Octreotide

Brand Nativa

In stock 1568 Items

Available since: 2019-09-19

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Clinical Pharmacology

Octreotide is a synthetic octapeptide, which is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but a significantly longer duration of action. The drug inhibits pathologically increased secretion (the process of production and secretion) of growth hormone, as well as peptides and serotonin, produced in the gastroenteropancreatic endocrine system (system including the stomach, small intestine and pancreas).
In healthy individuals, octreotide inhibits the secretion of growth hormone caused by arginine, stress, and insulin hypoglycemia (low blood sugar levels caused by insulin); secretion of insulin, glucagon, gastrin and other peptides of the gastroenteropancreatic endocrine system, caused by food intake, as well as insulin and glucagon secretion, stimulated by arginine; secretion of thyrotropin (a pituitary hormone that regulates the function of the thyroid gland), caused by thyreiberin.
In patients with acromegaly (endocrine disease, accompanied by an increase in the volume of the hands, nose, mandible, etc.), octreotide lowers the concentration of growth hormone and / or somatomedin A (a biologically active compound, usually produced by liver cells, stimulating tissue growth and exhibiting insulin-like activity ) in the blood plasma. A clinically significant decrease in the concentration of growth hormone (by 50% or more) is observed in almost all patients; the normalization of growth hormone levels in plasma (less than 5 ng / ml) is reached somewhere in half of the patients. In most patients with acromegaly, octreotide markedly reduces the severity of symptoms such as headache, swelling of the skin and soft tissues, hyperhidrosis (a disease of sweat glands with the formation of small pruritic vesicles), joint pain and paresis (decrease in strength and / or amplitude of movements). In patients with large adenomas (benign tumors) of the pituitary, treatment with octreotide may lead to some reduction in the size of the tumor.
In carcinoid (cancerous) tumors, the use of octreotide can lead to a decrease in the severity of symptoms such as hot flashes and diarrhea (diarrhea), which in many cases is accompanied by a decrease in plasma serotonin concentration and a decrease in 5-hydroxyindole acetic acid in the urine.
In tumors characterized by hyperproduction (enhanced formation) of a vasoactive intestinal peptide, the use of octreotide in most cases leads to a decrease in severe secretory diarrhea (diarrhea). At the same time, there is a decrease in concomitant electrolyte (ionic) balance disorders, in particular, hypokalemia (low potassium level in the blood). In some cases, the progression of the tumor slows down or stops and even decreases in size. Clinical improvement is often accompanied by a decrease (up to normal values) in plasma plasma concentration of the vasoactive intestinal peptide.
In glucagonomas (a malignant tumor / cancer / pancreas producing insulin), the use of octreotide in most cases leads to a marked decrease in necrotizing (leading to necrosis of tissue) of the migrating rash; body weight decreases (the effect on diabetes mellitus, but only slightly). For grocery stores (malignant tumor / cancer / stomach), Zollinger-Ellison syndrome (a complex of symptoms associated with the combination of gastric and duodenal ulcers with benign pancreatic tumors), octreotide reduces the hypersecretion (increased secretion) of hydrochloric acid in the stomach and the associated symptoms of gastric acid in the stomach and the associated symptoms of hearth and pancreatic ulcers; feeling of hot flashes.Some patients have a decrease in gastrin concentration (protein secreted by the gastric mucosa, which causes an increase in the secretion of digestive juices by the stomach and pancreas) in the blood plasma.
In patients with insulinomas (pancreatic insulin-producing tumors), octreotide normalizes glycemia (lowers high blood sugar), reducing insulin levels in the blood (this result, but maybe short-term, about 2 hours). Glycemia control can be improved even without a simultaneous long-term decrease in the level of insulin in the blood.
In patients with tumors that hyperproduce growth hormone releasing factor (emit an increased number of hypothalamic neurohormones that promote the secretion of growth hormone by the pituitary gland), octreotide reduces the severity of acromegaly symptoms. In the future, hypertrophy (volume increase) of the pituitary gland may decrease.
In patients with acquired immunodeficiency syndrome (AIDS), suffering from severe diarrhea (diarrhea), refractory (resistant) to anti-infective or other therapy, the use of octreotide leads to complete or partial normalization of stool somewhere in one third of cases.
In patients who undergo operations on the pancreas, the use of the drug during and after the operation reduces the incidence of typical postoperative complications (in particular, pancreatic fistulas / disease channels that connect the pancreas with internal organs or the external environment), abscesses / pus suck /, sepsis / infection of blood by microbes from a focus of purulent inflammation /, postoperative acute pancreatitis / inflammation of the pancreas /).

