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Activase

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Activase

Indications
Dosage
How Supplied

INDICATIONS

Acute Myocardial Infarction

Activase (alteplase) ® (Alteplase) is indicated for use in the management of acute myocardial infarction in adults for the improvement of ventricular function following AMI, the reduction of the incidence of congestive heart failure, and the reduction of mortality associated with AMI. Treatment should be initiated as soon as possible after the onset of AMI symptoms (see CLINICAL PHARMACOLOGY).

Acute Ischemic Stroke

Activase® (Alteplase) is indicated for the management of acute ischemic stroke in adults for improving neurological recovery and reducing the incidence of disability. Treatment should only be initiated within 3 hours after the onset of stroke symptoms, and after exclusion of intracranial hemorrhage by a cranial computerized tomography (CT) scan or other diagnostic imaging method sensitive for the presence of hemorrhage (see CONTRAINDICATIONS).

Pulmonary Embolism

Activase® (Alteplase) is indicated in the management of acute massive pulmonary embolism (PE) in adults:

-For the lysis of acute pulmonary emboli, defined as obstruction of blood flow to a lobe or multiple segments of the lungs.
-For the lysis of pulmonary emboli accompanied by unstable hemodynamics, e.g., failure to maintain blood pressure without supportive measures. The diagnosis should be confirmed by objective means, such as pulmonary angiography or noninvasive procedures such as lung scanning.

DOSAGE AND ADMINISTRATION

Activase® (Alteplase) is for intravenous administration only. Extravasation of Activase (alteplase) infusion can cause ecchymosis and/or inflammation. Management consists of terminating the infusion at that IV site and application of local therapy.

Acute Myocardial Infarction

Administer Activase (alteplase) as soon as possible after the onset of symptoms.

There are two Activase (alteplase) dose regimens for use in the management of acute myocardial infarction; controlled studies to compare clinical outcomes with these regimens have not been conducted.

A DOSE OF 150 mg OF ACTIVASE (alteplase) SHOULD NOT BE USED FOR THE TREATMENT OF ACUTE MYOCARDIAL INFARCTION BECAUSE IT HAS BEEN ASSOCIATED WITH AN INCREASE IN INTRACRANIAL BLEEDING.

Accelerated Infusion

The recommended total dose is based upon patient weight, not to exceed 100 mg. For patients weighing > 67 kg, the recommended dose administered is 100 mg as a 15 mg intravenous bolus, followed by 50 mg infused over the next 30 minutes, and then 35 mg infused over the next 60 minutes.

For patients weighing ≤ 67 kg, the recommended dose is administered as a 15 mg intravenous bolus, followed by 0.75 mg/kg infused over the next 30 minutes not to exceed 50 mg, and then 0.50 mg/kg over the next 60 minutes not to exceed 35 mg.

The safety and efficacy of this accelerated infusion of Alteplase regimen has only been investigated with concomitant administration of heparin and aspirin as described in CLINICAL PHARMACOLOGY.

  1. The bolus dose may be prepared in one of the following ways:
    1. By removing 15 mL from the vial of reconstituted (1 mg/mL) Activase (alteplase) 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 (alteplase) vial stopper. If the 100 mg vial is used, the needle should be inserted away from the puncture mark made by the transfer device.
    2. By removing 15 mL from a port (second injection site) on the infusion line after the infusion set is primed.
    3. By programming an infusion pump to deliver a 15 mL (1 mg/mL) bolus at the initiation of the infusion.
  2. The remainder of the Activase (alteplase) dose may be administered as follows:

50 mg vials-administer using either a polyvinyl chloride bag or glass vial and infusion set.

100 mg vial-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 (alteplase) . Hang the Activase (alteplase) vial from the plastic molded capping attached to the bottom of the vial.

3-Hour Infusion

The recommended dose is 100 mg administered as 60 mg in the first hour (of which 6 to 10 mg is 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, as described above, may be used.15

Although the value of the use of anticoagulants during and following administration of Activase (alteplase) has not been fully studied, heparin has been administered concomitantly for 24 hours or longer in more than 90% of patients.

Aspirin and/or dipyridamole have been given to patients receiving Alteplase during and/or following heparin treatment.

  1.  The bolus dose may be prepared in one of the following ways:
    1. By removing 6 to 10 mL from the vial of reconstituted (1 mg/mL) Activase (alteplase) 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 (alteplase) vial stopper. If the 100 mg vial is used, the needle should be inserted away from the puncture mark made by the transfer device.
    2. By removing 6 to 10 mL from a port (second injection site) on the infusion line after the infusion set is primed.
    3. By programming an infusion pump to deliver a 6 to 10 mL (1 mg/mL) bolus at the initiation of the infusion.
  2.   The remainder of the Activase (alteplase) dose may be administered as follows:

50 mg vials-administer using either a polyvinyl chloride bag or glass vial and infusion set.

100 mg vial-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 (alteplase) . Hang the Activase (alteplase) vial from the plastic molded capping attached to the bottom of the vial.

Acute Ischemic Stroke

THE TOTAL DOSE FOR TREATMENT OF ACUTE ISCHEMIC STROKE SHOULD NOT EXCEED 90 mg.

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

The safety and efficacy of this regimen with concomitant administration of heparin and aspirin during the first 24 hours after symptom onset has not been investigated.

