Octreotide: instructions for use of injection solution. Instructions for the drug Octreotide: why reduce the secretion of glands and how to do it correctly Octreotide side effects

Octreotide

pharmachologic effect

Octreotide is a synthetic octapeptide, which is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but 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 suppresses 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, as well as secretion of insulin and glucagon stimulated by arginine; secretion of thyrotropin (a pituitary hormone that regulates thyroid function) caused by thyrotropin-releasing hormone.
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, stimulating tissue growth and exhibiting 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 approximately 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 blisters), 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 may lead to a decrease in the severity of symptoms such as flushing and diarrhea, which in many cases is accompanied by a decrease in plasma serotonin concentrations and a decrease in the excretion of 5-hydroxyindoleacetic acid in the urine.
For tumors characterized by overproduction (increased formation) of vasoactive intestinal peptide, the use of octreotide leads to a reduction in severe secretory diarrhea (diarrhea) in most patients. At the same time, there is a decrease in concomitant disturbances in the electrolyte (ion) balance, for example, hypokalemia (low potassium levels in the blood). In some patients, tumor progression slows or stops and even reduces its size. Clinical improvement is usually accompanied by a decrease (down to normal values) in the concentration of vasoactive intestinal peptide in the blood plasma.
In case of glucagonomas (malignant tumor/cancer/of the pancreas that produces insulin), the use of octreotide in most cases leads to a noticeable reduction in the necrotizing (leading to tissue death) migratory rash; body weight decreases (the effect on diabetes mellitus, however, is insignificant). For gastronomas (malignant tumor / cancer / of the stomach), Zollinger-Ellison syndrome (a complex of symptoms when a gastric and duodenal ulcer is combined with a benign pancreatic tumor), octreotide reduces hypersecretion (increased secretion) of hydrochloric acid in the stomach and associated symptoms, including diarrhea , feeling of rush of blood. Some patients experience a decrease in the concentration of gastrin (a protein secreted by the gastric mucosa, which causes an increase in the secretion of digestive juices by the stomach and pancreas) in the blood plasma.
In patients with insulinomas (tumors of the pancreas that produce insulin), octreotide normalizes glycemia (reduces high blood sugar) by reducing the level of insulin in the blood (this effect, however, may be short-lived - about 2 hours). Glycemic control can improve without a simultaneous long-term decrease in blood insulin levels.
In patients with tumors that overproduce growth hormone releasing factor (producing increased amounts of hypothalamic neurohormones that promote the pituitary gland to release growth hormone), 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) who suffer from severe diarrhea (diarrhea) refractory to anti-infective or other therapy, the use of octreotide leads to complete or partial normalization of stool in approximately one third of cases.
In patients undergoing surgery on the pancreas, the use of the drug during and after surgery reduces the incidence of typical postoperative complications (for example, pancreatic fistulas /canals that form as a result of disease that connect the pancreas with internal organs or the external environment/, abscesses /ulcers/ , sepsis / blood poisoning by microbes from the focus of purulent inflammation /, postoperative acute pancreatitis / inflammation of the pancreas/).

Indications for use

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

Mode of application

For acromegaly, the drug is initially administered at 0.05-0.1 mg subcutaneously at intervals of 8 or 12 hours. Subsequent dose selection should be based on monthly determinations of the concentration of growth hormone in the blood, analysis of clinical symptoms and tolerability of the drug. In most patients, the optimal daily dose is 0.2-0.3 mg. The maximum dose is 1.5 mg per day. If after three months of treatment with octreotide 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 gastroenteropancreatic system, the drug 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 drug can be gradually increased to 0.1 -0.2 mg 3 once a day. In exceptional cases, higher doses may be required. Maintenance doses of the drug should be selected individually.
For refractory diarrhea in AIDS patients, the drug is administered subcutaneously in an initial dose (0.1 mg) 3 times a day. If after one week of treatment diarrhea does not subside, the dose of the drug should be increased individually, up to 0.25 mg 3 times a day. The dose of the drug should be selected based on monitoring the volume of stool and tolerability of the drug. If no improvement occurs within a week of treatment with octreotide at a dose of 0.25 mg 3 times a day, discontinue therapy.
To prevent complications after pancreatic surgery, the first dose of 0.1 mg is administered subcutaneously 1 hour before laparotomy (opening the abdominal cavity); then after surgery, 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 drug solution to room temperature before administration and administer a smaller volume of the drug. Multiple injections at the same site at short intervals should be avoided. To prevent bacterial contamination, it is recommended to pierce the stopper of a multi-dose vial no more than 10 times.

