在慢性缺血性心肌中对卡纳格利弗洛辛和西塔格利普丁的比较效果
Sharif A Sabe1, Dwight D Harris1, Mark Broadwin1
1Division of Cardiothoracic Surgery, Department of Surgery, Cardiovascular Research Center, Rhode Island Hospital, Alpert Medical School of Brown University, Rhode Island Hospital, Providence, RI 02905, USA.
Vessel plus
|August 23, 2024
概括
在慢性缺血病模型中,像canagliflozin这样的-葡萄糖共运输体2抑制剂 (SGLT2i) 改善了心脏功能,而不是像sitagliptin这样的二基酸酶-4抑制剂 (DPP4i). 两种药物类别都对心脏输液产生了类似的影响.
科学领域:
- 心脏病学 心脏病学
- 药理学 药理学是指药理学的学科.
- 缺血性心脏病是一种心脏病.
背景情况:
- -葡萄糖共运输体2抑制剂 (SGLT2i) 和二乙酶-4抑制剂 (DPP4i) 是抗糖尿病药物,具有已证明的心脏保护作用.
- 在改善心脏健康方面,SGLT2i和DPP4i的精确机制和相对有效性,特别是在心肌缺血的情况下,需要进一步阐明.
研究的目的:
- 为了比较SGLT2i (canagliflozin) 和DPP4i (sitagliptin) 对心脏功能,心肌 perfusion 和微血管密度的影响.
- 调查包括蛋白质表达和酶激活在内的潜在分子机制,与这些抗糖尿病药物的心脏保护作用相关,在慢性心肌缺血的猪模型中.
主要方法:
- 慢性心肌缺血症在约克郡猪中被诱导,使用的是阿梅洛伊德收缩剂.
- 动物被用载体 (CON),卡纳格里夫洛辛 (CANA) 或西塔格利普丁 (SIT) 治疗了五周.
- 评估心脏功能,输液,微血管密度和蛋白质表达,使用压力体积导管,微球分析,免疫光和免疫阻塞.
主要成果:
- 与西塔格利普丁 (SIT) 相比,卡纳格利弗洛辛 (CANA) 的使用导致中风容量和心脏输出改善,左心室硬度下降的趋势.
- 与对照组相比,CANA和SIT都显示了心肌输液改善的趋势,两种药物治疗之间没有显著差异.
- 西塔格利普丁 (SIT) 与毛细血管和动脉密度的增强有关,而这两种药物都增加了血管内皮卡德林的表达. 此外,SIT还显示AMPK和eNOS的激活发生变化.
结论:
- 在慢性心肌缺血中,卡纳格利弗洛辛在心脏功能方面表现出优异的改善,与西塔格利普丁相比.
- 尽管在微血管化方面存在差异,但SGLT2i和DPP4i在这个模型中对心肌输液具有相似的影响.
- 这些发现突出了SGLT2i和DPP4i在慢性缺血期间对心脏的不同功能和结构影响.
相关概念视频
01:23Dipeptidyl Peptidase 4 Inhibitors
179
Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
179
01:26Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
405
The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
405
01:26Heart Failure Drugs: Inotropic Agents
545
Positive inotropic agents are commonly used as the first line of treatment for heart failure. One such agent is digoxin, derived from the genus Digitalis, which has been known for centuries but effectively utilized since 1785. However, these cardiac glycosides can have potentially toxic effects due to their mechanism of action, which involves inhibiting Na+/K+-ATPase and increasing contractility. Digoxin is absorbed orally and distributed in various tissues, including the CNS. It has a long...
545
01:25Antianginal Drugs: Calcium Channel Blockers and Ranolazine
464
Angina pectoris, a primary symptom of ischemic heart disease, requires careful pharmacological interventions. In this context, calcium channel blockers (CCBs) and ranolazine have emerged as crucial pharmacotherapeutic agents, providing deep insights into the complexities of angina management.
CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...
CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...
464