Sandostatin LAR Octreotide Acetate Microspheres for Injection

1. Indications and Usage
Acromegaly:
Indicated for the long-term treatment of patients with acromegaly who have had an inadequate response to, or cannot be treated with, surgery and/or radiotherapy. It is used to reduce Growth Hormone (GH) and IGF-1 levels and improve symptoms (e.g., headache, joint pain, sweating).
Gastroenteropancreatic Neuroendocrine Tumors (GEP-NETs):
Indicated for the symptomatic control of patients with functional gastroenteropancreatic endocrine tumors, including:
Carcinoid tumors: To inhibit tumor secretion of serotonin and other substances, relieving flushing and diarrhea.
VIPomas: To control severe secretory diarrhea and electrolyte imbalance.
Glucagonomas: To improve necrolytic migratory erythema and diarrhea.
2. Dosage and Administration
Route of Administration:
For Deep Gluteal Intramuscular Injection ONLY.
Reconstitution: Must be reconstituted immediately before use with the supplied diluent (sodium carboxymethylcellulose). Do not use other substances.
Injection Site: Alternating buttocks (left and right) should be used for repeated injections.
Recommended Dosage:
Acromegaly: The recommended starting dose is 20 mg every 4 weeks for 3 months. Dosage adjustment (10 mg or 30 mg) should be based on serum GH and IGF-1 levels and clinical response.
GEP-NETs: The recommended starting dose is 20 mg every 4 weeks.
Transition from Short-Acting: For patients switching from octreotide acetate injection (short-acting), the first injection of the microsphere formulation should be overlapped with the short-acting formulation for at least 2–3 weeks to ensure adequate coverage during the lag phase of drug release.
3. Mechanism of Action
Synthetic Analogue:
Octreotide is a synthetic octapeptide analogue of naturally occurring somatostatin.
Inhibition of Secretion:
It has similar pharmacological effects to somatostatin but with greater potency and a significantly longer duration of action. It inhibits the pathological secretion of growth hormone (GH), gastrin, vasoactive intestinal peptide (VIP), glucagon, and insulin.
Microparticle Technology:
The microsphere formulation utilizes biodegradable polymer technology to release the drug gradually over 4 weeks, providing sustained therapeutic plasma concentrations.
4. Safety and Warnings
Gallbladder Abnormalities:
Long-term treatment may result in the formation of gallstones (cholelithiasis) due to inhibition of gallbladder contractility and bile secretion. Ultrasound screening is recommended periodically (e.g., every 6–12 months).
Glucose Regulation:
Since Octreotide inhibits both insulin and glucagon secretion, it may alter glucose tolerance. Hypoglycemia or hyperglycemia may occur; blood glucose should be monitored, especially in diabetic patients.
Injection Site Reactions:
Pain, swelling, or rash at the injection site are common but usually transient.
5. Adverse Reactions
Gastrointestinal:
Nausea, vomiting, abdominal pain, diarrhea, steatorrhea, and flatulence.
Hepatobiliary:
Cholelithiasis (gallstones), cholestasis.
Metabolic:
Hyperglycemia, hypoglycemia.
Dermatological:
Alopecia (hair loss), rash.
6. Drug Interactions
Cyclosporine:
Octreotide may decrease intestinal absorption of cyclosporine, potentially requiring dose adjustments.
Bromocriptine:
Octreotide may increase the bioavailability of bromocriptine.
Antidiabetic Agents:
Dose adjustments of insulin or oral hypoglycemic agents may be required during treatment.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Octreotide acetate.
Excipients: Poly(d,l-lactide-co-glycolide) (PLGA), mannitol, sodium carboxymethylcellulose.
Appearance: White to off-white lyophilized powder.
Storage:
Store in a refrigerator at 2°C to 8°C (36°F to 46°F) in the original package to protect from light.