Side effects

Anorexia (lack of appetite), nausea, vomiting, cramping 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 stool). Although the excretion of fat in the feces may be increased, there is no indication that long-term treatment with octreotide may lead to malabsorption problems. In rare cases, phenomena resembling acute intestinal obstruction may occur.
Gastrointestinal side effects may be reduced if octreotide injections are given between meals or at bedtime.
For pituitary tumors, careful monitoring of patients receiving the drug is necessary, since it is possible that the size of the tumors may increase with the development of such serious complications as visual impairment. In these cases, the need for other treatment methods should be considered.
When treating gastroenteropancreatic endocrine tumors with octreotide, in rare cases a sudden recurrence of symptoms may occur.
There are isolated cases of the development of acute hepatitis (inflammation of liver tissue) without cholestasis (stagnation of bile), as well as hyperbilirubinemia (increased content 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 .
Long-term use of the drug can lead to the formation of gallstones. 10-20% of patients receiving octreotide for a long time may develop gallstones. Therefore, before starting treatment, as well as during treatment with octreotide (every 6-12 months), an ultrasound examination of the gallbladder is recommended. If gallstones are detected before starting treatment, the question of using octreotide is decided individually. There is currently no indication that octreotide may adversely affect the development of existing gallstones or the prognosis of gallstone disease. If gallstones appear during treatment with the drug, the issue of continuing treatment is decided individually. If there are no symptoms of cholelithiasis and no special treatment is required, more frequent monitoring of the patient is indicated. If there are clinical manifestations of cholelithiasis, standard treatment of this disease should be carried out, including therapy with bile acid preparations.
Possible impairment of glucose tolerance (tolerance) after meals (due to suppression of insulin secretion by the drug); in rare cases, with long-term treatment, persistent hyperglycemia (persistent increase in blood sugar) may develop.
In patients with insulinomas (tumors of the pancreas that produce insulin), during treatment with octreotide, an increase in the severity and duration of glycemia may be observed (this is due to the relatively lesser effect of the drug on suppressing 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 carefully monitored at the start of treatment with octreotide, as well as whenever the dose of the drug is changed. Significant fluctuations in blood glucose concentrations can be reduced by administering the drug more frequently.
In diabetic patients receiving insulin, octreotide may reduce insulin requirements.

Links

Official instructions for the drug Octreotide.
Modern drugs: a complete practical guide. Moscow, 2000. S. A. Kryzhanovsky, M. B. Vititnova.

Attention!
Description of the drug " Octreotide"on this page is a simplified and expanded version of the official instructions for use. Before purchasing or using the drug, you should consult your doctor and read the instructions approved by the manufacturer.
Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use. The description is valid on 29.09.2014

Latin name: Octreotide
ATX code: H01CB02
Active substance: Octreotide
Manufacturer: F-Sintez JSC (Russia)

Compound

The solution contains an active component octreotide , presented as free . Auxiliary components: sodium chloride and water for injection.

Octreotide-Depot includes: active substance - Octreotide, auxiliary components: copolymer of DL-lactic and glycolic acids, D-mannitol, carboxymethylcellulose sodium salt, polysorbate-80, mannitol and water for injection.

Octreotide-Long consists of active substance octreotide acetate and additional components: DL-lactic and glycolic acid copolymer, D-mannitol, sodium carmellose, polysorbate-80.

Release form

The medicine is available in the form of an injection solution, placed in 1 ml ampoules or 5 ml bottles.

Octreotide-Depot And Octreotide-Long are available in the form of a lyophilized powder or a compacted and porous mass in the form of light-colored tablets of various dosages. Additionally, a colorless transparent solvent and a reconstituted suspension are included, which is a homogeneous suspension of a light shade.

Also, these medicinal variations can be offered in the form of a lyophilisate for the preparation of a suspension intended for intramuscular administration with a prolonged action of 0.01-0.03 g of the active component in dark glass bottles. In addition, the package contains a 2 ml ampoule with solvent, a disposable syringe, sterile needles and alcohol swabs. One set is designed to complete one .

pharmachologic effect

The drug has somatostatin-like action.

Pharmacodynamics and pharmacokinetics

This drug is a synthetic analogue , which has similar pharmacological effects, but a longer action.

Treatment with Octreotide is performed when suppression of growth hormone secretion, increased pathologically or caused by arginine , insulin hypoglycemia or physical activity. As a result, it is reduced insulin secretion and, which can also be increased pathologically or caused by food intake. Suppression of secretion was noted insulin and , which stimulates arginine , decreased secretion thyrotropin , caused by .

Using the drug before or during pancreatic surgery can reduce the incidence of typical postoperative complications, for example: pancreatic fistulas, sepsis, acute postoperative.

Therapy of bleeding from varicose veins in the gastrointestinal tract in patients suffering in combination with specific treatment - sclerosing and hemostatic - helps to effectively stop bleeding and prevent recurrent bleeding.

The active substance is rapidly and completely absorbed inside the body. In this case, the maximum concentration of Octreotide in the blood plasma is achieved after 30 minutes. The component is 65% bound to plasma proteins, but its connection with blood cells is very insignificant. The drug is eliminated in several phases through the intestines and the kidneys.

Indications for use

Octreotide-based drugs are prescribed for:

, if ineffectiveness is noted agonists , and also if it is impossible to perform surgical or radiation therapy;
endocrine tumors gastroenteropancreatic system;
glucagonomas, gastrinomas;
insulinomas,somatoliberinoma;
refractory in patients;
operations on the pancreas, including in the prevention of complications;
, preventing relapses in cases of varicose veins of the esophagus with cirrhosis of the liver, and so on.

Contraindications for use

The main contraindication to the use of this drug is hypersensitivity.

Caution is required when treating patients cholelithiasis, , at and .

Side effects

When treated with Octreotide, disturbances in the functioning of the gastrointestinal tract may occur in the form of: vomiting, nausea, anorexia , pain, , With theatorrhea, intestinal obstruction, acute hepatitis without cholestasis, increased activity of liver transaminases, hyperbilirubinemia, acute and others.

May also develop alopecia And . Local manifestations cannot be excluded: soreness, burning, redness or swelling . Long-term use is often accompanied by the formation of gallstones, decreased glucose tolerance, persistent hyperglycemia, hypoglycemia.

