Aprotinin (Trasylol®, Bayer) is medication administered by injection used to reduce bleeding during complex surgery, such as heart and liver surgery. Its main effect is the slowing down fibrinolysis, the process that leads to the breakdown of blood clots. The aim in its use is to decrease 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.

Chemistry

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Aprotinin is a 58 amino acid polypeptide extracted from cow lung. It has a molecular weight of 6512Mannucci PM. Hemostatic drugs. N Engl J Med 1998;339:245-53. PMID 9673304.Mahdy AM, Webster NR. Perioperative systemic haemostatic agents. Br J Anaesth 2004;93:842-58. PMID 15277296.. It has disulfide bonds in three places: between residues 5 and 55, 14 and 38 as well as 30 and 51.Kassell B, Laskowski M Sr. The basic trypsin inhibitor of bovine pancreas. V. The disulfide linkages. Biochem Biophys Res Commun 1965;20:463-8. PMID 5860161. Its amino acid sequence is RPDFC LEPPY TGPCK ARIIR YFYNA KAGLC QTFVY GGCRA KRNNF KSAED CMRTC GGA.Kassell B, Radicevic M, Ansfield MJ, Laskowski Sr M. The basic trypsin inhibitor of bovine pancreas IV. The linear sequence of the 58 amino acids. Biochem Biophys Res Commun 1965;18:255-8. PMID 14282026.

Mode of action

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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.

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