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调节血脂药

药物分类

当前应用的血脂调节药主要分为以下几类:

  1. 他汀类:如洛伐他汀、辛伐他汀等。
  2. 氯贝丁酯类及苯氧乙酸类:如氯贝丁酯、非诺贝特及吉非贝齐等。
  3. 烟酸及其衍生物:如烟酸、烟酸肌醇酯等。
  4. 胆酸螯合剂:如考来烯胺等。
作用机制

动脉粥样硬化主要是由于脂质代谢紊乱及纤维蛋白溶解活性降低而引起。因此,调整血脂代谢可以防治动脉粥样硬化。血脂调节药的作用机制包括以下几个方面:

  1. 他汀类:其主要作用为抑制胆固醇的体内生成。
  2. 氯贝丁酯类:通过增加脂蛋白脂肪酶和肝脂肪酶活性,促进富含甘油三酯蛋白质的分解代谢,并能抑制胆固醇和甘油三酯的合成,同时增加固醇类的排泄。
  3. 烟酸及其衍生物:可能通过抑制脂肪组织中的脂肪溶解,减少游离脂肪酸进入肝脏,从而降低极低密度脂蛋白的生成。
  4. 胆酸螯合剂:影响胆固醇及胆酸的吸收。
临床应用
  1. 他汀类药物:能够显著降低血胆固醇与低密度脂蛋白水平(降幅为15%~60%),也有略微减弱降血甘油三酯和升高血浆高密度脂蛋白的作用,且调脂作用与其剂量有关。
  2. 氯贝丁酯类:降低血甘油三酯的作用比降低胆固醇更强。
  3. 烟酸类:降低甘油三酯的能力远强于降低血低密度脂蛋白,并能显著升高血高密度脂蛋白水平。
  4. 胆酸螯合剂:能够有效降低血低密度脂蛋白水平,同时增加血清中高密度蛋白质的含量。
中文名称 英文名称 CAS号 化学式 结构式图片
—— (3S,5R)-fluvastatin sodium 93957-55-2 C24H26FNNaO4
(3S,5R)-fluvastatin sodium
—— calcium;(E,3R,5S)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid 147511-69-1 C25H24CaFNO4+2
calcium;(E,3R,5S)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid
—— "Saxagliptin (BMS-477118,Onglyza)" 361442-04-8 C18H25N3O2
"Saxagliptin (BMS-477118,Onglyza)"
—— Hesperetin-rutinoside 520-26-3 C28H34O15
Hesperetin-rutinoside
—— calcium;(E,3S,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate 147098-20-2 C44H54CaF2N6O12S2
calcium;(E,3S,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate
—— Pharmakon1600-01505803 81131-70-6 C23H36NaO7+
Pharmakon1600-01505803
—— Crestor (TN) 147098-20-2 C22H28CaFN3O6S+2
Crestor (TN)
—— rac-Rosuvastatin Sodium Salt (Mixture: R700515 and Sodium Salt of R700500) 147098-18-8 C22H27FN3NaO6S
rac-Rosuvastatin Sodium Salt (Mixture: R700515 and Sodium Salt of R700500)
—— 147098-20-2 (Calcium) 147098-20-2 C44H54CaF2N6O12S2
147098-20-2 (Calcium)
—— [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid 344423-98-9 C33H34FN2O5
[R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid
—— Fluvastatin acid 93957-54-1 C24H26FNO4
Fluvastatin acid
—— (2S)-5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxymethyl]oxan-2-yl]oxy-2,3-dihydrochromen-4-one 520-26-3 C28H34O15
(2S)-5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxymethyl]oxan-2-yl]oxy-2,3-dihydrochromen-4-one
—— (E)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-di(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoic acid 145599-86-6 C26H34FNO5
(E)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-di(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoic acid
—— cerivastatin sodium 143201-11-0 C26H33FNO5*Na
cerivastatin sodium
—— (4R)-4-[(3R,5R,6S,10R,13R,17R)-3,6-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid 83-49-8 C24H40O4
(4R)-4-[(3R,5R,6S,10R,13R,17R)-3,6-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
—— Methylhesperidin 11013-97-1 C29H36O15
Methylhesperidin
—— octadeca-9<i>c</i>,12<i>t</i>-dienoic acid ethyl ester 544-35-4 C20H36O2
octadeca-9<i>c</i>,12<i>t</i>-dienoic acid ethyl ester
—— alpha-Hydroxydeoxycholic acid 83-49-8 C24H40O4
alpha-Hydroxydeoxycholic acid
—— fluvastatin sodium 93957-55-2 C24H25FNO4*Na
fluvastatin sodium
—— rosuvastatin sodium 147098-18-8 C22H27FN3O6S*Na
rosuvastatin sodium
—— calcium;(3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoate;trihydrate 344423-98-9 C66H74CaF2N4O13
calcium;(3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoate;trihydrate
—— fluvastatin 93957-54-1 C24H26FNO4
fluvastatin
—— fluvastatin 93957-54-1 C24H26FNO4
fluvastatin
—— 3β-hydroxy ML-236B 81093-37-0 C23H36O7
3β-hydroxy ML-236B
—— pravastatin sodium salt 81131-70-6 C23H35O7*Na
pravastatin sodium salt
—— mevastatin 73573-88-3 C23H34O5
mevastatin
—— (+)-(3R,5S)-XU 62-320 (free acid) 93957-55-2 C24H25FNNaO4
(+)-(3R,5S)-XU 62-320 (free acid)
—— 1-[2-[(3-Hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile 1360862-63-0 C17H25N3O2
1-[2-[(3-Hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
—— 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2R)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3S,5S)- 361442-04-8 C18H25N3O2
2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2R)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3S,5S)-
—— Chondroitin, hydrogen sulfate 39455-18-0 C13H21NO15S
Chondroitin, hydrogen sulfate
—— 2-(3,4-Dimethoxyphenyl)-5-hydroxy-7-[3,4,5-trihydroxy-6-[(3,4,5-trihydroxy-6-methyloxan-2-yl)oxymethyl]oxan-2-yl]oxy-2,3-dihydrochromen-4-one 11013-97-1 C29H36O15
2-(3,4-Dimethoxyphenyl)-5-hydroxy-7-[3,4,5-trihydroxy-6-[(3,4,5-trihydroxy-6-methyloxan-2-yl)oxymethyl]oxan-2-yl]oxy-2,3-dihydrochromen-4-one
—— (3S,5R,E)-7-(3-(4-fluorophenyl)-1-isopropyl-1H-indol-2-yl)-3,5-dihydroxyhept-6-enoic acid 93957-54-1 C24H26FNO4
(3S,5R,E)-7-(3-(4-fluorophenyl)-1-isopropyl-1H-indol-2-yl)-3,5-dihydroxyhept-6-enoic acid
—— hyodeoxycholic acid 83-49-8 C24H40O4
hyodeoxycholic acid