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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Octreotide
Generic Name
Octreotide Acetate
Active Ingredient
OctreotideCategory
Somatostatin Analog [EPC]
Salt Form
Acetate
Variants
6
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Octreotide, you must consult a qualified healthcare professional.
| 63323-377 |
| 100 ug/mL | INJECTION, SOLUTION | INTRAVENOUS, SUBCUTANEOUS | 63323-376 |
Detailed information about Octreotide
Octreotide is a potent somatostatin analog used to manage growth hormone excess in acromegaly and symptoms of certain tumors. It works by mimicking the natural hormone somatostatin to inhibit various endocrine and exocrine functions.
The dosage of octreotide is highly individualized and depends on the condition being treated, the patient's clinical response, and laboratory values (such as GH or IGF-1 levels).
Octreotide is not FDA-approved for use in pediatric patients for the standard indications of acromegaly or carcinoid syndrome. However, it is occasionally used off-label in specialized pediatric centers for conditions like congenital hyperinsulinism or severe, refractory diarrhea. In these cases, dosing is strictly weight-based (e.g., 1-10 mcg/kg/day) and must be managed by a pediatric endocrinologist or gastroenterologist. Clinical data on the long-term safety and growth effects of octreotide in children are limited.
In patients with severe renal failure requiring dialysis, the elimination half-life of octreotide may be increased. Healthcare providers may start at the lower end of the dosing range and titrate slowly. The clearance of octreotide is reduced by approximately 50% in patients with end-stage renal disease.
In patients with liver cirrhosis, the elimination of the drug may be prolonged. While specific dose adjustment formulas are not standardized, close monitoring of clinical response and side effects is necessary, particularly when using the long-acting formulations.
Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine if they respond differently than younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function.
If you miss a dose of the immediate-release injection, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and continue with your regular schedule. Do not double the dose to catch up. For the LAR formulation, if you miss an appointment for your monthly injection, contact your healthcare provider immediately to reschedule.
Signs of an octreotide overdose may include severe nausea, diarrhea, abdominal pain, flushing, dizziness, and an irregular heartbeat (arrhythmia). In clinical trials, doses up to 2000 mcg TID were tolerated but caused significant gastrointestinal distress. If an overdose is suspected, seek emergency medical attention or contact a Poison Control Center immediately. Treatment is primarily supportive, focusing on managing symptoms and maintaining hydration.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop the medication without medical guidance, as this can lead to a rapid return of symptoms.
Because octreotide affects the gastrointestinal tract and the release of digestive enzymes, GI-related side effects are very common, especially during the first few weeks of treatment. These include:
Octreotide is a potent hormonal regulator that affects multiple organ systems. Patients must be aware that while it is highly effective for its intended uses, it requires regular medical follow-up to monitor for complications, particularly those involving the gallbladder and the endocrine system. It is not a cure for acromegaly or neuroendocrine tumors but a management tool to control hormone levels and symptoms.
No FDA black box warnings for Octreotide. The safety profile is well-established, provided that patients undergo the recommended monitoring for biliary and cardiac health.
There are no drugs that are strictly 'contraindicated' for use with octreotide in the sense of causing immediate fatality, but certain combinations are avoided because they negate the effects of the treatment or cause severe toxicity. For example, using octreotide with other somatostatin analogs (like lanreotide) is generally redundant and not recommended.
These are conditions where the benefit of octreotide must be carefully weighed against the risks, and the patient must be monitored closely:
Octreotide is classified as Pregnancy Category B. This means that animal reproduction studies (in rats and rabbits) have failed to demonstrate a risk to the fetus, but there are no adequate and well-controlled studies in pregnant women.
Octreotide is a synthetic octapeptide analog of somatostatin. It exerts its effects by binding with high affinity to somatostatin receptors (SSTRs), specifically subtypes 2 and 5. These receptors are coupled to inhibitory G-proteins (Gi). Binding leads to:
Through these mechanisms, octreotide suppresses the secretion of growth hormone, insulin, glucagon, gastrin, vasoactive intestinal peptide (VIP), and serotonin.
Common questions about Octreotide
Octreotide is primarily used to treat acromegaly, a condition where the body produces too much growth hormone, leading to enlarged bones and organs. It is also used to manage severe diarrhea and skin flushing caused by certain types of tumors, such as carcinoid tumors and vasoactive intestinal peptide tumors (VIPomas). By mimicking the natural hormone somatostatin, octreotide helps bring hormone levels back into a normal range and reduces the debilitating symptoms associated with these rare conditions. In some emergency settings, it is also used off-label to stop bleeding from esophageal varices. Always use this medication under the strict guidance of an endocrinologist or specialist.
