What the somatostatin hormone and its synthetic analogues are responsible for. Somatostatin: instructions for use Somatostatin hormone action

Somatostatin is one of the peptide hormones, the presence of which was first recorded in hypothalamic cells. And only after some time this element was identified in other tissues of the body.

By their name, somatostatins are similar to. However, these are not the same concept, and there are a number of differences between these substances. What kind of substance is this, and why is it important for human health?

Features and functions of the hormone somatostatin

Somatostatin is a hormonal element that is produced mainly by the pancreas, Langers cells. If their work is disrupted, intense or, conversely, decreased secretion of the substance occurs, entailing serious consequences for the entire body.

Composition, place of production

The hormone somatostatin is a rather complex protein compound. It contains more than 50 amino acids, and its mechanism of action affects not only the digestive system, but also the hematopoietic system.

The production of somatostatin occurs not only in the cells of the pancreas, although this is the main site of its synthesis. In addition to the pancreatic organ, the following are responsible for the secretion of this element:

• hypothalamus;
• some parts of the digestive tract;
• tissues of the nervous system.

But the fact that somatostatin is also produced by the cells of these parts of the body was recorded much later after its secretion from the pancreas was discovered.

Main functions of the substance

The functions of somatostatin are quite diverse and extensive. First of all, they are:

• decrease;
• slowing down blood flow in the abdominal organs;
• inhibition of intestinal motility.

That's not all. The functions of the hormone somatostatin are also aimed at inhibiting the production and suppressing the excessive activity of some other biologically active substances:

• insulin;
• somatomedin-C;
• cholecystokinin;
• vasoactive intestinal peptide.

Somatostatin affects the growth hormone somatotropin. In particular, it inhibits (suppresses) its production, due to which normal, full formation of the body occurs.

Remarkable. Among other things, somatostatin has a function that is to selectively regulate the functioning of the central nervous system. In particular, this substance contributes to the formation of human behavioral characteristics, affects memory and motor activity. In addition, the hormonal element can influence the endocrine and autonomic systems.

This is the biochemistry of somatostatin. This protein hormone is widely used in medical practice to treat various diseases. Based on it, medications are manufactured that are used both in gastroenterological and endocrine practice.

What is somatostatinoma?

Elevated levels of somatostatin can lead to the development of such a dangerous disease as somatostatinoma. This is a hormonally active tumor of the pancreas, in which there is a significant decrease in insulin and glucagon levels.

The first symptoms of the disease appear:

• dyspepsia;
• diarrhea;
• anemia;
• sudden and causeless weight loss;
• hypochlorhydria;
• the so-called inhibitory syndrome.

Somatostatinoma rarely occurs in isolation - it is usually accompanied by:

• diabetes mellitus;
• cholelithiasis;
• steatorrhea.

The danger of this tumor lies in the fact that it is diagnosed, as a rule, already in an advanced form. When it is large in size and metastasizes to other internal organs. As a rule, metastases affect the liver.

The prognosis for life with somatostatinoma is relatively favorable. In the presence of metastases, in 30–60% of cases, patients manage to live another 5 years. In the absence of metastases, survival rate is almost 100%.

The only treatment for such a tumor is its surgical removal. Sometimes doctors manage to achieve regression of metastases using the drug Streptozotocin and similar drugs.

Somatostatin drugs and their analogues

Somatostatin is used in medical practice to treat various diseases. Scientists were able to synthesize it for use in gastroenterology and endocrinology.

In the first case, the drug somatostatin is used in the treatment of bleeding in the gastrointestinal tract. In addition, its use is advisable when the patient has undergone surgical interventions in the pancreas. And this is understandable, since the operation causes a temporary disruption of hormonal release in this organ. And if we are talking about removing part of the pancreas, then the medicine can be prescribed for a long period of time, or even for life.

In endocrinological practice, somatostatin analogues are mainly used. This approach to therapy is explained by the fact that such drugs have a prolonged effect on the body. It is advisable to prescribe them for the treatment of gigantism, acromegaly, and diabetic coma.

Release form, application features

Preparations based on synthetic somatostatin are produced in the form of a powder for the preparation of a solution. The medication is prepared by mixing the powder with a solution of 0.9% sodium chloride (saline).

The medicinal product is intended exclusively for injection use. It is administered mainly intravenously.

Such drugs should not be used by women during gestation or if pregnancy is suspected, with hypersensitivity to the components of the solution and a tendency to allergic reactions to hormonal drugs of this kind. Also, the solution is not administered to breastfeeding mothers and patients in the postpartum period.

