Medicine & USMLE

Incretin Mimetics

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Diabetes Drugs
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  2. Rapid Acting Insulin
  3. Short Acting Insulin
  4. Intermediate Acting Insulin
  5. Long Acting Insulin
  6. Metformin
  7. Sulfonylureas
  8. Meglitinides
  9. Thiazolidinediones (TZDs)
  10. DPP-4 Inhibitors
  11. Incretin Mimetics
  12. SGLT2 Inhibitors
  13. Alpha Glucosidase Inhibitors
  14. Pramlintide

Summary

Incretin mimetics include the drugs exenatide and liraglutide and are used to treat type 2 diabetes mellitus.

These drugs work by acting on GLP-1 receptors. This causes an increase in insulin release and a decrease in glucagon release. These drugs also work by slowing gastric emptying and suppressing appetite.

One side effect of incretin mimetics is pancreatitis. These drugs are eliminated by the kidneys, so they should be used with caution in patients with kidney damage. Some GI effects include nausea, vomiting, and diarrhea. Incretin mimetics can block the absorption of oral medications, so if the patient takes other medications, they should generally be taken 1 hour prior to the administration of the incretin mimetic. Other side effects include thyroid cancer and weight loss.

When administering exenatide, give it 60 minutes before breakfast and dinner via a subcutaneous injection. Incretin mimetics must be refrigerated.

Key Points

  • Incretin Mimetics
    • Drug Names
      • Exenatide (Byetta)
      • Liraglutide (Victoza)
      • Semaglutide (Ozempic, Rybelsus)
    • Mechanism
      • Acts on GLP-1 receptors
        • Incretin mimetics are also called GLP-1 receptor agonists or GLP-1 analogs
        • GLP-1 is a specific type of incretin hormone. Incretin mimetics mimic GLP-1 and stimulate their receptors
      • Increases insulin release
        • Binds to GLP-1 receptors, telling the cell to release more insulin
      • Decreases glucagon release
      • Slows gastric emptying
        • This reduces the amount of food that moves at a time into the intestines, meaning less sugar is absorbed from the intestines into the bloodstream
      • Suppresses appetite
        • Increases satiety (sense of fullness)
    • Clinical Use
      • Treats Type 2 Diabetes Mellitus
        • The end result of incretin mimetics is a decrease in blood glucose levels of patients with type 2 diabetes mellitus
    • Side Effects
      • Gastrointestinal Effects
        • Causes nausea/vomiting
          • Common side effect, expected
        • Causes diarrhea
          • Common side effect, expected
        • Causes weight loss
          • Incretin mimetics are sometimes used (or abused) for their weight loss side effects
      • Causes pancreatitis
        • Avoid in patients with a history of pancreatitis
        • Notify provider of abdominal pain, which could be a sign of pancreatitis
      • Use with caution in renal failure
        • Incretin mimetics are eliminated by the kidneys
        • Decreased kidney function can cause a buildup of the drug in the bloodstream
        • Patients with renal failure may have more side effects than normal
      • Increase risk of thyroid cancer
        • Black box warning
        • Not recommended with family history of thyroid cancer
      • Delays oral medication absorption
        • Due to the effects of slowed gastric emptying
        • If the patient takes other oral medications, they should be taken at least one hour before the injection of the incretin mimetic
    • Administration
      • Given via subcutaneous injection
      • Administer exenatide 60 minutes before morning and evening meal (twice a day)
      • Store in refrigerator
        • The medication comes prepackaged in an injection pen that should be refrigerated