Generic Name and Formulations:
Alteplase 50mg, 100mg; per vial; lyophilized pwd for IV infusion after reconstitution and dilution.

Company:
Genentech, Inc.
Indications for ACTIVASE:
Management of acute myocardial infarction (AMI) to improve ventricular function and reduce the incidence of CHF and mortality. Management of acute ischemic stroke to improve neurologic recovery and reduce disability. Management of acute massive pulmonary embolism (PE).

Adult:
AMI: Max total dose: 100mg. Accelerated infusion: ≤67kg: 15mg IV bolus followed by 0.75mg/kg (max 50mg) infused over 30min, then 0.5mg/kg (max 35mg) over 60min. >67kg: 15mg IV bolus followed by 50mg infused over 30min, then 35mg infused over 60min; 3-hour infusion: >65kg: 60mg infused in the first hour (of which 6–10mg is given as bolus), then 20mg/hr for 2hrs; smaller patients (<65kg): 1.25mg/kg over 3hrs (as described above). Stroke: start treatment within 3hrs of symptom onset. 0.9mg/kg (max 90mg total dose) infused over 60min with 10% of the total dose given as an initial IV bolus over 1 minute. PE: 100mg infused over 2hrs. Heparin may be used concomitantly in MI or after infusion in PE.

Children:
Not recommended.

Contraindications:
AMI and PE: History of cerebrovascular accident. Intracranial or intraspinal surgery or trauma. Stroke: Intracranial or subarachnoid hemorrhage. Intracranial or intraspinal surgery, serious head trauma or previous stroke. Seizure at onset of stroke. All: Active internal bleeding. Intracranial neoplasm, arteriovenous malformation or aneurysm. Severe uncontrolled hypertension. Bleeding diathesis.

Warnings/Precautions:
Stroke: treatment >3hrs after symptom onset not recommended. Minor neurological deficit or rapidly improving symptoms: not recommended. Avoid IM inj and nonessential handling of patient during treatment. Increased bleeding risk at puncture sites (eg, arterial, internal jugular, subclavian venous); avoid. Discontinue if serious bleeding occurs or if INR >1.7 or prothrombin time >15 seconds, or an elevated activated partial thromboplastin time identified. Increased risk of complications with recent major surgery, GI or GU bleeding, recent trauma, cerebrovascular disease, hypertension (systolic BP >175mm Hg and/or diastolic BP >110mm Hg), left heart thrombus, acute pericarditis, endocarditis, hemostatic defects, hepatic dysfunction, pregnancy, hemorrhagic ophthalmic conditions, septic thrombophlebitis, major early infarct signs on CT scan, elderly, severe neurologic deficit. Avoid extravasation. Pregnancy (Cat.C). Nursing mothers.

Interactions:
Increased risk of bleeding with heparin, warfarin, vitamin K antagonists, drugs that alter platelet function (eg, aspirin, dipyridamole, abciximab). Angioedema risk with ACEI (monitor). May interfere with coagulation tests.

Pharmacological Class:
Tissue plasminogen activator (tPA).

Adverse Reactions:
Bleeding, hypersensitivity reactions. AMI: arrhythmias, AV block, cardiogenic shock, heart failure, recurrent ischemia, myocardial rupture, pericardial effusion, pericarditis, cardiac tamponade, pulmonary edema, nausea, vomiting, hypotension, fever. PE: pulmonary reembolization or edema, pleural effusion, thromboembolism. Stroke: cerebral edema or herniation, seizure, new ischemic stroke. Also: cholesterol embolism.

How Supplied:
Vials—1 (w. diluent)