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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.


/al·te·plase/ (al´tĕ-plās) a tissue plasminogen activator produced by recombinant DNA technology; used in fibrinolytic therapy for acute myocardial infarction and as a thrombolytic in the treatment of acute ischemic stroke and pulmonary embolism.


a tissue plasminogen activator.
indications This drug is used for lysis of obstructing thrombi associated with acute MI and for other ischemic conditions requiring thrombolysis.
contraindications Known hypersensitivity to this drug, active internal bleeding, recent cerebrovascular accident, severe uncontrolled hypertension, intracranial trauma or surgery, intraspinal trauma or surgery, aneurysm, and brain tumor prohibit the use of this drug.
adverse effects Adverse effects of this drug include urticaria and rash. Surface bleeding is a common side effect. Life-threatening side effects include sinus bradycardia, ventricular tachycardia, accelerated idioventricular rhythm, bradycardia, GI bleeding, genitourinary bleeding, intracranial bleeding, retroperitoneal bleeding, and anaphylaxis.


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 ?
Alteplase (rt-PA) is a recombinant tissue-type plasminogen activator, by binding to fibrin, it could activate and transfer the plasminogen into plasmin, thus dissolving thrombus.
In celebration of Brain Attack Awareness Week, the DOH on Tuesday launched the medical assistance program that will make stroke medication alteplase available to the public for free, in 26 selected government hospitals nationwide.
In consideration of the restricted time window available for alteplase treatment as well as the potential for improved patient outcomes with earlier alteplase administration, it would be valuable to determine if the required blood pressure targets could be attained more rapidly with the use of specific antihypertensive agents.
The independent expert panel, chaired by Prof Sir Ian Weller, said: "The evidence shows that for every 100 patients treated with alteplase, whilst there is an early risk of a fatal bleed in two patients, after three to six months, around 10 more in every 100 are disability-free when treated within three hours.
Most major stroke guidelines support use of alteplase up to four-and-a-half hours after stroke onset, but we believe that this guidance is based on uncertain evidence," explained Dr Alper.
Alteplase is the most common thrombolytic medication available in the market as it replaced urokinase as the drug of choice for clearing occluded central venous catheters (Adams & Holland, 2011).
Thrombolysis with urokinase, alteplase, streptokinase and reteplase has been investigated previously.
Effects of alteplase beyond 3 h after stroke in the Echoplanar Imaging Thrombolytic Evaluation Trial (EPITHET): A placebo-controlled randomised trial.
On her admission to the city's Queen Elizabeth II Hospital, she was given the drug Alteplase, which contains a protein which can break down blood clots in stroke victims.
Without a crucial early brain scan and an injection of clot-busting Alteplase she might not have been here today.
The proportion of patients with SICH, mortality, independence, and neurological improvement were calculated and compared with the corresponding proportions in the alteplase arm of the NINDS rt-PA and ECASS III trials, and with observational studies in developed and other developing countries.
Manawadu and her colleagues analyzed patients in the hospital's stroke registry who received alteplase (Activase) between January 2009 and December 2010.