Antifibrinolytics, such as aminocaproic acid (ε-aminocaproic acid) and tranexamic acid are used as inhibitors of fibrinolysis. These lysine-like drugs interfere with the formation of the fibrinolytic enzyme plasmin from its precursor plasminogen by plasminogen activators (primarily t-PA and u-PA) which takes place mainly in lysine rich areas on the surface of fibrin. These drugs block the binding sites of the enzymes or plasminogen respectively and thus stop plasmin formation.
They are used in menorrhagia and bleeding tendency due to various causes. Their application may be beneficial in patients with hyperfibrinolysis because they arrest bleeding rapidly if the other components of the haemostatic system are not severely affected. This may help to avoid the use of blood products such as fresh frozen plasma (FFP) with its associated risks of infections or anaphylactic reactions.
In 2010, the CRASH-2 trial showed that the antifibrinolytic drug tranexamic acid safely reduces mortality in bleeding trauma patients.
The antifibrinolytic drug aprotinin was abandoned after identification of major side effects, especially on kidney.
The indication for use of antifibrinolytic drugs is made with various methods. The most rapid and suitable one is thromboelastometry (TEM) in whole blood, which is even possible in patients on heparin. With various assays, an enhanced fibrinolysis becomes visible in the curve signature (TEMogram) and from the calculated values, e.g. the maximum lysis parameter. A special test for the identification of increased fibrinolysis (APTEM) compares the TEM in the absence or presence of the fibrinolysis inhibitor aprotinin. In severe cases of activated fibrinolysis, this assay confirms the syndrome already in less than 15 min during the early phases of clot formation
- "antifibrinolytic" at Dorland's Medical Dictionary
- The CRASH-2 Collaborators (2010). "Effects of tranexamic acid on death, vascular occlusive events, and blood transfusion in trauma patients with significant haemorrhage (CRASH-2): a randomised, placebo-controlled trial". Lancet. 376 (9734): 23–32. doi:10.1016/S0140-6736(10)60835-5. PMID 20554319.
- Levrat A, Gros A, Rugeri L, Inaba K, Floccard B, Negrier C, David JS. Evaluation of rotation thrombelastography for the diagnosis of hyperfibrinolysis in trauma patients. Br J of Anaesthesia 2008;100:792-7.
- Antifibrinolytics at the US National Library of Medicine Medical Subject Headings (MeSH)
- MeSH list of agents 82000933