Octreotide, instructions for use (Method and dosage)

The drug Octreotide is intended for intravenous, intramuscular or subcutaneous administration . The dosage is set individually, taking into account the nature of the disease and the characteristics of the patient. For example, acromegaly and tumors of the gastroenteropancreatic system require subcutaneous administration of 50–100 mcg 1-2 times daily. To prevent complications as a result of operations on the pancreas, it involves subcutaneous administration of the first dose an hour before laparotomy, then 100 mcg is administered 3 times daily for a week. When it is necessary to stop bleeding from varicose veins of the gastrointestinal tract, continuous intravenous infusions of 25 mcg/hour are administered for at least 5 days.

Instructions for use Octreotide-Depot And Octreotide-Long FS states that they are intended for deep intramuscular injection into the gluteal muscle. When subcutaneous administration of Octreotide allows patients to adequately control the manifestation of the disease, an initial dose of Depo and Long is prescribed at 20 mg, every 4 weeks for 3 months. The dosage is then adjusted based on biological markers of the disease and clinical symptoms.

If patients have not previously received subcutaneous Octreotide, then therapy should be started with this particular drug and method for 2 weeks. This approach will allow us to evaluate its effectiveness and tolerability, after which treatment with Octreotide-Depot or Long can be performed.

Overdose

In case of an overdose of Octreotide or Octreotide-Long, the following may occur: short-term decrease in heart rate , abdominal pain spastic nature, nausea , flushing of the face, . In this case, symptomatic treatment is carried out.

Cases of overdose with Octreotide-Depot have not been described in clinical practice.

Interaction

Simultaneous use of the drug with lowers its level in the serum and slows down absorption cimetidine and useful components from the gastrointestinal tract. If Octreotide is prescribed together with insulin , oral hypoglycemic drugs,beta blockers , BKK and diuretics, it is necessary to make adjustments to their dosage. Concomitant use with may increase its bioavailability.

This drug has been found to reduce the metabolic clearance of substances that are metabolized by cytochrome P450 enzymes caused by growth hormone suppression. Therefore, caution should be exercised when prescribing such drugs.

Terms of sale

Each form of the drug is released strictly according to prescription

Storage conditions

To store these drugs, it is necessary to provide a dry, dark place with a temperature of 2-8 degrees, well protected from children.

Best before date

The lyophilisate and solvent can be used for 3 years.

The Depot and Long forms remain suitable for 2 years. The finished product remains effective for no longer than 6 hours.

Octreotide analogues

Level 4 ATX code matches:

In pharmacology there are numerous analogues of Octreotide, the main one is .

The following have a similar effect: Somatostatin, And Sermorelin .

Alcohol

As is known, alcohol can suppress the synthesis , therefore its use with any form of Octreotide is contraindicated.

Reviews about Octreotide

It should be noted that online discussions regarding the use of this drug and its effectiveness are rare. Typically, users ask questions to specialists asking how effective therapy is for a particular disorder.

However, in clinical practice, the Depo form is predominantly used. At the same time, reviews on Octreotide-Depot show that it is used for pancreatitis , as well as acute and chronic forms of this disorder. Of course, this remedy is prescribed only by a specialist and you should expect that treatment will be carried out for at least a week.

Octreotide price, where to buy

Buy in Moscow Octreotide-Long FS 10 mg in the form of a microsphere for the preparation of a medicinal suspension intended for intramuscular administration can range from 30-32 thousand rubles.

Price Octreotide-Depot 20 mg is 46-48 thousand rubles.

Online pharmacies in Russia Russia
Online pharmacies in Ukraine Ukraine

Education: Graduated from Rivne State Basic Medical College with a degree in Pharmacy. Graduated from Vinnitsa State Medical University named after. M.I. Pirogov and internship at his base.

Experience: From 2003 to 2013, she worked as a pharmacist and manager of a pharmacy kiosk. She was awarded diplomas and decorations for many years of conscientious work. Articles on medical topics were published in local publications (newspapers) and on various Internet portals.

Note!

Information about medications on the site is for reference and general information, collected from publicly available sources and cannot serve as a basis for making a decision on the use of medications in the course of treatment. Before using the drug Octreotide, be sure to consult with your doctor.

In this article you can read the instructions for use of the drug Octreotide. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Octreotide in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Octreotide analogues in the presence of existing structural analogues. Use for the treatment of pancreatitis, bleeding from gastrointestinal ulcers in adults, children, as well as during pregnancy and lactation. Composition of the drug.

Octreotide- a synthetic analogue of somatostatin, which has similar pharmacological effects, but a significantly longer duration of action.

The drug suppresses the secretion of growth hormone, both pathologically increased and caused by arginine, physical 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.

In patients undergoing pancreatic surgery, the use of octreotide before, during and after surgery reduces the incidence of typical postoperative complications (eg, pancreatic fistulas, abscesses, sepsis, acute postoperative pancreatitis).

When bleeding from varicose veins of the esophagus and stomach in patients with liver cirrhosis, the use of octreotide in combination with specific treatment (for example, sclerosing and hemostatic therapy) leads to more effective stoppage of bleeding and prevention of rebleeding.

The drug Octreotide Depot is a long-acting dosage form of octreotide for intramuscular administration, ensuring the maintenance of stable therapeutic concentrations of octreotide in the blood for 4 weeks. Octreotide is a means of pathogenetic therapy for tumors that actively express somatostatin receptors. Octreotide is a synthetic octapeptide that is a derivative of the natural hormone somatostatin and has pharmacological effects similar to it, but a significantly longer duration of action. The drug suppresses the pathologically increased secretion of growth hormone (GH), as well as peptides and serotonin produced in the gastroenteric-pancreatic endocrine system.

Compound

Octreotide + excipients.

