repaglinide (Prandin)

Introduction

Tradename: Prandin.

Dosage

• 1-2 mg QAC
• start: 0.5 mg QAC for patients with Hgb A1c < 8% not previously on an oral hypoglycemic agent
• dose increase at 4 weeks if indicated

Tabs: 1 & 2 mg

Pharmacokinetics

• metabolized in the liver by cyt P450 3A4

elimination via liver

1/2life = 1 hours

protein binding = 98 %

Adverse effects

• hypoglycemia due to enhanced release of insulin
• increased risk of frailty

• drug adverse effects of hypoglycemic agents

Drug interactions

• any drug that inhibits cyt P450 3A4 may increase levels of repaglinide
• any drug that induces cyt P450 3A4 may diminish levels of repaglinide

• drug interaction(s) of gemfibrozil with repaglinide
• drug interaction(s) of fluoroquinolones with hypoglycemic agents

Laboratory

• repaglinide in serum/plasma
• repaglinide in urine

Mechanism of action

• stimulates closure of ATP-sensitive K+ channels on pancreatic beta cells
• this results in depolarization & opening of Ca+2 channels
• this promotes movement of insulin secretory granules to the cell membrane with enhanced release of insulin

More general terms

• meglitinide (Meglitinido, Meglitinidum)

Additional terms

• cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
• lipoma; adipocyte neoplasm

Component of

• metformin/repaglinide (PrandiMet)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=65981
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4547