Pharm

Glucagon

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Glucagon, GlucaGen, Bagsimi, Gvoke

  • Physiology
  1. Endogenous polypeptide Hormone
  2. Secreted by pancreatic alpha cells
  3. Opposite effect of Insulin
    1. While Insulin lowers Serum Glucose (glycogen storage, Glycolysis), Glucagon increases Serum Glucose
    2. However, both Insulin and Glucagon increase amino acid uptake from the liver
  4. Hypoglycemia effect (primary)
    1. Hypoglycemia Increases pancreatic secretion of Glucagon
    2. Glucagon stimulates Glucose release from glycogen (glycogenolysis)
    3. Glucagon also stimulates Glucose synthesis (Gluconeogenesis)
  5. Inhibitors of Glucagon release
    1. Hyperglycemia
      1. Inhibits pancreatic secretion of Glucagon
    2. GLP1 (Incretin)
      1. Secreted by Small Bowel
      2. Stimulates pancreatic beta cells and inhibits Glucagon
      3. See Incretin Mimetics (used in Type 2 Diabetes Mellitus)
  6. Amino Acid Excess Effect
    1. Increases pancreatic secretion of Glucagon
    2. Glucagon stimulates liver uptake of amino acids
      1. Both Insulin and Glucagon increase liver uptake of amino acids
  7. Acts at Catecholamine-independent receptors on cardiac cells
    1. Increases intracellular Calcium in cardiac cells
    2. Increases myocardial contractions
  • Pathophysiology
  1. Glucagonomas
    1. Glucagon Secreting tumor resulting in Diabetes Mellitus, as well as dermatitis (necrolytic migratory erythema)
  • Indications
  • Glucagon Administration
  • Pharmacokinetics
  1. Onset of action: 5 to 20 minutes
  • Preparations
  1. Background
    1. Cost approximately $280 for each agent (in 2019)
    2. Shelf-life: 2 years
  2. GlucaGen Hypokit (IM)
    1. Standard IM Injection
  3. Gvoke (SC)
    1. Subcutaneous Injection using a prefilled syringer (autoinjector release pending in 2020)
  4. Bagsimi (Intranasal)
    1. Powder sprayed into a single nostril
  1. Adult: 1 mg IV, IM or SC
  2. Pediatric
    1. Standard dose: 30 ug/kg IM
    2. Newborn of diabetic mother: 300 ug/kg IM
    3. Maximum dose: 1 mg
  • References
  1. Goldberg (2014) Clinical Physiology, Medmasters, Miami, 140-1
  2. (2019) Presc Lett 26(11): 62-3