Composition and form of release

Solution - 1 ml:

• Active substance: octreotide 100 μg.
• Auxiliary substances: sodium chloride - 9 mg, water d / and - up to 1 ml.

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

Description of the dosage form

The solution for V / B and n / k administration, transparent, colorless liquid, odorless.

pharmachologic effect

Synthetic analogue of somatostatin, which is similar to it pharmacological effects, but significantly greater duration of action.

The drug suppresses the secretion of growth hormone, both pathologically elevated and caused by arginine, exercise and insulin hypoglycemia. The drug also suppresses the secretion of insulin, glucagon, gastrine, serotonin, both pathologically increased and caused by meals; Also suppresses the secretion of insulin and glucagon, stimulated by arginine. Otreotide suppresses thyareotropin secretion caused by thyaroliberin.

In patients who plan to conduct an operation on the pancreas, the use of octreotide before the operation, during and after it reduces the frequency of typical postoperative complications (for example, pancreatic fistula, abscesses, sepsis, acute postoperative pancreatitis).

When bleeding from the varicose-extended veins of the esophagus and the stomach in patients with cirrhosis of the liver, the use of an octreotide in combination with specific treatment (for example, sclerosing and hemostatic therapy) leads to a more effective stopping of bleeding and preventing re-bleeding.

Pharmacokinetics

Suction

After n / k administration, the octreotide is quickly and completely absorbed. C Max octreotide in blood plasma is reached within 30 minutes.

Distribution

Binding with plasma proteins is 65%. The binding of an octreotide with uniform elements is extremely slight. VD is 0.27 l / kg.

Election

After p / to the injection of the drug T1 / 2, octreotide is 100 minutes. After in / in administration, the excretion of octreotide is carried out in 2 phases with T1 / 2 10 min and 90 minutes, respectively. Most of the octreotide is excreted through the intestines, about 32% is removed in the kidney unchanged. General clearance is 160 ml / min.

Pharmacokinetics in special clinical cases

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

With severe renal failure Clearance decreases by 2 times.

Pharmacodynamics

Otreiotide is a synthetic analogue of somatostatin, which is similar to it pharmacological effects, but much greater duration of action. Octreotide suppresses the secretion of growth hormone (GR), both pathologically increased and caused by arginine, physical activity and insulin hypoglycemia. The drug also suppresses the secretion of insulin, glucagon, gastrine, serotonin, both pathologically increased and caused by meals; Also suppresses the secretion of insulin and glucagon, stimulated by arginine. Otreotide suppresses thyareotropin secretion caused by thyaroliberin.

In patients who plan to carry out operations on the pancreas, the use of octreotide before the operation, during and after it reduces the frequency of typical postoperative complications (for example, pancreatic fistulas, abscesses, sepsis, acute postoperative pancreatitis). When bleeding from the varicose-extended veins of the esophagus and the stomach in patients with cirrhosis of the liver, the use of an octreotide in combination with specific treatment (for example, sclerosing and hemostatic therapy) leads to a more efficient stopping of bleeding and prophylaxis of re-bleeding.

Clinical pharmacology

Analogue somatostatin. The drug for intensive therapy in gastroenterology.

Indications for use

• Treatment of acute pancreatitis;
• stop bleeding at peptic disease stomach and duodenal estate;
• stopping bleeding and prevention of re-bleeding from varicose extended veins of the esophagus in patients with liver cirrhosis;
• prevention and treatment of complications after operations on the abdominal organs.

Contraindications for use

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

With caution: Heldlais (gallway disease), diabetes, Pregnancy, lactation period.

Application during pregnancy and children

The use of octreotide during pregnancy has not been studied. Octreotide should be applied during pregnancy only if the intended benefit for the mother exceeds the potential risk to the fetus.

It is not known whether the drug falls in breast milkTherefore, when using the drug during lactation, it should be abandoned to breastfeeding.

Application in children

Contraindicated children under the age of 18

Side effects

From the head of the gastrointestinal tract: it is possible - anorexia, nausea, vomiting, spastic abdominal pain, a feeling of bloating, excess gas formation, liquid chair, diarrhea, steatheree. Although the selection of fat fat may increase, there is no indication that long-term treatment with an octreotide can lead to the development of absorption disorders (Malabsorption). In rare cases, phenomena can be marked, resembling acute intestinal obstruction. There are certain cases of acute hepatitis without cholestasis, hyperbilirubinemia in combination with an increase in the activity of the SFF, GGT and, to a lesser extent, are other transaminases.

Long use of octreotide can lead to the formation of stones in bile bubble.

From side of cardio-vascular system: In some cases, arrhythmia, bradycardia.

From side carbohydrate exchange: A violation of glucose tolerance is possible after meals (due to the suppression of insulin secretion by the drug), hypoglycemia; In rare cases, during prolonged treatment, the development of persistent hyperglycemia is possible.

Local reactions: In the injection site, pain, the sensation of itch or burning, redness, swelling is possible (usually pass within 15 minutes).

Others: allergic reactions, Alopecia.

Medicinal interaction

Octreotide reduces the absorption of cyclosporin, slows down the suction of cimetidine.

Correction of the dosing mode of simultaneously used diuretics, beta-adrenoblockers, "slow" calcium channels, insulin, oral hypoglycemic drugs.

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

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

Dosage

For the treatment of acute pancreatitis, the drug is introduced in a dose of 100 μg 3 times / day for 5 days. It is possible to appoint up to 1200 μg / day using the I / on the route of administration.

To stop the ulcerative bleeding, introduced in / in a dose of 25-50 μg / h in the form of a / in infusion within 5 days.

To stop bleeding from varicosely extended veins of the esophagus, introduced in / in a dose of 25-50 μg / h in the form of a long-term in / in infusions within 5 days.

