Aprotinin




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Aprotinin
Aprotinin (Trasylol)
Aprotinin
(ah- PROH-tih-nin)
Pregnancy Category: B Trasylol (Rx)

Classification: Systemic hemostatic

Action/Kinetics: Aprotinin, a natural protease inhibitor derived from bovine lung, inhibits plasmin and kallikrein, thereby directly affecting fibrinolysis. It also inhibits the contact phase activation of coagulation which initiates coagulation and promotes fibrinolysis. In addition, aprotinin preserves the adhesive glycoproteins in the platelet membrane, rendering them resistant to damage from the increased plasmin levels and mechanical injury that occur during cardiopulmonary bypass. The net effect is to inhibit both fibrinolysis and turnover of coagulation factors and to decrease bleeding. t 1/2, IV: 150 min with a terminal elimination phase half-life of 10 hr. Aprotinin is slowly broken down by lysosomal enzymes, although depending on the dose, up to 9% may be excreted through the urine unchanged.

Uses: Prophylactically to reduce perioperative blood loss and the need for blood transfusions in clients undergoing cardiopulmonary bypass surgery in the course of repeat coronary artery bypass graft surgery. In selected cases of primary coronary artery bypass graft surgery where the risk of bleeding is high or where transfusion is unavailable or unacceptable. Use in coronary artery bypass graft is based on the risk of renal dysfunction and the risk of anaphylaxis (i.e., should a second procedure be required).

Contraindications: Hypersensitivity to aprotinin.

Special Concerns: All clients should first receive a test dose of aprotinin to assess for potential allergic reactions; caution is required when administering aprotinin (including test doses) to clients who have received the drug previously due to the risk of anaphylaxis. Safety and efficacy have not been determined in children.

Side Effects: CV: Atrial fibrillation, MI, heart failure, heart arrest, atrial flutter, ventricular tachycardia, hypotension, CHF, supraventricular tachycardia, pericarditis, phlebitis, heart block, hemolysis, CVA, ventricular fibrillation. Possibly an increased incidence of saphenous vein graft closure in clients undergoing primary or repeat coronary artery bypass graft. Respiratory: Pneumonia, respiratory disorder, asthma, apnea, dyspnea, lung edema, pleural effusion, pneumothorax. GU: Acute kidney failure kidney tubular necrosis. CNS: Confusion, convulsions, cerebral embolism. Body as a whole: Fever, sepsis, shock, allergic reactions, anaphylaxis. Miscellaneous: Liver damage.

Laboratory Test Alterations: Creatinine, transaminases, creatine kinase, PTT, activated clotting time, serum glucose. Incidence of postoperative renal dysfunction.

Drug Interactions: Captopril / Aprotinin may block the acute hypotensive drug effect Fibrinolytic drugs / Aprotinin may inhibit fibrinolytic effects Heparin / Aprotinin prolongs activated clotting time

How Supplied: Injection: 10,000 KIU/mL

Dosage
?IV Coronary bypass graft surgery.
A 1-mL (1.4-mg or 10,000-KIU) test dose must be given 10 min prior to the loading dose. Follow the test dose by the loading dose using either regimen A or B; the loading dose is then followed by the constant infusion dose. In addition, the "pump prime" dose is added to the priming fluid of the cardiopulmonary bypass circuit by replacing an aliquot of the priming fluid prior to beginning cardiopulmonary bypass. Regimen A, loading dose: 280 mg (or 2 million KIU) with 280 mg (or 2 million KIU) into the pump prime volume; constant infusion dose: 70 mg/hr (500,000 KIU/hr). Regimen B, loading dose: 140 mg (or 1 million KIU) with 140 mg (or 1 million KIU) into the pump prime volume; constant infusion dose: 35 mg/hr (250,000 KIU/hr). Total doses greater than 7 million KIU have not been studied.

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