Introduction
Tenecteplase is a tissue plasminogen activator (tPA) developed from modifications of natural human tPA complementary DNA (cDNA). It is a 527 amino acid with a substitution of threonine 103 with asparagine and substitution of asparagine 117 with glutamine within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.
Uses
Tenecteplase is a modified form of recombinant human tissue plasminogen activator used in the emergency treatment of myocardial infarction and pulmonary emboli.
For treatment of myocardial infarction and lysis of intracoronary emboli
Associated Conditions
Pharmacodynamics
Tenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and 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. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of Action
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.
Half Life
1.9 hours (mammalian reticulocytes, in vitro) >20 hours (yeast, in vivo) >10 hours (Escherichia coli, in vivo)
Clearance
- 99 - 119 mL/min [acute myocardial infarction patients]
Food Interactions
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
Dosage
- 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
