Octreotide
SANDOSTATIN
What it isSomatostatin-receptor agonist; acromegaly, neuroendocrine tumors, variceal bleeding, and secretory diarrhea.
Why this oneIt suppresses growth hormone and gut peptides while reducing splanchnic flow, giving one drug unusually broad endocrine and GI utility.
What limits itGallstones emerge with prolonged use; glucose can rise or fall because insulin and glucagon are both suppressed.
FDA-approved for
- acromegaly/carcinoid (1988)
Off-label
- variceal bleeding
- refractory diarrhea
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Acromegaly (reduce GH and IGF-1 after inadequate response to/unsuitability for surgery, irradiation, bromocriptine) | Adults | 50 mcg SC TID × first 2 weeks | 100–500 mcg SC TID (most common 100 mcg TID) | Doses >300 mcg/day seldom add benefit; up to 500 mcg TID |
| Metastatic carcinoid tumors (severe diarrhea and flushing) | Adults | 100–600 mcg/day SC in 2–4 divided doses × first 2 weeks (mean 300 mcg/day) | median ~450 mcg/day | Experience above 750 mcg/day is limited |
| VIPomas (profuse watery diarrhea) | Adults | 200–300 mcg/day SC in 2–4 divided doses × first 2 weeks (range 150–750) | usually ≤450 mcg/day |
Renal In severe renal failure requiring dialysis, half-life is increased — adjust maintenance dosage.
Hepatic In liver cirrhosis, half-life is increased — adjust maintenance dosage.
Carcinoid and VIPoma doses are given in 2–4 divided doses daily; acromegaly is dosed three times daily.
Instructions
- Administer subcutaneously (rotate injection sites) or intravenously; for SC use the smallest volume to reduce injection pain
- Not compatible with Total Parenteral Nutrition solutions
- Assess baseline and periodic thyroid function (TSH, total/free T4) during chronic therapy
- In acromegaly after irradiation, withdraw ~4 weeks yearly to assess disease activity
Cautions
- Cardiac conduction abnormalities: bradycardia, arrhythmias, higher-degree/complete AV block (especially with IV administration) — consider cardiac monitoring
- Cholelithiasis and biliary complications (inhibits gallbladder contractility) — monitor periodically; discontinue if complications suspected
- Hypoglycemia or hyperglycemia — monitor glucose; adjust antidiabetic therapy
- Hypothyroidism (suppresses TSH) — monitor thyroid function
- Steatorrhea and malabsorption of dietary fats — evaluate for pancreatic exocrine insufficiency
- Depressed vitamin B12 levels — monitor during therapy
Adverse reactions
- Gallbladder abnormalities (stones and/or biliary sludge)
- Sinus bradycardia, conduction abnormalities, arrhythmias
- Diarrhea, loose stools, nausea, abdominal discomfort
- Hyperglycemia, hypoglycemia
- Hypothyroidism, goiter
- Injection-site pain, headache, dizziness
- Pancreatitis; anaphylactoid reactions including anaphylactic shock (rare)
Pregnancy Limited data insufficient to assess risk; no congenital malformations in reported human exposures. May improve fertility in acromegalic women.
Lactation No human milk data; low transfer into rat milk; weigh maternal need against potential infant risk.
NO BOXED WARNINGS
Principal riskGallstones with prolonged use; it inhibits insulin too
Cost, est. cash$100–$5,000/month
Generic entryLong generic
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Octreotide ballicule
