Octreotide, 50 mcg/ml, solution for intravenous and subcutaneous administration, 1 ml, 5 pcs.


Octreotide, 50 mcg/ml, solution for intravenous and subcutaneous administration, 1 ml, 5 pcs.

Octreotide is a synthetic analogue of somatostatin, which is a derivative of the natural hormone somatostatin and has pharmacological effects similar to it, but a significantly longer duration of action. Octreotide suppresses the secretion of growth hormone, both pathologically increased and caused by arginine, exercise and insulin hypoglycemia. The drug also suppresses the secretion of insulin, glucagon, gastrin, serotonin, both pathologically increased and caused by food intake; also suppresses the secretion of insulin and glucagon stimulated by arginine. Octreotide suppresses the secretion of thyrotropin caused by thyrotropin-releasing hormone. Unlike somatostatin, octreotide suppresses growth hormone secretion to a greater extent than insulin secretion, and its administration is not accompanied by subsequent hypersecretion of hormones (for example, growth hormone in patients with acromegaly).

In patients with acromegaly, octreotide reduces the concentration of growth hormone and insulin-like growth factor (IGF-1) in the blood plasma. A decrease in the concentration of growth hormone by 50% or more is observed in 90% of patients, while a growth hormone concentration of at least 5 ng/ml is achieved in approximately half of the patients. In most patients with acromegaly, octreotide reduces the severity of headache, soft tissue swelling, hyperhidrosis, joint pain and paresthesia. In patients with large pituitary adenomas, treatment with octreotide may lead to some reduction in tumor size.

For secreting tumors of the gastroenteropancreatic endocrine system, in cases of insufficient effectiveness of the therapy (surgery, embolization of the hepatic artery, chemotherapy, including streptozotocin and fluorouracil), the administration of octreotide can lead to an improvement in the course of the disease. Thus, in carcinoid tumors, the use of octreotide can lead to a decrease in the severity of the sensation of flushing and diarrhea, which in many cases is accompanied by a decrease in the concentration of serotonin in plasma and the excretion of 5-hydroxyindoleacetic acid by the kidneys. For tumors characterized by overproduction of vasoactive intestinal peptide (VIP), the use of octreotide in most patients leads to a reduction in severe secretory diarrhea and, accordingly, an improvement in the patient’s quality of life. At the same time, there is a decrease in concomitant electrolyte imbalances, such as hypokalemia, which makes it possible to cancel enteral and parenteral administration of fluids and electrolytes. In some patients, tumor progression slows down or stops, its size decreases, as does the size of liver metastases. Clinical improvement is usually accompanied by a decrease in the plasma concentration of vasoactive intestinal peptide (VIP) or its normalization. For glucagonomas, the use of octreotide leads to a decrease in erythema migrans. Octreotide does not have any significant effect on the severity of hyperglycemia in diabetes mellitus, while the need for insulin or oral hypoglycemic drugs usually remains unchanged. The drug causes a decrease in diarrhea, which is accompanied by an increase in body weight. Although the decrease in plasma glucagon concentrations under the influence of octreotide is transient, clinical improvement remains stable throughout the period of drug use. In patients with gastrinomas/Zollinger-Ellison syndrome, when using octreotide as monotherapy or in combination with proton pump inhibitors or H2-histamine receptor blockers, it is possible to reduce the hypersecretion of hydrochloric acid in the stomach, reduce the concentration of gastrin in the blood plasma, as well as reduce the severity of diarrhea and tides In patients with insulinomas, octreotide reduces the level of immunoreactive insulin in the blood (this effect can be short-term - about 2 hours). In patients with operable tumors, octreotide can restore and maintain normoglycemia in the preoperative period. In patients with inoperable benign and malignant tumors, glycemic control may improve without a simultaneous prolonged decrease in blood insulin levels.

In patients with rare tumors that overproduce growth hormone releasing factor (somatoliberinomas), octreotide reduces the severity of symptoms of acromegaly. This is due to the suppression of the secretion of growth hormone releasing factor and growth hormone itself. In the future, pituitary hypertrophy may decrease.

