In vitro simulation of thrombolysis inhibition.
Hyperfibrinolysis is a serious clinical complication. The inhibitory concentrations 50% of antifibrinolytics were analyzed in the microtiter plate clot lysis assay, using 50 microL of plasma clots, 10 microL of antifibrinolytic drug, 10 microL of 354 IU/mL (final) urokinase, 4.46 microg/mL (final) tissue-type plasminogen activator or 0.6 mg/mL plasmin, and 50 microL of pooled normal plasma as clot supernatant. The inhibitory concentrations 50% of lysine against urokinase or tissue-type plasminogen activator is 2.0 or 4.2 mM, against epsilon-amino-caproic acid 0.7 or 1.5 mM, against tranexamic acid 0.03 or 0.17 mM, respectively. The inhibitory concentrations 50% of lysine, epsilon-amino-caproic acid, or tranexamic acid against plasmin is 7.4, 0.4, or 0.04 mM. The inhibitory concentrations 50% of aprotinin against urokinase or tissue-type plasminogen activator is about 60 KIU/mL, against plasmin 19 KIU/mL. Lysine might be a new antifibrinolytic drug with a clinically interesting rapid pharmacokinetic. This data help correct dosing of antifibrinolytics to patients with hyperfibrinolysis.
Stief
Thomas W
TW
Department of Clinical Chemistry, University Hospital, Marburg, Germany. thstief@med.uni
D015119:Aminocaproic Acid / Q000494:pharmacology*; D000933:Antifibrinolytic Agents / Q000494:pharmacology*; D007611:Aprotinin / Q000494:pharmacology*; D006801:Humans; D008239:Lysine / Q000494:pharmacology*; D014148:Tranexamic Acid / Q000494:pharmacology*
D000933:Antifibrinolytic Agents; D014148:Tranexamic Acid; D007611:Aprotinin; D008239:Lysine; D015119:Aminocaproic Acid