Indications for use

Somatostatin and its generics (analogues), in addition to the previously mentioned pathologies, can be used to treat:

• neoplasms of the pancreas and other gastrointestinal tract organs;
• carcinoids;
• severe diarrhea in patients with HIV infection;
• arterial bleeding of the esophagus;
• peptic ulcer;
• acute inflammation of the pancreas.

In the postoperative period, in addition to HRT, somatostatin is used to prevent the development of complications. This is especially important if the intervention was extremely serious or difficulties arose during it.

Somatostatin analogues are drugs from the list below:

• Octreodite;
• Modustatin;
• Stylamine.

Important! It should be borne in mind that neither Somatostatin nor its analogues can be used for self-medication! Even if the patient managed to “obtain” the medicine despite the ban on its over-the-counter sale, one should not get carried away with its use. Uncontrolled use of such medications can cause a number of side effects, and if dosed incorrectly, lead to severe disruptions in the functioning of the entire body!

Somatostatin, also known as growth hormone inhibitory hormone (GHIH), is produced by many tissues in the human body, mainly the nervous and digestive systems.

A hormone is a peptide substance that regulates the endocrine system.

Instructions for use of synthesized somatostatin describe it as a hormone that has a wide spectrum of effects on various organs and systems of the body.

Somatostatin is a peptide (containing amino acids) hormone that regulates a wide range of physiological functions, acting by inhibiting (slowing) the release of growth hormone from the anterior pituitary gland.

Somatostatin also inhibits the release of thyroid-stimulating hormone (thyrotropin, TSH) and adrenocorticotropic hormone (corticotropin, ACTH) from the pituitary gland, and the hormones glucagon and insulin from the pancreas.

Somatostatin regulates gastric and duodenal secretion. The hormone may also act as a neurotransmitter in the nervous system and play a role in pain perception.

The biologically active release of somatostatin occurs in two molecular forms - somatostatin-14 and somatostatin-28. Both of these hormones are products of post-translational processing of preprohormones (their precursors).

In the human body there are three organs responsible for the production of the hormone somatostatin:

1. gastrointestinal tract;
2. hypothalamus;
3. islets of Langerhans in the pancreas.

The hypothalamus is the area of ​​the brain that regulates the secretion of hormones from the pituitary gland, located beneath it.

Somatostatin produced in the hypothalamus, inhibits the secretion of pituitary growth hormone, as well as thyroid-stimulating hormone (TSH), which stimulates the production of the hormones T3 and T4, which are responsible for energy metabolism in the body.

Somatostatin produced by the pancreas, inhibits the secretion of its other hormones, such as insulin and glucagon. Somatostatin is also secreted by the pancreas in response to a variety of food-related factors, such as high levels of glucose and amino acids in the blood.

Somatostatin produced in the gastrointestinal tract paracrine cells located throughout the organ, acts locally, reducing gastric secretion, gastrointestinal motility and slowing the secretion of gastrointestinal hormones, including gastrin and secretin.

Indications and contraindications

Chemical equivalents of somatostatin are used in medical practice as medical therapy to control excessive hormonal secretion in acromegaly and other endocrine diseases and for the treatment of certain gastrointestinal pathologies (including neoplasms).

Because somatostatin regulates many physiological processes in the body, too little of this hormone can lead to a variety of problems, including too much growth hormone secretion (acromegaly).

The drug is also used for:

• bleeding due to varicose veins of the esophagus;
• bleeding of the stomach or duodenum;
• hemorrhagic gastritis;
• intestinal and pancreatic fistulas;
• hypersecretion of endocrine tumors of the gastrointestinal tract;
• to reduce the level of complications after pancreatic surgery;
• adjuvant therapy for diabetic ketoacidosis.

The use of somatostatin in acromegaly is somewhat limited. The drug is widely used to treat pituitary and neuroendocrine tumors.

The use of the drug is contraindicated during pregnancy, lactation, as well as in case of hypersensitivity to any of its components.

Caution should be exercised when taking this medication through monitoring blood glucose levels.

Side effects

Excessive levels of somatostatin in the blood lead to a sharp decrease in the secretion of many endocrine hormones.

An example of this is the suppression of insulin secretion from the pancreas, which leads to increased blood glucose levels and the risk of developing diabetes.

Because somatostatin inhibits many functions of the gastrointestinal tract, excessive levels can also lead to the formation of gallstones, dietary fat intolerance, and diarrhea.

Method and dosage

Somatostatin is available under various brands in the form of solutions of various concentrations for injection.

