Name:Octreotide (Octreotide)

Indications for use:
Acromegaly (in the absence of a sufficient effect of surgical treatment, radiation therapy and treatment with dopamine agonists; in inoperable patients, also in patients who refused surgical treatment); tumors of the gastroenteropancreatic endocrine system (carcinoid tumors / a common name for tumors arising from cells of the gastric mucosa /) with the presence of a carcinoid syndrome (a combination of “chronic enteritis / inflammation of the small intestine /, inflammation of the heart valves, telangiectasias / local excessive expansion of small vessels / and skin pigmentation ), tumors characterized by hyperproduction of vasoactive intestinal peptide, glucagonomas, gastrinomas / Zollinger-Ellison syndrome, insulinomas /), tumors characterized by hyperproduction of somatoliberin, refractory diarrhea in patients with AIDS;

Pharmacological action:
Octreotide is a synthetic octapeptide, which is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but with a significantly longer duration of action. The drug suppresses pathologically increased secretion (the process of production and release) of growth hormone, as well as peptides and serotonin produced in the gastroenteropancreatic endocrine system (a system that includes the stomach, small intestine and pancreas).
In healthy individuals, octreotide inhibits growth hormone secretion induced by arginine, stress, and insulin hypoglycemia (low blood sugar caused by insulin); secretion of insulin, glucagon, gastrin and other peptides of the gastroenteropancreatic endocrine system caused by food intake, also secretion of insulin and glucagon stimulated by arginine; secretion of thyrotropin (a pituitary hormone that regulates thyroid function) caused by thyroliberin.
In patients with acromegaly (an endocrine disease accompanied by an increase in the volume of the hands, nose, lower jaw, etc.), octreotide reduces the concentration of growth hormone and / or somatomedin A (a biologically active compound produced mainly by liver cells, which stimulates tissue growth and exhibits insulin-like activity ) in blood plasma. A clinically significant decrease in the concentration of growth hormone (by 50% or more) is observed in almost all patients, while normalization of the level of growth hormone in plasma (less than 5 ng / ml) is achieved in about half of the patients. In most patients with acromegaly, octreotide significantly reduces the severity of symptoms such as headache, swelling of the skin and soft tissues, hyperhidrosis (a disease of the sweat glands with the formation of small itchy vesicles), joint pain and paresis (decreased strength and / or range of motion). In patients with large adenomas (benign tumors) of the pituitary gland, treatment with octreotide may lead to some reduction in tumor size.
In carcinoid (cancerous) tumors, the use of octreotide can lead to a decrease in the severity of symptoms such as flushing sensations and diarrhea (diarrhea), which in many cases is accompanied by a decrease in plasma serotonin concentration and a decrease in the excretion of 5-hydroxyindoleacetic acid in the urine.
In tumors characterized by hyperproduction (increased formation) of vasoactive intestinal peptide, the use of octreotide in most patients leads to a decrease in severe secretory diarrhea (diarrhea). At the same time, there is a decrease in concomitant disorders of the electrolyte (ionic) balance, for example, hypokalemia (low levels of potassium in the blood). Some patients slow down or stop the progression of the tumor and even reduce its size. Clinical improvement is usually accompanied by a decrease (down to normal values) in the concentration of vasoactive intestinal peptide in blood plasma.
In glucagonomas (a malignant tumor/cancer/of the pancreas that produces insulin), the use of octreotide in most cases leads to a marked decrease in necrotizing (leading to tissue death) migratory rash; body weight is reduced (the effect on diabetes mellitus, however, is not dramatic). In gastronomy (malignant tumor / cancer / stomach), Zollinger-Ellison syndrome (complex of symptoms when gastric and duodenal ulcers are combined with a benign pancreatic tumor), octreotide reduces hypersecretion (increased secretion) of hydrochloric acid in the stomach and associated symptoms, including diarrhea feeling of flushing. In some patients, there is a decrease in the concentration of gastrin (a protein secreted by the gastric mucosa,
In patients with insulinomas (tumors of the pancreas that produce insulin), octreotide normalizes glycemia (reduces high blood sugar), reducing the level of insulin in the blood (this effect, however, can be short-lived – within 2 hours). Glycemic control may improve without a concomitant prolonged decrease in blood insulin levels.
In patients with tumors that overproduce growth hormone releasing factor (releasing an increased amount of hypothalamic neurohormones that promote the release of growth hormone by the pituitary gland), octreotide reduces the severity of symptoms of acromegaly. In the future, hypertrophy (increase in volume) of the pituitary gland may decrease.
In patients with acquired immunodeficiency syndrome (AIDS), suffering from severe diarrhea (diarrhea), refractory (resistant) to anti-infective or other therapy, the use of octreotide leads to complete or partial normalization of the stool in about one third of cases.
In patients undergoing pancreatic surgery, the use of the product during the operation and subsequently reduces the frequency of typical postoperative complications (for example, pancreatic fistulas / channels formed as a result of the disease, connecting the pancreas with internal organs or the external environment /, abscesses / abscesses/, sepsis /infection of the blood with microbes from the focus of purulent inflammation/, postoperative acute pancreatitis /inflammation of the pancreas/).

