Octreotide
Also known as: Sandostatin, Sandostatin LAR, CAM2029, SMS 201-995, octreotide acetate, octreotide LAR depot
Synthetic somatostatin analog; cyclic octapeptide; hormonal antineoplastic and antisecretory agent
What it is
Octreotide (brand name Sandostatin) is a prescription injection used by people with acromegaly, carcinoid tumors, and other hormone-secreting neuroendocrine tumors. It mimics a natural hormone that tells the body to stop releasing excess growth hormone and other substances that cause symptoms. It has been FDA-approved since 1988 and is available in short-acting and long-acting depot formulations.
The scientific side
Octreotide is described as a synthetic cyclic octapeptide analog of the naturally occurring inhibitory hormone somatostatin (also known as somatotropin release-inhibiting factor). While native somatostatin has a plasma half-life of less than two minutes due to rapid enzymatic degradation, octreotide's structural modifications confer a substantially longer duration of action, making it clinically practical. Octreotide exerts its effects primarily through high-affinity binding to somatostatin receptor subtypes (predominantly SSTR2 and SSTR5), which are widely expressed on neuroendocrine tumor cells, pituitary somatotrophs, and throughout the gastrointestinal tract. Activation of these receptors triggers intracellular signaling cascades — principally Gi protein coupling leading to reduced adenylyl cyclase activity, decreased cyclic AMP, and inhibition of calcium influx — that suppress hormone secretion and can induce cytostatic effects on tumor cells. In acromegaly, octreotide suppresses excessive pituitary growth hormone (GH) secretion and thereby normalizes downstream insulin-like growth factor-1 (IGF-1) levels, which are the mediators of the disease's systemic manifestations. In neuroendocrine tumors such as carcinoid tumors and VIPomas, octreotide suppresses the hypersecretion of vasoactive peptides (serotonin, vasoactive intestinal peptide, substance P) responsible for flushing, diarrhea, and other symptomatic features. In the portal circulation, octreotide reduces splanchnic arterial blood flow and portal venous pressure through vasoconstriction of mesenteric vessels, providing hemostatic benefit in variceal bleeding without reducing cardiac output. Additionally, octreotide possesses direct antiproliferative and antiangiogenic properties against tumor cells bearing somatostatin receptors, evidenced by objective tumor regression in metastatic neuroendocrine tumors treated with somatostatin analogs as monotherapy. Its ability to target somatostatin-receptor-expressing tumors has also been leveraged for diagnostic imaging with radiolabeled analogues and as a vehicle for targeted radiotherapy.
Class: Synthetic somatostatin analog; cyclic octapeptide; hormonal antineoplastic and antisecretory agent
Administration & storage
- Administration
- Subcutaneous injection (preferred route for outpatient use): abdomenthighor buttock; rotate sitesIntravenous bolus followed by continuous IV infusion: used acutely for variceal bleeding in hospital settingsDeep intramuscular injection into gluteal muscle: long-acting depot formulations administered by healthcare professional onlySubcutaneous depot injection (CAM2029 formulation): self-administered once monthly — studied in Phase 3 acromegaly trial (PMID: 39378125)
- Storage
- Short-acting multidose vials: refrigerate at 2–8°C; once opened, stable at room temperature (<25°C) for up to 2 weeks. Ampules: stable at room temperature for 24 hours when protected from light. Long-acting depot kit: refrigerate at 2–8°C; bring to room temperature 30–60 minutes before preparation; do not freeze.
