Pharm

Insulin Secretagogue

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Insulin Secretagogue

  • See Also
  1. Oral Hypoglycemic Agents
  • Background
  1. Sulfonylureas
    1. Sulfonylureas were first discovered in 1940's while investigating SulfonamideAntibiotics
    2. First Generation Sulfonylureas (e.g. Tolbutamide) were developed in the 1960s
    3. Second Generation Sulfonylureas were available in the 1980s
    4. Sulfonylureas are also used as herbicides (block specific plant Amino Acid biosynthesis)
  2. Meglitinides
    1. Meglitinide development started in the 1970s and were marketed in the U.S. in the late 1990s
  • Mechanism
  1. Sulfonylureas
    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
  2. Meglitinides
    1. Benzoic acid derived from Sulfonylureas
    2. 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
    3. 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. First Generation Sulfonylurea (Listed for historical purposes only)
  2. Second Generation Sulfonylurea (e.g. Glipizide, Glyburide)
  3. Non-Sulfonylurea Insulin Secretagogues (e.g. Meglitinide, Repaglinide)