Octreotide | Octreotide ampoules 0.005%, 1 ml, 5 pcs.
Special Price
$32.98
Regular Price
$41.00
In stock
SKU
BID501924
Latin name
Octreotide
Octreotide
Latin name
Octreotide
Release form
Solution for injection
Packing
5 ampoules of 1 ml.
Pharmacological action
Octreotide is a synthetic analogue of somatostatin, which is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but a significantly longer duration of action. Octreotide suppresses the secretion of growth hormone, both pathologically increased and caused by arginine, physical activity and insulin hypoglycemia. The drug also inhibits the secretion of insulin, glucagon, gastrin, serotonin, both pathologically increased and caused by food intake, also inhibits the secretion of insulin and glucagon, stimulated by arginine. Octreotide suppresses the secretion of thyrotropin, caused by thyroliberin. Unlike somatostatin, octreotide inhibits the secretion of growth hormone to a greater extent than insulin secretion, and its administration is not accompanied by subsequent hypersecretion of hormones (for example, growth hormone in patients with acromegaly).
In patients with acromegaly, octreotide reduces the concentration of growth hormone and insulin-like growth factor (IGF-1) in blood plasma. A decrease in the concentration of growth hormone by 50% or more is observed in 90% of patients, while a concentration of growth hormone of at least 5 ng / ml is achieved in about half of the patients. In most patients with acromegaly, octreotide reduces the severity of headache, soft tissue swelling, hyperhidrosis, joint pain and paresthesia. In patients with large pituitary adenomas, treatment with octreotide can lead to some reduction in tumor size.
In case of secreting tumors of the gastroenteropancreatic endocrine system in cases of insufficient effectiveness of the therapy (surgery, embolization of the hepatic artery, chemotherapy, including streptozotocin and fluorouracil), the administration of octreotide can lead to an improvement in the course of the disease. So, with carcinoid tumors, the use of octreotide can lead to a decrease in the severity of sensations of flushing of the face, diarrhea, which in many cases is accompanied by a decrease in the concentration of serotonin in the plasma and excretion of 5-hydroxyindoleacetic acid by the kidneys. In tumors characterized by hyperproduction of a vasoactive intestinal peptide (VIPoma), the use of octreotide in most patients leads to a decrease in severe secretory diarrhea and, accordingly, an improvement in the quality of life of the patient. At the same time, there is a decrease in concomitant disturbances in the electrolyte balance, for example, hypokalemia, which allows you to cancel the enteral and parenteral administration of fluid and electrolytes. In some patients, the progression of the tumor slows down or stops, and its size and the size of the liver metastases decrease. Clinical improvement is usually accompanied by a decrease in the concentration of vasoactive intestinal peptide (VIP) in plasma or its normalization. With glucagonomas, the use of octreotide leads to a decrease in migratory erythema. Octreotide does not have any significant effect on the severity of hyperglycemia in diabetes mellitus, while the need for insulin or oral hypoglycemic drugs usually remains unchanged. The drug causes a decrease in diarrhea, which is accompanied by an increase in body weight. Although the decrease in plasma glucagon concentration under the influence of octreotide is transient in nature, clinical improvement remains stable throughout the entire period of drug administration. In patients with gastrinomas / Zollinger-Ellison syndrome, when octreotide is used as monotherapy or in combination with proton pump inhibitors or H2 histamine receptor blockers, a decrease in hypersecretion of hydrochloric acid in the stomach, a decrease in the concentration of gastrin in the blood plasma, as well as a decrease in the severity of diarrhea and hot flashes . In patients with insulinomas, octreotide reduces the level of immunoreactive insulin in the blood (this effect can be short-term - about 2 hours). In patients with operable tumors, octreotide can ensure the restoration and maintenance of normoglycemia in the preoperative period. In patients with inoperable benign and malignant tumors, glycemic control may improve without a simultaneous prolonged decrease in blood insulin levels.
In patients with rare tumors that hyperproduce growth hormone releasing factor (somatoliberinomas), octreotide reduces the severity of acromegaly symptoms. This is due to the suppression of secretion of the releasing factor of growth hormone and growth hormone itself. In the future, pituitary hypertrophy may decrease.
