Za Pharmacy
Drugs, Supplies and Delivery
Tenecteplase
Tenecteplase is a thrombolytic (clot-busting) medication used to dissolve blood clots in acute myocardial infarction (heart attack) and ischemic stroke. Marketed under the brand name Metalyse (Europe) and TNKase (US), it is a modified tissue plasminogen activator (tPA) with enhanced fibrin specificity and a longer half-life, allowing for single-bolus administration. This article details its mechanism of action, uses, dosage, side effects, precautions, drug interactions, and generic names, referencing the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.
Tenecteplase is a recombinant tissue plasminogen activator (tPA) engineered for improved fibrin specificity and resistance to plasminogen activator inhibitor-1 (PAI-1). It binds to fibrin in blood clots and converts plasminogen to plasmin, an enzyme that degrades fibrin, dissolving the clot. Unlike older thrombolytics, tenecteplase’s modifications reduce systemic plasmin activation, lowering bleeding risks (Lippincott Textbook of Pharmacology).
- Acute Myocardial Infarction (STEMI):
- Restores blood flow in ST-segment elevation myocardial infarction (STEMI) when percutaneous coronary intervention (PCI) is unavailable or delayed (BNF).
- Acute Ischemic Stroke:
- Administered within 4.5 hours of symptom onset in eligible patients (Lange Basic & Clinical Pharmacology).
- STEMI:
- Single IV bolus dose based on weight:
- <60 kg: 30 mg
- 60–69 kg: 35 mg
- 70–79 kg: 40 mg
- 80–89 kg: 45 mg
- ≥90 kg: 50 mg
- Administered over 5–10 seconds (BNF).
- Single IV bolus dose based on weight:
- Ischemic Stroke:
- 0.25 mg/kg (max 25 mg) as a single IV bolus.
Renal/Hepatic Impairment: No dose adjustment required, but use cautiously in severe hepatic dysfunction.
- Common:
- Bleeding (e.g., gingival, gastrointestinal, or urinary tract).
- Hypotension, nausea, or vomiting.
- Serious:
- Intracranial hemorrhage (1–2% risk in stroke patients).
- Severe allergic reactions (e.g., anaphylaxis, angioedema).
- Reperfusion arrhythmias post-STEMI (Lippincott Textbook of Pharmacology).
- Absolute Contraindications:
- Active internal bleeding or hemorrhagic stroke.
- Recent major surgery/trauma (within 14 days).
- Intracranial neoplasm or aneurysm.
- Relative Contraindications:
- Uncontrolled hypertension (>180/110 mmHg).
- Pregnancy or lactation (use only if benefits outweigh risks).
- Monitoring:
- Vital signs, neurologic status, and signs of bleeding (e.g., hematuria, melena).
- Anticoagulants (e.g., heparin, warfarin): Increased bleeding risk.
- Antiplatelets (e.g., aspirin, clopidogrel): Avoid concurrent use.
- GP IIb/IIIa Inhibitors (e.g., abciximab): Contraindicated due to heightened bleeding risk.
- Generic Name: Tenecteplase.
- Brand Names: Metalyse (Europe), TNKase (US).
