Tenecteplase

Drug Information: Tenecteplase

Detailed information regarding Tenecteplase, a genetically engineered thrombolytic agent belonging to the class of tissue plasminogen activators (t-PA). It is primarily used in the treatment of acute myocardial infarction (AMI), also known as a heart attack, to dissolve blood clots and restore blood flow to the heart muscle. Tenecteplase is administered as a single intravenous bolus, making it a convenient and rapid option in emergency situations. Its modified structure compared to alteplase allows for slower plasma clearance and greater fibrin specificity, potentially leading to improved outcomes and reduced bleeding risk. It is critical to administer Tenecteplase as early as possible following the onset of symptoms to maximize its effectiveness in reducing myocardial damage and improving patient prognosis.

Category

Neurological Drugs – Drugs for stroke management

Mechanism of Action

Tenecteplase is a thrombolytic agent, meaning it dissolves blood clots. It achieves this by selectively binding to fibrin, a protein that forms the structural framework of blood clots. Once bound to fibrin, tenecteplase activates plasminogen, a naturally occurring proenzyme in the blood. This activation converts plasminogen into plasmin, an enzyme responsible for breaking down fibrin. Plasmin hydrolyzes the peptide bonds of fibrin, leading to the breakdown and dissolution of the clot. Tenecteplase is a recombinant tissue plasminogen activator (rt-PA), but it is modified to have a longer half-life and greater fibrin specificity compared to alteplase, another rt-PA. The increased fibrin specificity means tenecteplase is more likely to target the clot directly and less likely to activate plasminogen systemically, potentially reducing the risk of bleeding complications. The slower clearance from the body allows for single bolus administration, which simplifies the administration process in emergency situations.

Clinical Uses

Tenecteplase’s primary clinical use is in the management of acute myocardial infarction (AMI), specifically for thrombolysis in patients experiencing ST-elevation myocardial infarction (STEMI). STEMI is a type of heart attack characterized by a complete blockage of a coronary artery, leading to ST-segment elevation on an electrocardiogram (ECG). By dissolving the clot obstructing the coronary artery, tenecteplase helps restore blood flow to the ischemic heart muscle, limiting myocardial damage and potentially improving patient outcomes, including reduced mortality and heart failure risk. Its ease of administration as a single bolus injection makes it particularly useful in pre-hospital settings and emergency departments, enabling faster treatment times. While primarily used for STEMI, ongoing research investigates its potential applications in other thromboembolic conditions.

Dosage

Adults: Tenecteplase is administered as a single intravenous (IV) bolus injection. The dose is weight-based:

• <60 kg: 30 mg
• 60 to <70 kg: 35 mg
• 70 to <80 kg: 40 mg
• 80 to <90 kg: 45 mg
• ≥90 kg: 50 mg

It is crucial to administer the appropriate dose based on the patient’s current weight. Heparin and aspirin are typically administered concomitantly with tenecteplase.
Pediatric: Tenecteplase is not typically used in pediatric populations, and specific dosing guidelines are not established for children.

Indications

Tenecteplase is indicated for:

• Acute myocardial infarction (AMI)
• ST-elevation myocardial infarction (STEMI)

Specifically, it is used for thrombolysis (dissolving blood clots) in patients presenting with STEMI to improve blood flow to the heart and reduce myocardial damage.

Contraindications

Contraindications for tenecteplase include:

• Active internal bleeding
• History of intracranial hemorrhage
• Recent (within 3 months) ischemic stroke
• Significant closed head trauma or facial trauma within 3 months
• Known bleeding diathesis (tendency to bleed)
• Intracranial neoplasm, arteriovenous malformation, or aneurysm
• Severe uncontrolled hypertension
• Known hypersensitivity to tenecteplase or any component of the formulation

Careful consideration of risks and benefits is essential before administering tenecteplase.

FAQ

Q1: What is Tenecteplase used for?
A1: Tenecteplase is primarily used to dissolve blood clots in patients experiencing a heart attack (acute myocardial infarction or AMI), specifically ST-elevation myocardial infarction (STEMI).

Q2: How is Tenecteplase administered?
A2: Tenecteplase is administered as a single intravenous (IV) bolus injection. The dosage is based on the patient’s weight.

Q3: What are the common side effects of Tenecteplase?
A3: The most common side effect is bleeding. This can range from minor bruising to more serious internal bleeding. Other potential side effects include allergic reactions and, rarely, stroke.

Q4: What should I tell my doctor before receiving Tenecteplase?
A4: Inform your doctor about any bleeding disorders, recent surgeries or trauma, history of stroke or head injury, uncontrolled high blood pressure, or any allergies.

Q5: How quickly does Tenecteplase need to be administered after a heart attack?
A5: Tenecteplase should be administered as soon as possible after the onset of heart attack symptoms. The sooner the treatment is given, the greater the chance of minimizing heart damage.

Q6: Can Tenecteplase be given to everyone having a heart attack?
A6: No, Tenecteplase is contraindicated in certain situations, such as active bleeding, recent stroke, or uncontrolled high blood pressure. Your doctor will assess your condition to determine if it is safe and appropriate for you.

Q7: Is Tenecteplase better than other thrombolytics?
A7: Tenecteplase offers the advantage of single bolus administration and potentially higher fibrin specificity compared to some other thrombolytics like alteplase. This can simplify administration and potentially reduce bleeding risk, although specific benefits and risks need to be considered for each patient.

Q8: What happens after Tenecteplase is administered?
A8: After Tenecteplase administration, patients are closely monitored for bleeding and other potential complications. Further treatment, such as angioplasty and stenting, may be performed to further improve blood flow to the heart.