血液系统药物培训课件

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文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Drugs affecting the blood and blood-forming organsAnticoagulant drugs(Anticoagulant drugs(抗凝药抗凝药抗凝药抗凝药)Antiplatelet drugs(Antiplatelet drugs(抗血小板药抗血小板药抗血小板药抗血小板药)Thrombolytic drugs(Thrombolytic drugs(纤溶药纤溶药纤溶药纤溶药)Drugs for treatment of bleeding Drugs for treatment of bleeding Drugs for treatment of anemiaDrugs for treatment of anemia Hematopoietic growth agentsHematopoietic growth agentsn nDrugs for treatment of Drugs for treatment of hypovolemiahypovolemiaCoagulation-bleedingBlood cell growthBlood volume文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。heparin 肝素肝素肝素肝素 low molecular weight heparinlow molecular weight heparin 低分子量肝素低分子量肝素低分子量肝素低分子量肝素dermatan sulfate 硫酸皮肤素硫酸皮肤素硫酸皮肤素硫酸皮肤素lepirudin 重组水蛭素重组水蛭素重组水蛭素重组水蛭素coumarins 香豆素类香豆素类香豆素类香豆素类 warfarinwarfarin 华法林华法林华法林华法林 dicoumaroldicoumarol 双香豆素双香豆素双香豆素双香豆素 acenocoumarolacenocoumarol 醋硝香豆素醋硝香豆素醋硝香豆素醋硝香豆素Anticoagulant drugs文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Thrombosis injures vital organs文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Stage IStage IStage IIStage IIStage IIIStage IIIIIIIaIIa外源性外源性外源性外源性 (组织损伤)(组织损伤)(组织损伤)(组织损伤)内源性内源性内源性内源性 (血管壁损伤)(血管壁损伤)(血管壁损伤)(血管壁损伤)文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Major reactions of blood coagulationMajor reactions of blood coagulation文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Coumarins文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Anticoagulant drugsHeparin 肝素肝素Molecular weights:Molecular weights:330 kDa;mean 15 kDa330 kDa;mean 15 kDa文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。1.Pharmacological effects(1)Anticoagulation Increasing the activity of AT III:Increasing the activity of AT III:The AT III The AT III inhibiting the activity of the activated IIa,inhibiting the activity of the activated IIa,IXa,Xa,XIa,XIIa IXa,Xa,XIa,XIIa.Rapid action,short duration(24 h)Rapid action,short duration(24 h)Effective both Effective both in vitroin vitro and and in vivoin vivo.Heparin 肝素肝素文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。more rapidExample of the effect of heparin文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。(2)Anti atherosclerosis(2)Anti atherosclerosis blood lipids blood lipids protecting endothelial cells protecting endothelial cells inhibiting the hypertrophy of smooth muscle cells inhibiting the hypertrophy of smooth muscle cells(3)Other effects:(3)Other effects:Anti-inflammatory,anti-oxidant effects,Anti-inflammatory,anti-oxidant effects,etc.etc.Heparin 肝素肝素文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。2.Clinical uses(1)Thrombosis:(1)Thrombosis:pulmonary emboli,deep vein pulmonary emboli,deep vein thrombosis,cardiac infraction,thrombosis,cardiac infraction,etcetc.(2)Cardiac ischemia:(2)Cardiac ischemia:high-risk patientshigh-risk patients(3)Disseminated intravascular coagulation(3)Disseminated intravascular coagulation(DIC):(DIC):early use.early use.(4)Prevention of coagulation(4)Prevention of coagulation in vitroin vitro:cardiovascular surgery,hemodialysis,cardiac canula,cardiovascular surgery,hemodialysis,cardiac canula,etc.etc.Heparin 肝素肝素文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。