最新Tranexamic Acid in Gynaecology & Obstetrics:在妇产科止血环酸-PPT文档.ppt
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1、Blood The essence of Life,LIFE GOES ON,STOP BLOOD LOSS,STOP BLOOD LOSS,Women are always at Risk of Losing Blood,FROM MENARCHE TO MENOPAUSE,IN NORMALCY OR PREGNANCY,IN HEALTH OR DISEASE,DUB,APH,DUB,PPH,CX,DUB,HOW TO STOP IT?,Events in Hemostasis,1) Vasoconstriction,2) Platelet plug formation,3) Blood
2、 clotting,4) Fibrinolysis,Events in Haemostasis,COAGULATION:,Prothrombin,Thrombin,Fibrinogen,Fibrin,Clot,forms,Events in Haemostasis,FIBRINOLYSIS:,Plasminogen,Plasmin,dissolves,Clot,Events in Hemostasis,COAGULATION AND FIBRINOLYSIS,Events in Hemostasis,COAGULATION AND FIBRINOLYSIS,Presenting Tranexa
3、mic Acid,TRANEXAMIC ACID,Tranexamic Acid,Tranexamic Acid,Synthetic amino acid, first introduced in Sweden in1969. Chemically it is Tranexamic-stereo isomer of 1, 4, -aminomethylcyclohexane carboxylic acid. Formula C8H15NO2. Molecular Wt.-157. Prevents fibrinolysis and breakdown of clot. It is a comp
4、etitive inhibitor of plasminogen activation. At very high concentration, it is also a non competitive inhibitor of Plasmin. It is also a very weak inhibitor of thrombin.,Tranexamic Acid,Tranexamic acid inhibits conversion of plasminogen to plasmin, hence prevents breakdown of clot. Increases collage
5、n synthesis which preserves the fibrin matrix and increases the tensile strength of the clot These actions of Tranexamic acid help in stabilizing the clot,Mechanism of Action,Tranexamic Acid,Absorption after oral administration is 30-50% Food has no influence on absorption Peak plasma concentration
6、after 3 hours Presystemic metabolism nil. Bioavailability 30 50% Plasma half-life 1.4h Is able to cross the blood-aqueous barrier in the eyes. Can also cross the damaged blood-brain barrier Rapidly diffuses into joint fluid and the synovial membrane. Crosses placenta and also into breast milk. Excre
7、tion unchanged 2 hours.,Pharmacokinetics,Tranexamic Acid,Plasma protein binding is negligible Undergoes negligible metabolism in the body. Mainly eliminated unchanged in the urine. Excretion occurs by glomerular filtration via the kidneys. Passes through the placenta and its concentration in the cor
8、d blood may reach that of maternal blood.,Pharmacokinetics,Tranexamic Acid,The antifibrinolytic effect of Tranexamic acid is related mainly to a reversible complex formation with plasminogen, which prevents its activation to plasmin. Tranexamic acid is 7 to 10 times more potent than Epsilon-aminocap
9、roic acid EACA. Tranexamic acid produces a considerably higher and more sustained antifbrinolytic activity in tissues than does EACA.,Clinical Pharmacology,Tranexamic Acid,Adverse effects- are rare and mainly limited to Nausea, Vomiting & Diarrhea, Allergy and occasionally an Orthostatic reaction. T
10、here is a theoretical risk of an increased thrombotic tendency, like deep vein thrombosis, during prolonged treatment as with any fibrinolysis inhibitors. Contraindications: - Severe renal insufficiency Active intravascular clotting Thrombo embolic disease Colour vison disorders,Clinical Pharmacolog
11、y,Tranexamic Acid,Pregnancy:Tranexamic acid crosses over to the foetus. It is not known whether a reduction of the normally high fibrinolytic activity in the foetus and neonate is harmful. Lactation:Tranexamic acid is secreted in the mothers milk. This concentration is only a hundredth of the corres
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