Aprotinin: Uses, Dosage, Side Effects and More

This information is not country-specific. Please refer to the Malaysia prescribing information.

Generic Medicine Info

Indications and Dosage

Intravenous
Prophylaxis of perioperative blood loss in patients undergoing coronary artery bypass graft

Adult: Administer a test dose of 10,000 kallikrein inactivator units approx 10 minutes before the loading dose; an H₁ and H₂ antagonist may be given 15 minutes before the test dose. Loading dose: 1,000,000-2,000,000 kallikrein inactivator units via slow IV inj (Max rate: 5-10 mL/min) or infusion over 20-30 minutes after induction of anaesthesia but before sternotomy. An additional 1,000,000-2,000,000 kallikrein inactivator units should be added to the pump prime of the heart-lung machine. Maintenance dose: 250,000-500,000 kallikrein inactivator units/hour until the end of the operation via continuous infusion at 25-50 mL/hour. Max recommended dose per treatment course: 7,000,000 kallikrein inactivator units (including loading dose and maintenance dose). Doses are given to patients in the supine position. Dosage recommendations may vary between countries and individual products (refer to specific product guidelines).

Incompatibility

Incompatible with antibiotics (e.g. tetracyclines), corticosteroids, heparin, and nutrient solutions containing amino acids or fat emulsions.

Contraindications

Hypersensitivity. Known or suspected exposure to aprotinin, including through fibrin sealant products, within the past 12 months; positive aprotinin-specific IgG antibody tests.

Special Precautions

Patient with risk factors for altered renal function; receiving potential nephrotoxins (e.g. aminoglycosides). Repeated use; re-exposure within 12 months of previous use. Not recommended for routine use in cases of low to moderate risk of cardiac operations. Not for use when CABG surgery is combined with another CV surgery. Renal impairment. Pregnancy and lactation.

Adverse Reactions

Significant: Renal dysfunction.
Cardiac disorders: Myocardial ischaemia, coronary occlusion, MI, pericardial effusion.
Investigations: Increased blood creatinine.
Renal and urinary disorders: Oliguria, acute kidney injury, renal tubular necrosis.
Vascular disorders: Thrombosis, embolic stroke.
Potentially Fatal: Increased risk of mortality. Rarely, severe allergic reactions or anaphylactic shock.

Monitoring Parameters

Monitor aprotinin-specific IgG antibody (before administration); renal function. Assess for signs and symptoms of hypersensitivity reactions (e.g. blood pressure). Maintain adequate anticoagulation with heparin during therapy through recommended methods (e.g. activated clotting time test, fixed heparin dosing, or determination of heparin levels).

Drug Interactions

May reduce the therapeutic effects of thrombolytic drugs (e.g. streptokinase, urokinase, alteplase).

Lab Interference

May not reflect the actual degree of anticoagulation by heparin due to significant increase in aPTT and celite activated clotting time. Kaolin-based activated clotting times are not affected to the same degree as celite activated clotting times.

Action

Description:
Mechanism of Action: Aprotinin, a haemostatic agent, is a broad-spectrum protease inhibitor. It acts as an inhibitor of human trypsin, plasmin, plasma kallikrein and tissue kallikrein by forming reversible stoichiometric enzyme-inhibitor complexes, thereby inhibiting fibrinolysis. In addition, it also prevents the contact phase activation of coagulation which both initiates coagulation and promotes fibrinolysis.
Pharmacokinetics:
Distribution: Volume of distribution: 20 L.
Metabolism: Metabolised in the renal system via lysosomal enzymes.
Excretion: Via urine (25-40%; <5% as unchanged drug). Elimination half-life: 0.3-0.7 hours (plasma); 5-10 hours (terminal).

Storage

Store below 25°C. Protect from light.

MIMS Class

Haemostatics

ATC Classification

B02AB01 - aprotinin ; Belongs to the class of proteinase inhibitor antifibrinolytics. Used in the treatment of hemorrhage.

References

Aprotinin 10,000 KIU/mL Injection BP (Nordic Group B.V.). MHRA. https://products.mhra.gov.uk. Accessed 17/01/2025.

Aprotinin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 17/01/2025.

Brayfield A, Cadart C (eds). Aprotinin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 17/01/2025.

Disclaimer: This information is independently developed by MIMS based on Aprotinin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2025 MIMS. All rights reserved. Powered by MIMS.com