For bleeding from varices of the esophagus and stomach in patients with liver cirrhosis, the use of octreotide in combination with specific treatment (for example, sclerotherapy) leads to more effective stoppage of bleeding and early rebleeding, a reduction in the volume of transfusions and an improvement in 5-day survival. The mechanism of action of octreotide is believed to be associated with a decrease in organ blood flow through the suppression of vasoactive hormones such as VIP and glucagon.

Pharmacokinetics

Suction

After subcutaneous administration, octreotide is rapidly and completely absorbed. Tmax of octreotide in plasma is within 30 minutes.

Distribution

The connection with blood plasma proteins is 65%. The binding of octreotide to blood cells is extremely insignificant. Vd is 0.27 l/kg.

Removal

T1/2 after subcutaneous administration of octreotide is 100 minutes. After intravenous administration, octreotide is eliminated in 2 phases, with T1/2 - 10 and 90 minutes, respectively. Most of octreotide is excreted through the intestines, about 32% is excreted unchanged by the kidneys. The total clearance is 160 ml/min.

Octreotide-depot 20 mg No. 1 bottle + solvent

Content

Indications for the drug Octreotide-depot Contraindications Use during pregnancy and breastfeeding Side effects Interaction Method of administration and dose Rules for the preparation of the suspension and administration of the drug Precautions for use Special instructions Storage conditions for the drug Octreotide-depot Shelf life of the drug Octreotide-depot

Indications for the drug Octreotide-depot

Acromegaly therapy:

  • when adequate control of disease manifestations is achieved through subcutaneous administration of octreotide;
  • in the absence of sufficient effect from surgical treatment and radiation therapy;
  • for preparation for surgical treatment;
  • for treatment between courses of radiation therapy until a lasting effect develops;
  • in inoperable patients.

Therapy of endocrine tumors of the gastrointestinal tract and pancreas:

  • carcinoid tumors with symptoms of carcinoid syndrome;
  • insulinomas;
  • VIPs;
  • gastrinomas (Zollinger-Ellison syndrome);
  • glucagonomas (to control hypoglycemia in the preoperative period, as well as for maintenance therapy);
  • somatoliberinomas (tumors characterized by overproduction of growth hormone releasing factor).

Therapy of hormone-resistant prostate cancer: as part of combination therapy against the background of surgical or medical castration.

Prevention of the development of acute postoperative pancreatitis: during extensive surgical operations on the abdominal cavity and thoracoabdominal interventions (including for cancer of the stomach, esophagus, colon, pancreas, primary and secondary tumor lesions of the liver).

Contraindications

Hypersensitivity to octreotide or other components of the drug.

With caution: cholelithiasis; diabetes; pregnancy and lactation.

Use during pregnancy and breastfeeding

There is no experience with the use of Octreotide Depot during pregnancy and breastfeeding. Therefore, during pregnancy, the drug is prescribed only if the potential benefit to the mother outweighs the potential risk to the fetus. Breastfeeding is not recommended when using the drug during lactation.

Side effects

  • Local reactions: with intramuscular administration of the drug Octreotide-depot, pain is possible, less often - swelling and rashes at the injection site (usually mild and short-lived).
  • From the gastrointestinal tract: anorexia, nausea, vomiting, cramping abdominal pain, bloating, excessive gas formation, loose stools, diarrhea, steatorrhea. Although the excretion of fat in the feces may be increased, there is no evidence to date that long-term treatment with octreotide may lead to the development of certain nutritional deficiencies due to malabsorption. In rare cases, phenomena resembling acute intestinal obstruction may occur: progressive bloating, severe pain in the epigastric region, tension in the abdominal wall. Long-term use of Octreotide Depot can lead to the formation of gallstones.
  • On the part of the pancreas: rare cases of acute pancreatitis that developed in the first hours or days of use of octreotide have been reported. With long-term use, cases of pancreatitis associated with cholelithiasis have been reported.
  • From the liver: there are isolated reports of the development of liver dysfunction (acute hepatitis without cholestasis with normalization of transaminases after discontinuation of octreotide); slow development of hyperbilirubinemia, accompanied by an increase in alkaline phosphatase, GGT, and to a lesser extent other transaminases.
  • From the metabolic side: since the drug Octreotide-depot has an inhibitory effect on the formation of growth hormone, glucagon and insulin, it can affect glucose metabolism. Possible decrease in glucose tolerance after meals. With long-term use of subcutaneous octreotide, persistent hyperglycemia may develop in some cases. Hypoglycemic states have also been observed.
  • Other: in rare cases, temporary hair loss has been reported after administration of octreotide, bradycardia, tachycardia, shortness of breath, skin rash, and anaphylaxis. There are isolated reports of the development of hypersensitivity reactions.