- Cautions
- Cholelithiasis (gallstones): somatostatin analogs reduce gallbladder motility and alter bile composition; gallstones develop in up to 50% of patients on long-term octreotide therapy; periodic ultrasound surveillance recommended,Bradycardia and cardiac conduction abnormalities: octreotide can cause bradycardia, particularly in patients with pre-existing cardiac disease; monitor heart rate and ECG; use with caution alongside beta-blockers or calcium channel blockers,Hypoglycemia or hyperglycemia: octreotide suppresses both insulin and glucagon; glucose dysregulation is possible, particularly at initiation; blood glucose should be monitored, especially in diabetic patients,Hypothyroidism: long-term use is associated with reduced TSH secretion; thyroid function should be monitored periodically,Injection site reactions: pain, burning, stinging common at SC injection sites; typically transient,Gastrointestinal: nausea, diarrhea, abdominal discomfort, and steatorrhea are common, especially early in therapy; usually self-limiting,Neonatal necrotizing enterocolitis: reported in premature neonates receiving IV octreotide for chylothorax; risk-benefit assessment required in this population
Legal & regulatory status
FDA-approved (NDA) as Sandostatin (octreotide acetate) injection since 1988 for: (1) acromegaly to reduce GH and IGF-1 levels; (2) symptomatic treatment of metastatic carcinoid tumors; (3) vasoactive intestinal…
Octreotide is not explicitly listed on the WADA Prohibited List as a banned substance in sport. However, somatostatin analogs that suppress growth hormone secretion have been reviewed in anti-doping contexts. Athletes…
Approved by Health Canada as Sandostatin (octreotide acetate) for acromegaly, carcinoid tumors, and VIPomas. Long-acting formulation (Sandostatin LAR) also approved. Available on a prescription basis across Canadian…
What it's studied for
- Acromegaly — growth hormone and IGF-1 normalization Phase III RCT
- Carcinoid tumors and neuroendocrine tumors — symptom control and antiproliferative effect Mixed
- Variceal bleeding and portal hypertension — hemostasis Human RCT
- Angiodysplasia-related gastrointestinal bleeding — transfusion reduction Human RCT
- Prevention of postoperative pancreatic fistula after pancreatectomy Human RCT
- Chylothorax — reduction of lymphatic drainage Human observational
- Hyperinsulinism — blood glucose stabilization Human observational
Safety signals
- Cholelithiasis (gallstone formation)
- Bradycardia and cardiac conduction disturbances
- Glucose dysregulation (hypoglycemia and hyperglycemia)
- Gastrointestinal adverse effects (nausea, diarrhea, steatorrhea, abdominal pain)
- Hypothyroidism (with long-term use)
- Injection site pain and reactions
- Neonatal necrotizing enterocolitis
Contraindications
About these dose ranges
Dose ranges below reflect commonly reported community protocols. Where published research cites a specific dose, the PMID is linked. Doses without citations are not clinical recommendations — they reflect what practitioners and researchers commonly report using.
Community-reported dosing
| Route | Dose | Frequency / Duration | Population / context | Source tier |
|---|---|---|---|---|
| Unspecified | 50–600 µg subcutaneous injection per day | — | Adults with acromegaly (short-acting) | Research |
| Unspecified | 10–40 mg intramuscular injection | — | Adults with acromegaly (long-acting depot — Sandostatin LAR) | Research |
| Unspecified | 100–600 µg subcutaneous injection per day | — | Adults with carcinoid tumors (short-acting) | Research |
| Unspecified | 20–30 mg intramuscular injection | — | Adults with carcinoid tumors (long-acting depot) | Research |
| Unspecified | 25–50 µg bolus followed by 25–50 µg/hour | — | Adults with acute variceal hemorrhage (IV) | Research |
| Unspecified | 20 mg intramuscular depot | — | Adults with angiodysplasia-related bleeding (OCEAN trial) | Research |
| Unspecified | 1–10 µg/kg/hour IV or 5–40 µg/kg/day SC | — | Neonates/infants with chylothorax | Research |
| Subcutaneous injection (short-acting); deep intramuscular injection (long-acting depot) | Short-acting: 50 µg SC TID titrated to 100–200 µg SC TID; Long-acting depot: 20 mg IM every 4 weeks | TID for short-acting; every 4 weeks for depot | Adults with acromegaly initiating medical therapy or transitioning from surgery/radiation | |
| Subcutaneous injection (short-acting); deep intramuscular injection (long-acting depot) | Short-acting: 100–200 µg SC TID; Long-acting depot: 20–30 mg IM every 4 weeks | TID for short-acting; every 4 weeks for depot | Adults with symptomatic metastatic carcinoid tumors or other functional neuroendocrine tumors (VIPomas, glucagonomas) | |
| Intravenous | 50 µg IV bolus, then 25–50 µg/hour continuous IV infusion | Continuous infusion | Adults with acute esophageal variceal hemorrhage in hospital setting |