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 (e.g. sclerotherapy) leads to more effective stopping of bleeding and early rebleeding, reducing the volume of transfusions and improving 5-day survival. Believed that the mechanism of action of octreotide is associated with a decrease in organ blood flow through the suppression of vasoactive hormones such as VIP and glucagon.
Pharmacokinetics
Absorption
After s / c administration, octreotide is rapidly and completely absorbed. Tmax of octreotide in plasma - within 30 minutes.
Distribution of
Communication with plasma proteins is 65%. Linking Octreotide to Shaped Elblood counts very little. Vd is 0.27 L / kg.
Excretion of
T1 / 2 after sc administration of octreotide is 100 min. After iv administration, the excretion of octreotide is carried out in 2 phases, with T1 / 2 - 10 and 90 minutes, respectively. Most of octreotide is excreted through the intestines, about 32% - unchanged by the kidneys. The total clearance is 160 ml / min.
Indications
prevention and treatment of complications after operations on the pancreas and gastroduodenal zone
stopping bleeding and prevention of rebleeding from varicose veins of the esophagus in patients with cirrhosis (as part of complex therapy)
treatment of acute pancreatic ulcer disease stomach and duodenum.
Contraindications
Hypersensitivity to octreotide or other components of the drug children under 18 years of age.
Precautions: cholelithiasis (gallstone disease) diabetes mellitus.
Pregnancy and lactation
Experience with octreotide in pregnant women is limited. The drug Octreotide should be used during pregnancy only if if the intended benefit to the mother outweighs the potential risk to the fetus.
It is not known whether the drug passes into breast milk, so if you use the drug during lactation, you should refuse to breast-feed.
Composition
1 ml injection contains:
Active ingredient: octreotide
Excipients: sodium chloride, water d / i.
Dosage and administration
Intravenously (as infusion), subcutaneously.
In the treatment of acute pancreatitis, Octreotide® FSynthesis is administered subcutaneously at a dose of 100 mcg 3 times a day for 5–7 days. It is possible to prescribe up to 1200 μg / day, the selection of the dose is based on the determination of the concentration of amylase, lipase, inflammatory blood cytokines.
For the prevention of complications after pancreatic surgery, the first dose of Octreotide® FSynthesis 100 μg is administered s.c. 1 hour before laparotomy, then after the operation, s / cpo 100 μg is administered 3 times a day for 7 consecutive days.
To stop bleeding from varicose veins of the esophagus, the drug is administered iv in a dose of 25 mcg / h in the form of continuous infusions for 5 days.
To stop bleeding with gastric ulcer and duodenal ulcer, it is recommended to administer Octreotide® FSynthesis in the form of iv infusion at a dose of 25 mcg / h for 5 days.
Elderly patients do not need to reduce the dose of Octreotide® FSynthesis.
Patients with impaired renal function correction of the dosage regimen of octreotide is not required.
In patients with impaired liver function, a maintenance dose adjustment is recommended because there is evidence of an increase in T1 / 2 octreotide in patients with cirrhosis.
Experience with octreotide in children is very limited.
Rules for the preparation and administration of the
solution To reduce the symptoms of discomfort at the injection site, the Octreotide® FSynthesis solution must be at room temperature before administration. With s / c administration of the drug, several injections at the same place should be avoided at short intervals. Ampoules with the drug should be opened immediately before administration, the unused amount of the solution must be destroyed.
Before iv use of the drug, you should carefully examine the solution and make sure it is transparent, there are no suspended particles, sediment, and color changes. You can not use the drug if it is cloudy, contains suspended particles, sediment.
The prepared Octreotide® FSynthesis solution maintains physical and chemical stability at a temperature of 8 to 25 РC for 24 hours. To avoid microbial contamination, diluted solutions must be used immediately after preparation. If the solution is not to be used immediately, it should be stored at a temperature of 2 to 8 РC until its use.
Hold the solution at room temperature before use.
The total time between dilution, storage in the refrigerator and the end of the solution should not exceed 24 hours.
Preparation of a solution for iv drip
The contents of one ampoule containing 500 μg of octreotide, diluted in 60 ml of 0.9% sodium chloride solution. The infusion is repeated with the necessary frequency in accordance with the recommended duration of treatment. Octreotide can also be administered at lower concentrations.
