Octreotide
From PeptidePlaza, the free peptide reference · Entry #1049 · Metabolic · Sources fetched 2026-09-10 · Editorial standards
Octreotide (also known as Octreotida, Octreotidum, Compound 201995, Octreotide Acetate Salt) is a metabolic research peptide. Octreotide is a somatostatin analog indicated for reducing growth hormone and IGF-1 levels in acromegaly, and for managing severe diarrhea and flushing associated with metastatic carcinoid tumors and VIPomas.
Octreotide is a synthetic somatostatin analog that mimics the natural hormone somatostatin. It is FDA-approved and primarily used to reduce blood levels of growth hormone (GH) and insulin growth factor-1 (IGF-1) in patients with acromegaly who have not responded adequately to other treatments. Additionally, it is indicated for the symptomatic treatment of severe diarrhea and flushing episodes associated with metastatic carcinoid tumors and for managing profuse watery diarrhea linked to vasoactive intestinal peptide-secreting tumors (VIPomas). Research on octreotide also includes its use in protein-losing enteropathy and hyperinsulinism, and it has been studied for its delivery systems. It is administered intravenously or subcutaneously.
1 Reported effects
Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.
1.1 Indicated / studied for
- Acromegaly
- Severe diarrhea associated with metastatic carcinoid tumors
- Flushing episodes associated with metastatic carcinoid tumors
- Profuse watery diarrhea associated with VIP-secreting tumors
1.2 Side effects
- Gallbladder abnormalities (stones and/or biliary sludge)
- Sinus bradycardia
- Diarrhea
- Loose stools
- Nausea
- Abdominal discomfort
2 Chemical and physical properties
| CAS number | 83150-76-9 |
|---|---|
| Molar mass | 1019.2 g/mol |
| Purity (typical) | Not independently verified |
| Half-life | ~1.7–1.9 hours |
| Brand names | Octreotide Acetate |
| Route | INTRAVENOUS, SUBCUTANEOUS |
| Storage | −20 °C, lyophilised powder, desiccated |
| Solubility | Sterile water / bacteriostatic water |
2.1 Amino acid sequence
D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-ol (cyclic 2–7 disulfide)
3 Research dosages
50 mcg three times daily during the initial 2 weeks of therapy. Maintenance dose 100 mcg to 500 mcg three times daily.
4 Research studies (8)
- Octreotide and Octreotide-derived delivery systems
Journal of drug targeting (2023) · Review - Use of octreotide for the treatment of protein-losing enteropathy in dogs: Retrospective study of 18 cases
Journal of veterinary internal medicine (2024) - Octreotide
Neonatal network : NN (2006) · Review - Octreotide in hyperinsulinism
The Annals of pharmacotherapy (1997) · Review - Octreotide-induced bradycardia
Pharmacotherapy (1998) · Case Series - Population Pharmacokinetic Analysis of an Octreotide Depot (CAM2029) in the Treatment of Acromegaly
Clinical pharmacokinetics (2025) · RCT - Octreotide in variceal bleeding
Gut (1994) · Meta-Analysis - Octreotide, a new somatostatin analogue
Clinical pharmacy (1989) · Review
5 Safety and risk profile
5.1 Regulatory status
Octreotide is currently classified as FDA approved. Approval applies to specific clinical indications and dosing; research-grade material is not the approved product.
5.2 Contraindications
Conditions and populations in which use is contraindicated:
- Sensitivity to octreotide or any of its components
5.3 Drug interactions
| Drug or class | Interaction | Risk |
|---|---|---|
| Cyclosporine | May decrease blood levels of cyclosporine, potentially leading to transplant rejection. | Moderate |
| Insulin and oral hypoglycemic agents | Octreotide inhibits insulin and glucagon secretion, requiring blood glucose monitoring and anti-diabetic treatment adjustment. | Moderate |
| Bromocriptine | Increases the availability of bromocriptine. | Low |
| Bradycardia-inducing drugs (e.g., beta-blockers) | May have an additive effect on heart rate reduction. | Moderate |
| Drugs metabolized by cytochrome P450 enzymes (especially CYP3A4 with low therapeutic index, e.g., quinidine, terfenadine) | May decrease metabolic clearance of these compounds. | Moderate |
| Lutetium Lu 177 Dotatate Injection | Interferes with efficacy; discontinue octreotide at least 24 hours prior to each dose. | High |
5.4 Long-term risks
- Cardiac Function Abnormalities: increased risk for higher degree of atrioventricular blocks, bradycardia, arrhythmias, or conduction abnormalities
- Cholelithiasis and Complications of Cholelithiasis
- Glucose Metabolism: hypoglycemia or hyperglycemia
- Thyroid Function: hypothyroidism
- Steatorrhea and Malabsorption of Dietary Fats: new onset steatorrhea, stool discoloration, loose stools, abdominal bloating, and weight loss
5.5 Research best practices
- For prolonged storage, store at refrigerated temperatures 2°C to 8°C (36°F to 46°F)
- Store in outer carton to protect from light
- At room temperature (20°C to 30°C or 70°F to 86°F), stable for 14 days if protected from light
- Vials should be opened just prior to administration and the unused portion discarded
6 Frequently asked questions
- What is Octreotide used for?
- Octreotide is used to reduce high levels of growth hormone and IGF-1 in patients with acromegaly. It also treats severe diarrhea and flushing associated with metastatic carcinoid tumors, and profuse watery diarrhea caused by VIP-secreting tumors (VIPomas).
- How does Octreotide work?
- Octreotide is a synthetic analog of somatostatin, a natural hormone. It works by mimicking somatostatin's actions, which include inhibiting the secretion of various hormones such as growth hormone, insulin, glucagon, and certain gastrointestinal peptides, thereby managing the symptoms of conditions like acromegaly and neuroendocrine tumors.
- Is Octreotide FDA approved?
- Yes, Octreotide is an FDA-approved medication. It was first approved in 1988 and is marketed under various names, including Octreotide Acetate Injection, for its indicated uses.
- What are the side effects of Octreotide?
- Common side effects of Octreotide include gallbladder abnormalities like stones or sludge, sinus bradycardia, diarrhea, loose stools, nausea, and abdominal discomfort. Other potential issues include changes in glucose metabolism, thyroid function abnormalities, and steatorrhea.
- How is Octreotide administered?
- Octreotide is administered either intravenously (IV) or subcutaneously (SC). The specific route and dosage depend on the condition being treated and the patient's individual needs, as determined by a healthcare professional.
7 References
- Octreotide — compound summary PubChem. View source
- Octreotide — molecule record ChEMBL. View source
- Octreotide — FDA approved prescribing information U.S. Food and Drug Administration. View source
- Octreotide — published literature (9,339 records) PubMed. View source
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