Pharmacokinetics

After subcutaneous administration, Octreotide is quickly and completely absorbed. Plasma protein binding is 65%. The binding of Octreotide to blood cells is extremely insignificant. After intravenous administration, octreotide is eliminated in 2 phases with half-lives of 10 minutes and 90 minutes, respectively. Most of octreotide is excreted through the intestines, about 32% is excreted unchanged by the kidneys.

Indications

treatment of acute pancreatitis;
stopping bleeding from gastric and duodenal ulcers;
stopping bleeding and preventing re-bleeding from esophageal varices in patients with cirrhosis of the liver;
prevention of complications after pancreatic surgery;
diarrhea in AIDS patients, refractory to other types of therapy.

In the treatment of acromegaly:

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.

In the treatment 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);
treatment of patients with secreting and non-secreting common (metastatic) neuroendocrine tumors of the jejunum, ileum, cecum, ascending colon, transverse colon and vermiform appendix, or metastases of neuroendocrine tumors without a primary identified focus.

In the treatment of hormone-resistant prostate cancer:

as part of combination therapy against the background of surgical or medical castration.

To prevent 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).

Release forms

Solution for intravenous and subcutaneous administration 50 mcg and 100 mcg.

Solution for infusion and subcutaneous administration (Octreotide Actavis).

Lyophilisate for the preparation of a suspension for intramuscular administration of prolonged action 10 mg, 20 mg and 30 mg (Octreotide Depot).

Lyophilisate for the preparation of a solution for intramuscular administration of prolonged action (microspheres) 20 mg (Octreotide Long).

Instructions for use and dosage

The dose is set individually, depending on the nature of the disease, the treatment regimen, as well as the dosage form used.

Octreotide in the form of a dosage form with a normal duration of action is used subcutaneously and intravenously (in the form of a dropper), in the form of a depot form - deep intramuscularly.

For the treatment of acute pancreatitis, the drug is administered subcutaneously at a dose of 100 mcg 3 times a day for 5 days. It is possible to prescribe up to 1200 mcg per day using the intravenous route of administration.

To stop ulcer bleeding, it is administered intravenously at a dose of 25-50 mcg/hour in the form of intravenous infusions for 5 days.

To stop bleeding from varicose veins of the esophagus, it is administered intravenously at a dose of 25-50 mcg/hour in the form of continuous intravenous infusions for 5 days.

To prevent complications after pancreatic surgery, the first dose of 100-200 mcg is administered subcutaneously 1-2 hours before laparotomy; then after surgery, 100-200 mcg is administered subcutaneously 3 times a day for 5-7 consecutive days.

Depot

Octreotide Depot should only be administered deep intramuscularly (IM), 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 GH 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 GH remains above 2.5 μg/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 GH below 1 mcg/l, normalization of IGF-1 concentrations and the disappearance of reversible symptoms of acromegaly, the dose of Octreotide Depot can be reduced to 10 mg. However, in these patients receiving a relatively small dose of Octreotide Depot, serum concentrations of GH and IGF-1, as well as disease symptoms, should continue to be closely monitored.

For patients receiving a stable dose of Octreotide Depot, GH 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 octreotide subcutaneously, 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 advanced (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 the drug should be continued until signs of tumor progression.

For the treatment of hormone-resistant prostate cancer, the recommended starting 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 is 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 per day for 1 month, then 2 mg per day for 2 weeks, then 1 mg per 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 gonadotropin-releasing hormone (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 in elderly patients, there is no need to adjust the dosage regimen of Octreotide Depot.

To prevent acute postoperative pancreatitis, 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 Octreotide Depot is administered only intramuscularly. A suspension for intramuscular injection is prepared using the supplied solvent immediately before administration. The drug should be prepared and administered only by specially trained medical personnel.

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. By lightly tapping the bottle, ensure that all the lyophilisate is at the bottom of the bottle.

Open the package with the syringe and attach a 1.2 mm x 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 2.0 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 vial with the lyophilisate through the center of the rubber stopper and carefully inject the solvent along the inner wall of the vial, without touching the contents of the vial with the needle.

Remove the syringe from the vial. The bottle should remain motionless until the lyophilisate solvent 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 the presence of dry lyophilisate at the walls and bottom of the bottle. If dry residues of the lyophilisate are detected, leave the bottle until completely saturated.

After you have ensured that there are no residues of dry lyophilisate, the contents of the bottle should be carefully mixed in a circular motion for 30-60 seconds until a homogeneous suspension is formed. Do not invert or shake the bottle, as 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 the bevel of the needle is lowered down and, tilting the bottle at an angle of 45 degrees, slowly draw the entire suspension into the syringe. Do not invert the bottle when drawing. 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 x 40 mm), carefully turn the syringe over and remove the air from the syringe.

Octreotide Depot suspension should be administered immediately after preparation. Octreotide Depot suspension 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 make sure 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, change the injection site and needle. If the needle becomes clogged, replace it with another needle of the same diameter.

For repeated injections, the left and right sides should be alternated.

Side effect

anorexia;
nausea, vomiting;
cramping abdominal pain;
severe pain in the epigastric region;
abdominal wall tension;
feeling of bloating;
excessive gas formation;
loose stools;
diarrhea;
steatorrhea;
in rare cases, phenomena resembling acute intestinal obstruction may occur;
hyperbilirubinemia in combination with increased activity of alkaline phosphatase, GGT and, to a lesser extent, other transaminases
formation of gallstones;
arrhythmia;
bradycardia;
tachycardia;
dyspnea;
possible impairment of glucose tolerance after meals (due to suppression of insulin secretion by the drug);
hypoglycemia;
in rare cases, with long-term treatment, persistent hyperglycemia may develop;
pain, itching or burning sensation, redness, swelling are possible at the injection site (usually disappear within 15 minutes);
allergic reactions;
skin rash;
alopecia.

