[Glimepiride (Amaryl): a review of its pharmacological and clinical profile].

Abstract

In Type 2 diabetes, it is considered that the lowered insulin secretion and the lowered insulin sensitivity cause hyperglycemia. Sulfonylureas have strong blood-glucose lowering effect by stimulating insulin secretion and have been widely used in the treatment of Type 2 diabetes. However, the use of sulfonylurea has several problematic issues (weight gain, hypoglycemia, second failure and so on), which would due to stimulation of strong insulin secretion. Glimepiride, a new sulfonylurea, has a blood-glucose lowering effect as strong as those of existing sulfonylureas, but only induces mild insulin secretion. The sulfonylurea receptor has a weaker affinity for glimepiride than glibenclamide. The association and dissociation to the sulfonylurea receptor of glimepiride are faster than those of glibenclamide. Additionally, it is confirmed by basic studies that part of the glimepiride effect is attributable to improving insulin sensitivity. Glimepiride has already been used in more than 60 countries in the world. Outside of Japan, several clinical studies have demonstrated that glimepiride shows less hypoglycemia and no weight gain. Glimepiride is expected to be a new efficient agent for the treatment of Type 2 diabetes.

• Authors: K Bando, Y Yamada
• Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica (Nihon Yakurigaku Zasshi) Vol. 118 Issue 1 Pg. 59-67 (Jul 2001) ISSN: 0015-5691 [Print] Japan
• PMID: 11496829 (Publication Type: Journal Article, Review)

Chemical References

• Hypoglycemic Agents
• Insulin
• Sulfonylurea Compounds
• glimepiride

Topics

• Animals
• Clinical Trials as Topic
• Diabetes Mellitus, Type 2 (drug therapy)
• Humans
• Hypoglycemic Agents (pharmacology, therapeutic use)
• Insulin (metabolism)
• Insulin Secretion
• Stimulation, Chemical
• Sulfonylurea Compounds (pharmacology, therapeutic use)