Generic
Tenecteplase
2 brands available in the market
At a glance
Tenecteplase is a fibrin-specific thrombolytic used for emergency treatment of acute myocardial infarction. It dissolves blood clots by converting plasminogen to plasmin.
Description
Tenecteplase is a recombinant tissue plasminogen activator (tPA) with three modifications to natural human tPA. It binds to the fibrin component of the thrombus and selectively converts thrombus-bound plasminogen to plasmin, which degrades the fibrin matrix. It has higher fibrin specificity and greater resistance to PAI-1 inactivation.
Indications
- Acute myocardial infarction (AMI)
Therapeutic class
Fibrinolytics (Thrombolytics)
Pharmacological class
Recombinant Tissue Plasminogen Activator
Pharmacology
Tenecteplase binds to fibrin-rich clots and converts plasminogen to plasmin. Plasmin degrades the fibrin matrix of the thrombus, dissolving the blood clot and restoring blood flow.
Mechanism of action
Dissolves blood clots by converting plasminogen to plasmin.
Dosage
Adult Dose (IV):
- Weight <60 kg: 30 mg
- 60-<70 kg: 35 mg
- 70-<80 kg: 40 mg
- 80-<90 kg: 45 mg
- ≥90 kg: 50 mg
- Single IV bolus dose over 5 seconds – as soon as possible after symptom onset
Administration
- IV administration only; single bolus over 5 seconds
- Reconstitute with 10 mL SWFI to make 5 mg/mL solution
- Administered by a healthcare professional in a hospital
Missed dose
Missed dose is not applicable (used in emergency).
Side effects
Most Common Side Effects:
- Bleeding (most frequent)
- Intracranial hemorrhage (0.9%)
- Hematoma (12.3% minor; 1.7% major)
- Gastrointestinal bleeding (1%)
- Epistaxis (1.5%)
- Nausea, vomiting, hypotension, fever
Precautions & warnings
- Do not use in active internal bleeding, recent cerebrovascular accident, intracranial/intraspinal surgery or trauma within 2 months
- Do not use in intracranial neoplasm, AV malformation or aneurysm, bleeding diathesis, severe uncontrolled hypertension
- Minimize arterial and venous punctures
- Discontinue heparin and antiplatelets in serious bleeding
Contraindications
- Active internal bleeding
- History of cerebrovascular accident
- Intracranial or intraspinal surgery or trauma within 2 months
- Intracranial neoplasm, AV malformation or aneurysm
- Bleeding diathesis
- Severe uncontrolled hypertension
Drug interactions
- Heparin, oral anticoagulants, antiplatelet drugs: Increased bleeding risk
Food interactions
It is not known whether alcohol is safe with Tenecteplase; consult your doctor.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies show harmful effects; use only if clearly needed; consult your doctor.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if excreted in human milk; caution required; hold breastfeeding until treatment is completed; consult your doctor.
Pediatric use
Safety and efficacy not established in pediatric patients
Geriatric use
ICH and stroke rates are higher in elderly; weigh benefit-risk
Renal / hepatic impairment
Renal Impairment: Limited information; consult your doctor.
Hepatic Impairment: Limited information; consult your doctor.
Overdose effects
Overdose increases bleeding risk; in severe prolonged bleeding, consider plasma and platelet replacement.
Storage conditions
Lyophilized: Store below 30°C or at 2-8°C; reconstituted solution should be used immediately; keep out of reach of children.
Chemical structure
Tenecteplase