Alteplase

What is Alteplase?

TPA 23

TPA 023 3D ball

• Alteplase (Activase) is a tissue plasminogen activator (tPA) used used to treat acute ischemic stroke, acute ST-elevation myocardial infarction (a type of heart attack), pulmonary embolism associated with low blood pressure.
• Alteplase is used under brand name Cathflo Activase for the treatment of blocked central venous catheter.

What are the uses of this medicine?

Alteplase (Activase) is used for the treatment of

• Acute Ischemic Stroke (AIS).
• Acute Myocardial Infarction (AMI) to reduce mortality and incidence of heart failure.
• Acute Massive Pulmonary Embolism (PE) for lysis.

Limitation of Use in AMI:

• The risk of stroke may be greater than the benefit in patients at low risk of death from cardiac causes.

How does this medicine work?

• Alteplase is a recombinant therapeutic agent which is chemically identical to or similar to endogenous tissue plasminogen activator (tPA).
• tPA is a serine protease which converts plasminogen to plasmin, a fibrinolytic enzyme.
• Upon administration, alteplase increases plasmin enzymatic activity, resulting in hyperfibrinolysis and potential dissolution of a thrombus or embolism.

Who Should Not Use this medicine ?

Do not administer Activase to treat acute ischemic stroke in the following situations in which the risk of bleeding is greater than the potential benefit:

• Current intracranial hemorrhage
• Subarachnoid hemorrhage
• Active internal bleeding
• Recent (within 3 months) intracranial or intraspinal surgery or serious head trauma
• Presence of intracranial conditions that may increase the risk of bleeding (e.g., some neoplasms, arteriovenous malformations, or aneurysms)
• Bleeding diathesis
• Current severe uncontrolled hypertension

Do not administer Activase for treatment of Acute Myocardial Infarction or Pulmonary Embolism in the following situations in which the risk of bleeding is greater than the potential benefit

• Active internal bleeding
• History of recent stroke
• Recent (within 3 months) intracranial or intraspinal surgery or serious head trauma
• Presence of intracranial conditions that may increase the risk of bleeding (e.g. some neoplasms, arteriovenous malformations, or aneurysms)
• Bleeding diathesis
• Current severe uncontrolled hypertension

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention if you are taking any of the following:

• Anticoagulants and antiplatelet drugs
• Angiotensin-converting enzyme inhibitors

Is this medicine FDA approved?

• Alteplase was approved for medical use in the United States in November 1987 for the treatment of myocardial infarction.

How should this medicine be used?

Recommended dosage: Acute Ischemic Stroke:

• The recommended dose is 0.9 mg/kg (not to exceed 90 mg total dose) infused intravenously over 60 minutes with 10% of the total dose administered as an initial bolus over 1 minute.
• Administer Activase as soon as possible but within 3 hours after onset of symptoms.
• During and following Activase administration for the treatment of acute ischemic stroke, frequently monitor and control blood pressure.

Acute Myocardial Infarction:

• Administer Activase as soon as possible after the onset of symptoms.
• The recommended total dose is based on patient weight, not to exceed 100 mg.

Acute Massive Pulmonary Embolism:

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

Administration:

• Activase is for [[intravenous] administration only.
• Do not add any other medication to infusion solutions containing Activase.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Lyophilized powder: 50 mg and 100 mg with Sterile Water for Injection USP for reconstitution at 1 mg per 1 mL.

This medicine is available in fallowing brand namesː

• Activase

What side effects can this medication cause?

The most common side effects of this medicine include:

• bleeding
• Hypersensitivity
• Thromboembolism
• Cholesterol Embolization

What special precautions should I follow?

• Activase can cause significant, sometimes fatal, internal or external bleeding, especially at arterial and venous puncture sites. Avoid intramuscular injections and trauma to the patient while on Activase. Perform venipunctures carefully and only as required. Monitor for bleeding. If serious bleeding occurs, discontinue Activase.
• Hypersensitivity, including urticarial / anaphylactic reactions, have been reported after administration of Activase (e.g., laryngeal edema, rash and shock). Monitor patients during and for several hours after infusion for hypersensitivity. If signs of hypersensitivity develop, discontinue Activase.
• The use of thrombolytics can increase the risk of thrombo-embolic events in patients with high likelihood of left heart thrombus, such as patients with mitral stenosis or atrial fibrillation. Consider the risk of reembolization from the lysis of underlying deep venous thrombi in patients with pulmonary embolism.
• Cholesterol embolism has been reported rarely in patients treated with thrombolytic agents; the true incidence is unknown. It is associated with invasive vascular procedures (e.g., cardiac catheterization, angiography, vascular surgery) and/or anticoagulant therapy.
• Coagulation tests and measures of fibrinolytic activity may be unreliable during Activase therapy. Activase remains active under in vitro conditions, which can result in degradation of fibrinogen in blood samples removed for analysis.

What to do in case of emergency/overdose?

In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Published studies and case reports on alteplase use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes.

Can this medicine be used in children?

• Safety and effectiveness of Activase in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• ALTEPLASE

Inactive ingredients:

• ARGININE
• PHOSPHORIC ACID
• POLYSORBATE 80

Who manufactures and distributes this medicine?

Manufactured by:

• Genentech, Inc.
• A Member of the Roche Group
• 1 DNA Way
• South San Francisco, CA

• Activase® is a registered trademark of Genentech, Inc.

What should I know about storage and disposal of this medication?

• 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.

• Dailymed label info on Alteplase
• FDA Alteplase