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Sitagliptin

内分泌

关键词内分泌 治疗药物 内分泌

词汇介绍

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解析

Sitagliptin  

释    义   西格列汀(糖尿病类治疗药物名称)

例    句   Conclusion The sitagliptin can improve the insulin resistance situation in type 2 diabetes patients. 结论西格列汀可改善2型糖尿病患者胰岛素抵抗水平。

概述

西格列汀是一种口服药物,可降低2型糖尿病患者的血糖水平。西格列汀被认为是除饮食和运动降糖以外的辅助手段。西格列汀不宜用于1型糖尿病患者或用于治疗糖尿病酮症酸中毒,因为在这些情况下无效。西格列汀尚未在有胰腺炎史的患者中研究,尚不清楚有胰腺炎病史的患者在使用西格列汀时是否有增加罹患胰腺炎的风险。不良反应①上市后已有急性胰腺炎的报道,包括致命性和非致命性出血性或坏死性胰腺炎。如果怀疑是胰腺炎,请立即停用西格列汀。②上市后有急性肾功能衰竭的报告,对于中度或重度肾功能不全的患者以及ESRD患者,建议调

Sitagliptin decreases visceral fat and blood glucoses in women with polycystic ovarian syndrome 复制标题

西格列汀降低多囊卵巢综合征女性内脏脂肪和血液葡萄糖

发表时间:2019-09-15

影响因子:5.6

作者: Jessica K Devin

期刊:J Clin Endocrinol Metab

Growth hormone (GH) is secreted in a pulsatile fashion from the pituitary gland and exerts its effects either directly, via activation of the GH receptor, or indirectly, through hepatic insulin-like growth factor-1 (IGF-1). In adults, GH has important effects on the vasculature and body composition. GH increases endothelium-dependent vasodilator function and reduces inflammation. We have previously shown that patients with low GH have impaired conduit artery vasodilator function along with decreased tissue-type plasminogen activator (tPA) activity and a defective fibrinolytic response to venous occlusion. Others have corroborated these findings and further demonstrated that these vascular indices improve with GH replacement therapy. GH also has anabolic and lipolytic effects. Conversely, GH secretion is reduced in obesity and particularly in individuals with visceral adiposity. Women with increased visceral adipose tissue (VAT) demonstrate a four-fold reduction in mean GH levels as compared to those without. Normalization of GH secretion in patients with diminished GH affords one potential mechanism to address simultaneously both VAT and cardiovascular risk. Unfortunately, therapy with recombinant GH does not restore pulsatile secretion, is not subject to physiologic negative feedback by IGF-1, and is limited by hyperglycemia. We propose that an alternative strategy to enhance endogenous GH secretion in humans is to inhibit the degradation of endogenous GH releasing hormone (GHRH) by the dipeptidyl peptidase-4 (DPP4) enzyme. GHRH is the primary stimulus for pituitary GH secretion and determines GH pulsatility. Endogenous GHRH has a half-life of six minutes as it is degraded and inactivated by DPP4. Sitagliptin was the first oral DPP4 inhibitor approved by the US Food and Drug Administration for the management of hyperglycemia in patients with type 2 diabetes mellitus. Sitagliptin improves post-prandial hyperglycemia in a glucose-dependent manner by decreasing the degradation of the incretin hormone, glucagon-like peptide-1 (GLP1), and can therefore be safely given to patients without diabetes mellitus. We recently found that acute DPP4 inhibition with sitagliptin enhances stimulated GH secretion and free IGF-1 levels in healthy, lean women. Moreover, while vasodilation and tPA activity levels increased in both men and women during stimulated GH secretion, women demonstrated an enhanced vascular response to increased GH. The effect of chronic DPP4 inhibition on pulsatile GH secretion in individuals with low GH levels has not been studied.

译文

垂体腺以脉冲方式分泌生长激素(GH),并通过激活GH受体直接发挥作用,或通过肝胰岛素样生长因子1(IGF-1)间接发挥作用。在成年人中,生长激素对血管和身体组成有重要影响。 GH可增加内皮依赖性血管舒张功能并减少炎症。先前我们已经发现,低GH患者的导管动脉血管舒张功能受损,组织型纤溶酶原激活剂(tPA)活性降低,对静脉阻塞的纤溶反应不良。其他人证实了这些发现,并进一步证明GH替代疗法可改善这些血管指数。 GH还具有合成代谢和脂肪分解作用。相反,肥胖者尤其是内脏肥胖者的GH分泌减少。内脏脂肪组织(VAT)增加的女性与没有的女性相比,平均GH水平降低了四倍。 GH减少的患者中GH分泌的正常化提供了一种同时解决增值税和心血管疾病风险的潜在机制。不幸的是,用重组GH治疗不能恢复搏动性分泌,不受IGF-1的生理负反馈作用,并且受高血糖症的限制。我们建议,增强人类内源性GH分泌的另一种策略是通过二肽基肽酶4(DPP4)酶抑制内源性GH释放激素(GHRH)的降解。 GHRH是垂体GH分泌的主要刺激因素,它决定了GH的搏动性。内源性GHRH被DPP4降解并失活时,其半衰期为6分钟。西他列汀是美国食品和药物管理局批准的第一种口服DPP4抑制剂,用于治疗2型糖尿病患者的高血糖症。西他列汀通过减少肠降血糖素激素,胰高血糖素样肽1(GLP1)的降解,以葡萄糖依赖的方式改善餐后高血糖,因此可以安全地用于没有糖尿病的患者。我们最近发现,西他列汀对DPP4的急性抑制作用可增强健康,瘦弱妇女的刺激性GH分泌和游离IGF-1水平。此外,尽管在刺激的GH分泌过程中,男性和女性的血管舒张和tPA活性水平均升高,但女性对GH升高的血管反应增强。尚未研究慢性DPP4抑制对低GH水平个体的搏动性GH分泌的影响。