Effect of Glimepiride on Metabolic – Cardiovascular Risk Factors in Patients with T2DM

Effect of Glimepiride on Metabolic – Cardiovascular Risk Factors in Patients with T2DM (The Roles of Amaryl-M®, the Rationale FDC of Glimipiride and Metformin) at Symposium Hyperglikemia of Patients with Diabetes Mellitus in Clinical Practice Medan, 28 November 2010

Askandar Tjokroprawiro
Surabaya Diabetes and Nutrition Center – Dr. Soetomo Teaching Hospital
Faculty of Medicine Airlangga University, Surabaya

Summary

Patients with type-2 diabetes mellitus (T2DM) are prone to metabolic cardiovascular complication, which can occur earlier and more earlier anf more frequently as compared to nondiabetic patients.

Glimipiride is a novel 3rd generation of Sulfonylurea which has been widely reported having 7 (seven) MECAR (metabolic cardiovascular) properties, such as : optimal glycemic control, cardioprotective and insulin sparing effects, 3B-3A-9D specific, glycogenic effect, antiplatelet effect, and adiponectin-raiser. The 3B-3A-9D effects of glimipiride means, that this OAD has 3 fold higher rete Binding (3B) to receptor (that means more rapid action), a 3 fold weaker Affinity (3A) to receptor (means rare hypoglycemic episode), and a 9 fold rate of Dissociation (9D) from its receptor (means rare episode of hypoglycemia). It had been proven that glimipiride remarkably improve insulin resistense by increasing plasma adiponectin and decreasing plasma TNFα . Most recently in 2010, glimipiride can rapidly and stably improve glycemic control (FPG, PPG, and A1C), lipoprotein metabolism, and cardiovascular risk factors (TC, TG, LDL-C, HDL-C, HOMA-R, t-PA, and PAI-I), hence glimipiride can significantly alleviates insulin resistence and enhance fibrinolytic activity.

Recent study demonstrated that after 8 week treatment with glimipiride (Amaryl-M®) on insulin resistant elderly patient with T2DM resulted in a significant increase in plasma adiponectin. Glimipiride – induced adiponectinemia may increase insulin sensitivity and preserve β-cell function of pancreas.

Metformin is unique in being more than an oral antihyperglicemic agent and having clinical properties to improves clinical outcomes in prediabetic individuals, patients with estabilished T2DM, and potentially also having metabolic cardio-and cancer protective properties.

Due to the pleiotropic properties of metformin, this antidiabetic agent has such a “broad spectrum” mechanism for improving the function of the endocrine (insulin resistance, etc) and reducing risk of cardiovascular disease. Hence therapeutic profile of metformin identifies this drug as the treatmen of choice for diabetes prevention of cardiovascular complication in patient with T2DM.

As reported in “the Metformin the Gold Standart. A Scientific Hand Book” in the memorial publication of 50 years of metformin, for future indication, metformin has potential therapeutic value for the treatment of neoplastic disease (cancer suppressor or cancer protector).

Recently, metformin has triple properties (MCC), that means, in the past: Metabolic effect (M), and at present: Metabolic-Cardiovascular effect (C), and in future: Metabolic – Cardiovascular, and Cancer protective effects (C).

Recent study with glimipiride / metformin demonstrated being more efficacious than other sulfonylurea / metformin combination at reaching the glycemic control goals with less hypoglycemic events in patients with uncontrolled T2DM.