Cardiovascular effects of sitagliptin – An anti‐diabetes medicine

Abstract

Dipeptidyl-peptidase-4 (DPP-4) inhibitors, as the most recent available anti-diabetic agents, were generally used in clinical treatment of type 2 diabetes (T2DM). In addition to anti-diabetic effects, the five most widely used DPP-4 inhibitors (sitagliptin, vildagliptin, saxagliptin, linagliptin and alogliptin) also exert cardiovascular protective effects. In recent years, increasing studies suggest that sitagliptin shows pleiotropic impacts towards the cardiovascular system either with or without diabetes. In this review, we summarized the recent reports to provide an update discussion about cardiovascular protective effects of sitagliptin and the corresponding mechanisms. Sitagliptin has positive effects towards ischaemic cardiovascular diseases, atherosclerosis and hypertension. These effects are mainly conducted through DPP-4 inhibitions. In addition, sitagliptin exerts anti-inflammation, anti-oxidative stress, anti-apoptosis, mediation on lipid accumulation and so on, which also contribute to its cardiovascular effects.

Sitagliptin promotes mitochondrial biogenesis in human SH‐SY5Y cells by increasing the expression of PGC‐1α/NRF1/TFAM

“…Sitagliptin, an important member of the dipeptidyl-peptidase-4 (DPP-4) inhibitor family, has been recently licensed for the treatment of type 2 diabetes (T2DM) for exerting antihyperglycemia actions via upregulation of glucagon-like peptide 1 (GLP-1). 7 Interestingly, T2DM-associated insulin resistance plays an important role in contributing to neurological disorders including AD and Parkinson's disease. 8 The protective effects of DPP-4 inhibitors against neuronal degeneration have been reported in previous studies as well.…”

Melatonin postconditioning combined with sitagliptin exerts full cardioprotection in diabetic hearts of aged rats through an AMPK-dependent mechanism

“…Sitagliptin works by inhibiting DPP-4 and thereby increasing the hormone glucagon-like peptide-1 (GLP-1) activity in cells, thus having diverse activities to reduce insulin resistance, regulate intracellular energy homeostasis and ion channel function, boost mitochondrial function and improve the lipid profile [33]. These actions may contribute to the cardioprotective advantage of sitagliptin in combination therapy in aged diabetic rats.…”

Clinical Pharmacology of Dipeptidyl Peptidase 4 Inhibitors: Comparative Review

“…В метаанализе 11 клинических исследований ситаглиптина в режиме моноили комбинированной терапии (n = 2338) у пациентов с СД 2 типа выявлено снижение концентрации триглицеридов плазмы крови на 0,24 ммоль/л (95% ДИ 0,09-0,40; p = 0,002) и повышение уровня холестерина липопротеинов высокой плотности на 0,05 ммоль/л (95% ДИ 0,02-0,07; p < 0,001) по сравнению с контролем (плацебо или другими сахароснижающими средствами -метформином, тиазолидиндионами, инсулином) [72]. Более подробно протективные эффекты ингибиторов ДПП-4 в отношении сердечно-сосудистой патологии обобщены в специальных обзорах [73][74][75]. Обсуждаются также нефропротективные свойства ингибиторов ДПП-4 у больных СД 2 типа.…”