Instructions for the drug Octreotide: why lower the secretion of glands and how to do it correctly. Octreotide: instructions for use of the injection solution The drug octreotide

Composition and form of release

Solution - 1 ml:

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

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

Description of the dosage form

Solution for intravenous and s / c administration, clear, colorless liquid, odorless.

pharmachologic effect

Synthetic analogue of somatostatin, which has similar pharmacological effects, but with a much longer duration of action.

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

In patients scheduled for 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 cirrhosis of the liver, the use of octreotide in combination with specific treatment (for example, sclerosing and hemostatic therapy) leads to more effective control of bleeding and prevention of rebleeding.

Pharmacokinetics

Suction

After subcutaneous administration, Octreotide is rapidly and completely absorbed. C max octreotide in plasma is achieved within 30 minutes.

Distribution

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

breeding

After s / c injection of the drug T1 / 2 octreotide is 100 minutes. After intravenous administration, the excretion of octreotide is carried out in 2 phases with a 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.

With severe kidney failure clearance is reduced by 2 times.

Pharmacodynamics

Octreotide is a synthetic analog of somatostatin with similar pharmacological effects, but a much longer duration of action. Octreotide suppresses the secretion of growth hormone (GH), 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 inhibits thyrotropin secretion caused by thyreoliberin.

In patients scheduled for 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 control of bleeding and prevention of rebleeding.

Clinical pharmacology

analogue of somatostatin. The drug for intensive care in gastroenterology.

Indications for use

• Treatment of acute pancreatitis;
• stop bleeding at peptic ulcer stomach and duodenum;
• stop bleeding and prevention of rebleeding from esophageal varices in patients with cirrhosis of the liver;
• prevention and treatment of complications after organ operations abdominal cavity.

Contraindications for use

• Children's age up to 18 years;
• hypersensitivity to octreotide or other components of the drug.

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

Use in pregnancy and children

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

It is not known if the drug enters breast milk therefore, when using the drug during lactation, breastfeeding should be abandoned.

Use in children

Contraindicated in children under the age of 18

Side effects

From the gastrointestinal tract and pancreas: possible - anorexia, nausea, vomiting, abdominal cramps, a feeling of bloating, excessive gas formation, liquid stool, diarrhea, steatorrhea. Although fecal fat excretion may increase, there is no indication that long-term treatment octreotide can lead to the development of malabsorption. In rare cases, there may be phenomena resembling acute intestinal obstruction. 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.

Prolonged use of octreotide can lead to the formation of stones in gallbladder.

From the side cordially- vascular system: in some cases - arrhythmia, bradycardia.

On the part of carbohydrate metabolism: a violation of glucose tolerance after a meal is possible (due to the suppression of insulin secretion by the drug), hypoglycemia; in rare cases, with prolonged treatment, persistent hyperglycemia may develop.

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

Others: allergic reactions, alopecia.

drug interaction

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

It is necessary to correct the dosing regimen of simultaneously used diuretics, beta-blockers, blockers of "slow" calcium channels, insulin, oral hypoglycemic drugs.

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

Drugs metabolized by enzymes of the cytochrome P450 system and having a narrow therapeutic dose range should be administered with caution.

Dosage

For the treatment of acute pancreatitis, the drug is administered s / c at a dose of 100 mcg 3 times / day for 5 days. Perhaps the appointment of up to 1200 mcg / day using the / in the route of administration.

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

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

To prevent complications after operations on the pancreas, the first dose of 100-200 mcg is administered s / c 1-2 hours before laparotomy; then after the operation, s / c is injected at 100-200 mcg 3 times / day for 5-7 consecutive days.

Overdose

Symptoms: a short-term decrease in heart rate, a feeling of "rush" of blood to the face, spastic pain in the abdomen, diarrhea, nausea, a feeling of emptiness in the stomach.

Treatment: symptomatic.

Precautionary measures

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

If gallstones are identified prior to treatment, the use of octreotide is decided on an individual basis, 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.

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

Influence on the ability to drive vehicles and control mechanisms

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

Octreotide is a synthetic derivative of the natural hormone somatostatin, characterized by similar pharmacological effects, but a much longer duration of action; inhibits the secretion of thyrotropin, serotonin, gastrin, insulin, glucagon, growth hormone, both pathologically elevated and conditioned external factors(arginine, food intake, insulin hypoglycemia, etc.).

