Drug intelligence / Profile preview

glimepiride + metformin + rosiglitazone

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of glimepiride, metformin, and rosiglitazone is a triple antidiabetic medication used primarily for the management of type 2 diabetes mellitus. This combination brings together three different mechanisms of action to provide better glycemic control when single or dual therapy is not effective. ## Composition and Mechanism This medication combines three distinct antidiabetic agents: 1. **Glimepiride** - A third-generation sulfonylurea that stimulates insulin secretion from pancreatic beta cells. It has high selectivity toward pancreatic ATP-sensitive potassium channels and shows various extrapancreatic effects in muscle and fat cells[3][8]. 2. **Metformin** - A biguanide that improves insulin resistance by lowering glucose production in the liver, delaying glucose absorption from the intestines, and increasing the body's sensitivity to insulin[8]. 3. **Rosiglitazone** - A thiazolidinedione that further increases insulin sensitivity in peripheral tissues[8]. ## Brand Names The combination is marketed under brand names including: - Adride RM (by Strides Shasun Ltd) - Roglim (by Wockhardt Ltd) - Rosinorm GM (by Micro Labs Ltd)[8] ## Side Effects Common side effects of this triple combination include: - Hypoglycemia (low blood glucose level) - Gastrointestinal issues (nausea, diarrhea, stomach pain) - Taste changes - Headache - Edema (swelling) - Weight gain - Blurred vision - Bone fracture (particularly in postmenopausal women with rosiglitazone) - Respiratory tract infections[6][8] More serious but less common side effects may include cardiovascular events. Historical data showed that rosiglitazone was associated with increased cardiovascular risk, particularly when used in combination with insulin or metformin[7]. ## Usage Guidelines - The medication should be taken with food to reduce gastrointestinal side effects[8]. - Patients should always carry sugary food or fruit juice to manage potential hypoglycemic episodes[8]. - Regular liver function monitoring is recommended as rosiglitazone may affect liver function[8]. - The combination is typically prescribed when dual therapy with metformin and either glimepiride or rosiglitazone fails to achieve adequate glycemic control[3][10]. ## Clinical Evidence Studies have shown that adding rosiglitazone to a combination of glimepiride and metformin therapy in patients with insufficiently controlled type 2 diabetes can significantly reduce HbA1c levels and fasting plasma glucose. In one 26-week study, mean HbA1c levels decreased from 7.54% to 6.57%, and fasting plasma glucose levels fell from 169 mg/dL to 136 mg/dL[10]. This triple combination therapy represents an effective approach for patients who have not achieved target glycemic levels with dual therapy, though careful monitoring for side effects is essential.

Brand names
Adride RMRoglimRosinorm GM
02

Targets

SUR1 (Sulfonylurea receptor 1)AMPK (Adenosine monophosphate–activated protein kinase)PPARG (Peroxisome proliferator-activated receptor gamma)

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