Natural patients do not need to reduce the octreotide dose.

For the prevention of complications after the pancreas operations, the first dose of 100-200 μg is introduced in 1-2 hours to laparotomy; Then, after surgery, p / k at 100-200 μg 3 times / day for 5-7 consecutive days.

Overdose

Symptoms: short-term gentlemen, the feeling of "tide" of blood to face, spastic abdominal pain, diarrhea, nausea, the sensation of emptiness in the stomach.

Treatment: symptomatic.

Precautions

In patients with diabetes mellitus receiving insulin, octreotide can reduce the need for insulin.

If the stones in the bustling bubble are revealed before the start of treatment, the question of the use of octreotide is solved individually, depending on the ratio of the potential therapeutic effect of the drug and possible risk factors associated with the presence of stones in the gallbladder.

Side effects from the heading of the gastrointestinal tract can be reduced if the injections of the octreotide do in the intervals between the meals or before bedtime.

To reduce discomfort phenomena at the injection site, it is recommended to bring the solution of the drug before administration to room temperature and introduce a smaller volume of the drug. Several injections should be avoided at the same place through short time intervals.

Impact on the ability to driving vehicles and control mechanisms

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

pR D / INJECTIONS 50 μg / ml: 1 ml of AMP.

Injection Colorless, transparent.

Excipients:

pR D / INJECTIONS 100 μg / ml: 1 ml of AMP.
Reg. No: 9959/12/17 of 30.10.2017 - the validity period reg. UD. is not limited

Injection Colorless, transparent.

Excipients: Acetic acid Ice - 2 mg, sodium acetate trihydrate - 2 mg, sodium chloride - 7 mg, water d / and - up to 1 ml.

1 ml - 1 ml ampoules (1) - packs cardboard.

Description active ingredients drug Okters. The reduced scientific information is generalizing and cannot be used to make a decision on the possibility of applying a specific medicinal preparation. Renewal date: 07/31/2019

pharmachologic effect

Synthetic analogue of somatostatin, characterized by greater duration of action. Inhibits the secretion of the lead's front fractions of the pituitary gland, as well as the secretion of TSH. Inhibits exocrine and endocrine (insulin, glucagon) secretion of the pancreas, as well as the secretion of gastrin, of hydrochloric acid, cholecystokinin, secretine, digestive enzymes, vasointsinal peptide and some other peptides, biologically active substances whose secretion is carried out by a gastro-entero-pancreatic system. Suppresses the motility of the stomach and intestines.

Pharmacokinetics

After p / to injection quickly and completely absorbed into the systemic blood flow. C MAX active substance in plasma is achieved for 30 minutes. Binding with plasma proteins is 65%. Binding with uniform elements is extremely slight. V d is 0.27 l / kg.

General clearance is 160 ml / min. T 1/2 after p / to injection - 100 min. After in / in the introduction, the removal process occurs in 2 phases, with T 1/2 10 min and 90 minutes, respectively.

Indications for use

Acromegaly (with insufficient effectiveness surgical treatment, radiotherapy, medication treatment with agonists of dopamine receptors); tumors characterized by increased production of somatolyberine (Rilizing Factor STG); The relief of symptoms caused by the presence of secreting tumors of the gastro-entero-pancreatic system (including carcinoid tumors with the presence of carcinoid syndrome, glucagon, strokes, gastrices); Prevention of complications after the operations on the pancreas; Diarrhea in Patients AIDS, refractming to other types of therapy.

In order to stop the bleeding and prevention of re-bleeding from the varicose-extended veins of the esophagus during cirrhosis of the liver (in combination with endoscopic sclerosing therapy).

Dosing mode

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

The octreotide in the form of a dosage form with the usual duration of action is used in / to and in / in drip, in the form of a depot-form - deep in / m.

Side effects

From side digestive system: Anorexia, abdominal pain, nausea, vomiting, bloating, diarrhea, steatherea;

violation of glucose tolerance;

rarely - severe pain in epigastrics, palpation pain, abdominal muscle tension, acute hepatitis, hyperbilirubinemia, improving the activity of liver enzymes;

for long use In some cases - the formation of stones in the bustling bubble.

Local reactions: Pain, burning, itching, redness, swelling at the injection site.

With simultaneous use, bioavailability of bromocriptine increases; with insulin - it is possible to increase hypoglycemic action; With cyclosporin - the absorption of cyclosporine decreases, with cimetidine - slows down the suction of cimetidine.

India Russia

Group of goods

Hormonal drugs

Analogue somatostatin. The drug for intensive therapy in gastroenterology

Forms of release

• 1 ml - ampoules (5) - Contour packaging (1) - Putures cardboard. 1 ml - ampoules (5) - Contour packaging (2) - packs cardboard. 1 ml - ampoules (5) - Contour Packaging Plastic (1) - Cardboard packs. 1 ml - ampoules (5) - Contour Packaging Plastic (1) - Cardboard packs. 1 ml - ampoules (5) - Contour Packaging Plastic (2) - Cardboard packs. 10 ampoules 1 ml in UE 5 ampoules 1 ml in UP AMPUILS 1ML - 10 pcs in UE. Ampoules on 1ml - 5 pcs in pack. intravenous solution subcutaneous administration 100 μg / ml 1 ml in an ampoule having a label in the form of a green ring of dark glass vials (1) complete with solvent (AMP), a syringe with disposable and needles d / and (2) - cardboard packs. Dark glass vials (1) complete with solvent (AMP), a syringe with disposable and needles d / and (2) - packs cardboard. Dark glass vials (1) complete with solvent (AMP), a syringe with disposable and needles d / and (2) - packs cardboard. Dark glass vials (1) bundled with solvent (AMP), Disposable syringe, needles d / and (2) and alcohol tampons (2) - Cardboard packs.