Release form and composition

Dosage forms of Octreotide:

• Solution for intravenous and subcutaneous injection at a dose of 50 and 100 mcg: colorless, transparent liquid, odorless (1 ml per ampoule, 5 ampoules (50 mcg) in a blister pack; 5 ampoules (100 mcg) in a contour pack, 1 or 2 packs in a carton box) ;
• Solution for intravenous and subcutaneous administration at a dose of 300 and 600 mcg: colorless, transparent liquid, odorless (1 ml in a dark glass ampoule with a tension ring for opening or with a break point, or in a colorless glass ampoule marked as two green strips; in a blister pack 1 or 2 ampoules, in a carton pack 1 pack; in a blister pack 5 ampoules, in a carton pack 1 or 2 packs).

Composition of 1 ml solution for intravenous and subcutaneous administration at a dose of 50 and 100 mcg:

• Active substance: octreotide - 50 and 100 mcg;

Composition of 1 ml solution for intravenous and subcutaneous administration at a dose of 300 and 600 mcg:

• Active substance: octreotide acetate, in terms of octreotide - 300 and 600 mcg;
• Additional components: water for injections, sodium chloride.

Indications for use

• Acute pancreatitis (at a dose of 50 and 100 mcg);
• Peptic ulcer of the stomach and duodenum, in order to stop bleeding (at a dose of 50 and 100 mcg);
• Acromegaly (to control the main manifestations of the lesion and a decrease in the level of growth hormone and insulin-like growth factor-1 (IGF-1); with insufficient effectiveness or impossibility of surgical treatment or radiotherapy; when the patient refuses surgery or during short-term treatment between courses of radiation therapy, until the full development of its effect);
• Secreting endocrine tumors of the pancreas and gastrointestinal tract, in order to control symptoms (carcinoid tumors (with the presence of carcinoid syndrome), glucagonomas, VIPomas, gastrinomas / Zollinger-Ellison syndrome (in combination with histamine H2 receptor blockers and inhibitors proton pump), insulinomas (including for maintenance therapy and control of hypoglycemia before surgery), somatoliberinoma).

The solution is used for the treatment and prevention of complications in the period after surgery on the abdominal cavity, as well as in patients with cirrhosis of the liver to stop bleeding and prevent re-bleeding from varicose veins of the stomach and esophagus. The use of the agent is possible in combination with specific therapeutic measures (for example, with endoscopic sclerotherapy).

Contraindications

• Children's and adolescence up to 18 years;
• Hypersensitivity to the components of the drug.

With extreme caution, the drug should be used for cholelithiasis (cholelithiasis) and diabetes mellitus. Experience with the use of the drug during pregnancy is not available. As a result, Octreotide is recommended for pregnant women only when the expected benefit of therapy outweighs the potential risk of adverse reactions.

If it is necessary to administer the drug during lactation, it is required to refuse breastfeeding (because it is not known whether the drug passes into breast milk).

Method of application and dosage

Octreotide is used subcutaneously and intravenously.

In the treatment of acute pancreatitis, 100 mcg of the solution is administered subcutaneously 3 times a day for 5 days; intravenous infusion at a dose not exceeding 1200 mcg per day is also acceptable.

To stop bleeding from varicose veins of the esophagus or peptic ulcer, long-term intravenous infusions are prescribed at a dose of 25-50 mcg / hour for 5 days.

In order to prevent complications after undergoing surgical interventions on the pancreas, the agent is administered subcutaneously. The first injection at a dose of 100-200 mcg is carried out 1-2 hours before laparotomy, and the next - at a dose of 100-200 mcg after surgery, 3 times a day, daily for 5-7 days.

In acromegaly, it is recommended to administer 300 micrograms of Octreotide subcutaneously at intervals of 8 or 12 hours, this dose is prescribed if there is no effect during initial therapy (50-100 micrograms of solution at intervals of 8 or 12 hours). The effectiveness of treatment is determined by taking into account monthly concentrations growth hormone in the blood, drug tolerance and clinical symptoms. To achieve the desired effect, if necessary, it is possible to use the drug in a dose exceeding 300 mcg, but not more than 1500 mcg per day.

If there is no improvement within 3 months of therapy clinical picture and a sufficient decrease in the level of growth hormone, the use of the drug is impractical.

