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octreotide (Sandostatin)

Tradename: Sandostatin. A somatostatin analog. Indications: 1) acromegaly: - 100 ug SC TID can be used to suppress growth hormone (GH) secretion while awaiting effect of radiation therapy for incompletely resected GH-secreting pituitary adenoma. 2) *esophageal variceal hemorrhage* 3) hormone-secreting tumors a) carcinoid - carcinoid syndrome b) VIPomas 200-300 ug SC QD in 2-4 divided doses c) insulinoma d) gastrinoma (Zollinger-Ellison syndrome) e) glucagonoma f) nesidioblastosis 4) AIDS (HIV1)-associated viral enteritis (possibly helpful) a) start 50-100 ug every 8 hours b) increase by 100 ug/dose every 48 hours c) maximum 500 mg every 8 hours 5) short-bowel syndrome or dumping syndrome (possibly helpful) 6) irritable bowel syndrome 7) GI & pancreatic fistulas 8) chylous pleural effusion [6] 9) in combination with midodrine for treatment of hepatorenal syndrome * of no benefit in reducing mortality or preventing need for blood transfusion [7] Dosage: - carcinoid a) 100-600 ug QD in 2-4 divided doses b) long acting form for monthy IM injection into the gluteus maximus - VIPomas 200-300 ug SC QD in 2-4 divided doses - esophageal variceal hemorrhage* - 50 ug IV bolus, then 50 ug/hr IV drip for 2-5 days - for reduction of portal hypertension in patients with acute variceal hemorrhage; may offer efficacy similar to vasopressin infusion with fewer side effects - vasoactive agent of choice, preferably prior to endoscopy [8] Injection: 0.05 mg (1 mL), 0.1 mg (1 mL), 0.2 mg (5 mL), 0.5 mg (1 mL), 1 mg (5 mL) Syringe: tuberculin syringe, 1mL, 26 g, 3/8 inch * of no benefit in reducing mortality or preventing need for blood transfusion Pharmacokinetics: 1) rapidly & completely absorbed after SC administration 2) 1/2life is 1.7 hours 3) duration of action is variable, may last up to 12 hours 4) decrease dose in elderly because of decreased clearance Adverse effects: 1) not common (1-10%) - nausea/vomiting, pain at site of injection, diarrhea, abdominal pain, headache, fat malabsorption, dizziness, hyperglycemia, fatigue, flushing, hypoglycemia, edema, weakness 2) uncommon (< 1%) - anxiety, erythema, hair loss, constipation, flatulence, hepatitis, shortness of breath, burning eyes, fever, throat discomfort, leg cramps, rhinorrhea, chest pain, Bell's palsy, rash, galactorrhea 3) other [3] - mild abdominal discomfort - cholelithiasis with long-term use - sinus bradycardia - pancreatitis - vitamin B12 deficiency - ischemia Drug interactions: 1) cyclosporine a) possible transplant rejection b) octreotide decreases absorption of fat-soluble substance like cyclosporine 2) beta blockers or calcium channel blockers used in combination with octreotide may cause bradycardia Laboratory: - octreotide in serum/plasma Mechanism of action: 1) octapeptide analogue of somatostatin 2) inhibits growth hormone, glucagon & insulin secretion 3) supresses LH response to GnRH 4) decreases splanchnic blood flow 5) inhibits release of serotonin, gastrin, VIP, secretin, motilin & pancreatic polypeptide 6) decreases plasma IGF-1 & TSH 7) inhibits gall bladder contraction 8) inhibits intestinal secretion & motility (inhibits diarrhea)

Related

somatostatin; growth hormone release-inhibiting factor; contains: somatostatin-28, somatostatin-14 (SST)

General

endocrine agent

Properties

MISC-INFO: elimination route LIVER KIDNEY 1/2life 1.7 HOURS pregnancy-category B safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 351, 478
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 586
  6. Deprecated Reference
  7. The NNT: Somatostatin Analogues (Octreotide) for Acute Variceal Bleeding. http://www.thennt.com/nnt/octreotide-for-acute-variceal-bleeding/ - Gotzsche PC, Hrobjartsson A Somatostatin analogues for acute bleeding oesophageal varices. Cochrane Database Syst Rev. 2008 Jul 16;(3):CD000193 PMID: 18677774
  8. Garcia-Tsao G et al. AGA clinical practice update on the use of vasoactive drugs and intravenous albumin in cirrhosis: Expert review. Gastroenterology 2024 Jan; 166:202. PMID: 37978969 https://www.gastrojournal.org/article/S0016-5085(23)05143-0/fulltext