Generic Name: octreotide

Brand Names: Sandostatin, Sandostatin LAR, Bynfezia Pen, Mycapssa

Drug Class: Antidiarrheals; Somatostatin Analogs

What is octreotide, and what is it used for?

Octreotide is a medication used in the treatment of acromegaly, a disorder associated with excessive blood levels of growth hormone, and severe, watery diarrhea caused by certain types of gastrointestinal (GI) tumors.

Octreotide is a somatostatin analog that is structurally similar to and mimics the activity of somatostatin, a natural hormone that inhibits growth hormone and various gastrointestinal hormones involved in the digestive process.

Acromegaly causes excessive growth of body tissues, typically characterized by abnormally large hands, feet and face, and metabolic dysfunction. It may cause enlargement of internal organs and insulin resistance, and can be life-threatening. Most often, acromegaly is the result of an anterior pituitary growth hormone-releasing tumor. Carcinoid tumors are a type of slow-growing cancer of hormone-secreting nerve cells (neuroendocrine) that can grow anywhere in the body. Gastrointestinal carcinoid tumors cause severe diarrhea and flushing.

Octreotide works by binding to protein particles (receptors) on cells that respond to somatostatin and inhibit their activity. This suppresses secretion of growth hormone from pituitary gland and insulin-like growth factor-1 (IGF-1) from liver, reducing the metabolic and other symptoms of acromegaly. Octreotide also suppresses the response of the reproductive hormone luteinizing hormone (LH) to gonadotropin-releasing hormone (GnRH), and the pancreatic secretion of glucagon and insulin, the two hormones that regulate blood glucose levels.

In the gastrointestinal tract, octreotide reduces visceral (splanchnic) blood flow and inhibits the release of serotonin and secretion of various gastrointestinal hormones including gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide, reducing the hormone release by gastrointestinal tumors and resultant diarrhea.

Uses of octreotide include:

Adult:

FDA-approved:

  • Acromegaly
  • Carcinoid tumors
  • Vasoactive intestinal peptide-secreting tumors (VIPomas)

Off-label:

  • Carcinoid crisis
  • Esophageal variceal bleeding
  • Gastrointestinal or pancreatic fistula
  • Gastroenteropancreatic neuroendocrine tumors
  • Diarrhea associated with acute graft-versus-host disease (GVHD)
  • Acquired immunodeficiency syndrome (AIDS)-related diarrhea
  • Ileostomy-related diarrhea
  • Chemotherapy-related diarrhea
  • Dumping syndrome
  • Chylothorax, a disorder with lymphatic fluid collection in the chest
  • Hepatorenal syndrome type 1 or acute kidney injury
  • Hypoglycemia, sulfonylurea-induced
  • Malignant bowel obstruction
  • Advanced thymic epithelial malignancies

Pediatric:

Off-label:

  • Gastrointestinal bleeding
  • Diarrhea
  • Chylothorax
  • Hyperinsulinemia/hypoglycemia in infancy
  • Sulfonylurea overdose

Warnings

  • Do not use in patients with hypersensitivity to any of the components in octreotide.
  • Octreotide may inhibit contractility of gallbladder and bile secretion. Monitor patients for gallstones and impairment of gallbladder function.
  • Octreotide alters the balance between insulin, glucagon, and growth hormone levels which may alter blood glucose levels. Monitor patient’s blood sugar levels and adjust antidiabetic medications appropriately.
  • Octreotide suppresses the secretion of thyroid-stimulating hormone, which may cause hypothyroidism. Monitor the patient’s thyroid function periodically.
  • Cardiac function abnormalities including irregular rhythms (arrhythmias), slow or rapid heart rate (bradycardia/tachycardia), and other conduction problems have been reported with octreotide therapy. Use with caution in patients with pre-existing heart disease and adjust the cardiac medications as necessary.
  • Octreotide may alter absorption of dietary fats, monitor the patient for pancreatitis.
  • Octreotide may impair absorption of vitamin B12, monitor the patient’s B12 levels.
  • Use with caution in liver or kidney impairment and adjust dose if necessary.
  • Octreotide reduces excessive fluid loss from the GI tract which may result in abnormally high zinc levels in patients receiving total parenteral nutrition (TPN). Monitor zinc levels in such patients periodically.
  • Octreotide may restore fertility and lead to unintended pregnancy. Women of reproductive potential who do not wish to become pregnant should use effective contraception during therapy.

