alteplase

Alteplase is an injectable drug, given directly into a vein, that is used to treat conditions caused by arterial blood clots including heart attacks, strokes, chest pain at rest (unstable angina), blood clots in the lungs (pulmonary thrombosis or embolus), and other less common conditions involving blood clots.

• Alteplase is used to treat persons with heart attacks (acute myocardial infarctions), strokes, chest pain at rest (unstable angina), blood clots in the lungs (pulmonary thrombosis or embolism), and other less common conditions involving blood clots.
• It also is used for clearing blood clots from blocked venous catheters.

The most common and serious side effect of alteplase is bleeding. Minor bleeding is more common, but significant bleeding such as into the brain (intracranial hemorrhage) or fatal bleeding also occurs.

Other important side effects include:

• Nausea
• Vomiting

Other possible serious side effects include:

• Pulmonary embolism
• Cholesterol embolism
• Abnormal heartbeats
• Allergic reactions
• Re-embolization of deep DVT venous thrombi during treatment of acute massive pulmonary embolism
• Angioedema

• Clogged catheter: Alteplase is injected intravenously or directly into a clogged catheter.
• Heart attack: For heart attacks the recommended dose is a 15 mg injection followed by 50 mg or 0.75 mg/kg (up to 50 mg) infused over 30 minutes then 35 mg or 0.5 mg/kg (up to 35 mg) over 60 minutes. The total dose is 100 mg. It also can be infused over 3 hours.
• Pulmonary embolism: The dose for treating pulmonary embolism is 100 mg infused over 2 hours.
• Stroke: The dose for treating acute ischemic stroke is 0.9 mg/kg infused over one hour not to exceed 90 mg. Clogged catheters are cleared by injecting 2 mg/2 ml solution into the clogged catheter.

Alteplase breaks down clots and thereby interferes with the body's ability to stop bleeding. Therefore, drugs which also interfere with the body's ability to form blood clots (or the clot-promoting effects of platelets) increase the risk of bleeding in patients receiving alteplase. Such drugs include

• warfarin (Jantoven),
• aspirin, and
• nonsteroidal anti-inflammatory drugs (NSAIDs), for example,
  • ibuprofen (Motrin, Advil),
  • naproxen (Naprosyn, Aleve),
  • nabumetone (Relafen), and
  • platelet inhibitors such as clopidogrel (Plavix), prasugrel (Effeint), cangrelor (Kengreal), ticagrelor (Brilinta).

• Alteplase has been shown to cause damage to embryos of rabbits. No damage has been reported in humans. Doctors must carefully balance potential risks and possible benefits when prescribing alteplase to pregnant women.
• It is not known whether alteplase passes into breast milk.

What preparations of alteplase (TPA, Activase, Cathflo Activase) are available?

Powder is mixed with sterile water for injection: 2, 50, and 100 mg vials.

How should I keep alteplase (TPA, Activase, Cathflo Activase) stored?

• The vials are stored at room temperature up to 80 F (30 C) or under refrigeration at 2-8 C (36-46 F).
• Once mixed with sterile water, it must be used immediately.
• Any drug not used must be thrown away.

How does alteplase (TPA, Activase, Cathflo Activase) work?

• Alteplase is an enzyme that occurs naturally in man and causes blood clots to dissolve. It is a man-made protein manufactured by recombinant DNA technology. The naturally occurring protein, known as tissue plasminogen activator (TPA), is made by ovarian cells from the Chinese hamster. The amount that is given to patients is far greater than the amount naturally made by the body itself.

When was alteplase (TPA, Activase, Cathflo Activase) approved by the FDA?

• Alteplase was first approved for heart attacks in 1987. In 1996, it was approved for strokes.