ACTIVASE

Alteplase in acute myocardial infarction (AMI) patients is rapidly cleared from the plasma with an initial half-life of less than 5 minutes. There is no difference in the dominant initial plasma half-life between the 3-hour and accelerated regimens for AMI. The plasma clearance of alteplase is 380-570 mL/min, primarily mediated by the liver. The initial volume of distribution approximates plasma volume.

14.1 Acute Ischemic Stroke (AIS) Two placebo-controlled, double-blind trials (Studies 1 and 2) were conducted in patients with AIS. Both studies enrolled patients with measurable neurological deficit who could complete screening and begin study treatment within 3 hours from symptom onset. A cranial computerized tomography (CT) scan was performed prior to treatment to rule out the presence of intracranial hemorrhage. Blood pressure was actively controlled (185/110 mm Hg or lower) for 24 hours. Patients were randomized (1:1) to receive either 0.9 mg/kg Activase (maximum of 90 mg) or placebo. Act...

The following adverse reactions are discussed in greater detail in the other sections of the label: Bleeding [see Contraindications (4) , Warnings and Precautions (5.1) ] Hypersensitivity [see Warnings and Precautions (5.2) ] Thromboembolism [see Warnings and Precautions (5.3) ] Cholesterol Embolization [see Warnings and Precautions (5.4) ] The most frequently occurring adverse reaction ( > 5%) is bleeding. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Genentech at 1-888-835-2555 or FDA a...

General Active internal bleeding. ( 4.1 , 4.2 ) Recent intracranial or intraspinal surgery or serious head trauma. ( 4.1 , 4.2 ) Intracranial conditions that may increase the risk of bleeding. ( 4.1 , 4.2 ) Bleeding diathesis. ( 4.1 , 4.2 ) Current severe uncontrolled hypertension. ( 4.1 , 4.2 ) Acute Ischemic Stroke Current intracranial hemorrhage. ( 4.1 ) Subarachnoid hemorrhage. ( 4.1 ) Acute M...

Increases the risk of bleeding. Avoid intramuscular injections. Monitor for bleeding. If serious bleeding occurs, discontinue Activase. ( 5.1 ) Monitor patients during and for several hours after infusion for hypersensitivity. If signs of hypersensitivity develop, discontinue Activase. ( 5.2 ) Consider the risk of reembolization from the lysis of underlying deep venous thrombi in patients with pulmonary embolism. ( 5.3 ) Cholesterol embolism has been reported rarely in patients treated with thro...

7 DRUG INTERACTIONS The interaction of Activase with other cardioactive or cerebroactive drugs has not been studied. Anticoagulants and antiplatelet drugs increase the risk of bleeding if administered prior to, during, or after Activase therapy. In the post-marketing setting, there have been reports of angioedema in patients (primarily patients with AIS) receiving concomitant angiotensin-convertin...