Octreotide
Also known as: Sandostatin, SMS 201-995
Octreotide is a synthetic somatostatin analog that inhibits growth hormone, glucagon, and insulin release while reducing gastrointestinal secretions. This peptide mimics the effects of naturally occurring somatostatin but with significantly longer duration of action.
Octreotide is a 1019.24 g/mol research peptide. Octreotide is a synthetic somatostatin analog that inhibits growth hormone, glucagon, and insulin release while reducing gastrointestinal secretions. This peptide mimics the effects of naturally occurring somatostatin but with significantly longer duration of action.
Also called: Sandostatin, SMS 201-995
1019.24 g/mol
Molecular Weight
Daltons
4
Strong Evidence
benefits
4
Studies Cited
peer-reviewed
50-200
Typical Dose
mcg
Overview
Octreotide represents a synthetic octapeptide analog of somatostatin, designed to overcome the extremely short half-life of natural somatostatin. The peptide binds to somatostatin receptors (particularly SSTR2 and SSTR5) throughout the body, producing potent inhibitory effects on hormone secretion and cellular proliferation. Unlike endogenous somatostatin which has a half-life of only 2-3 minutes, octreotide maintains biological activity for several hours, making it practical for research applications. The peptide's primary mechanism involves G-protein coupled receptor activation, leading to decreased cyclic adenosine monophosphate (cAMP) levels and subsequent inhibition of hormone release. Octreotide demonstrates particular effectiveness in suppressing growth hormone from pituitary somatotrophs, insulin and glucagon from pancreatic islet cells, and various gastrointestinal hormones including gastrin, vasoactive intestinal peptide, and secretin.
Key Takeaways: Octreotide
- Strongest evidence supports Octreotide for growth hormone suppression and gastrointestinal secretion control
- Research doses typically range from 50 to 200 mcg via subcutaneous
- 4 benefits with strong evidence, 2 moderate, 1 preliminary
- Half-life: 1.7-1.9 hours (subcutaneous)
- 4 cited research studies in this guide
Mechanism of Action
Octreotide binds to somatostatin receptors (SSTR1-5), with highest affinity for SSTR2 and SSTR5 subtypes. Receptor activation triggers inhibitory G-protein signaling pathways, reducing intracellular cAMP levels and calcium influx. This cascade suppresses hormone secretion from target cells, inhibits cellular proliferation, and reduces gastrointestinal motility. The peptide also demonstrates anti-angiogenic properties through VEGF suppression and can induce apoptosis in certain tumor cell lines expressing somatostatin receptors.
Research Benefits
Octreotide at a Glance
Octreotide binds to somatostatin receptors (SSTR1-5), with highest affinity for SSTR2 and SSTR5 subtypes.
Growth Hormone Suppression
Strong EvidencePotently inhibits growth hormone release from pituitary somatotrophs, achieving 70-90% suppression in research models. The mechanism involves direct binding to SSTR2 receptors on somatotroph cells, disrupting growth hormone releasing hormone signaling.
Gastrointestinal Secretion Control
Strong EvidenceSignificantly reduces gastric acid, pancreatic enzyme, and bile secretion through inhibition of gastrin, cholecystokinin, and secretin. Research demonstrates 40-60% reduction in gastric acid output and marked decrease in pancreatic volume.
Tumor Growth Inhibition
Strong EvidenceExhibits antiproliferative effects against neuroendocrine tumors expressing somatostatin receptors. Studies show direct growth inhibition through cell cycle arrest and indirect effects via suppression of growth factors like IGF-1.
Insulin and Glucagon Modulation
Strong EvidenceSuppresses both insulin and glucagon release from pancreatic islet cells, with preferential inhibition of glucagon. This dual action helps stabilize glucose homeostasis in research models of hyperinsulinemia.
Portal Hypertension Reduction
Moderate EvidenceDecreases portal venous pressure through splanchnic vasoconstriction and reduced portal blood flow. Research indicates 20-30% reduction in portal pressure, attributed to decreased cardiac output and splanchnic vasodilation inhibition.
Anti-angiogenic Activity
Moderate EvidenceInhibits new blood vessel formation through VEGF suppression and endothelial cell proliferation inhibition. Studies demonstrate reduced microvessel density in tumor models treated with octreotide.
Neuroprotective Properties
PreliminaryShows protective effects against neuronal damage in models of cerebral ischemia and traumatic brain injury. The mechanism involves reduction of inflammatory cytokines and oxidative stress markers.
Research Dosing Protocols
Research Purposes Only: All content is for informational and research purposes only. This site does not provide medical advice, diagnosis, or treatment. Consult a qualified healthcare professional before using any peptide or supplement.
| Research Protocol | Dose Range | Route |
|---|---|---|
| Growth hormone suppression | 50–200 mcg | subcutaneous |
| Gastrointestinal studies | 100–500 mcg | subcutaneous |
| Tumor research | 150–600 mcg | subcutaneous |
| Portal hypertension models | 25–100 mcg | intravenous |
Frequency
2-3 times daily
Timing
Before meals for GI studies, consistent timing for hormonal research
Cycle Length
7-28 days for acute studies, longer for chronic research protocols
Research Notes
- 1Inject at room temperature to reduce injection site reactions
- 2Rotate injection sites to prevent lipodystrophy
- 3Monitor blood glucose during research due to insulin/glucagon suppression
- 4Doses above 300 mcg may require division into multiple injections
Reconstitution Guide
Standard Reconstitution
Vial Size
100 mg
Bacteriostatic Water
1 mL
Concentration
1000 mcg
per 0.1 mL (10 units)
Step-by-Step Guide
Gather Materials
Octreotide vial, bacteriostatic water, alcohol swabs, insulin syringes.
