Section 13 · Monograph
Alteplase
Reviewed Nov 2026FDA label
ActivaseThrombolytic (tPA)
- Forms
- IV: 50, 100mg vials
- Dose
- Acute ischemic stroke: 0.9mg/kg (max 90mg); 10% as IV bolus over 1 min, remainder over 60 min
- MOA
- Converts plasminogen to plasmin, lysing fibrin clot
Indications
- Acute ischemic stroke (label window; guidelines extend eligible treatment to 4.5 hours)FDA-labeled
- Acute myocardial infarction to reduce mortalityFDA-labeled
- Acute massive pulmonary embolismFDA-labeled
Mechanism of Action
- Recombinant tissue plasminogen activator; binds fibrin and converts plasminogen to plasmin, lysing the clot
Full Dosing
Adult / usual
- Acute ischemic stroke: 0.9mg/kg (max 90mg); 10% as IV bolus over 1 minute, remainder infused over 60 minutes
- Obtain CT to exclude hemorrhage first; BP must be below 185/110 before and below 180/105 for 24 hours after treatment
- Avoid antithrombotics for 24 hours after thrombolysis unless otherwise indicated
Contraindications
- Active internal bleeding
- History of intracranial hemorrhage; recent (within 3 months) intracranial/spinal surgery or serious head trauma; intracranial neoplasm, AVM or aneurysm
- Severe uncontrolled hypertension
- Bleeding diathesis; for stroke also platelets under 100,000, INR above 1.7, recent anticoagulant effect, glucose under 50 mg/dL
Drug Interactions
- Anticoagulants and antiplatelets increase bleeding risk
- Recent DOAC or heparin exposure may preclude use
Adverse Effects
- Symptomatic intracranial hemorrhage (about 6% in stroke trials)
- Systemic bleeding including GI/GU bleeding
- Orolingual angioedema, especially with ACE inhibitor use
- Reperfusion arrhythmias (MI)
Monitoring Parameters
- Neuro checks and BP every 15 min x2h, every 30 min x6h, then hourly to 24h
- Stop infusion and obtain urgent CT for severe headache, acute hypertension, nausea/vomiting or neurologic worsening
- Repeat imaging at 24 hours before starting antithrombotics
Pregnancy & Lactation
- Limited data; use only if benefit outweighs risk
- Unknown whether present in milk