Repaglinide

Repaglinide is a class of orally active antidiabetic drugs, the meglitinides:

• meglitinides are non-sulphonylurea beta-cell stimulators for the treatment of patients with type 2 diabetes - work by closing ATP-dependent potassium channels in the beta cell membrane
• aim is to improve post-prandial insulin profiles - therefore can only be taken before meals and cannot be taken if meals are omitted
• it has a licence for use as combination with metformin in patients with type 2 diabetes who are inadequately controlled by maximally tolerated doses of metformin alone; repaglinide is also licensed for use as a monotherapy in type 2 diabetes
  • it is a derivative of carbamoylmethyl benzoic acid
  • its oral bioavailability is about 63% - plasma concentrations peak within 1 hour of administration
  • following an oral dose the insulinotropic response to a meal occurs within 30 minutes and insulin concentrations return to fasting levels within 4-6 hours
  • metabolised mainly by the liver - elimination half-life about 1 hour
  • unwanted effects are rare (less than 1 in 1,000 patients) and include hypoglycaemia, constipation, abdominal pain, diarrhoea, nausea, vomiting, visual disturbances, hypersensitivity reactions such as rashes and itching, and transient, mild elevations in liver enzymes that rarely lead to discontinuation of therapy

The summary of product characteristics must be consulted before prescribing this drug.

Note - nateglinide (sold under the brand name Starlix) was permanently discontinued and withdrawn from the UK market in August 2020.

Reference

1. Prioletta A et al. The role of nateglinide and repaglinide, derivatives of meglitinide, in the treatment of type 2 diabetes mellitus. Arch Med Sci. 2013 Apr 30;9(5):936–943