DPP-4抑制剂治疗糖尿病的临床疗效

目的探讨DPP-4抑制剂治疗糖尿病的临床疗效。方法选取2013年3月—2015年3月晋中市第一人民医院收治的84例糖尿病患者,分为对照组和观察组,每组42例。对照组患者接受双胍类(二甲双胍)药物治疗,观察组患者在对照组基础上接受DPP-4抑制剂(西格列汀)治疗。比较两组患者的临床疗效及不良反应发生情况。结果观察组患者空腹血糖(FPG)、餐后2h血糖(2h PG)及糖化血红蛋白(Hb A1c)低于对照组,总有效率高于对照组,不良反应发生率低于对照组,差异有统计学意义(P<0.05)。结论 DPP-4抑制剂治疗糖尿病的临床疗效显著,不良反应少,安全性高。     

DPP-4抑制剂——糖尿病治疗新里程碑

糖尿病在人类历史中并不是个陌生的疾病,早在几千年前的文献古籍中就已有消渴者……每发即小便至甜"的描述.但古人对糖尿病一直没有行之有效的治疗方法,直到1922年胰岛素首次应用,使糖尿病的治疗取得了突破性的进展,糖尿病不再是无法控制的疾病,众多患者得以延续生命,第1例接受胰岛素治疗的患者甚至活到了74岁高龄.     

DPP-4抑制剂研究进展

DPP-4抑制剂是一类用于治疗2型糖尿病的口服降糖新药,可改善血糖控制,并且不会诱发低血糖和增加体重。与原有药物相比,DPP-4抑制剂在用药安全性方面具有显著的优势。本综述介绍已上市的DPP-4抑制剂及其作用机理和临床研究。     

DPP-4抑制剂在2型糖尿病治疗中的作用

2型糖尿病已成为全球范围内发病率增长最快的疾病之一,其发病和进展的重要原因是：胰岛的β细胞胰岛素分泌缺陷和α细胞胰升糖素不适当的分泌造成的胰岛素与胰升糖素比例失调,目前药物治疗不能从根本上阻止β细胞和α细胞的功能恶化.肠促胰素能同时改善胰岛α及β细胞功能,成为治疗糖尿病的新靶点.由于其血浆半衰期仅2 min,很快被二肽基肽酶（DPP-4）降解,口服给药的DPP-4抑制剂成为2型糖尿病治疗的新选择.其作用机制抑制二肽基肽酶的活性,保护内源性肠促胰素活性,发挥葡萄糖依赖性降糖作用.其代表药物有西格列汀、维格列汀、沙格列汀等.其在2型糖尿病中的作用,能够显著降低HbA1c,空腹和餐后血糖,与磺脲类相比DPP-4抑制剂非劣效于磺脲类,由于是葡萄糖依赖性降糖,不会出现低血糖.能改善胰岛素抵抗,同时改善α及β细胞功能障碍,DPP-4抑制剂总体上不增加体重或轻度减轻体重,降低心血管事件的风险,有良好的安全性和耐受性,是2型糖尿病早期治疗的理想药物.     

DPP-4抑制剂联合阿卡波糖治疗2型糖尿病的疗效分析

目的探讨DPP-4抑制剂联合阿卡波糖治疗2型糖尿病的疗效。方法选取2015年3月至2017年3月我院收治的应用阿卡波糖降糖治疗血糖尚未达标的2型糖尿病患者64例为研究对象,在继续应用阿卡波糖的基础上加用DPP-4抑制剂降糖治疗。1个月后与加药前进行对比分析。结果加药后患者的糖化血红蛋白水平、空腹及餐后2 h血糖低于加药前。加药后,患者的NO高于加药前,ET-1低于加药前。结论 DPP-4抑制剂联合阿卡波糖治疗2型糖尿病的应用效果显著,症状和指标得到改善,提高了治疗效果,值得应用。     

DPP-4抑制剂对2型糖尿病依从性的影响

目前,2型糖尿病的发病率在世界范围内增长迅速,全世界约有2.46亿人患有2型糖尿病,我国2型糖尿病的总人数位居世界第一.然而对于血糖的良好持久控制并不乐观,尚存在诸多的困难.目前,治疗糖尿病的药物主要有胰岛素分泌促进剂(磺酰脲类、瑞格列奈)、胰岛素、胰岛素增敏剂(双胍类、噻唑烷二酮类)和α-葡萄糖苷酶抑制剂,但它们常具有不同程度的不良反应,如低血糖、体重增加、心血管不良反应等.     

