What is octreotide injection, and how does it work (mechanism of action)?
Octreotide acetate is an injectable medicine that is very similar to the hormone somatostatin, which is naturally produced in the body that has several effects including inhibition of the release of hormones. Octreotide works in a similar fashion as somatostatin, but is degraded more slowly and is a stronger inhibitor of glucagon, growth hormone, and insulin release. Like somatostatin, octreotide also decreases the release of growth stimulating hormones, decreases blood flow to the digestive organs, and inhibits the release of digestive hormones such as serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide. Based on these actions, octreotide acetate is used to treat symptoms of severe diarrhea and flushing caused by cancer.
Octreotide is also used to treat acromegaly. Acromegaly is a rare hormonal disorder that affects adults in which there is an over production of growth hormone that leads to the abnormal growth of the hands, feet, or facial features. Octreotide significantly decreases the levels of growth hormone and IGF-I (somatomedin C) in patients with acromegaly.
Other actions of octreotide include suppression of thyroid stimulating hormone (TSH) release, inhibition of gallbladder contractility, and the secretion of bile.
The FDA approved octreotide acetate in October 1988.
What brand names are available for octreotide injection?
Sandostatin, Sandostatin LAR
Is octreotide injection available as a generic drug?
Do I need a prescription for octreotide injection?
What are the side effects of octreotide injection?
Side effects reported with octreotide include:
- gallbladder problems,
- slow heart rate (bradycardia),
- irregular heartbeat (arrhythmias),
- stomach pain,
- gas (flatulence),
- abnormal stools,
- stomach distention,
- low and high blood glucose,
- low thyroid levels,
- injection site pain, and
Other side effects that occurred in 1% to 4% of patients included:
- joint pain,
- urinary tract infection (UTI),
- cold symptoms,
- flu symptoms,
- injection site hematoma,
- blurred vision,
- fat malabsorption,
- hair loss,
- visual disturbance, and
Other side effects include:
- increase in liver enzymes,
- gastrointestinal (GI) bleeding,
- gastric or peptic ulcer,
- gallbladder polyp,
- superficial skin infections,
- basal cell carcinoma (skin cancer),
- joint effusion,
- muscle pain,
- Raynaud's phenomenon,
- chest pain,
- shortness of breath,
- congestive heart failure,
- high blood pressure,
- hypertensive reaction,
- heart palpitations,
- orthostatic hypotension,
- low sex drive (low libido),
- fainting (syncope),
- Bell's Palsy,
- pituitary apoplexy,
- increased intraocular pressure,
- hearing loss,
- pulmonary nodule,
- status asthmaticus,
- diabetes insipidus,
- iron deficiency,
- ear infection (otitis),
- allergic reaction,
- increased creatine kinase, and
- weight loss.
What is the dosage for octreotide injection?
- Although injection into fatty tissue (subcutaneously) is preferred, octreotide acetate also can be given by injection into the vein (intravenously). Hands should be washed before and after administration.
- Before injecting, octreotide should be allowed to come to room temperature.
- To decrease pain associated with subcutaneous injection the smallest possible volume to deliver the drug should be used.
- Injection sites should be rotated to decrease injection site reactions.
- If the solution becomes cloudy, has particles, or is leaking, it should not be used. Used needles should be thrown away in a needle or sharps container.
- Treatment may be started with 50 mcg three times daily. For most patients, 100 mcg three times daily was found to be effective. However, some patients required up to 500 mcg three times daily.
Carcinoid tumor treatment
- To treat symptoms of severe diarrhea and flushing in patients with metastatic carcinoid tumors, the recommended daily dose of octreotide acetate during the first 2 weeks of treatment ranges from 100-600 mcg/day in 2-4 divided doses (average daily dose is 300 mcg).
Vasoactive intestinal peptide tumor (VIPomas) treatment
- To treat severe diarrhea associated with VIP-secreting tumors, the recommended daily dose of octreotide acetate during the first 2 weeks of therapy is 200-300 mcg in 2-4 divided doses (150-700 mcg) to achieve symptom control. Dose may be adjusted based on individual patient response but usually doses > 450 mcg/day are not required.
The safety and effectiveness of octreotide acetate has not been demonstrated in pediatric patients. No formal studies have been performed to evaluate the safety and effectiveness of octreotide acetate in patients under the age of 6. Serious side effects including hypoxia, necrotizing enterocolitis, and death have been reported with its use in children, especially those under the age of 2.
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Which drugs or supplements interact with octreotide injection?
: Octreotide acetate can alter nutrient absorption and may interfere with the absorption of some orally taken medications.
If taken with octreotide acetate, dose adjustments may be required for some medications including insulin, oral anti-diabetes medicines, beta blockers, calcium channel blockers (CCBs), and agents used to control fluid and electrolyte balance.
Octreotide may decrease the removal of certain drugs broken down by the CYP3A4 liver enzymes. Therefore, octreotide should be used cautiously with other drugs that are extensively metabolized by these enzymes or those that have a low therapeutic index.
Co-administration of octreotide and bromocriptine may increase the blood levels of bromocriptine (Cycloset).
Pancreatitis is inflammation of an organ in the abdomen called the pancreas.
Is octreotide injection safe to take if I’m pregnant or breastfeeding?
There are no adequate and well-controlled studies of octreotide acetate use in pregnancy. There was no evidence of fetal harm in studies performed in rats and rabbits. However, as animal studies cannot be always used to predict response in humans, octreotide acetate should be used in pregnancy only if clearly needed. Octreotide acetate is classified as FDA pregnancy risk category B.
It is not known if octreotide acetate can enter breast milk. As many drugs can enter human milk and cause side effects in the nursing infant, octreotide acetate should be used cautiously during breastfeeding.
What else should I know about octreotide injection?
What preparations of octreotide-injection are available?
- Octreotide injection is available in ampuls and vials.
- Ampuls containing solution for injection: 0.05, 0.1, 0.2, 0.5, and 1 mg/ml
- Depot injection (Sandostatin LAR): 10, 20, and 30 mg per vial
How should I keep octreotide-injection stored?
- Octreotide acetate is stored in the refrigerator between 36 F and 46 F (2 C to 8 C).
- It should be stored in its outer carton to protect it from light.
- If stored at room temperature, octreotide acetate is stable for 14 days if protected from light.
- Prior to injection the solution should be allowed to warm up to room temperature.
- The manufacturer recommends against the use of artificial means to warm up the solution.
- Multi-dose vials should be used within 14 days of opening.
- Ampuls are intended for single-use only and any unused portion should be discarded after opening.