If you are rummaging for a reliable somatostatin agonist, you got to try out the octreotide acetate treatment. Check out the benefits of taking this drug, its therapeutic applications, side effects, and how to access the medication legally.
Did you know that octreotide acetate is a chemo drug?
There are numerous somatostatin agents in the market. However, getting the pick of the bunch can be a real hassle. Not only should you be acquainted with the adverse risk factors but also figure out whether the negative upshots will outweigh the gains.
The primary octreotide acetate function is to act as an antagonist to the excessive release of hormones. For this reason, it is among the original prescription drugs for some gastrointestinal carcinomas.
Forget about clinical applications of synthetic somatostatin. Sometimes, you can take the performance-enhancing HGH and suffer the acromegaly consequences. Well, if your fingers become too gigantic for the gloves, you should hold your horses and take octreotide acetate.
Are you ready to use this treatment? Let’s find out the prerequisites.
The use of octreotide acetate dates back to 1979 when chemist Wilfred Bauer first synthesized it. However, the drug won the approval of the FDA a decade later.
Octreotide acetate raw powder exhibits a similar mechanism of action as that of the natural polypeptide hormone. Unlike endogenous somatostatin, the drug is stable and long-acting with slightly extended half-life.
The long half-life of octreotide acetate is attributed to the four sequential amino acids, which are resistance to metabolic degradation. They include L-terminal amino alcohol, cysteine, N-phenylalanine, and D-tryptophan.
Octreotide acetate is a synthetic cyclic octapeptide chemical with CAS no. 83150-76-9. It is available in liquid or ready-to-inject form. However, if you want some bulky powder for your research, you can rummage around for a trustworthy octreotide acetate manufacturer.
The treatment suppresses the release of Human Growth Hormone, insulin, secretin, serotonin, and glucagon. Despite being a prescription drug for some types of gastroenteropancreatic cancers, octreotide acetate injection is used in the treatment of acromegaly. This medication will also bottle up the response of luteinizing hormone (LH) to gonadotropin-releasing hormone (GnRH).
(1)Octreotide Acetate Structural Formula
Octreotide acetate has a high binding affinity for somatostatin receptor-2 (SSTR2) and SSTR5 more than it does with SSSTR3.
Octreotide acetate functions as an inhibitory agent of HGH, insulin, glucagon, and adrenocorticotropin when it binds to SSTR2. SSTR3 triggers cell apoptosis. Studies reveal that this binding has a groundbreaking potentiality in tumor angiogenesis. The activation of SSTR5 has similar effects as those of the previous somatostatin receptors.
Octreotide acetate works by interacting with the somatostatin receptors via G-protein coupling. The mechanism inhibits the release of several secondary hormones, including GH, glucagon, and insulin. This inhibitory hormone has an impact on both the anterior pituitary and the gastrointestinal system.
For instance, it antagonizes the effects of the growth hormone-releasing hormone, and therefore, controls the induction of HGH and IGF-1. Besides, the octreotide acetate function is to suppress the production of TSH (Thyroid-Stimulating Hormone) and adenylyl cyclase.
In the GIT, octreotide acetate works to the expression of gastrointestinal and pancreatic hormones, glucagon, insulin, and the exocrine secretory actions.
In patients with acromegaly, the treatment normalizes the level of growth hormone and IGF-1.
The metabolism of octreotide acetate occurs in the liver.
Octreotide acetate raw powder has a wide range of therapeutic uses. Its physiological activities are synonymous with that of the endogenous somatostatin hormone. Take, for example, both of them inhibit secretion of growth hormone, glucagon, insulin, cholecystokinin, thyroid-stimulating hormone, and gastrin.
(1)Treatment of acromegaly
The root cause of acromegaly is excessive production of human growth hormone. If this abnormality occurs, the hypothalamus will naturally stimulate the release of somatostatin, which initiates negative feedback. However, acromegaly or gigantism will eventually develop when the body can no longer control the HGH levels.
Taking octreotide acetate inhibits the synthesis of growth hormone from the pituitary gland. This hormonal drug is more potent than the endogenous somatostatin. So, if you have misused the exogenous HGH and your gloves no longer fit, you can buy octreotide acetate to counteract the symptoms.
(2)Treatment of certain tumors
Octreotide acetate raw powder is a prescription drug for HGH-producing tumors. In instances where the radiation therapy fails, or surgery is not an option, the treatment will come in hand.
Medical practitioners recommend octreotide acetate to patients with thyrotropinoma, carcinoid syndrome, and vasoactive intestinal peptide carcinomas. In most cases, these tumors secrete excess natural hormones.