The most common side effects of octreotide are gastrointestinal in nature, including nausea, diarrhea, abdominal pain, and gas. Many patients also experience 'steatorrhea,' which is fatty, foul-smelling stool caused by the drug's effect on digestive enzymes. Another very common side effect is the development of gallstones or biliary sludge, which occurs in up to 50% of long-term users. Local reactions at the injection site, such as pain or redness, are also frequently reported. Most of the digestive side effects tend to improve over time as your body adjusts to the medication. If these symptoms are severe or persistent, you should contact your healthcare provider.
While there is no known direct chemical interaction between alcohol and octreotide, it is generally recommended to limit alcohol consumption. Alcohol can irritate the gastrointestinal tract, potentially worsening the nausea and diarrhea that are already common side effects of octreotide. Additionally, both alcohol and octreotide can affect blood sugar levels, making it more difficult for you and your doctor to manage glycemic control. For patients with acromegaly or carcinoid syndrome, maintaining a stable internal environment is key to successful treatment. Discuss your specific alcohol habits with your doctor to determine what is safe for your situation.
Octreotide is classified as a Pregnancy Category B drug, meaning animal studies haven't shown harm to the fetus, but there isn't enough data from human trials to guarantee safety. Because it is a potent hormone inhibitor, there is a theoretical risk that it could affect the development of the baby's own endocrine system. Most doctors recommend using octreotide during pregnancy only if the benefits to the mother significantly outweigh the potential risks to the fetus. Women of childbearing age should discuss contraception with their doctor, as octreotide can sometimes restore fertility by normalizing hormone levels. If you become pregnant while taking octreotide, notify your healthcare provider immediately.
The time it takes for octreotide to work depends on the formulation and the symptom being treated. For the immediate-release (IR) injection, hormone levels like growth hormone can begin to drop within 30 minutes to an hour, and symptoms like flushing or diarrhea may improve within the first day of treatment. However, for the long-acting release (LAR) version, it can take several weeks or even a few monthly injections to reach a 'steady state' where the full therapeutic effect is realized. In acromegaly, it may take several months of dose titration to see a significant reduction in IGF-1 levels. Your doctor will use blood tests to monitor how well the drug is working.
Stopping octreotide suddenly is generally not recommended, as it can cause a rapid and severe return of your symptoms. For patients with acromegaly, growth hormone levels will spike, leading to the return of headaches, joint pain, and soft tissue swelling. For those with carcinoid tumors or VIPomas, stopping the drug can trigger a 'rebound' effect of profuse diarrhea and severe flushing, which can lead to dehydration and electrolyte imbalances. If you need to stop the medication due to side effects or a planned surgery, your doctor will provide a specific plan to transition you safely. Never alter your dosing schedule without professional medical advice.
If you miss a dose of the immediate-release (IR) injection, you should take it as soon as you remember. If it is nearly time for your next scheduled injection, skip the missed dose and return to your regular routine; do not double the dose to make up for the one you missed. For the long-acting (LAR) injection, which is given once a month by a healthcare professional, missing a dose is more significant. If you miss your appointment, call your doctor's office immediately to reschedule. Consistency is vital for keeping hormone levels stable and preventing the return of symptoms.
Weight gain is not a primary side effect of octreotide, but it can occur indirectly. In some patients, octreotide causes hypothyroidism (low thyroid function) by suppressing the release of Thyroid Stimulating Hormone (TSH), and weight gain is a common symptom of an underactive thyroid. Additionally, by controlling the severe diarrhea associated with carcinoid tumors or VIPomas, patients may begin to absorb more nutrients and calories, leading to weight recovery. If you notice unexpected or rapid weight gain, your doctor should check your thyroid levels and overall metabolic health. It is important to distinguish between healthy weight recovery and side-effect-related weight gain.
Octreotide can interact with several other medications, so a full review of your drug list is essential. It is known to decrease the absorption of cyclosporine, which can lead to transplant rejection if not monitored. It also interacts with diabetes medications (insulin and oral drugs), as octreotide affects how the body releases its own insulin and glucagon. Other drugs that slow the heart rate, such as beta-blockers, can have an additive effect with octreotide, leading to bradycardia. Always inform your healthcare provider about all prescriptions, over-the-counter medicines, and herbal supplements you are taking to avoid dangerous interactions.
Yes, octreotide acetate immediate-release injection is available as a generic medication, which is typically more cost-effective than the brand-name Sandostatin. However, the long-acting release (LAR) formulation and the oral capsule (Mycapssa) may still be under patent protection or have limited generic availability depending on your region. Generic versions must meet the same FDA standards for safety, purity, and effectiveness as the brand-name versions. If you are concerned about the cost of your medication, ask your pharmacist or doctor if a generic version of the specific formulation you require is available.
