Endocrinology Book

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Second Generation SulfonylureaAka: Insulin Secretagogue, Sulfonylurea, Glipizide, Glyburide

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  1. See Also
    1. First Generation Sulfonylurea
    2. Oral Hypoglycemic Agents
  2. Indications: Type II Diabetes Mellitus (early, phase 1-2)
    1. Better effect in lean patients
    2. Consider when Hemoglobin A1C <9%
    3. Second-line to Metformin in most patients
    4. Consider as first-line in specific cohorts
      1. Consider when post-prandial glucose 200 to 300 mg/dl
      2. Consider when Type II with polyuria, polydipsia
  3. Contraindication
    1. Sulfa allergy (applies to sulonylureas)
    2. Renal and liver dysfunction
      1. Use caution with Sulfonylureas
      2. Repaglinide or Nateglinide may be preferred here
  4. Mechanism
    1. Pancreatic beta cell stimulation for Insulin release
    2. Secretagogues do not burn out the beta cells sooner
  5. Dosing Pearls
    1. Use Long acting agents
    2. Increase dose every 1-2 weeks until adequate response
    3. No response in 25-30% of Type II Diabetics
    4. Never combine secretagogues
      1. They all have same site of activity
      2. If one does not work, then all will not work
  6. Preparations
    1. Glimepiride (Amaryl)
      1. Start: 1-2 mg PO qd
      2. Usual: 4 mg PO qd
      3. Maximum: 8 mg PO qd
      4. Advantages
        1. More rapid onset with longer duration
        2. Lower Incidence of Hypoglycemia
        3. Preferred of class for Coronary Artery Disease
    2. Glipizide (Glucotrol)
      1. Start: 5 mg PO qd
      2. Usual: 10-20 mg PO qd
      3. Maximum: 20 mg PO bid
    3. Glipizide Extended Release (Glucotrol XL)
      1. Start: 5 mg PO qd
      2. Usual: 5-10 mg PO qd
      3. Maximum: 20 mg PO qd
      4. Advantages: Least expensive Sulfonylurea
    4. Glyburide (DiaBeta, Micronase)
      1. Start: 2.5 to 5 mg PO qd
      2. Usual: 5-20 mg PO qd
      3. Maximum: 20 mg PO qd
    5. Glyburide Micronized (Glynase, PresTab)
      1. Start: 1.5 to 3 mg PO qd
      2. Usual: 3-12 mg PO qd
      3. Maximum: 12 mg PO qd
  7. Adverse Effects
    1. Weight gain
    2. Hypoglycemia
  8. References
    1. Defronzo (1999) Ann Intern Med 131:281
    2. Luna (1999) Prim Care 26:895

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