Sandostatin LAR Octreotide Acetate Microspheres for Injection

1. Indications and Usage
Acromegaly: Treatment of adult patients who have not responded to or have relapsed after surgery or radiotherapy, or who prefer medical therapy, provided their symptoms are controlled by standard subcutaneous octreotide.
Gastroenteropancreatic Neuroendocrine Tumors (GEP-NETs): Treatment of patients with symptomatic carcinoid tumors (carcinoid syndrome) and functional pancreatic tumors (e.g., VIPomas, glucagonomas, gastrinomas/Zollinger-Ellison syndrome, insulinomas).
2. Dosage and Administration
Route of Administration: For Deep Intramuscular (IM) Injection ONLY (buttock muscle). Deep IV injection must not be used.
Recommended Dosage:
Acromegaly: Initial dose is 20 mg every 4 weeks for 3 months. If not controlled (GH >2.5 μg/L), increase to 30 mg. If well controlled (GH <1.0 μg/L and normal IGF-1), may decrease to 10 mg.
GEP-NETs: Initial dose is 20 mg every 4 weeks. If not controlled after 3 months, increase to 30 mg. If controlled, may decrease to 10 mg.
Critical Administration Instructions:
Preparation: The vial must reach room temperature (30 min to 24 h) before preparation. After adding the suspension vehicle, let stand upright for 5 min, then gently rotate for ≥30 s to form a uniform suspension.
Timing: The suspension must be used immediately prior to administration.
3. Mechanism of Action
Somatostatin Receptor Agonism: Octreotide is a synthetic polypeptide analogue of natural somatostatin.
Hormonal Suppression: It binds with high affinity to somatostatin receptors (particularly subtypes 2 and 5) on neuroendocrine cells, inhibiting the secretion of growth hormone (GH), insulin, glucagon, and various gastrointestinal peptides.
4. Safety and Warnings
Cholelithiasis: Long-term use may cause gallstones and biliary sludge due to reduced gallbladder contractility. Biliary ultrasound is recommended before initiation and every 6 months during treatment.
Glucose Metabolism: Can cause disturbances in glucose homeostasis, leading to both hyperglycemia and hypoglycemia.
Gastrointestinal Effects: Can cause nausea, abdominal pain, diarrhea, and constipation. Rarely, symptoms mimicking acute intestinal obstruction may occur.
Thyroid Function: May lead to mild, reversible reductions in thyroid-stimulating hormone (TSH) and thyroid hormones.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Injection site reactions (pain, erythema, induration), gastrointestinal symptoms (diarrhea, nausea, abdominal pain, flatulence), headache, and gallstones.
Clinical Research Highlights: Clinical studies demonstrate that the microspheres provide sustained plasma concentrations of octreotide, significantly reducing the frequency of injections from multiple times daily to once every 4 weeks while maintaining biochemical and clinical control.
6. Drug Interactions
Cyclosporine and Cimetidine: Octreotide may decrease the intestinal absorption of cyclosporine and delay the absorption of cimetidine.
Insulin and Oral Hypoglycemics: Due to the inhibition of insulin secretion, concurrent use with antidiabetic agents requires close monitoring and potential dose adjustments.
Beta-Blockers: May enhance the bradycardic effect of beta-blockers.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Octreotide Acetate. Excipients: Poly(lactic-co-glycolic acid) (PLGA) microspheres, sodium carboxymethylcellulose, poloxamer 188, mannitol.
Appearance: White to off-white powder. Forms a milky white suspension after mixing with the vehicle.
Packaging: Single-use vial (10 mg, 20 mg, or 30 mg calculated as octreotide acetate).
Storage: Store in the original carton at 2°C to 8°C. Do not freeze.