II. Indications

  1. Early Type II Diabetes Mellitus Oral Agent
    1. Elevated postprandial Glucose
    2. Consider if only used intermittently for pre-meal Hyperglycemia

III. Contraindications

  1. Sulfa Hypersensitivity
  2. Chronic Kidney Disease Stage 5 (eGFR <15 ml/min)

IV. Mechanism

  1. Insulin secretogogue
  2. Benzoic acid derived from Sulfonylureas
  3. Directly stimulates pancreatic beta cells (Similar to Sulfonylureas)
    1. Binds different sites from Sulfonylureas (Sulfonylurea Receptors 1, 1A and 1B)
    2. Closes ATP sensitive K+ channels
    3. Results in Insulin secretion
  4. Effects
    1. Predominately effects postprandial Glucose
    2. Faster oral absorption and onset than Sulfonylureas
    3. Shorter duration of binding and shorter effect than Sulfonylureas

V. Medications

  1. Repaglinide (Prandin) tablets: 0.5 mg, 1 mg, 2 mg

VI. Dosing

  1. General
    1. Take only before meals, especially before the largest meal (and skip if Fasting)
  2. Adults (not FDA approved in children)
    1. Take 0.5 to 2 mg orally before meals, from 3 to 4 times daily
    2. Titrate dose in 1 week intervals
    3. Maximum 16 mg/day
    4. Starting Dose
      1. A1C<8%: Start at 0.5 mg orally three times daily before meals
      2. A1C>8%: Start at 1 to 2 mg orally three times daily before meals
      3. CrCl 20 to 40 ml/min: Start at 0.5 mg orally three times daily before meals

VII. Pharmacokinetics

  1. Renal excretion
  2. Hepatic metabolism (CYP3A4, CYP2C9)

VIII. Adverse Effects

  1. Hypoglycemia (lower risk than Sulfonylureas)

IX. Safety

  1. Pregnancy Category C
  2. Unknown safety in Lactation

X. Efficacy

  1. Lowers HBA1C by 0.5 to 1%
  2. Repaglinide is significantly stronger than Nateglinide (Starlix)
  3. Advantages in comparison to Sulfonylureas
    1. Low risk of Hypoglycemia (2.4%) than Sulfonylureas
    2. Effect depends on Ambient Blood Glucose levels
    3. No significant gastrointestinal side effects
    4. Minimal weight gain
    5. No lab monitoring required
    6. No significant Drug Interactions
    7. No Lactic Acidosis
    8. No adjustments needed (other than per meal)
      1. No adjustment in Congestive Heart Failure
      2. No adjustment for age
      3. No adjustment in Renal Insufficiency
  4. Disadvantages in comparison to Sulfonylureas
    1. Two to three times as expensive as Sulfonylureas

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Related Studies

Cost: Medications

repaglinide (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
REPAGLINIDE 0.5 MG TABLET Generic $0.11 each
REPAGLINIDE 1 MG TABLET Generic $0.12 each
REPAGLINIDE 2 MG TABLET Generic $0.13 each

Ontology: repaglinide (C0246689)

Definition (NCI) A nonsulfonylurea insulin secretagogue belonging to the melgitinide class with hypoglycemic activity. Repaglinide is rapidly absorbed and has a rapid onset and short duration of action. This agent is metabolized in the liver by CYP2C8 and CYP3A4 and its metabolites are excreted in the bile. Repaglinide has a half-life of one hour.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C072379
SnomedCT 109074004, 386964000
LNC LP34567-5, MTHU017515
English repaglinide, (+)-2-Ethoxy-alpha-(((S)-alpha-isobutyl-o-piperidinobenzyl)carbamoyl)-p-toluic Acid, Benzoic Acid, 2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)-,(S)-, repa-glinide, repaglinide (medication), REPAGLINIDE, repaglinide [Chemical/Ingredient], (S)-2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)-phenyl)butyl)amino)-2-oxoethyl)-benzoic acid, Repaglinide, Repaglinide (product), Repaglinide (substance)
Japanese レパグリニド
Spanish repaglinida (producto), repaglinida (sustancia), repaglinida

Ontology: Prandin (C0722725)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C072379
English Prandin, repaglinide (Prandin), prandin, Novo Nordisk brand 2 of repaglinide