APROTININ

APROTININ (a-pro'ti-nin) Trasylol Classifications: coagulator, hemostatic, systemic; Therapeutic:hemostatic; antifibrinolytic Prototype: Aminocaproic acid Pregnancy Category: B

Availability

10,000 KIU/mL injection (one KIU equals 0.14 mg)

Action

A proteolytic enzyme inhibitor of bovine origin. It inhibits protease by interaction with certain proteases; aprotinin has antifibrinolytic effect, hemostatic stabilizing effect, and weak anticoagulant effect.

Therapeutic Effect

Aprotinin reduces postoperative bleeding in coronary bypass surgery patients by inhibiting fibrinolytic activity while preserving platelet adhesive function and prolonging postoperative bleeding time.

Uses

Patients at increased risk of blood loss and blood transfusion during cardiopulmonary bypass in the course of repeat coronary artery bypass surgery.

Contraindications

Hypersensitivity to aprotinin and bovine products.

Cautious Use

Patients with heparinized blood; patients previously treated with aprotinin; renal impairment, renal failure, pregnancy (category B). Safety and efficacy in children are not established.

Route & Dosage

Cardiac Surgery Adult: IV Test Dose 1 mL [10,000 kallikrein inactivator units (KIU)] given at least 10 min prior to loading dose (observe for signs of an allergic reaction) Standard Regimen IV Loading Dose 2 million KIU over 20–30 min; add 2 million KIU to the priming fluid of the cardiopulmonary priming  pump; constant infusion of 500,000 KIU/h, continue until the patient leaves the OR Alternate Regimen IV Loading Dose 1 million KIU over 20–30 min; 1 million into pump prime volume; 250,000 KIU/h while in OR

Administration

Intravenous PREPARE: IV Test Dose/Loading Dose: Use as supplied (1 mL = 1.4 mg or 10,000 KIU) without further dilution.   ADMINISTER: IV Test Dose: Give direct IV push over 1 min.  IV Loading Dose: Give over 20–30 min.  Continuous: Follow with infusion at 50 mL/h (70 mg/h or 500,000 KIU/h). Use central venous catheter exclusively for aprotinin.   INCOMPATIBILITIES Solution/additive: amino acids, corticosteroids, fat emulsion, heparin, tetracyclines.

• Store at controlled room temperature.

Adverse Effects (≥1%)

Body as a Whole: Hypersensitivity reactions (rash, urticaria, anaphylaxis). CV: Tachycardia, stroke, MI, congestive heart failure. Hematologic: Thromboembolism. Skin: Rash, urticaria. Urogenital: Nephrotoxicity (elevated serum creatinine). Other: Bronchospasm.

Interactions

Drug: Heparin results in further prolongation of the whole blood activated clotting time (ACT).

Pharmacokinetics

Distribution: Rapidly into extracellular fluid, then accumulates in proximal renal tubular epithelial cells; crosses placenta; distributed into breast milk. Metabolism: Primarily in kidneys to small peptides or amino acids. Elimination: By kidneys. Half-Life: Initial 0.7 h, terminal 7 h.

Nursing Implications

Assessment & Drug Effects

• Monitor carefully for S&S of hypersensitivity during administration (see Appendix F). If hypersensitivity occurs, immediately discontinue aprotinin and begin emergency treatment to prevent anaphylaxis.
• Monitor cardiac status and pulmonary function carefully during infusion. Patients with a history of hypersensitivity to any allergens or who have previously received aprotinin are at special risk for hypersensitivity.
• Lab tests: After surgery, monitor aPTT, ACT, and cardiac, pulmonary, renal, and liver functions.

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Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug