Octreotide Injection Ampoule 0.01% 1ml N5
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Description
Octreotide is a synthetic analogue of somatostatin, which is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but a much longer duration of action. Octreotide inhibits 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, gastrin, serotonin, both pathologically increased, and caused by food intake, also inhibits the secretion of insulin and glucagon, stimulated by arginine.
Active ingredients
Octreotide
Pharmacological effect
Octreotide is a synthetic analogue of somatostatin, which is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but a much longer duration of action. Octreotide inhibits the secretion of growth hormone (GH), both pathologically elevated, 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 inhibits the secretion of insulin and glucagon, stimulated by arginine. Octreotide suppresses thyrootropin secretion caused by thyroliberin. Unlike somatostatin, octreotide suppresses GH secretion to a greater extent than insulin secretion, and its administration is not accompanied by subsequent hypersecretion of hormones (for example, GH in patients with acromegaly). insulin-like growth factor (IGF-1) in plasma. A decrease in the concentration of GH by 50% or more is observed in 90% of patients, while the concentration of GH is not less than 5 ng / ml is reached 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 may lead to some reduction in tumor size. For secreting tumors of the gastroenteropancreatic endocrine system in cases of insufficient efficacy of therapy (surgery, embolization of the hepatic artery, chemotherapy, including streptozototsinom and fluorouracil, purpose of surgery, embolization of the hepatic artery, chemotherapy, including streptozototsinom and fluorouracil, purpose of surgery, embolization of the hepatic artery, chemotherapy, including streptozototsinom and fluorouracil, purpose of surgery, embolization of the hepatic artery, chemotherapy, including streptozototsinom and fluorouracil, purpose of surgery, embolization of the hepatic artery, chemotherapy, including streptozototsinom and fluorouracil, purpose of surgery, embolization of the hepatic artery, chemotherapy, including streptozototsinom and fluorouracil, purpose of surgery, chemotherapy, including streptozotocin and fluorouracil, purpose of surgery lead to an improvement in the course of the disease.Thus, in case of carcinoid tumors, the use of octreotide can lead to a decrease in the severity of the sensation of hot flashes to the face, diarrhea, which in many cases is accompanied by a decrease in serotonin concentration in plasma and the excretion of 5-hydroxyindolecetic acid by the kidneys. For tumors characterized by hyperproduction of vasoactive intestinal peptide (VIPomas), the use of octreotide in most patients reduces severe secretory diarrhea and, consequently, improves the quality of life of the patient. At the same time, there is a decrease in concomitant electrolyte imbalances, for example, hypokalemia, which allows you to cancel enteral and parenteral administration of fluid and electrolytes. In some patients, the progression of the tumor slows down or stops, its size decreases, as well as the size of metastases to the liver. Clinical improvement is usually accompanied by a decrease in plasma concentration of the vasoactive intestinal peptide (VIP) or its normalization. With glucagonomas, the use of octreotide leads to a decrease in migrating 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 the concentration of glucagon in the blood plasma under the influence of octreotide is transient in nature, clinical improvement remains stable during the entire period of use of the drug. In patients with gastrinomas / Zollinger-Ellison syndrome, when using octreotide as monotherapy or in combination with proton pump inhibitors or H2-histamine receptor blockers, hypersecretion of hydrochloric acid in the stomach may decrease, plasma concentrations of gastrin may decrease, and diarrhea and tides may be reduced . In patients with insulinoma, octreotide reduces the level of immunoreactive insulin in the blood (this effect may 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 can be improved even without simultaneously reducing blood insulin levels. In patients with rare tumors that hyperproduce releasing growth factor hormone (somatoliberinomas), octreotide reduces the severity of acromegaly symptoms. This is due to the suppression of secretion of the releasing factor of growth hormone and the growth hormone itself. Hypertrophy of the pituitary can be further reduced. When bleeding from varicose veins of the esophagus and stomach in patients with liver cirrhosis, using octreotide in combination with specific treatment (for example, sclerotherapy) results in more effective hemostasis and early rebleeding, reduction in transfusions and improvement 5-day survival. It is believed that the mechanism of action of octreotide is associated with a decrease in organ blood flow through the suppression of such vasoactive hormones as VIP and glucagon.
Pharmacokinetics
Suction. After s / c administration, octreotide is rapidly and completely absorbed. Cmax of octreotide in plasma is achieved within 30 minutes. Distribution. Communication with proteins of a blood plasma makes 65%. The binding of octreotide with the formed elements of blood is extremely insignificant. The Vd is 0.27 l / kg. Excretion. T1 / 2 after s / c administration of octreotide is 100 minutes. After intravenous injection, octreotide elimination is carried out in 2 phases, with T1 / 2 - 10 and 90 min, respectively. Most of the octreotide is excreted through the intestines, about 32% - unchanged by the kidneys. Total clearance is 160 ml / min.
Indications
- Treatment of acute pancreatitis, - Stopping bleeding in gastric ulcer and duodenal ulcer, - Stopping bleeding and preventing re-bleeding from esophageal varicose veins in patients with cirrhosis of the liver, - Prevention and treatment of complications after operations on the abdominal cavity.
Dosage and administration
For the treatment of acute pancreatitis, the drug is injected s / c at a dose of 100 mcg 3 times / day for 5 days. You can assign up to 1200 mcg / day using the / in the route of administration. To stop ulcerative bleeding, it is injected intravenously at a dose of 25-50 mcg / h as an intravenous infusion for 5 days. To stop bleeding from esophageal varices administered intravenously in a dose of 25–50 mcg / h in the form of prolonged intravenous infusions for 5 days. In elderly patients there is no need to lower the dose of Octreotide. To prevent complications after operations on the pancreas, the first dose of 100–200 mcg is administered s / c for 1-2 hours before laparotomy,then, after the operation, SCs are administered at 100–200 mcg 3 times / day for 5–7 consecutive days.