Contraindications

children under 18 years of age;
hypersensitivity to octreotide or other components of the drug.

Use during pregnancy and breastfeeding

The use of Octreotide and Octreotide Depot and Long during pregnancy has not been studied. The drug should be used during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus.

It is not known whether the drug passes into breast milk, therefore, when using the drug during lactation, breastfeeding should be avoided.

Use in children

Contraindicated in children and adolescents under 18 years of age.

Use in elderly patients

In elderly patients there is no need to reduce the dose of Octreotide.

special instructions

In diabetic patients receiving insulin, Octreotide may reduce the need for insulin.

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

If gallstones are detected before starting treatment, the issue of using Octreotide is decided individually, depending on the ratio of the potential therapeutic effect of the drug and possible risk factors associated with the presence of gallstones.

Gastrointestinal side effects can be reduced if Octreotide injections are given between meals or before bedtime.

To reduce discomfort at the injection site, it is recommended to bring the drug solution to room temperature before administration and administer a smaller volume of the drug. Multiple injections into the same site at short intervals should be avoided.

Impact on the ability to drive vehicles and operate machinery

Some side effects of Octreotide may negatively affect the ability to drive vehicles and other mechanisms that require increased concentration and speed of psychomotor reactions.

Drug interactions

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

It is necessary to adjust the dosage regimen of simultaneously used diuretics, beta-blockers, blockers of “slow” calcium channels, insulin, and oral hypoglycemic drugs.

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

There is evidence that somatostatin analogs may reduce the metabolic clearance of substances metabolized by cytochrome P450 isoenzymes, which may be caused by GH suppression. Since it is impossible to exclude similar effects of Octreotide, drugs metabolized by isoenzymes of the cytochrome P450 system and having a narrow therapeutic range (quinidine and terfenadine) should be prescribed with caution.

Analogues of the drug Octreotide

Structural analogues of the active substance:

Genfastat;
Octreotide Kabi;
Octreotide Sun;
Octreotide Actavis;
Octreotide Depot;
Octreotide Long;
Octreotide Long FS;
Octreotide Fsynthesis;
Octreotide acetate;
Octretex;
Octride;
Seraxtal;
Sandostatin.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

Composition and release form

Solution - 1 ml:

Active substance: octreotide 100 mcg.
Excipients: sodium chloride - 9 mg, water for injection - up to 1 ml.

1 ml - ampoules (5) - contour packages (2) - cardboard packs.

Description of the dosage form

Solution for intravenous and subcutaneous administration, clear, colorless liquid, odorless.

pharmachologic effect

A synthetic analogue of somatostatin, which has similar pharmacological effects, but a significantly longer duration of action.

Pharmacokinetics

Suction

After subcutaneous administration, Octreotide is quickly and completely absorbed. Cmax of octreotide in blood plasma is achieved within 30 minutes.

Distribution

Plasma protein binding is 65%. The binding of Octreotide to blood cells is extremely insignificant. Vd is 0.27 l/kg.

Removal

After subcutaneous injection of the drug, T1/2 of octreotide is 100 minutes. After intravenous administration, octreotide is eliminated in 2 phases with T1/2 of 10 minutes 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.

Pharmacokinetics in special clinical situations

In elderly patients, clearance decreases and T1/2 increases.

In severe renal failure, clearance is reduced by 2 times.

Pharmacodynamics

Octreotide is a synthetic analogue of somatostatin, which has similar pharmacological effects, but a significantly longer duration of action. Octreotide suppresses growth hormone (GH) secretion, both pathologically elevated and induced 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.

In patients planning to undergo pancreatic surgery, the use of octreotide before, during and after surgery reduces the incidence of typical postoperative complications (for example, pancreatic fistulas, abscesses, sepsis, acute postoperative pancreatitis). When bleeding from varicose veins of the esophagus and stomach in patients with cirrhosis of the liver, the use of octreotide in combination with specific treatment (for example, sclerosing and hemostatic therapy) leads to more effective stoppage of bleeding and prevention of rebleeding.

Clinical pharmacology

Somatostatin analogue. A drug for intensive therapy in gastroenterology.

Indications for use

Treatment of acute pancreatitis;
stopping bleeding from gastric and duodenal ulcers;
stopping bleeding and preventing re-bleeding from esophageal varices in patients with cirrhosis of the liver;
prevention and treatment of complications after abdominal surgery.

Contraindications for use

Children under 18 years of age;
hypersensitivity to octreotide or other components of the drug.

With caution: cholelithiasis (cholelithiasis), diabetes mellitus, pregnancy, lactation.

Use during pregnancy and children

The use of octreotide during pregnancy has not been studied. Octreotide should be used during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus.

It is not known whether the drug passes into breast milk, therefore, when using the drug during lactation, breastfeeding should be avoided.

Use in children

Contraindicated in children under 18 years of age

Side effects

From the gastrointestinal tract and pancreas: possible - anorexia, nausea, vomiting, cramping abdominal pain, feeling of bloating, excessive gas formation, loose stools, diarrhea, steatorrhea. Although the excretion of fat in the feces may be increased, there is no indication that long-term treatment with octreotide may lead to the development of malabsorption problems (malabsorption). In rare cases, phenomena resembling acute intestinal obstruction may occur. There are isolated cases of acute hepatitis without cholestasis, hyperbilirubinemia in combination with an increase in the activity of alkaline phosphatase, GGT and, to a lesser extent, other transaminases.