Interaction

Octreotide reduces the absorption of cyclosporine from the intestine and slows down the absorption of cimetidine.

With simultaneous use of octreotide and bromocriptine, the bioavailability of the latter increases.

There is literature evidence that somatostatin analogues may reduce the metabolic clearance of substances metabolized by cytochrome P450 enzymes, which may be caused by growth hormone suppression. Since similar effects of octreotide cannot be excluded, drugs metabolized by cytochrome P450 enzymes and with a narrow therapeutic index (quinidine and terfenadine) should be prescribed with caution.

Directions for use and doses

Intramuscularly, deep into the gluteal muscle. For repeated injections, the left and right sides should be alternated. The suspension should be prepared immediately before injection. On the day of injection, the bottle with the drug and the ampoule with the solvent can be kept at room temperature.

When treating acromegaly in patients for whom subcutaneous administration of octreotide provides adequate control of the manifestations of the disease, the recommended initial dose of Octreotide-depot is 20 mg every 4 weeks for 3 months. Treatment with Octreotide-depot can be started the day after the last subcutaneous administration of octreotide. Subsequently, the dose is adjusted taking into account the serum concentrations of growth hormone and IGF-1, as well as clinical symptoms. If after 3 months of treatment it is not possible to achieve an adequate clinical and biochemical effect (in particular, if the concentration of growth hormone remains above 2.5 mcg/l), the dose can be increased to 30 mg administered every 4 weeks.

In cases where, after 3 months of treatment with Octreotide-depot at a dose of 20 mg, there is a persistent decrease in the serum concentration of growth hormone below 1 μg/l, normalization of IGF-1 concentration and the disappearance of reversible symptoms of acromegaly, you can reduce the dose of Octreotide-depot to 10 mg. However, in these patients receiving a relatively small dose of Octreotide Depot, serum concentrations of growth hormone and IGF-1, as well as symptoms of the disease, should continue to be carefully monitored.

In patients receiving a stable dose of Octreotide Depot, growth hormone and IGF-1 concentrations should be determined every 6 months.

For patients in whom surgery and radiation therapy are ineffective or ineffective, and for patients who require short-term treatment between courses of radiation therapy until it is fully effective, it is recommended that a trial course of treatment with subcutaneous injections of octreotide be undertaken to evaluate its effectiveness and general tolerability and only after that switch to using the drug Octreotide-depot according to the above scheme.

In the treatment of endocrine tumors of the gastrointestinal tract and pancreas in patients for whom subcutaneous administration of octreotide provides adequate control of the manifestations of the disease, the recommended initial dose of Octreotide Depot is 20 mg every 4 weeks. Subcutaneous administration of octreotide should be continued for another 2 weeks after the first administration of Octreotide-depot.

In patients who have not previously received subcutaneous octreotide, it is recommended to begin treatment with subcutaneous administration of octreotide at a dose of 0.1 mg 3 times a day for a relatively short period of time (approximately 2 weeks) in order to assess its effectiveness and overall tolerability. Only after this is the drug Octreotide-depot prescribed according to the above scheme.

In cases where therapy with Octreotide-depot for 3 months provides adequate control of clinical manifestations and biological markers of the disease, it is possible to reduce the dose of Octreotide-depot to 10 mg, prescribed every 4 weeks.

In cases where, after 3 months of treatment with Octreotide-depot, only partial improvement was achieved, the dose of the drug can be increased to 30 mg every 4 weeks. During treatment with Octreotide-depot, on some days there may be an increase in clinical manifestations characteristic of endocrine tumors of the gastrointestinal tract and pancreas. In these cases, additional subcutaneous administration of octreotide is recommended at the dose used before the start of treatment with Octreotide-depot. This may occur mainly in the first 2 months of treatment, until therapeutic plasma concentrations of octreotide are achieved.

