Somatostatin Analogues in Pharmacotherapy: Introduction

Somatostatin inhibits a variety of physiological functions in the gastrointestinal tract, like gastrointestinal motility, gastric acid production, pancreatic enzyme secretion, and bile and colonic fluid secretion. It inhibits the secretion of pancreatic and intestinal hormones like insulin, glucagon, secretin, and vasoactive intestinal polypeptide. The multiple simultaneous effects of pharmacological concentrations of somatostatin in different organs, the need for intravenous administration, the short duration of action (a half-life in the circulation of less than 3 min), and the postinfusion rebound hypersecretion of hormones considerably hampered the initial enthusiasm, as well as its clinical use. Octreotide acetate was the first octapeptide somatostatin analogue that was synthesized. Expression of somatostatin receptors by endocrine tumors is essential for the control of hormonal hypersecretion by the octapeptide somatostatin analogues.

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