Metalyse IV Injection 5 mg/ml
Metalyse IV Injection 5 mg/ml Uses, Dosage, Side Effects, Food Interaction and all others data.
Metalyse IV Injection 5 mg/ml is a tissue plasminogen activator (tPA) produced by recombinant DNA technology using an established mammalian cell line (Chinese Hamster Ovary cells). Metalyse IV Injection 5 mg/ml is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA (cDNA) for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296–299 in the protease domain. Tenectaplase is a sterile, white to off-white, lyophilized powder for single intravenous (IV) bolus administration after reconstitution with Sterile Water for Injection (SWFI), USP. Each vial of Tenectaplase nominally contains 52.5 mg Metalyse IV Injection 5 mg/ml, 0.55 g L-arginine, 0.17 g phosphoric acid, and 4.3 mg polysorbate 20, which includes a 5% overfill. Each vial will deliver 50 mg of Metalyse IV Injection 5 mg/ml. Metalyse IV Injection 5 mg/ml is a modified form of human tissue plasminogen activator (tPA) that binds to fibrin and converts plasminogen to plasmin. In the presence of fibrin, in vitro studies demonstrate that Metalyse IV Injection 5 mg/ml conversion of plasminogen to plasmin is increased relative to its conversion in the absence of fibrin. This fibrin specificity decreases systemic activation of plasminogen and the resulting degradation of circulating fibrinogen as compared to a molecule lacking this property. Following administration of 30, 40, or 50 mg of Metalyse IV Injection 5 mg/ml, there are decreases in circulating fibrinogen (4%-15%) and plasminogen (11%-24%). The clinical significance of fibrinspecificity on safety (e.g., bleeding) or efficacy has not been established. Biological potency is determined by an in vitro clot lysis assay and is expressed in Metalyse IV Injection 5 mg/ml-specific units. The specific activity of Metalyse IV Injection 5 mg/ml has been defined as 200 units/mg.
Metalyse IV Injection 5 mg/ml is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Trade Name | Metalyse IV Injection 5 mg/ml |
Availability | Prescription only |
Generic | Tenecteplase |
Tenecteplase Other Names | Tenecteplasa, Tenecteplase, TNK-tPA |
Related Drugs | aspirin, lisinopril, metoprolol, propranolol, Plavix, Brilinta |
Weight | 5 mg/ml |
Type | IV Injection |
Formula | C2561H3919N747O781S40 |
Weight | 58951.2 Da |
Groups | Approved |
Therapeutic Class | Fibrinolytics (Thrombolytics) |
Manufacturer | Radiant Pharmaceuticals Ltd. |
Available Country | Bangladesh |
Last Updated: | October 19, 2023 at 6:27 am |
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Uses
Metalyse IV Injection 5 mg/ml is used for use in the reduction of mortality associated with acute myocardial infarction (AMI). Treatment should be initiated as soon as possible after the onset of acute myocardial infarction symptoms.
Pediatric Use: The safety and effectiveness of Metalyse IV Injection 5 mg/ml in pediatric patients have not been established.
In elderly patients: The benefits of Metalyse IV Injection 5 mg/ml on mortality should be carefully weighed against the risk of increased adverse events, including bleeding.
Metalyse IV Injection 5 mg/ml is also used to associated treatment for these conditions: ST Elevation Myocardial Infarction (STEMI)
How Metalyse IV Injection 5 mg/ml works
Metalyse IV Injection 5 mg/ml binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
Dosage
Metalyse IV Injection 5 mg/ml dosage
Metalyse IV Injection 5 mg/ml is for intravenous administration only. The recommended total dose should not exceed 50 mg and is based upon patient weight. A single bolus dose should be administered over 5 seconds based on patient weight. Treatment should be initiated as soon as possible after the onset of AMI symptoms.
- Patient Weight <60 kg: 30 mg Metalyse IV Injection 5 mg/ml
- Patient Weight ≥60 to <70 kg: 35 mg Metalyse IV Injection 5 mg/ml
- Patient Weight ≥70 to <80 kg: 40 mg Metalyse IV Injection 5 mg/ml
- Patient Weight ≥80 to <90 kg: 45 mg Metalyse IV Injection 5 mg/ml
- Patient Weight ≥90 kg: 50 mg Metalyse IV Injection 5 mg/ml
- The product should be visually inspected prior to administration for particulate matter and discoloration. Metalyse IV Injection 5 mg/ml may be administered as reconstituted at 5 mg/mL.
- Precipitation may occur when Metalyse IV Injection 5 mg/ml is administered in an IV line containing dextrose. Dextrose-containing lines should be flushed with a saline-containing solution prior to and following single bolus administration of Metalyse IV Injection 5 mg/ml.
- Reconstituted Metalyse IV Injection 5 mg/ml should be administered as a single IV bolus over 5 seconds.
- Because Metalyse IV Injection 5 mg/ml contains no antibacterial preservatives, it should be reconstituted immediately before use. If the reconstituted Metalyse IV Injection 5 mg/ml is not used immediately, refrigerate the Metalyse IV Injection 5 mg/ml vial at 2-8°C and use within 8 hours.
- Although the supplied syringe is compatible with a conventional needle, this syringe is designed to be used with needleless IV systems. From the information below, follow the instructions applicable to the IV system in use.
