4.1 适应证

 根据现有研究结果,建议将依折麦布用于以下患者:①经合理饮食控制和常规剂量他汀(相当于每日阿托伐他汀10～20 mg,辛伐他汀 20～40 mg,普伐他汀40 mg,或氟伐他汀40～80 mg)治疗后TC水平仍不能达标者,可联合应用依折麦布;②经合理饮食控制后TC水平仍不能达标且不适于或不能耐受他汀治疗的患者,可应用依折麦布单药治疗;③以TG升高为主要表现的混合型血脂异常患者,可联合应用非诺贝特与依折麦布;④接受特殊治疗(如血浆置换疗法)无效或虽然有效但血脂仍未能达标的纯合子型家族性高TC血症患者,可联合应用依折麦布与他汀治疗;⑤在饮食控制基础上,依折麦布可用于纯合子型谷甾醇血症(或植物甾醇血症)患者的治疗。

 4.2 用法与用量

 依折麦布的推荐用药剂量为10 mg/d,可在每日任意时间服用,食物不影响其疗效。老年患者一般无需调整剂量。根据患者具体情况,可与不同剂量的他汀类药物联合使用。研究显示,与10 mg/d的剂量相比,服用依折麦布5 mg/d时即可发挥大部分调脂疗效[10]。因此,对于血脂异常程度较轻的患者,亦可考虑选择5 mg/d依折麦布单独或与他汀联合治疗。
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 4.3 不良反应与注意事项

 依折麦布治疗过程中不良反应少见且轻微,其发生率与安慰剂相似,较为常见者包括头痛、腹痛、腹泻,一般无需特殊处理,多不影响继续治疗。禁用于已知对此药及其添加剂过敏者以及活动性肝病患者。由于尚无充分研究证实本药对于胎儿和哺乳期婴幼儿的安全性,因此,不推荐妊娠和哺乳期妇女服用依折麦布。

 [参考文献]

 [1]Burnett JR, Huff MW. Cholesterol absorption inhibitors as a therapeutic option for hypercholesterolaemia [J]. Expert Opin Investig Drugs,2006,15(2):1337-1351.

 [2]Grundy SM, Cleeman JI, Merz CN, et al. Implications of recent clinical trials for the national cholesterol education program adult treatment panel Ⅲ guidelines [J]. Circulation,2004,110(Suppl1):227-239.
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 [3]Garcia-Calvo M, Lisnock J, Bull HG, et al. The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1) [J]. Proc Natl Acad Sci USA,2005,102(23):8132-8137.

 [4]Sudhop T, Lutjohann D, Kodal A, et al. Inhibition of intestinal cholesterol absorption by ezetimibe in humans [J]. Circulation,2002,106(15):1943-1948.

 [5]Pearson TA, Denke MA, McBride PE, et al. A community-based, randomized trial of ezetimibe added to statin therapy to attain NCEP ATP III goals for LDL cholesterol in hypercholesterolemic patients: the ezetimibe add-on to statin for effectiveness (EASE) trial [J]. Mayo Clin Proc,2005,80(5):587-595.
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 [6]Masana L, Mata P, Gagne C, et al. Long-term safety and, tolerability profiles and lipid-modifying efficacy of ezetimibe coadministered with ongoing simvastatin treatment: a multicenter, randomized, double-blind, placebo-controlled, 48-week extension study [J]. Clin Ther,2005,27(2):174-184.

 [7]Davidson MH, Ballantyne CM, Kerzner B, et al. Efficacy and safety of ezetimibe coadministered with statins: randomised, placebo-controlled, blinded experience in 2382 patients with primary hypercholesterolemia [J]. Int J Clin Pract,2004,58(8):746-755.
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 [8]McKenney JM, Farnier M, Lo KW, et al. Safety and efficacy of long-term co-administration of fenofibrate and ezetimibe in patients with mixed hyperlipidemia [J]. J Am Coll Cardiol, 2006,47(8):1584-1587.

 [9]Farnier M, Freeman MW, Macdonell G, et al. Efficacy and safety of the coadministration of ezetimibe with fenofibrate in patients with mixed hyperlipidaemia [J]. J Eur Heart,2005,26(9):897-905.

 [10]Bays HE, Moore PB, Drehobl MA, et al. Effectiveness and tolerability of ezetimibe in patients with primary hypercholesterolemia: pooled analysis of two phase II studies [J]. Clin Ther,2001,23(8):1209-1230.

 [11]Dujovne CA, Ettinger MP, McNeer JF, et al. Efficacy and safety of a potent new selective cholesterol absorption inhibitor, ezetimibe in patients with primary hypercholesterolemia [J]. Am J Cardiol,2002,90(10):1092-1097., 百拇医药(郭艺芳,胡大一) 上一页 第 1 2 3 页 下一页
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