Secreting and non-secreting common (metastatic) neuroendocrine tumors of the jejunum, ileum, cecum, ascending colon, transverse colon and appendix or metastases of neuroendocrine tumors without a primary identified focus - the recommended dose of Octreotide-depot is 30 mg every 4 weeks.

Therapy with Octreotide Depot should be continued until signs of tumor progression.

When treating HRPC, the recommended initial dose of Octreotide-depot is 20 mg every 4 weeks for 3 months. Subsequently, the dose is adjusted taking into account the dynamics of PSA concentration in the serum, as well as clinical symptoms. If after 3 months of treatment it was not possible to achieve an adequate clinical and biochemical effect (decrease in PSA), the dose can be increased to 30 mg administered every 4 weeks.

Treatment with Octreotide-depot is combined with the use of dexamethasone, which is prescribed orally according to the following regimen: 4 mg/day for 1 month, then 2 mg/day for 2 weeks, then 1 mg/day (maintenance dose).

Treatment with Octreotide-depot and dexamethasone in patients who have previously received drug antiandrogen therapy is combined with the use of a GnRH analogue. In this case, an injection of a GnRH analogue (depot form) is carried out once every 4 weeks.

For patients receiving Octreotide Depot, PSA concentrations should be determined every month.

In patients with impaired renal function, liver function and elderly patients, there is no need to adjust the dosage regimen of the drug Octreotide-depot.

To prevent acute postoperative pancreatitis, the drug Octreotide-depot in a dose of 10 or 20 mg is administered once, no earlier than 5 days and no later than 10 days before the intended surgical intervention.

Rules for preparing the suspension and administering the drug

  • the drug should only be administered intramuscularly;
  • prepare the suspension for intramuscular injection using the supplied solvent immediately before administration;
  • Only specially trained medical personnel should prepare and administer the drug;
  • before injection, the ampoule with the solvent and the bottle with the drug must be removed from the refrigerator and brought to room temperature (30–50 minutes are required);
  • Keep the bottle with Octreotide-depot strictly vertical. Lightly tapping the bottle to ensure that all the lyophilisate is at the bottom of the bottle;
  • open the package with the syringe, attach a 1.2 × 50 mm needle to the syringe to withdraw the solvent;
  • open the ampoule with the solvent and draw the entire contents of the ampoule with the solvent into the syringe, set the syringe to a dose of 2 ml;
  • remove the plastic cap from the bottle containing the lyophilisate. Disinfect the rubber stopper of the bottle with an alcohol swab. Insert the needle into the bottle with the lyophilisate through the center of the rubber stopper and carefully introduce the solvent along the inner wall of the bottle, without touching the contents of the bottle with the needle. Remove the syringe from the bottle;
  • the bottle should remain motionless until the lyophilisate is completely saturated with the solvent and a suspension is formed (approximately 3–5 minutes). After which, without turning the bottle over, you should check for the presence of dry lyophilisate on the walls and bottom of the bottle. If dry residues of the lyophilisate are detected, leave the bottle until completely saturated;
  • After the health care worker ensures that there are no residues of dry lyophilisate, the contents of the bottle should be carefully mixed in a circular motion for 30–60 s until a homogeneous suspension is formed. Do not turn over or shake the bottle; this may cause flakes to fall out and the suspension to become unusable;
  • quickly insert the needle through the rubber stopper into the bottle. Then lower the cut of the needle down and, tilting the bottle at an angle of 45°, slowly draw the entire suspension into the syringe. Do not invert the bottle when taking it. A small amount of the drug may remain on the walls and bottom of the bottle. Consumption for the residue on the walls and bottom of the bottle is taken into account;
  • immediately after drawing the suspension, replace the needle with a pink pavilion with a needle with a green pavilion (0.8×40 mm), carefully turn the syringe over and remove air from the syringe;
  • administer the Octreotide-depot suspension immediately after preparation;
  • the suspension of the drug Octreotide-depot should not be mixed with any other drug in the same syringe;
  • Use an alcohol swab to disinfect the injection site. Insert the needle deep into the gluteal muscle, then pull the syringe plunger back slightly to ensure that there is no damage to the vessel. Inject the suspension intramuscularly slowly, with constant pressure on the syringe plunger;
  • if it gets into a blood vessel, the injection site and needle should be changed;
  • if the needle becomes clogged, replace it with another needle of the same diameter;
  • with repeated injections, the left and right sides should be alternated.

