tissue plasminogen activator
Also found in: Dictionary, Thesaurus, Legal, Financial, Acronyms, Encyclopedia, Wikipedia.
alteplase (tissue plasminogen activator, recombinant)
Actilyse (UK), Activase, Activase rt-PA (CA), Cathflo Activase
Pharmacologic class: Plasminogen activator
Therapeutic class: Thrombolytic
Pregnancy risk category C
Converts plasminogen to plasmin, which in turn breaks down fibrin and fibrinogen, thereby dissolving thrombus
Injection: 2-mg single-patient vials; 50-mg, 100-mg vials
⊘Indications and dosages
➣ Lysis of thrombi obstructing coronary arteries in acute myocardial infarction (MI)
Adults: 100 mg I.V. over 3 hours as follows: 60 mg over first hour (give 6 to 10 mg as bolus over first 1 to 2 minutes), then 20 mg I.V. over second hour, then 20 mg I.V. over third hour
Adults weighing less than 65 kg (143 lb): 1.25 mg/kg I.V. in divided doses over 3 hours, not to exceed 100 mg Accelerated infusion-
Adults weighing more than 67 kg (147 lb): Give total dosage of 100 mg as follows: 15 mg I.V. bolus over 1 to 2 minutes, then 50 mg I.V. over next 30 minutes, then 35 mg I.V. over next 60 minutes.
Adults weighing 67 kg (147 lb) or less: 15 mg I.V. bolus over 1 to 2 minutes, followed by 0.75 mg/kg I.V. over next 30 minutes (not to exceed 50 mg), followed by 0.5 mg/kg I.V. over next hour, not to exceed 35 mg
➣ Acute ischemic cerebrovascular accident (CVA)
Adults: 0.9 mg/kg I.V. over 1 hour, to a maximum dosage of 90 mg, with 10% of total dosage given as I.V. bolus within first minute
➣ Acute massive pulmonary embolism
Adults: 100 mg I.V. over 2 hours, followed by heparin
➣ Restoration of function of central venous access device
Adults weighing 30 kg (66 lb) or more:Cathflo Activase-2 mg/2-ml concentration instilled in dysfunctional catheter. If catheter function isn't restored in 120 minutes after first dose, may give second dose.
Adults weighing 10 kg (22 lb) to less than 30 kg:Cathflo Activase-Use 110% of catheter lumen volume not to exceed 2 mg/2-ml concentration instilled in dysfunctional catheter. If catheter function isn't restored in 120 minutes after first dose, may give second dose.
• Small-vessel occlusion by microthrombi
• Peripheral arterial thromboembolism
• Hypersensitivity to drug or its components (Cathflo Activase)
• Seizures, stroke, aneurysm, intracranial neoplasm, bleeding diathesis
Use cautiously in:
• hypersensitivity to anistreplase or streptokinase
• GI or genitourinary bleeding, ophthalmic hemorrhage, organ biopsy, severe hepatic or renal disease
• elderly patients
• pregnant or breastfeeding patients
☞ Be aware that intracranial hemorrhage must be ruled out before therapy begins.
☞ To treat acute ischemic CVA, give within 3 hours of initial signs or symptoms.
☞ If uncontrolled bleeding occurs, stop infusion and notify prescriber immediately.
• Give I.V. only, using controlled-infusion pump.
• Reconstitute with unpreserved sterile water for injection. May be further diluted with normal saline solution or D5W.
CNS: cerebral hemorrhage, cerebral edema, CVA (with accelerated infusion)
CV: hypotension, bradycardia, recurrent ischemia, pericardial effusion, pericarditis, mitral regurgitation, electromechanical dissociation, arrhythmias, cardiogenic shock, heart failure, cardiac arrest, cardiac tamponade, myocardial rupture, embolization, venous thrombosis
GI: nausea, vomiting, GI bleeding
GU: GU tract bleeding
Hematologic: spontaneous bleeding, bone marrow depression
Musculoskeletal: musculoskeletal pain
Respiratory: pulmonary edema
Skin: bruising, flushing
Other: fever, edema, phlebitis or bleeding at I.V. site, hypersensitivity reaction (including rash, anaphylactic reaction, laryngeal edema), sepsis
Drug-drug.Aspirin, drugs affecting platelet activity (such as abciximab, heparin, dipyridamole, oral anticoagulants, vitamin K antagonists): increased risk of bleeding
Drug-diagnostic tests.Blood urea nitrogen: elevated level
• Monitor vital signs, ECG, and neurologic status.
• Maintain strict bed rest.
• Watch for signs and symptoms of bleeding tendency and hemorrhage.
• Monitor patient on Cathflo Activase for GI bleeding, venous thrombosis, and sepsis.
• Evaluate results of clotting studies.
• As appropriate, explain therapy and monitoring to patient and family.
tis·sue plas·min·o·gen ac·ti·va·tor (TPA, tPA),[MIM*173370]
TPA is a single-chain glycoprotein with a molecular weight of about 70 kD. Released by endothelial cells at sites of vascular injury, it modulates thrombogenesis by converting fibrin-bound plasminogen to plasmin, cleaving the arginine-valine bond of plasminogen at the 560-561 position. As a result, fibrin strands in a clot are chemically degraded and platelet adhesion and aggregation are inhibited. TPA has little effect on plasminogen in the absence of fibrin, and its release does not significantly reduce systemic concentrations of fibrinogen. Alteplase, a synthetic TPA produced by recombinant DNA technology, improves outcomes when administered intravenously in acute myocardial infarction and in selected cases of stroke, pulmonary embolism, and peripheral ischemia due to thrombosis. It has a circulating half-life of only 4-6 minutes, but persists in clots up to 7 hours. see thrombolytic therapy