Octreotide

Aka: Octreotide, L-Cysteinamide, Sandostatin, Sandostatin LAR

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II. Indications

  1. Emergency Indications
    1. Esophageal Variceal Hemorrhage
      1. May decrease Upper Gastrointestinal Bleeding rate while awaiting definitive endoscopic management
      2. Decreases pressure in Portal Hypertension
        1. Decreases splanchnic Blood Flow and portal venous pressure
    2. Sulfonylurea Overdose
      1. Decreases recurrent Hypoglycemia risk
      2. Octreotide inhibits Insulin release from pancreatic beta cells
  2. Endocrine Indications
    1. Diarrhea associated with endocrine tumors
      1. Carcinoid Tumors
      2. Intestinal peptide-Secreting tumors
      3. Has also been used in HIV related Diarrhea, Irritable Bowel Syndrome and gastrointestinal fistulas
    2. Endocrine conditions in children
      1. Congenital hyperinsulinism
      2. Hypothalamic Obesity

III. Mechanism

  1. Similar to Somatostatin, an endogenous Hormone
    1. Octreotide is a synthetic long-acting cyclic octapeptide that mimics Somatostatin activity
  2. Broad hormonal release inhibition
    1. Inhibits Serotonin release
    2. Inhibits Gastrin release
    3. Inhibits vasoactive intestinal peptide (VIP) release
    4. Inhibits Insulin release
    5. Inhibits Glucagon release
    6. Inhibits Secretin release
    7. Inhibits motilin release
    8. Inhibits pancreatic peptide release
    9. Inhibits Growth Hormone and IGF-1 release
    10. Decreases Luteinizing Hormone (LH) release in response to Gonadotrophin-Releasing Hormone (GnRH)
    11. Decreases Thyroid Stimulating Hormone release (TSH)
  3. Activity
    1. Vasoconstriction
    2. Decreases portal vessel pressure
    3. Decreased splanchnic Blood Flow

IV. Dosing: Emergent Conditions (off-label)

  1. Esophageal Varices
    1. See Bleeding Esophageal Varices
    2. Bolus: 50 mcg IV every 1 hour for up to 2 doses
    3. Maintenance: 25-50 mcg/hour for 2-5 days
  2. Sulfonylurea Overdose
    1. See Sulfonylurea Overdose
    2. Subcutaneous (preferred SQ, but also be given as IV bolus)
      1. Adult: 50 mcg SQ (up to 100 mcg) every 6-12 hours as needed
      2. Child: 1 to 1.25 mcg/kg SQ or IV every 6-12 hours (consult poison control)
    3. IV infusion: 25-50 mcg/hour for up to 1-2 days as needed for persistent and recurrent Hypoglycemia
    4. Precautions
      1. Rebound Hypoglycemia risk when Octreotide is stopped (monitor Glucose for 12-24 hours after last dose)

V. Dosing: Endocrine

  1. Diarrhea associated with Carcinoid Tumors or intestinal peptide-Secreting tumors
    1. Sandostatin 200-300 mcg divided 2-4 times daily given SQ or IV
    2. Sandostatin LAR 20 mg IM every 4 weeks for 2 months
      1. Do not start Sandostatin LAR until stabilized on the short-acting Sandostatin
  2. Endocrine conditions in children
    1. Congenital hyperinsulinism
    2. Hypothalamic Obesity

VI. Pharmacokinetics

  1. Subcutaneous (SQ) absorption is rapid with clinical effects within 30 minutes
  2. Plasma Half-Life: 1.5 to 2 hours
    1. However clinical effects last for several hours
    2. Requires repeat dosing for ongoing indication effects (e.g. Hypoglycemia in Sulfonylurea Overdose)
  3. Renal Insufficiency
    1. Octreotide clearance may be reduced

VII. Adverse Effects

  1. Hyperglycemia (<27%)
  2. Fatigue (<10%)
  3. Headache
  4. Cardiovascular
    1. Bradycardia (<25%)
    2. QT Prolongation
  5. Gastrointestinal
    1. Nausea
    2. Abdominal Pain
    3. Diarrhea
    4. Gall Bladder sludging and Biliary Colic

VIII. References

  1. Kraus and LoVecchio (2018) Crit Dec Emerg Med 32(9): 28
  2. LoVecchio and Mourad (2018) Crit Dec Emerg Med 40(8): 38

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