一、烟 酸 类
【药理作用】
烟酸属B族维生素,当用量超过维生素作用的用量时,可有明显的降脂作用。烟酸类药物降脂作用机制尚不十分明确,可能与抑制脂肪组织中脂解及减少肝脏中VLDL的合成及分泌有关。
此外,烟酸还具有促进脂蛋白酯酶的活性,加速脂蛋白中三酰甘油水解的作用,因而其降三酰甘油的作用明显。
【常用药物】
1.烟酸 有速释剂和缓释剂两种剂型。速释剂不良反应明显,一般难以耐受,现已不用。
缓释型烟酸片不良反应明显减轻,较易耐受。
烟酸缓释片常用量为1~2g,1/d。一般临床上建议,开始用量为0.375~0.5g,睡前服用;4周后增量至1g/d,逐渐增至最大剂量2g/d。
烟酸可使TC降低5%~20%,LDL-C降低5%~25%,TG降低20%~50%,HDL-C升高15%~35%。适用于高三酰甘油血症、低HDL-C血症或以TG升高为主的混合型高脂血症。
2.阿昔莫司 又名氧甲吡嗪、乐脂平。常用剂量0.25g,2~3/d,其降脂作用机制、临床适用范围及不良反应与烟酸相似。可使TC降低25%,TG降低50%,使HDL-C升高20%
二、胆固醇吸收抑制药
胆固醇吸收抑制药依折麦布口服后迅速吸收且广泛地结合成依折麦布-葡萄糖苷酸,作用于小肠细胞刷状缘,有效地抑制胆固醇及植物胆固醇的吸收,由于减少胆固醇向肝脏释放,促进肝脏LDL受体的合成,又加速LDL的代谢。
常用剂量为10mg/d,此剂量可使LDL-C降低约18%,与他汀类合用对LDLC、HDL-C和TG的作用进一步增强。
最常见的不良反应是头痛和恶心,CK和肝酶升高。
三、胆酸螯合剂
【作用机制】
这类药物也称为胆酸隔置剂,主要为碱性阴离子交换树脂,在肠道内能与胆酸呈不可逆性结合,因而阻碍胆酸的肠肝循环,促进胆酸随大便排出体外,阻断胆汁酸中胆固醇的重吸收。同时伴有肝内胆酸合成增加,引起肝细胞内游离胆固醇含量减少,反馈性上调肝细胞表明LDL受体表达,加速血浆LDL分解代谢,使血浆胆固醇和LDL-C浓度降低。
【常用药物】
1.考来烯胺 即消胆胺,4~5g,3/d,总量每日不超过24g。为了减少不良反应,增加患者耐受性,可从小剂量开始用药,1~3个月内达最大耐受量。
考来烯胺(24g/d)可使TC降低13.4%,LDL-C降低20.3%。不良反应是含异味,常引起肠道不良反应,如恶心、厌食、便秘甚至脂肪痢。
2.考来替泊 即降胆宁,10~20mg,1~2/d。考来替泊30mg/d和烟酸3~12g/d可使TC、TG、LDL-C降低22%、26%、23%,HDL-C升高37%。不良反应与考来烯胺相似。
参考文献
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