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What are the side effects of octreotide?

Common side effects of octreotide include:

Less common side effects of octreotide include:

Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:

  • Serious heart symptoms include fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness;
  • Severe headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady;
  • Severe nervous system reaction with very stiff muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, and feeling like you might pass out; or
  • Serious eye symptoms include blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

What are the dosages of octreotide?

Capsule, Delayed-Release (Mycapssa)

  • 20 mg

Injectable Solution (Sandostatin)

  • 0.05 mg/mL
  • 0.1 mg/mL
  • 0.2 mg/mL
  • 0.5 mg/mL
  • 1 mg/mL

Depot Injection (Sandostatin LAR Depot)

  • 10 mg/kit
  • 20 mg/kit
  • 30 mg/kit

Injectable Solution (Bynfezia Pen)

  • 2500 mcg/mL (single-patient-use pen)

Adult:

Acromegaly

Reduction of growth hormone (GH) and insulin-like growth factor 1 (IGF-1) [somatomedin C] in adults with acromegaly who have had inadequate response to or cannot be treated with surgical resection, pituitary irradiation, and bromocriptine mesylate at maximally tolerated doses

Bynfezia Pen

  • 50 mcg subcutaneous (SC) thrice daily initially
  • Usual dose: 100 mcg SC thrice daily; some patients require up to 500 mcg thrice daily
  • Doses higher than 300 mcg/day seldom result in additional benefit; if an increase in dose fails to provide additional benefit, reduce dosage
  • Dosing titration
    • Measure IGF-I levels every 2 weeks after initiation or dosage change
    • Alternatively, measuring growth hormone levels at 1-4-hour intervals for 8-12 hours after administration; goal is to achieve growth hormone levels below 5 ng/mL or IGF-I levels within normal reference ranges for age and sex
    • Once biochemical normalization, or maximal benefit is achieved, re-evaluate IGF-I or growth hormone levels at 6-month intervals

Sandostatin LAR depot

Patients not currently receiving octreotide

  • Begin therapy with solution as listed above
  • Maintain on SC solution for at least 2 weeks as listed above to determine tolerance to octreotide
  • Patients who respond to the drug, based on GH and IGF-1 levels and who tolerate the drug, then switch to octreotide suspension

Patients currently receiving octreotide

  • Switch to octreotide suspension 20 mg intramuscular/IM (gluteal) every 4 weeks for 3 months; titrate up or down to 10-30 mg IM every 4 weeks, depending on response; not to exceed 40 mg
  • After 3 months, dosage may be adjusted as follows:
    • GH 2.5 ng/mL or less, IGF-1 normal, and clinical symptoms controlled: Maintain octreotide suspension at 20 mg every 4 weeks
    • GH higher than 2.5 ng/mL, IGF-1 elevated, and/or clinical symptoms uncontrolled: Increase octreotide suspension to 30 mg every 4 weeks
    • GH 1 ng/mL or less, IGF-1 normal, and clinical symptoms controlled: Reduce octreotide suspension to 10 mg every 4 weeks
    • If GH, IGF-1, or symptoms are not adequately controlled at a dose of 30 mg, the dose may be increased to 40 mg every 4 weeks; doses higher than 40 mg are not recommended
    • In patients who have received pituitary irradiation, withdraw yearly for 8 weeks to assess disease activity; if GH or IGF-1 levels increase and signs and symptoms recur, resume therapy

Mycapssa

  • 20 mg orally twice daily (40 mg/day) initially
  • May titrate up in increments of 20 mg/day, based on IGF-1 levels and signs and symptoms; maximum dosage is 80 mg/day
  • Monitor IGF-1 levels and signs and symptoms every 2 weeks during the dose titration, monthly during maintenance dosage, or as indicated
  • For 60 mg/day dose, administer as 40 mg in the morning and 20 mg in the evening
  • Dosage interruptions and modifications
    • If IGF-1 levels remain above the UNL after treatment with the maximum recommended dosage of 80 mg/day or the patient cannot tolerate treatment, consider discontinuing treatment and switching patient to another somatostatin analog
    • Withdraw therapy periodically to assess disease activity
    • If IGF-1 levels increase and signs and symptoms recur, resume therapy

Carcinoid Tumor

Indicated for treatment of adults with severe diarrhea and flushing episodes associated with metastatic carcinoid tumors

Bynfezia Pen

  • 100-600 mcg/day SC in 2-4 divided doses for the first 2 weeks
  • In clinical studies, median daily maintenance dosage was 450 mcg, but clinical and biochemical benefits were obtained in some patients ranged from 50-1,500 mcg/day
  • Experience with doses higher than 750 mcg/day is limited
  • Monitor urinary 5-hydroxyindole acetic acid (5-HIAA), plasma serotonin, and plasma substance

Sandostatin LAR depot

Patients not currently receiving octreotide

  • Begin therapy with solution as listed above
  • Maintain on SC solution for at least 2 weeks as listed above to determine tolerance to octreotide
  • Patients who respond to the drug, based on GH and IGF-1 levels and who tolerate the drug, then switch to octreotide suspension

Patients currently receiving octreotide

  • 20 mg IM every 4 weeks for 2 months then modify dose based on response; may increase to 30mg every 4 weeks if symptoms are inadequately controlled; decrease to 10 mg IM every 4 weeks for trial period if initially responsive to 20 mg dose; dose higher than 30 mg not recommended
  • Patients who have periodic exacerbation of symptoms (regardless of whether they are being maintained on Sandostatin injection or Sandostatin LAR Depot)
  • During these periods, SC Sandostatin injection may be given for a few days at the dosage they were receiving prior to switching to Sandostatin LAR depot; once symptoms resolve; discontinue SC Sandostatin injection

VIPoma

Indicated for treatment of adults with the profuse watery diarrhea associated with VIP-secreting tumors

Bynfezia Pen

  • 200-300 mcg/day SC in 2-4 divided doses for the first 2 weeks
  • Adjust dosage to achieve a therapeutic response; daily dosage is 150-750 mcg but usually doses higher than 450 mcg/day are not required
  • Monitor plasma vasoactive intestinal peptide (VIP)

Sandostatin LAR depot

Patients not currently receiving octreotide

  • Begin therapy with solution as listed above
  • Maintain on SC solution for at least 2 weeks as listed above to determine tolerance to octreotide
  • Patients who respond to the drug, based on GH and IGF-1 levels and who tolerate the drug, then switch to octreotide suspension

Patients currently receiving octreotide

  • 20 mg IM every 4 weeks for 2 months then modify dose based on response; may increase to 30mg every 4 weeks if symptoms are inadequately controlled; decrease to 10 mg IM every 4 weeks for trial period if initially responsive to 20 mg dose; dose higher than 30 mg not recommended
  • Patients who have periodic exacerbation of symptoms (regardless of whether they are being maintained on Sandostatin injection or Sandostatin LAR Depot)
  • During these periods, SC Sandostatin injection may be given for a few days at the dosage they were receiving prior to switching to Sandostatin LAR depot; once symptoms resolve; discontinue SC Sandostatin injection

Esophageal Variceal Bleeding (Off-label)

  • Solution: 25-100 mcg intravenous (IV) bolus (usual bolus dose: 50 mcg); follow by continuous IV infusion of 25-50 mcg/hour for 2-5 days; may repeat bolus in first hour if hemorrhage not controlled

