Octreotide (brand name Sandostatin,[1] Novartis Pharmaceuticals) is an octapeptide that

mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth

hormone, glucagon, and insulin than the natural hormone. It was first synthesized in 1979 by
the chemist Wilfried Bauer.

Contents

1 Medical uses
o 1.1 Tumors
o

1.2 Bleeding esophageal varices

1.3 Radiolabelling

2 Contraindications

3 Adverse effects

4 Interactions

5 Pharmacological effects

6 Pharmacokinetics

7 Research

8 See also

9 References

Medical uses
Tumors
Octreotide is used for the treatment of growth hormone producing tumors (acromegaly and
gigantism), pituitary tumors that secrete thyroid stimulating hormone (thyrotropinoma),
diarrhea and flushing episodes associated with carcinoid syndrome, and diarrhea in people
with vasoactive intestinal peptide-secreting tumors (VIPomas).

Bleeding esophageal varices

Octreotide is often given as an infusion for management of acute haemorrhage from
esophageal varices in liver cirrhosis on the basis that it reduces portal venous pressure,
though current evidence suggests that this effect is transient and does not improve survival.[2]

Radiolabelling
Further information: Octreotide scan
Octreotide is used in nuclear medicine imaging by labelling with indium-111 (Octreoscan) to
noninvasively image neuroendocrine and other tumours expressing somatostatin receptors.[3]
More recently, it has been radiolabelled with carbon-11[4] as well as gallium-68, enabling

imaging with positron emission tomography (PET), which provides higher resolution and
sensitivity.
Octreotide can also be labelled with a variety of radionuclides, such as yttrium-90 or
lutetium-177, to enable peptide receptor radionuclide therapy (PRRT) for the treatment of
unresectable neuroendocrine tumours.

Contraindications
Octreotide has not been adequately studied for the treatment of children, pregnant and
lactating women. The drug is given to these groups of patients only if a risk-benefit analysis
is positive.[5][6]

Adverse effects
The most frequent adverse effects (more than 10% of patients) are headache, hypothyroidism,
cardiac conduction changes, gastrointestinal reactions (including cramps, nausea/vomiting
and diarrhoea or constipation), gallstones, reduction of insulin release, hyperglycemia[7] or
hypoglycemia, and (usually transient) injection site reactions. Slow heart rate, skin reactions
such as pruritus, hyperbilirubinemia, hypothyroidism, dizziness and dyspnoea are also fairly
common (more than 1%). Rare side effects include acute anaphylactic reactions, pancreatitis
and hepatitis.[5][6] One study reported a possible association with rheumatoid arthritis.[8]
Some studies reported alopecia in patients who were treated by octreotide.[9] Rats which were
treated by octreotide experienced erectile dysfunction in a 1998 study.[10]
A prolonged QT interval has been observed in patients, but it is uncertain whether this is a
reaction to the drug or part of the patients' illnesses.[5]
Identifiers
Symbol
OPM superfamily
OPM protein

N/A
167
1soc

Interactions
Octreotide can reduce the intestinal resorption of ciclosporin, possibly making it necessary to
increase the dose.[11] Patients with diabetes mellitus might need less insulin or oral
antidiabetics when treated with octreotide. The bioavailability of bromocriptine is increased;
[6]
besides being an antiparkinsonian, bromocriptine is also used for the treatment of
acromegaly.

Pharmacological effects
Since octreotide resembles somatostatin in physiological activities, it can:

inhibit secretion of many hormones, such as gastrin, cholecystokinin, glucagon,

growth hormone, insulin, secretin, pancreatic polypeptide, TSH, and vasoactive
intestinal peptide,
reduce secretion of fluids by the intestine and pancreas,

reduce gastrointestinal motility and inhibit contraction of the gallbladder,

inhibit the action of certain hormones from the anterior pituitary,

cause vasoconstriction in the blood vessels, and

reduce portal vessel pressures in bleeding varices.

It has also been shown to produce analgesic effects, most probably acting as a partial agonist
at the mu opioid receptor.[12][13]

Pharmacokinetics
Octreotide is absorbed quickly and completely after subcutaneous application. Maximal
plasma concentration is reached after 30 minutes. The elimination half-life is 100 minutes
(1.7 hours) on average when applied subcutaneously; after intravenous injection, the
substance is eliminated in two phases with half-lives of 10 and 90 minutes, respectively.[5][6]

Research
Octreotide has also been used off-label for the treatment of severe, refractory diarrhea from
other causes. It is used in toxicology for the treatment of prolonged recurrent hypoglycemia
after sulfonylurea and possibly meglitinides overdose. It has also been used with varying
degrees of success in infants with nesidioblastosis to help decrease insulin hypersecretion.
Several clinical trials also proves the effect of octreotide as acute treatment (abortive agent)
in cluster headache, where it shows that administration of subcutaneous octreotide is effective
when compared with placebo.[14]
Octreotide has been used experimentally to treat obesity, particularly obesity caused by
lesions in the hunger and satiety centers of the hypothalamus, a region of the brain central to
the regulation of food intake and energy expenditure.[15] The circuit begins with an area of the
hypothalamus, the arcuate nucleus, that has outputs to the lateral hypothalamus (LH) and
ventromedial hypothalamus (VMH), the brain's feeding and satiety centers, respectively.[16][17]
The VMH is sometimes injured by ongoing treatment for acute lymphoblastic leukemia
(ALL) or surgery or radiation to treat posterior cranial fossa tumors.[15] With the VMH
disabled and no longer responding to peripheral energy balance signals, "Efferent
sympathetic activity drops, resulting in malaise and reduced energy expenditure, and vagal
activity increases, resulting in increased insulin secretion and adipogenesis."[18] "VMH
dysfunction promotes excessive caloric intake and decreased caloric expenditure, leading to
continuous and unrelenting weight gain. Attempts at caloric restriction or pharmacotherapy
with adrenergic or serotonergic agents have previously met with little or only brief success in
treating this syndrome."[15] In this context, octreotide suppresses the excessive release of
insulin and may increase its action, thereby inhibiting excessive adipose storage. In a small
clinical trial in eighteen pediatric patients with intractable weight gain following therapy for
ALL or brain tumors and other evidence of hypothalamic dysfunction, octreotide reduced
body mass index (BMI) and insulin response during glucose tolerance test, while increasing

parent-reported physical activity and quality of life (QoL) relative to placebo.[15] In a separate
placebo-controlled trial of obese adults without known hypothalamic lesions, obese patients
who received long-acting octreotide lost weight and reduced their BMI compared to patients
receiving placebo; post hoc analysis suggested greater effects in patients receiving the higher
dose of the drug, and among "Caucasian patients having insulin secretion greater than the
median of the cohort." "There were no statistically significant changes in QoL scores, body
fat, leptin concentration, Beck Depression Inventory, or macronutrient intake", although
patients taking octreotide had higher blood glucose after a glucose tolerance test than those
receiving placebo.[19]
Octreotide has also been investigated for patients with pain from chronic pancreatitis.[20]
It has been used in the treatment of malignant bowel obstruction.[21]
Octreotide may be used in conjunction with midodrine to partially reverse peripheral
vasodilation in the hepatorenal syndrome. By increasing systemic vascular resistance, these
drugs reduce shunting and improve renal perfusion, prolonging survival until definitive
treatment with liver transplant.[22] Similarly, octreotide can be used to treat refractory chronic
hypotension.[23]
While successful treatment has been demonstrated in case reports,[24][25] larger studies have
failed to demonstrate efficacy in treating chylothorax.[26]
A small study has shown that octreotide may be effective in the treatment of idiopathic
intracranial hypertension.[27][28]