Pharm

Nateglinide

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Nateglinide, Starlix

  • Indications
  1. Early Type II Diabetes Mellitus Oral Agent
    1. Elevated postprandial Glucose
    2. Consider if only used intermittently for pre-meal Hyperglycemia
  • Contraindications
  1. Sulfa Hypersensitivity
  2. Chronic Kidney Disease Stage 5 (eGFR <15 ml/min)
  • 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
  • Medications
  1. Nateglinide (Starlix): 60 mg, 120 mg
  • 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
  • Pharmacokinetics
  1. Renal excretion
  2. Hepatic metabolism (CYP3A4, CYP2C9)
  • Adverse Effects
  1. Hypoglycemia (lower risk than Sulfonylureas)
  • Safety
  1. Pregnancy Category C
  2. Unknown safety in Lactation
  • 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