Recombinant tissue plasminogen activator

Recombinant tissue plasminogen activator (rtPA) is a protein involved in the breakdown of blood clots. It is a serine protease (EC 3.4.21.68) found on endothelial cells, the cells that line the blood vessels. As an enzyme, it catalyzes the conversion of plasminogen to plasmin, the major enzyme responsible for clot breakdown.

History

The rtPA protein was first identified in 1982. It was approved by the Food and Drug Administration (FDA) in 1987 for use in acute myocardial infarction (heart attack) and in 1996 for acute ischemic stroke.

Medical uses

rtPA is used in some cases of diseases that feature blood clots, such as an acute ischemic stroke. However, use is contraindicated in cases of active internal bleeding, or a history of recent surgery.

Mechanism of action

rtPA is a serine protease that is produced by endothelial cells. This enzyme is released into the blood where it binds to fibrin clots and converts plasminogen to plasmin. Plasmin then degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.

Side effects

The most common side effect of rtPA is bleeding. Other side effects can include allergic reactions, cardiac arrhythmias, and a decrease in blood pressure.

See also

• Thrombolysis
• Stroke
• Myocardial infarction

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References

External links

• MedlinePlus Drug Information: Tissue plasminogen activator (tPA)
• Drugs.com Monograph: Alteplase