SANDOSTATIN AMPOULES 0.1MG 1ML

Dosage form

Injection

Packaging

5 amp. on 1 ml.

Mechanism of action

Sandostatin is a synthetic octapeptide that is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but a much longer duration of action.

Sandostatin inhibits the secretion of growth hormone (GH), both pathologically increased, and caused by arginine, exercise and insulin hypoglycemia. The drug also suppresses the secretion of insulin, glucagon, gastrin, serotonin, both pathologically increased, and caused by food intake; also inhibits the secretion of insulin and glucagon, stimulated by arginine. Sandostatin inhibits the secretion of thyrotropin, 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).

In patients with acromegaly, Sandostatin reduces the concentration of GH and 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 value of the concentration of GH 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.

When secreting endocrine tumors of the gastrointestinal tract and pancreas in cases of insufficient efficacy of therapy (surgery, embolism of the hepatic artery, Chemotherapy, including streptozotocin and 5-fluorouracil), Sandostatin may improve the course of the disease. Thus, with carcinoid tumors, the use of Sandostatin helps to reduce the severity of the sensation of hot flashes to the face, diarrhea, which in many cases is accompanied by a decrease in plasma serotonin concentration and 5-hydroxyindolecetic acid excretion with urine. For tumors characterized by hyperproduction of vasoactive intestinal peptide (VIPomas), the use of Sandostatin 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 Sandostatin reduces the erythema migrans. Sandostatin has no 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 Sandostatin 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 Sandostatin as monotherapy or in combination with proton pump inhibitors or histamine H2 receptor blockers, it is possible to decrease the hypersecretion of hydrochloric acid in the stomach, decrease the concentration of gastrin in the blood plasma, as well as decrease the severity of diarrhea and tides

In patients with insulinomas, Sandostatin reduces the level of immunoreactive insulin in the blood (this effect may be short-term - about 2 hours). In patients with operable tumors, Sandostatin 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 the level of insulin in the blood.

In patients with rare tumors that hyperproduce the releasing factor of growth hormone (somatoliberinomas), Sandostatin reduces the severity of the symptoms of acromegaly. This is due to the suppression of secretion of the releasing factor of growth hormone and the growth hormone itself. In the future, the pituitary hypertrophy may decrease.

With refractory diarrhea in patients with AIDS, the use of Sandostatin results in complete or partial normalization of stool in approximately one third of patients suffering from diarrhea that are not controlled by adequate antimicrobial therapy and / or antidiarrheals.

In patients who are scheduled for surgery on the pancreas, the use of Sandostatin during and after the operation reduces the incidence of typical postoperative complications (for example, pancreatic fistulas, abscesses, sepsis, postoperative acute pancreatitis).

When bleeding from varicose veins of the esophagus and stomach in patients with liver cirrhosis, the use of Sandostatin in combination with specific treatment (for example, sclerotherapy) leads to more effective hemostasis and early re-bleeding, reducing the volume of transfusions and improving 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.

Indications and usage

Acromegaly:
- To control the main manifestations of the disease and reduce the levels of GH and IGF-1 in plasma in cases where there is no sufficient effect from surgical treatment or radiation therapy.
- Treatment of patients with acromegaly, abandoning the operation or having contraindications to it, as well as for short-term treatment in the intervals between courses of radiation therapy until its effect is fully developed.

Carcinoid tumors with carcinoid syndrome.
- VIPomas.
- Glucagonomas.
- Gastrinomas / Zollinger-Ellison syndrome - usually in combination with proton pump inhibitors and histamine H 2 -receptor blockers.
- Insulinoma (to control hypoglycemia in the preoperative period, as well as for maintenance therapy).
- Somatoliberinomas (tumors characterized by overproduction of growth hormone releasing factor).

Contraindications

Hypersensitivity to the drug.

Pregnancy and Breastfeeding

Experience with Sandostatin in pregnant women and nursing mothers is limited, so this category of patients is prescribed the drug only if the intended benefit to the mother outweighs the potential risk to the fetus or infant.

Dosage and administration

For acromegaly, the drug is initially administered at 50-100 mcg sc with 8 or 12 h intervals. Further dose adjustment should be based on monthly determinations of the concentration of GH and IGF-1 in the blood (target concentration: GH <2.5 ng / ml; IGF- 1 within normal values), analysis of clinical symptoms and tolerability of the drug. In most patients, the optimal daily dose is 300 micrograms. Do not exceed the maximum dose of 1.5 mg / day. In patients receiving a stable dose of Sandostatin, determination of the concentration of GH should be carried out every 6 months. If, after 3 months of treatment with Sandostatin, there is not a sufficient decrease in the level of growth hormone and an improvement in the clinical picture of the disease, the therapy should be stopped.

For endocrine tumors of the gastrointestinal tract and pancreas, the drug is injected s / c at an initial dose of 50 mcg 1-2 times / day. In the future, depending on the achieved clinical effect, the effect on hormone levels produced by the tumor (in the case of carcinoid tumors, the effect on the release of 5-hydroxyindole acetic acid in the urine) and tolerability, the dose can be gradually increased to 100-200 mg 3 times / day. In exceptional cases, higher doses may be required. Maintenance doses of the drug should be selected individually. For carcinoid tumors, if Sandostatin therapy at the maximum tolerated dose for 1 week was not effective, treatment should not be continued.