Description of the dosage form

• The lyophilisate for the preparation of a suspension for the introduction of the prolonged effect of white or white with a weak yellowish tint of color, in the form of a powder or porous, compacted into a mass tablet; The applied solvent is a colorless transparent liquid; Prepared suspension - white or white lyophilisate for the preparation of a suspension for the introduction of the prolonged effect of white or white with a weak yellowish tint of color, in the form of a powder or compacted in a mass tablet; The applied solvent is a colorless transparent liquid; Prepared suspension - white transparent colorless liquid odorless transparent, colorless solution for V / B and p / k administration 0.005% transparent, colorless, odorless injection solution 0.005% transparent, colorless, odorless. A solution for injection 0.01% transparent, colorless, odorless. A solution for injection 0.01% transparent, colorless, odorless. Solution for injection 0.01%, transparent

pharmachologic effect

Octreotide depot is dosage form Otreotida long action For in / m of administration, ensuring the maintenance of stable therapeutic concentrations of octreotide in the blood for 4 weeks. Otreotide is a synthetic octapeptide, which is an analogue of a natural hormone of somatostatin and possessing similar pharmacological effects similar to it, but significantly greater action. The drug suppresses pathologically increased secretion of growth hormone, as well as peptides and serotonin produced in a gastroenteropancreatic endocrine system. In healthy people, octreotide, like somatostatin, suppresses the secretion of growth hormone, caused by arginine, physical activity and insulin hypoglycemia; Secrecy of insulin, glucagon, gastrin and other Gastroenteropancreatic peptides endocrine systemcaused by food intake, as well as secretion of insulin and glucagon, stimulated by arginine; The secretion of thyrotropin caused by thyaroliberin. The overwhelming effect on the secretion of growth hormone in an octreotide, in contrast to somatostatin, is expressed significantly more than on the secretion of insulin. The administration of octreotide is not accompanied by a phenomenon of hormones hypersection by a negative feedback mechanism. In patients with acromegaly, the administration of octreotide depot provides in the overwhelming majority of cases a resistant reduction in the level of growth hormone and normalization of the concentration of insulin-like growth factor 1 / somatomedin C (IFR-1). Most patients with acromegaly octreotide depot significantly reduces the severity of such symptoms as headache, increased sweating, paresthesia, fatigue, bone pain and joints, peripheral neuropathy. It was reported that treatment with an octreotide of individual patients with pituitary adenomas, secreting growth hormone, led to a decrease in tumor dimensions. In carcinoid tumors, the use of octreotide can lead to a decrease in the severity of the symptoms of the disease, first of all, such as tides and diarrhea. In many cases, clinical improvement is accompanied by a decrease in serotonin concentration in plasma and excretion of 5-hydroxyindoluxous acid with urine. In tumors characterized by hyperproduction of a vasoactive intestinal peptide (VIPOMA), the use of octreotide leads in most patients to a decrease in severe secretory diarrhea, which is characteristic of this state, which in turn leads to an improvement in the quality of life of the patient. At the same time there is a decrease in concomitant violations. electrolyte balance, for example, hypokalemia, which allows you to cancel enteral and parenteral administration of fluid and electrolytes. According to computer tomography, some patients have a slowdown or a stop of the progression of the tumor, and even a decrease in its size, especially metastases in the liver. Clinical improvement is usually accompanied by a decrease (up to normal values) Concentration of a vasoactive intestinal peptide (VIP) in plasma. When glucagonomas, the use of octreotide in most cases leads to a noticeable decrease in the necrotic migratory rash, which is characteristic of this state. Octreotide does not have any significant effect on the severity of diabetes, often observing with glucagonomas, and usually does not lead to a decrease in the need for insulin or oral hypoglycemic drugs. In patients suffering from diarrhea, the octreotide causes its decrease, which is accompanied by an increase in body weight. When applying an octreotide is often noted fast decline The concentration of glucagon in the plasma, however, with long-term treatment, this effect is not preserved. At the same time, symptomatic improvement remains a stable long time. With gastrium / Zolinger-Ellison syndrome, an octreotide used as a 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 in relation to diarrhea. It is also possible to reduce the severity and other symptoms probably associated with the synthesis of peptide tumor, incl. tides. In some cases, there is a decrease in the concentration of gastrin in plasma. In patients with insulinians, octreotide reduces the level of immunoreactive insulin in the blood. In patients with operational tumors, the octreotide can ensure the restoration and maintenance of normoglycemia in the preoperative period. In patients with non-cultural benign and malignant tumors The control of glycemia can improve and without a simultaneous continuous reduction in the level of insulin in the blood. In patients with rarely occurring tumors, hyperproduction of the growth hormone rhythm (somatolybering), octreotide reduces the severity of symptoms of acromegaly. This, apparently, is due to the suppression of the secretion of the rillation factor of the growth hormone and the most growth hormone. In the future, it is possible to reduce the size of the pituitary gland, which before the start of treatment have been increased. In patients with hormonistant cancer prostatic gland The pool of neuroendocrine cells expressing somatostatin receptors, Athena to octreotide (SS2 and SS5 types), increases, which determines the tumor sensitivity to octreotide. The use of octreotide depot in a complex with dexamethasone against the background of the androgen blockade (drug or surgical castration) in patients with hormon-resistant prostate cancer restores the sensitivity to hormone therapy and leads to a decrease in the prostatic specific antigen (PSA) of more than 50% of patients. In patients with hormonistant cancer of the prostate gland with metastases in the bone, this therapy is accompanied by a pronounced and long-term painkillers. At the same time, all patients who responded to combined therapy with octreotide-depot, significantly improves the quality of life and median of non-dedicional survival.

