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
  • Indications
  1. Type II Diabetes Mellitus (historical)
    1. Replaced by Second Generation Sulfonylurea agents
  • Mechanism
  1. Sulfonylureas stimulate Potassium channel closure on pancreatic beta cell surface
    1. Triggers Insulin release
  • 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