DPP-4抑制剂对2型糖尿病患者血清GLP-1的影响

目的：观察GLP-1在2型糖尿病患者血清中的表达水平及DPP-4抑制剂干预后对T2DM患者的影响。方法：筛选60例2型糖尿病患者为实验组,30例健康者为正常对照组,均检测血清GLP-1水平,应用酶联免疫法（ELISA）测定实验组应用DPP-4干预治疗4周及12周后空腹及餐后血糖、胰岛素及GLP-1水平。结果：2型糖尿病患者血清GLP-1水平明显低于正常对照组。干预后血清空腹及餐后GLP-1水平升高（P〈0.01）。相关分析显示,GLP-1与INS具有相关性（P〈0.05）。结论：应用DPP-4干预治疗,可以使2型糖尿病患者血清GLP-1水平升高,是治疗早期糖尿病的新途径。     

DPP-4抑制剂治疗2型糖尿病的研究进展及临床应用

DPP-4抑制剂是治疗2型糖尿病的新型药物。较传统的降糖药物而言,DPP-4抑制剂对降低2型糖尿病患者的血糖有更好的疗效,可以降低低血糖的危险,安全性及耐受性良好。本文通过分析DPP-4抑制剂类药物,综述其化学性质、物理作用、临床研究和当前待解决的问题,对DPP-4抑制剂类药物的研究进展及临床应用疗效进行探究和展望。     

DPP-4抑制剂单药治疗和联合治疗方案及疗效分析

多种因素导致的胰岛素抵抗和胰岛细胞功能进行性减退是2型糖尿病的主要发病机制,其中胰岛细胞功能逐步衰竭在2型糖尿病的发生、发展过程中起着主导作用,因此,对2型糖尿病的治疗需要针对同时存在的多种病理生理缺陷。肠促胰素通过改善胰岛A和B细胞的敏感性,在葡萄糖稳态的调节中起重要作用。     

DPP-4抑制剂不能替代磺脲类药物

胰岛素促泌剂是治疗2型糖尿病的重要手段。近年来,为了得到疗效更好,更安全的胰岛素促泌剂,人们做了大量的研究。二肽基肽酶-4（DPP-4）抑制剂就是一种基于肠促胰素的新型降糖药,它不仅具有胰岛素促泌效应,还有减少低血糖、不增加体重、改善糖脂代谢、减少B细胞凋亡等优点,有人提出其可能取代磺脲类药物。下面就从机制、疗效、经济学、并发症等等方面将两类药物进行比较,以指导I临床应用。     

DPP-4的基因组学研究进展与DPP-4抑制剂的临床应用

二肽基肽酶IV(DPP-4)是一种分布广泛的膜相关性丝氨酸蛋白酶,能够影响糖代谢、脂质代谢、免疫调节、神经调节、信号转导、癌症发展等多种生理功能。随着全基因组关联研究(GWAS)的发展,DPP-4基因的基因多态性,主要是单核苷酸多态性已被证实影响血脂水平和mRNA表达,还影响心血管疾病的易感性,可能与DPP-4抑制剂在血脂紊乱和心血管疾病方面的疗效具有密切关系,这在2型糖尿病的治疗中具有重要意义。本文对国内外所有关于DPP-4基因多态性的研究进行综述,并在此基础上探讨其对DPP-4抑制剂在2型糖尿病治疗中的影响。     

The safety of DPP-4 inhibitor and SGLT2 inhibitor combination therapies

Introduction: Type 2 diabetes (T2D), a multifactorial and chronic disease, requires in an elevated percentage of patients the association of several antidiabetic drugs to achieve optimal glycemic control. Dipeptidyl peptidase-4 inhibitors (DPP-4i) and sodium–glucose cotransporter inhibitors (SGLT2i) are new classes of oral antidiabetic drugs developed over the last years.

Areas covered: This paper summarizes the safety of DPP-4i and SGLT2i combination therapies. Relevant studies were identified through searches in PubMed.

