Clinical pharmacokinetics and pharmacodynamics of repaglinide

Clin Pharmacokinet. 2002;41(7):471-83. doi: 10.2165/00003088-200241070-00002.


Repaglinide is a novel, fast-acting prandial oral hypoglycaemic agent developed for the treatment of patients with type 2 diabetes whose disease cannot be controlled by diet and exercise alone. Although repaglinide binds to the sulphonylurea binding sites on pancreatic beta-cells and has a similar mechanism of action, repaglinide exhibits distinct pharmacological properties compared with these agents. Following administration, repaglinide is absorbed rapidly and has a fast onset of dose-dependent blood-glucose lowering effect. The drug is eliminated rapidly via the biliary route, without accumulation in the plasma after multiple doses. Repaglinide is well tolerated in patients with type 2 diabetes, including elderly patients and patients with hepatic or renal impairment. The pharmacokinetic profile of repaglinide and the improvements in post-prandial hyperglycaemia and overall glycaemic control make repaglinide suitable for administration preprandially, with the opportunity for flexible meal arrangements, including skipped meals, without the risk of hypoglycaemia.

Publication types

  • Review

MeSH terms

  • Adult
  • Aged
  • Blood Glucose / analysis
  • Carbamates / pharmacokinetics*
  • Carbamates / pharmacology*
  • Clinical Trials as Topic
  • Diabetes Mellitus, Type 2 / complications
  • Diabetes Mellitus, Type 2 / drug therapy
  • Diabetes Mellitus, Type 2 / metabolism
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Female
  • Humans
  • Hypoglycemic Agents / pharmacokinetics*
  • Hypoglycemic Agents / pharmacology*
  • Liver Diseases / complications
  • Liver Diseases / metabolism
  • Male
  • Piperidines / pharmacokinetics*
  • Piperidines / pharmacology*
  • Renal Insufficiency / etiology
  • Renal Insufficiency / metabolism
  • Rifampin / therapeutic use


  • Blood Glucose
  • Carbamates
  • Hypoglycemic Agents
  • Piperidines
  • repaglinide
  • Rifampin