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a tissue plasminogen activator produced by recombinant DNA technology; used in therapy for acute myocardial infarction, acute ischemic stroke, and acute pulmonary embolism, administered intravenously.

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)

3-hour infusion-

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.

Off-label uses

• 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

• children.


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.

Adverse reactions

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

Patient monitoring

• 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.

Patient teaching

• As appropriate, explain therapy and monitoring to patient and family.


A tissue plasminogen activator made by recombinant DNA technology, used as a thrombolytic.


Activase® Cardiology A thrombolytic used to manage and prevent pulmonary embolism. See Pulmonary embolism, Thrombolytic therapy.


A TISSUE PLASMINOGEN ACTIVATOR drug made by recombinant DNA technology. In mid-2003 the drug was approved for the treatment of ischaemic stroke by experts. It must be given within three hours and cerebral haemorrhage must be excluded. A brand name is Actilyse.
References in periodicals archive ?
One-year follow-up of the ASSENT-2 trial: a double-blind, randomized comparison of single-bolus tenecteplase and front-loaded alteplase in 16,949 patients with ST-elevation acute myocardial infarction.
reported a successful treatment with alteplase in 2 of 12 patients with PE and concomitant paradoxical embolism.
Intravenous alteplase for stroke: beyond the guidelines and in particular clinical situations.
A recent review on the use of idarucizumab reversal of dabigatran concluded that giving alteplase after reversing dabigatran in acute ischemic stroke might be feasible for patients with less severe stroke in an early time window.
The researchers found that the primary outcome occurred in 22 and 10 percent of those treated with tenecteplase and alteplase, respectively (incidence ratio, 2.2; 95 percent confidence interval, 1.1 to 4.4; P = 0.002 for non-inferiority; P = 0.03 for superiority).
Early management of stroke involves first determining whether someone is a candidate for reperfusion therapy with alteplase or thrombectomy and then, if not, admitting them to a monitored setting to screen for atrial fibrillation and evaluation for carotid stenosis.
(20.) Poppe AY, Majumdar SR, Jeerakathil T, Ghali W, Buchan AM, Hill MD; Canadian Alteplase for Stroke Effectiveness Study Investigators.
Luijckx, "Intravenous alteplase for stroke: Beyond the guidelines and in particular clinical situations," Stroke, vol.
Moss et al., "Hemi-orolingual angioedema and ACE inhibition after alteplase treatment of stroke," Neurology, vol.
Viana-Baptista, "Orolingual angioedema associated with alteplase treatment of acute stroke: a reappraisal," Journal of Stroke and Cerebrovascular Disease, vol.
"The doctors came in and gave us the devastating news - they said that after looking at the brain activity they could not give her the clot-busting medication, Alteplase, which would improve the chances of a full recovery."
Previous award winners have established important standards of care in neurology, including Activase (alteplase) and induced hypothermia treatment.