From the Guidelines
Octreotide is a synthetic somatostatin analog that acts by binding to somatostatin receptors throughout the body, primarily inhibiting the release of various hormones, as demonstrated in the most recent study 1. The action of octreotide involves suppressing the secretion of growth hormone, insulin, glucagon, gastrin, and other peptides produced in the gastrointestinal tract. This medication is commonly used to treat conditions characterized by excessive hormone production, such as acromegaly, carcinoid tumors, and vasoactive intestinal peptide tumors (VIPomas). Some key points about octreotide include:
- It is used to control symptoms and tumor growth in patients with neuroendocrine tumors (NETs) and carcinoid syndrome, as shown in studies 1.
- The medication is typically administered via subcutaneous or intravenous injection, with dosing dependent on the specific condition being treated.
- Side effects may include injection site pain, gastrointestinal disturbances, and potential gallstone formation with long-term use.
- The drug's effectiveness stems from its ability to mimic natural somatostatin but with a significantly longer half-life, allowing for more practical clinical application, as noted in 1. The most recent study 1 provides guidance on the use of octreotide in patients with NETs and carcinoid syndrome, including dosing and administration recommendations. Overall, octreotide is a valuable treatment option for patients with conditions characterized by excessive hormone production, and its use should be guided by the most recent and highest-quality evidence, such as that provided in 1.
From the FDA Drug Label
Octreotide acetate injection exerts pharmacologic actions similar to the natural hormone, somatostatin. It is an even more potent inhibitor of growth hormone (GH), glucagon, and insulin than somatostatin Like somatostatin, it also suppresses luteinizing hormone (LH) response to gonadotropin releasing hormone (GnRH), decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, vasoactive intestinal peptide (VIP), secretin, motilin, and pancreatic polypeptide
The action of Octreotide (Somatostatin analogue) is to inhibit the release of various hormones, including:
- Growth hormone (GH)
- Glucagon
- Insulin
- Luteinizing hormone (LH)
- Serotonin
- Gastrin
- Vasoactive intestinal peptide (VIP)
- Secretin
- Motilin
- Pancreatic polypeptide It also decreases splanchnic blood flow 2
From the Research
Action of Octreotide
The action of Octreotide, a somatostatin analogue, can be described as follows:
- Inhibits the release of anterior pituitary growth hormone and thyroid-stimulating hormone 3
- Inhibits the release of peptides of the gastroenteropancreatic endocrine system 3, 4
- Reduces splanchnic blood flow, gastric acid secretion, GI motility, and pancreatic exocrine function 4
- Alters the absorption of water, electrolytes, and nutrients from the GI tract 4
- Binds to somatostatin receptor subtypes 2 and 5 with high potency to reduce the production and secretion of growth hormone (GH) and insulin-like growth factor (IGF)-I 5
Therapeutic Effects
The therapeutic effects of Octreotide include:
- Effective in the treatment of acromegaly and thyrotrophinomas 3
- Provides a significant advantage over existing therapies in the management of the carcinoid syndrome 3
- Effective in reversing carcinoid crises 3
- Effective in reducing stool/fistula output in patients with high-output secretory diarrhoea 3
- Improves facial appearance and soft tissue thickening, and eliminates or reduces the incidence of symptoms such as headache, fatigue, arthralgia and excessive perspiration in patients with acromegaly 6, 7
Administration and Tolerability
Octreotide can be administered:
- Subcutaneously 3, 4
- Intramuscularly once every 28 days (Octreotide LAR) 6, 7, 5 The most commonly occurring adverse events are:
- Gastrointestinal or hepatobiliary in nature 6, 7, 5
- Pain at the site of injection and gastrointestinal symptoms such as abdominal cramps, nausea, bloating, flatulence, diarrhoea and steatorrhoea 3