Equilibrate Temperature
Remove the vial from storage and allow it to reach room temperature (5-10 minutes).
Sanitize
Swab the rubber stopper of both the peptide vial and bacteriostatic water vial with alcohol.
Draw Water
Draw 1 mL of bacteriostatic water into a syringe.
Add Water to Vial
Insert the needle into the peptide vial and direct the water stream against the glass wall — not directly onto the powder.
Mix Gently
Swirl the vial gently until the powder is fully dissolved. Never shake. The solution should be clear and colorless.
Store Properly
Refrigerate at 2-8°C (refrigerated). 28 days refrigerated after reconstitution.
Storage Temperature
2-8°C (refrigerated)
Shelf Life
28 days refrigerated after reconstitution
Important Notes
- •Use bacteriostatic water for multi-dose vials
- •Allow to reach room temperature before injection
- •Do not shake vigorously - gentle swirling only
- •Protect from light during storage
- •Single-use ampules should be used immediately
Octreotide Dosing Calculator
Calculate daily intake, cycle totals, and vials needed with pre-filled protocols →
Octreotide Reconstitution Calculator
Calculate concentration, syringe units, and doses per vial with auto-filled values →
Safety & Side Effects
Reported Side Effects
- !Injection site reactions (pain, swelling, redness)
- !Gastrointestinal disturbances (nausea, diarrhea, abdominal cramps)
- !Cholelithiasis (gallstone formation) with chronic use
- !Hyperglycemia or hypoglycemia due to insulin/glucagon suppression
- !Sinus bradycardia and cardiac conduction abnormalities
- !Hypothyroidism with prolonged administration
- !Malabsorption and steatorrhea
- !Hair loss (alopecia) with chronic use
- !Headache and dizziness
- !Local lipodystrophy at injection sites
Potential Interactions
- ⚡Antidiabetic medications - enhanced hypoglycemic effects require monitoring
- ⚡Beta-blockers and calcium channel blockers - increased risk of bradycardia
- ⚡Cyclosporine - reduced bioavailability requires dose adjustment
- ⚡Oral contraceptives - decreased effectiveness due to altered GI absorption
- ⚡Insulin - unpredictable glucose effects necessitate careful monitoring
Important: Side effects and interactions listed here are compiled from published research and community reports. This is not a complete list. No formal drug interaction studies have been conducted for most research peptides. Always consult a qualified healthcare provider.
Research Studies
The following studies are referenced in this profile. PubMed IDs are provided where available for independent verification.
Octreotide inhibits growth hormone secretion in acromegalic patients
Demonstrated potent growth hormone suppression in patients with acromegaly, with 70-90% reduction in GH levels following subcutaneous octreotide administration.
Effects of octreotide on portal hypertension in patients with cirrhosis
Showed significant reduction in portal venous pressure and hepatic blood flow, with sustained effects lasting 2-4 hours post-injection.
Octreotide therapy for neuroendocrine tumors: efficacy and safety
First major study demonstrating tumor growth inhibition and symptom control in patients with carcinoid syndrome and other neuroendocrine tumors.
Somatostatin receptors in human neuroendocrine tumors
Characterized somatostatin receptor expression patterns in various tumor types, establishing the molecular basis for octreotide's antiproliferative effects.
Note: This is not an exhaustive list of all published research. Studies are selected for relevance and quality. Click PubMed IDs to verify sources independently. Inclusion does not imply endorsement of the peptide for any clinical use.
Frequently Asked Questions
Octreotide has a half-life of approximately 1.7-1.9 hours when given subcutaneously, with effects lasting 6-12 hours. Complete elimination typically occurs within 24-48 hours, though metabolites may persist longer.
Octreotide is a synthetic analog of natural somatostatin with much longer duration of action. While somatostatin has a half-life of 2-3 minutes, octreotide lasts several hours, making it practical for research applications.
Yes, octreotide can cause both hypoglycemia and hyperglycemia by suppressing insulin and glucagon release. The net effect depends on the balance between these hormones and individual metabolic status.
Reconstituted octreotide should be refrigerated at 2-8°C and used within 28 days. Allow it to reach room temperature before injection to reduce discomfort and injection site reactions.
The most frequent side effects include injection site reactions, gastrointestinal disturbances (nausea, diarrhea), and glucose metabolism changes. Gallstone formation may occur with chronic use.
Octreotide can be administered subcutaneously or intravenously depending on the research protocol. Subcutaneous injection is most common due to better bioavailability and sustained effects.
Growth hormone suppression begins within 30 minutes of injection, reaches maximum effect at 1-2 hours, and can last 6-12 hours depending on the dose administered.
Octreotide may cause sinus bradycardia and conduction abnormalities, particularly in research subjects with pre-existing cardiac conditions. Heart rate monitoring is recommended during studies.
Research & Educational Use Only
All content is for informational and research purposes only. This site does not provide medical advice, diagnosis, or treatment. Consult a qualified healthcare professional before using any peptide or supplement.
The information presented here is compiled from published research studies and is intended for informational purposes only. Individual results may vary. Always consult with a licensed healthcare provider.