Octreotide

Octreotide is used to treat severe watery diarrhea and sudden reddening of the face and neck caused by certain types of tumors (e.g., carcinoid tumors, vasoactive intestinal peptide tumors) that are found usually in the intestines and pancreas. The symptoms occur when these tumors make too much of certain natural substances (hormones). This medication works by blocking the production of these hormones. By decreasing watery diarrhea, octreotide helps to reduce the loss of body fluids and minerals.

Octreotide is also used to treat a certain condition (acromegaly) that occurs when the body makes too much of a certain natural substance called growth hormone. Treating acromegaly helps reduce the risk of serious problems such as diabetes and heart disease. Octreotide works by decreasing the amount of growth hormone to normal levels.

Octreotide is not a cure for these conditions. Octreotide is usually used with other treatment (e.g., surgery, radiation, other drugs).

Octreotide is available under the following different brand names: Sandostatin, and Sandostatin LAR.

Dosage Forms and Strengths

Injectable solution

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

Depot injection

• 10 mg/kit
• 20 mg/kit
• 30 mg/kit

Dosage Considerations – Should be Given as Follows:

Acromegaly

Solution: 50 mcg subcutaneously (SC) every 8 hours initially (geriatric: every 8-12 hours); 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 intramuscularly (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, as follows

Symptoms controlled: If growth hormone (GH) less than 1 ng/mL and IGF-1 normal, decrease dose to 10 mg IM every 4 weeks; if GH less than 2.5 ng/mL and IGF-1 normal, maintain dose at 20 mg IM every 4 weeks

Symptoms uncontrolled: If GH greater than 2.5 ng/mL or IGF-I elevated, increase dose to 30 mg IM every 4 weeks; if symptoms persist, increase to 40 mg IM

Dosing Considerations

• Monitor IGF-1 levels every 2 weeks to guide titration; goal: GH levels less than 5 ng/mL or IGF-1 levels less than1.9 units/mL (men) and less than2.2 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
• Geriatric: Dose adjustment may be necessary; clearance may decrease by 26% and half-life by 46%

Carcinoid Tumor

Adult and Geriatric:

• Solution: 100-600 mcg/day subcutaneously (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 intramuscularly (IM) every 4 weeks if regular injection well tolerated

VIPoma

Adult and Geriatric:

• Solution: 200-300 mcg/day subcutaneously (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 intramuscularly (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)

Adult and Geriatric:

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

GI or Pancreatic Fistula (Off-label)

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

AIDS-Related Diarrhea (Off-label)

• Solution: 100-500 mcg subcutaneously (SC) every 8 hours

Ileostomy-Related Diarrhea (Off-label)

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

Chemotherapy-Related Diarrhea (Off-label)

• Low-grade or uncomplicated: Solution: 100-150 mcg subcutaneously (SC) every 8 hours for 1-30 days
• Complicated: Solution: 100-150 mcg SC every 8 hours or 25-50 mcg/hour intravenously (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 subcutaneously/intravenously (SC/IV) every 8 hours

Dumping Syndrome (Off-label)

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

Chylothorax (Off-label)

• Solution: 50-100 mcg subcutaneously (SC) every 8 hours

GI Bleeding, Pediatric (Off-label)

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

Diarrhea, Pediatric (Off-label)

• 1-10 mcg/kg/day intravenously/subcutaneously (IV/SC)

Chylothorax, Pediatric (Off-label)

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

Hyperinsulinemia/Hypoglycemia of Infancy (Off-label)

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

Sulfonylurea Overdose, Pediatric (Off-label)

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

Dosing Modifications

• Hepatic impairment: Cirrhosis, 10 mg intramuscularly (IM) every 4 weeks initially, then titrate to effect
• Renal impairment: Without dialysis, dose adjustment not necessary; with dialysis, 10 mg IM every 4 weeks initially, then titrate to effect

Common side effects of octreotide include:

• Gallbladder problems: Decreased gallbladder contractility, gallstones, cholecystitis, cholestatic hepatitis
• Blood sugar imbalances
• Hypothyroidism
• Slow heart rate
• ECG changes
• Irregular heartbeat (arrhythmia)
• Pancreatitis
• Upper respiratory tract infection
• Fatigue
• Headache
• Malaise
• Rash
• Diarrhea
• Nausea
• Vomiting
• Pain at injection site
• Joint pain
• Blurred vision
• Loose/oily stools
• Constipation
• Stomach pain or upset
• Gas
• Bloating
• Dizziness

Serious side effects of octreotide include:

• Signs of gallbladder or liver problems (e.g., fever, stomach or abdominal pain, severe nausea or vomiting, yellowing eyes/skin, unexplained pain in the back or right shoulder)
• Signs of underactive thyroid (e.g., unexplained weight gain, cold intolerance, slow heartbeat, severe constipation, unusual or extreme tiredness, growth/lump/swelling on the front of the neck)
• Worsening heart condition symptoms (e.g., trouble breathing, slow/fast/irregular heartbeat)
• Numbness or tingling of the arms or legs

Postmarketing side effects of octreotide reported include:

Pediatric Patients

• No formal controlled clinical trials have been performed to evaluate the safety and effectiveness of octreotide depot injection in children younger than 6 years
• Serious adverse events, including hypoxia, necrotizing enterocolitis, and death, have been reported in children (mostly in those younger than 2 years)
• The relation of these events to octreotide has not been established, because the majority of these pediatric patients had serious underlying comorbid conditions

This is not a complete list of side effects and other serious side effects may occur. Call your doctor for information and medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

If your doctor has directed you to use this medication for your condition, your doctor or pharmacist may already be aware of any possible drug interactions or side effects and may be monitoring you for them. Do not start, stop, or change the dosage of this medicine or any medicine before getting further information from your doctor, healthcare provider or pharmacist first.

• Severe Interactions of octreotide include:
  • astemizole
  • cisapride
  • disopyramide
  • ibutilide
  • indapamide
  • pentamidine
  • pimozide
  • procainamide
  • quinidine
  • sotalol
  • terfenadine
• Octreotide has serious interactions with at least 52 different drugs.
• Octreotide has moderate interactions with at least 51 different drugs.
• Mild interactions of octreotide include:
  • cyanocobalamin
  • food
  • methadone

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

This medication contains octreotide. Do not take Sandostatin or Sandostatin LAR if you are allergic to octreotide or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Hypersensitivity

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Octreotide?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Octreotide?"

Cautions

• Hepatic or renal impairment may necessitate dosing adjustments.
• May alter fat absorption in some patients (monitor for pancreatitis).
• May decrease vitamin B12 levels (monitor).
• Monitor for hypothyroidism (octreotide suppresses secretion of thyroid-stimulating hormone, TSH).
• Use caution when giving drug to patients with cardiovascular disease.
• May enhance toxicity of QTc-prolonging agents.
• Do not use depot formulation in patients with sulfonylurea-induced hypoglycemia.
• Dosage adjustments may be necessary in the elderly.
• Females of childbearing age should use adequate contraception because the treatment may restore fertility

Pregnancy and Lactation

• Octreotide may be acceptable for use during pregnancy. Either animal studies show no risk but human studies are not available or animal studies showed minor risks and human studies were done and showed no risk.
• Whether octreotide crosses into breast milk is not known; avoid giving to lactating women.