上海交通大学：《药理学 Pharmacology》课程教学资源（讲义课件）antiAS drugs

Lipidemic modulating drugs Antiatherosclerotic agents Abnormal blood flow Plaque Narrowing of artery Narrowed Plaque artery

Lipidemic modulating drugs Antiatherosclerotic agents

Causes High blood cholesterol ■High blood pressure o Smoking o( Obesity Lack of physical activity

 High blood cholesterol High blood cholesterol  High blood pressure High blood pressure  Smoking Smoking  Obesity Obesity  Lack of physical activity Lack of physical activity

section 1 introduction 1.atherosclerosis 2.the composition of blood lipid 口cholesteryl esters(CE,胆固醇酯) ▣triglycerides(TG,甘油三酯)， ▣cholesterol,.(Ch胆固醇 ▣phospholipids (PL磷脂) 口apolipoproteins(载脂蛋白)

section 1 introduction  1.atherosclerosis 1.atherosclerosis  2.the composition of blood lipid 2.the composition of blood lipid  cholesteryl cholesteryl esters(CE esters(CE, 胆固醇酯 )  triglycerides (TG triglycerides (TG，甘油三酯),  cholesterol, (Ch cholesterol, (Ch 胆固醇 )  phospholipids (PL phospholipids (PL磷脂）  apolipoproteins apolipoproteins（载脂蛋白）

3.major lipoprotein classes: *chylomicron VLDL IDL LDL HDL 4.the action of lipoprotein in atherosclerosis formation VLDL,LDL,IDL,apoB HDL,apoA

 3. major lipoprotein classes: 3. major lipoprotein classes:  chylomicron chylomicron VLDL IDL LDL HDL VLDL IDL LDL HDL  4. the action of lipoprotein in atherosclerosis 4. the action of lipoprotein in atherosclerosis formation formation  VLDL, LDL, IDL, VLDL, LDL, IDL, apoB  HDL, apoA

4.forms of hyperlipoproteinemia form ipoprotein abnormality plasma lipid abnormality CM t TG TC LDL Tc Ib VLDL,LDL TGTC m IDL TGTC VLDL TG CM,VLDL

4. forms of hyperlipoproteinemia form ipoprotein ipoprotein abnormality abnormality plasma lipid abnormality plasma lipid abnormality I CM TG TC TG TC IIa LDL TC IIb VLDL, LDL VLDL, LDL TG TC TG TC III IDL TG TC TG TC IV VLDL TG V CM, VLDL CM, VLDL TG TC TG TC

section 2 lipidemic-modulating drugs Drugs which lower the TC and LDL 1.inhibitors of HMMG-CoA reductase Drugs: mevastatin(美伐他汀) lovastatin(洛伐他汀) pravastatin(普伐他汀) simvastatin(辛伐他汀) fluvastatin(氟伐他汀)

section 2 lipidemic-modulating drugs Drugs which lower the TC and LDL Drugs which lower the TC and LDL 1.inhibitors of HMG 1.inhibitors of HMG-CoAreductase reductase Drugs:mevastatin mevastatin (美伐他汀 ) lovastatin lovastatin (洛伐他汀 ) pravastatin pravastatin (普伐他汀 ) simvastatin simvastatin (辛伐他汀 ) fluvastatin fluvastatin (氟伐他汀 )

drugs which lower the TC and LDL 2.Bile acid-binding resins 胆汁骏结合树脂) Drugs:cholestyramine(考来烯胺) colestipol(考来替泊)

drugs which lower the TC and LDL 2.Bile acid 2.Bile acid -binding resins binding resins (胆汁酸结合树脂 胆汁酸结合树脂 ) Drugs : Drugs : cholestyramine cholestyramine (考来烯胺 ) colestipol colestipol (考来替泊 )

drugs which lower the TG and VLDL Phenyloxygen acid (fibrates) Drugs:gemfibrozil(吉非贝齐) benzafibrate(苯扎贝特) fenofibrate(非诺贝特)

drugs which lower the TG and VLDL Phenyloxygen Phenyloxygen acid (fibrates fibrates ) Drugs: gemfibrozil gemfibrozil (吉非贝齐) benzafibrate benzafibrate (苯扎贝特 ) fenofibrate fenofibrate (非诺贝特 )

Drugs which lower the TG and VLDL Nicotinic acid(烟酸 Pharmacological action (1)decrease VLDL,TG,LDL;increase HDL (2)inhibit platelet aggregation &(③)dilate vessel

Drugs which lower the TG and VLDL Nicotinic acid ( Nicotinic acid (烟酸 ) Pharmacological action Pharmacological action  (1) decrease VLDL, TG, LDL; increase (1) decrease VLDL, TG, LDL; increase HDL  (2) inhibit platelet aggregation (2) inhibit platelet aggregation  (3) dilate vessel (3) dilate vessel

section 3 Antioxidants Probucol(普罗布考) 1.pharmacological action decrease TC,LDL-c,HDL-c protect LDL from hydroperoxidation. 2.Clinical use hypercholesterylemia

section 3 Antioxidants Probucol Probucol (普罗布考 ) 1.pharmacological action 1.pharmacological action decrease TC, LDL decrease TC, LDL -c, HDL - c protect LDL from protect LDL from hydroperoxidation hydroperoxidation . 2.Clinical use 2.Clinical use hypercholesterylemia hypercholesterylemia