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Introduction

  1. Pharmacology
    1. Octreotide is a synthetic polypeptide and a long-acting analog of somatostatin. It significantly antagonizes pancreatic insulin release and is useful for the management of hypoglycemia from xenobiotic-induced endogenous insulin secretion.
    2. Octreotide also suppresses pancreatic exocrine and endocrine secretion, gastric acid production, and biliary and GI tract motility.
    3. It is mainly metabolized in the liver, although 30-35% of octreotide is excreted unchanged in the urine. The elimination half-life is 1.7 hours which may be prolonged in the elderly or in patients with renal or hepatic dysfunction.
  2. Indications. Treatment of recurrent hypoglycemia from sulfonylurea (Diabetic Drugs), meglitinide (Diabetic Drugs), quinine, or quinolone medications. It may be used as a first-line agent in addition to oral or intravenous glucose supplementation as it can reduce glucose requirements and prevent rebound hypoglycemia. There is limited evidence for its role in the management of exogenous insulin poisoning.
  3. Contraindications. Hypersensitivity to the drug (anaphylactic shock has occurred).
  4. Adverse effects. It is generally well tolerated. Some patients may experience pain or burning at the injection site, abdominal cramping, nausea, and diarrhea within hours of administration. Additional adverse effects can be seen with long-term therapy for other disease states.
    1. Changes in gallbladder contractility and bile composition may result in gallstones, biliary sludge, cholecystitis, cholestatic hepatitis, and pancreatitis.
    2. Headache, dizziness, and fatigue have been observed.
    3. Cardiac effects may include bradycardia, conduction abnormalities (QT prolongation), hypokalemia, hyperkalemia, hypertension, and exacerbation of congestive heart failure.
    4. Use in pregnancy. FDA Category B. Not likely to cause harm with short-term therapy (Introduction).
  5. Drug or laboratory interactions
    1. Octreotide may inhibit the absorption of dietary fats and cyclosporine.
    2. The drug depresses vitamin B12 levels and can lead to abnormal Schilling test results.
  6. Dosage and method of administration for hypoglycemia from xenobiotic-induced endogenous insulin secretion.
    1. Give 50-100 mcg (children: 1-2 mcg/kg) by subcutaneous or intravenous injection every 6-12 hours as needed. Some patients with sulfonylurea poisoning may require more frequent (every 4 hours), higher doses, and several days of therapy. Continuous infusions of up to 50-125 mcg/h have been used. Some children have been successfully treated with a 1-2 mcg/kg IV dose, followed by a 1-2 mcg/kg/h infusion. Most patients require approximately 24 hours of therapy and typically do not experience recurrent hypoglycemia upon discontinuation of octreotide (although hypoglycemia has recurred 30 hours after a glipizide exposure). Monitor for recurrent hypoglycemia for 12-24 hours after termination of octreotide therapy.
    2. Subcutaneous injection sites should be rotated.
    3. For IV administration, dilute in 50 mL of normal saline or 5% dextrose and infuse over 15-30 minutes. Alternatively, the dose may be given as an IV push over 3 minutes.
    4. Note: Optimal dosage regimen is not known. For other indications, the dosage range for children is 2-40 mcg/kg/d, and daily doses of up to 1,500 mcg are used in adults (120 mg has been infused over 8 hours without severe adverse effects).