The medication not only blocks this hormone-secreting mechanism but also suppresses the symptoms brought about by the swellings. Take, for example; octreotide acetate decreases severe watery diarrhea and flushing, which show up in patients with carcinoid and vasoactive intestinal peptide tumors.
In diarrhea, octreotide acetate injection triggers the absorption of electrolytic fluid in the intestinal wall.
(3)Radiolabeling in Nuclear Medicine Imaging
Medics and research scientists have labeled Octreotide with several radio-nucleotides. For instance, radiolabeling the compound with lutetium-177 is a treatment for some neuroendocrine tumors.
Recently, the compound has been radiolabeled with gallium-68 and carbon-11. This radiolabeling has proved to be highly sensitive with excellent resolution, hence, an ideal imaging method with positron emission tomography.
In octreoscan, Octreotide is labeled with indium-111 to image neuroendocrine tumors, which express somatostatin receptors.
(4) Managing Bleeding Esophageal Varices
Health providers recommend octreotide acetate to victims of liver cirrhosis with acute hemorrhaging esophageal varices. The treatment works to reduce portal venous pressure, especially in patients who have cirrhosis. It constricts the splanchnic arterioles to slow down blood flow to the portal system.
A couple of studies have suggested the efficacy of octreotide acetate in the treatment of obesity.
Hypothalamic lesions around the hunger and satiety regions of the brain can be responsible for high BMI and obesity. Treating posterior cranial tumors or acute lymphoblastic leukemia with radiotherapy or surgery can injure the hypothalamus.
As a result, this part of the brain will no longer be responsive to energy balance signals. Eventually, there will be an increase in vagal activity, insulin hypersecretion, and adipose deposition. Besides, the body will take in more calories than it requires, leading to abnormal weight gain.
Taking octreotide acetate injection suppresses the excessive release of insulin and the build-up of adipose tissues. In a particular clinical trial involving 18 patients with hypothalamic dysfunction, the research scientists found out that octreotide acetate lowered the BMI of the subjects relative to the placebo.
(6)Treatment of Gastrointestinal Fistula
Other medical applications of this somatostatin agent include;
Treatment of hypoglycemia in both neonates and adults
Decreasing insulin hypersecretion
Management of chronic refractory hypotension
Reversing peripheral vasodilation when used alongside midodrine
Managing idiopathic intracranial hypertension
The absorption of octreotide acetate is as fast as lightning, especially with the subcutaneous application.
After administering the octreotide acetate injection, it will only take half an hour for the drug to reach the maximal plasma concentration. Subcutaneously, the bioavailability of octreotide acetate is at the maximum. Intramuscularly, the plasma concentration of the drug can be as low as 60%.
The typical elimination half-life of this medication is about 1.8 hours. Up to 32% of it will be excreted in the urine.
The half-life of octreotide acetate is usually high in cirrhotic patients. Therefore, the dosage should be as low as possible to avoid the drug from accumulating in the system. Similarly, medics would modify the dose in victims of renal impairment since the plasma clearance is usually run down.
Most states have approved its use as a pharmaceutical prescription drug. Therefore, you can freely buy octreotide acetate if your doctor prescribes.
You can either inject it yourself or seek help from a healthcare provider. If you prefer injecting yourself, make sure to pick instructions from a professional or read through the directions from the instruction booklet. Ensure you connect with a credible octreotide acetate manufacturer for sterilized vials.
Start by cleaning the injection site with an alcohol swab. Use sterile needles and appropriately discard them after use. Lastly, make sure to shift from one injection spot to the next to give enough room for healing and prevent skin irritations. To avoid microbial contamination, do not use octreotide acetate if the suspension is discolored, it’s leaking, or it has particulate matter.
After everything is set, you can prepare the octreotide acetate suspension and administer it immediately. To avoid missing a dose, make a habit of injecting yourself at regular times of the day.
(1)Octreotide Acetate injection
There are three modes of octreotide acetate administration. Although the ideal method is through the subcutaneous application, you can as well opt for intramuscular (IM) or intravenous (IV) injections.
Octreotide acetate suppliers avail the medication in two different formulations, which are long-acting and short-acting (immediate-release) versions. The immediate-release injection is suitable for managing diarrhea and the symptoms related to carcinoid tumors. When using this version, ensure to take octreotide acetate two to four times daily. You can either inject it subcutaneously or intravenously.
The long-acting injection is to be administered once every four weeks. This formulation is only given intramuscularly, preferably in the hip. It is recommended for intermediate and advanced octreotide users. In most cases, pharmacists would put beginners in the short-acting cycle for about two weeks before shifting to the long-acting version.
