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Repaglinide

PRANDIN

What it isMeglitinide closing the beta-cell KATP channel; postprandial hyperglycemia in type 2 diabetes.

Why this oneMeal-linked dosing can be omitted with a skipped meal, reducing prolonged hypoglycemia compared with sulfonylureas.

What limits itFrequent meal-time dosing burdens adherence. Gemfibrozil is contraindicated because CYP2C8 inhibition can cause severe hypoglycemia.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Type 2 diabetesAdults, HbA1c <8%0.5 mg before each meal0.5-4 mg before meals16 mg/day
Type 2 diabetesAdults, HbA1c >=8%1-2 mg before each meal0.5-4 mg before meals16 mg/day

Titration At least 1 week between dose adjustments

Renal Severe impairment (CrCl 20-40): start 0.5 mg before each meal; CrCl <20/dialysis not studied

Hepatic Use caution; longer intervals between dose adjustments; higher hypoglycemia risk

Dose before each meal (2-4x daily)

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Limited data show no clear drug-associated risk; poorly controlled diabetes carries risk

Lactation Not recommended when breastfeeding

NO BOXED WARNINGS

Principal riskHypoglycemia; contraindicated with gemfibrozil

Cost, est. cash$5–$150/month

Generic entry2013

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability1 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk0 / 4

Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent

Defining liabilityAgent-specific hypoglycemia, ketoacidosis, volume, renal or gastrointestinal toxicity.

Mechanism of action: Repaglinide ballicule

Repaglinide ballicule: receptor binding, kinetics and half-life diagram

Open Repaglinide in the interactive console ↗

Memory aids: mascots and interaction avatars

Repaglinide PRANDIN mascot mnemonic cartoon
“Repay gliding Panda (Brandon)”
sugar → insulin secretagogue
Repaglinide CYP2C8 substrate avatar
CYP2C8 substrate
Repaglinide OATP substrate avatar
OATP substrate

Open Repaglinide in the interactive console ↗