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  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 resulting from drug-induced endogenous secretion of insulin.

    2. Octreotide also suppresses pancreatic function, gastric acid secretion, and biliary and GI tract motility.

    3. As a polypeptide, it is bioavailable only by parenteral administration (intravenously or subcutaneously). Approximately 30% of octreotide is excreted unchanged in the urine, and it has an elimination half-life of 1.7 hours. Its half-life may be increased in patients with renal dysfunction and in the elderly.

  2. Indications. Oral sulfonylurea hypoglycemic overdose (See Antidiabetic Agents) or quinine-induced hypoglycemia (See Quinine) when serum glucose concentrations cannot be maintained with an intravenous 5% dextrose infusion. It may also be considered a first-line agent along with dextrose because it can reduce glucose requirements and prevent rebound hypoglycemia in patients with sulfonylurea poisoning. This agent is preferred over diazoxide (See Diazoxide). It is not used in the management of exogenous insulin poisoning, where it has a theoretic disadvantage of blocking beneficial counterregulatory reactions (prevents glucagon and growth hormone secretion) to hypoglycemia.

  3. Contraindications. Hypersensitivity to the drug (anaphylactic shock has occurred).

  4. Adverse effects. In general, the drug is well tolerated. Patients may experience pain or burning at the injection site. For the most part, the adverse-effect profile is based on long-term therapy for other disease states.

    1. The suppressive effects on the biliary tract may lead to significant gallbladder disease (cholelithiasis) and pancreatitis.

    2. Gastrointestinal effects (diarrhea, nausea, discomfort) may occur in 5–10% of users. Headache, dizziness, and fatigue have also been observed.

    3. Cardiac effects may include bradycardia, conduction abnormalities (QT prolongation), hypertension, and exacerbation of congestive heart failure. These effects have been observed primarily in patients treated for acromegaly.

    4. Use in pregnancy. FDA Category B. Not likely to cause harm with short-term therapy (See Introduction in Section III).

  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

    1. Oral sulfonylurea overdose. Give 50–100 mcg (children: 1–1.25 mcg/kg) by subcutaneous or intravenous injection every 6–12 hours as needed (some patients with sulfonylurea poisoning may require higher doses and several days of therapy). Some children have been successfully treated with a 2- to 2.5-mcg/kg IV dose followed by a 2-mcg/kg/h infusion. Most patients require approximately 24 hours of therapy and do not experience recurrent hypoglycemia upon discontinuation of octreotide. Monitor for recurrent hypoglycemia for 24 hours after termination of octreotide therapy.

    2. Quinine-induced hypoglycemia. A dose of 50 mcg/h has been used in adult patients who are being treated with quinine for malaria.

    3. Subcutaneous injection sites should be rotated.

    4. 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.

    5. Note: Optimal dosage regimen is not known. For other indications, the dosage range ...

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