The usual dosage for the treatment of cavitary bleeding due to portal hypertension (high blood pressure syndrome in the portal vein system) is 250 mcg as a bolus injection over 3-5 minutes, followed by a continuous infusion of 3.5 mcg/kg/h until the bleeding stops.

For acromegaly, the dosage used is 30-60 mg in the form of intramuscular injections.

An initial rapid release of the drug is observed 1-2 hours after injection, followed by a prolonged exacerbation phase two days later. The half-life is 5.2 BB ± 2.5 days, the bioavailability of the drug in this case is 30-60%.

Take somatostatin only as directed by your doctor. The dosage of the drug depends on age, health status and the body's response to treatment.

Somatostatin-based medications should be taken regularly to obtain maximum therapeutic benefit. To do this, it is best to take somatostatin at the same time.

Overdose

In case of an overdose of the drug, specific reactions are possible:

• nausea;
• hyperemia (overflow of blood in the blood vessels of any organ);
• bradycardia (sinus rhythm disturbances, or sinus arrhythmia).

Interaction

While taking somatostatin, you should not stop taking or change the dosage of any medicine you are taking without your doctor's approval.

Interaction of somatostatin with Hexabarbitone and other drugs is possible.

When taking somatostatin, keep a list of all prescription and over-the-counter medications and herbal foods on hand in case any unexpected reactions occur to report to your healthcare provider.

Somatostatin occupies a prominent place in therapeutic gastrointestinal endocrinology.

The development of synthetic analogues of this drug has led to the possibility of treating many clinical disorders, including acromegaly, hormone-secreting tumors of the gastrointestinal tract, and bleeding from portal hypertension.

Given the wide spectrum of action of this hormone, it is not surprising that it is the subject of modern scientific research and its active use in various clinical areas.

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Name:

Somatostatin

Pharmachologic effect:

A synthetic 14-amino acid peptide, similar in structure and action to natural somatostatin.

Somatostatin prevents the release of gastrin (a protein secreted by the gastric mucosa, which causes an increase in the secretion of digestive juices by the stomach and pancreas), gastric juice, pepsin (an enzyme that destroys proteins) and reduces both endocrine and exocrine secretion of the pancreas (the release of hormones and digestive juices), including suppressing the secretion of glucagon (a pancreatic hormone that stimulates the secretion of insulin), which explains the positive effect of the drug in diabetic ketoacidosis (acidification due to excess ketone bodies in the blood). It also prevents the release of growth hormone. In addition, somatostatin significantly reduces the volume of blood flow in the internal organs without causing significant fluctuations in systemic blood pressure.

Indications for use:

Severe acute bleeding in case of gastric or duodenal ulcer, acute bleeding from esophageal varices (altered veins characterized by nodular protrusion), severe acute bleeding in erosive “ulcerative gastritis (chronic inflammation of the stomach with the formation of mucosal defects and bleeding), auxiliary treatment fistulas (formed as a result of disease of the channels connecting hollow organs to each other or to the external environment) of the pancreas, biliary and intestinal fistulas, prevention of complications arising after surgical interventions on the pancreas, auxiliary treatment for diabetic ketoacidosis, diagnostic and research tests requiring suppression secretion of growth hormone, insulin, glucagon.

Method of application:

Somatostatin is administered intravenously - first, slowly in a stream over 3-5 minutes at a “shock” dose of 250 mcg, then switched to a continuous infusion at a rate of 250 mcg/h (which corresponds to approximately 3.5 mcg/kg/h). The active substance is diluted with the supplied solvent immediately before administration. To prepare a solution intended for infusion over 12 hours, use an ampoule containing 3000 mcg of the active substance. To dilute it, use an isotonic sodium chloride solution or a 5% glucose solution. The use of a perfusion syringe pump is recommended. A solution of somatostatin in an isotonic solution of potassium chloride preserves stability for 72 hours. The prepared solution of the drug is stored in the refrigerator.

For the treatment of severe acute bleeding from the upper gastrointestinal tract, including from esophageal varices, the drug is used as indicated above. If there is a break between two infusions of the drug exceeding 3-5 minutes (change of intravenous administration system or perfusion syringe), an additional slow intravenous infusion of somatostatin is performed at a dose of 250 mcg to ensure continuity of treatment. After the bleeding has stopped (usually this occurs in less than 12-24 hours), treatment with the drug is continued for 48-72 hours to avoid relapse (recurrence) of bleeding. Usually the total duration of treatment is up to 120 hours.

