Anistreplase
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Anistreplase is a
thrombolytic Thrombolysis, also called fibrinolytic therapy, is the breakdown (lysis) of blood clots formed in blood vessels, using medication. It is used in ST elevation myocardial infarction, stroke, and in cases of severe venous thromboembolism (massive p ...
drug. It is also known as anisoylated plasminogen streptokinase activator complex (APSAC). As a thrombolytic drug, it is used to treat
blood clots A thrombus (plural thrombi), colloquially called a blood clot, is the final product of the blood coagulation step in hemostasis. There are two components to a thrombus: aggregated platelets and red blood cells that form a plug, and a mesh of cr ...
in emergency situations.


Uses

Anistreplase is used to treat
blood clots A thrombus (plural thrombi), colloquially called a blood clot, is the final product of the blood coagulation step in hemostasis. There are two components to a thrombus: aggregated platelets and red blood cells that form a plug, and a mesh of cr ...
in emergency situations such as
myocardial infarction A myocardial infarction (MI), commonly known as a heart attack, occurs when blood flow decreases or stops to the coronary artery of the heart, causing damage to the heart muscle. The most common symptom is chest pain or discomfort which may ...
. Early treatment gives better outcomes.


Mechanism of action

Anistreplase is a complex of purified human
plasminogen Plasmin is an important enzyme () present in blood that degrades many blood plasma proteins, including fibrin clots. The degradation of fibrin is termed fibrinolysis. In humans, the plasmin protein (in the zymogen form of plasminogen) is encode ...
and bacterial
streptokinase Streptokinase (SK) is a thrombolytic medication activating plasminogen by nonenzymatic mechanism. As a medication it is used to break down clots in some cases of myocardial infarction (heart attack), pulmonary embolism, and arterial thromboemboli ...
that has been acylated to protect the enzyme's active site. When the drug is administered, the acyl group gets hydrolyzed, thereby freeing the activator complex. It converts
plasminogen Plasmin is an important enzyme () present in blood that degrades many blood plasma proteins, including fibrin clots. The degradation of fibrin is termed fibrinolysis. In humans, the plasmin protein (in the zymogen form of plasminogen) is encode ...
to
plasmin Plasmin is an important enzyme () present in blood that degrades many blood plasma proteins, including fibrin clots. The degradation of fibrin is termed fibrinolysis. In humans, the plasmin protein (in the zymogen form of plasminogen) is encoded ...
, which in turn degrades fibrin (
blood clot A thrombus (plural thrombi), colloquially called a blood clot, is the final product of the blood coagulation step in hemostasis. There are two components to a thrombus: aggregated platelets and red blood cells that form a plug, and a mesh of c ...
s) to fibrin split products.


History

Anistreplase has been developed by
Beecham Beecham is a surname. Notable people with the surname include: * Audrey Beecham (1915–1989), poet and niece of the conductor * Betty Humby Beecham (1908–1958), British pianist and wife of the conductor * Earl Beecham (born 1965), American foo ...
under the brand name Eminase. It is also known as anisoylated plasminogen streptokinase activator complex (APSAC) after its components.


References

Antithrombotic enzymes {{blood-drug-stub