
liver pathologies with severe disorders of the hemostasis system;
puncture of non-compressed vessels (v. subclavia);
diabetic hemorrhagic retinopathy;
previous hemorrhagic stroke;
diastolic blood pressure (BP) ≥ 110 mm. rt. Art., refractory to therapy, systolic blood pressure ≥ 180 mm Hg. Art.;
suspicion of aortic dissection;
septic endocarditis;
pregnancy;
lactation period;
children under the age of 18;
individual intolerance to the components of Purolase.

Purolaza, instructions for use: method and dosage

The Purolaz solution prepared from the lyophilisate is administered intravenously as early as possible in the first 6 hours after the development of clinical signs of the disease. It is allowed to use the drug in the period from 6 to 12 hours from the moment of the onset of the pathology if the patient has appropriate indications for thrombolytic treatment. It is important to take into account that the effectiveness of the therapy during this period may decrease.

The total recommended dose of the drug should not exceed 100,000 IU per 1 kg of body weight.

Purolaza can be entered at choice according to one of two schemes:

Double bolus.
Bolus plus infusion.

When choosing the first scheme, the first bolus of 4,000,000 ME + the second bolus (0 ÷ 4,000,000) IU is administered, in a dose of 4,000,000 ÷ 8,000,000 ME, depending on the patient's weight.

Purolase dose and volume of solution for administration (2,000,000 IU vial diluted with 20 ml of 0.9% sodium chloride solution) for the first bolus (two 2,000,000 IU vials) / second bolus (after 25 minutes; 1-2 vials 2 000 000 IU), depending on the patient's body weight when using the double bolus scheme, are:

up to 60 kg: 4,000,000 IU (single bolus) and 40/0;
from 60 to 75 kg: 4,000,000 + 1,000,000 IU and 40/10 (½ bottle);
from 75 to 90 kg: 4,000,000 + 2,000,000 IU and 40/20 (1 bottle);
from 90 to 110 kg: 4,000,000 + 3,000,000 IU and 40/30 (1.5 bottles);
more than 110 kg: 4,000,000 + 4,000,000 IU and 40/40 (2 bottles).

The lyophilisate contained in two vials (4,000,000 IU) is added to 40 ml of 0.9% sodium chloride solution (20 ml per 1 bottle of Purolase) and thoroughly dissolved. The resulting solution in full (40 ml) is injected intravenously in a stream in the form of the first bolus. If the patient's weight exceeds 60 kg, a second bolus is additionally administered. To do this, the contents of an additional vial / vials with a lyophilisate are dissolved in 20 ml of 0.9% sodium chloride solution and from 10 to 40 ml (from 1,000,000 to 4,000,000 ME) of the total volume is injected intravenously in a stream 25 minutes after the first bolus as a second bolus.

In order to ensure reliable solubility of the drug, it is recommended to dissolve each vial with lyophilisate in 20 ml of 0.9% sodium chloride solution, and not in a smaller volume. The content of Purolase in 0.9% sodium chloride solution should not be more than 100,000 IU per 1 ml. The solution from the lyophilisate is prepared immediately before administration and is not subject to storage.

When choosing the second scheme, Purolaz is administered intravenously in doses, the size of which is set depending on the patient's body weight, namely:

up to 60 kg: 2,000,000 IU is administered as a bolus, after which it is administered as an infusion over 1 hour, the dose of which is set on the basis of 100,000 IU / per 1 kg x (body weight, kg) - 2,000,000 IU;
from 60 to 85 kg: total dose - 6,000,000 ME (2,000,000 ME is administered as a bolus, and then over 1 hour - 4,000,000 ME as an infusion);
more than 85 kg: total dose - 8,000,000 ME (2,000,000 ME is administered as a bolus, and then within 1 hour - 6,000,000 ME as an infusion).

The lyophilisate contained in 1 vial (2,000,000 IU) is dissolved in 20 ml of 0.9% sodium chloride solution and administered as a bolus. To prepare the infusion solution, the contents of two / three vials (respectively 4,000,000/6,000,000 ME) are dissolved in 0.9% sodium chloride solution (20 ml for each bottle). After that, the total volume of the solution is brought to 100 ml and injected intravenously over 1 hour.

In order to ensure reliable solubility of Purolase, it is recommended to dissolve the contents of each vial in 20 ml of 0.9% sodium chloride solution, and not in a smaller volume. The content of the drug in 0.9% sodium chloride solution should not exceed 100,000 IU per 1 ml.

The solution is prepared immediately before administration, do not store.