The pharmacist may help you administer the medication. However, time constraints and medical bills will scare away most people to the extent that they inject themselves.
(2) Octreotide Acetate Dosage
You have to inject octreotide acetate twice or thrice a day, depending on the doctor’s directions. The dosage hinges on the condition you wish to manage, your health status, height, and weight. Take, for instance; the starting dose is as low as 10mg for patients with liver cirrhosis and renal impairment, which calls for dialysis.
Beginners use octreotide acetate three times daily with an initial immediate-release dose of 50mcg. Once the patient tolerates and positively responds to the drug, the pharmacist can increase the prescribed amount or recommend the long-acting formulation.
Patients typically receive between 100mcg and 200mcg of the medication to be split into two or four times daily. However, some would take as high as 500mcg. The octreotide acetate price range of these single vials rarely hit a 30 dollar mark.
Here is an example of a two-week octreotide acetate cycle;
|Clinical Condition||Dosage per day|
|Carcinoid tumors||100 – 500 mcg|
|Vasoactive intestinal peptide tumors||200 – 300mcg|
|Chemo and AIDs-induced diarrhea||100-2000mcg|
|Bleeding varices||25mcg per hour for two days|
② Long-Acting Injections
Once a patient comes out of the immediate-release formulation, the healthcare professional will administer the long-acting 20mg octreotide acetate dose. You should neither take this injection subcutaneously or intravenously. The only choice you are left with is through IM.
Use octreotide acetate at an interval of weeks. If you are fresh from the immediate-release shot, continue with the dosage for the next two weeks before bringing it to a halt. The reason is that there’s a need for the treatment to reach the maximal therapeutic levels following the injection of the slow-acting Octreotide. Failure to adhere to this instruction could worsen the clinical symptoms.
After three months of using this treatment, your pharmacist will check out any improvements, record the octreotide acetate side effects, and adjust the dosage. In case the clinical symptoms have dropped off, and the IGF-1 levels are normal, you will continue with the initial dose. However, this aspect applies if the growth hormone levels are slightly high.
In situations where IGF-1 is elevated, GH is greater than 2.5ng/mL, and the clinical symptoms are still uncontrolled, the dose will have to increase. Your physician can give you up to 30mg of octreotide acetate every four weeks. Although the quantity can go as high as 40mg due to slow response, research scientists and medical professionals advice against high doses.
Some patients would record a fall in growth hormone and IGF-1, and positive response to the clinical symptoms. In this case, the doctor may lower the dose to 10mg. However, if symptoms recur, you will have to backtrack to the 20mg dosage.
Unlike for the immediate-release injection, the long-acting octreotide acetate price costs an arm and a leg. The ballpark figure for a 10mg vial is $2000.
(3) What should I know before injecting Octreotide Acetate?
① Drug Interactions
Any octreotide acetate user suffering from diabetes mellitus will have to lower the insulin dose. The reason is that the drug strongly inhibits the secretion of glucagon more than it induces insulin release.
If you’re using cyclosporine, it will be necessary for you to increase the dosage. Octreotide acetate works to reduce the absorption of cyclosporine through the intestinal walls. As a result, the patient may experience transplant rejection.
A single octreotide acetate injection will increase the bioavailability of bromocriptine, a drug for managing Parkinson disease. Moreover, this somatostatin agent has high chances of interfering with nutrient consumption. Therefore, this effect may alter the absorption of oral drugs.
Summarily, you should make sure to discuss with your pharmacist about any other prescriptions, vitamins, supplements, or over-the-counter drugs you are taking. The reason is that these medications may interact negatively or positively when you use octreotide acetate alongside them.
② Medical history
Before you can buy octreotide acetate, ensure to seek counsel from your doctor concerning your current health and medical history. For instance, if you have diabetes, the pharmacist may adjust your dose and monitor the blood sugar level.
Unless the doctor prescribes it, do not use octreotide acetate when you have kidney disease, thyroid conditions, diabetes, or liver cirrhosis. Also, avoid the medication like the plague if you suffer from nutrition problems, gallstones, and deficiency of vitamin B12.
③ Age factor
This drug is recommended for adults over 18 years old. In rare cases, healthcare providers would prescribe it to neonates, especially in the treatment of refractory hyperglycemia.
Children should not take octreotide acetate injections for prolonged periods. Ideally, the cycle should less than a year. The reason is that this medication will slow down the growth rate of a child. For the elderly, the dose ought to be at the low end as you factor in the possibilities of age-related diseases.
For short-term storage of octreotide acetate, keep it at room temperature within the range of 20 and 30 degrees Celsius. In this case, the validity of the medication will only last for two weeks.