Indications

prevention and treatment of complications after operations on the pancreas and gastroduodenal zone;
as part of complex therapy to stop bleeding and prevent recurrent bleeding from esophageal varicose veins in patients with cirrhosis of the liver;
treatment of acute pancreatitis;
stop bleeding with gastric ulcer and 12 duodenal ulcer.

Composition

1 ml of solution contains:

Active ingredient: Octreotide acetate (in terms of octreotide) 0.050 mg, 0.100 mg and 0.300 mg

Excipients:

Sodium Chloride 9.0 mg
Water for injection to 1.0 ml

Octreotide is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Octreotide	Nativa	Russia	solution
Octreotide	Farm Synthesis	Russia	solution
Octretex	Sotex	Russia	ampoules
Sandostatin Lar	Novartis	Switzerland	vials
Octreotide	Farm Synthesis	Russia	ampoules
Sandostatin	Novartis	Switzerland	ampoules

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Dosage and Administration

In the treatment of acute pancreatitis, Octreotide is injected sc / c at a dose of 100 mcg 3 times / day for 5-7 days. You can assign up to 1200 mcg / day, dose selection is based on determining the concentration of amylase, lipase, inflammatory blood cytokines.

For the prevention of complications after operations on the pancreas, the first dose of Octreotide 100 μg is injected s / c 1 hour before laparotomy; then after the operation, injected sc / c 100 mcg 3-4 times / day for 7 consecutive days.

To stop bleeding from esophageal varicose veins, the drug is administered intravenously at a dose of 25 mcg / h in the form of continuous infusions for 5 days.

To stop bleeding in gastric ulcer and duodenal ulcer, it is recommended to administer Octreotide in the form of intravenous infusion at a dose of 25 μg / hour for 5 days.

Elderly patients do not need to reduce the dose of Octreotide. In patients with impaired renal function, the correction of octreotide dosing regimen is not required.

In patients with impaired liver function, a maintenance dose adjustment is recommended, since there is evidence of an increase in T1 / 2 octreotide in patients with liver cirrhosis.

The experience of using octreotide in children is very limited.

Rules for the preparation and administration of the solution

To reduce the phenomena of discomfort at the injection site, Octreotide solution should be at room temperature before administration. When s / c administration of the drug should be avoided several injections in the same place at short intervals of time. Ampoules with the drug should be opened immediately before the introduction, the unused amount of the solution should be destroyed. With the on / in the introduction should carefully inspect the solution for transparency, the presence of particles, sediment, discoloration. Do not use the drug if it is cloudy, contains particles, sediment. Octreotide for 24 hours maintains physical and chemical stability in sterile 0.9% sodium chloride solution at a temperature of 8 to 25 ° C. To avoid microbial contamination, diluted solutions should be used immediately after preparation. If the solution is not used immediately, it should be stored at a temperature of from 2 to 8 ° C until its use. Before using the solution should be kept at room temperature. The total time between dilution, storage in the refrigerator and the end of the introduction of the solution should not exceed 24 hours. If necessary, the / in the introduction of the contents of one ampoule containing 500 mcg of octreotide, should be diluted in 60 ml of 0.9% sodium chloride solution, the prepared solution should be introduced into / in the drip. Infusions are repeated with the required frequency in accordance with the recommended duration of treatment. Octreotide can also be administered in lower concentrations.

Adverse reactions

Local reactions: pain, itching or burning sensation, redness and swelling are possible at the injection site (usually disappear within 15 minutes). On the part of the gastrointestinal tract, pancreas, liver and gallbladder: anorexia, nausea, vomiting, cramping abdominal pain, bloating, excessive gas formation, loose stools, diarrhea and steatorrhea are possible. Although the excretion of fat with feces may increase, there is no indication that long-term treatment with octreotide may lead to the development of malabsorption disorders. In rare cases, there may be phenomena resembling acute intestinal obstruction: progressive abdominal distension, severe pain in the epigastric region, tension in the abdominal wall. Prolonged use of octreotide can lead to the formation of gallstones. There are isolated cases of acute hepatitis without cholestasis (normalization of transaminase parameters after discontinuation of octreotide), as well as hyperbilirubinemia in combination with an increase in the activity of alkaline phosphatase, gamma glutamyltransferase, and other transaminases.There are isolated reports of rare cases of acute pancreatitis that developed during the first hours or days of octreotide use. Since the cardiovascular system: in some cases - tachycardia, bradycardia. Metabolism: impaired glucose tolerance after a meal (octreotide has a suppressive effect on the formation of GH, glucagon and insulin), hypoglycemia; in rare cases, prolonged treatment may develop persistent hyperglycemia. Other: rarely - allergic reactions, alopecia; in some cases - anaphylactic reaction.

