Effects of nafamostat mesilate and minimal-dose aprotinin on blood-foreign surface interactions in cardiopulmonary bypass

Ann Thorac Surg. 2004 Feb;77(2):644-50. doi: 10.1016/S0003-4975(03)01513-3.

Abstract

Background: The pharmacological inhibition of blood-foreign surface interactions is an attractive strategy for reducing the morbidity associated with cardiopulmonary bypass. We compared the inhibitory effects of nafamostat mesilate (a broad-spectrum synthetic protease inhibitor) and minimal-dose aprotinin on blood-surface interactions in clinical cardiopulmonary bypass.

Methods: Eighteen patients undergoing coronary surgery were divided into three groups: (1) the control group (heparin, 4 mg/kg; n = 6), (2) the nafamostat mesilate group (heparin plus nafamostat, 0.2 mg/kg bolus followed by 2.0 mg/kg/h during cardiopulmonary bypass; n = 6), and (3) the aprotinin group (heparin plus aprotinin, 2.0 x 10(4) KIU/kg; n = 6). Platelet count, platelet aggregation, beta-thromboglobulin, prothrombin fragment F1.2, thrombin-antithrombin complex, plasminogen activator inhibitor-1, alpha2-plasmin inhibitor-plasmin complex, D-dimer, neutrophil elastase, and interleukin-6 were measured before, during, and after bypass. Bleeding times and blood loss were recorded.

Results: There were no significant differences between groups in platelet count, beta-thromboglobulin, plasminogen activator inhibitor-1, interleukin-6, bleeding times, or blood loss. Platelet aggregation was better preserved at 12 hours after surgery in the nafamostat and aprotinin groups than in the control group. Prothrombin fragment F1.2, thrombin-antithrombin complex and neutrophil elastase levels were significantly reduced by aprotinin, but not by nafamostat as compared with the control group. The alpha2-plasmin inhibitor-plasmin complex and D-dimer were significantly lower with either of the drugs. Aprotinin showed better control of D-dimer than did nafamostat.

Conclusions: Nafamostat mesilate fails to reduce thrombin formation and neutrophil elastase release, whereas minimal-dose aprotinin inhibits both. Neither nafamostat nor aprotinin inhibits platelet activation. Nafamostat reduces fibrinolysis during cardiopulmonary bypass, although its effect is not as potent as aprotinin.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Aprotinin / administration & dosage*
  • Aprotinin / adverse effects
  • Benzamidines
  • Cardiopulmonary Bypass / adverse effects*
  • Dose-Response Relationship, Drug
  • Drug Therapy, Combination
  • Female
  • Fibrin Fibrinogen Degradation Products / metabolism
  • Guanidines / administration & dosage*
  • Guanidines / adverse effects
  • Heparin / administration & dosage
  • Heparin / adverse effects
  • Humans
  • Japan
  • Leukocyte Elastase / blood
  • Male
  • Middle Aged
  • Postoperative Complications / prevention & control*
  • Postoperative Hemorrhage / prevention & control*
  • Premedication
  • Protease Inhibitors / administration & dosage*
  • Protease Inhibitors / adverse effects
  • Risk Factors
  • Systemic Inflammatory Response Syndrome / prevention & control*
  • Thrombin / metabolism
  • Thrombosis / prevention & control*

Substances

  • Benzamidines
  • Fibrin Fibrinogen Degradation Products
  • Guanidines
  • Protease Inhibitors
  • fibrin fragment D
  • Heparin
  • Aprotinin
  • Leukocyte Elastase
  • Thrombin
  • nafamostat