Repaglinide

Aka: Repaglinide, Prandin

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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

XI. Resources

  1. Repaglinide (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d7673e22-0dbb-4395-ad60-943d249203a1

XII. References

  1. Luna (2001) Am Fam Physician 63(9):1747-56 [PubMed]
  2. Luna (1999) Prim Care 26:895-915 [PubMed]
  3. Vaughan (2024) Am Fam Physician 109(4): 333-42 [PubMed]

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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
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Related Topics in Pharmacology

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