Side Effects
The most frequent adverse reaction associated with Metalyse IV Injection 5 mg/ml is bleeding. Should serious bleeding occur, concomitant heparin and antiplatelet therapy should be discontinued. Death or permanent disability can occur in patients who experience stroke or serious bleeding episodes. For Metalyse IV Injection 5 mg/ml-treated patients in ASSENT-2, the incidence of intracranial hemorrhage was 0.9% and any stroke was 1.8%. The incidence of all strokes, including intracranial bleeding, increases with increasing age
Precaution
General: Standard management of myocardial infarction should be implemented concomitantly with Metalyse IV Injection 5 mg/ml treatment. Arterial and venous punctures should be minimized. Noncompressible arterial puncture must be avoided and internal jugular and subclavian venous punctures should be avoided to minimize bleeding from the noncompressible sites. In the event of serious bleeding, heparin and antiplatelet agents should be discontinued immediately. Heparin effects can be reversed by protamine.
Readministration: Readministration of plasminogen activators, including Metalyse IV Injection 5 mg/ml, to patients who have received prior plasminogen activator therapy has not been systematically studied. Three of 487 patients tested for antibody formation to Metalyse IV Injection 5 mg/ml had a positive antibody titer at 30 days. The data reflect the percentage of patients whose test results were considered positive for antibodies to Metalyse IV Injection 5 mg/ml in a radioimmunoprecipitation assay, and are highly dependent on the sensitivity and specificity of the assay. Additionally, the observed incidence of antibody positivity in an assay may be influenced by several factors including sample handling, concomitant medications, and underlying disease. For these reasons, comparison of the incidence of antibodies to Metalyse IV Injection 5 mg/ml with the incidence of antibodies to other products may be misleading. Although sustained antibody formation in patients receiving one dose of Metalyse IV Injection 5 mg/ml has not been documented, readministration should be undertaken with caution.
Hypersensitivity: Hypersensitivity, including urticarial / anaphylactic reactions, have been reported after administration of Metalyse IV Injection 5 mg/ml (e.g., anaphylaxis, angioedema, laryngeal edema, rash, and urticaria). Monitor patients treated with Metalyse IV Injection 5 mg/ml during and for several hours after infusion. If symptoms of hypersensitivity occur, appropriate therapy should be initiated.
Interaction
Formal interaction studies of Tenectaplase with other drugs have not been performed. Patients studied in clinical trials of Metalyse IV Injection 5 mg/ml were routinely treated with heparin and aspirin. Anticoagulants (such as heparin and vitamin K antagonists) and drugs that alter platelet function. (such as acetylsalicylic acid, dipyridamole, and GP IIb/IIIa inhibitors) may increase the risk of bleeding if administered prior to, during, or after Tenectaplase therapy.
Food Interaction
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
Metalyse IV Injection 5 mg/ml Hypertension interaction
[Major] The most common complication encountered during tenecteplase therapy is bleeding.
Metalyse IV Injection 5 mg/ml therapy in patients with acute myocardial infarction is contraindicated in patients with active internal bleeding, history of cerebrovascular accident, intracranial or intraspinal surgery or trauma within 2 months, intracranial neoplasms, arteriovenous malformations or aneurysm, bleeding diathesis or severe uncontrolled hypertension, due to an increased risk of bleeding.
Each patient being considered for therapy should be carefully evaluated and anticipated benefits weighed against potential risks associated with therapy.
Metalyse IV Injection 5 mg/ml Drug Interaction
Major: enoxaparin, heparinModerate: aspirin, clopidogrelUnknown: alteplase, pioglitazone, albumin human, spironolactone, diltiazem, ciprofloxacin, sulfamethoxazole / trimethoprim, glucose, ethanol, arginine, metoprolol, sodium chloride, acetaminophen, tramadol, valproic acid, phytonadione
Metalyse IV Injection 5 mg/ml Disease Interaction
Half Life
1.9 hours (mammalian reticulocytes, in vitro) >20 hours (yeast, in vivo) >10 hours (Escherichia coli, in vivo)
Clearance
- 99 - 119 mL/min [acute myocardial infarction patients]
Pregnancy & Breastfeeding use
Pregnancy: Tenectaplase has been shown to elicit maternal and embryo toxicity in rabbits given multiple IV administrations. In rabbits administered 0.5, 1.5, and 5.0 mg/kg/day during organogenesis, vaginal hemorrhage resulted in maternal deaths. Subsequent embryonic deaths were secondary to maternal hemorrhage and no fetal anomalies were observed. Tenectaplase does not elicit maternal and embryo toxicity in rabbits following a single IV administration. Thus, in developmental toxicity studies conducted in rabbits, the no observable effect level (NOEL) of a single IV administration of Tenectaplase on maternal or developmental toxicity (5 mg/kg) was approximately 7 times human exposure (based on AUC) at the dose for AMI. There are no adequate and well controlled studies in pregnant women. Tenectaplase should be given to pregnant women only if the potential benefits justify the potential risk to the fetus.
Nursing Mothers: It is not known if Tenectaplase is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Tenectaplase is administered to a nursing woman.
Contraindication
Metalyse IV Injection 5 mg/ml therapy in patients with acute myocardial infarction is contraindicated in the following situations because of an increased risk of bleeding:
- Active internal bleeding
- History of cerebrovascular accident
- Intracranial or intraspinal surgery or trauma within 2 months
- Intracranial neoplasm, arteriovenous malformation, or aneurysm
- Known bleeding diathesis
- Severe uncontrolled hypertension
Storage Condition
Store lyophilized Metalyse IV Injection 5 mg/ml at controlled room temperature not to exceed 30°C or under refrigeration 2-8°C. Do not use beyond the expiration date stamped on the vial.
Innovators Monograph
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Metalyse IV Injection 5 mg/ml contains Tenecteplase see full prescribing information from innovator Metalyse IV Injection 5 mg/ml Monograph, Metalyse IV Injection 5 mg/ml MSDS, Metalyse IV Injection 5 mg/ml FDA label