DOSAGE FORM: Liquid Injection, 1Lakh KIU/10ml, 5Lakh KIU/50ml.

BIOLOGICAL SIGNIFICANCE

Aprotinin, also known as bovine pancreatic trypsin inhibitor, BPTI is a protein that is used as medication administered by injection to reduce bleeding during complex surgery, such as heart and liver surgery. Its main effect is the slowing down of fibrinolysis, the process that leads to the breakdown of blood clots. The aim in its use is to decrease the need for blood transfusions during surgery, as well as end-organ damage due to hypotension (low blood pressure) as a result of marked blood loss. The drug was temporarily withdrawn worldwide in 2007 after studies suggested that its use increased the risk of complications or death.

CLINICAL USE
Small amounts of aprotinin can be added to tubes of drawn blood to enable laboratory measurement of certain rapidly degraded proteins such as glucagon.

In cell biology aprotinin is used as an enzyme inhibitor to prevent protein degradation during lysis or homogenizaton of cells and tissues.

Reducing blood loss and the need for blood transfusions in patients undergoing certain types of heart surgery.

MODE OF ACTION

Aprotinin inhibits several serine proteases, specifically trypsin, chymotrypsin and plasmin at a concentration of about 125,000 IU/ml, and kallikrein at 300,000 IU/ml. Its action on kallikrein leads to the inhibition of the formation of factor XIIa. As a result, both the intrinsic pathway of coagulation and fibrinolysis are inhibited. Its action on plasmin independently slows fibrinolysis. Aprotinin may also work as an irritant substance (this type of injection is called 'prolotherapy') stimulating the body to produce more healing.

STRUCTURE: