Octreotide

Intravenous
Subcutaneous
Intramuscular
Class
Somatostatin receptor modulators
Subclass
Somatostatin analogs
Substance name
Octreotide acetate
Brand names
Sandostatin®, Bynfezia Pen®
Common formulations
Solution for injection
See also
Octreotide DR (Mycapssa®)
Dosage and administration
Adults patients
Symptomatic relief
Carcinoid tumor • Metastatic
•
Start at: 100-600 mcg IV daily, in 2-4 divided doses, for 2 weeks
•
Maintenance: 450 mcg IV daily, in 2-4 divided doses
•
Maximum: 1,500 mcg per day
Consider measuring urinary 5-hydroxyindole acetic acid, plasma serotonin, and plasma substance P to monitor treatment progress.
Diarrhea in patients with vasoactive intestinal peptide tumors
•
Start at: 200-300 mcg IV daily, in 2-4 divided doses, for 2 weeks
•
Maintenance: 150-450 mcg IV daily, in 2-4 divided doses
•
Maximum: 750 mcg per day
Consider measuring plasma vasoactive intestinal peptide to monitor treatment progress.
Diarrhea in patients with acute GvHD • Off-label
•
500 mcg IV q8h for a maximum of 7 days or until 24 hours after resolution of diarrhea
Treatment
Acromegaly • Inadequate response to or ineligible for surgery, pituitary irratiation, or bromocriptine
•
Start at: 50 mcg IV q8h for 2 weeks
•
Maintenance: 100-300 mcg IV q8h
•
Maximum: 1,500 mcg per day
Titrate to achieve target GH or IGF-1 levels. Monitor GH or IGF-1 every 2 weeks after initiating treatment and with any dosage change, and to guide titration. Withdraw treatment every year for 4 weeks in patients treated with irradiation, and consider resuming if GH or IGF-1 levels increase or symptoms recur.
Acute variceal hemorrhage • Off-label
•
Loading: 50 mcg IV bolus, repeated within the first hour if bleeding persists
•
Subsequently: 50 mcg/h IV continuous infusion for 2-5 days
Carcinoid crisis, during surgery • Off-label
•
500-1,000 mcg IV bolus, repeated at 5-minute intervals if needed
Alternative
•
Loading: 500-1,000 mcg IV bolus
•
Subsequently: 50-200 mcg/h IV continuous infusion
Chemotherapy-induced diarrhea • Not responding to loperamide, severe dehydration • Off-label
•
25-50 mcg/h IV continuous infusion
Hepatorenal syndrome-AKI • Off-label
•
50 mcg/h IV continuous infusion until 24 hours after the return of serum creatinine level to within ≤ 0.3 mg/dL of baseline for 2 consecutive days or for a total of 14 days
Administered in combination with midodrine.
Sulfonylurea-induced hypoglycemia • Off-label
•
50-100 mcg IV q6-12h
Administered in combination with intravenously dextrose.
Prevention
Prevention of carcinoid crisis in patients with carcinoid syndrome, during surgery • Off-label
•
50-200 mcg/h IV continuous infusion, starting 12 hours before surgery, and continued for at least 48 hours postoperatively
Indications for use
Labeled indications
Adults
•
Symptomatic relief of carcinoid tumor (metastatic)
•
Symptomatic relief of diarrhea in patients with vasoactive intestinal peptide tumors
•
Treatment of acromegaly (inadequate response to or ineligible for surgery, pituitary irratiation, or bromocriptine)
Off-label indications
Adults
•
Symptomatic relief of diarrhea in patients with acute GvHD
•
Treatment of acute variceal hemorrhage
•
Treatment of carcinoid crisis, in patients undergoing surgery
•
Treatment of chemotherapy-induced diarrhea (not responding to loperamide, severe dehydration)
•
Treatment of hepatorenal syndrome-AKI
•
Treatment of sulfonylurea-induced hypoglycemia
•
Prevention of carcinoid crisis in patients with carcinoid syndrome, in patients undergoing surgery
Safety risks
Contraindications
Hypersensitivity to octreotide or its components
Concomitant use of lutetium Lu-177 dotatate
Warnings and precautions
Abnormal ECG, AV block
•
Maintain a high level of suspicion, as octreotide has been associated with an increased risk of cardiac conduction abnormalities and other ECG changes, including QT prolongation, axis shift, early repolarization, low voltage, R/S transition, and early R wave progression. Octreotide IV has been associated with an increased risk for higher degree AV blocks.
Bradycardia
•
Use caution in patients taking bradycardia-inducing drugs, such as β-blockers.
Cholelithiasis
•
Maintain a high level of suspicion, as octreotide may inhibit gallbladder contractility and decrease bile secretion, potentially leading to gallbladder abnormalities, sludge, and associated complications such as cholecystitis, cholangitis, and pancreatitis. Monitor patients periodically.
Decreased serum cyclosporine levels
•
Use caution in patients taking cyclosporine.
Decreased serum vitamin B12
•
Maintain a high level of suspicion, as octreotide has been associated with an increased risk of decreased vitamin B12 levels and abnormal Schilling test results. Monitor serum vitamin B12 levels.
Hypothyroidism
•
Maintain a high level of suspicion, as octreotide may suppress the secretion of TSH. Monitor thyroid function periodically.
Increased blood glucose, decreased blood glucose
•
Maintain a high level of suspicion, as octreotide may alter the balance between the counter-regulatory hormones, insulin, glucagon, and GH, resulting in hypoglycemia, hyperglycemia, or diabetes mellitus. Monitor blood glucose levels. Adjust insulin and other antidiabetic treatment accordingly.
Increased serum bromocriptine levels
•
Use caution in patients taking bromocriptine.
Increased serum drug levels
•
Use caution in patients taking drugs mainly metabolized by CYP3A4 and having a narrow therapeutic index, such as quinidine and terfenadine.
Steatorrhea, fat malabsorption
•
Maintain a high level of suspicion, as somatostatin analogs, including octreotide, may cause steatorrhea, stool discoloration, diarrhea, and fat malabsorption.
Specific populations
Renal impairment
CrCl ≥ 15 mL/min
•
Use acceptable. No dose adjustment required.
CrCl < 15 mL/min
•
Reduce maintenance dose.
Renal replacement therapy
Any modality
•
Dose as in CrCl < 15 mL/min.
Hepatic impairment
Any severity
•
Reduce maintenance dose.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: C
•
Use only if clearly needed. Evidence of fetal harm in animals. Discuss the potential for unintended pregnancy with premenopausal females, as octreotide may improve improve fertility in patients with acromegaly.
•
Consider discontinuing medical therapy for acromegaly once pregnancy is established. Consider initiating or re-initiating medical therapy only for tumor control or severe clinical symptoms attributable to acromegaly.
Breastfeeding
Use only if benefits outweigh potential risks.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Unlikely to cause adverse effects in breastfed infants.
No overt adverse effects on lactation reported.
Adverse reactions
Very common > 10%
•
Bile duct dilatation, biliary sludge, bradycardia, gallstones, hypothyroidism, ↑ blood glucose, nausea, abdominal discomfort, diarrhea
Common 1-10%
•
Cardiac arrhythmias, ↓ blood glucose, goiter, dizziness, fatigue, weakness, pruritus, back pain, arthralgia, flu-like symptoms, injection site hemorrhage, skin flushing, blurred vision, fat malabsorption, hair loss, depression, visual disturbances, urinary frequency, steatorrhea, headache, injection site pain, vomiting, flatulence, abdominal distension, constipation, urinary tract infections
Rare < 0.1%
•
Abdominal tenderness, abdominal guarding
Unknown frequency
•
Acute pancreatitis, anaphylaxis, acute cholecystitis, bowel obstruction, pancreatic insufficiency, ↓ platelet count, AV block, ↓ serum vitamin B12
Interactions
Drug(s)
Check Interactions
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