Long-term use of Octreotide may lead to the formation of gallstones.

From the cardiovascular system: in some cases - arrhythmia, bradycardia.

From the side of carbohydrate metabolism: possible impairment of glucose tolerance after meals (due to suppression of insulin secretion by the drug), hypoglycemia; in rare cases, with long-term treatment, persistent hyperglycemia may develop.

Local reactions: pain, itching or burning sensation, redness, swelling are possible at the injection site (usually disappear within 15 minutes).

Other: allergic reactions, alopecia.

Drug interactions

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

It is necessary to adjust the dosage regimen of simultaneously used diuretics, beta-blockers, blockers of “slow” calcium channels, insulin, and oral hypoglycemic drugs.

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

Drugs that are metabolized by enzymes of the cytochrome P450 system and have a narrow therapeutic dose range should be prescribed with caution.

Dosage

For the treatment of acute pancreatitis, the drug is administered subcutaneously at a dose of 100 mcg 3 times a day for 5 days. It is possible to prescribe up to 1200 mcg/day using the intravenous route of administration.

To stop ulcer bleeding, it is administered intravenously at a dose of 25-50 mcg/hour as an intravenous infusion for 5 days.

To stop bleeding from varicose veins of the esophagus, it is administered intravenously at a dose of 25-50 mcg/hour in the form of continuous intravenous infusions for 5 days.

In elderly patients there is no need to reduce the dose of Octreotide.

Overdose

Symptoms: short-term decrease in heart rate, a feeling of a “rush” of blood to the face, cramping abdominal pain, diarrhea, nausea, a feeling of emptiness in the stomach.

Treatment: symptomatic.

Precautionary measures

In diabetic patients receiving insulin, octreotide may reduce insulin requirements.

If gallstones are identified before starting treatment, the use of octreotide is decided individually, depending on the relationship between the potential therapeutic effect of the drug and possible risk factors associated with the presence of gallstones.

Gastrointestinal side effects may be reduced if octreotide injections are given between meals or at bedtime.

Impact on the ability to drive vehicles and operate machinery

Some side effects of octreotide may negatively affect the ability to drive vehicles and other mechanisms that require increased concentration and speed of psychomotor reactions.

India Russia

Product group

Hormonal drugs

Somatostatin analogue. Drug for intensive therapy in gastroenterology

Release forms

1 ml - ampoules (5) - contour packages (1) - cardboard packs. 1 ml - ampoules (5) - contour packages (2) - cardboard packs. 1 ml - ampoules (5) - contour plastic packaging (1) - cardboard packs. 1 ml - ampoules (5) - contour plastic packaging (1) - cardboard packs. 1 ml - ampoules (5) - contour plastic packaging (2) - cardboard packs. 10 ampoules of 1 ml per pack 5 ampoules of 1 ml per pack ampoules of 1 ml - 10 pcs per pack. ampoules of 1 ml - 5 pcs per pack. solution for intravenous and subcutaneous administration 100 mcg/ml, 1 ml in an ampoule marked with a green ring Dark glass bottles (1) complete with solvent (amp.), disposable syringe and needles (2) - cardboard packs . Dark glass bottles (1) complete with solvent (amp), disposable syringe and needles (2) - cardboard packs. Dark glass bottles (1) complete with solvent (amp), disposable syringe and needles (2) - cardboard packs. Dark glass bottles (1) complete with solvent (amp), disposable syringe, d/i needles (2) and alcohol swabs (2) - cardboard packs.

Description of the dosage form

Lyophilisate for the preparation of a suspension for intramuscular administration of prolonged action, white or white with a slight yellowish tint, in the form of a powder or a porous mass compacted into a tablet; the attached solvent is a colorless transparent liquid; prepared suspension - white or white Lyophilisate for preparing a suspension for intramuscular administration of prolonged action, white or white with a slight yellowish tint, in the form of a powder or a mass compacted into a tablet; the attached solvent is a colorless transparent liquid; prepared suspension - white, transparent, colorless, odorless liquid. Transparent, colorless solution. Solution for intravenous and subcutaneous administration 0.005% transparent, colorless, odorless. Solution for injection 0.005% transparent, colorless, odorless. Solution for injection 0.01% transparent, colorless, odorless. Solution for injection 0.01% transparent, colorless, odorless. Solution for injection 0.01%, transparent

