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Alteplase, recombinant
Alteplase, recombinant (Activase)
Alteplase, recombinant
(AL-teh-playz)
Pregnancy Category: C Activase Activase rt-PA; (Rx)

Classification: Thrombolytic agent (tissue plasminogen activator)

Action/Kinetics: Alteplase, a tissue plasminogen activator, is synthesized by a human melanoma cell line using recombinant DNA technology. This enzyme binds to fibrin in a thrombus, causing a conversion of plasminogen to plasmin. This conversion results in local fibrinolysis and a decrease in circulating fibrinogen. Within 10 min following termination of an infusion, 80% of the alteplase has been cleared from the plasma by the liver. The enzyme activity of alteplase is 580,000 IU/mg. t1/2, initial: 4 min; final: 35 min (elimination phase).

Uses: Improvment of ventricular function following acute MI, including reducing the incidence of CHF and decreasing mortality. Treat acute ischemic stroke, after intracranial hemorrhage has been excluded by CT scan or other diagnostic imaging. Acute pulmonary thromboembolism. Investigational: Unstable angina pectoris.

Contraindications: Acute MI or pulmonary embolism: Active internal bleeding, history of CVA, within 2 months of intracranial or intraspinal surgery or trauma, intracranial neoplasm, AV malformation or aneurysm, bleeding diathesis, severe uncontrolled hypertension.
Acute ischemic stroke: Symptoms of intracranial hemorrhage on pretreatment evaluation, suspected subarachnoid hemorrhage, recent intracranial surgery or serious head trauma, recent previous stroke, history of intracranial hemorrhage, uncontrolled hypertension (above 185 mm Hg systolic or above 110 Hg diastolic) at time of treatment, active internal bleeding, seizure at onset of stroke, intracranial neoplasm, AV malformation or aneurysm, bleeding diathesis.

Special Concerns: Use with caution in the presence of recent GI or GU bleeding (within 10 days), subacute bacterial endocarditis, acute pericarditis, significant liver dysfunction, concomitant use of oral anticoagulants, diabetic hemorrhagic retinopathy, septic thrombophlebitis or occluded arteriovenous cannula (at infected site), lactation, mitral stenosis with atrial fibrillation. Since fibrin will be lysed during therapy, careful attention should be given to potential bleeding sites such as sites of catheter insertion and needle puncture sites. Use with caution within 10 days of major surgery (e.g., obstetrics, coronary artery bypass) and in clients over 75 years of age. Safety and efficacy have not been established in children. NOTE: Doses greater than 150 mg have been associated with an increase in intracranial bleeding.

Side Effects: Bleeding tendencies: Internal bleeding (including the GI and GU tracts and intracranial or retroperitoneal site). Superficial bleeding (e.g., gums, sites of recent surgery, venous cutdowns, arterial punctures). Ecchymosis, epistaxis. CV: Bradycardia, hypotension, cardiogenic shock, arrhythmias, heart failure, cardiac arrest, cardiac tamponade, myocardial rupture recurrent ischemia, reinfarction, mitral regurgitation, pericardial effusion, pericarditis, venous thrombosis and embolism, electromechanical dissociation. Allergic: Rash, laryngeal edema, anaphylaxis. GI: N&V. Miscellaneous: Fever, urticaria, pulmonary edema, cerebral edema.
Due to accelerated infusion: Strokes, hemorrhagic stroke nonfatal stroke. Incidence increases with age.

Overdose Mangement: Symptoms: Bleeding disorders. Treatment: Discontinue therapy immediately as well as any concomitant heparin therapy.

Drug Interactions: Abciximab / Risk of bleeding Acetylsalicylic acid / Risk of bleeding Dipyridamole / Risk of bleeding Heparin / Risk of bleeding, especially at arterial puncture sites

How Supplied: Powder for injection: 50 mg, 100 mg

Dosage
•IV Infusion Only AMI, accelerated infusion.
Weight >67 kg: 100 mg as a 15-mg IV bolus, followed by 50 mg infused over the next 30 min and then 35 mg infused over the next 60 min. Weight <67 kg: 15 mg IV bolus, followed by 0.75 mg/kg infused over the next 30 min (not to exceed 50 mg) and then 0.50 mg/kg infused over the next 60 min (not to exceed 35 mg). The safety and efficacy of this regimen have only been evaluated using heparin and aspirin concomitantly.AMI, 3-hr infusion.
100 mg total dose subdivided as follows: 60 mg (34.8 million IU) the first hour with 6-10 mg given in a bolus over the first 1-2 min and the remaining 50-54 mg given over the hour; 20 mg (11.6 million IU) over the second hour and 20 mg (11.6 million IU) given over the third hour. Clients less than 65 kg: 1.25 mg/kg given over 3 hr, with 60% given the first hour with 6%-10% given by direct IV injection within the first 1-2 min; 20% is given the second hour and 20% during the third hour. Doses of 150 mg have caused an increase in intracranial bleeding.
Pulmonary embolism.
100 mg over 2 hr; heparin therapy should be instituted near the end of or right after the alteplase infusion when the partial thromboplastin or thrombin time returns to twice that of normal or less.
Acute ischemic stroke.
0.9 mg/kg (maximum of 90 mg) infused over 60 min with 10% of the total dose given as an initial IV bolus over 1 min. Doses greater than 0.9 mg/kg may cause an increased incidence of intracranial hemorrhage. Use with aspirin and heparin during the first 24 hr after onset of symptoms has not been investigated.