Tacelli Matteo, Celsa Ciro, Magro Bianca, Giannetti Aurora, Pennisi Grazia, Spatola Federica, Petta Salvatore
Sezione di Gastroenterologia e Epatologia, DiBiMIS, University of Palermo, 90127 Palermo, Italy.
Pharmaceuticals (Basel). 2018 Nov 8;11(4):121. doi: 10.3390/ph11040121.
Non-Alcoholic Fatty Liver Disease (NAFLD) is the most common cause of chronic liver disease in Western countries, accounting for 20⁻30% of general population and reaching a prevalence of 55% in patients with type 2 diabetes mellitus (T2DM). Insulin resistance plays a key role in pathogenic mechanisms of NAFLD. Many drugs have been tested but no medications have yet been approved. Antidiabetic drugs could have a role in the progression reduction of the disease. The aim of this review is to summarize evidence on efficacy and safety of antidiabetic drugs in patients with NAFLD. Metformin, a biguanide, is the most frequently used drug in the treatment of T2DM. To date 15 randomized controlled trials (RCTs) and four meta-analysis on the use of metformin in NAFLD are available. No significant improvement in histological liver fibrosis was shown, but it can be useful in the treatment of co-factors of NAFLD, like body weight, transaminase or cholesterol levels, and HbA1c levels. A possible protective role in various types of cancer has been reported for Metformin. Thiazolidinediones modulate insulin sensitivity by the activation of PPAR-γ. The RCTs and the meta-analysis available about the role of these drugs in NAFLD show an improvement in ballooning, lobular inflammation, and perhaps fibrosis, but some side effects, in particular cardiovascular, were showed. GLP-1 analogues stimulate insulin secretion by pancreatic beta cell and inhibit glucagon release; Liraglutide is the most used drug in this class and significantly improves steatosis, hepatocyte ballooning and transaminase levels. Scanty data about the role of DPP-4 and SGLT inhibitors were published. No data about insulin effects on NAFLD are available but it was showed a possible association between insulin use and the development of solid neoplasms, in particular HCC. In conclusion, antidiabetic drugs seem to be promising drugs, because they are able to treat both NAFLD manifestations and diabetes, preventing worsening of hepatic damage, but data are still conflicting. All antidiabetic drugs can be safely used in patients with compensated cirrhosis, while insulin is the preferred drug in decompensated Child C cirrhosis.
非酒精性脂肪性肝病(NAFLD)是西方国家慢性肝病最常见的病因,占普通人群的20%-30%,在2型糖尿病(T2DM)患者中的患病率达55%。胰岛素抵抗在NAFLD的发病机制中起关键作用。许多药物已进行了试验,但尚无药物获批。抗糖尿病药物可能在减缓该疾病进展方面发挥作用。本综述的目的是总结抗糖尿病药物治疗NAFLD患者有效性和安全性的证据。二甲双胍,一种双胍类药物,是治疗T2DM最常用的药物。迄今为止,有15项关于二甲双胍用于NAFLD的随机对照试验(RCT)和四项荟萃分析。未显示肝组织学纤维化有显著改善,但它可用于治疗NAFLD的相关因素,如体重、转氨酶或胆固醇水平以及糖化血红蛋白水平。据报道,二甲双胍对各类癌症可能有保护作用。噻唑烷二酮类通过激活过氧化物酶体增殖物激活受体γ(PPAR-γ)来调节胰岛素敏感性。关于这些药物在NAFLD中作用的RCT和荟萃分析显示,在气球样变和小叶炎症以及可能的纤维化方面有改善,但也显示出一些副作用,尤其是心血管方面的副作用。胰高血糖素样肽-1(GLP-1)类似物刺激胰腺β细胞分泌胰岛素并抑制胰高血糖素释放;利拉鲁肽是该类中最常用的药物,可显著改善脂肪变性、肝细胞气球样变和转氨酶水平。关于二肽基肽酶-4(DPP-4)和钠-葡萄糖协同转运蛋白(SGLT)抑制剂作用的资料很少。尚无关于胰岛素对NAFLD作用的数据,但显示胰岛素使用与实体肿瘤尤其是肝细胞癌(HCC)的发生之间可能存在关联。总之,抗糖尿病药物似乎是有前景的药物,因为它们能够治疗NAFLD的表现和糖尿病,防止肝损伤恶化,但数据仍存在矛盾。所有抗糖尿病药物均可安全用于代偿期肝硬化患者,而胰岛素是失代偿期Child C级肝硬化患者的首选药物。