3.Adverse effects(1)(1)Bleeding(at larger doses)Bleeding(at larger doses)Protamine is the inhibitor of heparin.Protamine is the inhibitor of heparin.1 mg(protamine 1 mg(protamine 鱼精蛋白鱼精蛋白鱼精蛋白鱼精蛋白)=100 U(heparin)=100 U(heparin)(2)Thrombocytopenia(2)Thrombocytopenia (血小板减少血小板减少血小板减少血小板减少):):warfarin should warfarin should be substituted if the platelet count fallsbe substituted if the platelet count falls(3)Others:(3)Others:allergy,local necrosis,long-term use:allergy,local necrosis,long-term use:alpecia(alpecia(脱发脱发脱发脱发),osteoporosis(),osteoporosis(骨质疏松骨质疏松骨质疏松骨质疏松),),etc.etc.Heparin 肝素肝素文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Low molecular weight heparin MW 7 kDa Features:Stronger effects on Xa than on IIa Stronger effects on Xa than on IIa Stronger in inhibiting thrombosis/coagulation Stronger in inhibiting thrombosis/coagulation High bioavailability;Longer half life(200-300 min)High bioavailability;Longer half life(200-300 min)Weak bleeding effects Weak bleeding effectsHeparin 肝素肝素文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Fondaparinux:合成肝素衍生物合成肝素衍生物文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。heparin 肝素肝素肝素肝素 low molecular weight heparinlow molecular weight heparin 低分子量肝素低分子量肝素低分子量肝素低分子量肝素dermatan sulfate 硫酸皮肤素(硫酸皮肤素(硫酸皮肤素(硫酸皮肤素(activate HC II,activate HC II,Heparin-cofactor IIHeparin-cofactor II)lepirudin 重组水蛭素(重组水蛭素(重组水蛭素(重组水蛭素(thrombin inhibitorthrombin inhibitor)coumarins 香豆素类香豆素类香豆素类香豆素类 warfarinwarfarin 华法林华法林华法林华法林 dicoumaroldicoumarol 双香豆素双香豆素双香豆素双香豆素 acenocoumarolacenocoumarol 醋硝香豆素醋硝香豆素醋硝香豆素醋硝香豆素Anticoagulant drugs文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Anticoagulant drugsWarfarin 华法林华法林文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。1.Pharmacological effects(1)Mechanisms of action:(1)Mechanisms of action:antagonizing vitamine K,antagonizing vitamine K,inhibiting of carboxylation of the inhibiting of carboxylation of the glutamic acid residues of the glutamic acid residues of the factorsfactors II,VII,IX,XII,VII,IX,X,and ,and reducing the activated II,VII,IX,Xreducing the activated II,VII,IX,X(2)Properties:(2)Properties:slowly and longer duration:slowly and longer duration:effect appears after effect appears after p.o.p.o.13 13 days,and lasts for 4 daysdays,and lasts for 4 days effective only effective only in vivoin vivoWarfarin 华法林华法林文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Sites of warfarin action文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。warfarin actionFactor II,Factor II,VII,IX,XVII,IX,XActivated factor Activated factor II,VII,IX,XII,VII,IX,X氢醌型氢醌型氢醌型氢醌型Vit KVit K环氧型环氧型环氧型环氧型Vit KVit KCOO-文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。1.Pharmacological effects(1)Mechanisms of action:(1)Mechanisms of action:antagonizing vitamine K,antagonizing vitamine K,inhibiting of carboxylation of the inhibiting of carboxylation of the glutamic acid residues of the glutamic acid residues of the factorsfactors II,VII,IX,XII,VII,IX,X,and ,and reducing the activated II,VII,IX,Xreducing the activated II,VII,IX,X(2)Properties:(2)Properties:slowly and longer duration:slowly and longer duration:effect appears after effect appears after p.o.p.o.13 13 days,and lasts for 4 daysdays,and lasts for 4 days effective only effective only in vivoin vivoWarfarin 华法林华法林文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。2.Clinical uses Anticoagulation Anticoagulation in vivoin vivo 3.Adverse effects(1)(1)Bleeding:Bleeding:v vitamine K may antagonize the reaction;interreaction with other agents(2)Necrosis of skin and parenchyma(2)Necrosis of skin and parenchyma (软组织软组织软组织软组织)(3)Liver injury(3)Liver injury(4)Serious birth defect(4)Serious birth defect Warfarin 华法林华法林文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。