Octreotideis a synthetic polypeptide and a long-acting analog of somatostatin. Itsignificantly antagonizes pancreatic insulin release and is useful forthe management of poisonings from drug-induced endogenous secretion ofinsulin-, oral sulfonylurea–, and quinine-induced hyperinsulinemic andhypoglycemic poisonings.

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

Asa polypeptide, it is bioavailable only by parenteral administration(intravenously or subcutaneously). Approximately 30% of octreotide isexcreted unchanged in the urine, and it has an elimination half-life of1.7 hours. Its half-life may be increased in patients with renaldysfunction and in the elderly.

Drug Indications ::

Indications. Oralsulfonylurea hypoglycemic overdose (see Antidiabetic Agents) andquinine-induced hypoglycemia (Quinine) when serum glucoseconcentrations cannot be maintained by an intravenous 5% dextroseinfusion. It may also be considered a first-line agent along withdextrose since it can reduce glucose requirements and prevent reboundhypoglycemia in patients with sulfonylurea poisoning. This agent ispreferred over diazoxide (Diazoxide). It is uncertain whetheroctreotide has a role with exogenous insulin poisoning, and it has atheoretical disadvantage of blocking counterregulatory reactions(prevents glucagon and growth hormone secretion) to hypoglycemia.

Drug Contra-Indications ::

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

Drug Adverse Effects ::

IV. Adverse effects. Ingeneral, the drug is well tolerated. Patients may experience pain orburning at the injection site. For the most part, the adverse effectprofile is based on long-term therapy for other disease states.

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

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

Cardiaceffects may include bradycardia, conduction abnormalities (QTprolongation), hypertension, and exacerbation of congestive heartfailure. These effects have been observed primarily in patients treatedfor acromegaly.

Use in pregnancy. FDA category B. Not likely to cause harm with short-term therapy (see Table III–1).

Drug Lab Interactions ::

Drug or laboratory interactions

Octreotide may inhibit the absorption of dietary fats and cyclosporine.

The drug depresses vitamin B12 levels and can lead to abnormal Schilling’s test results.

Drug Dose Management ::

Dosage and method of administration

Oral sulfonylurea overdose. Give50–100 mcg (children: 4–5 mcg/kg/day divided every 6 hours) bysubcutaneous or intravenous injection once or every 6–12 hours asneeded (some sulfonylurea poisonings may require days of therapy).Infusions up to 125 mcg/h have been used (see note below). Mostpatients require approximately 24 hours of therapy and do notexperience recurrent hypoglycemia upon discontinuation of octreotide.Monitor for recurrent hypoglycemia for 24 hours after termination ofoctreotide therapy.

Quinine-induced hypoglycemia. A dose of 50 mcg/h has been used in adult patients with malaria.

Subcutaneous injection sites should be rotated.

ForIV administration, dilute in 50 mL normal saline or 5% dextrose andinfuse over 15–30 min. Alternatively, the dose may be given IV pushover 3 min.

E. Note:Optimal dosage regimen is not known. For other indications, daily dosesup to 1500 mcg are utilized (120 mg has been infused over 8 hourswithout severe adverse effects).

Drug Chemical Formulations ::

Formulations

Parenteral. Octreotideacetate (Sandostatin, generic): 0.05, 0.1, and 0.5 mg/mL in 1-mLampules and vials; 0.2 and 1 mg/mL in 5-mL multidose vials. Note: Avoid use of the long-acting agent Sandostatin LAR Depot. This product is for once-a-month dosing in patients with acromegaly.

The suggested minimum stocking levelto treat a 70-kg adult for the first 24 hours is two (1-mL) ampules orvials (0.1 mg/mL) or one (5-mL) multidose vial (0.2 mg/mL).

Disclaimer ::

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