造血系统药物（英文版）.ppt

Low Molecular Weight Heparin - 2 Less likely to cause thrombocytopenia Can be given SC once or twice daily without monitoring. Is cleared unchanged by kidney (do not use in renal failure!) rather than by mononuclear phagocyte system (RE system) as is for standard heparin. * ppt课件 Anticoagulants Coumarins * ppt课件 Warfarin – History 1900. Sweet clover was planted in Canada, the Dakotas, and Wisconsin because it would flourish in poor soil. ~improperly cured silage of sweet clover fed to cattle would kill them. 1939. Campbell and Link isolated the substance as bishydroxycoumarin (dicumerol), a coumarin compound 1948. Wisconsin Alumni Research Foundation developed a patentable product called Warfarin (from the initials of the foundation + -arin to indicate a coumarin compound). 1 * ppt课件 Warfarin – History 1948 -51. Warfarin becomes a common rodenticide (it still is). 1951. Army inductee tried to commit suicide with Warfarin. He was saved, but the physicians remarked at how good an anticoagulant it was. 1952. Warfarin introduced into clinical use as an oral anticoagulant. 2 * ppt课件 Coumarins - structure * ppt课件 Mechanism of action Courmarin decrease blood coagulation by inhibiting vitamin K epoxide reductase.This enzyme recycles oxidized vitamin K to its reduced form. And then the reduced vitamine K will go back to the recycle and participate in the carboxylation (羧化作用）of several blood coagulation proteins, factor II,VII,VI,X. For this reason, drugs in this class are also referred to as vitamin K antagonists. * ppt课件 Action of Coumarins Vitamin K Coumarins are competitive inhibitors * ppt课件 Coumarins - Action Inhibits the synthesis of (in order of potency) Factor II Factor X Factor VII Factor IX * ppt课件 Coumarins - Effect The activity of anticoagulation is delayed about 8-12 hrs until the clotting factors exhaust. * ppt课件 Administered orally Biotransformed by the liver Completely absorbed – crosses all membranes Crosses GI mucosa Crosses placenta – is ter