Metalize
Metalize: 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. For violations of liver function
- 11. Use in the elderly
- 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: Metalyse
ATX code: B01AD11
Active ingredient: tenecteplase (Tenecteplase)
Manufacturer: Boehringer Ingelheim Pharma (Germany)
Description and photo updated: 2018-29-11
Prices in pharmacies: from 61,945 rubles.
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Metalize is a fibrinolytic drug, a genetically modified recombinant plasminogen activator.
Release form and composition
The drug is produced in the form of a lyophilisate for the preparation of a solution for intravenous (IV) administration: a white or pale yellow mass practically odorless [in glass vials, colorless, in a cardboard box 1 bottle complete with a solvent (water for injection in a plastic syringe), disposable needle and adapter, and instructions for use of Metalise].
1 bottle contains:
- active substance: tenecteplase - 30, 40 or 50 mg, which is equivalent to 6000 (unit of action), 8000 or 10,000 units, respectively, 1 ml of the finished solution contains 5 mg or 1000 units;
- auxiliary components: arginine, phosphoric acid 85% (solution acidity 7.3), polysorbate 20.
Pharmacological properties
Pharmacodynamics
Metalize is a fibrinolytic drug. Its active ingredient, tenecteplase, is a recombinant fibrin-specific plasminogen activator, a derivative of the natural tissue plasminogen activator, modified in three areas.
The mechanism of action is due to the ability of tenecteplase to bind to the fibrin component of the thrombus. This allows it to selectively accelerate the conversion of plasminogen associated with a thrombus into plasmin, which in turn destroys the fibrin base of the thrombus. Tenecteplase is distinguished from the natural tissue plasminogen activator by a higher affinity for fibrin and resistance to the inactivating effect of the endogenous inhibitor of plasminogen activator I.
The effect of plasminogen activation is confirmed by the dose-dependent consumption of α 2 -antiplasmin (plasmin inhibitor in the liquid phase) after intravenous administration of tenecteplase and a subsequent increase in the concentration of systemic plasmin. The results of comparative studies have shown that the use of the maximum dose of tenecteplase (10,000 U) causes a decrease in the concentration of fibrinogen and plasminogen by less than 15% and 25%, respectively, whereas with the use of alteplase, their level decreases by approximately 50%. Antibodies to tenecteplase were not detected 30 days after the start of Metalize administration. On the basis of angiographic data, it was established that recanalization of the artery, the thrombosis of which caused the development of acute myocardial infarction, is achieved with a single intravenous injection of tenecteplase. The effect is dose dependent.
The use of the drug reduces the mortality rate from myocardial infarction (by 6.2% after 30 days). At the same time, the frequency of bleeding (except intracranial) is lower than with the use of alteplase, and amounts to 26.4%. A decrease in the risk of bleeding is associated with a higher specificity of the drug for fibrin and the selection of a therapy regimen taking into account the body weight of patients. This contributes to a significant decrease in the need for transfusion therapy against the background of the use of tenecteplase, compared with alteplase. The incidence of intracranial hemorrhage in the tenecteplase group was 0.93%, in the alteplase group - 0.94%. The use of tenecteplase, in comparison with alteplase, had advantages in cases when, after the onset of symptoms of myocardial infarction, treatment was started later than 6 hours later. The 30-day mortality rates in the tenecteplase group were 4.3%, while in the alteplase group - 9.6%, the incidence of stroke - 0.4% and 3.3%, respectively, the incidence of intracranial hemorrhage - 0% and 1.7%, respectively …
Pharmacokinetics
Tenecteplase is eliminated from the bloodstream by binding to receptors in the liver and the formation of small peptides as a result of degradation.
In acute myocardial infarction, after a single intravenous injection of Metalize, there is a two-phase elimination of the tenecteplase antigen from the blood plasma. When using the drug in therapeutic doses, the size of the administered dose does not affect the nature of the elimination of tenecteplase.
The initial half-life (T ½) is approximately 0.5 hours, which is 5 times the T ½ of the natural tissue plasminogen activator. The final T ½ of tenecteplase can range from 0.7 to 3.6 hours.
Plasma clearance - from 70 to 168 ml / min.
In patients with increased body weight, there is a moderate increase in plasma clearance. Plasma clearance rates are usually lower in women than in men.
The older the patient's age, the lower the plasma clearance rate.
In case of impaired renal function, changes in the pharmacokinetics of tenecteplase are not expected, the drug is excreted in the bile.
The effect of liver dysfunction on the pharmacokinetics of Metalize has not been established.
Indications for use
Application Metalize is indicated for thrombolytic therapy of acute myocardial infarction.
