Schernthaner Guntram, Schernthaner-Reiter Marie Helene, Schernthaner Gerit-Holger
Rudolfstiftung Hospital, Vienna, Austria.
Department of Medicine III, Division of Endocrinology and Metabolism, Medical University of Vienna, Vienna, Austria.
Clin Ther. 2016 Jun;38(6):1288-1298. doi: 10.1016/j.clinthera.2016.04.037. Epub 2016 May 19.
During the last decade, the armamentarium for glucose-lowering drugs has increased enormously by the development of DPP-4 inhibitors, GLP-1 receptor agonists and SGLT2 inhibitors, allowing individualization of antidiabetic therapy for patients with type 2 diabetes (T2DM). Some combinations can now be used without an increased risk for severe hypoglycemia and weight gain. Following a request of the US Food and Drug Administration, many large cardiovascular (CV) outcome studies have been performed in patients with longstanding disease and established CV disease. In the majority of CV outcome studies, CV risk factors were well controlled and a high number of patients were already treated with ACE inhibitors/angiotensin receptor blockers, statins and antiplatelet drugs. Most studies with insulin glargine and newer glucose-lowering drugs (saxagliptin, alogliptin, sitagliptin, lixisenatide) demonstrated safety of newer glucose-lowering agents but did not show superiority in the CV outcomes compared with placebo. By contrast, in the EMPA-REG OUTCOME (Empagliflozin Cardiovascular Outcome Event Trial in Type 2 Diabetes Mellitus Patients) study, CV death, all-cause mortality, and hospitalization for heart failure were significantly decreased when empagliflozin was added instead of placebo to therapy for patients with high CV risk and T2DM already well treated with statins, glucose-lowering drugs, and blood pressure-lowering drugs as well as antiplatelet agents. In addition, renal endpoints including endstage renal disease were also significantly reduced when empagliflozin was added instead of placebo. Interestingly, the reduction of these clinically relevant end points was observed after a few months, making antiatherogenic effects an unlikely cause. The fact that the incidence of myocardial infarction (MI) and stroke were not reduced is in line with the hypothesis that hemodynamic factors in particular have contributed to the impressive improvement of the prognosis. To reduce the CV burden of patients with T2DM, drugs influencing factors involved in atherogenesis (eg, insulin resistance, chronic inflammation, increase of HDL, prothrombotic state) are more promising. The recent IRIS (Insulin Resistance Intervention after Stroke) study documented a significant reduction in stroke and MI when pioglitazone instead of placebo was given to nondiabetic patients presenting with both stroke/transient ischemic attack and insulin resistance, confirming results from the PROactive (Prospective Pioglitazone Clinical Trial in Macrovascular Events) study in patients with T2DM. Based on these new data, we suggest that the addition of both empagliflozin and pioglitazone to metformin might be the relative best option to reduce the high CV morbidity and mortality of patients with T2DM and already established CV complications. The very recent announcement that the CV outcome study with liraglutide (LEADER) also demonstrated a significant reduction of the composite endpoint (cardiovascular death, non-fatal myocardial infarction or non-fatal stroke) gives new hope for further beneficial treatment options for T2DM patients with established CVD.
在过去十年中,随着二肽基肽酶-4(DPP-4)抑制剂、胰高血糖素样肽-1(GLP-1)受体激动剂和钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂的研发,降糖药物的种类大幅增加,这使得2型糖尿病(T2DM)患者的抗糖尿病治疗能够实现个体化。现在,一些联合用药方案在使用时不会增加严重低血糖和体重增加的风险。应美国食品药品监督管理局的要求,许多大型心血管(CV)结局研究已在患有长期疾病和已确诊心血管疾病的患者中开展。在大多数CV结局研究中,CV危险因素得到了良好控制,并且大量患者已经在使用血管紧张素转换酶(ACE)抑制剂/血管紧张素受体阻滞剂、他汀类药物和抗血小板药物进行治疗。大多数关于甘精胰岛素和新型降糖药物(沙格列汀、阿格列汀、西他列汀、利司那肽)的研究表明了新型降糖药物的安全性,但与安慰剂相比,在CV结局方面并未显示出优越性。相比之下,在恩格列净心血管结局事件试验(EMPA-REG OUTCOME)研究中,对于已经接受他汀类药物、降糖药物、降压药物以及抗血小板药物充分治疗的高CV风险T2DM患者,在治疗中添加恩格列净而非安慰剂时,CV死亡、全因死亡率以及心力衰竭住院率均显著降低。此外,当添加恩格列净而非安慰剂时,包括终末期肾病在内的肾脏终点指标也显著降低。有趣的是,在几个月后就观察到了这些临床相关终点指标的降低,这使得抗动脉粥样硬化作用不太可能是其原因。心肌梗死(MI)和中风的发生率未降低这一事实与如下假设相符,即特别是血流动力学因素促成了预后的显著改善。为降低T2DM患者的CV负担,影响动脉粥样硬化发生相关因素(如胰岛素抵抗、慢性炎症、高密度脂蛋白增加、血栓前状态)的药物更具前景。最近的胰岛素抵抗干预卒中(IRIS)研究记录了,对于同时患有中风/短暂性脑缺血发作和胰岛素抵抗的非糖尿病患者,给予吡格列酮而非安慰剂时,中风和MI显著减少,这证实了T2DM患者前瞻性吡格列酮大血管事件临床试验(PROactive)研究的结果。基于这些新数据,我们建议,在二甲双胍基础上加用恩格列净和吡格列酮可能是降低已出现CV并发症T2DM患者高CV发病率和死亡率的相对最佳选择。最近关于利拉鲁肽CV结局研究(LEADER)也证明复合终点指标(心血管死亡、非致死性心肌梗死或非致死性中风)显著降低的声明,为患有已确诊CVD的T2DM患者带来了更多有益治疗选择的新希望。