Pharm

First Generation Sulfonylurea

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First Generation Sulfonylurea, Tolbutamide, Tolazamide, Chlorpropamide, Acetohexamide

  • See Also
  1. Second Generation Sulfonylurea
  2. Oral Hypoglycemic Agents
  • Background
  1. Listed for historical purposes only
  2. See Second Generation Sulfonylurea instead
  • Indications
  1. Type II Diabetes Mellitus (historical)
    1. Replaced by Second Generation Sulfonylurea agents
  • Mechanism
  1. Sulfonylureas trigger Insulin release from pancreatic beta cells
    1. Sulfonylureas stimulate Potassium channel closure on pancreatic beta cell surface
    2. Secretagogues do NOT burn out the beta cells sooner
  2. Sulfonylureas may also increase tissue Insulin sensitivity
  • Medications
  1. Acetohexamide (Dymelor)
    1. Dose: 500 to 750 mg orally daily or divided twice daily
  2. Chlorpropamide (Diabinese)
    1. Dose: 100 to 250 mg up to 750 mg daily or divided twice daily
    2. Antidiuretic effect (used in Diabetes Insipidus)
  3. Tolazamide (Tolinase)
    1. Dose: 250-500 mg orally daily or divided twice daily
  4. Tolbutamide (Orinase)
    1. Dose: 1000 to 2000 mg orally daily or divided twice daily