AnTicol山 anr dru Low molecular weight heparin LMWH,低分子肝素 Low dollar weathe 常用LMW Fatcor Xa 人 enoxaparin(依诺肝素) Tedelparin(替地肝素 Fraxiparin(弗希肝素) oparin(洛吉肝素) loO0 picoo 人 Lomoparin(洛莫肝素) Mean MW=1-12 KD Stronger Effects on Xa.Ⅻ a than onⅡa
Low molecular weight heparin (LMWH, 低分子肝素) Anticoagulant drugs Mean MW = 1~12 kD Stronger Effects on Ⅹa, Ⅻa than on Ⅱa 常用LMWH: enoxaparin (依诺肝素) Tedelparin (替地肝素) Fraxiparin (弗希肝素) Logiparin(洛吉肝素) Lomoparin (洛莫肝素) FatcorⅩa
Comparison of the Features of Heparin, LMWH, and Fondaparinux FEATURES HEPARIN LMWH FONDAPARINUX Source biological Bic ological Synthetic Molecular weight(Da) 15000 5000 1500 Xa and lla Xa and la Xa Bioavailability (%o) 90 t,,(h) 2 Renal excretion Antidote effect Complete Partial N one Thrombocytopenia 5% <l% <1% c Fatcor Xa oooo coo
FatcorⅩa
Anricoac山 ani drugs Coumarins(香豆素类) Warfarin(华法林) Dicoumarol(双香豆素) Acenocoumarol醋硝香豆素 CH2-c0 c ONa CHz 双香豆素 Dicumarol 华法林 Warfarin sodium CHz CHE CH2-CH= -el 苯茚二酮Ph phenindione Phytonadione(vitamin K1
Coumarins(香豆素类) Warfarin(华法林); Dicoumarol(双香豆素); Acenocoumarol(醋硝香豆素) Anticoagulant drugs 苯茚二酮 双香豆素 华法林
AnTicoagu山 uT drugs 1. Pharmacological effects (1)Properties Slowly and longer duration The effect appears after p.o. 1w3 days and lasts for 4 days Effective only in vivo (2)Mechanisms of action Antagonizes vitamin K It inhibits carboxylation of the gluta-mic acid residues of the factorsⅡ、Ⅶ、Ⅸ、Ⅹ to decrease the activation of factorsⅡ、Ⅶ、 Ⅸ、Ⅹ
1. Pharmacological effects (1)Properties: Slowly and longer duration: The effect appears after p.o. 1~3 days, and lasts for 4 days Effective only in vivo. (2)Mechanisms of action: Antagonizes vitamin K. It inhibits carboxylation of the gluta-mic acid residues of the factors Ⅱ、Ⅶ、Ⅸ、Ⅹ, to decrease the activation of factors Ⅱ、Ⅶ、 Ⅸ、Ⅹ. Anticoagulant drugs
o Mechanism of Coumarins Non-functional Functional prozymogens Zygomens utama carboxylase CHa reduced Vitamin K Vitamin K oxid zed Vitamin K cle R R NAD (VKORC1 vitamin K NADH reductase CPYS 1A1 1A2.3A R-warfarin Warfarin CYP209 6-OH. 8-OH and 7-OH-warfarin 10-OH warfarin warfarin
Mechanism of Coumarins