Side effects
Local reactions: pain may occur at the injection site, sensation of itching or burning, redness and swelling (usually go away within 15 minutes).
From the gastrointestinal tract, pancreas, liver and gall bladder: possible - anorexia, nausea, vomiting, spastic abdominal pain, sensation of bloating, excessive gas formation, loose stools, diarrhea and steatorrhea. Although the excretion of fat with feces may increase, there is no indication that prolonged treatment with octreotide may lead to the development of malabsorption (malabsorption). In rare cases, phenomena resembling acute intestinal obstruction (progressive bloating, severe pain in the epigastric region, tension of the abdominal wall) can be noted.
Prolonged use of octreotide can lead to gallstones.
Certain cases of acute hepatitis without cholestasis are known (transaminase values normalize after cancellation of octreotide), as well as hyperbilirubinemia in combination with increased activity of alkaline phosphatase, GGT, and to a lesser extent other transaminases.
There are some reports of rare cases of acute pancreatitis, which developed in the first hours or days of the use of octreotide.
From the CCC: in some cases - tachycardia, bradycardia.
From the side of carbohydrate metabolism: impaired glucose tolerance after eating is possible (octreotide has an overwhelming effect on the formation of GR, glucagon and insulin), hypoglycemia in rare cases with prolonged treatment may develop persistent hyperglycemia.
Other: rarely - allergic reactions, alopecia in some cases - anaphylactic reactions.
Drug Interaction
Octreotide reduces the absorption of cimetidine, cyclosporine, diuretics, beta-blockers, calcium antagonists, insulin, oral hypoglycemic agents. With the simultaneous use of octreotide and bromocriptine, the bioavailability of the latter increases. Drugs metabolized with the participation of cytochrome P450 isoenzymes and having a narrow therapeutic dose range should be administered with caution.
Overdose
Symptoms: short-term heart rate, feeling of blood flow to the face, spastic abdominal pain, diarrhea, nausea, feeling of emptiness in the stomach.
Treatment: Symptomatic therapy is carried out if necessary.
Storage conditions
The drug should be stored in a dark place at a temperature of 8 ° to 25 РC.
Expiration
5 Chron
dosage form
dosage form
injection
Octreotide
Release form
Solution for injection
Packing
5 ampoules of 1 ml.
Pharmacological action
Octreotide is a synthetic analogue of somatostatin, which is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but a significantly longer duration of action. Octreotide suppresses the secretion of growth hormone, both pathologically increased and caused by arginine, physical activity and insulin hypoglycemia. The drug also inhibits the secretion of insulin, glucagon, gastrin, serotonin, both pathologically increased and caused by food intake, also inhibits the secretion of insulin and glucagon, stimulated by arginine. Octreotide suppresses the secretion of thyrotropin, caused by thyroliberin. Unlike somatostatin, octreotide inhibits the secretion of growth hormone to a greater extent than insulin secretion, and its administration is not accompanied by subsequent hypersecretion of hormones (for example, growth hormone in patients with acromegaly).
In patients with acromegaly, octreotide reduces the concentration of growth hormone and insulin-like growth factor (IGF-1) in blood plasma. A decrease in the concentration of growth hormone by 50% or more is observed in 90% of patients, while a concentration of growth hormone of at least 5 ng / ml is achieved in about half of the patients. In most patients with acromegaly, octreotide reduces the severity of headache, soft tissue swelling, hyperhidrosis, joint pain and paresthesia. In patients with large pituitary adenomas, treatment with octreotide can lead to some reduction in tumor size.