For tumors of the gastroenteropancreatic endocrine system the drug is administered subcutaneously. The initial dose of Octreotide is 50 mcg, applied 1-2 times a day, in the future it is possible to increase the dose to 100-200 mcg with a frequency of administration 3 times a day. With the ineffectiveness of initial therapy, assessed by the concentration of hormones produced by the tumor, the tolerability of the drug and the achieved clinical effect, appoint 1-2 times a day subcutaneous injections at a dose of 300 mcg. In exceptional cases, a gradual increase in dose to 300-600 mcg, administered 3 times a day, is acceptable. If during the treatment of carcinoid tumors with Octreotide at the maximum tolerated dose, there is no therapeutic effect within 7 days, treatment should be discontinued.

Elderly people and patients with functional disorders kidney does not require correction of the dosing regimen.

When prescribing an intravenous drip infusion of the drug, the contents of the ampoule at a dose of 600 μg must be dissolved in 60 ml of physiological sodium chloride solution (0.9%). Diluted solutions must be administered immediately after preparation (to avoid microbial contamination). If it is impossible to use the drug immediately after dilution, it can be stored at a temperature of 2-8 ° C for no longer than 24 hours ( total time from the moment of dilution until the end of its introduction).

Side effects

• Digestive system: very often - bloating, constipation, nausea, abdominal pain, diarrhea; often - anorexia, discoloration / soft stool consistency, steatorrhea, feeling of heaviness / fullness of the abdomen, vomiting, dyspeptic disorders;
• Endocrine system: very often - hyperglycemia; often - hypothyroidism, impaired activity thyroid gland(decrease in the levels of free and total thyroxine, and thyroid-stimulating hormone); impaired glucose tolerance, hypoglycemia;
• Hepatobiliary system: very often - the formation of stones in the gallbladder (cholelithiasis); often - increased activity of hepatic transaminases, hyperbilirubinemia, impaired colloidal stability of bile, cholecystitis;
• Nervous system: very often - headache; often - dizziness;
• Cardiovascular system: often - bradycardia; sometimes - tachycardia;
• Respiratory system: often - shortness of breath;
• Skin: often - itching, rash, hair loss;
• General disorders and local reactions: very often - pain at the injection site; sometimes dehydration.

Also, when using the drug in clinical practice the following undesirable effects were observed (regardless of the presence of a causal relationship with the use of the agent): cholestatic jaundice, cholestasis, jaundice, cholestatic hepatitis, acute hepatitis without the phenomena of cholestasis, acute pancreatitis, increased levels of gamma-glutamyl transferase (GGT) and alkaline phosphatase (AP), arrhythmia, allergic reactions, urticaria, anaphylactic reactions.

With subcutaneous injections of octreotide at a daily dose of 3000-30000 mcg, divided into several injections, no new side effects were detected in patients with tumors (other than those indicated above).

With accidental intravenous administration of the drug at a dose of 2400-6000 mcg per day (at a rate of 100-250 mcg / h) or subcutaneous administration of 1500 mcg 3 times a day, the following reactions were observed: weight loss, lactic acidosis, hepatomegaly, lethargy, weakness, diarrhea, fatty degeneration of the liver, pancreatitis, cerebral hypoxia, sudden cardiac arrest, decreased blood pressure development of arrhythmias. Treatment is symptomatic.

special instructions

Patients with diabetes who take insulin may experience a decrease in insulin requirements during therapy.

Before starting treatment, as well as during a long course, it is recommended to conduct an ultrasound examination of the gallbladder at intervals of 6-12 months.

In the case of detection of stones in the gallbladder before the start of therapy, the issue of using the drug is decided individually, after the ratio of the potential benefits of therapy and the risk of developing possible complications associated with the presence of stones.

Manifestations of adverse reactions from digestive system may be reduced by administering octreotide at bedtime or between meals.

With a long course, thyroid function should be monitored.

In rare cases, during the treatment of endocrine tumors of the gastrointestinal tract and pancreas, there may be a sudden relapse of the symptoms of the disease.

When using octreotide in patients with a history of vitamin B12 (cobalamin) deficiency, it is recommended to control its content in the body (the absorption of cobalamin worsens).

To reduce discomfort and pain at the injection site, it is recommended to warm the solution to room temperature before use and inject it in a smaller volume. Injections of the drug at short intervals at the same injection site should be avoided.

drug interaction

The effect of octreotide on concomitantly taken substances / drugs:

• Cyclosporine - reduces its absorption;
• Bromocriptine - increases its bioavailability;
• Cimetidine - slows down its absorption;
• Drugs metabolized by the cytochrome P450 system (terfenadine, quinidine) - reduces their metabolism.

