Activase Generic Name & Formulations
Alteplase 50mg, 100mg; per vial; lyophilized pwd for IV infusion after reconstitution and dilution.
Tissue plasminogen activator (tPA).
Vials—1 (w. diluent)
Mechanism of Action
Alteplase is a serine protease responsible for fibrin-enhanced conversion of plasminogen to plasmin. It produces limited conversion of plasminogen in the absence of fibrin. When introduced into the systemic circulation at pharmacologic concentration, alteplase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin. This initiates local fibrinolysis with limited systemic proteolysis.
Treatment of acute myocardial infarction (AMI) to reduce mortality and incidence of heart failure. Treatment of acute ischemic stroke. Treatment of acute massive pulmonary embolism (PE) for lysis.
Limitations of Use
The risk of stroke may outweigh the benefit of thrombolytic therapy in patients whose AMI puts them at low risk for death or heart failure.
Activase Dosage and Administration
AMI: start as soon as possible after symptom onset. Max total dose: 100mg. Accelerated infusion: ≤67kg: 15mg IV bolus followed by 0.75mg/kg (max 50mg) infused over 30mins, then 0.5mg/kg (max 35mg) over 60mins. >67kg: 15mg IV bolus followed by 50mg infused over 30mins, then 35mg infused over 60mins. 3-hour infusion: (<65kg): 1.25mg/kg over 3hrs (of which 0.075mg/kg as bolus, 0.675mg/kg for the rest of the first hour, then 0.25mg/kg/hr for 2hrs); (≥65kg): 60mg infused in the first hour (of which 6–10mg is given as IV bolus), then 20mg/hr for 2hrs. Stroke: start treatment within 3hrs of symptom onset. 0.9mg/kg (max 90mg total dose) infused over 60mins with 10% of the total dose given as an initial IV bolus over 1 minute. Monitor frequently and control blood pressure. PE: 100mg infused over 2hrs. Initiate parenteral anticoagulation near the end of or immediately after Activase infusion when PTT or thrombin time returns to twice normal or less.
AMI and PE: History of recent stroke. Stroke: Intracranial or subarachnoid hemorrhage. All: Active internal bleeding. Intracranial or intraspinal surgery or serious head trauma within 3 months. Intracranial neoplasm, arteriovenous malformation or aneurysm. Bleeding diathesis. Current severe uncontrolled hypertension.
Activase Boxed Warnings
Stroke: treatment >3hrs after symptom onset not recommended. Avoid IM inj and trauma to the patient while on therapy. Increased bleeding risk at puncture sites (eg, arterial, internal jugular, subclavian venous); avoid. Discontinue if serious bleeding occurs, if INR >1.7, or activated partial thromboplastin time is elevated. Increased risk of complications with recent major surgery, intracranial hemorrhage, GI or GU bleeding, or trauma, cerebrovascular disease, hypertension (systolic BP >175mm Hg and/or diastolic BP >110mm Hg), acute pericarditis, subacute bacterial endocarditis, hemostatic defects, hepatic dysfunction, pregnancy, hemorrhagic ophthalmic conditions, septic thrombophlebitis or occluded AV cannula, elderly. Increased risk of thromboembolism in left heart thrombus (eg, mitral stenosis, A-fib). PE: consider possible risk of reembolization due to lysis of underlying deep venous thrombi. Avoid extravasation. Pregnancy. Nursing mothers.
Half-life: <5 minutes (initial), 72 minutes (terminal).
Increased risk of bleeding with anticoagulants, antiplatelets. Angioedema risk with ACEI; monitor; discontinue if occurs. May interfere with coagulation tests.
Activase Adverse Reactions
Bleeding (may be fatal), hypersensitivity reactions (eg, anaphylactoid, angioedema, urticaria, laryngeal edema, rash, shock; monitor and discontinue if occurs); rare: cholesterol embolism.
Activase Clinical Trials
Activase Patient Counseling