4.Drug interactionsPlasma protein binding replacementHepatic metabolism:inhibitioninhibition potentiationpotentiation文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Antiplatelet drugs Inhibition of platelet metabolismsInhibition of platelet metabolismsInhibitors of cyclic nucleotide Inhibitors of cyclic nucleotide phosphodiesterasephosphodiesterase:dipyridamoledipyridamole 双嘧达莫双嘧达莫双嘧达莫双嘧达莫 (潘生丁潘生丁潘生丁潘生丁)COX inhibitors:COX inhibitors:aspirinaspirin 阿司匹林阿司匹林阿司匹林阿司匹林TXATXA2 2 receptor antagonists and TXA receptor antagonists and TXA2 2 synthetasesynthetase inhibitors:inhibitors:ridogrelridogrel 利多格雷利多格雷利多格雷利多格雷,picotamidepicotamide 匹可托安匹可托安匹可托安匹可托安 Activators of adenosine Activators of adenosine cyclasecyclase:epoprostenolepoprostenol 依前列醇依前列醇依前列醇依前列醇 Inhibition of ADP-induced platelet activation Inhibition of ADP-induced platelet activation ticlopidineticlopidine 噻氯匹定噻氯匹定噻氯匹定噻氯匹定 GpGp IIb/IIIaIIb/IIIa receptor antagonists receptor antagonists abciximababciximab 阿昔单抗阿昔单抗阿昔单抗阿昔单抗 (c7E3Fab(c7E3Fab)文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Antiplatelet drugsAspirin 阿司匹林阿司匹林Acetylsalicylic acid 乙酰水杨酸乙酰水杨酸Aspirin Aspirin 阿司匹林阿司匹林阿司匹林阿司匹林文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。small doses(40small doses(4080 mg/d):80 mg/d):inhibiting TXA inhibiting TXA2 2 synthesis,preventing thrombosis.synthesis,preventing thrombosis.used to treat ischemic heart disease,reduce the used to treat ischemic heart disease,reduce the mortality of myocardiac infarction,and prevent mortality of myocardiac infarction,and prevent cerebral thrombosis.cerebral thrombosis.larger doses:larger doses:inhibiting PGI inhibiting PGI2 2 synthesis,synthesis,promoting thrombosis.promoting thrombosis.PGIPGI2 2:vasodilation and platelet depolymerization(vasodilation and platelet depolymerization(血小板血小板血小板血小板 解聚解聚解聚解聚).).Aspirin 阿司匹林阿司匹林文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。The mechanism of The mechanism of aspirin:aspirin:Target enzymes Target enzymes acetylatedacetylated文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Thrombolytic drugs文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Thrombolytic drugsStreptokinase(SK)(T(T1/21/2=23 min;)=23 min;)Urokinase(UK)(T(T1/21/2=15 min;)=15 min;)Tissue plasminogen activator(t-PA,组组组组织织织织纤溶酶原激活剂纤溶酶原激活剂纤溶酶原激活剂纤溶酶原激活剂)i.v.i.v.T T1/21/2=38 min=38 min文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Action of thrombolytic drugsAction of thrombolytic drugst-PAt-PA(+(+)文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Thrombolytic drugsCommon adverse effects bleeding antidotes:antifibrinolytic drugs文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。BleedingBleedingThrombolysisThrombolysis文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Drugs for treatment of bleeding Vitamine KCarboxylation of the glutamic acid Carboxylation of the glutamic acid residues of factors II,IIV,IX,X,protein C.residues of factors II,IIV,IX,X,protein C.Preventing Preventing bleeding bleeding with with vitamine vitamine K K deficiency or warfarin-induced bleedingdeficiency or warfarin-induced bleeding文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Vitamin KVitamin KVitamin KVitamin K文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Drugs for treatment of bleedingThrombin-like agents thrombin prothrombin complex used for various bleeding文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Drugs for treatment of bleedingDrugs preventing activation of antifibrinolyticsDrugs preventing activation of antifibrinolytics aprotinin aprotinin(抑肽酶)抑肽酶)抑肽酶)抑肽酶)tranexamic acid tranexamic acid(AMCHA,(AMCHA,氨甲环酸氨甲环酸氨甲环酸氨甲环酸)p-aminomethylbenzoic acidep-aminomethylbenzoic acide (PAMBA,(PAMBA,氨甲苯酸)氨甲苯酸)氨甲苯酸)氨甲苯酸)used forused for preventing the activation fibrinolysis preventing the activation fibrinolysis and resultant bleedingand resultant bleeding 文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Inhibiting plasminogen activationInhibiting plasminogen activation文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Drugs for treatment of anemiaAnemia may result from the excess destruction of Anemia may result from the excess destruction of erythrocytes,and nutritional deficiencies(iron,erythrocytes,and nutritional deficiencies(iron,minerals,cobalt,vitamin