Contraindicated in:
- Active internal bleeding
- History of cerebrovascular accident (for MI and PE only)
- Recent (within 3 mo) intracranial or intraspinal injury or trauma
- Intracranial neoplasm, arteriovenous malformation, or aneurysm
- Known bleeding diathesis
- Severe uncontrolled hypertension (systolic BP >185 mmHg or diastolic BP >110 mmHg specifically for stroke indication)
- Evidence or suspicion of intracranial hemorrhage on pretreatment evaluation (for stroke indication only)
- Recent (within 3 mo) stroke (for stroke indication only)
- History of intracranial hemorrhage (for stroke indication only)
- Seizure at the onset of stroke (for stroke indication only)
- Current use of oral anticoagulants or an INR >1.7 or a prothrombin time >15 sec (for stroke indication only)
- Administration of heparin 48 hr before the onset of stroke with an elevated aPTT at presentation (for stroke indication only)
- Platelet count <100,000/mm3 (for stroke indication only)
- Hypersensitivity (for central venous access device occlusion indication only).
Use Cautiously in:
- Recent (within 10 days) major surgery, trauma, GI or GU bleeding
- Cerebrovascular disease
- Systolic BP
175 mmHg and/or diastolic BP 110 mmHg - High likelihood of left heart thrombus
- Hemostatic defects
- Severe hepatic impairment
- Hemorrhagic ophthalmic conditions
- Septic thrombophlebitis
- Previous puncture of a noncompressible vessel
- Subacute bacterial endocarditis or acute pericarditis
- Severe neurological deficit (NIHSS >22) at presentation (for stroke indication only)
- Major early infarct signs on CT scan (for stroke indication only)
- Known or suspected infection in catheter (for central venous access device occlusion indication only)
- Geri: >75 yr; ↑ risk of intracranial bleeding
- OB: Lactation: Pedi: Safety not established.
Exercise Extreme Caution in:
- Patients receiving concurrent anticoagulant therapy (↑ risk of intracranial bleeding).
CNS: INTRACRANIAL HEMORRHAGE.
EENT: epistaxis, gingival bleeding.
Resp: bronchospasm, hemoptysis.
CV: reperfusion arrhythmias, hypotension, RECURRENT ISCHEMIA/THROMBOEMBOLISM.
GI: GI BLEEDING, nausea, RETROPERITONEAL BLEEDING, vomiting.
GU: GU TRACT BLEEDING.
Derm: ecchymoses, flushing, urticaria.
Hemat: BLEEDING.
Local: hemorrhage at injection site, phlebitis at injection site.
MS: musculoskeletal pain.
Misc: ALLERGIC REACTIONS INCLUDING ANAPHYLAXIS, fever.
Myocardial Infarction (Accelerated or Front-Loaded Regimen)
- IV (Adults): 15 mg bolus, then 0.75 mg/kg (up to 50 mg) over 30 min, then 0.5 mg/kg (up to 35 mg) over next 60 min; usually accompanied by heparin therapy.
Myocardial Infarction (Standard Regimen)
- IV (Adults >65 kg): 60 mg over 1st hr (6–10 mg given as a bolus over first 1–2 min), 20 mg over the 2nd hr, and 20 mg over the 3rd hr for a total dose of 100 mg.
- IV (Adults <65 kg): 0.75 mg/kg over 1st hr (0.075–0.125 mg/kg given as a bolus over first 1–2 min), 0.25 mg/kg over the 2nd hr, and 0.25 mg/kg over the 3rd hr for a total dose of 1.25 mg/kg (not to exceed 100 mg total).
Acute Ischemic Stroke
- IV (Adults): 0.9 mg/kg (not to exceed 90 mg), given as an infusion over 1 hr, with 10% of the dose given as a bolus over the 1st min.
Pulmonary Embolism
- IV (Adults): 100 mg over 2 hr; follow with heparin.
Occluded Venous Access Devices
- IV (Adults and Children >30 kg): 2 mg/2 mL instilled into occluded catheter; if unsuccessful, may repeat once after 2 hr.
- IV (Adults and Children <30 kg): 110% of the lumen volume (not to exceed 2 mg in 2 mL) instilled into occluded catheter; if unsuccessful, may repeat once after 2 hr.
Activase, Cathflo Activase, tissue plasminogen activator, t-PA
Therapeutic Classification: thrombolytics
Pharmacologic Classification: plasminogen activators
Absorption: Complete after IV administration. Intracoronary administration or administration into occluded catheters or cannulae has a more localized effect.
Distribution: Unknown.
Metabolism/Excretion: Rapidly metabolized by the liver.
Half-life: 35 min.
