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Octreotide

SANDOSTATIN

Pronunciation: ok-TREE-oe-tide

Octreotide ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Octreotide ballicule

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.

Octreotide molecular structure (skeletal formula)
Molecular structure: Octreotide

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Acromegaly (reduce GH and IGF-1 after inadequate response to/unsuitability for surgery, irradiation, bromocriptine)Adults50 mcg SC TID × first 2 weeks100–500 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)Adults100–600 mcg/day SC in 2–4 divided doses × first 2 weeks (mean 300 mcg/day)median ~450 mcg/dayExperience above 750 mcg/day is limited
VIPomas (profuse watery diarrhea)Adults200–300 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

Available strengths

Cautions

Adverse reactions

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.

Cost

Octreotide (SANDOSTATIN)
What pharmacies pay · NADAC 9/30/26
Strength#/mogeneric $/unitCostPlus
0.05 mg/mLinjper unit$2.64/mLnot offered
0.1 mg/mLinjper unit$2.53/mLnot offered
0.2 mg/mLinjper unit$5.34/mLnot offered
0.5 mg/mLinjper unitnot offered
1 mg/mLinjper unitnot offered

Generic entryLong generic

NO BOXED WARNINGS

Principal riskGallstones with prolonged use; it inhibits insulin too

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

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.

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