GI or Pancreatic Fistula (Off-label)

  • Solution: 50-200 mcg SC every 8 hours for 2-12 days

AIDS-Related Diarrhea (Off-label)

  • Solution: 100-500 mcg SC every 8 hours

Ileostomy-Related Diarrhea (Off-label)

  • Solution: 25 mcg/hour IV or 50 mcg SC every 12 hours

Chemotherapy-Related Diarrhea (Off-label)

  • Low-grade or uncomplicated: Solution: 100-150 mcg SC every 8 hours for 1-30 days
  • Complicated: Solution: 100-150 mcg SC every 8 hours or 25-50 mcg/hour IV; may increase to 500 mcg every 8 hours until controlled
  • Severe: Solution: 100-150 mcg SC every 8 hours; may increase to 500-1500 mcg SC/IV every 8 hours

Dumping Syndrome (Off-label)

  • Solution: 50-150 mcg/day IV; may adjust to 25-600 mcg/day dose range
  • Suspension (depot injection): 10-20 mg/month IM

Chylothorax (Off-label)

  • Solution: 50-100 mcg SC every 8 hours

Dosage Modifications

Coadministration with proton pump inhibitors, H2-receptor antagonists, or antacids

  • Mycapssa only
  • Concomitant use of oral octreotide and proton pump inhibitors, H2-receptor antagonists, or antacids may require increased dosages of oral octreotide

Renal impairment

  • Sandostatin or Sandostatin LAR depot
    • Mild-to-severe without dialysis: No dosage adjustment necessary
    • With dialysis: 10 mg IM every 4 weeks initially, then titrate to effect
  • Mycapssa
    • Mild-to-severe: No dosage adjustment necessary
    • End-stage renal disease: 20 mg orally every day initially, then titrate to effect
  • Bynfezia Pen
    • Patients on dialysis: Half-life of octreotide may increase, may require dosage adjustment on maintenance dose

Hepatic impairment

  • Sandostatin or Sandostatin LAR depot
    • Cirrhosis: 10 mg IM every 4 weeks initially, then titrate to effect
  • Mycapssa
    • Patients with liver cirrhosis and patients with fatty liver disease showed prolonged elimination of octreotide following SC administration

Geriatric:

Acromegaly

  • Solution: 50 mcg SC every 8-12 hours initially; titrate up to 500 mcg SC every 8 hours if necessary; after successful treatment with solution for 2 weeks, initiate treatment with suspension (depot injection)
  • Suspension (depot injection): 20 mg IM intragluteally every 4 weeks for 3 months; titrate up or down to 10-30 mg IM every 4 weeks, depending on response; not to exceed 40 mg

Dosing Considerations

  • Dose adjustment may be necessary; clearance may decrease by 26% and half-life by 46%
  • Monitor IGF-1 levels every 2 weeks to guide titration; goal: GH levels less than 5 ng/mL or IGF-1 levels less than 1.9 units/mL (men) and less than 2.2 units/mL (women)
  • Monitor IGF-1 or GH levels every 6 months
  • Withdraw drug yearly for 4 weeks (solution) or 8 weeks (suspension) from patients who have undergone irradiation to assess

Carcinoid Tumor

  • Solution: 100-600 mcg/day SC divided every 6-12 hours; may titrate to 1500 mcg/day; after successful treatment with solution for 2 weeks, initiate treatment with suspension (depot injection)
  • Suspension (depot injection): 20 mg IM every 4 weeks if regular injection well tolerated

VIPoma

  • Solution: 200-300 mcg/day SC divided every 6-12 hours; after successful treatment with solution for 2 weeks, initiate treatment with suspension (depot injection)
  • Suspension (depot injection): 20 mg IM (gluteal) every 4 weeks for 2 months; continue solution for first 2 weeks; titrate suspension up or down to 10-30 mg IM every 4 weeks

Esophageal Variceal Bleeding (Off-label)