Precautions for use

For pituitary tumors that secrete growth hormone, careful monitoring of patients is necessary, because it is possible that the size of the tumors may increase with the development of such a serious complication as a narrowing of the visual fields. In these cases, the need for other treatment methods should be considered.

Gallstones may develop in 15–30% of patients receiving subcutaneous octreotide for a long time. Prevalence in the general population (ages 40–60 years) is 5–20%. Experience of long-term treatment with long-acting octreotide in patients with acromegaly and tumors of the gastrointestinal tract and pancreas indicates that long-acting octreotide, in comparison with short-acting octreotide, does not lead to an increase in the incidence of gallstones. However, it is recommended to perform an ultrasound scan of the gallbladder before starting treatment with Octreotide Depot and approximately every 6 months during treatment. Gallstones, if they are found, are usually asymptomatic. If clinical symptoms are present, conservative treatment (for example, the use of bile acid preparations) or surgery is indicated.

In patients with type 1 diabetes mellitus, Octreotide Depot can affect glucose metabolism and, therefore, reduce the need for administered insulin. For patients with type 2 diabetes mellitus and patients without concomitant carbohydrate metabolism disorders, subcutaneous injections of octreotide may lead to postprandial glycemia. In this regard, it is recommended to regularly monitor the concentration of glucose in the blood and, if necessary, adjust hypoglycemic therapy.

In patients with insulinomas, during treatment with octreotide, an increase in the severity and duration of hypoglycemia may be observed (this is due to a more pronounced suppressive effect on the secretion of growth hormone and glucagon than on insulin secretion, as well as a shorter duration of the inhibitory effect on insulin secretion). Systematic monitoring of these patients is indicated.

Before prescribing octreotide, patients should undergo a baseline ultrasound of the gallbladder.

During treatment with Octreotide Depot, repeat ultrasound of the gallbladder should be performed, preferably at intervals of 6–12 months.

If gallstones are detected before starting treatment, it is necessary to evaluate the potential benefits of therapy with Octreotide Depot versus the possible risks associated with the presence of gallstones.

Currently, there is no evidence that Octreotide Depot adversely affects the course or prognosis of existing gallstone disease.

Management of patients in whom gallstones form during treatment with Octreotide-depot

Asymptomatic gallstones. The use of the drug Octreotide-depot can be stopped or continued - in accordance with the assessment of the benefit/risk ratio. In any case, no other measures are required other than continuing inspections, making them more frequent if necessary.

Gallstones with clinical symptoms. The use of the drug Octreotide-depot can be stopped or continued - in accordance with the assessment of the benefit/risk ratio. In any case, the patient should be treated in the same way as in other cases of cholelithiasis with clinical manifestations. Drug treatment includes the use of combinations of bile acid preparations (for example, chenodeoxycholic acid at a dose of 7.5 mg cm/day in combination with UDCA at the same dose) under ultrasound control until the stones completely disappear.

special instructions

Special precautions when destroying unused medicinal products. The bottle with the drug, syringe and needles are destroyed separately.

Influence on the ability to drive a car and other mechanisms. Currently, there is no data on the effect of the drug Octreotide-depot on the ability to drive a car and operate machinery, which requires increased attention and speed of mental and motor reactions.

Storage conditions for the drug Octreotide-depot

In a dry place, protected from light, at a temperature of 2 to 8 °C.

Keep out of the reach of children.

Shelf life of the drug Octreotide-depot

Lyophilisate - 3 years; solvent - 5 years.

Do not use after the expiration date stated on the package.

