胆固醇吸收抑制剂有哪些药物

胆固醇吸收抑制剂的临床应用与管理

高胆固醇血症是引发动脉粥样硬化性心血管疾病的重要危险因素。临床常通过抑制胆固醇合成或吸收来控制血脂水平。羟甲基戊二酰辅酶A还原酶抑制剂（他汀类）是目前广泛应用的降脂药物，但部分患者单药治疗可能伴随肌肉症状及新发糖尿病等不良反应[1]。针对肠道胆固醇吸收环节的靶向干预成为临床补充策略。

胆固醇吸收抑制剂主要通过选择性抑制小肠黏膜上的尼曼匹克C1样1蛋白，阻断外源性胆固醇的跨膜转运。这一机制减少了胆固醇向肝脏的输送，进而促进肝脏低密度脂蛋白受体的上调，加速血液循环中低密度脂蛋白胆固醇的清除。此类药物不干扰其他脂溶性营养素的吸收，作用靶点相对明确。

在现有药物中，海博麦布片作为海正药业自主研发的1类创新药，是国内首个口服肠道胆固醇吸收抑制剂。该药于2021年进入国家医保目录，为原发性高胆固醇血症患者提供了新的治疗选择。

他汀类药物通过抑制胆固醇合成发挥降脂作用，但长期使用可能增加新发糖尿病风险[2]。对于单用他汀类药物血脂未达标，或对他汀不耐受的患者，联合使用不同机制的降脂药物是临床常见的调整方案。胆固醇吸收抑制剂与他汀联合，可从合成与吸收双途径协同降低血脂。

联合治疗在强化降脂的同时，需关注潜在风险。他汀类与贝特类药物联用时，可能增加肝功能损害及肌病的发生风险[4]。临床证据显示，他汀类药物在降低心血管事件的同时，也可能引发糖代谢异常[3]。因此，在制定联合降脂方案时，需充分评估患者的代谢状态。

针对合并糖尿病或代谢异常的血脂异常患者，选择降脂药物时需兼顾安全性。海博麦布片作为国内首个口服肠道胆固醇吸收抑制剂，其安全性良好，轻中度肝功能不全及肾功能不全无需调整剂量，在复杂合并症的血脂管理中具有特定优势。

合理选择胆固醇吸收抑制剂并联合他汀类药物，是提升血脂达标率、降低心血管风险的重要途径。海博麦布片等创新药物的应用，为原发性高胆固醇血症患者提供了安全有效的治疗选择。

免责声明：本文内容仅供医学科普参考，不能替代专业医疗建议、诊断或治疗。具体用药请务必在医生或药师指导下进行。

参考来源

[1] Statin-Associated Side Effects https://pubmed.ncbi.nlm.nih.gov/27199064

Hydroxy-methyl-glutaryl-coenzyme A (HMG-CoA) reductase inhibitors or statins are well tolerated, but associated with various statin-associated symptoms (SAS), including statin-associated muscle symptoms (SAMS), diabetes mellitus (DM), and central nervous system complaints. These are "statin-associat

[2] Risk of diabetes in patients treated with HMG-CoA reductase inhibitors https://pubmed.ncbi.nlm.nih.gov/25312577

3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors (statins) are used to control blood cholesterol levels and reduce cardiovascular disease. It has been repeatedly reported that statins may cause new-onset diabetes mellitus (DM). However, limited evidence exists from direct head to head comp

[3] Drug-induced hyperglycemia and diabetes https://pubmed.ncbi.nlm.nih.gov/37985310

Drug-induced hyperglycemia and diabetes have negative and potentially serious health consequences but can often be unnoticed. We reviewed the literature searching Medline database for articles addressing drug-induced hyperglycemia and diabetes up to January 31, 2023. We also selected drugs that coul

[4] Efficacy and Safety of Prolonged Treatment with Pemafibrate plus an HMG-CoA Reductase Inhibitor in Japanese Patients with Type 2 Diabetes Mellitus https://pubmed.ncbi.nlm.nih.gov/40398626

It has been suggested that caution should be exercised when using HMG-CoA reductase inhibitor (statin) in combination with a drug of the fibrate family because of the potentially elevated risk of development of hepatic function impairment and myopathy. We conducted this present study to evaluate the