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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 trademark used for a synthetic tissue plasminogen activator.


a trademark for a commercial form of tissue plasminogen activator (alteplase recombinant).


A proprietary thrombolytic, which is used to manage acute ischaemic strokes. Current guidelines support Activase use in eligible stroke patients within 3 hours of symptom onset. 
Mechanism Activation of fibrinolysis by stimulating conversion of plasminogen to plasmin.


A proprietary thrombolytic, which may ↑ survival in TIA victims by 33% Mechanism Activation of the body's fibrinolytic system by stimulating conversion of plasmin from plasminogen, and several other clotting factors. See TIA, tPA.
References in periodicals archive ?
The scientists have managed to crystallize the activase protein from the creosote bush, which is a shrub that's abundant in the Arizona desert.
The team discovered the existence of rubisco activase in 1985 and proved that it activates rubisco.
We conducted a survey of cardiologists and found that 98 percent of them said if they had a heart attack, they would want Activase.
The researchers are currently putting the gene for rubisco activase from a desert shrub into cotton.
A plant could end up with more inactive than active rubisco if rubisco activase were to somehow become impaired.
5: Market for Activase (Alteplase), 2012-2019 191 Figure 8.
11 Activase Sales Forecast ($m), 2010-2022Figure 5.
REACH Call, the leading provider of 100 percent Web-based solutions for the remote treatment of medical conditions such as stroke, announces an educational collaboration with Genentech, the manufacturer of Activase (Alteplase), a tissue plasminogen activator (tPA) approved for treating acute ischemic stroke in adults.
Activase, a recombinant tissue plasminogen activator (t-PA) developed by Genentech, is approved for the management of acute ischemic stroke in adults.
From this data, a cost analysis was conducted, comparing the cost of heparin, connectors, syringes, activase, sodium citrate, and equipment for both CVC locks and Tego connectors to the cost of recombinant tissue plasminogen activator (rt-PA).
Jones held various key positions at biopharma companies, including Medimmune, where he was responsible for the launch of both Respigam and Synagis and Genentech, where he was responsible for the launch of Protropin, Activase and Pulmozyme.
Gorman played a key role in the development of a number of marketed products including Kogenate, Activase, Herceptin, Xolair, and Raptiva.