First Generation Sulfonylurea

Aka: First Generation Sulfonylurea, Tolbutamide, Tolazamide, Chlorpropamide, Acetohexamide

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II. Background

  1. Listed for historical purposes only

III. Indications

  1. Type II Diabetes Mellitus (historical)
    1. Replaced by Second Generation Sulfonylurea agents

IV. Mechanism

  1. Sulfonylureas stimulate Potassium channel closure on pancreatic beta cell surface
    1. Triggers Insulin release

V. 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

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