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. t 1/2, 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.
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.
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.
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.
Bradycardia, hypotension, cardiogenic shock, arrhythmias,
cardiac arrest, cardiac tamponade, myocardial rupture recurrent ischemia,
reinfarction, mitral regurgitation, pericardial effusion, pericarditis, venous thrombosis
and embolism, electromechanical dissociation.
urticaria, pulmonary edema, cerebral edema.
Overdose Mangement: Symptoms: Bleeding disorders. Treatment: Discontinue therapy immediately as well as any concomitant heparin therapy.
How Supplied: Powder for injection: 50 mg, 100 mg