Pharmacokinetics

Absorption after p / to the administration of octreotide is quickly and completely absorbed. Cmax octreotide in blood plasma is reached within 30 minutes. Distribution binding with plasma proteins is 65%. The binding of an octreotide with uniform elements is extremely slight. VD is 0.27 l / kg. Establishing General clearance is 160 ml / min. About 32% is displayed unchanged by the kidneys. After p / to the injection of the drug T1 / 2, octreotide is 100 minutes. After in / in administration, the excretion of octreotide is carried out in 2 phases with T1 / 2 10 min and 90 minutes, respectively. Pharmacokinetics in special clinical cases in elderly patients decreases clearance, and T1 / 2 increases. With severe renal failure, the clearance decreases by 2 times.

Special conditions

With pituitary tumors, secreting GR, careful observation of patients is necessary, since it is possible to increase the size of tumors with the development of such serious complications as the narrowing of fields of vision. In these cases, we should consider the need to apply other methods of treatment. In 15-30% of patients receiving octreotide p / k for a long time, it is possible to appear stones in the bustling bubble. The prevalence in the overall population (age of 40-60 years) is 5-20%. The experience of prolonged treatment with an octreotide of the prieved action of patients with acromegaly and tumors of the gastrointestinal tract and pancreas suggests that an octreotide of a prurable action, in comparison with the octreotide short actiondoes not lead to an increase in the frequency of the formation of the gallbladder stones. Nevertheless, the ultrasound of the gallbladder is recommended before starting treatment with octreotide and approximately every 6 months in the treatment process. Stones in the bustling bubble, if they are still detected, as a rule, asymptomatic. In the presence of clinical symptoms shown conservative treatment (for example, the use of bile acids) or operational intervention. In patients with diabetes mellitus 1, the octreotide type can influence the exchange of glucose and, therefore, reduce the need for insulin intimidated. For patients with type 2 diabetes and patients without a concomitant impairment of carbohydrate metabolism, the subcutaneous octreotide injections can lead to postprandial glycemia. In this regard, it is recommended to regularly monitor the level of glycemia and, if necessary, correlate hypoglycemic therapy. In patients with insulinami, against the background of treatment with octreotide, an increase in the severity and duration of hypoglycemia may be noted (this is due to the more pronounced overwhelming effect on the secretion of gr and glucagon than on the secretion of insulin, as well as with a smaller duration of the inhibitory effect on the secretion of insulin). The systematic observation of these patients is shown. Before appointing an octreotide, patients must pass the initial ultrasound of the gallbladder. During treatment with octreotide, repeated ultrasound of the gallbladder should be carried out, preferably at intervals of 6-12 months. If the bubble stones are found even before the start of treatment, it is necessary to estimate the potential advantages of octreotide therapy compared to possible riskassociated with the presence of gallstones. Currently, there are no evidence that octreotide adversely affects the course or forecast of an existing biliary disease. The maintenance of patients in which the bubble stones are formed during the treatment with octreotide. a) asymptomatic gallbladder stones. The use of octreotide can be terminated or continued - in accordance with the assessment of the benefit / risk ratio. In any case, no other measures are required, except for the continuation of inspections by making them, if necessary, more frequent. b) the stones of the gallbladder with clinical symptoms. The use of octreotide can be terminated 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 gallway disease with clinical manifestations. Medicia treatment Includes the use of combinations of bile acid preparations (for example, hanodoxycholic acid at a dose of 7.5 mg / kg / day. In combination with ursodeoxycholic acid in the same dose) under ultrasonic control - until the stones are completely disappeared. The effect on the ability to drive vehicles and control mechanisms does not have data on the effect of octreotide on the ability to drive a car and working with mechanisms.

Structure

• 1 ml of octreotide (in the form of a free peptide) 50 μg. Auxiliary substances: sodium chloride - 9 mg, water d / and - up to 1 ml. 1 ml of octreotide (in the form of a free peptide) 50 μg. Auxiliary substances: sodium chloride - 9 mg, water d / and - up to 1 ml. 1 ml of octreotide (in the form of free peptide) 100 μg Auxiliary substances: sodium chloride, water d / and. 1 ml of octreotide (in the form of free peptide) 100 μg Auxiliary substances: sodium chloride, water d / and. 1 ml of octreotide (in the form of free peptide) 50 μg Auxiliary substances: sodium chloride, water d / and. 1 ml of octreotide 100 μg 1 FL. Octreotide 10 mg - "- 20 mg -" - 30 mg Auxiliary substances: Copolymer DL-dairy and glycolic acids, D-mannitol, carboxymethylcellulose sodium salt, Polysorbat-80. Solvent: rr Mannitol 0.8% - 2 ml. 1 FL. Octreotide 10 mg - "- 20 mg -" - 30 mg Auxiliary substances: copolymer DL-dairy and glycolic acids, D-mannitol, carboxymethylcellulose sodium salt, polysorbat-80. Solvent: rr Mannitol 0.8% - 2 ml. 1 ml of solution contains: active substance: octreotide acetate (which is equivalent to an octreotide content) -0.064 (0.050 mg) μg and 0.128 mg (0,100 mg); Auxiliary substances: acetic acid Ice, sodium acetate (trihydrate), sodium chloride, water for octreotide injection 10 mg. Auxiliary substances: Copolymer DL-milk and glycolic acids - 270 mg, D-mannitol - 85 mg, carboxymethylcellulose sodium salt - 30 mg, Polysorbat-80 - 2 mg. Solvent: rr Mannitol 0.8% - 2 ml.