In case of secreting tumors of the gastroenteropancreatic endocrine system in cases of insufficient effectiveness of the therapy (surgery, embolization of the hepatic artery, chemotherapy, including streptozotocin and fluorouracil), the administration of octreotide can lead to an improvement in the course of the disease. So, with carcinoid tumors, the use of octreotide can lead to a decrease in the severity of sensations of flushing of the face, diarrhea, which in many cases is accompanied by a decrease in the concentration of serotonin in the plasma and excretion of 5-hydroxyindoleacetic acid by the kidneys. In tumors characterized by hyperproduction of a vasoactive intestinal peptide (VIPoma), the use of octreotide in most patients leads to a decrease in severe secretory diarrhea and, accordingly, an improvement in the quality of life of the patient. At the same time, there is a decrease in concomitant disturbances in the electrolyte balance, for example, hypokalemia, which allows you to cancel the enteral and parenteral administration of fluid and electrolytes. In some patients, the progression of the tumor slows down or stops, and its size and the size of the liver metastases decrease. Clinical improvement is usually accompanied by a decrease in the concentration of vasoactive intestinal peptide (VIP) in plasma or its normalization. With glucagonomas, the use of octreotide leads to a decrease in migratory erythema. Octreotide does not have any significant effect on the severity of hyperglycemia in diabetes mellitus, while the need for insulin or oral hypoglycemic drugs usually remains unchanged. The drug causes a decrease in diarrhea, which is accompanied by an increase in body weight. Although the decrease in plasma glucagon concentration under the influence of octreotide is transient in nature, clinical improvement remains stable throughout the entire period of drug administration. In patients with gastrinomas / Zollinger-Ellison syndrome, when octreotide is used as monotherapy or in combination with proton pump inhibitors or H2 histamine receptor blockers, a decrease in hypersecretion of hydrochloric acid in the stomach, a decrease in the concentration of gastrin in the blood plasma, as well as a decrease in the severity of diarrhea and hot flashes . In patients with insulinomas, octreotide reduces the level of immunoreactive insulin in the blood (this effect can be short-term - about 2 hours). In patients with operable tumors, octreotide can ensure the restoration and maintenance of normoglycemia in the preoperative period. In patients with inoperable benign and malignant tumors, glycemic control may improve without a simultaneous prolonged decrease in blood insulin levels.
In patients with rare tumors that hyperproduce growth hormone releasing factor (somatoliberinomas), octreotide reduces the severity of acromegaly symptoms. This is due to the suppression of secretion of the releasing factor of growth hormone and growth hormone itself. In the future, pituitary hypertrophy may decrease.
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 (e.g. sclerotherapy) leads to more effective stopping of bleeding and early rebleeding, reducing the volume of transfusions and improving 5-day survival. Believed that the mechanism of action of octreotide is associated with a decrease in organ blood flow through the suppression of vasoactive hormones such as VIP and glucagon.
Pharmacokinetics
Absorption
After s / c administration, octreotide is rapidly and completely absorbed. Tmax of octreotide in plasma - within 30 minutes.
Distribution of
Communication with plasma proteins is 65%. Linking Octreotide to Shaped Elblood counts very little. Vd is 0.27 L / kg.
Excretion of
T1 / 2 after sc administration of octreotide is 100 min. After iv administration, the excretion of octreotide is carried out in 2 phases, with T1 / 2 - 10 and 90 minutes, respectively. Most of octreotide is excreted through the intestines, about 32% - unchanged by the kidneys. The total clearance is 160 ml / min.
Indications
prevention and treatment of complications after operations on the pancreas and gastroduodenal zone
stopping bleeding and prevention of rebleeding from varicose veins of the esophagus in patients with cirrhosis (as part of complex therapy)
treatment of acute pancreatic ulcer disease stomach and duodenum.
Contraindications
Hypersensitivity to octreotide or other components of the drug children under 18 years of age.
Precautions: cholelithiasis (gallstone disease) diabetes mellitus.
Pregnancy and lactation
Experience with octreotide in pregnant women is limited. The drug Octreotide should be used during pregnancy only if if the intended benefit to the mother outweighs the potential risk to the fetus.
It is not known whether the drug passes into breast milk, so if you use the drug during lactation, you should refuse to breast-feed.
Composition
1 ml injection contains:
Active ingredient: octreotide
Excipients: sodium chloride, water d / i.
Dosage and administration
Intravenously (as infusion), subcutaneously.
In the treatment of acute pancreatitis, Octreotide® FSynthesis is administered subcutaneously at a dose of 100 mcg 3 times a day for 5–7 days. It is possible to prescribe up to 1200 μg / day, the selection of the dose is based on the determination of the concentration of amylase, lipase, inflammatory blood cytokines.
