Octreotide

Summary

Octreotide is a synthetic octapeptide analogue of natural somatostatin with a longer half-life. It is used to treat acromegaly, carcinoid tumors, VIPomas, and to manage bleeding from esophageal varices. Available in immediate-release and long-acting formulations (LAR).

Mechanism of Action

Binds to somatostatin receptors (primarily SSTR2 and SSTR5), inhibiting the release of growth hormone, insulin, glucagon, gastrin, and other gastrointestinal hormones; also reduces splanchnic blood flow and portal pressure.

Routes of Administration

Goals & Uses

• Esophageal variceal bleedingGastroenterologyHigh
• Acromegaly managementEndocrinologyHigh
• Neuroendocrine tumor (NET) antiproliferative therapyOncologyHigh
• Carcinoid syndrome symptom controlOncology/GastroenterologyHigh
• Dumping syndrome managementGastroenterologyModerate
• VIPoma managementOncology / NeuroendocrineHigh

Contraindications

• Hypersensitivity to octreotide or excipientsAllergyHigh
• Pregnancy (relative)ReproductiveModerate

Adverse Effects

• Gastrointestinal disturbances (nausea, diarrhea, abdominal pain)GastrointestinalCommon
• Cholelithiasis / gallstonesGastrointestinalCommon
• Injection site reactionsLocalCommon
• Bradycardia / cardiac conduction abnormalitiesCardiovascularUncommon
• Hypoglycemia or hyperglycemiaMetabolicUncommon
• HypothyroidismEndocrineUncommon

Drug Interactions

• QT-prolonging drugs (e.g., amiodarone, sotalol)Moderate
• Insulin / Oral antidiabeticsModerate
• Beta-blockersModerate
• CyclosporineModerate
• BromocriptineLow

Population Constraints

• PregnancyReproductive SafetyRelative
• Hepatic impairment (cirrhosis)Organ ImpairmentRelative
• Renal impairmentOrgan ImpairmentRelative
• Pediatric patientsAgeRelative
• Diabetic PatientsMetabolicRelative
• BreastfeedingReproductiveRelative

Regulatory Status

• European UnionApprovedApproved: Acromegaly, Carcinoid tumors, VIPomas, Prevention of complications after pancreatic surgeryEMA-approved; LAR formulation also approved. Additional indication for pancreatic surgery prophylaxis in some EU countries.
• United StatesApprovedApproved: Acromegaly, Carcinoid tumors (symptom control), VIPomas (symptom control)FDA-approved for both immediate-release (Sandostatin) and LAR (Sandostatin LAR Depot) formulations. Orphan drug designation for certain NETs.
• United KingdomApprovedApproved: Acromegaly, Carcinoid tumors, VIPomas, Prevention of complications after pancreatic surgeryMHRA-approved; aligns largely with EU labeling post-Brexit.

FDA-approved for acromegaly, carcinoid tumors, and VIPomas. Long-acting release (LAR) formulation also approved. Designated orphan drug for certain indications.

Evidence & Sources

No sources recorded yet.