Octreotide indications for use

• Acromegaly (when adequate control of the manifestations of the disease is carried out by subcutaneous installation of the octreotide, in the absence of sufficient effect from surgical treatment and radiation therapy; To prepare for surgical treatment, for the treatment between radiotherapy courses to the development of a persistent effect, in non-cultural patients). In therapy of endocrine tumors gastrointestinal tract (GCC) and pancreas: carcinoid tumors with carcinoid syndrome phenomena; insulinas; VIPOMA; Gastric (Zlinger-Ellison syndrome); glucagon (to control hypoglycemia in a preoperative period, as well as for supporting therapy). In the therapy of endocrine tumors of the gastrointestinal tract (gastrointestinal tract) and pancreas: carcinoid tumors with carcinoid syndrome phenomena; insulinas; VIPOMA; Gastric (Zlinger-Ellison syndrome); glucagon (to control hypoglycemia in a preoperative period, as well as for supporting therapy). Somatolyberinomes (tumors characterized by hyperpr

Otreotide Contraindication

• - childhood up to 18 years; - Increased sensitivity to octreotide or other components of the drug. With caution: choletiasis (gallway disease), diabetes, pregnancy, lactation period.

Octreotide dosage

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

Otreiotide Side effects

• Local reactions: pain, the sensation of itching, or burning, redness, or swelling in the place of p / to injection (usually pass within 15 minutes). The severity of local reactions can be reduced if it is used to use a room temperature solution, or to introduce a smaller volume of a concentrated solution. From the head of the gastrointestinal tract: anorexia, nausea, vomiting, spastic abdominal pain, scrawling, excess gas formation, liquid chair, diarrhea, steatheree. Although the release of fat with the fee may increase, today there is no evidence that prolonged treatment with an octreotide can lead to the development of nutritional deficiency due to absorption disorders (Map'absorption). In rare cases, phenomena can be marked, resembling acute intestinal. Near: The progressive bloating of the abdomen, expressed pain in the epigastric region, the tension of the abdominal wall. Prolonged use of octreotide can lead to the formation of stones in the gallbub. The frequency of side effects by the gastrointestinal tract can be reduced by increasing the intervals between meals and the administration of octreotide. From the pancreas side: it has been reported rare cases of acute pancreatitis, which has developed in the first hours or the days of the use of octreotide. With long-term use, cases of pancreatitis associated with choletiasis were noted. On the part of the liver: there are separate reports on the development of disorders of the liver function (acute hepatitis without cholestasis with normalization of transaminase indicators after cancellation of the octreotide); The slow development of hyperbilirubinemia, accompanied by an increase in alkaline phosphatase, gamma glutamilitrase and, to a lesser extent, other transaminases. From side cardiovascular Systems: In some cases - bradycardia. From the metabolism: Since the octreotide has an overwhelming effect on the formation of GR, glucagon and insulin, it can influence the glucose exchange. It is possible to reduce glucose tolerance after meals. With prolonged use of octreotide P / k in some cases, persistent hyperglycemia can develop. The state of hypoglycemia was also observed. Others: In rare cases, a temporary loss of hair has been reported after the administration of the octreotide. There are separate reports on the development of increased sensitivity reactions: rarely -kened allergic reactions; In some cases, anaphylactic reactions.

Medicinal interaction

Octreotide reduces the absorption of cyclosporin, slows down the suction of cimetidine. With the simultaneous use of octreotide and bromocriptine, the bioavailability of the latter increases. Correction of the dosing mode of simultaneously used diuretics, beta-adrenerblockers, "slow" calcium channels, insulin, oral hypoglycemic medicines, glucagon. There is evidence that the analogues of somatostatin can reduce the metabolism of drugs, metabolizing cytochrome P450 enzymes (may be due to the suppression of growth hormone). Since it is impossible to exclude such effects of the rally, drugs, metabolized by enzymes of the cytochrome P450 system and having a narrow therapeutic dose range, should be prescribed with caution.

Overdose

It is known that the administration of an octreotide in a dose to 2000 μg in the form of an injection 3 times over several months was moved well. Maximum motherwise dose When in / in bolus administration, an adult patient was 1000 μg. At the same time, there were such symptoms as a decrease in heart rate, "tides" of blood to face, abdominal pain of spastic nature, diarrhea, nausea, the sensation of emptiness in the stomach. All these symptoms were resolved within 24 hours from the moment of administration of the drug. An excess dose of octreotide 250 μg / h (instead of 25 μg / h) was introduced to one patient for a long-term infusion method (instead of 25 μg / h), which was not accompanied by side effects. In case of acute overdose, there were no dangerous reactions. Treatment: symptomatic therapy.

Storage conditions

• dry
• bear from children
• storing

Information provided

An octreotide can be used to treat pancreatitis in acute and chronic form, which is a synthetic analogue of growth hormone. This medicine effectively suppresses signs of inflammation of the pancreas.

Release form and composition

Octreotide is a synthetic analogue of the hormone of somatostatin produced in the hypothalamus and pancreas. This drug for a short time suppresses the development of enzymes, which allows you to treat patients with chronic and acute form of pancreatitis.

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

Optreotide is produced in the form of a solution for intravenous and subcutaneous injectionswhich contain 0.005 and 0.01% active substance. The drug does not smell and colors, and its use is permissible only under the supervision of the doctor.

You can find an octreotide from domestic and foreign manufacturers. The latter are distinguished by the quality of manufacture and are recommended by the majority of specialists. The cost of imported drugs can be 20-30% higher than domestic.

The octreotide can be used as follows:

• Intravenously using a dropper when daily for 15 days the patient is introduced to 1,200 micrograms of the drug.
• Subcutaneous injections are performed three times a day. Depending on the stage of the disease and localization of the pancreas lesion, the daily dose in the first 5 days can be 50-300 micrograms of the drug, and subsequently, the dosage is reduced by relying on the existing symptoms.
• For intramuscular administration, the lyophilisate suspension is used, which is broken by the patient once a month.

