Metabolic effects of octreotide

One discussion this week involved the effects of octreotide.

Reference: Octreotide: a drug often used in the critical care setting but not well understood. Chest. 2013 Dec;144(6):1937-1945. doi:10.1378/chest.13-0382.

Summary: While a majority of octreotide is metabolized by the liver, 30-35% of octreotide acetate is excreted in the urine. Thus, octreotide accumulates in patients with moderate to severe renal or hepatic insufficiency.

Compared with SST-14, it exhibits 45-fold more potent inhibition of growth hormone, 11-fold more of glucagon, and 1.3-fold more insulin secretion.



Octreotide inhibits insulin secretion in the following ways (p.1943):

  • Binds to SSTR-5 present on pancreatic B islet cells, inhibiting the formation of cAMP and reducing influx of calcium into the cytoplasm, thus preventing insulin secretion.
  • Inhibition of direct phosphorylation of specific proteins required for secretion of insulin-containing vesicles.

Additional reading:  Adabala M, et al. Severe hyperkalaemia resulting from octreotide use in a haemodioalysis patient. Nephrology, Dialysis, Transplantation. 2010 Oct;25(10):3439-3442. doi:10.1093/ndt/gfq381.

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