Contraindications
- hemorrhagic stroke, stroke of unknown etiology in history;
- transient ischemic attack or ischemic stroke within the past six months;
- neoplasm with a high likelihood of bleeding;
- hemorrhagic diathesis;
- the simultaneous use of oral anticoagulants (International normalized ratio greater than 1.3);
- diseases that are accompanied by severe bleeding within the last six months;
- period of exacerbation of gastric ulcer or duodenal ulcer;
- a history of central nervous system diseases such as aneurysm, neoplasms, or surgery on the brain and spinal cord;
- severe stage of uncontrolled arterial hypertension;
- significant trauma, major surgical interventions, biopsy of the parenchymal organ within the last two months, recent traumatic brain injury (including trauma in combination with current acute myocardial infarction);
- traumatic or prolonged (more than 2 minutes) cardiopulmonary resuscitation during the previous two weeks;
- severe liver dysfunction, including cirrhosis, liver failure, portal hypertension (including esophageal varices), active hepatitis;
- aneurysm of the artery, the presence of arterial or venous vascular malformation;
- subacute bacterial endocarditis and / or acute pericarditis;
- acute pancreatitis;
- established hypersensitivity to gentamicin (due to residual traces from the manufacturing process);
- individual intolerance to tenecteplase and excipients of the drug.
With caution, after a thorough assessment of the degree of the intended benefit and the possible risk of bleeding, Metalize should be prescribed to patients with cerebrovascular diseases, systolic blood pressure (BP) above 160 mm Hg, and who have suffered bleeding from the gastrointestinal tract or urinary tract within the last 10 days, with an intramuscular injection performed within the last 2 days, over the age of 75 years, with a body weight of less than 60 kg.
In acute myocardial infarction during pregnancy or breastfeeding, the administration of the drug is possible if the intended benefit of therapy to the mother outweighs the risk to the fetus or child.
Metalize, instructions for use: method and dosage
The prepared solution is injected intravenously for 5-10 seconds.
The solution should be prepared before direct administration of the drug, observing the following recommendations:
- Before opening the lid of the vial, make sure that it is intact and that the volume is sufficient to prepare the drug solution, taking into account the patient's weight.
- To dissolve the lyophilisate into the vial, add the entire volume of water for injection from the supplied syringe. To do this, after removing the protective cap from the vial and removing the cap from the supplied syringe, screw the syringe onto the vial adapter and pierce the vial cap in the center with the tip. Then, avoiding the appearance of foam, very slowly add the water for injection into the vial and gently rotate it until the powder is completely dissolved.
- Without removing the syringe, examine the resulting solution. It should have a transparent, colorless or pale yellow structure. Do not use a cloudy solution or with small particles found during visual inspection.
- Before direct administration, the bottle must be turned over so that the syringe is at the bottom, and the required volume of solution must be taken, calculated taking into account the patient's body weight.
- After disconnecting the syringe from the vial adapter, immediately inject the drug. The catheter, through which dextrose was previously injected, should not be used for the introduction of Metalize.
- The rest of the unused solution must be disposed of.
- You can also dilute the drug using the supplied needle.
It should be borne in mind that the use of Metalize is indicated for thrombolytic therapy only for acute myocardial infarction, therefore, therapy should be started within the first hours after symptoms are detected.
Recommended doses of Metalise taking into account the patient's weight:
- less than 60 kg: 6000 U (30 mg of tenecteplase), the volume of the prepared solution is 6 ml;
- from 60 to 70 kg: 7000 U (35 mg), solution volume - 7 ml;
- from 70 to 80 kg: 8000 U (40 mg), solution volume - 8 ml;
- from 80 to 90 kg: 9000 U (45 mg), solution volume - 9 ml;
- 90 kg and above: 10,000 U (50 mg), solution volume - 10 ml.
The prescribed dose is administered once by intravenous injection for 5-10 seconds. The maximum dose of Metalize is 10,000 units.
To administer the drug, you can use a previously installed catheter for intravenous administration of only 0.9% sodium chloride solution. After the introduction of tenecteplase, the catheter must be rinsed for the purpose of its further use for the administration of other drugs.
It is contraindicated to mix the drug in an infusion bottle and a general system for intravenous administration with heparin and other drugs.
Metalize is not compatible with dextrose solution!
Side effects
- from the immune system: anaphylactoid reactions, accompanied by rash, urticaria, bronchospasm, laryngeal edema;
- from the nervous system: drowsiness, aphasia, convulsions, hemiparesis, intracranial hemorrhage (cerebral hematoma, intracranial hematoma, cerebral hemorrhage, hemorrhagic stroke, hemorrhagic transformation of stroke, subarachnoid bleeding);
- from the heart: reperfusion arrhythmias - arrhythmia, idioventricular tachyarrhythmia, asystole, extrasystole, bradycardia, tachycardia, atrioventricular block of varying degrees, ventricular fibrillation, atrial fibrillation, ventricular arrhythmia, ventricular arrhythmia, including ventricular arrhythmias pericardial bleeding;
- from the side of the vessels: bleeding, embolism;
- from the respiratory system: epistaxis and / or pulmonary bleeding;
- from the digestive system: nausea, vomiting, bleeding from the mouth, bleeding from a stomach ulcer, gastric bleeding, bloody vomiting, bleeding from the rectum, melena, bleeding into the retroperitoneal space (retroperitoneal hematoma);
- on the part of the organ of vision: intraocular hemorrhage;
- from the genitourinary system: urogenital bleeding - bleeding from the urinary tract, hematuria;
- dermatological reactions: ecchymosis;
- local reactions: external bleeding from puncture sites or from injured blood vessels;
- others: an increase in body temperature, a decrease in blood pressure, fatty embolism, the need for blood transfusion.
