octreotide (Sandostatin)
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Introduction
Tradename: Sandostatin. A somatostatin analog.
Indications
- 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.
- esophageal variceal hemorrhage*
- hormone-secreting tumors
- carcinoid
- VIPomas 200-300 ug SC QD in 2-4 divided doses
- insulinoma
- gastrinoma (Zollinger-Ellison syndrome)
- glucagonoma
- nesidioblastosis
- AIDS (HIV1)-associated viral enteritis (possibly helpful)
- start 50-100 ug every 8 hours
- increase by 100 ug/dose every 48 hours
- maximum 500 mg every 8 hours
- short-bowel syndrome or dumping syndrome (possibly helpful)
- irritable bowel syndrome
- GI & pancreatic fistulas
- chylous pleural effusion[6]
- in combination with midodrine for treatment of hepatorenal syndrome
* of no benefit in reducing mortality or preventing need for blood transfusion[7]
Dosage
- carcinoid
- 100-600 ug QD in 2-4 divided doses
- 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
- rapidly & completely absorbed after SC administration
- 1/2life is 1.7 hours
- duration of action is variable, may last up to 12 hours
- decrease dose in elderly because of decreased clearance
elimination via liver
elimination via kidney
1/2life = 1.7 hours
Adverse effects
- not common (1-10%)
- nausea/vomiting, pain at site of injection, diarrhea, abdominal pain, headache, fat malabsorption, dizziness, hyperglycemia, fatigue, flushing, hypoglycemia, edema, weakness
- 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
- other[3]
- mild abdominal discomfort
- cholelithiasis with long-term use
- sinus bradycardia
- pancreatitis
- vitamin B12 deficiency
- ischemia
Drug interactions
- cyclosporine
- possible transplant rejection
- octreotide decreases absorption of fat-soluble substance like cyclosporine
- beta blockers or calcium channel blockers used in combination with octreotide may cause bradycardia
Laboratory
Mechanism of action
- octapeptide analogue of somatostatin
- inhibits growth hormone, glucagon & insulin secretion
- supresses LH response to GnRH
- decreases splanchnic blood flow
- inhibits release of serotonin, gastrin, VIP, secretin, motilin & pancreatic polypeptide
- decreases plasma IGF-1 & TSH
- inhibits gall bladder contraction
- inhibits intestinal secretion & motility (inhibits diarrhea)
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 351, 478
- ↑ 3.0 3.1 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 586
- ↑ 6.0 6.1 Deprecated Reference
- ↑ 7.0 7.1 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: https://www.ncbi.nlm.nih.gov/pubmed/18677774 - ↑ 8.0 8.1 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: https://www.ncbi.nlm.nih.gov/pubmed/37978969 https://www.gastrojournal.org/article/S0016-5085(23)05143-0/fulltext
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=383414
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=123864
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=448601
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=54373
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=441258
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=383413