GENERIC NAME: alteplase

BRAND NAME: Activase; TPA

DRUG CLASS AND MECHANISM: 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), and other less common conditions involving blood clots. 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. Alteplase was first approved for heart attacks in 1987. In 1996, it was approved for strokes.

GENERIC AVAILABLE: no

PRESCRIPTION: yes

PREPARATIONS: Powder to be mixed with sterile water for injection at concentrations of 50 mg/50 mL and 100mg/100 mL.

STORAGE: 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.

PRESCRIBED FOR: 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.

DOSING: Alteplase is injected intravenously. Depending on the condition being treated, it is given once quickly or as a brief infusion over 30 to 60 minutes.

DRUG INTERACTIONS: 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 medicines include warfarin (Coumadin), aspirin, and nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (Motrin), naproxen (Naprosyn), and nabumetone (Relafen). Specific platelet inhibitors, for example, clopidogrel (Plavix) do not appear to interact with alteplase and increase the risk of bleeding.

PREGNANCY: Alteplase has been shown to cause damage to embryos of rabbits. No damage has been reported in humans. Physicians must carefully balance potential risks and possible benefits when prescribing alteplase to pregnant women.

NURSING MOTHERS: It is not known whether alteplase passes into breast milk.

SIDE EFFECTS: The most common and serious side effect with alteplase is bleeding. Most commonly, such bleeding is minor, but significant, even fatal bleeding has been reported.

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