Expert opinion: DPP4i and SGLT2i are antidiabetic drugs that lower blood glucose without causing hypoglycaemia or weight increase. More importantly, cardiovascular trials have clearly demonstrated the cardiovascular safety of DPP4i and a reduction in cardiovascular events with SGLT2i (empagliflozin and canagliflozin). Therefore, the association of both therapeutic groups could be an attractive option to achieve optimal blood glucose control in T2D because of their complementary mechanism of action. Clinical trials evaluating the combination of SGLT2i and DPP4i show that the co-administration of these drugs in fixed-dose combinations in comparison to separate tablets does not carry additional safety concerns that each individual drug, but increases therapeutic effects. Therefore, this antidiabetic combination is a safe and effective therapy for patients with T2D.     

二肽基肽酶4抑制剂和钠-葡萄糖转运蛋白2抑制剂 联合治疗2型糖尿病的临床应用进展

DPP-4抑制剂与SGLT2抑制剂联合治疗,可以在减轻副作用的基础上更加有效地降低2型糖尿病患者的血糖,但是对于不同剂量的组合,仍需大量临床试验以评估其临床疗效和安全性,使临床医生根据T2DM病人的具体情况选择治疗药物的组合。     

奥格列汀:一种新的长效二肽基肽酶-4抑制剂

糖尿病是一种以高血糖为特征的代谢性疾病,目前常用的口服降糖药均需要每天服药,给患者带来不便。奥格列汀是一个小分子二肽基肽酶-4（DPP-4）抑制剂,由默克公司研发,主要用于二型糖尿病的治疗,且只需1周服用1次即可,从而提高了患者的顺应性和坚持性,最终提高了治疗效果。介绍了奥格列汀的合成方法、药理学、药物代谢动力学、临床研究等信息,为更好地应用临床与研发类似新药提供依据。     

市售DPP-4抑制剂类抗糖尿病药物的比较研究

DPP-4抑制剂是近年来上市的一类高效、高选择性抗2型糖尿病药物,通过检索文献,综述已上市的五种DPP-4抑制剂在结构、药代药动、选择性、药物相互作用、副作用等方面的差异.     

Clinical Effects of Exposure to DPP-4 Inhibitors as Reported to the National Poison Data System

DPP-4 inhibitors (sitagliptin, saxagliptin, and linagliptin) are approved for the treatment of diabetes. They are considered safe due to their hyperglycemia dependent mechanism of action. We examined all isolated exposures to DPP-4 inhibitors reported to the National Poison Database System since 2006 to determine if significant toxicity occurs after exposure with attention to pediatric and intentional overdoses. NPDS data regarding DPP-4 ingestions in all age groups between January 2006 and March 2013 was collected. Cases were reviewed, and the following inclusion criteria applied: (1) reported ingestion of a DPP-4 inhibitor and (2) known clinical outcome. Exclusion criteria included the following: (1) exposure to more than a single substance, (2) no known outcome, and (3) clinical outcome judged to be unrelated to the exposure. One thousand four hundred seventy-six cases were reviewed while 826 were excluded. Of 650 included cases, 562 developed no clinical effects. Mild effects were noted in 77. There were no deaths. Moderate/major effect cases were investigated: two medication-naive nondiabetic individuals with accidental exposures developed clinically significant hypoglycemia requiring treatment. One diabetic patient on a DPP-4 inhibitor developed prolonged hypoglycemia requiring admission and continuous exogenous dextrose. Of 650 included exposures to DPP-4 inhibitors, 639 (98.3%) had either no or minor clinical effects. Three resulted in clinically significant hypoglycemia requiring intervention. None of the moderate or major clinical outcomes were the result of intentional overdoses for the purpose of self-injury. No exploratory ingestions resulted in moderate or major effects. Based on this data, exposure to DPP-4 inhibitors may rarely result in clinically significant hypoglycemia.     