Octreotide (Octreotide) method of administration and doses:
In acromegaly, the product is initially administered at 0.05-0.1 mg subcutaneously at intervals of 8 or 12 hours. In the future, dose selection should be based on monthly determinations of the concentration of growth hormone in the blood, analysis of clinical symptoms and product tolerance. In most patients, the optimal daily dose is 0.2-0.3 mg. The maximum dose is 1.5 mg every day. If after three months of treatment with octreotide there is not a sufficient decrease in the level of growth hormone and improvement in the clinical picture of the disease, therapy should be discontinued.
In case of endocrine tumors of the gastroenteropancreatic system, the product is administered subcutaneously at an initial dose of 0.05 mg 1-2 times a day. In the future, depending on the achieved clinical effect, the effect on the levels of hormones produced by the tumor (in the case of carcinoid tumors, the effect on the excretion of 5-hydroxyindoleacetic acid in the urine) and tolerability, the dose of the product can be gradually increased to 0.1-0.2 mg 3 times every day. In exceptional cases, higher doses may be required. Maintenance doses of the product should be selected individually.
For refractory diarrhea in patients with AIDS, the product is administered subcutaneously at the initial dose (0.1 mg) 3 times a day. If after one week of treatment diarrhea does not subside, the dose of the product should be increased individually, up to 0.25 mg 3 times a day. The selection of the dose of the product should be based on the control of stool volume and product tolerance. If no improvement occurs within a week of treatment with octreotide at a dose of 0.25 mg 3 times every day, therapy should be discontinued.
To prevent complications after operations on the pancreas, the first dose of 0.1 mg is administered subcutaneously 1 hour before laparotomy (opening the abdominal cavity); then, after the operation, 0.1 mg is administered subcutaneously 3 times a day for seven consecutive days.
In elderly patients, there is no need to reduce the dose of octreotide.
At the injection site, pain, itching or burning sensation, redness and swelling are possible (usually disappear within 15 minutes). To reduce discomfort at the injection site, it is recommended to bring the product solution to room temperature before administration and inject a smaller volume of the product. Multiple injections at the same site at short intervals should be avoided. To prevent bacterial contamination, it is recommended to pierce the stopper of the multi-dose vial no more than 10 times.

Octreotide (Octreotide) contraindications:
Increased susceptibility to the product. Pregnancy, breastfeeding.

Octreotide (Octreotide) side effects:
Anorexia (lack of appetite), nausea, vomiting, spasmodic pain (associated with a sharp contraction of smooth mouse internal organs) in the abdomen, a feeling of bloating, excessive gas formation, loose stools, diarrhea (diarrhea) and steatorrhea (high fat content in feces). Although the excretion of fat in the feces may increase, there is no indication that long-term treatment with octreotide can lead to the development of malabsorption. In rare cases, there may be phenomena resembling acute intestinal obstruction.
Gastrointestinal side effects may be reduced if octreotide injections are given between meals or at bedtime.
In case of pituitary tumors, careful monitoring of patients receiving the product is necessary, since an increase in the size of tumors with the development of such serious complications as visual impairment is possible. In these cases, the need for other treatments should be considered.
In the treatment of gastroenteropancreatic endocrine tumors with octreotide, in rare cases, a sudden relapse (recurrence) of symptoms may occur.
There are isolated cases of the development of acute hepatitis (inflammation of the liver tissue) without cholestasis (bile stasis), also hyperbilirubinemia (increased levels of bilirubin / bile pigment / in the blood) in combination with an increase in the activity of enzymes: alkaline phosphatase, gammaglutamyltransferase and, to a lesser extent, transaminases.
Prolonged use of the product may lead to the formation of gallstones. In 10-20% of patients receiving octreotide for a long time, gallstones may appear. Therefore, before starting treatment, also during treatment with octreotide (after 6-12 months), an ultrasound examination of the gallbladder is recommended. If gallstones are identified before starting treatment, the use of octreotide is decided on a case-by-case basis. Currently, there is no indication that octreotide can adversely affect the dynamics of the development of already existing gallstones or the prognosis of gallstone disease. If gallstones appear during treatment with the product, the issue of continuing treatment is decided individually. When, if there are no symptoms of gallstone disease and no special treatment is required, more frequent monitoring of the patient is indicated. If there are clinical manifestations of cholelithiasis, the conventional treatment of this disease, including therapy with bile acids, should be carried out.
Perhaps a violation of tolerance (tolerance) to glucose after eating (due to the suppression of insulin secretion by the product); in rare cases, with long-term treatment, persistent hyperglycemia (persistent increase in blood sugar) may develop.
Patients with insulinomas (tumors of the pancreas that produce insulin) may experience an increase in the severity and duration of glycemia during treatment with octreotide (this is due to the relatively less effect of the drug on the suppression of insulin secretion compared to the effect on the secretion of growth hormone and glucagon / pancreatic hormone, stimulating the formation of insulin/). Such patients should be closely monitored at the start of octreotide treatment, and also at each change in the dose of the product. Significant fluctuations in blood glucose concentrations can be attempted to be reduced by more frequent administration of the product.
In diabetic patients receiving insulin, octreotide may reduce the need for insulin.

Release form:
Solution for injection in ampoules of 1 ml (0.05, 0.1 or 0.5 mg of octreotide) in packs of 10; solution for injection in vials of 5 ml (1 g of octreotide).


Storage conditions:
At a temperature of +2 – +5 C. During use, ampoules and vials can be kept at room temperature for up to 2 weeks.

Before using the medication“Octreotide (Octreotide)” should be consulted with a doctor.
The instructions are provided solely for familiarization with “Octreotide (Octreotide) ».

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