May 28, 2017
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How Supplied


Acute Ischemic Stroke

Activase is indicated for the treatment of acute ischemic stroke.

Exclude intracranial hemorrhage as the primary cause of stroke signs and symptoms prior to initiation of treatment [see CONTRAINDICATIONS]. Initiate treatment as soon as possible but within 3 hours after symptom onset.

Acute Myocardial Infarction

Activase is indicated for use in acute myocardial infarction (AMI) for the reduction of mortality and reduction of the incidence of heart failure.

Limitation Of Use

The risk of stroke may outweigh the benefit produced by thrombolytic therapy in patients whose AMI puts them at low risk for death or heart failure.

Pulmonary Embolism

Activase is indicated for the lysis of acute massive pulmonary embolism, defined as:

  • Acute pulmonary emboli obstructing blood flow to a lobe or multiple lung segments.
  • Acute pulmonary emboli accompanied by unstable hemodynamics, e.g., failure to maintain blood pressure without supportive measures.


Acute Ischemic Stroke

Administer Activase as soon as possible but within 3 hours after onset of symptoms.

The recommended dose is 0.9 mg/kg (not to exceed 90 mg total dose), with 10% of the total dose administered as an initial intravenous bolus over 1 minute and the remainder infused over 60 minutes.

During and following Activase administration for the treatment of acute ischemic stroke, frequently monitor and control blood pressure.

In patients without recent use of oral anticoagulants or heparin, Activase treatment can be initiated prior to the availability of coagulation study results. Discontinue Activase if the pretreatment International Normalized Ratio (INR) is greater than 1.7 or the activated partial thromboplastin time (aPTT) is elevated [see CONTRAINDICATIONS].

Acute Myocardial Infarction

Administer Activase as soon as possible after the onset of symptoms.

The recommended total doses for acute myocardial infarction (AMI) is based on patient weight, not to exceed 100 mg, regardless of the selected administration regimen (accelerated or 3 hour, described below).

There are two Activase dose regimens (accelerated and 3-hour) for use in the management of AMI; there are no controlled studies to compare clinical outcomes with these regimens [see Clinical Studies].

Accelerated Infusion

The recommended accelerated infusion dose consists of an IV bolus [see Administration] followed by an IV infusion as set forth in Table 1.

Table 1: Accelerated Infusion Weight-Based Doses for Patients with AMI

Patient weight Intravenous Bolus First 30 min Next 60 min
> 67 kg 15 mg 50 mg 35 mg
≤ 67 kg 15 mg 0.75 mg/kg 0.50 mg/kg

The safety and efficacy of accelerated infusion of Activase have only been investigated with concomitant administration of heparin and aspirin [see Clinical Studies].

3-Hour Infusion

For patients weighing ≥ 65 kg, the recommended dose is 100 mg administered as 60 mg in the first hour (6-10 mg administered as a bolus), 20 mg over the second hour, and 20 mg over the third hour. For smaller patients (< 65 kg), a dose of 1.25 mg/kg administered over 3 hours may be used. Weight-based doses are shown in Table 2.

Table 2: 3-hour Infusion Weight-Based Doses for Patients with AMI

Patient weight Bolus Rest of 1st hour 2nd hour 3rd hour
≥ 65 kg 6-10 mg 50-54 mg 20 mg 20 mg
< 65 kg 0.075 mg/kg 0.675 mg/kg 0.25 mg/kg 0.25 mg/kg

Pulmonary Embolism (PE)

The recommended dose is 100 mg administered by IV infusion over 2 hours.

Institute parenteral anticoagulation near the end of or immediately following the Activase infusion when the partial thromboplastin time or thrombin time returns to twice normal or less.

Preparation For Administration


Use only the accompanying Sterile Water for Injection (SWFI), USP without preservatives. Do not use Bacteriostatic Water for Injection, USP.

Reconstitute using aseptic technique. Do not add other medication to solutions containing Activase. Reconstitute Activase no more than 8 hours before use, as it contains no antibacterial preservatives [see HOW SUPPLIED/Storage and Handling].

Slight foaming is not unusual; let stand undisturbed for several minutes to allow large bubbles to dissipate. Inspect parenteral drug products for particulate matter and discoloration prior to administration whenever solution and container permit.

Activase may be administered as reconstituted at 1 mg/mL or further diluted immediately before administration in an equal volume of 0.9% Sodium Chloride Injection, USP, or 5% Dextrose Injection, USP, to yield a concentration of 0.5 mg/mL, using either polyvinyl chloride bags or glass vials.

