Approved & therapeutic
Octreotide
Sandostatin
Octreotide is a synthetic octapeptide analogue of somatostatin, approved in the US for acromegaly and for the severe diarrhea and flushing associated with metastatic carcinoid tumours and VIPomas. It resists degradation far better than natural somatostatin, which is what makes it usable as a drug.
Also known as: Sandostatin LAR, SMS 201-995
- Status
- Octreotide is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- Roughly 1.5 to 2 hours after subcutaneous injection of the immediate-release form, versus 1 to 3 minutes for endogenous somatostatin. The depot formulation releases over approximately 4 weeks.
- How it's taken
- Subcutaneous or intravenous injection; long-acting depot given intramuscularly
- Mechanism
- Other
- Pathways
- GH axis
How Octreotide works
Octreotide binds somatostatin receptors, with highest affinity for SSTR2 and useful affinity for SSTR5. Activation suppresses release of growth hormone, and also of glucagon, insulin, gastrin, VIP and serotonin. In acromegaly this lowers GH and consequently IGF-1; in functional neuroendocrine tumours it suppresses the hormone driving the symptoms.
What research has looked at
- In acromegaly the label describes reduction of growth hormone and IGF-1 levels, used where surgery or radiotherapy has not produced adequate control or as an interim measure.
- In carcinoid syndrome it reduces the frequency of diarrhea and flushing episodes driven by tumour secretion. This is symptom control, not antitumour therapy.
- In VIPoma it reduces the severe secretory diarrhea caused by vasoactive intestinal peptide.
- A long-acting depot formulation allows monthly intramuscular dosing once a patient has been stabilised on the immediate-release form.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- Gallbladder abnormalities are common with prolonged use — cholelithiasis, biliary sludge and, less often, cholecystitis and pancreatitis. Periodic gallbladder ultrasound is advised on long-term therapy.
- Both hyperglycemia and hypoglycemia occur, because octreotide suppresses insulin and glucagon simultaneously. Patients with diabetes may need their insulin or oral agents adjusted.
- Bradycardia, conduction abnormalities and arrhythmias have been reported, particularly in acromegaly.
- Injection-site pain, abdominal cramping, flatulence, nausea, loose stools and steatorrhea are frequent, especially early in treatment.
- Hypothyroidism has been reported with chronic use; thyroid function monitoring is recommended.
- Vitamin B12 deficiency has been reported with long-term use.
Sources
- FDA approved-drug listing for octreotide · U.S. Food & Drug Administration
- DailyMed prescribing information for octreotide · NIH · DailyMed
- PubMed research on octreotide acromegaly carcinoid · NIH · National Library of Medicine
- DrugBank record for octreotide · DrugBank
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Related compounds
Octreotide FAQ
What is Octreotide?
Octreotide is a synthetic octapeptide analogue of somatostatin, approved in the US for acromegaly and for the severe diarrhea and flushing associated with metastatic carcinoid tumours and VIPomas. It resists degradation far better than natural somatostatin, which is what makes it usable as a drug.
How does Octreotide work?
Octreotide binds somatostatin receptors, with highest affinity for SSTR2 and useful affinity for SSTR5. Activation suppresses release of growth hormone, and also of glucagon, insulin, gastrin, VIP and serotonin. In acromegaly this lowers GH and consequently IGF-1; in functional neuroendocrine tumours it suppresses the hormone driving the symptoms.
Is Octreotide FDA approved?
Yes. Octreotide is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Octreotide?
Reported half-life: Roughly 1.5 to 2 hours after subcutaneous injection of the immediate-release form, versus 1 to 3 minutes for endogenous somatostatin. The depot formulation releases over approximately 4 weeks.
How is Octreotide taken?
Subcutaneous or intravenous injection; long-acting depot given intramuscularly.
What side effects have been reported with Octreotide?
Reported in the sources: Gallbladder abnormalities are common with prolonged use — cholelithiasis, biliary sludge and, less often, cholecystitis and pancreatitis. Periodic gallbladder ultrasound is advised on long-term therapy; Both hyperglycemia and hypoglycemia occur, because octreotide suppresses insulin and glucagon simultaneously. Patients with diabetes may need their insulin or oral agents adjusted; Bradycardia, conduction abnormalities and arrhythmias have been reported, particularly in acromegaly; Injection-site pain, abdominal cramping, flatulence, nausea, loose stools and steatorrhea are frequent, especially early in treatment; Hypothyroidism has been reported with chronic use; thyroid function monitoring is recommended; Vitamin B12 deficiency has been reported with long-term use.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.