Clinical pharmacokinetics and pharmacodynamics of repaglinide.
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.
Hatorp
Vibeke
V
Danish Toxicology Center, Kogle Alle 2, DK-2870 Hoersholm, Denmark. vh@dtc.dk
D000328:Adult; D000368:Aged; D001786:Blood Glucose / Q000032:analysis; D002219:Carbamates / Q000493:pharmacokinetics* / Q000494:pharmacology*; D002986:Clinical Trials as Topic; D003924:Diabetes Mellitus, Type 2 / Q000150:complications / Q000188:drug therapy / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D005260:Female; D006801:Humans; D007004:Hypoglycemic Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D008107:Liver Diseases / Q000150:complications / Q000378:metabolism; D008297:Male; D010880:Piperidines / Q000493:pharmacokinetics* / Q000494:pharmacology*; D051437:Renal Insufficiency / Q000209:etiology / Q000378:metabolism; D012293:Rifampin / Q000627:therapeutic use
D001786:Blood Glucose; D002219:Carbamates; D007004:Hypoglycemic Agents; D010880:Piperidines; C072379:repaglinide; D012293:Rifampin