  • Solution: 50 mcg IV bolus, then 25-50 mcg/hour for 1-5 days

Pediatric:

  • Safety and efficacy not established

GI Bleeding (Off-label)

  • 1 mcg/kg bolus, then 1 mcg/kg/hour infusion; taper by 50% when no active bleeding for 24 hours

Diarrhea (Off-label)

  • 1-10 mcg/kg/day IV/SC

Chylothorax (Off-label)

  • 0.3-4 mcg/kg/hour SC/IV, depending on nature of chylothorax

Hyperinsulinemia/Hypoglycemia of Infancy (Off-label)

  • 2-10 mcg/kg/day SC/IV divided every 12 hours; increase on basis of response

Sulfonylurea Overdose (Off-label)

  • 1 mcg/kg SC/IV every 12 hours OR 25 mcg once; monitor blood glucose concentrations

Overdose

  • Octreotide overdose may cause irregular heart rhythm (arrhythmia), low blood pressure (hypotension), cardiac arrest, low oxygen in brain tissue (brain hypoxia), pancreatitis, fatty liver disease (hepatitis steatosis), liver enlargement (hepatomegaly), lactic acidosis, flushing, diarrhea, lethargy, weakness, and weight loss.
  • Overdose treatment includes supportive and symptomatic care.

What drugs interact with octreotide?

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or healthcare provider from all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or healthcare provider if you have any questions about the medication.

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Pregnancy and breastfeeding

  • Octreotide may be used in women with acromegaly who wish to become pregnant. The drug should be discontinued once pregnancy occurs.
  • Octreotide improves fertility and may result in unintended pregnancy in premenopausal women.
  • Animal studies showed transient growth retardation in the fetus, with no impact on postnatal development and there was no other evidence of octreotide-related adverse effects on fetal development.
  • Available reports from octreotide use in pregnant women are insufficient to identify drug-associated risks of major birth defects, miscarriage or adverse maternal or fetal outcomes.
  • Use octreotide during pregnancy only if clearly needed. If treatment for acromegaly is required during pregnancy, use the lowest effective dose.
  • There is no information on the presence of octreotide in breast milk, or its effects on milk production or on the breastfed infant, however, the drug is present in animal milk. The decision to breastfeed during octreotide therapy should be made considering the mother’s clinical need, and the benefits of breastfeeding, risks from the mother’s underlying condition, and risks of drug exposure to the infant.

What else should I know about octreotide?

  • Take octreotide capsules exactly as prescribed.
  • Contact your healthcare provider if you:
    • Experience symptoms of gallstones or other gallbladder problems
    • Notice changes in normal sugar levels
    • Experience irregular heartbeat
  • You may need to be tested periodically for thyroid function, vitamin B12 levels, or other parameters periodically. Follow up with your healthcare provider.
  • Store carefully out of reach of children.
  • In case of overdose, seek immediate medical help or call Poison Control.

Summary

Octreotide is a medication used in the treatment of acromegaly, a disorder associated with excessive blood levels of growth hormone, and severe, watery diarrhea caused by certain types of gastrointestinal (GI) tumors. Common side effects of octreotide include headache, dizziness, fatigue, pain at injection site, abdominal distress, abdominal pain, diarrhea, flatulence, constipation, nausea, vomiting, dry mouth (xerostomia), biliary tract disease, and others. Do not take if pregnant or breastfeeding.

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Medically Reviewed on 11/1/2022
References
REFERENCES:

https://www.rxlist.com/consumer_octreotide_sandostatin/drugs-condition.htm

https://reference.medscape.com/drug/sandostatin-lar-octreotide-342836

https://www.uptodate.com/contents/octreotide-drug-information

https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/019667s058,021008s023lbl.pdf

https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021008s043lbl.pdf

https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/208232s000lbl.pdf

https://www.ncbi.nlm.nih.gov/books/NBK544333/

https://go.drugbank.com/drugs/DB00104