Characteristics and Mechanism of Action
The sole clinical representative of this group is drotrecogin alfa (activated), which is a recombinant analogue of activated protein C.
The anticoagulant effect is achieved through the proteolytic inactivation of blood coagulation cofactors — factor Va and factor VIIIa. Consequently, this blocks the further generation of thrombin.
Additional Pharmacological Properties
In addition to affecting blood coagulation, the agent exhibits other important properties:
- Fibrinolytic activity: achieved by reducing the concentration of plasminogen activator inhibitor type 1 (PAI-1), which stimulates fibrinolysis.
- Anti-inflammatory action: the drug suppresses the release of TNF-alpha (tumor necrosis factor) from monocytes.
Clinical Application and Risks
The medical application of these agents includes the treatment of septic shock. This therapeutic strategy is justified by the pathogenesis of severe sepsis, which concurrently involves systemic inflammation and pronounced hypercoagulation.
The primary adverse effect associated with the use of this drug is hemorrhagic reactions.