pharmachologic effect

Octreotide depot is a long-acting dosage form of octreotide for intramuscular administration, ensuring the maintenance of stable therapeutic concentrations of octreotide in the blood for 4 weeks. Octreotide is a synthetic octapeptide that is an analogue of the natural hormone somatostatin and has pharmacological effects similar to it, but a much longer duration of action. The drug suppresses the pathologically increased secretion of growth hormone, as well as peptides and serotonin produced in the gastroenteropancreatic endocrine system. In healthy individuals, octreotide, like somatostatin, suppresses growth hormone secretion induced by arginine, exercise, and insulin hypoglycemia; secretion of insulin, glucagon, gastrin and other peptides of the gastroenteropancreatic endocrine system caused by food intake, as well as secretion of insulin and glucagon stimulated by arginine; secretion of thyrotropin caused by thyrotropin-releasing hormone. The suppressive effect on growth hormone secretion in octreotide, in contrast to somatostatin, is much more pronounced than on insulin secretion. Administration of octreotide is not accompanied by the phenomenon of hormone hypersecretion via a negative feedback mechanism. In patients with acromegaly, the administration of Octreotide Depot provides, in the vast majority of cases, a persistent decrease in the level of growth hormone and normalization of the concentration of insulin-like growth factor 1/somatomedin C (IGF-1). In most patients with acromegaly, Octreotide Depot significantly reduces the severity of symptoms such as headache, increased sweating, paresthesia, fatigue, pain in bones and joints, and peripheral neuropathy. Treatment with octreotide in selected patients with growth hormone-secreting pituitary adenomas has been reported to result in tumor shrinkage. For carcinoid tumors, the use of octreotide may lead to a decrease in the severity of symptoms of the disease, primarily such as hot flashes and diarrhea. In many cases, clinical improvement is accompanied by a decrease in plasma serotonin concentrations and urinary 5-hydroxyindoleacetic acid excretion. For tumors characterized by overproduction of vasoactive intestinal peptide (VIP), the use of octreotide in most patients leads to a decrease in the severe secretory diarrhea that is characteristic of this condition, 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. According to computed tomography data, in some patients the progression of the tumor slows down or stops, and even reduces its size, especially metastases to the liver. Clinical improvement is usually accompanied by a decrease (down to normal values) in the plasma concentration of vasoactive intestinal peptide (VIP). In glucagonomas, the use of octreotide in most cases leads to a noticeable reduction in the necrotizing migratory rash that is characteristic of this condition. Octreotide does not have any significant effect on the severity of diabetes mellitus, which is often observed in glucagonomas, and usually does not lead to a decrease in the need for insulin or oral hypoglycemic drugs. In patients suffering from diarrhea, octreotide causes a decrease in diarrhea, which is accompanied by an increase in body weight. With the use of octreotide, a rapid decrease in plasma glucagon concentrations is often observed, but this effect does not persist with long-term treatment. At the same time, symptomatic improvement remains stable for a long time. In gastrinomas/Zollinger-Ellison syndrome, octreotide, used as monotherapy or in combination with histamine H2 receptor blockers and proton pump inhibitors, can reduce the formation of hydrochloric acid in the stomach and lead to clinical improvement, incl. and regarding diarrhea. It is also possible to reduce the severity of other symptoms, probably associated with the synthesis of peptides by the tumor, incl. tides In some cases, there is a decrease in plasma gastrin concentration. In patients with insulinomas, octreotide reduces the level of immunoreactive insulin in the blood. 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 appears to be due to suppression of the secretion of growth hormone releasing factor and growth hormone itself. In the future, it is possible to reduce the size of the pituitary gland, which was enlarged before treatment. In patients with hormone-resistant prostate cancer, the pool of neuroendocrine cells expressing somatostatin receptors affinity for octreotide (SS2 and SS5 types) increases, which determines the sensitivity of the tumor to octreotide. The use of octreotide depot in combination with dexamethasone against the background of androgen blockade (medical or surgical castration) in patients with hormone-resistant prostate cancer restores sensitivity to hormonal therapy and leads to a decrease in prostate specific antigen (PSA) in more than 50% of patients. In patients with hormone-resistant prostate cancer with bone metastases, this therapy is accompanied by a pronounced and long-lasting analgesic effect. Moreover, in all patients who responded to combination therapy with octreotide depot, the quality of life and median relapse-free survival significantly improved.

Pharmacokinetics

Absorption After subcutaneous administration, Octreotide is rapidly and completely absorbed. Cmax of octreotide in blood plasma is achieved within 30 minutes. Distribution Plasma protein binding is 65%. The binding of Octreotide to blood cells is extremely insignificant. Vd is 0.27 l/kg. Excretion Total clearance is 160 ml/min. About 32% is excreted unchanged by the kidneys. After subcutaneous injection of the drug, T1/2 of octreotide is 100 minutes. After intravenous administration, octreotide is eliminated in 2 phases with T1/2 of 10 minutes and 90 minutes, respectively. Pharmacokinetics in special clinical situations In elderly patients, clearance decreases and T1/2 increases. In severe renal failure, clearance is reduced by 2 times.

Special conditions

In case of pituitary tumors that secrete GH, careful monitoring of patients is necessary, since it is possible that the size of the tumors may increase with the development of such serious complications as narrowing of visual fields. In these cases, the need for other treatment methods should be considered. In 15-30% of patients receiving octreotide subcutaneously for a long time, gallstones may appear. Prevalence in the general population (ages 40-60 years) is 5-20%. The experience of long-term treatment with extended-acting octreotide in patients with acromegaly and tumors of the gastrointestinal tract and pancreas indicates that extended-acting octreotide, in comparison with short-acting octreotide, does not lead to an increase in the incidence of gallstones. However, an ultrasound scan of the gallbladder is recommended before starting treatment with octreotide 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 may affect glucose metabolism and, therefore, reduce the need for injected 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 glycemic levels 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 GH 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, repeated ultrasounds of the gallbladder should be performed, preferably at intervals of 6-12 months. If gallstones are detected before treatment begins, the potential benefits of octreotide therapy must be assessed against the possible risks associated with the presence of gallstones. There is currently no evidence that octreotide adversely affects the course or prognosis of existing gallstone disease. Management of patients in whom gallstones form during treatment with octreotide. a) Asymptomatic gallstones. The use of octreotide 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. b) Gallstones with clinical symptoms. The use of octreotide 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/kg/day in combination with ursodeoxycholic acid at the same dose) under ultrasound control until the stones completely disappear. Effect on the ability to drive vehicles and operate machinery There is no data on the effect of octreotide on the ability to drive a car and operate machinery.