With refractory diarrhea in AIDS patients, the drug is injected s / c in the initial dose of 100 mg 3 times / day. If, after 1 week of treatment, diarrhea does not subside, the dose of the drug should be increased individually, up to 250 mg 3 times / day. Dose adjustment is carried out taking into account the dynamics of stool and tolerability of the drug. If during the week of treatment with Sandostatin in a dose of 250 mcg 3 times / day there is no improvement, therapy should be stopped.

To prevent complications after operations on the pancreas, subcutaneous doses of 100 mcg 3 times / day are administered for 7 consecutive days, starting from the day of surgery (at least 1 hour before laparotomy).

When bleeding from varicose veins of the esophagus and stomach, the drug is administered at a dose of 25 mcg / h by continuous IV infusion for 5 days. Sandostatin can be diluted with isotonic sodium chloride solution. Patients with cirrhosis of the liver with bleeding from esophageal varicose veins showed good tolerability of Sandostatin, which was applied for 5 days to 50 mcg / h as a continuous IV infusion.

Application in violation of liver function: In patients with impaired liver function, maintenance dose adjustment is recommended, since there is evidence of an increase in T 1/2 octreotide in patients with liver cirrhosis.

Use in violation of renal function: In patients with impaired renal function, the correction of the dosage regimen Sandostatin is not required.

Use in elderly patients: Currently there are no data that would indicatethat elderly patients have reduced the tolerability of Sandostatin and require a change in dosage regimen.

Nausea, vomiting, anorexia, spastic abdominal pain, bloating, flatulence, loose stools, diarrhea and steatorrhea, symptoms of acute intestinal obstruction (progressive bloating, severe epigastric pain, pain and abdominal tension during palpation); abnormal liver function; the formation of gallstones (with prolonged use), acute pancreatitis, impaired postmentional glucose tolerance, hyperglycemia, hypoglycemia, hair loss. At the injection site - pain, itching or burning sensation, redness and swelling.

For pituitary tumors secreting GH, careful monitoring of patients receiving Sandostatin is necessary, since an increase in the size of tumors is possible with the development of such a serious complication as a narrowing of the visual fields. In these cases, the need for other treatments should be considered.

In the case of the development of bradycardia with the use of Sandostatin, it is necessary to reduce the dose of beta-blockers, Calcium channel blockers or drugs that affect the water-electrolyte balance.

In some patients, octreotide may alter the absorption of fat in the intestine. Against the background of the use of octreotide, there was a decrease in the content of cyanocobalamin (vitamin B 12) and abnormal indicators of the cyanocobalamin absorption test (Schilling test).

When Sandostatin is used in patients with vitamin B 12 deficiency in history, it is recommended to control the content of cyanocobalamin in the body.

In the treatment of endocrine tumors of the gastrointestinal tract and pancreas Sandostatin in rare cases may come a sudden recurrence of symptoms of the disease. Patients with insulinomas during treatment with octreotide may experience an increase in the severity and duration of hypoglycemia (this is due to a more pronounced suppressive effect on the secretion of GH and glucagon than on insulin secretion, as well as a shorter duration of inhibiting effect on insulin secretion). Careful regular monitoring of these patients should be ensured, both at the start of Sandostatin treatment and at each dose change. Significant fluctuations in the concentration of glucose in the blood can be tried to reduce by more frequent administration of Sandostatin in lower doses. In patients with type 1 diabetes, Sandostatin may reduce the need for insulin. In patients without diabetes mellitus and with type 2 diabetes with partially intact insulin secretion, administration of Sandostatin can lead to postprandial hyperglycemia. When using Sandostatin in patients with diabetes mellitus, it is recommended to monitor blood glucose and antidiabetic therapy.

Since after bleeding from esophageal and gastric varicose veins, the risk of developing type 1 diabetes mellitus is increased, and in patients with suffering from diabetes, it is also possible to change the need for insulin; in these cases, it is necessary to systematically control the concentration of glucose in the blood.

Correction of the dosing regimen of simultaneously used diuretics, beta-blockers, slow calcium channel blockers, insulin, oral hypoglycemic agents, glucagon is necessary.

Recommendations for the management of patients during treatment with Sandostatin regarding the formation of gallbladder stones
- Before the appointment of Sandostatin, patients should undergo an initial ultrasound examination of the gallbladder.
- During treatment with Sandostatin, repeated ultrasound examinations of the gallbladder should be carried out, preferably at intervals of 6-12 months.
- If gallbladder stones are detected even before treatment, it is necessary to evaluate the potential benefits of Sandostatin therapy compared with the possible risk associated with their presence. There is no evidence of any adverse effect of Sandostatin on the course or prognosis of an existing gallstone disease.
- Management of patients in whom gallbladder stones are formed during the treatment with Sandostatin.
- Asymptomatic gallbladder stones. The use of Sandostatin can be stopped or continued - in accordance with the assessment of the ratio of benefit / risk. In any case, there is no need to do anything other than continue observation, making it more frequent if necessary.
- Gallbladder stones with clinical symptoms. The use of Sandostatin can be stopped or continued - in accordance with the assessment of the ratio of benefit / risk. In any case, the patient should be treated in the same way as in other cases of gallstone disease with clinical manifestations. Drug treatment includes the use of combinations of drugs of bile acids (for example, chenodeoxycholic acid at a dose of 7.5 mg / kg per day in combination with ursodeoxycholic acid at the same dose) under ultrasound control until the stones disappear completely.

In the dark place at a temperature of 4-10 ° C.