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| Primary information |
|---|
| ID | 10695 |
| Therapeutic ID | Th1158 |
| Protein Name | Aprotinin |
| Sequence | >Th1158_Aprotinin
RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA
|
| Molecular Weight | 6511.439 |
| Chemical Formula | C284H432N84O79S7 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | >100 |
| Half-life | Plasma half life: 150 minutes, Elimination half life: 10hrs |
| Description | Aprotinin, also known as bovine pancreatic trypsin inhibitor, BPTI (Trasylol, Bayer) 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. |
| Indication/Disease | 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. |
| Pharmacodynamics | 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. |
| 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 plasmin independently slows fibrinolysis. |
| Toxicity | NA |
| Metabolism | Aprotinin is slowly degraded by lysosomal enzymes. |
| Absorption | 100% (IV) |
| NA |
| Clearance | NA |
| Categories | NA |
| Patents Number | US5198534 |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Captopril- aprotinin infused intravenously in a dose of 2 million KIU over two hours blocked the acute hypotensive effect of 100mg of captopril. |
| Target | Trypsin-1,Chymotrypsinogen B,Plasminogen,Kallikrein-1 |
| Brand Name | Trasylol |
| Company | Bayer Pharmaceuticals |
| Brand Description | Bayer Pharmaceuticals |
| Prescribed For | Trasylol (aprotinin) is indicated 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. |
| Chemical Name | NA |
| Formulation | Each milliliter contains 10,000 KIU (Kallikrein Inhibitor Units) (1.4 mg/mL) and 9 mg sodium chloride in water for injection. Hydrochloric acid and/or sodium hydroxide is used to adjust the pH to 4.5-6.5. |
| Physical Appearance | It is supplied as a clear, colorless, sterile isotonic solution |
| Route of Administration | Intravenous administration |
| Recommended Dosage | dosage is given as two regimens: Regimen A and Regimen B intial dose is same 1ml (1.4mg or 10000 KIU) but loading dose and PumpPrime dose is 200ml in case of regimen A and 100ml in case of regimen B, and constant infusion rate is 50ml/hr in A and 25ml/hr in B. |
| Contraindication | Administration of Trasylol (aprotinin) to patients with a known or suspected previous aprotinin exposure during the last 12 months is contraindicated. For patients with known or suspected history of exposure to aprotinin greater than 12 months previously. |
| Side Effects | Ventricular fibrillation, heart arrest, bradycardia, congestive heart failure, hemorrhage, bundle branch block, myocardial ischemia, ventricular tachycardia, heart block, pericardial effusion, ventricular arrhythmia, shock, pulmonary hypertension. Hyperglycemia, hypokalemia, hypervolemia, acidosis. Arthralgia. Agitation, dizziness, anxiety, convulsion. Pneumonia, apnea, increased cough, lung edema. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |