Nateglinide

Aka: Nateglinide, Starlix

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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. Nateglinide (Starlix): 60 mg, 120 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 60 to 120 mg orally before meals, from 1 to 3 times daily
    2. Typical dosing is 120 mg
      1. However, may use 60 mg dose if patient near glycemic control goals

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. Of the Meglitinides, Nateglinide is significantly weaker than Repaglinide (Prandin)
  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. Nateglinide (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=88698921-cd8f-4d41-96e6-ff671913c5c3

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

nateglinide (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
NATEGLINIDE 120 MG TABLET Generic $0.30 each
NATEGLINIDE 60 MG TABLET Generic $0.27 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.

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