Actilyse

ACTILYSE
 Generic Name: alteplase

 Brand Name: Actilyse
Drug Description
What Is Actilyse and how is it used?
Actilyse (alteplase) is an enzyme, which works to break up and

dissolve blood clots that can block arteries, used in the treatment of an
acute heart attack or pulmonary embolism.
What are side effects of Actilyse?
The most common side effect of Actilyse is bleeding,

including gastrointestinal bleeding, genitourinary bleeding,
bruising, nosebleed, and bleeding gums. Other side effects of Actilyse
include:
 nausea,
 vomiting,
 low blood pressure (hypotension),
 dizziness,
 mild fever, or
 allergic reactions (swelling, rash, hives).
DESCRIPTION
Actilyse is a tissue plasminogen activator produced by recombinant DNA

technology. It is a sterile, purified glycoprotein of 527 amino acids. It is
synthesized using the complementary DNA (cDNA) for natural human
tissue-type plasminogen activator obtained from a human melanoma cell
line. Actilyse is a sterile, white to off-white, lyophilized powder for
intravenous administration after reconstitution with Sterile Water for
Injection, USP.
Table 6 : Quantitative Composition of the Lyophilized Product

100 mg Vial 50 mg Vial
Alteplase 100 mg (58 million IU) 50 mg (29 million IU)
L-Arginine 3.5 g 1.7 g
Phosphoric Acid 1g 0.5 g
Polysorbate 80 10 mg 5 mg
Vacuum No Yes
Biological potency is determined by an in vitro clot lysis assay and is

expressed in International Units (IU).
The reconstituted preparation results in a colorless to pale yellow

transparent solution containing Actilyse 1 mg/mL at approximately pH 7.3.
The osmolality of this solution is approximately 215 mOsm/kg.
Indications
INDICATIONS
Acute Ischemic Stroke
Actilyse 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
Actilyse 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
Actilyse 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.
Dosage
DOSAGE AND ADMINISTRATION
Acute Ischemic Stroke
Administer Actilyse 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 Actilyse administration for the treatment of acute

ischemic stroke, frequently monitor and control blood pressure.
In patients without recent use of oral anticoagulants or heparin, Actilyse

treatment can be initiated prior to the availability of coagulation study
results. Discontinue Actilyse 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 Actilyse 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 Actilyse 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 DOSAGE AND 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 Actilyse 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 Actilyse infusion when the partial thromboplastin time or thrombin time
returns to twice normal or less.
Preparation For Administration
Reconstitution
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 Actilyse. Reconstitute Actilyse 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.
Actilyse 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
DO NOT USE IF VACUUM IS NOT PRESENT.
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 Actilyse, directing the SWFI stream into the lyophilized cake.
100 mg Vials
THE 100 mg VIALS DO NOT CONTAIN VACUUM.
Using the transfer device provided, reconstitute by adding the contents of

the accompanying 100 mL vial of SWFI to the 100 mg vial of Actilyse.
1. Use aseptic technique.

2. Remove the protective flip-caps from one vial of Actilyse 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 Actilyse 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 Actilyse down so that the piercing pin is
inserted through the center of the Actilyse vial stopper.
7. Invert the two vials so that the vial of Actilyse 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 Actilyse 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
Actilyse vial and discard.
9. Swirl gently to dissolve the Actilyse 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) Actilyse 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 Actilyse 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
Administration
Following bolus dose, if indicated [see Acute Ischemic Stroke and 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 and 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 Actilyse. Peel the clear plastic hanger from the vial label.
Hang the Actilyse vial from the resulting loop.
Actilyse is for intravenous administration only. Extravasation of Actilyse

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 Actilyse.

Actilyse

Uploaded by

Copyright:

Available Formats

Actilyse

Uploaded by

Document Information

Copyright

Available Formats

Share this document

Share or Embed Document

Sharing Options

Did you find this document useful?

Is this content inappropriate?

Copyright:

Available Formats

Actilyse

Uploaded by

Copyright:

Available Formats

ACTILYSE

 Generic Name: alteplase

What Is Actilyse and how is it used?

Actilyse (alteplase) is an enzyme, which works to break up and

What are side effects of Actilyse?

The most common side effect of Actilyse is bleeding,

Actilyse is a tissue plasminogen activator produced by recombinant DNA

Table 6 : Quantitative Composition of the Lyophilized Product

Alteplase 100 mg (58 million IU) 50 mg (29 million IU)

L-Arginine 3.5 g 1.7 g

Phosphoric Acid 1g 0.5 g

Biological potency is determined by an in vitro clot lysis assay and is

The reconstituted preparation results in a colorless to pale yellow

Acute Ischemic Stroke

Actilyse is indicated for the treatment of acute ischemic stroke.

Exclude intracranial hemorrhage as the primary cause of stroke signs and

Acute Myocardial Infarction

The risk of stroke may outweigh the benefit produced by thrombolytic

Actilyse is indicated for the lysis of acute massive pulmonary embolism,

DOSAGE AND ADMINISTRATION

Acute Ischemic Stroke

Administer Actilyse as soon as possible but within 3 hours after onset of

The recommended dose is 0.9 mg/kg (not to exceed 90 mg total dose),

During and following Actilyse administration for the treatment of acute

In patients without recent use of oral anticoagulants or heparin, Actilyse

Acute Myocardial Infarction

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

The recommended total doses for acute myocardial infarction (AMI) is

The recommended accelerated infusion dose consists of an IV bolus

Patient weight Intravenous Bolus First 30 min Next 60 min

≤ 67 kg 15 mg 0.75 mg/kg 0.50 mg/kg

For patients weighing ≥ 65 kg, the recommended dose is 100 mg

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

< 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

Institute parenteral anticoagulation near the end of or immediately following

Preparation For Administration

Actilyse may be administered as reconstituted at 1 mg/mL or further diluted

DO NOT USE IF VACUUM IS NOT PRESENT.

Using a large bore needle (e.g., 18 gauge) and a syringe, reconstitute by

THE 100 mg VIALS DO NOT CONTAIN VACUUM.

Using the transfer device provided, reconstitute by adding the contents of

1. Use aseptic technique.

 50 mg vials - administer using either a polyvinyl chloride bag or glass vial

Actilyse is for intravenous administration only. Extravasation of Actilyse

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

You might also like