Use of the drug Octreotide

For acromegaly, octreotide is first administered at 0.05–0.1 mg subcutaneously at intervals of 8 or 12 hours. Subsequently, the dose is selected individually. Typically, the optimal daily dose is 0.2–0.3 mg. The maximum dose of 1.5 mg per day should not be exceeded. If after 3 months of treatment there is no sufficient reduction in growth hormone levels and improvement in the clinical picture of the disease, therapy should be discontinued. For endocrine tumors of the digestive tract and pancreas, octreotide is administered subcutaneously at an initial dose of 0.05 mg 1–2 times a day. Subsequently, 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 octreotide can be gradually increased to 0.1–0.2 mg 3 once a day. In exceptional cases, higher doses may be required. Maintenance doses are selected individually. For refractory diarrhea in patients with AIDS, octreotide is administered subcutaneously at an initial dose of 0.1 mg 3 times a day. If after 1 week of treatment the symptoms of diarrhea do not disappear, the dose should be increased individually up to 0.25 mg 3 times a day. Dose adjustment is carried out taking into account the dynamics of bowel movements and tolerability of the drug. If no improvement occurs within 1 week of treatment with octreotide at a dose of 0.25 mg 3 times daily, therapy should be discontinued. To prevent complications after pancreatic surgery, 0.1 mg is administered subcutaneously 3 times a day for 7 consecutive days starting from the day of surgery (at least 1 hour before laparotomy). For bleeding from varicose veins of the esophagus, a dose of 25 mcg/hour is administered by continuous intravenous infusion for 5 days.

Special instructions for the use of the drug Octreotide

In case of a pituitary tumor that secretes growth hormone, strict medical supervision of patients receiving octreoid is necessary, since it is possible that the size of the tumors may increase with the development of such a serious complication as a narrowing of the visual fields. When treating endocrine tumors of the digestive tract and pancreas with octreotide, in rare cases a sudden relapse of the disease may occur. In patients with insulinoma during treatment with octreoid, an increase in the severity and duration of hypoglycemia may be observed. In diabetic patients receiving insulin, Octreoid may reduce the need for insulin. There is no experience with the use of Octreoid during pregnancy and lactation; during this period the drug is prescribed only for absolute indications.

Octreotide

Octreotide is a synthetic octapeptide that is a derivative of the natural hormone somatostatin and has similar pharmacological properties, but a significantly longer duration of action. Octreotide inhibits the secretion of growth hormone (GH), as well as peptides and serotonin produced by secreting endocrine tumors of the gastrointestinal tract (GIT) and pancreas. In healthy volunteers, octreotide, like somatostatin, suppressed GH secretion induced by arginine, exercise, and insulin hypoglycemia. Octreotide suppresses the secretion of insulin, glucagon, gastrin and other peptides secreted by endocrine tumors of the gastrointestinal tract and pancreas, caused by food intake, and also suppresses the secretion of insulin and glucagon stimulated by arginine. Octreotide also suppresses thyrotropin secretion caused by thyrotropin-releasing hormone.

Unlike somatostatin, octreotide suppresses GH secretion to a greater extent than insulin secretion, and its use is not accompanied by subsequent negative feedback hypersecretion of hormones (for example, GH in patients with acromegaly).

The use of octreotide before and after pancreatic surgery reduced the incidence of typical postoperative complications (for example, the formation of pancreatic fistulas, abscesses and the development of sepsis and postoperative acute pancreatitis).

Acromegaly

In patients with acromegaly, octreotide reduces plasma concentrations of GH and insulin-like growth factor 1 (IGF-1). In most patients, octreotide reduced the severity of clinical symptoms of the disease - headache, hyperhidrosis, paresthesia, fatigue, joint pain and carpal tunnel syndrome. In selected patients with pituitary adenoma, the use of octreotide led to a reduction in tumor size.

Secreting endocrine tumors of the gastrointestinal tract and pancreas

In patients with secreting endocrine tumors of the gastrointestinal tract and pancreas, in cases of insufficient effectiveness of therapy (surgery, hepatic artery embolization, chemotherapy, including streptozotocin and fluorouracil), the use of octreotide may lead to an improvement in the course of the disease. The effect of octreotide on tumor size, progression and metastasis has not been clearly demonstrated.

Carcinoid tumors

The use of octreotide may lead to a decrease in the severity of symptoms of the disease, especially flushing and diarrhea. In many cases, clinical improvement is accompanied by a decrease in plasma serotonin concentrations and renal excretion of 5-hydroxyindoleacetic acid.