Side effects

During therapy with Purolaza, bleeding of varying severity may occur. If local bleeding is noted (for example, from the gums, puncture sites, and others), which are among the most frequent adverse events when using the drug, as a rule, additional interventions are not required. If the patient has serious complications - internal bleeding (a decrease in hemoglobin by more than 3 g per 1 dl), the administration of Purolase is canceled, and, if necessary, blood transfusions are made.

In cases of suspected hemorrhagic stroke, an urgent consultation with a neurologist and an appropriate examination (computed tomography and others) and therapy are required.

With effective coronary thrombolysis, the development of reperfusion arrhythmia is likely. Its occurrence may require the appointment of a generally accepted antiarrhythmic treatment.

The introduction of Purolase in therapeutic doses usually does not lead to a decrease in blood pressure.

The use of the drug in most cases is either not accompanied by the development of allergic reactions at all, or they are very weakly expressed. When they appear, conventional antiallergic treatment is carried out. Anaphylactic reactions (that is, due to immunoglobulin E) were not observed even after repeated administration of the solution.

Overdose

The main symptoms of a prourokinase overdose: hemorrhagic complications.

Therapy: stopping minor bleeding is possible without stopping the administration of Purolase, by temporarily stopping the infusion of heparin with additional control of the activated partial thromboplastin time. The administration of the drug should be abandoned if life-threatening bleeding develops. In such cases, fresh frozen plasma or whole blood is prescribed. In order to neutralize the effect of the drug, if necessary, an antifibrinolytic agent (for example, tranexamic or aminocaproic acid) can be administered.

special instructions

Therapy should be carried out by qualified specialists, following the standards of medical care for patients with acute myocardial infarction, with the obligatory prescription of antiplatelet and anticoagulant treatment.

In order to increase the effectiveness of Purolase, it is recommended to use it in combination with heparin, clopidogrel and acetylsalicylic acid (ASA). These drugs should be administered immediately after the diagnosis of acute myocardial infarction.

The initial dose of ASA varies from 160 to 250 mg. For a quick onset of action of the drug, ASA should be used in non-enteric coated tablets. The patient should chew the first dose and wait for its absorption from the oral cavity. In the future, from 75 to 100 mg of ASA is used per day for an indefinitely long period after a heart attack.

The loading dose of clopidogrel is 300 mg with a transition to a maintenance dose - 75 mg per day during the first year after myocardial infarction.

The dosage of heparin is set individually, depending on the patient's weight. Its introduction begins with an IV bolus at the rate of 60 U per 1 kg of body weight, but not more than 4000 U, followed by infusion of heparin for 24-48 hours at a rate of 1000 U per 1 hour under the control of activated partial thromboplastin time every 3 h before its increase by 2–2.5 times compared with the initial values.

Like other thrombolytic drugs, Purolazu is recommended to be used in conditions where standard resuscitation equipment and appropriate drugs are available.

The most common complication associated with drug therapy is bleeding. The combined use of dual antiplatelet therapy and low molecular weight heparins or unfractionated heparin (250 mg ASA + 300 mg clopidogrel) increases the risk of bleeding. In this regard, when carrying out thrombolytic therapy, it is important to carefully monitor the areas of possible bleeding, including the site of catheter insertion, venous and arterial punctures, injections and incisions. The use of rigid catheters, intravenous injections and punctures of uncompressible vessels is not recommended.

Application during pregnancy and lactation

Pregnancy and lactation are contraindications to Purolaz.

Pediatric use

Patients under 18 years of age are not prescribed Purolaza due to the lack of data on the safety and efficacy of its use in patients of this age group.

For violations of liver function

Prescribing the drug is contraindicated in patients with liver pathologies with severe disorders of the hemostatic system.

Drug interactions

With the combined use of Purolase with indirect anticoagulants, antiplatelet agents, other drugs that affect the blood coagulation system, as well as with an overdose of heparin (using a dose of more than 4000 U), the likelihood of bleeding may increase.

Analogs

The analogue of Purolaza is Aktilize, Gemaza. Reveliza, Streptokinase, Thromboflux, Urokinase Medak, Eberkinase (recombinant streptokinase), etc.

Terms and conditions of storage

Store in a place protected from light and moisture at temperatures up to 20 ° C. Keep out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Purolaz

Reviews about Purolaz are ambiguous. There are reports both confirming its effectiveness, and vice versa, indicating the absence of a therapeutic effect. Among the advantages most often noted is the absence of the need for stenting after using the drug. As a disadvantage, the high cost of Purolaza is mainly indicated.

Price for Purolazu in pharmacies

The approximate price for Purolazu (1 bottle in the package containing 50 ml of lyophilisate) is 8500 rubles.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, 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!