Regardless of the method of applying this drug, it is forbidden to prescribe an octreotide. The medicine is released in pharmacies exclusively by the recipe, and a specialist can write it only after a full examination of the patient.

With incorrect dosage and independent assignment of the drug, serious damage to the pancreas is possible, up to the disability of the patient.

Side Effects and Contraindications

Wrong reception of the drug and an octreotide overdose may result in different side effects. Contraindications include:

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

When appointing the drug, the doctor must take into account possible complications Pancreatitis, and the patient itself is obliged to follow the recommendations of the doctor, without increasing their own dosage of medication. In more detail with contraindications can be found in the instructions for the use of octreotide in pancreatitis.

With overdose, various side effects may be marked. The patient, when they appear, it is necessary to stop taking the drug and consult a doctor for advice. TO by-phenomena For therapy, octreotide includes:

• Various allergic reactions, including the difficulty of breathing, itching, peeling of the skin and urticaria.
• Local reactions, including pain, painting in the injection area.
• Failure heart Rhythm and bradycardia.
• Violation of metabolism and problems with the absorption of carbohydrates.
• Dyspeptic phenomena: liquid chair, bloating, spasms, vomiting and nausea.
• In rare cases, the side effect of the hormone reception is the formation in the bustling bubble and ureters of stones that will require crushing or surgical removal. With short-term treatment courses, there should be no fear of such serious consequences.

Pharmacological properties

When receiving an 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 agent allows to eliminate possible postoperative complications, including acute abscess, sepsis and pancreatic fistulas.

The active substance in the body is quickly absorbed, and the maximum concentration of the drug in the blood plasma is achieved after 40 minutes after the injection. Subsequently, the drug is excreted by the kidneys and by the intestine.

Instructions for use

The dosage of the drug, as well as the duration of the course of treatment, is chosen by a specialist based on diagnostic data, the stages of the pathology that have symptoms of the disease.

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

• For stopping ulcerative bleeding Conduct a five-day course of infusions daily by 50 mg of one-thorough solution.
• Treatment bleedings from the stomach and esophagus Performing infusions of 25-50 micrograms daily for 5 days.
• For therapy acute pancreatitis For 5 days, 3 days of infusion of the drug are performed. In rare cases, in the presence of acute symptoms, the doctor may prescribe a large dose of medication, while such treatment is performed under the supervision of a specialist in a hospital.
• As prevention of postoperative complications on the pancreas Patients perform three-time infusions of 100-200 micrograms of the drug.
• For tumors of the endocrine system The initial octreotide dose is 50 micrograms. In the subsequent doctor, depending on the patient's condition and diagnostic data, can increase or decrease the dose of the drug.

It is necessary not only to determine the disease available in a patient and competently choose therapy, but also correctly perform the subcutaneous administration of the octreotide.

Rules for the introduction of injections:

• Put injections in the same place after a short period of time prohibited.
• Unused solution is not recommended.
• The ampoule is opened immediately before performing the injection.
• The solution is heated to room temperature.
• Before opening, an ampoule should be inspecting for changing the color of the drug and the presence of foreign impurities in it.

The drip administration of the octreotide is performed by diluting the drug in 0.9% sodium chloride or the corresponding amount of saline. Injection solution is prepared before using the medication. After breeding the drug for a dropper, its storage is allowed in the refrigerator no more than a day.

special instructions

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

The administration of octreotide with pancreatitis in the intervals between sleep and food intake allows you to reduce side effects from the gastrointestinal tract. To identify allergies 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-term treatment courses that can reach 12 months, it is necessary to perform an ultrasound of the gallbladder on a regular basis. This will diagnose the appearance of stones in ureters.

Biliary disease is asymptomatic, respectively, revealing such education on early stage, It is possible to crush them with ultrasound, which will avoid the need to perform a complex operation.

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

With proper diagnosis and timely appointment of the octreotide, the forecast is positive. The patient soon after the start of injection and dropper feels improved well-being, and with long-term courses it is possible to complete recovery even with severe forms of the disease.

Excellent results show octreotide as preventing pancreatic diseases. The components contained in the drug reduce inflammation of this. internal organ, its cells regenerate, eliminate all the symptoms of the diseases available.

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 oily food. This will ensure complete recovery even in the presence of chronic pathologies.

Medicinal interaction

It is necessary to proper dosing of drugs while receiving an octreotide with overtoral tools, calcium channels, insulin and diuretics blockers.

The following features of interaction should be taken into account:

• Octreotide slows down the adsorption of cimetidine;
• the bioavailability of bromocriptine increases;
• the suction of cyclosporine is reduced.

Analogs and cost

Currently, pharmacies can be selected both the original octreotide preparation and its numerous counterparts. Substitutes are distinguished by their composition, indications and number of active substance. The following drugs received the greatest distribution:

• Serakstal;
• Sandostatin LAR;
• Sandostatin;
• Okrid;
• Octerex;
• Otreotide FSintesis;
• Aktavis;
• Genfasi.

You can find on sale Otreotide Longwhich contains an increased amount of active substance, which ensures maximum efficiency and duration of the drug. This drug is used as for treatment. acute forms Diseases of the pancreas and as therapy of pancreatitis with cirrhosis of the liver.

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

Store ampoules should be in a dark place at a temperature of 8-25 degrees. Under the storage conditions, the shelf life of the solution is 5 years. Open ampoules stored prohibited. Detailed information on the shelf life is available in the instructions for applying an octreotide depot.

Otreotide - synthetic analogue of somatostatin; The preparation with somatostatin-like action.

