Antidiarrheals / Types / Octreotide
Somatostatin analogue: OCTREOTIDE
Mechanism of action
- SOMATOSTATIN is a key regulatory peptide of lower GI function - overall, it:
- decreases intestinal fluid secretion
- has dose dependent effects on GI motility:
- low doses stimulate motility
- high doses inhibit motility
- has a short half-life (3 minutes) that limits its use as a pharmaceutical agent
- OCTREOTIDE is a synthetic analogue of SOMATOSTATIN, with a t½ of 1.5 hours by IV, 6-12 hours when given SC (can also be given monthly by IM injection)
Therapeutic uses
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inhibition of the effects of carcinoid tumors and VIPomas (you will hear more about these in the Endocrine course)
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off-label use for severe diarrhea due to vagotomy or dumping syndrome, short bowel syndrome, AIDS
- you may ask why vagotomy is listed here as producing severe diarrhea, since in other circumstances, vagotomy decreases motility and produces constipation
- to quote Schwarz’s Principles of Medicine (available via Access Medicine):
“Diarrhea following gastric surgery may be the result of truncal vagotomy, dumping, or malabsorption. Truncal vagotomy is associated with clinically significant diarrhea in 5 to 10% of patients. … The cause of postvagotomy diarrhea is unclear. Possible mechanisms include intestinal dysmotility and accelerated transit, bile acid malabsorption, rapid gastric emptying, and bacterial overgrowth.”
Side effects
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impaired pancreatic secretion à malabsorption of fats à fat-soluble vitamin deficiency and steatorrhea
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impaired GI motility à nausea, abdominal pain, flatulence
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inhibition of gallbladder contractility à gallstones (50% of patients), acute cholecystitis (rare)
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altered balance among insulin, glucagon and growth hormone à hyper- or hypo-glycemia
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hypothyroidism, bradycardia