When octreotide is combined with diuretics, oral hypoglycemic drugs, insulin, slow calcium channel blockers, beta-blockers, a correction of the dosing regimen is required.

Terms and conditions of storage

Store in a place protected from moisture and light, out of the reach of children, at a temperature of 8 to 25 °C.

Shelf life - 5 years.

Synthetic derivative of the hormone somatostatin, which has similar pharmacological effects and a much longer duration of action. Reduces the secretion of growth hormone, TSH, has an antithyroid, antispasmodic effect. Reduces acid production, gastrointestinal motility. Suppresses pathologically increased secretion of growth hormone, peptides and serotonin produced in the gastroentero-pancreatic endocrine system.

Normally, it reduces the secretion of growth hormone caused by arginine, stress and insulin hypoglycemia; secretion of insulin, glucagon, gastrin, and other peptides of the gastroentero-pancreatic endocrine system, caused by food intake, as well as the secretion of insulin and glucagon, stimulated by arginine; thyrotropin secretion caused by thyroliberin.

Suppression of growth hormone secretion by octreotide (unlike somatostatin) occurs to a much greater extent than by insulin. The introduction of octreotide is not accompanied by the phenomenon of hormone hypersecretion by the "negative feedback" mechanism. In patients with acromegaly, it reduces the concentration of growth hormone and / or somatomedin A in plasma. A clinically significant decrease in the concentration of growth hormone (by 50% or more) is observed in almost all patients, while the normalization of the content of growth hormone in plasma (less than 5 ng / ml) is achieved in about half of the patients.

In carcinoid tumors, the administration of octreotide can lead to a decrease in the severity of the symptoms of the disease, primarily such as "flushing" of blood to the skin of the face and diarrhea, clinical improvement is accompanied by a decrease in plasma serotonin concentration and excretion of 5-hydroxyindoleacetic acid in the urine.

In tumors characterized by hyperproduction of vasoactive intestinal peptide (VIP), a decrease in severe secretory diarrhea, which is characteristic of given state which in turn improves the quality of life of the patient. 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. It is possible to slow down or stop the progression of the tumor and even reduce its size and especially liver metastases. Clinical improvement is usually accompanied by a decrease (up to normal values) plasma VIP concentrations.

In glucagonomas, despite a marked reduction in necrotizing migratory rash, it does not have any significant effect on the severity of diabetes mellitus (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, causes its decrease, which is accompanied by an increase in body weight, often noted rapid decline plasma glucagon concentrations, however, this effect does not persist with long-term treatment. At the same time, symptomatic improvement remains stable long time.

In gastrinomas (Zollinger-Ellison syndrome), octreotide, used as monotherapy or in combination with H2 receptor blockers and proton pump inhibitors, can reduce the formation of HCl in the stomach, it is possible to reduce the severity and other symptoms, probably associated with the synthesis of peptides by the tumor, including "tides". In some cases, there is a decrease in the concentration of gastrin in plasma.

In patients with insulinomas, it reduces the concentration of immunoreactive insulin in the blood (this effect, however, can be short-lived - about 2 hours).

In patients with resectable tumors, it can ensure the restoration and maintenance of normoglycemia in the preoperative period. In patients with inoperable benign and malignant tumors normoglycemia can be achieved without a simultaneous prolonged decrease in blood insulin.

In patients with rare tumors that hyperproduce growth hormone releasing factor (somatoliberinoma), it 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 were increased before the start of treatment.

In patients with acromegaly, the administration of octreotide provides, in the vast majority of cases, a persistent decrease in growth hormone and normalization of the concentration of insulin-like growth factor 1 / somatomedin C (IGF1). Significantly reduces the severity of symptoms such as headache, increased sweating, paresthesia, fatigue, bone and joint pain, peripheral neuropathy. In patients with pituitary adenomas that secrete growth hormone, it is possible to reduce the size of the tumor.

Sandostatin LAR is dosage form long-acting octreotide, designed to be administered at intervals of 4 weeks, which ensures the maintenance of stable therapeutic serum concentrations of octreotide. The composition of the microspheres includes a polymer matrix that serves as a carrier active substance. After i / m administration, as a result of the destruction of microspheres in muscle tissue, a prolonged and gradual release of the active substance occurs.

