Bone & endocrine

Octreotide

The first synthetic somatostatin analogue, approved for acromegaly, neuroendocrine tumours and variceal bleeding.

Moderate evidenceApproved drugAdd to compare
01

What it is

Octreotide is a synthetic eight-amino-acid analogue of somatostatin. It activates somatostatin receptors, mainly subtypes 2 and 5, which broadly inhibit hormone secretion and gut motility, and it resists enzymatic breakdown far better than the natural hormone. It comes as a short-acting subcutaneous injection and as a monthly long-acting depot (octreotide LAR).

02

How it works

  1. 1

    Activates somatostatin receptors SSTR2 and SSTR5 on pituitary and neuroendocrine tumour cells, suppressing hormone release.

  2. 2

    Inhibits secretion of growth hormone, gastrin, VIP, glucagon, insulin and serotonin.

  3. 3

    Reduces splanchnic blood flow, lowering portal pressure.

  4. 4

    Slows gut transit and reduces exocrine pancreatic and intestinal secretion.

  5. 5

    The depot formulation releases slowly from polymer microspheres over about four weeks.

03

What it's studied for

Acromegaly
Carcinoid syndrome and other functioning neuroendocrine tumours
VIPoma and glucagonoma
Acute variceal bleeding as an adjunct
Secretory diarrhoea and high-output stomas
TSH-secreting pituitary adenoma
04

Reported and studied effects

  • Falls in growth hormone and IGF-1 in acromegaly, with biochemical control in roughly half of patients
  • Rapid relief of flushing and diarrhoea in carcinoid syndrome
  • Lower portal pressure during bleeding
  • Gallstones and biliary sludge over months of use
  • Slower progression of tumour markers, though not reliably tumour shrinkage

Research protocol notes

Research context only

Research context only - prescription medicine. Short-acting octreotide is typically 50 to 200 micrograms subcutaneously two to three times daily, with higher doses used in carcinoid crisis, while the long-acting depot is commonly 20 to 30 mg intramuscularly every four weeks after a short-acting run-in. Acromegaly endpoints are measured over months, and gallbladder ultrasound is routine during long-term use.

These figures are described so you can understand what researchers did. They are not a dose, a schedule, or a suggestion — and they are not a substitute for a doctor.

05

Possible side effects and contraindications

Safety profile

Possible side effects

  • Gallstones and biliary sludge
  • Diarrhoea and steatorrhoea
  • Abdominal pain and nausea
  • Glucose swings, both hyperglycaemia and hypoglycaemia
  • Bradycardia
  • Injection-site pain
  • Hypothyroidism with long-term use

Contraindications and cautions

  • Prior hypersensitivity to octreotide
  • Uncontrolled diabetes needs close monitoring rather than avoidance
  • Cardiac conduction abnormalities need caution
  • Pregnancy only if clearly needed

A side-effect list is never complete, and these are not the only situations that warrant caution. Anything unexpected, or anything you are unsure about, should be discussed with a doctor before use.

06

Evidence assessment

Moderate evidenceSeveral human trials, some inconsistencies
Several human trials, some inconsistencies

Long clinical use and consistent biochemical or symptom endpoints, but most acromegaly and neuroendocrine trials are small and open-label rather than large placebo-controlled studies.

07

References

  1. 01European Medicines Agency - Sandostatin product information
  2. 02Melmed et al., Guidelines for acromegaly management, Journal of Clinical Endocrinology and Metabolism 2009

References link to published literature, regulator pages or literature indexes. Where a link points to a search, it collects the peer-reviewed work on that molecule rather than a single study.