Overdose
Symptoms: development of bleeding.
Treatment: the use of conservative treatment methods, with significant prolonged bleeding, blood transfusion is possible.
special instructions
A specialist with experience in thrombolytic therapy should prescribe the drug Metalize. The use of the drug is also possible at the prehospital stage, subject to qualified control of the effectiveness of the treatment. It is recommended to administer the solution in a hospital setting, in the presence of standard resuscitation equipment and medicines.
If percutaneous coronary intervention (PCI) is planned in accordance with current treatment standards, it is not recommended to pre-use Metalize in full dose in combination with unfractionated heparin (single bolus up to 4000 IU), administered 1–3 hours before primary PCI in extensive myocardial infarction.
Against the background of the introduction of Metalize, the most common complication is bleeding. It should be borne in mind that the simultaneous use of heparin can potentiate these processes. Treatment should be accompanied by a thorough visual examination of the patient's body for bleeding in the areas of catheter insertion, injections, arterial and venous punctures or incisions. After using tenecteplase, it is recommended to avoid the use of rigid catheters, unreasonable manipulations and intramuscular injections.
When diagnosed with intracranial hemorrhage and other serious bleeding, heparin should be stopped immediately. If heparin was used within 4 hours prior to bleeding, protamine sulfate may be prescribed. In case of ineffectiveness of conservative therapy, transfusion administration of cryoprecipitate, fresh frozen plasma and platelets is indicated. It is produced in accordance with clinical indications based on the results of laboratory tests carried out after each injection. It is advisable to continue the cryoprecipitate infusion until a fibrinogen concentration of about 1 g / L is reached. Antifibrinolytic agents can be used if necessary.
In coronary thrombolysis, the risk of reperfusion-related arrhythmias should be considered. Reperfusion arrhythmias are associated with the risk of cardiac arrest, a threat to life, therefore, the immediate use of conventional antiarrhythmic therapy is required.
Concomitant therapy with glycoprotein IIb or IIIa antagonists increases the risk of bleeding.
With thrombosis of the left heart, including mitral stenosis or atrial fibrillation, the risk of thromboembolic complications increases in patients with Metalize.
There is no experience with re-use of tenecteplase.
If symptoms of anaphylactoid reaction appear, the administration of Metalize should be discontinued.
The prepared solution is stable at a storage temperature of 2–8 ° C for 24 hours and at a temperature of 30 ° C for 8 hours. From a microbiological point of view, storage of the finished solution should not be allowed, it must be introduced immediately after the lyophilisate is diluted.
Application during pregnancy and lactation
Caution should be exercised when prescribing the drug Metalize during pregnancy or breastfeeding.
The use of Metalize in acute myocardial infarction is possible if the intended benefits of therapy for the mother outweigh the risk to the fetus or child.
For violations of liver function
The appointment of Metalize is contraindicated in case of severe liver dysfunction, including patients with cirrhosis, hepatic failure, portal hypertension (including esophageal varices), active hepatitis.
Use in the elderly
Particular care should be taken when prescribing Metalize to patients over the age of 75, it is necessary to assess the likelihood of bleeding and compare the degree of risk and benefit of therapy.
Drug interactions
No clinically significant interaction of Metalize with other agents often used in patients with acute myocardial infarction has been established.
Introduction Metalyse before, simultaneously or after the use of drugs that change the coagulation properties of blood or affect platelet function, may increase the risk of bleeding.
Tenecteplase is incompatible with dextrose solutions.
Analogs
Analogs of Metalize are: Gemaza, Aktilize, Fibrinolysin, Trombovazim, Distreptaza, Zigris, Streptokinase, Celiasis, Eberkinase, Tobarpin, Biostrepta, Elaxim, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 30 ° C in a dark place.
Shelf life: lyophilisate - 2 years, solvent - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Metalize
Reviews about Metaliz are positive. Experts and patients point to a high degree of effectiveness of the drug when it is administered within the first four hours from the onset of the pain syndrome of acute myocardial infarction.
Price for Metalise in pharmacies
The price on Metalliz for a package containing 1 bottle of lyophilisate (50 mg) complete with a solvent, a disposable needle and an adapter can range from 77,760 rubles.
Metalize: prices in online pharmacies
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Drug name Price Pharmacy |
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Metalese 50 mg lyophilisate for preparation of solution for intravenous administration 10 ml 1 pc. RUB 61945 Buy |
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!