  1. The bolus dose may be prepared in one of the following ways:
    1. By removing the appropriate volume from the vial of reconstituted (1 mg/mL) Activase (alteplase) 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 (alteplase) vial stopper. If the 100 mg vial is used, the needle should be inserted away from the puncture mark made by the transfer device.
    2. By removing the appropriate volume from a port (second injection site) on the infusion line after the infusion set is primed.
    3. By programming an infusion pump to deliver the appropriate volume as a bolus at the initiation of the infusion.
  2. The remainder of the Activase (alteplase) dose may be administered as follows:

50 mg vials-administer using either a polyvinyl chloride bag or glass vial and infusion set.

100 mg vial-remove from the vial any quantity of drug in excess of that specified for patient treatment. 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 (alteplase) . Hang the Activase (alteplase) vial from the plastic molded capping attached to the bottom of the vial.

Pulmonary Embolism

The recommended dose is 100 mg administered by intravenous infusion over 2 hours. Heparin therapy should be instituted or reinstituted near the end of or immediately following the Activase (alteplase) infusion when the partial thromboplastin time or thrombin time returns to twice normal or less.

The Activase (alteplase) dose may be administered as follows:

50 mg vials-administer using either a polyvinyl chloride bag or glass vial and infusion set.

100 mg vial-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 (alteplase) . Hang the Activase (alteplase) vial from the plastic molded capping attached to the bottom of the vial.

Reconstitution and Dilution

Activase (alteplase) should be reconstituted by aseptically adding the appropriate volume of the accompanying Sterile Water for Injection, USP, to the vial. It is important that Activase (alteplase) be reconstituted only with Sterile Water for Injection, USP, without preservatives. Do not use Bacteriostatic Water for Injection, USP. The reconstituted preparation results in a colorless to pale yellow transparent solution containing Activase (alteplase) 1mg/mL at approximately pH 7.3. The osmolality of this solution is approximately 215 mOsm/kg.

Because Activase (alteplase) contains no antibacterial preservatives, it should be reconstituted immediately before use. The solution may be used for intravenous administration within 8 hours following reconstitution when stored between 2-30oC (36-86oF). Before further dilution or administration, the product should be visually inspected for particulate matter and discoloration prior to administration whenever solution and container permit.

Activase (alteplase) may be administered as reconstituted at 1 mg/mL. As an alternative, the reconstituted solution may be diluted further 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. Either polyvinyl chloride bags or glass vials are acceptable. Activase (alteplase) is stable for up to 8 hours in these solutions at room temperature. Exposure to light has no effect on the stability of these solutions. Excessive agitation during dilution should be avoided; mixing should be accomplished with gentle swirling and/or slow inversion. Do not use other infusion solutions, e.g., Sterile Water for Injection, USP, or preservative- containing solutions for further dilution.

50 mg Vials

Reconstitution should be carried out using a large bore needle (e.g., 18 gauge) and a syringe, directing the stream of Sterile Water for Injection, USP, into the lyophilized cake. DO NOT USE IF VACUUM IS NOT PRESENT. Slight foaming upon reconstitution is not unusual; standing undisturbed for several minutes is usually sufficient to allow dissipation of any large bubbles.

No other medication should be added to infusion solutions containing Activase (alteplase) .

Any unused infusion solution should be discarded.

100 mg Vial

Reconstitution should be carried out using the transfer device provided, adding the contents of the accompanying 100 mL vial of Sterile Water for Injection, USP, to the contents of the 100 mg vial of Activase (alteplase) powder. Slight foaming upon reconstitution is not unusual; standing undisturbed for several minutes is usually sufficient to allow dissipation of any large bubbles. Please refer to the accompanying Instructions for Reconstitution and Administration. 100 mg VIALS DO NOT CONTAIN VACUUM.

100 mg VIAL RECONSTITUTION

  1.  Use aseptic technique throughout.
  2.  Remove the protective flip-caps from one vial of Activase (alteplase) and one vial of Sterile Water for Injection, USP (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.  Holding the vial of Activase (alteplase) upside-down, position it so that the center of the stopper is directly over the exposed piercing pin of the transfer device.
  7.  Push the vial of Activase (alteplase) down so that the piercing pin is inserted through the center of the Activase (alteplase) vial stopper.
  8.  Invert the two vials so that the vial of Activase (alteplase) 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 (alteplase) vial (approximately 0.5 cc of SWFI will remain in the diluent vial). Approximately 2 minutes are required for this procedure.
  9.  Remove the transfer device and the empty SWFI vial from the Activase (alteplase) vial. Safely discard both the transfer device and the empty diluent vial according to institutional procedures.
  10. Swirl gently to dissolve the Activase (alteplase) powder. DO NOT SHAKE.

No other medication should be added to infusion solutions containing Activase (alteplase) .

Any unused infusion solution should be discarded.

HOW SUPPLIED

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

Each 50 mg Activase (alteplase) 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 (alteplase) 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.

Storage

Store lyophilized Activase (alteplase) 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. Do not use beyond the expiration date stamped on the vial.

Manufactured by: GENENTECH, INC. 1 DNA Way, South San Francisco, CA 94080-4990. Revision Date December 2005. FDA Approval Date May 2002. FDA rev date: 1/4/2005 

Last reviewed on RxList: 5/9/2008
This monograph has been modified to include the generic and brand name in many instances.

Indications
Dosage
How Supplied
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Additional Activase Information

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