Solution for iv and sc administration.
In an ampoule of 1 ml of solution. In a cardboard package 5 ampoules.
Sandostatin is a synthetic octapeptide that is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but a significantly longer duration of action. Sandostatin inhibits the secretion of growth hormone (GH), as pathologically increased, and caused by arginine, exercise 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. Sandostatin inhibits thyrotropin secretion caused by thyroliberin.
Unlike somatostatin, octreotide suppresses the secretion of GH to a greater extent than the secretion of insulin, and its administration is not accompanied by subsequent hypersecretion of hormones (for example, GH in patients with acromegaly).
In patients with acromegaly, Sandostatin reduces the concentration of GR and insulin-like growth factor (IGF-1) in blood plasma. A decrease in the concentration of GR by 50% or more is observed in 90% of patients, while the concentration of GR less than 5 ng / ml is achieved in about half of the patients. In most patients with acromegaly, Sandostatin reduces the severity of headache, soft tissue swelling, hyperhidrosis, joint pain and paresthesia. In patients with large pituitary adenomas, treatment with Sandostatin may lead to some reduction in tumor size.
In case of secreting endocrine tumors of the gastrointestinal tract and pancreas in cases of insufficient effectiveness of the therapy (surgery, hepatic artery embolism, chemotherapy, including streptozotocin and 5-fluorouracil), the appointment of Sandostatin can improve the course of the disease. So, with carcinoid tumors, the use of Sandostatin helps to reduce 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 plasma and excretion of 5-hydroxyindoleacetic acid in the urine. In tumors characterized by hyperproduction of a vasoactive intestinal peptide (VIPoma), the use of Sandostatin in most patients leads to a decrease in severe secretory diarrhea, and, accordingly, to an improvement in the patient’s quality of life. 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 decreases, as well as the size of the liver metastases. 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 Sandostatin leads to a decrease in migratory erythema. Sandostatin does not significantly affect 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 Sandostatin is transient in nature, clinical improvement remains stable throughout the entire period of use of the drug.
In patients with gastrinomas / Zollinger-Ellison syndrome, when using Sandostatin as a monotherapy or in combination with proton pump inhibitors or histamine H2 receptor blockers, it is possible to reduce hypersecretion of hydrochloric acid in the stomach, decrease the concentration of gastrin in the blood plasma, and also reduce the severity of diarrhea and tides.
In patients with insulinomas, Sandostatin reduces the level of immunoreactive insulin in the blood (this effect can be short-term – about 2 hours). In patients with operable tumors, Sandostatin can restore and maintain normoglycemia in the preoperative period. In patients with inoperable benign and malignant tumors, glycemic control may improve without a simultaneous prolonged decrease in blood insulin levels.
In patients with rare tumors, hyperproducing growth hormone releasing factor (somatoliberinomas), Sandostatin 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.
With refractory diarrhea in patients with AIDS, the use of Sandostatin leads to complete or partial normalization of stool in about 1/3 of patients suffering from diarrhea that is not controlled by adequate antimicrobial and / or antidiarrheal therapy.
In patients who are scheduled for pancreatic surgery, the use of Sandostatin during and after surgery reduces the incidence of typical postoperative complications (e.g., pancreatic fistula, abscesses, sepsis, postoperative acute pancreatitis).
When bleeding from varicose veins of the esophagus and stomach in patients with cirrhosis of the liver, the use of Sandostatin in combination with specific treatment (for example, sclerotherapy) leads to a more effective stop of bleeding and early rebleeding, reduce transfusion volume and improve 5-day survival. It is believed that the mechanism of action of Sandostatin is associated with a decrease in organ blood flow through the suppression of such vasoactive hormones as VIP and glucagon.
After s / c administration, Sandostatin is rapidly and completely absorbed. Cmax of octreotide in plasma is reached within 30 minutes.
Plasma protein binding is 65%. The binding of Sandostatin to blood cells is extremely negligible. Vd is 0.27 L / kg.
T1 / 2 after sc injection of the drug is 100 min. After iv administration, the drug is excreted in 2 phases, with T1 / 2 10 and 90 minutes, respectively. Most of the drug is excreted in feces, about 32% – unchanged in urine. The total clearance is 160 ml / min.
Acromegaly: to control the main manifestations of the disease and reduce the levels of GR and IGF-1 in plasma in cases where there is no sufficient effect of surgical treatment or radiation therapy
treatment of patients with acromegaly who have refused surgery or have contraindications to it, and also for short-term treatment in the intervals between courses of radiation therapy until its effect is fully developed.
Secreting endocrine tumors of the gastrointestinal tract and pancreas – for symptom control: carcinoid tumors with carcinoid syndrome
gastrinoma / Zollinger-Ellison syndrome – usually in combination with inhibitors of the proton-influenza group 2 in the preoperative period, as well as for maintenance therapy)
somatoliberinomas (tumors characterized by overproduction of growth hormone releasing factor).
Sandostatin is not an antitumor drug and its use cannot lead to the cure of this category of patients.
Control of symptoms of refractory diarrhea in AIDS patients.
Prevention of complications after pancreatic surgery.
Stopping bleeding and preventing recurrence of bleeding from varicose veins of the esophagus and stomach in patients with cirrhosis. Sandostatin is used in combination with specific therapeutic measures, for example, endoscopic sclerotherapy.
Pregnancy and lactation
Experience with Sandostatin in pregnant women and nursing mothers is limited, therefore, this category of patients is prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus or infant.
1 ml of solution contains:
Active substances: octreotide (in the form of a free peptide) 100 mcg.
Excipients: lactic acid, mannitol, sodium bicarbonate, carbon dioxide, water d / i.
Dosage and administration of