In the auxiliary treatment of pancreatic fistulas, biliary or intestinal fistulas, continuous administration of somatostatin is carried out simultaneously with total parenteral nutrition (bypassing the gastrointestinal tract). In this case, the dose of the drug is 250 mcg/hour. When the swish is closed, treatment with the drug is continued for 1-3 days and stopped gradually to avoid the “withdrawal” effect (deterioration in health after abrupt cessation of somatostatin).

To prevent complications after surgery on the pancreas, somatostatin is administered at the beginning of surgery at a rate of 250 mcg/hour and continued for 5 days.

In the auxiliary treatment of diabetic ketoacidosis, Grel&rat administers at a rate of 100-500 mcg/hour together with insulin (injection of a “loading” dose of 10 units and simultaneous injection at a rate of 1-4.9 units/hour). Normalization of glycemia (reduction of high blood sugar) occurs within 4 hours, and disappearance of acidosis (acidification) within 3 hours.

Adverse events:

Dizziness and a feeling of flushing of the face (very rare), nausea and vomiting (only at an injection rate above 50 mcg/min).

At the beginning of treatment, a temporary decrease in blood sugar levels is possible (due to the inhibitory / suppressive / effect of the drug on the secretion / release / of insulin and glucagon). Therefore, in patients with diabetes mellitus during this period, the blood glucose level is determined every 3-4 hours. At the same time, if possible, the intake of carbohydrates is excluded. If necessary, insulin is administered.

Contraindications:

Pregnancy, the period immediately following childbirth, breastfeeding, increased sensitivity to somatostatin.

Repeated courses of treatment with the drug should be avoided in order to minimize the possibility of sensitization (hypersensitivity to the drug).

Release form of the drug:

Dry substance for injection in ampoules of 250 and 3000 mcg, complete with a solvent - 0.09% sodium chloride solution in ampoules of 2 ml.

Storage conditions:

At a temperature not exceeding +25 * C.

Additionally:

Stylamine.

Drugs with similar effects:

Sermorelin Nafarelin Octreotide Sandostatin

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Somatostatin INN

Description of the active substance (INN) Somatostatin.

Pharmacology: pharmachologic effect - somatostatin-like .

Indications: Acute bleeding from the upper gastrointestinal tract (including from esophageal varices), pancreatic fistulas, biliary and intestinal fistulas (auxiliary treatment), diabetic ketoacidosis (additional therapy), prevention of postoperative complications during pancreatic surgery .

Contraindications: Hypersensitivity, pregnancy, early postpartum period, breastfeeding (breastfeeding should be stopped).

Side effects: Dizziness, feeling of flushing (very rare), bradycardia, nausea and vomiting (only at injection rates above 50 mcg/min).

Interaction: Increases the effect of histamine H2-blockers (reducing the secretion of hydrochloric acid), hexobarbital and pentetrazole (accelerating falling asleep and prolonging sleep). Pharmaceutically incompatible (in one syringe) with other medications.

Directions for use and dosage: IV. After an initial slow (over 3-5 minutes) jet injection at a loading dose of 250 mcg/h (approximately equivalent to 3.5 mcg/kg/h), the drip infusion is continued. Immediately before the first administration, dilute with the supplied solvent. A solution for long-term infusion (over 12 hours) is prepared using an ampoule containing 3 mg of active substance and sodium chloride solution or 5% dextrose solution. The use of a syringe perfusion pump is recommended. If there is a break between two infusions exceeding 3-5 minutes (change of system for intravenous administration or syringe perfusion pump), an additional slow intravenous infusion is administered at a dose of 250 mcg. After bleeding stops (after 12-24 hours), treatment is continued for 48-72 hours; usually the total duration is up to 120 hours. For pancreatic, biliary or intestinal fistulas, a dose of 250 mcg/h is continuously administered simultaneously with total parenteral nutrition until the fistula is closed and for another 1-3 days (to avoid the development of withdrawal syndrome, therapy is stopped gradually) . To prevent complications after surgical interventions on the pancreas, it is administered at the beginning of the operation at a rate of 250 mcg/h and the administration is continued for 5 days. For ketoacidosis - at a rate of 100-500 mcg/hour together with insulin (injection of a loading dose of 10 units and simultaneous infusion at a rate of 1-4.9 units/hour). Normalization of glycemia occurs within 4 hours, and correction of acidosis occurs within 3 hours.

Precautions: At the beginning of treatment, temporary hyper- or hypoglycemia (blockade of insulin and glucagon secretion) may develop, and therefore blood glucose levels should be monitored every 3-4 hours, especially in patients with diabetes mellitus. Repeated courses should be avoided (sensitization is possible).

