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QuickView for Aprotinin (compound)

Summary
General Info

DrugBank

Identification

Name:	Aprotinin
Name (isomeric):	DB06692
Drug Type:	biotech
Description:	A single-chain polypeptide derived from bovine tissues consisting of 58 amino-acid residues. It is an inhibitor of proteolytic enzymes including CHYMOTRYPSIN; KALLIKREIN; PLASMIN; and TRYPSIN. It is used in the treatment of HEMORRHAGE associated with raised plasma concentrations of plasmin. It is also used to reduce blood loss and transfusion requirements in patients at high risk of major blood loss during and following open heart surgery with EXTRACORPOREAL CIRCULATION. (Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)
Synonyms:	Bayer A 128; bovine pancreatic trypsin inhibitor; Trazinin; Iniprol; BPTI
Brand:	Trasylol
Brand name mixture:	Tisseel Kit Vh 2.0(Aprotinin (Bovine) + Calcium Chloride + Factor Xiii + Fibrinogen (Human) + Plasmafibronectin (Cig) + Plasminogen + Thrombin (Human) + Total Protein), Tisseel Kit Vh 5.0(Aprotinin (Bovine) + Calcium Chloride + Factor Xiii + Fibrinogen (Human) + Plasmafibronectin (Cig) + Plasminogen + Thrombin (Human) + Total Protein), Tisseel K... show more » Tisseel Kit Vh 2.0(Aprotinin (Bovine) + Calcium Chloride + Factor Xiii + Fibrinogen (Human) + Plasmafibronectin (Cig) + Plasminogen + Thrombin (Human) + Total Protein), Tisseel Kit Vh 5.0(Aprotinin (Bovine) + Calcium Chloride + Factor Xiii + Fibrinogen (Human) + Plasmafibronectin (Cig) + Plasminogen + Thrombin (Human) + Total Protein), Tisseel Kit Vh 1.0(Aprotinin (Bovine) + Calcium Chloride + Factor Xiii + Fibrinogen (Human) + Plasmafibronectin (Cig) + Plasminogen + Thrombin (Human) + Total Protein) show less «
Category:	Antifibrinolytic Agents
CAS number:	9087-70-1

Pharmacology

Indication:	For prophylactic use to reduce perioperative blood loss and the need for blood transfusion in patients undergoing cardiopulmonary bypass in the course of coronary artery bypass graft surgery who are at an increased risk for blood loss and blood transfusion.
Pharmacology:	Aprotinin is a broad spectrum protease inhibitor which modulates the systemic inflammatory response (SIR) associated with cardiopulmonary bypass (CPB) surgery. SIR results in the interrelated activation of the hemostatic, fibrinolytic, cellular and humoral inflammatory systems. Aprotinin, through its inhibition of multiple mediators [e.g., kallikre... show more » Aprotinin is a broad spectrum protease inhibitor which modulates the systemic inflammatory response (SIR) associated with cardiopulmonary bypass (CPB) surgery. SIR results in the interrelated activation of the hemostatic, fibrinolytic, cellular and humoral inflammatory systems. Aprotinin, through its inhibition of multiple mediators [e.g., kallikrein, plasmin] results in the attenuation of inflammatory responses, fibrinolysis, and thrombin generation. Aprotinin inhibits pro-inflammatory cytokine release and maintains glycoprotein homeostasis. In platelets, aprotinin reduces glycoprotein loss (e.g., GpIb, GpIIb/IIIa), while in granulocytes it prevents the expression of pro-inflammatory adhesive glycoproteins (e.g., CD11b). The effects of aprotinin use in CPB involves a reduction in inflammatory response which translates into a decreased need for allogeneic blood transfusions, reduced bleeding, and decreased mediastinal re-exploration for bleeding. show less «
Mechanism 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... show more » 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. show less «
Absorption:	100% (IV)
Biotransformation:	Aprotinin is slowly degraded by lysosomal enzymes.
Route of elimination:	Following a single IV dose of radiolabelled aprotinin, approximately 25-40% of the radioactivity is excreted in the urine over 48 hours. After a 30 minute infusion of 1 million KIU, about 2% is excreted as unchanged drug. After a larger dose of 2 million KIU infused over 30 minutes, urinary excretion of unchanged aprotinin accounts for approximately 9% of the dose.
Half Life:	Following this distribution phase, a plasma half-life of about 150 minutes is observed. At later time points, (i.e., beyond 5 hours after dosing) there is a terminal elimination phase with a half-life of about 10 hours.
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Heparin	Aprotinin, in the presence of heparin, has been found to prolong the activated clotting time (ACT) as measured by a celite surface activation method. The kaolin activated clotting time appears to be much less affected.
Urokinase	Aprotonin may antagonize the effect of Urokinase. Monitor for decreased effects of Urokinase.
Tenecteplase	Aprotonin may antagonize the effect of Tenecteplase. Monitor for decreased effects of Tenecteplase.
Captopril	In study of nine patients with untreated hypertension, aprotinin infused intravenously in a dose of 2 million KIU over two hours blocked the acute hypotensive effect of 100mg of captopril.

Targets

Chymotrypsinogen B