Contraindications

Hypersensitivity to the drug.

With caution - diabetes, gallstone disease.

Drug interactions

Octreotide reduces the absorption of cyclosporine, slows down the absorption of cimetidine. Adjustment of doses of simultaneously used diuretics, beta-blockers, blockers of “slow” calcium channels, insulin, oral hypoglycemic drugs is necessary. With the simultaneous use of Octreotide and bromkriptina bioavailability of the latter increases. Drugs metabolized by cytochrome P450 enzymes and having a narrow therapeutic dose range should be administered with caution.

Pregnancy and Lactation

No adequate and well-controlled studies have been conducted. Use during pregnancy and lactation only by absolute indications, taking into account the risk / benefit ratio, i.e. when the intended benefits to the mother outweigh the perceived risk to the fetus or infant.

Special instructions

In patients with type 1 diabetes (receiving insulin), Octreotide may reduce the need for insulin. In patients without disturbed carbohydrate metabolism and patients with type 2 diabetes mellitus, administration of the drug can lead to postprandial glycemia. Patients with diabetes on the background of antidiabetic therapy are advised to monitor the concentration of glucose in the blood. In some patients, octreotide may alter the absorption of fat in the intestine. Against the background of the use of octreotide, a decrease in the content of cyanocobalamin (vitamin B12) and a deviation from the norm of the indicators of the cyanocobalamin absorption test (Schilling test) are observed. In patients with a history of vitamin Bj2 deficiency in the use of octreotide, it is recommended to monitor the content of cyanocobalamin. If, against the background of the use of octreotide, bradycardia develops, it is necessary to reduce the doses of beta-blockers, blockers of “slow” calcium channels or drugs that affect the water-electrolyte balance. Before prescribing octreotide, patients must undergo an initial ultrasound of the gallbladder. If gallstones are detected before treatment, the question of using Octreotide is solved individually, depending on the ratio of the potential therapeutic effect of the drug and possible risk factors associated with the presence of stones in the gallbladder. During treatment with octreotide. should be an ultrasound of the gallbladder, with an interval of 6-12 months. Maintaining patients in whom gallbladder stones are formed during the treatment with octreotide. a) Asymptomatic gallbladder stones. The use of octreotide can be discontinued or continued - in accordance with the assessment of the benefit / risk ratio. In any case, no other measures are required, apart from the continuation of inspections, making them, if necessary, more frequent. b) Gallbladder stones with clinical symptoms. The use of octreotide can be discontinued or continued - in accordance with the assessment of the benefit / risk ratio. In any case, the patient should be treated in the same way as in other cases of gallstone disease with clinical manifestations. Side effects from the gastrointestinal tract can be reduced if Octreotide injections are given between meals or before bedtime.Correction of the dosing regimen of simultaneously used diuretics, beta-blockers, blockers of “slow” calcium channels, insulin, oral hypoglycemic agents, glucagon is necessary. Impact on the ability to drive a car and other vehicles, to work with moving mechanisms: to date, there is no data on the effect of octreotide on the ability to drive a car and work with mechanisms.

Overdosage

It is known that the administration of octreotide in a dose of up to 2000 mcg as a sc injection 3 times over several months was well tolerated. The maximum single dose for intravenous bolus administration to an adult patient was 1000 μg. At the same time, such symptoms as a decrease in the heart rate, "flushing" of blood to the face, abdominal pain of a spastic nature, diarrhea, nausea, and a feeling of emptiness in the stomach were noted. All these symptoms resolved within 24 hours from the moment of administration. One patient by mistake by the method of long-term infusion was administered an excessive dose of octreotide 250 mcg / h (instead of 25 mcg / h), which was not accompanied by side effects. In acute overdose, no life-threatening reactions were noted. Treatment: symptomatic therapy.