Special instructions: The solution in saline remains stable for 72 hours (stored in the refrigerator).

L-Alanylglycyl-L-cysteinyl-L-lysyl-L-asparaginyl-L-phenylalanyl-L-phenylalanyl-L-tryptophyl-L-lysyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L- cysteine ​​cyclic (1″14) disulfide

Chemical properties

Somatostatin – peptide hormone , which is produced hypothalamus And delta cells of the islets of Langerhans in the pancreas.

According to its chemical structure, the hormone exists in two forms, which differ in the length of the N-terminal sequence amino acids .

Synthetic somatostatin is cyclic peptide out of 14 amino acids .

This substance is produced in the form of injection solutions of various concentrations, lyophilisate to prepare a suspension, which is then administered intramuscularly.

pharmachologic effect

Somatostatin-like.

Pharmacodynamics and pharmacokinetics

The product has the ability to suppress the production of various growth hormones , namely somatotropin-releasing hormone by the hypothalamus; somatotropic And thyroid hormone by the pituitary gland . The substance also inhibits the production , some peptides , reduces the content , , , , insulin-like growth factor And vasoactive intestinal peptide .

Thanks to the properties of the drug listed above, the volume of blood in the internal organs decreases and the motility of the intestines and stomach decreases. If there is bleeding in the upper gastrointestinal tract, taking somatostatin will stop it.

After intravenous or intramuscular administration, the substance is broken down by endo- And aminopeptidases . The half-life is short - about 2-3 minutes.

Indications for use

Somatostatin drugs are prescribed:

• to stop acute bleeding from Gastrointestinal tract at varicose veins of the esophagus , hemorrhagic gastritis ;
• as a prophylactic after pancreatic surgery;
• for intestinal and biliary fistulas , pancreatic fistulas;
• for diagnostics, if it is necessary to reduce the intensity of production growth hormones, glucagon or insulin .

Contraindications

• if the patient is on the drug;
• pregnant women;
• in the early postpartum period;
• when breastfeeding.

Side effects

The hormone somatostatin is usually well tolerated.

However, the following may appear: ,bradycardia , pain and discomfort in the abdomen, vomiting and nausea with rapid administration, flushing of the face.

Somatostatin, instructions for use (Method and dosage)

The substance is administered intravenously and intramuscularly.

Depending on the purpose of use and the clinical situation, different dosages and duration of administration of the drug are chosen.

Before use, the solution is diluted in 5% or .

As a rule, 250 mcg of the drug is administered intravenously in a slow stream, then switched to drip administration. The average rate is 3.5 mcg per kg of patient weight per minute.

If it is necessary to take a break of more than 5 minutes between two infusions, it is recommended to administer an additional 250 mcg of the drug slowly intravenously.

Duration of treatment if it was necessary to stop bleeding from Gastrointestinal tract , is up to 120 hours. Usually the bleeding stops after 12 hours or a day, but as a preventive measure it is recommended to administer the medication for another 2-3 days.

For treatment fistulas the drug is administered continuously at 250 mcg per hour, combined with parenteral nutrition until the fistula closes. Therapy is continued for another 24-72 hours, the medicine is discontinued, gradually reducing the dose.

As a prophylactic agent in the postoperative period, Somatostatin continues to be administered for 5 days after surgery. The administration of 250 mcg of the drug per hour is also indicated.

At ketoacidosis use 100-500 mcg of medication per hour + insulin injections. Usually, normalizes within 4 hours.

Overdose

There is no evidence of an overdose of the drug, since it is usually used in a hospital setting and under medical supervision. personnel, which significantly reduces the likelihood of an overdose.

Interaction

When combining a drug with hexobarbital the hypnotic effect of the latter increases.

Combination use of the drug with histamine H2 blockers reduces secretion of hydrochloric acid .

The substance enhances the effect pentetrazole , speeds up falling asleep.

The product should not be mixed in the same syringe or dropper with other medications.

Terms of sale

On prescription.

Storage conditions

The solution can be stored in a cool place, at a temperature no higher than 25 degrees and no lower than 10. Do not allow the product to fall into the hands of small children or freeze.

Best before date

Somatostatin solution in physical solution Can be stored in the refrigerator for 2 days.

special instructions

At the beginning of drug therapy, sometimes develops hypo- or hyperglycemia . It is recommended to regularly monitor your blood sugar levels. Particular care must be taken when working with patients.

Treatment with the drug can only be done in a hospital setting.

During therapy, nutrition should be parenteral.

Drugs containing (Somatostatin analogues)

Level 4 ATX code matches:

Stylamine, Modustatin.