Product group

analogue of somatostatin. The preparation for intensive care in gastroenterology

Release form

• 1 ml - ampoules (5) - contour packaging (1) - cardboard packs. 1 ml - ampoules (5) - contour packaging (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. 1 ml ampoules - 5 pcs. 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 a solvent (amp.), a disposable syringe and needles for and (2) - packs of cardboard . Dark glass bottles (1) complete with a solvent (amp.), a disposable syringe and needles for injection (2) - packs of cardboard. Dark glass bottles (1) complete with a solvent (amp.), a disposable syringe and needles for injection (2) - packs of cardboard. Dark glass bottles (1) complete with a solvent (amp.), a disposable syringe, needles for injections (2) and alcohol swabs (2) - cardboard packs.

Description of the dosage form

• Lyophilisate for the preparation of a suspension for intramuscular administration of a prolonged action of white or white with a slight yellowish tint, in the form of a powder or a porous mass compacted into a tablet; the applied solvent is a colorless transparent liquid; prepared suspension - white or white Lyophilizate for the preparation of a suspension for intramuscular administration of a prolonged action of white or white with a slight yellowish tint, in the form of a powder or a mass compacted into a tablet; the applied solvent is a colorless transparent liquid; prepared suspension - white, transparent, colorless liquid, odorless Clear, colorless solution Solution for intravenous and s / c administration 0.005% transparent, colorless, odorless Injection solution 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

Pharmacokinetics

Special conditions

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 injections. 1 ml octreotide (in the form of free peptide) 100 mcg Excipients: sodium chloride, water for injections. 1 ml octreotide (in the form of free peptide) 50 mcg Excipients: sodium chloride, water for injections. 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: solution of mannitol 0.8% - 2 ml. 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: solution of mannitol 0.8% - 2 ml. 1 ml of solution contains: Active substance: Octreotide acetate (which is equivalent to the content of octreotide) -0.064 (0.050 mg) mcg and 0.128 mg (0.100 mg); Excipients: acetic acid glacial, sodium acetate (trihydrate), sodium chloride, water for injection octreotide 10 mg mg. Solvent: solution of mannitol 0.8% - 2 ml.

Octreotide indications for use

• Acromegaly (when adequate control of the manifestations of the disease is carried out due to the subcutaneous administration of octreotide, in the absence of a sufficient effect of surgical treatment and radiation therapy; to prepare for surgical treatment, for treatment between courses of radiotherapy until the development of a persistent effect, in inoperable patients). In the treatment of endocrine tumors of the gastrointestinal tract (GIT) and pancreas: carcinoid tumors with symptoms of carcinoid syndrome; insulinomas; VIPomas; gastrinomas (Zollinger-Ellison syndrome); glucagonomas (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; VIPomas; gastrinomas (Zollinger-Ellison syndrome); glucagonomas (to control hypoglycemia in the preoperative period, as well as for maintenance therapy). Somatoliberinomas (tumors characterized by hyperpigmentation)

Octreotide contraindications

• - childhood up to 18 years; - 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, redness or swelling at the injection site (usually disappear within 15 minutes). The severity of local reactions can be reduced if a room temperature solution is used, or a smaller volume of a more concentrated solution is administered. From the gastrointestinal tract: anorexia, nausea, vomiting, abdominal cramps, bloating, excessive gas formation, loose stools, diarrhea, steatorrhea. Although fecal fat excretion may increase, there is no evidence to date that long-term treatment with octreotide can lead to malnutrition due to malabsorption. In rare cases, there may be phenomena resembling acute intestinal. obstruction: progressive bloating, severe pain in the epigastric region, tension abdominal wall. Prolonged use of octreotide can lead to the formation of gallstones. The frequency of side effects from the gastrointestinal tract can be reduced by increasing the time intervals between meals and the introduction of octreotide. From the side of the pancreas: rare cases of acute pancreatitis have been reported that developed in the first hours or days of octreotide use. With prolonged use, there have been cases of pancreatitis associated with cholelithiasis. From the side of the liver: there are separate reports of the development of liver dysfunction (acute hepatitis without cholestasis with normalization of transaminase levels after the abolition of octreotide); slow development of hyperbilirubinemia, accompanied by an increase in alkaline phosphatase, gamma-glutamyl transferase and, to a lesser extent, other transaminases. Since the cardiovascular system: in some cases - bradycardia. From the side of metabolism: since octreotide has a suppressive effect on the formation of GH, glucagon and insulin, it can affect glucose metabolism. Perhaps a decrease in glucose tolerance after a meal. With prolonged use of octreotide s / c, in some cases, persistent hyperglycemia may develop. Hypoglycemia has also been observed. Other: In rare cases, temporary hair loss has been reported following the administration of octreotide. There are separate reports on the development of reactions hypersensitivity: rarely - skin allergic reactions; in some cases - anaphylactic reactions.