二肽基肽酶-4(DPP-4)抑制剂西格列汀在2型糖尿病治疗中的作用

目的:介绍新型口服降糖药二肽基肽酶-4(DPP-4)抑制剂西格列汀及其最新研究进展。方法 :对西格列汀的药理作用、药代动力学、不良反应及药物相互作用等方面的临床研究进行论述。结果和结论 :西格列汀是一种安全、有效的新型口服降糖药,具有良好的临床应用前景。     

An update on the safety and efficacy of oral antidiabetic drugs: DPP-4 inhibitors and SGLT-2 inhibitors

Introduction: Oral antidiabetic medications are important in many type 2 diabetes care plans

Areas covered: The article summarizes the cardiovascular and renal safety data for DPP-4 inhibitors and SGLT-2 inhibitors and specific safety data particular to each class.

Expert opinion: DPP-4 and SGLT-2 inhibitors provide unique anti-hyperglycemic mechanisms. The cardiovascular safety profiles of DPP-4 inhibitors are promising, but do not show the strong CV risk reduction of empagliflozin and canagliflozin. The heart failure signal associated with DPP-4 inhibitor use is unclear with differing agents, demonstrating increased risk or maybe even protective effects. The risk reduction in cardiovascular disease associated with SGLT-2 inhibitors has translated to recommendations to consider these therapies early in the treatment pathway. Both classes have potential safety concerns that necessitate appropriate patient selection and thorough education on potential side-effects. DPP-4 inhibitors are considered to have neutral or in some studies beneficial renoprotective effects. SGLT-2 inhibitor safety effects on the kidney are more complex. There are reports of acute kidney injury occurring soon after initiating SGLT-2 inhibitor therapy. However, there are large recent studies that have demonstrated the beneficial effect of SGLT-2 inhibitors in slowing the progression of established chronic kidney disease.     

Discovery of Imigliptin,a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes

相似文献   

Inhibition of DPP-4: a new therapeutic approach for the treatment of type 2 diabetes

ABSTRACT

Background: Glucagon-like peptide-1 (GLP?1) and glucose-dependent insulinotropic polypeptide (GIP) are hormones secreted by the enteroendocrine cells of the gut in response to the ingestion of nutrients. These incretin hormones, so called because they increase insulin secretion, are key modulators of pancreatic islet hormone secretion and, thus, glucose homeostasis. The glucoregulatory effects of incretins are the basis for new therapies currently being developed for the treatment of type 2 diabetes mellitus (T2DM). Drugs that inhibit dipeptidyl peptidase-4 (DPP?4), a ubiquitous enzyme that rapidly inactivates both GLP-1 and GIP, increase active levels of these hormones and, in doing so, improve islet function and glycemic control in T2DM.

Scope: In this review, we briefly describe (1) the role of pancreatic islet dysfunction in the onset and progression of T2DM, (2) the rationale for developing drugs that enhance incretin activity, (3) the evidence that inhibition of DPP?4 is effective in ameliorating islet dysfunction and improving glycemic control in T2DM, (4) the efficacy, safety, and tolerability of DPP?4 inhibitors as monotherapy and in combination with other antidiabetic agents, and (5) the potential utility of DPP?4 inhibitors relative to existing oral antidiabetic agents and newer antidiabetic drugs in the pipeline. The review is based upon MEDLINE literature searches (1966–August 2006) and abstracts and presentations from the American Diabetes Association Scientific Sessions (2002–2006) and the European Association for the Study of Diabetes Annual Meetings (1998–2006). Basic science, preclinical, and clinical studies and review articles published in the English language were evaluated and selected based upon consideration of their originality, relevance, and frequency of citation.

Findings: DPP?4 inhibitors are a new class of antidiabetogenic drugs that provide comparable efficacy to current treatments. They are effective as monotherapy in patients inadequately controlled with diet and exercise and as add-on therapy in combination with metformin, thiazolidinediones, and insulin. The DPP?4 inhibitors are well tolerated, carry a low risk of producing hypoglycemia, and are weight-neutral. The long-term durability of effect on glycemic control and β?cell morphology and function remain to be established.

Conclusions: Islet cell dysfunction is central to the pathogenesis of T2DM. Incretin-based therapies, including GLP-1 analogues and DPP?4 inhibitors, have been shown to restore glucose homeostasis and improve glycemic control. The DPP?4 inhibitors, which can be used as monotherapy or in combination with other antidiabetic drugs, are a promising new treatment option, especially for patients with early-stage T2DM and more severe hyperglycemia.