Octreotide
Octreotide (Synthetic Somatostatin Analog)
Synthetic Somatostatin Analog for Hormonal Health
What is Octreotide?
Octreotide is a synthetic octapeptide analog of somatostatin, the endogenous hypothalamic hormone that broadly inhibits the secretion of multiple other hormones throughout the body. The natural somatostatin molecule has a half-life of only 1-3 minutes in circulation, making it impractical for therapeutic use. Octreotide was engineered to be pharmacologically equivalent to somatostatin while achieving a half-life of approximately 1.7 hours (immediate-release) or weeks (depot formulation), enabling effective hormonal management in clinical settings.
Octreotide binds with high affinity to somatostatin receptor subtype 2 (SSTR2) and with lesser affinity to SSTR3 and SSTR5. This receptor binding profile closely mirrors natural somatostatin activity and produces inhibition of a wide range of secretory hormones: growth hormone (GH), glucagon, insulin, gastrin, cholecystokinin, secretin, vasoactive intestinal peptide (VIP), thyroid-stimulating hormone (TSH), and pancreatic polypeptide. It also reduces intestinal fluid secretion, slows gastrointestinal motility, and inhibits gallbladder contraction.
FDA-approved indications include acromegaly (excess GH secretion from a pituitary adenoma), carcinoid syndrome associated with metastatic carcinoid tumors, and symptoms from vasoactive intestinal peptide-secreting tumors (VIPomas). In acromegaly, octreotide suppresses GH secretion and reduces circulating insulin-like growth factor-1 (IGF-1) levels. Long-term treatment can stabilize and sometimes reduce pituitary tumor volume.
Beyond approved uses, octreotide is investigated in off-label contexts including prevention of post-operative pancreatic complications, management of gastrointestinal bleeding from portal hypertension, treatment of dumping syndrome, and as a component of peptide receptor radionuclide therapy (PRRT) protocols for neuroendocrine tumors. It has the longest-established efficacy and safety profile within the somatostatin analog class.
Research Supply
Source high-purity Octreotide for your research
Dosage Guide
Route: Subcutaneous injection (immediate-release) or intramuscular depot injection
Dosing Schedule
| Period | Dose |
|---|---|
| Acromegaly (starting) | 50 mcg three times daily (TID) subcutaneous; titrate to 100-250 mcg TID over 2-4 weeks |
| Carcinoid/VIPoma | 100-600 mcg/day in 2-4 divided doses; 150 mcg TID median maintenance |
| Maximum reported (divided doses) | Up to 1,500 mcg/24 hours with monitoring |
| Sandostatin LAR depot 10 mg | 10 mg IM every 28 days |
| Sandostatin LAR depot 20 mg | 20 mg IM every 28 days |
| Sandostatin LAR depot 30 mg | 30 mg IM every 28 days |
Reconstitution
Injection Volumes
| Dose | Volume | Syringe Units |
|---|
Administration Tips
- Warm immediate-release solution to room temperature before injection to reduce discomfort
- Inject subcutaneously; rotate sites to minimize lipodystrophy
- The depot formulation must be administered by a healthcare professional into the gluteal muscle
- Avoid inadvertent IV or subcutaneous administration of the depot suspension
- Establish clinical response and tolerability with immediate-release before transitioning to depot formulation
Risks & Side Effects
Commonly Reported
Serious Risks
Gallstones (cholelithiasis)
Octreotide reduces gallbladder contractility, leading to bile stasis and stone formation. Prevalence increases significantly with chronic use. Monitor with ultrasound periodically.
Hypoglycemia or hyperglycemia
Octreotide suppresses both insulin and glucagon; the net glycemic effect is variable and requires monitoring, particularly in diabetic patients.
Bradycardia and conduction abnormalities
QT prolongation risk; monitor with ECG in at-risk patients.
Hypothyroidism
Risk increases with long-term use due to TSH suppression.
Pancreatitis
Rare, reported with somatostatin analog class.
Cardiac valve disorders
Documented more prominently with lanreotide; data for octreotide limited but warrants monitoring with long-term use.
Contraindications
- Known hypersensitivity to octreotide or any component of the formulation
- Caution with insulin-dependent diabetes mellitus (requires dose adjustment and glucose monitoring)
- Caution with cardiac conduction disorders (bradycardia, QT prolongation risk)
- Caution with hypothyroidism (TSH suppression effect may worsen subclinical hypothyroidism)
- Pregnancy (limited data; use only if clearly necessary and benefits outweigh risks)
Frequently Asked Questions
Related Peptides
Experts Covering Octreotide
LEGAL DISCLAIMER
The information provided on this page is for educational and informational purposes only and is not intended as medical advice. Octreotide is FDA-approved for specific indications including acromegaly and carcinoid tumors; all other uses described here are investigational or off-label. Always consult with a qualified healthcare professional before starting any peptide therapy. Individual results may vary. Peptides Institute is not responsible for any adverse effects resulting from the use of information provided on this site.