Release form and composition

Dosage form - a solution for intravenous and subcutaneous administration: transparent liquid without color and odor (50 and 100 μg / ml - 1 ml in dark glass ampoules with an opening tension ring, in ampoules with a point of fault or colorless glass ampoules with color marking in The form of two green strips, 5 ampoules in the packing of cell contour, 1 or 2 packs in a pack of cardboard; 300 and 600 μg / ml - 1 ml in dark glass ampoules with an autopsy tension ring, in ampoules with a point of fault or colorless glass ampoules With color marking in the form of two green stripes, 1, 2 or 5 ampoules in the packing of the circuit in circuit, 1 package 1, 2 or 5 ampoules or 2 packs of 5 ampoules in a pack of cardboard).

The active ingredient: octreotide, in 1 ml of solution - 50, 100, 300 or 600 μg.

Auxiliary components: sodium chloride and water for injection.

Indications for use

• Acromegaly - to reduce the level of growth hormone and insulin-like growth factor-1 (IFR-1) in the blood plasma and control of the main manifestations of the disease in cases where the effect of the use of radiation therapy or surgical treatment is not enough; treatment of acromegaly in patients who refused to surgery or having a contraindication to its conduct; short-term treatment in the intervals between radiation therapy courses until the sufficient effect is obtained from its implementation;
• Secretting endocrine tumors of the gastrointestinal tract and pancreas (for monitoring symptoms): glucagon, vipoma, carcinoid tumors with the presence of carcinoid syndrome, somatolybering (tumors, characterized by hyperproduction of growth hormone rhythm), gastrices or Zolinger Ellison syndrome (usually in combination with Blockers H 2-pistamic receptors and proton pump inhibitors), insulinoma (for hypoglycemia control in the preoperative period, for supporting therapy);
• Stop bleeding from varicose veins of the esophagus and stomach in patients with cirrhosis of the liver and prophylaxis of repeated bleeding (in combination with specific medical events, For example, with endoscopic sclerosing therapy).

Additionally, for octreotide in a dose of 50 and 100 μg / ml:

• Stop bleeding with ulcer of the stomach and 12-rosysome intestine;
• Therapy of acute pancreatitis;
• Treatment and prevention of complications after surgical operations on the abdominal organs.

The octreotide is not an antitumor drug, its use cannot lead to curable patients with secreting endocrine tumors of the gastrointestinal tract and pancreas.

Contraindications

Absolute:

• Age up to 18 years;
• Hypersensitivity to the drug.

Relative:

• Diabetes;
• Holithiasis (gallway disease);
• Pregnancy;
• Lactation.

Method of application and dosage

The drug is administered subcutaneously (p / k) or intravenously (in / c) drip.

Octreotide in a dose of 50 and 100 μg / ml

• Treatment of acute pancreatitis: p / k at 100 μg 3 times a day with a 5-day course. It is also possible in / in the introduction in a daily dose to 1200 μg;
• Stop ulcerative bleeding: in the form of a / in infusion of 25-50 μg / h daily within 5 days;
• Stop bleeding from varicosely expanded veins of the esophagus: in the form of long-term in / in infusion at a dose of 25-50 μg / hour for 5 days;
• Prevention of complications after surgical intervention in the pancreas: the first dose - 100-200 μg n / k 1-2 hours to laparotomy, after the operation - p / k at 100-200 μg 3 times a day daily within 5-7 days ;
• Acromegaly: P / C at a dose of 50-100 μg with intervals of 8 or 12 hours;
• Tumors of the gastroenteropancreatic endocrine system: n / to 50 μg 1-2 times a day with a gradual increase in dose to 100-200 μg 3 times a day.

Octreotide in a dose of 300 and 600 μg / ml

• Acromegaly (in case of ineffectiveness initial therapy Using an octreotide in a dose of 50-100 μg, which is estimated on the basis of a monthly determination of the concentration of blood growth hormone (target concentration: growth hormone less than 2.5 ng / ml, IFR-1 - within normal values), analysis clinical signs Diseases and tolerance of the drug: p / k at a dose of 300 μg at intervals of 8 or 12 hours. If this dose is not enough, the selection of the dose is carried out further in accordance with the specified criteria. Maximum allowable daily dose It is 1500 μg. In patients receiving octreotide in a stable dose, every 6 months it is necessary to determine the concentration of growth hormone. If after 3 months of therapy, there is no improvement clinical picture diseases and sufficient reduction in the concentration of growth hormone, further treatment with the drug is inappropriate;
• The tumors of the gastroenteropancreatic endocrine system (in the event of the ineffectiveness of initial therapy using an octreotide at a dose of 50 μg 1-2 times a day with a gradual increase in dose to 100-200 μg 3 times a day, which is estimated on the basis of a clinical effect achieved, influence on hormone concentration, produced by a tumor and tolerance of the drug): p / k 300 μg 1-2 times in essence, with insufficient effectiveness possible gradual increase in the dose of the drug, in exceptional cases - to a dose of 300-600 μg 3 times in essence. Supporting doses are selected individually for each patient. If, with carcinoid tumors, the treatment with octreotide in the maximum portable dose for 1 week turned out to be ineffective, further treatment with the drug is inappropriate;
• Stop bleeding from varicose veins of the stomach and esophagus: in / in drip at a speed of 25 μg / hour with a 5-day course.

The correction of the maintenance dose is required by patients with impaired liver function.

The experience of applying an octreotide in children is limited.

The rules of subcutaneous administration of the drug:

• Before administration to heat the solution to room temperature, this will reduce the unpleasant sensations at the injection site;
• Not to enter into the same place through short time intervals;
• Ampoules open immediately before administration;
• Unused amount of drug throwing out.

Subcutaneous administration patients can be carried out independently. For this they should get detailed instructions From the attending physician or nurse.