drug interaction

Overdose

Storage conditions

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

For the treatment of pancreatitis in acute and chronic form Octreotide, which is a synthetic analogue of growth hormone, can be used. This medicine effectively suppresses signs of inflammation of the pancreas.

Release form and composition

Octreotide is a synthetic analogue of the somatostatin hormone produced in the hypothalamus and pancreas. This drug is a short time inhibits the production of enzymes, which allows the treatment of patients with chronic and acute forms of pancreatitis.

The hormone has a pronounced analgesic property, eliminates seizures with sluggish and necrotic exacerbation, removes the symptoms of liver cirrhosis.

Octreotide is produced in the form of a solution for intravenous and subcutaneous injections, which contain 0.005 and 0.01% active substance. The drug is odorless and colorless, and its use is permissible only under medical supervision.

On sale you can find Octreotide from domestic and foreign manufacturers. The latter differ in workmanship and are recommended by most experts. The cost of imported drugs can be 20-30% higher than domestic ones.

Octreotide can be used as follows:

• Intravenously using a dropper, when up to 1200 micrograms of the drug is administered to the patient daily for 15 days.
• Subcutaneous injections are performed three times a day. Depending on the stage of the disease and the location of the pancreatic lesion, the daily dose for the first 5 days can be 50-300 micrograms of the drug, and subsequently the dosage is reduced, based on the existing symptoms.
• For intramuscular injection a suspension lyophilisate is used, which is injected to the patient once a month.

Regardless of the method of using this drug, it is prohibited to prescribe Octreotide on your own. The medicine is dispensed in pharmacies exclusively by prescription, and a specialist can write it out only after complete examination sick.

With the wrong dosage and self-administration of the drug, serious damage to the pancreas is possible, up to the patient's disability.

Side effects and contraindications

Misuse of the drug and an overdose of Octreotide can lead to various side effects. Contraindications include:

• individual intolerance;
• breastfeeding and pregnancy;
• age up to 18 years.

When prescribing the drug, the doctor should take into account possible complications pancreatitis, and the patient himself is obliged to follow the doctor's recommendations exactly, without increasing the dosage of the medicine on his own. More details on contraindications can be found in the instructions for use of Octreotide in pancreatitis.

In case of overdose, various side effects may occur. When they appear, the patient should stop taking the drug and consult a doctor for advice. To side effects when treated with octreotide include:

• Various allergic reactions, including difficulty breathing, itching, peeling skin and hives.
• Local reactions, including pain, redness at the injection site.
• crash heart rate and bradycardia.
• Metabolic disorders and problems with the absorption of carbohydrates.
• Dyspeptic phenomena: loose stools, bloating, cramps, vomiting and nausea.
• In rare cases, a side effect of taking hormones is the formation of stones in the gallbladder and ureters, which will require crushing or surgical removal. With short-term courses of treatment, such serious consequences should not be feared.

Pharmacological properties

When taking Octreotide in the body, the secretion of growth hormone is suppressed, which allows you to restore the functionality of the pancreas, removing acute and chronic inflammatory processes.

The use of this tool allows you to eliminate possible postoperative complications, including acute abscess, sepsis and pancreatic fistulas.

The active substance in the body is rapidly absorbed, and the maximum concentration of the drug in the blood plasma is reached within 40 minutes after the injection. Subsequently, the drug is excreted by the kidneys and with the help of the intestines.

Instructions for use

The dosage of the drug, as well as the duration of the course of treatment, is chosen by a specialist on the basis of diagnostic data, the stage of the pathology, and the symptoms of the disease that he has.