Bminerals,cobalt,vitamin B1212,folic acid,ascorbic,folic acid,ascorbic acid,riboflavin,copper,zinc,etc.acid,riboflavin,copper,zinc,etc.)Iron:anemia due to loss of erythrocytes and iron deficiency anemia due to loss of erythrocytes and iron deficiency Folic acid and vitamin B12:megaloblastic anemia megaloblastic anemia Erythropoietin(EPO)promoting red cell proliferation and differentiation promoting red cell proliferation and differentiation文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Iron ferrous sulfateferrous sulfate 硫酸亚铁硫酸亚铁硫酸亚铁硫酸亚铁 ferric ammonium citrate ferric ammonium citrate 枸橼酸铁铵枸橼酸铁铵枸橼酸铁铵枸橼酸铁铵1.1.Interaction with other drugs or diet in the GI tractInteraction with other drugs or diet in the GI tract2.Used for anemia due to loss of erythrocytes and 2.Used for anemia due to loss of erythrocytes and iron deficiency iron deficiency 3.Adverse effects:3.Adverse effects:GI reactions,hypersensitivity GI reactions,hypersensitivityAcute intoxication:Acute intoxication:severe CVS and GI reactions severe CVS and GI reactions-treated with deferoxamine-treated with deferoxamine(去铁敏)(去铁敏)(去铁敏)(去铁敏)文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Folic acid1.1.Pharmacological effectsPharmacological effects Regulating nucleic acid,amino acid metabolism Regulating nucleic acid,amino acid metabolism2.2.Clinical usesClinical uses Megaloblastic anemia;MTX-induced anemia Megaloblastic anemia;MTX-induced anemia3.3.Adverse effectsAdverse effects Rarely reported Rarely reportedVitamin B12Co-factor of folic acidCo-factor of folic acidImportant in maintaining neuron myelinationImportant in maintaining neuron myelination文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Effect of EPO on red cell proliferation and differentiationEffect of EPO on red cell proliferation and differentiation文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Erythropoietin(EPO)rhEPOrhEPO1.1.Pharmacological effectsPharmacological effects Promoting red cell proliferation and Promoting red cell proliferation and differetiationdifferetiation2.2.Clinical usesClinical uses Anemia due to Anemia due to chronic renal failure with chronic renal failure with hemodialysishemodialysis,radiotherapy,chemotherapy,AIDS radiotherapy,chemotherapy,AIDS3.3.Adverse effectsAdverse effects Hypertension,epilepsy,thrombosis,Hypertension,epilepsy,thrombosis,etc.etc.文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Hematopoietic growth agentsGranulaocyte colony-stimulating factor G-CSF G-CSF 粒细胞集落刺激因子粒细胞集落刺激因子粒细胞集落刺激因子粒细胞集落刺激因子Granulaocyte/macrophage colony-stimulating factor GM-CSF GM-CSF 粒细胞粒细胞粒细胞粒细胞/巨噬细胞集落刺激因子巨噬细胞集落刺激因子巨噬细胞集落刺激因子巨噬细胞集落刺激因子Used for Used for neutropenianeutropenia(chemotherapy or (chemotherapy or radiotherapy),autologous bone marrow radiotherapy),autologous bone marrow transplantation,myelodysplasia,aplastic anemia,transplantation,myelodysplasia,aplastic anemia,AIDS-associated neutropeniaAIDS-associated neutropeniaAllergy,GI and hepatic injuries,local irritation,Allergy,GI and hepatic injuries,local irritation,etc.etc.文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Drugs for treatment of hypovolemiaDextran 右旋糖酐(葡聚糖右旋糖酐(葡聚糖右旋糖酐(葡聚糖右旋糖酐(葡聚糖)Hydroxyethyl starch 羟乙基淀粉羟乙基淀粉羟乙基淀粉羟乙基淀粉Increasing blood volumeIncreasing blood volumeInhibiting platelet aggregation(MW 40,000)Inhibiting platelet aggregation(MW 40,000)Osmotic diuretic effectsOsmotic diuretic effects文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。hydroxyethyl starch 羟乙基淀粉羟乙基淀粉文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Enzymatic degradation and excretion of hydroxyethyl starchEnzymatic degradation and excretion of hydroxyethyl starch文档仅供参考,不能作为科学依据,请勿模仿;如有不当之处,请联系网站或本人删除。Thanks!
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