Chong P H, Bachenheimer B S
College of Pharmacy, University of Illinois, and Cook County Hospital, Chicago 60612-3785, USA.
Drugs. 2000 Jul;60(1):55-93. doi: 10.2165/00003495-200060010-00005.
The new therapeutic options available to clinicians treating dyslipidaemia in the last decade have enabled effective treatment for many patients. The development of the HMG-CoA reductase inhibitors (statins) have been a major advance in that they possess multiple pharmacological effects (pleiotropic effects) resulting in potent reductions of low density lipoproteins (LDL) and prevention of the atherosclerotic process. More recently, the newer fibric acid derivatives have also reduced LDL to levels comparable to those achieved with statins, have reduced triglycerides, and gemfibrozil has been shown to increase high density lipoprotein (HDL) levels. Nicotinic acid has been made tolerable with sustained-release formulations, and is still considered an excellent choice in elevating HDL cholesterol and is potentially effective in reducing lipoprotein(a) [Lp(a)] levels, an emerging risk factor for coronary heart disease (CHD). Furthermore, recent studies have reported positive lipid-lowering effects from estrogen and/or progestogen in postmenopausal women but there are still conflicting reports on the use of these agents in dyslipidaemia and in females at risk for CHD. In addition to lowering lipid levels, these antihyperlipidaemic agents may have directly or indirectly targeted thrombogenic, fibrinolytic and atherosclerotic processes which may have been unaccounted for in their overall success in clinical trials. Although LDL cholesterol is still the major target for therapy, it is likely that over the next several years other lipid/lipoprotein and nonlipid parameters will become more generally accepted targets for specific therapeutic interventions. Some important emerging lipid/lipoprotein parameters that have been associated with CHD include elevated triglyceride, oxidised LDL cholesterol and Lp(a) levels, and low HDL levels. The nonlipid parameters include elevated homocysteine and fibrinogen, and decreased endothelial-derived nitric oxide production. Among the new investigational agents are inhibitors of squalene synthetase, acylCoA: cholesterol acyltransferase, cholesteryl ester transfer protein, monocyte-macrophages and LDL cholesterol oxidation. Future applications may include thyromimetic therapy, cholesterol vaccination, somatic gene therapy, and recombinant proteins, in particular, apolipoproteins A-I and E. Non-LDL-related targets such as peroxisome proliferator-activating receptors, matrix metalloproteinases and scavenger receptor class B type I may also have clinical significance in the treatment of atherosclerosis in the near future. Before lipid-lowering therapy, dietary and lifestyle modification is and should be the first therapeutic intervention in the management of dyslipidaemia. Although current recommendations from the US and Europe are slightly different, adherence to these recommendations is essential to lower the risk of atherosclerotic vascular disease, more specifically CHD. New guidelines that are expected in the near future will encompass global opinions from the expert scientific community addressing the issue of target LDL goal (aggressive versus moderate lowering) and the application of therapy for newer emerging CHD risk factors.
在过去十年中,临床医生在治疗血脂异常方面有了新的治疗选择,这使得许多患者能够得到有效治疗。HMG-CoA还原酶抑制剂(他汀类药物)的开发是一项重大进展,因为它们具有多种药理作用(多效性作用),可有效降低低密度脂蛋白(LDL)并预防动脉粥样硬化进程。最近,新型纤维酸衍生物也能将LDL降低到与他汀类药物相当的水平,还能降低甘油三酯,并且已证明吉非贝齐可提高高密度脂蛋白(HDL)水平。烟酸通过缓释制剂已变得更易耐受,并且在升高HDL胆固醇方面仍被认为是一个极佳选择,在降低脂蛋白(a)[Lp(a)]水平方面可能也有效,而Lp(a)是冠心病(CHD)一个新出现的危险因素。此外,最近的研究报告了雌激素和/或孕激素对绝经后女性有积极的降脂作用,但关于这些药物在血脂异常和有CHD风险的女性中的应用仍存在相互矛盾的报告。除了降低血脂水平外,这些降血脂药物可能直接或间接针对血栓形成、纤维蛋白溶解和动脉粥样硬化进程,而这些在其临床试验的总体成功中可能未被考虑到。虽然LDL胆固醇仍然是主要治疗靶点,但在未来几年,其他脂质/脂蛋白和非脂质参数可能会更普遍地成为特定治疗干预的公认靶点。一些与CHD相关的重要新出现的脂质/脂蛋白参数包括甘油三酯升高、氧化型LDL胆固醇和Lp(a)水平升高以及HDL水平降低。非脂质参数包括同型半胱氨酸和纤维蛋白原升高以及内皮源性一氧化氮生成减少。新的研究药物包括角鲨烯合成酶抑制剂、酰基辅酶A:胆固醇酰基转移酶抑制剂、胆固醇酯转运蛋白抑制剂、单核细胞 - 巨噬细胞抑制剂和LDL胆固醇氧化抑制剂。未来的应用可能包括甲状腺激素模拟疗法、胆固醇疫苗接种、体细胞基因疗法和重组蛋白,特别是载脂蛋白A-I和E。非LDL相关靶点,如过氧化物酶体增殖物激活受体、基质金属蛋白酶和B类I型清道夫受体,在不久的将来对动脉粥样硬化的治疗可能也具有临床意义。在进行降脂治疗之前,饮食和生活方式的改变过去是、现在也应该是血脂异常管理中的首要治疗干预措施。尽管美国和欧洲目前的建议略有不同,但遵循这些建议对于降低动脉粥样硬化性血管疾病,尤其是CHD的风险至关重要。预计在不久的将来出台的新指南将涵盖专家科学界对目标LDL目标(积极降低与适度降低)问题以及针对新出现的CHD危险因素的治疗应用的全球意见。