For long-term storage, store it in the refrigerator at two to eight degrees Celsius. In case you need to inject yourself, take it out of the fridge and allow it to cool down to room temperature for about an hour. Do not use artificial means to heat or warm the vial.
Ensure to keep the octreotide acetate vials away from direct light. Once you open a single dose, dispose of the unused portion to avoid contamination. If your drug formulation is a multi-dose, the vial will remain valid for 14 days. However, the validity stands on the condition that you maintain room temperatures and protect the medication from light.
⑤ Risk of Pregnancy
When treating acromegaly, make sure you are on potent contraception. Studies suggest that acromegaly causes infertility in some women. Once you take octreotide acetate, the chances are that the drug will normalize the HGH levels and restore fertility. Unless you are ready to raise an offspring, ensure to use adequate contraception.
⑥ Octreotide acetate preparation
The treatment is mainly available in vials and ampules. The immediate-release injections are obtainable in ampules of about 0.05 to 1mg/mL. For these units, the octreotide acetate price is less than $25. However, they are only meant for single-doses. Once opened, the unused portion ought to be discarded.
Contrary, long-acting formulations come in vials of between 10 and 20mg. They are multi-dose. Once open, you can store it in a refrigerator and use to a maximum of 14 days.
- Skin reactions at the injection site
- Changes in cardiac conduction
- Abdominal cramping
- Stomach upset
- Flatulence and bloating
- Irregular heartbeat
- Changes in the insulin response
- Loose and oily stools
Many users do not register adverse octreotide acetate side effects. The reason is that pharmacists and health practitioners would prescribe the medication only if they are sure that the benefits outweigh the drug’s negative upshots. Most of these symptoms are reversible and will disappear when you discontinue the treatment.
Take note that high doses translate to more side effects.
Although octreotide acetate rarely interferes with the blood sugar in patients with diabetes, it is vital that you monitor the changes and adjust your medications. Pains, headaches, and fever are treatable with ibuprofen or acetaminophen. In point of fact, acetaminophen tends to increase the serum concentration of octreotide acetate.
This medication is available in octreotide acetate suppliers as a prescription drug in the United States. It is obtainable from local pharmaceutical depots. However, if you want to save time and money, an online store can be a safe bet.
Obtaining a valid medication is not a walk in the park, especially if you are flicking through scores of websites and online pages. You ought to find the right octreotide acetate supplier by checking the customer’s feedback, review, and product rating. Also, the seller has to provide comprehensive information about the drug, including precautions, Octreotide acetate side effects, benefits, and the dose.
Octreotide acetate price varies depending on various factors. For example, you might spend more when buying small units of the drug than splashing out on the 83150-76-9 raw bulky powder. Besides, your location has a hand on the shipping charges and the total cost of the product.
The long-acting Sandostatin LAR® has a higher price tag than its short-acting counterpart. For a 30mg kit, the ballpark figure can be as high as 3000 bucks or more. A 1000 mcg/ml of 5ml single vial costs between $120 and $150.
This somatostatin agonist has a wide range of therapeutic applications, some of which are still under research.
Although it’s only obtainable through a doctor’s recommendation, you can still access the drug from an online-based octreotide acetate manufacturer. At least, this step saves you the fuss of obtaining a prescription, especially when you want to counter the effects of overdosing with synthetic HGH.
The octreotide acetate benefits are extensive. Over the years, it has been incorporated in the management of carcinoid tumors and VIPomas. Where surgery fails and a radiotherapy is no longer an option, this drug will be the next course of action.
Octreotide acetate price should not scare you. After all, a beginner can shell out less than 15 bucks for a starting dose.
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Lamberts, S.W., Van der Lely, A.J, and De Herder, W.W. (1997). A Risk-Benefit Assessment of Octreotide in the Treatment of Acromegaly.
Gotzsche, P.C., and Hrobjartsson, A. (2008). Somatostatin Analogues for Acute Bleeding Esophageal Varices.
Lustig, R.H., Xiong, X., Hinds, P.S., et al. (2003). Octreotide Therapy of Pediatric Hypothalamic Obesity.
Chadha, K.M., Lombardo, J., Mashtare, T., et al. (2009). High Dose Octreotide Acetate for Management of Gastroenteropancreatic Neuroendocrine Tumors. International Journal of Cancer Research and Treatment.
Chaudhry, R., Singh, B., and Subhas, P. (2017). Octreotide in Gastroenterology. Medical Journal, Armed Forces India.
Sharkey, A.J., and Rap, N.J. (2012). The Successful Use of Octreotide in the Treatment of Traumatic Chylothorax. Texas Heart Institute Journal.