Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Review on New Drug
Glimepiride (Amaryl®): a review of its pharmacological and clinical profile
Katsuhiro BANDOYoshikazu YAMADA
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2001 Volume 118 Issue 1 Pages 59-67

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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.
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© 2001 by The Japanese Pharmacological Society
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