Octreotide - instructions for use, dose, side effects, contraindications

Octreotide is a synthetic analog of somatostatin, which has similar pharmacological effects, but a much longer duration of action. Octreotide suppresses the secretion of growth hormone (GH), both pathologically elevated, and caused by arginine, exercise and insulin hypoglycemia. The drug also inhibits the secretion of insulin, glucagon, gastrin, serotonin, both pathologically elevated, and caused by eating; also suppresses the secretion of insulin and glucagon stimulated with arginine. Octreotide suppresses the secretion of thyrotropin, caused by thyroidiberin.

In patients with pancreas surgery, the use of octreotide before surgery, during and after it reduces the incidence of typical postoperative complications (eg, pancreatic fistula, abscesses, sepsis, acute postoperative pancreatitis). When bleeding from varicose veins of the esophagus and stomach in patients with cirrhosis of the liver, the use of octreotide in combination with specific treatment (eg, sclerosing and haemostatic therapy) leads to more effective stopping of bleeding andprevention of rebleeding.

Pharmacokinetics:

After subcutaneous (SC) administration octreotide quickly and completely absorbed. The maximum concentration of octreotide in plasma is reached within 30 minutes. Binding to plasma proteins is 65%. The binding of octreotide to the formed elements of the blood is extremely insignificant. The volume of distribution is 0.27 l / kg. Half-life (T_1/2) after SC administration of octreotide is 100 minutes. After intravenous (iv) administration octreotide removal is carried out in 2 phases, with T_1/2 - 10 and 90 minutes, respectively. Most of the octreotide is excreted through the intestine, about 32% is excreted unchanged by the kidneys.

The total clearance is 160 ml / min. In elderly patients, clearance is reduced, and T_1/2 increases. In severe chronic renal failure, the clearance decreases by a factor of 2.

Indications:

- Treatment of acute pancreatitis;

- stop bleeding for peptic ulcer and 12 duodenal ulcer;

- stop bleeding and prevent bleeding from varicose veins of the esophagus in patients with cirrhosis;

- prevention and treatment of complications after operations on the organs of the abdominal cavity.

Contraindications:

Hypersensitivity to octreotide or other components of the drug. Children under 18 years.

Carefully:

Chololithiasis (cholelithiasis), diabetes, pregnancy, lactation.

Pregnancy and lactation:

The use of octreotide in pregnancy has not been studied. Octreotide It should be used during pregnancy only if the intended benefit to the mother exceeds the potential risk to the fetus.

It is not known whether the drug enters the breast milk, so when using the drug during lactation, breastfeeding should be abandoned.

Dosing and Administration:

The drug is injected intravenously into the drip, subcutaneously.

For treatment of acute pancreatitis the drug is administered SC at a dose of 100 μg 3 times / day for 5 days. It is possible to administer up to 1200 μg / day using an intravenous route of administration.

For stopping ulcerous bleeding administered intravenously at a dose of 25-50 μg / h in the form of intravenous infusions for 5 days.

For stop bleeding from varicose veins of the esophagus introduce iv in a dose of 25-50 μg / h in the form of continuous intravenous infusions for 5 days.In elderly patients, there is no need to reduce the dose of Octreotide.

For prevention of complications after operations on the pancreas - the first dose of 100-200 mcg injected p / k for 1-2 hours before laparotomy; then after the operation, enter sc to 100-200 μg 3 times / day for 5-7 consecutive days.

Side effects:

From the gastrointestinal tract, pancreas, liver and gallbladder: Anorexia, nausea, vomiting, abdominal cramps, a sensation of bloating, excessive gas formation, loose stools, diarrhea, and steatorrhea are possible. Although the release of fat with feces may increase, there is no indication that prolonged treatment with Octreotide can lead to the development of malabsorption (malabsorption). In rare cases, there may be phenomena reminiscent of acute intestinal obstruction.

There are isolated cases of acute hepatitis without cholestasis, as well as hyperbilirubinemia in combination with an increase in the activity of alkaline phosphatase, gamma-glutamyltransferase and, to a lesser extent, other transaminases.

Long-term use of Octreotide can lead to the formation of stones in the gallbladder.

From the side of the cardiovascular system: in some cases - an arrhythmia, a bradycardia.

From the side of carbohydrate metabolism: possibly a violation of glucose tolerance after eating (due to the suppression of insulin secretion by the drug), hypoglycemia; In rare cases, long-term treatment may develop persistent hyperglycemia.

Local reactions: at the injection site, pain, itching or burning sensation, redness and swelling are possible (usually within 15 minutes).

Other: allergic reactions, alopecia.

Overdose:

The following are possible symptoms: a short-term reduction in the heart rate, a feeling of "tide" of blood to the face, spastic pain in the abdomen, diarrhea, nausea, a feeling of emptiness in the stomach.

Treatment symptomatic.

Interaction:

Octreotide reduces the absorption of cyclosporine, slows the absorption of cimetidine. It is necessary to correct the dosage regimen of concurrently used direc- tors, beta-blockers, blockers of "slow" calcium channels, insulin, oral hypoglycemic drugs.

With the simultaneous use of Octreotide and bromocriptine, the bioavailability of the latter increases.

Drugs metabolized by enzymes of the cytochrome P450 system and having a narrow therapeutic range of doses should be administered with caution.

Special instructions:

In diabetic patients receiving insulin, Octreotide can reduce the need for insulin.

If gallstones are detected before starting treatment, the question of the use of Octreotide is decided individually, depending on the ratio of the potential therapeutic effect of the drug and the possible risk factors associated with the presence of gallstones.

Gastrointestinal side effects can be reduced if Octreotide injections are done in between meals or at bedtime.

To reduce the phenomena of discomfort at the injection site, it is recommended to bring the drug solution before introducing it to room temperature and introduce a smaller volume of the drug. Several injections should be avoided in the same place at short intervals.

Effect on the ability to drive transp. cf. and fur:

Some of the side effects of octreotide may adversely affect the ability to drive vehicles and other mechanisms,requiring increased concentration of attention and speed of the speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and subcutaneous administration, 50, 100 μg / ml.

Packaging:

1 ml per ampoule of colorless glass with a color marking in the form of two green strips or in ampoules of dark glass, having a ring of tension for opening or ampoule with a break point.

5 ampoules per contour cell packaging made of polyvinyl chloride film.

1 or 2 contour mesh packages with instructions for use are placed in a pack of cardboard box.

Storage conditions:

In the dark place at a temperature of 8 to 25 ° C, in places inaccessible to children.

Shelf life:

5 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N002374 / 01-2003

Date of registration:21.04.2008 / 23.04.2012

Expiration Date:Unlimited

The owner of the registration certificate:F-SYNTHESIS, CJSC F-SYNTHESIS, CJSC Russia