Other drugs with the same active ingredient (Octreotide)
> Warning: Stop taking Octreotide and call your doctor immediately if you experience any of these serious symptoms:
The most significant long-term concern with octreotide is the development of gallstones. While many of these stones are 'silent' (asymptomatic), some can lead to acute cholecystitis (gallbladder inflammation) or bile duct obstruction. Regular ultrasound monitoring of the gallbladder is often recommended for patients on chronic therapy. Additionally, long-term suppression of TSH may require thyroid hormone replacement therapy in some individuals. There is also a theoretical risk of vitamin B12 deficiency over many years due to altered gastric acid secretion and intrinsic factor release, though this is clinically rare.
No FDA black box warnings for Octreotide. Unlike some other medications, the FDA has not mandated a boxed warning for octreotide. However, the warnings regarding biliary tract abnormalities and cardiac conduction are considered major safety precautions that require diligent clinical monitoring.
Report any unusual symptoms or persistent side effects to your healthcare provider. Many GI side effects can be managed by reducing the fat content in your diet or by taking the injection between meals or at bedtime.
To ensure the safe use of octreotide, your doctor will likely order the following tests:
Octreotide generally does not cause significant impairment of motor skills or cognitive function. However, some patients may experience dizziness or fatigue, especially when first starting the medication or during a dosage increase. It is advisable to see how the drug affects you before driving or operating heavy machinery.
There is no direct chemical interaction between alcohol and octreotide. However, alcohol can worsen some of the gastrointestinal side effects of octreotide, such as nausea and diarrhea. Furthermore, alcohol can affect blood sugar levels, which may complicate the glycemic management already being influenced by octreotide. Moderation is advised, and you should discuss your alcohol consumption with your doctor.
Octreotide should not be stopped abruptly without medical supervision. In patients with acromegaly, stopping the drug will lead to a rapid rise in growth hormone levels and a return of symptoms (headache, joint pain, swelling). In patients with carcinoid tumors, discontinuation can lead to a 'rebound' of severe diarrhea and flushing. If the drug must be stopped, it is usually done under close observation.
> Important: Discuss all your medical conditions, especially heart disease, diabetes, and history of gallstones, with your healthcare provider before starting Octreotide.
For each major interaction, the management strategy usually involves more frequent monitoring of the patient's clinical status and laboratory values, rather than avoiding the drug entirely.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter drugs.
There is a potential for cross-sensitivity between octreotide and other somatostatin analogs, such as lanreotide or pasireotide. If a patient has had a severe reaction to one drug in this class, they should generally not be prescribed another unless under the strict supervision of an allergist and endocrinologist.
> Important: Your healthcare provider will evaluate your complete medical history, including any previous drug allergies or gallbladder issues, before prescribing Octreotide.
It is not known whether octreotide is excreted in human milk. Many drugs are excreted in milk, and because of the potential for serious adverse reactions in nursing infants (such as growth suppression), a decision should be made whether to discontinue nursing or discontinue the drug. Most clinicians advise against breastfeeding while using octreotide, or they monitor the infant's growth very closely if breastfeeding is continued.
As previously mentioned, octreotide is not FDA-approved for children. The safety and effectiveness in the pediatric population have not been established. There are concerns that long-term use could lead to growth retardation due to the suppression of growth hormone. If used off-label for conditions like hyperinsulinism, it must be under the care of a specialist.
In clinical trials, elderly patients did not show significantly different safety profiles compared to younger patients. However, the elderly are more likely to have decreased renal function and a higher prevalence of cardiovascular disease. This increases the risk of drug accumulation and bradycardia. Dosage titration in the elderly should be slow and cautious.
In patients with severe renal impairment (Creatinine Clearance < 30 mL/min), the half-life of octreotide is prolonged. For the immediate-release form, starting doses should be reduced. For the LAR formulation, the 10 mg or 20 mg dose is often preferred over the 30 mg dose to start. Octreotide is not significantly removed by hemodialysis.
In patients with liver cirrhosis, the half-life of the drug is increased to approximately 3 hours (compared to 1.5 hours in healthy subjects). This may lead to higher steady-state levels. While specific dose adjustments are not always required for mild impairment, those with moderate to severe hepatic impairment (Child-Pugh Class B or C) require careful monitoring for increased side effects.
> Important: Special populations require individualized medical assessment and more frequent laboratory monitoring.
| Parameter | Value |
|---|---|
| Bioavailability | ~100% (Subcutaneous) |
| Protein Binding | ~65% (primarily to lipoproteins) |
| Half-life | 1.5 to 1.7 hours (IR); ~2-3 weeks (LAR) |
| Tmax | 0.4 to 1.0 hours (Subcutaneous) |
| Metabolism | Hepatic and tissue peptidases |
| Excretion | Renal 32%, Fecal <2% |
Octreotide is the prototypical Somatostatin Analog [EPC]. Related medications include Lanreotide (Somatuline) and Pasireotide (Signifor). It is categorized therapeutically as an Antigrowth Hormone Agent and an Antidiarrheal Agent for specific tumor-related conditions.