Tplase 5 mg/ml

Tplase 5 mg/ml | INDICATIONS AND USES

Tenecteplase is indicated in Acute phase of myocardial infarction (AMI).

Tplase 5 mg/ml | PHARMACOLOGY

Tenecteplase is a recombinant fibrin-specific plasminogen activator that is derived from native t-PA by modifications at three sites of the protein structure. It binds to the fibrin component of the thrombus (blood clot) and selectively converts thrombus-bound plasminogen to plasmin, which degrades the fibrin matrix of the thrombus. Tenecteplase has a higher fibrin specificity and greater resistance to inactivation by its endogenous inhibitor (PAI-1) compared to native t-PA. Tenecteplase 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.

Tplase 5 mg/ml | DOSAGE

Tenecteplase 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 Tenecteplase 
Patient Weight ≥60 to <70 kg: 35 mg Tenecteplase 
Patient Weight ≥70 to <80 kg: 40 mg Tenecteplase 
Patient Weight ≥80 to <90 kg: 45 mg Tenecteplase 
Patient Weight ≥90 kg: 50 mg Tenecteplase

Tplase 5 mg/ml | DRUG INTERACTIONS

No formal interaction studies with Tenecteplase and medicinal products commonly administered in patients with AMI have been performed. Medicinal products that affect coagulation or those that alter platelet function may increase the risk of bleeding prior to, during or after Tenecteplase therapy.

Tplase 5 mg/ml | SIDE EFFECTS

The most frequent adverse reaction associated with Tenecteplase is bleeding. If serious bleeding occurs, concomitant heparin and antiplatelet therapy should be discontinued. Death or permanent disability can occur in patients who experience stroke or serious bleeding episodes.For Tenecteplase-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. Non-intracranial major bleeding and the need for blood transfusions were lower in patients treated with Tenecteplase.Types of major bleeding reported in 1% or more of the patients were hematoma (1.7%) and gastrointestinal tract (1%). Types of major bleeding reported in less than 1% of the patients were urinary tract, puncture site (including cardiac catheterization site), retroperitoneal, respiratory tract, and unspecified. Types of minor bleeding reported in 1% or more of the patients were hematoma (12.3%), urinary tract (3.7%), puncture site (including cardiac catheterization site) (3.6%), pharyngeal (3.1%), gastrointestinal tract (1.9%), epistaxis (1.5%), and unspecified (1.3%).The following adverse reactions have been reported among patients receiving tenecteplase in clinical trials. These reactions are frequent sequelae of the underlying disease, and the effect of tenecteplase on the incidence of these events is unknown. These events include cardiogenic shock, arrhythmias, atrioventricular block, pulmonary edema, heart failure, cardiac arrest, recurrent myocardial ischemia, myocardial reinfarction, myocardial rupture, cardiac tamponade, pericarditis, pericardial effusion, mitral regurgitation, thrombosis, embolism, and electromechanical dissociation. These events can be life-threatening and may lead to death. Nausea and/or vomiting, hypotension, and fever have also been reported.

Tplase 5 mg/ml | USE DURING PREGNANCY AND LACTATION

The benefit of treatment must be evaluated against the potential risks in case of myocardial infarction during pregnancy. It is not known if tenecteplase is excreted into breast milk. It is not known if Tenecteplase is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when tenecteplase is administered to a nursing woman.

Tplase 5 mg/ml | PRECAUTIONS & WARNINGS

General: Standard management of myocardial infarction should be implemented concomitantly with Tenecteplase 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.Hypersensitivity: Hypersensitivity, including urticarial / anaphylactic reactions, have been reported after administration of Tenecteplase (e.g., anaphylaxis, angioedema, laryngeal edema, rash, and urticaria). Monitor patients treated with Tenecteplase during and for several hours after infusion. If symptoms of hypersensitivity occur, appropriate therapy should be initiated.

Tplase 5 mg/ml | USE IN SPECIAL POPULATIONS

Pediatric Use: The safety and effectiveness of tenecteplase in pediatric patients have not been established.Geriatric Use: Of the patients in ASSENT-2 who received tenecteplase, 4,958 (59%) were under the age of 65; 2,256 (27%) were between the ages of 65 and 74; and 1,244 (15%) were 75 and over. The 30-day mortality rates by age were 2.5% in patients under the age of 65, 8.5% in patients between the ages of 65 and 74, and 16.2% in patients age 75 and over. The ICH rates were 0.4% in patients under the age of 65, 1.6% in patients between the ages of 65 and 74, and 1.7% in patients age 75 and over. The rates of any stroke were 1.0% in patients under the age of 65, 2.9% in patients between the ages of 65 and 74, and 3.0% in patients age 75 and over. Major bleeding rates, defined as bleeding requiring blood transfusion or leading to hemodynamic compromise, were 3.1% in patients under the age of 65, 6.4% in patients between the ages of 65 and 74, and 7.7% in patients age 75 and over. In elderly patients, the benefits of tenecteplase on mortality should be carefully weighed against the risk of increased adverse events, including bleeding.

Tplase 5 mg/ml | THERAPEUTIC CLASS

Fibrinolytics (Thrombolytics)

Tplase 5 mg/ml | STORAGE CONDITIONS

Store lyophilized Tenecteplase at temperature not exceeding 30°C or under refrigerator 2-8°C. Keep out of reach of children.