Aprotinin: a pharmacologic overview
Related Experiment Video
Updated: Aug 23, 2026

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
Published on: May 24, 2024
Jerrold H Levy1, Edward Sypniewski
1Department of Anesthesiology, Emory University School of Medicine, Cardiothoracic Anesthesiology and Critical Care, Emory Healthcare, Atlanta, Ga, USA.
Abstract:
Aprotinin is a polypeptide with serine protease inhibitory activity of key enzymes associated with inflammatory, fibrinolytic, and hemostatic pathways. The drug binds directly to the fibrinolytic plasmin at the lower plasmin-inhibiting dose (plasma concentration, 137 KIU/mL), and the inflammatory mediator, kallikrein, using the higher kallikrein-inhibiting dose (plasma concentration, >250 KIU/mL). Aprotinin inhibits platelet glycoprotein loss (GpIb and GpIIb/IIIa receptors) associated with cardiopulmonary bypass and has been described as platelet sparing. Current literature supports direct anti-inflammatory effects through modulation of neutrophil activation, attachment, and transmigration, with resultant blunting in the rise of proinflammatory cytokine levels and deleterious tissue damaging enzymes. The pharmacologic properties of aprotinin may lead clinicians to consider this therapy for use as a hemostatic and anti-inflammatory agent in surgeries beyond its established use in coronary artery bypass graft surgery.
Related Concept Videos
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Direct-Acting Cholinergic Agonists: Pharmacokinetics
Indirect-Acting Cholinergic Agonists: Mechanism of Action
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex, leading to...
Cholinergic Antagonists: Pharmacokinetics

