Metiglinide Analogues

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Information about Metiglinide Analogues

Metiglinide analogues are insulin secretagogues that are structurally unrelated to the sulfonylureas, but share a similar mechanism of action. These compounds are named for the initial, prototype molecule, metiglinide, found to have a sulfonylurea-like effect in stimulating the pancreatic beta cell to secret insulin. Metiglinides have been found to improve postprandial hyperglycemia in diabetic patients and to improve glycemic control and hemoglobin A1c levels.

FDA approval information for Metiglinide Analogues

Two metiglinides have been approved for use in the United States: repaglinide in 1997 and nateglinide in 2000. Both are now available generically as well as under the initial brand names of Prandin and Starlix. These agents are generally used in combination with other oral hypoglycemic agents and, because they rely upon stimulation of beta cells, are useful only in type 2 diabetes. Repaglinide and nateglinide are generally well tolerated.

Side effects of Metiglinide Analogues

Common side effects include diarrhea, nausea, dizziness, headache, malaise and hypoglycemia.

Liver safety of Metiglinide Analogues

  • Repaglinide has been implicated in several instances of clinically apparent liver injury which have been reported in the literature.
  • Nateglinide has been available for a shorter period of time and, while not the subject of published cases, is said to have been linked to cases of hepatitis and jaundice in the product label.


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