Compound

1 ml octreotide (in the form of a free peptide) 50 mcg Excipients: sodium chloride - 9 mg, water for injection - up to 1 ml. 1 ml octreotide (in the form of a free peptide) 50 mcg Excipients: sodium chloride - 9 mg, water for injection - up to 1 ml. 1 ml octreotide (in the form of free peptide) 100 mcg Excipients: sodium chloride, water for injection. 1 ml octreotide (in the form of free peptide) 100 mcg Excipients: sodium chloride, water for injection. 1 ml octreotide (in the form of free peptide) 50 mcg Excipients: sodium chloride, water for injection. 1 ml octreotide 100 mcg 1 vial. octreotide 10 mg -"- 20 mg -"- 30 mg Excipients: copolymer of DL-lactic and glycolic acids, D-mannitol, carboxymethylcellulose sodium salt, polysorbate-80. Solvent: mannitol solution 0.8% - 2 ml. 1 fl. octreotide 10 mg -"- 20 mg -"- 30 mg Excipients: copolymer of DL-lactic and glycolic acids, D-mannitol, carboxymethylcellulose sodium salt, polysorbate-80. Solvent: mannitol solution 0.8% - 2 ml. 1 ml of solution contains: Active substance: Octreotide acetate (equivalent to the content of octreotide) -0.064 (0.050 mg) mcg and 0.128 mg (0.100 mg); Excipients: glacial acetic acid, sodium acetate (trihydrate), sodium chloride, water for injection octreotide 10 mg Excipients: copolymer of DL-lactic and glycolic acids - 270 mg, D-mannitol - 85 mg, carboxymethylcellulose sodium salt - 30 mg, polysorbate-80 - 2 mg. Solvent: mannitol solution 0.8% - 2 ml.

Octreotide indications for use

Acromegaly (when adequate control of the manifestations of the disease is carried out 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). In the treatment of endocrine tumors of the gastrointestinal tract (GIT) and pancreas: carcinoid tumors with symptoms of carcinoid syndrome; insulinomas; VIPs; gastrinomas (Zollinger-Ellison syndrome); glucagonoma (to control hypoglycemia in the preoperative period, as well as for maintenance therapy). In the treatment of endocrine tumors of the gastrointestinal tract (GIT) and pancreas: carcinoid tumors with symptoms of carcinoid syndrome; insulinomas; VIPs; gastrinomas (Zollinger-Ellison syndrome); glucagonoma (to control hypoglycemia in the preoperative period, as well as for maintenance therapy). Somatoliberinomas (tumors characterized by hyperplasmic

Octreotide contraindications

- children under 18 years of age; - hypersensitivity to octreotide or other components of the drug. With caution: cholelithiasis (cholelithiasis), diabetes mellitus, pregnancy, lactation.

Octreotide dosage

10 mg 100 µg/ml 100 µg/ml 20 mg 30 mg 300 µg/ml 50 µg/ml

Octreotide side effects

Local reactions: possible pain, itching, or burning sensation, redness or swelling at the site of subcutaneous injection (usually disappears within 15 minutes). The severity of local reactions can be reduced if you use a solution at room temperature, or administer a smaller volume of a more concentrated solution. 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 can lead to the development of nutritional deficiencies due to malabsorption (mapabsorption). In rare cases, phenomena resembling acute intestinal symptoms may occur. obstruction: progressive abdominal bloating, severe pain in the epigastric region, tension in the abdominal wall. Long-term use of octreotide may lead to the formation of gallstones. The incidence of gastrointestinal side effects can be reduced by increasing the time interval between meals and octreotide administration. 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, gamma-glutamyl transferase and, to a lesser extent, other transaminases. From the cardiovascular system: in some cases - bradycardia. From the metabolic side: since octreotide has an inhibitory effect on the formation of GH, glucagon and insulin, it can affect glucose metabolism. Possibly decreased 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 following administration of octreotide. There are isolated reports of the development of hypersensitivity reactions: rarely, allergic skin reactions; in some cases - anaphylactic reactions.

Drug interactions

Octreotide reduces the absorption of cyclosporine and slows down the absorption of cimetidine. With simultaneous use of octreotide and bromocriptine, the bioavailability of the latter increases. It is necessary to adjust the dosage regimen of simultaneously used diuretics, beta-blockers, blockers of “slow” calcium channels, insulin, oral hypoglycemic drugs, glucagon. There is evidence that somatostatin analogues may reduce the metabolism of drugs metabolized by cytochrome P450 enzymes (may be due to growth hormone suppression). Since it is impossible to exclude similar effects of ocreotide, drugs that are metabolized by enzymes of the cytochrome P450 system and have a narrow therapeutic dose range should be prescribed with caution.

Overdose

It is known that administration of octreotide in a dose of up to 2000 mcg as a subcutaneous injection 3 times over several months was well tolerated. The maximum single dose for intravenous bolus administration to an adult patient was 1000 mcg. In this case, symptoms such as a decrease in heart rate, “flushes” of blood to the face, abdominal pain of a spastic nature, diarrhea, nausea, and a feeling of emptiness in the stomach were noted. All these symptoms resolved within 24 hours of drug administration. One patient was mistakenly given an excessive dose of octreotide 250 mcg/h (instead of 25 mcg/h) by continuous infusion, which was not accompanied by side effects. No life-threatening reactions were observed in acute overdose. Treatment: symptomatic therapy.

Storage conditions

store in a dry place
keep away from children
store in a place protected from light

Information provided