Dutta D, Kalra S, Sharma M
Department of Endocrinology, Post-graduate Institute of Medical Education and Research and Dr. Ram Manohar Lohia Hospital, New Delhi, India.
Department of Endocrinology, Bharti Hospital and BRIDE, Karnal, Haryana, India.
J Postgrad Med. 2017 Apr-Jun;63(2):114-121. doi: 10.4103/0022-3859.191007.
The current classification of both diabetes and antidiabetes medication is complex, preventing a treating physician from choosing the most appropriate treatment for an individual patient, sometimes resulting in patient-drug mismatch. We propose a novel, simple systematic classification of drugs, based on their effect on adenosine monophosphate-activated protein kinase (AMPK). AMPK is the master regular of energy metabolism, an energy sensor, activated when cellular energy levels are low, resulting in activation of catabolic process, and inactivation of anabolic process, having a beneficial effect on glycemia in diabetes. This listing of drugs makes it easier for students and practitioners to analyze drug profiles and match them with patient requirements. It also facilitates choice of rational combinations, with complementary modes of action. Drugs are classified as stimulators, inhibitors, mixed action, possible action, and no action on AMPK activity. Metformin and glitazones are pure stimulators of AMPK. Incretin-based therapies have a mixed action on AMPK. Sulfonylureas either inhibit AMPK or have no effect on AMPK. Glycemic efficacy of alpha-glucosidase inhibitors, sodium glucose co-transporter-2 inhibitor, colesevelam, and bromocriptine may also involve AMPK activation, which warrants further evaluation. Berberine, salicylates, and resveratrol are newer promising agents in the management of diabetes, having well-documented evidence of AMPK stimulation medicated glycemic efficacy. Hence, AMPK-based classification of antidiabetes medications provides a holistic unifying understanding of pharmacotherapy in diabetes. This classification is flexible with a scope for inclusion of promising agents of future.
目前糖尿病和抗糖尿病药物的分类都很复杂，这使得治疗医生难以针对个体患者选择最合适的治疗方法，有时会导致患者与药物不匹配的情况。我们提出了一种基于药物对腺苷单磷酸激活蛋白激酶（AMPK）作用的新颖、简单的系统分类方法。AMPK是能量代谢的主要调节因子，是一种能量传感器，在细胞能量水平较低时被激活，从而导致分解代谢过程的激活和合成代谢过程的失活，对糖尿病患者的血糖水平有有益影响。这种药物分类方法使学生和从业者更容易分析药物概况并使其与患者需求相匹配。它还有助于选择具有互补作用模式的合理药物组合。药物被分类为AMPK活性的刺激剂、抑制剂、混合作用、可能作用和无作用。二甲双胍和格列酮类药物是AMPK的纯刺激剂。基于肠促胰素的疗法对AMPK有混合作用。磺脲类药物要么抑制AMPK，要么对AMPK无影响。α-葡萄糖苷酶抑制剂、钠-葡萄糖协同转运蛋白2抑制剂、考来维仑和溴隐亭的降糖疗效可能也涉及AMPK激活，这值得进一步评估。黄连素、水杨酸盐和白藜芦醇是糖尿病管理中有前景的新型药物，有充分的证据证明其通过刺激AMPK发挥降糖疗效。因此，基于AMPK的抗糖尿病药物分类为糖尿病药物治疗提供了全面统一的认识。这种分类具有灵活性，有纳入未来有前景药物成分的空间。
