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

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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

Ontology: nateglinide (C0903898)

Definition (NCI) A phenylalanine derivative of the meglitinide class of agents with hypoglycemic activity. Nateglinide, compared to repaglitinide, binds with a higher affinity to the SUR1 subunit and with a faster onset of action and a shorter duration of action. This agent is metabolized by the cytochrome P450 isoenzyme CYP2C9, and, to a lesser extent, by CYP3A4. The parent drug and metabolites are mainly excreted in the urine and its half-life is about 1.5 hours.
Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
MSH C060142
SnomedCT 129496008, 134604002, 387070004
LNC LP64443-2, MTHU026435
English IPCCPA, N-((4-isopropylcyclohexyl)carbonyl)phenylalanine, nate-glinide, nateglinide (medication), NATEGLINIDE, nateglinide [Chemical/Ingredient], nateglinide, D-phenylalanine, N-((trans-4-(1-methylethyl)cyclohexyl)carbonyl)-, senaglinide, Nateglinide (product), Nateglinide (substance), Nateglinide
Spanish nateglinida (concepto no activo), nateglinida (producto), nateglinida (sustancia), nateglinida

Ontology: Starlix (C1323198)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C060142
English starlix, Starlix, Novartis brand of nateglinide