The following doses of Octreotide are prescribed depending on the purpose of use and symptoms:

• To stop ulcer bleeding conduct a five-day course of infusions daily, 50 mg of a one percent solution.
• Treatment bleeding from the stomach and esophagus performed by infusions of 25–50 micrograms daily for 5 days.
• During therapy acute pancreatitis for 5 days, 3 infusions of the drug are performed per day. In rare cases, in the presence of acute symptoms, the doctor may prescribe a large dose of the drug, while such treatment is performed under the supervision of a specialist in a hospital setting.
• As prevention of postoperative complications on the pancreas patients perform three infusions of 100-200 micrograms of the drug.
• At tumors of the endocrine system The initial dose of Octreotide is 50 micrograms. Subsequently, the doctor, depending on the patient's condition and diagnostic data, may increase or decrease the dose of the drug.

It is necessary not only to determine the patient's diseases and choose the right therapy, but also to correctly perform the subcutaneous administration of Octreotide.

Injection rules:

• It is forbidden to put injections in the same place after a short period of time.
• Unused solution should not be stored.
• The ampoule is opened immediately before the injection.
• The solution is warmed to room temperature.
• Before opening, the ampoule should be inspected for the presence of a change in the color of the drug and the presence of foreign impurities in it.

Drip administration of Octreotide is performed by diluting the drug in 0.9% sodium chloride or an appropriate amount of saline. The injection solution is prepared before using the medicine. After diluting the drug for a dropper, it is allowed to store it in the refrigerator for no more than a day.

special instructions

In the presence of a pituitary tumor, it is necessary to monitor the patient's condition, in particular, constantly monitor the size of the neoplasms and change the dosage of the drug accordingly. In the treatment of endocrine gastropancreatic tumors, a sudden acute relapse of symptoms may occur.

The introduction of Octreotide in pancreatitis in the intervals between sleep and meals can reduce side effects from the gastrointestinal tract. In order to identify an allergy to the drug, it is recommended to conduct a trial infusion, according to the results of which the doctor will decide on the appointment of this medication and its optimal dosage.

With long courses of treatment, which can reach 12 months, it is necessary to perform ultrasound of the gallbladder on a regular basis. This will allow diagnosing the appearance of stones in the ureters.

Gallstone disease is asymptomatic, respectively, revealing such formations on early stage, you can crush them with ultrasound, which will avoid the need for a complex operation.

During the treatment period, regardless of the duration of the course and dosage of the drug, systematic monitoring of the patient's condition is necessary. The physician should monitor the concentration of glucose in the blood, especially in patients with cirrhosis of the liver and varicose veins veins of the esophagus.

With correct diagnosis and timely administration of Octreotide, the prognosis is positive. Shortly after the start of injections and droppers, the patient feels better, and with long courses, complete recovery is possible even with severe forms illness.

Octreotide shows excellent results as a prevention of pancreatic diseases. The components contained in the preparation reduce the inflammation of this internal organ, regenerate its cells, eliminate all the symptoms of existing diseases.

High-quality treatment implies an integrated approach, including the correct selection of therapy, as well as adherence to a special diet that contains a minimum of fatty foods. This will ensure complete recovery even in the presence of chronic pathologies.

drug interaction

Proper dosing of drugs is necessary while taking Octreotide with oral agents, calcium channel blockers, insulin and diuretics.

It is necessary to take into account the following features of interaction:

• Octreotide slows down the adsorption of Cimetidine;
• the bioavailability of Bromocriptine increases;
• reduced absorption of cyclosporine.

Analogues and cost

Currently, in pharmacies you can pick up as original drug Octreotide and its numerous analogues. Substitutes differ in their composition, indications and the amount of active substance. The following drugs are most widely used:

• Serakstal;
• Sandostatin lar;
• Sandostatin;
• Octrid;
• Octretex;
• Octreotide Fsintez;
• Actavis;
• Genfasi.

On sale you can find Octreotide Long, which contains an increased amount of the active substance, which ensures maximum efficiency and duration of the drug. This drug is used as a treatment acute forms diseases of the pancreas, and as a therapy for pancreatitis with cirrhosis of the liver.

The cost of the original drug and analogues in the capital depends on the manufacturer and the amount of the active substance. The price of Octreotide depot at a dosage of 20 mg can be 600-800 rubles. In pharmacies, the original drug and its substitutes are dispensed exclusively by prescription.

Ampoules should be stored in a dark place at a temperature of 8-25 degrees. If the storage conditions are observed, the shelf life of the solution is 5 years. Opened ampoules should not be stored. Detailed information on expiration dates is available in the instructions for use of Octreotide Depot.