Avoid excessive agitation during dilution; mix by gently swirling and/or slow inversion.

50 mg Vials


Using a large bore needle (e.g., 18 gauge) and a syringe, reconstitute by adding the contents of the accompanying 50 mL vial of SWFI to the 50 mg vial of Activase, directing the SWFI stream into the lyophilized cake.

100 mg Vials


Using the transfer device provided, reconstitute by adding the contents of the accompanying 100 mL vial of SWFI to the 100 mg vial of Activase.

  1. Use aseptic technique.
  2. Remove the protective flip-caps from one vial of Activase and one vial of SWFI.
  3. Open the package containing the transfer device by peeling the paper label off the package.
  4. Remove the protective cap from one end of the transfer device and keeping the vial of SWFI upright, insert the piercing pin vertically into the center of the stopper of the vial of SWFI.
  5. Remove the protective cap from the other end of the transfer device. DO NOT INVERT THE VIAL OF SWFI.
  6. Hold the vial of Activase upside down, position it so that the center of the stopper is directly over the exposed piercing pin of the transfer device, and push the vial of Activase down so that the piercing pin is inserted through the center of the Activase vial stopper.
  7. Invert the two vials so that the vial of Activase is on the bottom (upright) and the vial of SWFI is upside-down, allowing the SWFI to flow down through the transfer device. Allow the entire contents of the vial of SWFI to flow into the Activase vial (approximately 0.5 cc of SWFI will remain in the diluent vial).
  8. Remove the transfer device and the empty SWFI vial from the Activase vial and discard.
  9. Swirl gently to dissolve the Activase powder. DO NOT SHAKE.
Preparation Of Bolus Dose
  • Prepare the bolus dose in one of the following ways: Remove the appropriate volume from the vial of reconstituted (1 mg/mL) Activase using a syringe and needle. If this method is used with the 50 mg vials, the syringe should not be primed with air and the needle should be inserted into the Activase vial stopper. If the 100 mg vial is used, the needle should be inserted away from the puncture mark made by the transfer device.
  • Remove the appropriate volume from a port (second injection site) on the infusion line after the infusion set is primed.
  • Program an infusion pump to deliver the appropriate volume as a bolus at the initiation of the infusion


Following bolus dose, if indicated [see Acute Ischemic Stroke, Acute Myocardial Infarction]:

  • 50 mg vials - administer using either a polyvinyl chloride bag or glass vial and infusion set.
  • 100 mg vials - remove from the vial any quantity of drug in excess of that specified for patient treatment [see Acute Ischemic Stroke, Acute Myocardial Infarction]. Insert the spike end of an infusion set through the same puncture site created by the transfer device in the stopper of the vial of reconstituted Activase. Peel the clear plastic hanger from the vial label. Hang the Activase vial from the resulting loop.

Activase is for intravenous administration only. Extravasation of Activase infusion can cause ecchymosis or inflammation. If extravasation occurs, terminate the infusion at that IV site and apply local therapy.

Do not add any other medication to infusion solutions containing Activase.


Dosage Forms And Strengths

  • 50 mg lyophilized powder per single use vial with 50 mL SWFI USP for reconstitution
  • 100 mg lyophilized powder per single use vial with 100 mL SWFI USP for reconstitution

Storage And Handling

Activase is supplied as a sterile, lyophilized powder in 50 mg vials containing vacuum and in 100 mg vials without vacuum.

Each 50 mg Activase vial (29 million IU) is packaged with diluent for reconstitution (50 mL Sterile Water for Injection, USP): NDC 50242-044-13.

Each 100 mg Activase vial (58 million IU) is packaged with diluent for reconstitution (100 Ml Sterile Water for Injection, USP), and one transfer device: NDC 50242-085-27.

Stability And Storage

Store lyophilized Activase at controlled room temperature not to exceed 30°C (86°F), or under refrigeration (2-8°C/36-46°F). Protect the lyophilized material during extended storage from excessive exposure to light. If stored between 2-30°C (36-86°F), Activase may be used within 8 hours following reconstitution. Discard any unused solution after administration is complete.

Do not use beyond the expiration date stamped on the vial.

Manufactured by: Genentech, Inc., A Member of the Roche Group, 1 DNA Way, South San Francisco, CA. Revised: Feb 2015

This monograph has been modified to include the generic and brand name in many instances.

Last reviewed on RxList: 7/12/2016

How Supplied

Additional Activase Information

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