For the prevention of complications after pancreatic surgery, the first dose of Octreotide® FSynthesis 100 μg is administered s.c. 1 hour before laparotomy, then after the operation, s / cpo 100 μg is administered 3 times a day for 7 consecutive days.
To stop bleeding from varicose veins of the esophagus, the drug is administered iv in a dose of 25 mcg / h in the form of continuous infusions for 5 days.
To stop bleeding with gastric ulcer and duodenal ulcer, it is recommended to administer Octreotide® FSynthesis in the form of iv infusion at a dose of 25 mcg / h for 5 days.
Elderly patients do not need to reduce the dose of Octreotide® FSynthesis.
Patients with impaired renal function correction of the dosage regimen of octreotide is not required.
In patients with impaired liver function, a maintenance dose adjustment is recommended because there is evidence of an increase in T1 / 2 octreotide in patients with cirrhosis.
Experience with octreotide in children is very limited.
Rules for the preparation and administration of the
solution To reduce the symptoms of discomfort at the injection site, the Octreotide® FSynthesis solution must be at room temperature before administration. With s / c administration of the drug, several injections at the same place should be avoided at short intervals. Ampoules with the drug should be opened immediately before administration, the unused amount of the solution must be destroyed.
Before iv use of the drug, you should carefully examine the solution and make sure it is transparent, there are no suspended particles, sediment, and color changes. You can not use the drug if it is cloudy, contains suspended particles, sediment.
The prepared Octreotide® FSynthesis solution maintains physical and chemical stability at a temperature of 8 to 25 РC for 24 hours. To avoid microbial contamination, diluted solutions must be used immediately after preparation. If the solution is not to be used immediately, it should be stored at a temperature of 2 to 8 РC until its use.
Hold the solution at room temperature before use.
The total time between dilution, storage in the refrigerator and the end of the solution should not exceed 24 hours.
Preparation of a solution for iv drip
The contents of one ampoule containing 500 μg of octreotide, diluted in 60 ml of 0.9% sodium chloride solution. The infusion is repeated with the necessary frequency in accordance with the recommended duration of treatment. Octreotide can also be administered at lower concentrations.
Side effects
Local reactions: pain may occur at the injection site, sensation of itching or burning, redness and swelling (usually go away within 15 minutes).
From the gastrointestinal tract, pancreas, liver and gall bladder: possible - anorexia, nausea, vomiting, spastic abdominal pain, sensation of bloating, excessive gas formation, loose stools, diarrhea and steatorrhea. Although the excretion of fat with feces may increase, there is no indication that prolonged treatment with octreotide may lead to the development of malabsorption (malabsorption). In rare cases, phenomena resembling acute intestinal obstruction (progressive bloating, severe pain in the epigastric region, tension of the abdominal wall) can be noted.
Prolonged use of octreotide can lead to gallstones.
Certain cases of acute hepatitis without cholestasis are known (transaminase values normalize after cancellation of octreotide), as well as hyperbilirubinemia in combination with increased activity of alkaline phosphatase, GGT, and to a lesser extent other transaminases.
There are some reports of rare cases of acute pancreatitis, which developed in the first hours or days of the use of octreotide.
From the CCC: in some cases - tachycardia, bradycardia.
From the side of carbohydrate metabolism: impaired glucose tolerance after eating is possible (octreotide has an overwhelming effect on the formation of GR, glucagon and insulin), hypoglycemia in rare cases with prolonged treatment may develop persistent hyperglycemia.
Other: rarely - allergic reactions, alopecia in some cases - anaphylactic reactions.
Drug Interaction
Octreotide reduces the absorption of cimetidine, cyclosporine, diuretics, beta-blockers, calcium antagonists, insulin, oral hypoglycemic agents. With the simultaneous use of octreotide and bromocriptine, the bioavailability of the latter increases. Drugs metabolized with the participation of cytochrome P450 isoenzymes and having a narrow therapeutic dose range should be administered with caution.
Overdose
Symptoms: short-term heart rate, feeling of blood flow to the face, spastic abdominal pain, diarrhea, nausea, feeling of emptiness in the stomach.
Treatment: Symptomatic therapy is carried out if necessary.
Storage conditions
The drug should be stored in a dark place at a temperature of 8 ° to 25 РC.
Expiration
5 Chron
dosage form
dosage form
injection
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