Tumors

,
characterized by overproduction of vasoactive intestinal peptide (VIPomas)
The use of octreotide for VIPomas in most cases leads to a decrease in the severe secretory diarrhea typical of this disease, which in turn leads to an improvement in the patient’s quality of life. At the same time, there is a decrease in concomitant electrolyte imbalances, for example, hypokalemia, which makes it possible to cancel enteral and parenteral administration of fluids and electrolytes. In some patients, tumor progression slowed down or stopped, its size decreased, as well as the size of liver metastases. Clinical improvement is usually accompanied by a decrease in plasma vasoactive intestinal peptide (VIP) concentrations to normal values.

Glucagonoma

The use of octreotide in most cases leads to a significant reduction in erythema migrans, which is characteristic of this disease. Octreotide does not have a significant effect on the severity of hyperglycemia in diabetes mellitus, while the need for insulin and oral hypoglycemic drugs usually remains unchanged. Octreotide significantly reduces diarrhea, which is accompanied by an increase in body weight. Although the decrease in plasma glucagon concentrations under the influence of octreotide is transient, clinical improvement remains stable throughout the period of drug use.

In patients with gastrinomas/Zolliiger-Ellisol syndrome

when using octreotide as monotherapy or in combination with proton pump inhibitors or H2-histamine receptor blockers, it is possible to reduce hypersecretion of hydrochloric acid in the stomach, reduce the concentration of gastrin in the blood plasma, as well as reduce the severity of diarrhea and “flushing” of blood to the face.

In patients with insulinomas

octreotide reduces the concentration of immunoreactive insulin in the blood (this effect can be short-term - about 2 hours). In patients with operable tumors, octreotide can restore and maintain normoglycemia in the preoperative period. In patients with inoperable benign or malignant tumors, glycemic control may improve without a simultaneous prolonged decrease in blood insulin concentrations.

In patients with rare tumors

,
hyperproducing GH-releasing factor
(somatoliberinomas), octreotide reduces the severity of acromegaly symptoms. This is due to the suppression of the secretion of growth hormone releasing factor and GH itself. In the future, pituitary hypertrophy may decrease.

Prevention of complications after pancreatic surgery

Studies have shown that the use of octreotide during or after pancreatic surgery reduces the incidence of a typical postoperative complication such as fistula formation. The incidence of other postoperative complications, such as abscess development, which increases the risk of sepsis, and acute pancreatitis, is reduced to a lesser extent. The study included patients who had undergone elective pancreatectomy and/or pancreaticojejunostomy for pancreatic tumors, periampullary carcinoma, or chronic pancreatitis.

Side effects of the drug Octreotide

Possible pain, itching or burning sensation, redness and swelling at the injection site, anorexia, nausea, vomiting, cramping abdominal pain, bloating, flatulence, loose stools, diarrhea and steatorrhea, phenomena resembling acute intestinal obstruction (progressive bloating, severe pain in the epigastric region, muscle protection), formation of gallstones (with long-term use in 10–20% of patients), acute pancreatitis, hair loss, liver dysfunction, including acute hepatitis without cholestasis, hyperbilirubinemia, accompanied by increased alkaline levels phosphatases, γ-glutamyltransferases and, to a lesser extent, transaminases, decreased glucose tolerance, persistent hyperglycemia or hypoglycemia (with long-term use).

Indications for use of the drug Octreotide

Acromegaly (control of the main manifestations of the disease and a decrease in the level of growth hormone and somatomedin C in the blood plasma in cases where the effect of surgical treatment, radiation therapy and treatment with dopamine agonists is not sufficient); relief of symptoms of endocrine tumors of the digestive tract and pancreas: carcinoid tumors with the presence of carcinoid syndrome; VIPs; glucagonomas; gastrinomas/Zollinger-Ellison syndrome (usually in combination with H2-histamine receptor blockers); insulinomas (to control hypoglycemia in the preoperative period, as well as for maintenance therapy); somatoliberins; refractory diarrhea in patients with AIDS; prevention of complications after pancreatic surgery; stopping bleeding and preventing re-bleeding from esophageal varices in patients with cirrhosis of the liver (in combination with specific therapeutic measures, for example, endoscopic sclerotherapy).

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