Rules of intravenous drip administration of the drug:

• Before administration, carefully inspect the ampoule for the availability of extraneous inclusions and color changes;
• The contents of 1 ampoules with a content of 600 μg of an octreotide are divorced in 60 ml of sodium solution of chloride 0.9%;
• Prepare a solution immediately before administration;
• If necessary, stored at a temperature of 2-8 ºС not more than 24 hours. Before use, warm to room temperature.

Side effects

Classification of side effects:

• Very often: ≥1 / 10;
• Often: ≥1 / 100, but<1/10;
• Sometimes: ≥1 / 1000, but<1/100.

Side effects identified during clinical studies of the drug:

• Gastrointestinal tract: Very often - nausea, bloating, abdominal pain, diarrhea, constipation; Often - a feeling of filling / gravity of the belly, changing the color of the chair, steatherea, dyspeptic disorders, soft consistency of the chair, vomiting, anorexia;
• Nervous System: Very often - Headache; Often - dizziness;
• Endocrine system: Very often - hyperglycemia; Often - a violation of glucose tolerance, hypoglycemia, hypothyroidism or a violation of the function of the thyroid gland (reducing the levels of thyrotropic hormone, total and free thyroxine);
• Respiratory system: often - shortness of breath;
• Cardiovascular system: often - bradycardia; sometimes - tachycardia;
• Hepatobiliary system: Very often - the formation of stones in the bustling bubble (cholelyatiasis); often - hyperbilirubinemia, cholecystitis, increasing the activity of hepatic transaminases, violation of the colloidal bile stability (manifests itself by the formation of cholesterol microcrystals);
• Dermatological reactions: often - rash, itching, hair loss;
• Others: sometimes - dehydration;
• Local reactions: very often - pain in the injection site.

Side effects caused by the consequent relationship of which with the use of octreotide is not installed:

• Immune system: allergic and anaphylactic reactions;
• Dermatological reactions: urticaria;
• Cardiovascular system: arrhythmias;
• Hepatobiliary system: acute pancreatitis, cholestatic hepatitis, jaundice, cholestasis, cholestatic jaundice, acute hepatitis without cholestasis phenomena, improving the level of alkaline phosphatase and gamma glovedransferase.

special instructions

Side effects from the gastrointestinal tract can be reduced if you enter the drug before bedtime or between meals.

To reduce discomfort when introducing a solution before injection, the ampoule is recommended to heat to room temperature. Do not make injections at the same place through short intervals.

Some side effects can have a negative impact on the speed of reactions and the ability to concentrate attention, this should be taken into account in patients, controlling vehicles and employed in production with potentially hazardous activities.

Patients with pituitary tumors who secrete growth hormone need careful observation during treatment, because It is possible to increase the tumor in size with the development of such a complication as the narrowing of the fields. If this happened, it is necessary to consider the feasibility of applying other methods of therapy.

Women, patients with acromegaly, childbearing, during treatment, it is necessary to use reliable ways of contraception, since with a decrease in the level of hormone growth and normalization of the IFR-1 level, the use of an octreotide can lead to recovery of a childbearing function.

When applying the drug for a long time, the thyroid function should be monitored.

If bradycardia is developing, it is necessary to reduce the dose of beta-adrenobloclars, calcium channels or drugs affecting the water and electrolyte balance.

In some cases, the octreotide can influence the absorption of fats in the intestine.

The drug can contribute to a decrease in the level of cobalamin (vitamin B12) and deviation from the norm of indicators of the test of shillling (suction of cobalamin). When the octreotide is prescribed, patients with anamnestic instructions for vitamin B12 deficiency are recommended to control the concentration of kobalamin in the body.

Before the prescription of the drug, the patient is directed to an ultrasound study (ultrasound) of the gallbladder, during treatment, repeated ultrasounds are carried out every 6-12 months. If the stones in the bustling bubble are diagnosed before the start of therapy, the question of the use of octreotide is solved individually, after the ratio of potential benefits and possible risks. There are no data on the negative influence of the octreotide for the course or forecast of the existing biliary disease.

Cases of formation of gallbladder stones in the treatment process:

• Asymptomatic stones: the use of the drug must be stopped or continuing after estimating the benefit and risk ratio. Doing any measures do not need to be taken, only continue to observe the patient, making it more thorough and frequent;
• Stones with clinical symptoms: Application of the drug must be stopped or continuing after estimating the benefit and risk ratio. In any case, the patient should be treated similarly to other patients with bile disease, accompanied by clinical manifestations. Medication therapy includes the use of combinations of drugs of bile acids (for example, hanodoxichetic acid at a dose of 7.5 mg / kg / day in combination with URSO-Osodoxicole acid in the same dose) under the control of the ultrasound until the stones are completely disappeared.

In the treatment with octreotide of endocrine pancreatic tumors and the gastrointestinal tract in rare cases, a sudden recurrence of symptoms of the disease may occur. In patients with insulinians during the treatment period, it is possible to enhance severity and an increase in the duration of hypoglycemia. For these patients, it is necessary to ensure a thorough regular observation, especially at the beginning of treatment and with each dose change.

Significant fluctuations in blood glucose concentration in some cases can be reduced due to more frequent administration of the drug in smaller doses. In patients with insulin-independent diabetes mellitus, the drug can reduce the need for insulin. In patients with diabetes mellitus 2 with partially preserved secretion of insulin and patients without diabetes, octreotide can lead to the development of postprandial hyperglycemia. Patients with diabetes mellitus during treatment with octreotide should receive anti-diabetic therapy and control blood glucose concentration.

Systematic control of the blood glucose concentration is also necessary after bleeding from varicose veins of the stomach / esophagus, since such patients have increased the risk of the development of type 1 diabetes mellitus, and in patients with diabetes, changes in the need of insulin are possible.

Medicinal interaction

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