Octreotide

Somatostatin Analogapproved

Also known as: Sandostatin, Sandostatin LAR, SMS 201-995

A synthetic octapeptide analog of somatostatin with prolonged activity, used to treat acromegaly, carcinoid tumors, and vasoactive intestinal peptide-secreting tumors.

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Overview

Octreotide is a synthetic 8-amino acid peptide that mimics the natural hormone somatostatin but with a much longer duration of action (1.5 hours vs 2-3 minutes). It was first synthesized by Sandoz (now Novartis) and approved by the FDA in 1988. Octreotide binds preferentially to somatostatin receptor subtypes 2 and 5, inhibiting the secretion of growth hormone, insulin, glucagon, gastrin, and other GI hormones. It is available as immediate-release subcutaneous injections (Sandostatin) and as a long-acting depot formulation (Sandostatin LAR) given monthly. It is a cornerstone therapy for acromegaly, neuroendocrine tumors, and severe diarrheal conditions.

Mechanism of Action

Octreotide mimics somatostatin through multiple inhibitory actions: (1) Binds somatostatin receptors SSTR2 and SSTR5 with high affinity; (2) Inhibits GH secretion from the anterior pituitary; (3) Suppresses insulin and glucagon secretion from the pancreas; (4) Reduces splanchnic blood flow and portal pressure; (5) Inhibits GI hormone secretion (gastrin, VIP, secretin, motilin); (6) Decreases GI motility and fluid secretion; (7) In neuroendocrine tumors, directly inhibits tumor hormone secretion and may have antiproliferative effects via SSTR2-mediated apoptosis.

Molecular Formula

C49H66N10O10S2

Molecular Weight

1019.24 g/mol

Sequence

D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-ol (cyclic disulfide)

Dosage Protocols

Dose Range

50mcg – 500mcg

Frequency

Three times daily (SC) or monthly (LAR)

Route

subcutaneous / intramuscular

Cycle Length

Ongoing

SC: Start 50mcg TID, titrate based on GH/IGF-1 levels. LAR: 20mg IM monthly, adjustable to 10-40mg. Switch to LAR after SC dose stabilization.

Source: FDA prescribing information

🧮 Personalized Dosage Calculator

💰 Estimated Pricing

$100 – $3000per month supplypharmacy

Typical Supply

20mg or 30mg LAR depot

Last Updated

2026-02

Brand Sandostatin. For acromegaly, carcinoid tumors. SC: $100-500/mo. LAR depot: $2,000-3,000/injection. Insurance critical.

⚠️ Prices are estimates based on publicly available data and may vary significantly by vendor, location, and prescription status. This is not medical or financial advice.

Side Effects

EffectSeverity
Gallstonesmoderate
Diarrhea / Steatorrheamoderate
Abdominal painmild
Hyperglycemiamoderate
Injection site painmild

Pros & Cons

✓

Well-established therapy with decades of clinical use and extensive safety data

✓

Long-acting depot (LAR) allows once-monthly dosing for chronic conditions

✓

Highly effective for symptom control in neuroendocrine tumors and acromegaly

✓

Can reduce tumor size in some acromegaly patients and slow NET progression

✗

High rate of gallstone formation with long-term use (15-30%)

✗

Can worsen glucose tolerance due to insulin suppression

✗

Expensive, particularly the LAR depot formulation

✗

Does not normalize IGF-1 in all acromegaly patients (~65% normalization)

Research Studies

🩸 Blood Work

No specific bloodwork requirements reported for this peptide. General health panels are always recommended before starting any peptide protocol.

Legal Status

FDA-approved (1988) for acromegaly, carcinoid tumors, and VIPomas. Prescription-only. Available in SC injection and monthly LAR depot formulation.

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