ELAXIM 50

Indications

• Acute myocardial infarction
• Acute ischemic stroke (off-label)
• Pulmonary embolism (off-label)

Dosage

Children: Refer to the BNF for Children for appropriate dosing information for paediatric patients.

Adults: Refer to specific guidelines and protocols for dosing in acute myocardial infarction. Dosing typically involves a single intravenous bolus based on body weight.

Mechanism of action

Tenecteplase acts by specifically binding to fibrin within a thrombus, catalyzing the conversion of plasminogen to plasmin. This process leads to the degradation of fibrin clots, ultimately resulting in thrombolysis. The modification of tenecteplase enhances its fibrin specificity and prolongs its half-life compared to native tPA, which allows for more effective clot resolution with a single administration.

Pharmacodynamics

The pharmacodynamic effects of tenecteplase include rapid fibrinolysis leading to the resolution of occlusive thrombi in coronary arteries. The onset of action occurs within minutes of administration, with peak effects observed when blood flow is restored. Tenecteplase is associated with a lower risk of bleeding complications compared to older thrombolytic agents, due to its improved fibrin specificity.

Pharmacokinetics

Tenecteplase exhibits a half-life of approximately 20 to 24 minutes, allowing for rapid clearance from the bloodstream following administration. It is predominantly eliminated via the liver, with a small portion excreted renally. The pharmacokinetic profile of tenecteplase supports its use in acute settings where rapid thrombolysis is required.

Contra-indications

• Active bleeding or bleeding disorders
• Recent surgery or trauma
• Severe hypertension
• History of intracranial hemorrhage
• Known hypersensitivity to tnktpa or any component of the formulation

Adverse effects

• Hemorrhage
• Hypotension
• Allergic reactions
• Nausea
• Vomiting
• Anaphylaxis

Interactions

• Anticoagulants (e.g., warfarin, heparin) may increase the risk of bleeding
• Antiplatelet agents (e.g., aspirin, clopidogrel) may also enhance bleeding risk
• Other thrombolytics may increase the risk of serious bleeding

Precautions

• Monitor for signs of bleeding during and after therapy
• Use caution in patients with renal or hepatic impairment
• Careful consideration in patients with a history of stroke or transient ischemic attack
• Evaluate the risk of bleeding versus the benefit of thrombolysis in each patient

Pregnancy

Tnktpa should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus, as there are limited data on its safety.

Breast-feeding

It is not known whether tnktpa is excreted in human milk. Caution should be exercised when administering to breastfeeding women.

Storage

Store at 2 to 8 degrees Celsius. Do not freeze. Protect from light.

Formulations

• Injection: 10 mg vial for reconstitution