Octreotide, a long-acting structural derivative of somatostatins, is a synthetic peptide analog of somatostatin with the same pharmacologic effects. Octreotide is a cyclic octapeptide containing two D-configuration amino acids, with high binding affinity for somatostatin receptor (SSTR) 2 and 5, reduced affinity for SSTR3, and no affinity for SSTR1 and SSTR4. Its primary advantages over somatostatin are a longer half-life in the circulation, a higher potency, and good bioavailability after subcutaneous administration. The half-life of octreotide is 1-2 h compared with 2-3 minutes for somatostatin. Consequently, octreotide has largely supplanted somatostatin as a therapeutic agent for several diseases. >> Read More
5. Constitutive and inflammation-dependent antimicrobial peptides produced by epithelium are differentially processed and inactivated by the commensal Finegoldia magna and the pathogen Streptococcus pyogenes
The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects and drug interactions, dosage, availability and cost, and indications for use of octreotide, a new synthetic analogue of the peptide hormone somatostatin (SS), are reviewed. Like SS, octreotide suppresses secretion of pituitary growth hormone (GH) and thyrotropin and decreases release of a variety of pancreatic islet cell hormones including insulin, glucagon, and vasoactive intestinal peptide (VIP). Octreotide also reduces splanchnic blood flow, gastric acid secretion, GI motility, and pancreatic exocrine function and alters the absorption of water, electrolytes, and nutrients from the GI tract. The elimination half-life of i.v. octreotide is 72-98 minutes, compared with 2-3 minutes for i.v. SS. Usual administration of octreotide is by the i.v. or s.c. route. Octreotide has been studied in the treatment of hormone-secreting pituitary tumors and pancreatic islet cell tumors. Octreotide therapy lowers GH secretion and improves clinical symptoms in patients with acromegaly and may suppress clinical symptoms to a greater degree than bromocriptine. Patients with carcinoid syndrome and VIP-secreting tumors (vipomas) have had substantial improvement in clinical symptoms with administration of octreotide. .
Katz, M. D., & Erstad, B. L. (1989). Octreotide, a new somatostatin analogue. Clinical pharmacy, 8(4), 255-273.
While the canonical function of somatostatin (SST) is to inhibit the secretion of growth hormone, it has a number of other physiologic effects that are less widely appreciated. Octreotide, an analog of SST, is not uncommonly used in the critical care setting, particularly for the treatment of variceal hemorrhage. Herein, we discuss the biology and pharmacology of SST, octreotide, and other SST analogs. We also review the evidence behind their use in esophageal variceal bleeds, hepatorenal syndrome, hypoglycemia due to sulfonylurea poisoning, and chylous pleural effusions.
Chan, M. M., Chan, M. M., Mengshol, J. A., Fish, D. N., & Chan, E. D. (2013). Octreotide: a drug often used in the critical care setting but not well understood. Chest, 144(6), 1937-1945.