Oktreotid

General characteristics. Structure:

Active ingredient: 50 mkg or 100 mkg of an oktreotid.

Excipients: sodium chloride, water for injections.

The choice drug for anti-secretory therapy and prevention of acute pancreatitis making combined effect on all major factors of its pathogeny, drug of complex therapy of ulcer bleedings and bleedings from varicose expanded veins of a gullet and cardial department of a stomach at patients with cirrhosis. Drug is used for treatment of pancreatitis, for prevention and treatment of complications after abdominal organs operations, for a stop of ulcer bleedings and bleedings from varicose expanded veins of a gullet at patients with cirrhosis.

Pharmacological properties:

Pharmacodynamics. Oktreotid - the synthetic analog of somatostatin having pharmacological effects, similar to it, but considerable the bigger duration of action. Oktreotid suppresses the secretion of the growth hormone (GH) both patholologically increased, and caused by arginine, an exercise stress and an insulin hypoglycemia. Drug suppresses also the secretion of insulin, a glucagon, gastrin, serotonin both patholologically increased, and caused meal; also suppresses secretion of insulin and a glucagon, stimulated arginine. Oktreotid suppresses the thyrotropin secretion caused tireoliberiny.

At patients to whom carrying out operation on a pancreas is planned use of an oktreotid before operation, in time and after it reduces the frequency of typical postoperative complications (for example, pancreatic fistulas, abscesses, sepsis, acute postoperative pancreatitis). At bleeding from varicose veins of a gullet and a stomach at patients with cirrhosis use of an oktreotid in a combination with specific treatment (for example, sclerosing and haemo static therapy) leads to more effective stop of bleeding and prevention of repeated bleeding.

Pharmacokinetics. After hypodermic (п / to) introductions октреотид it is quickly and completely soaked up. The maximum concentration of an oktreotid in plasma is reached within 30 min.

Linkng with proteins of plasma makes 65%. Linkng of an oktreotid with uniform elements of blood is extremely insignificant. The volume of distribution makes 0.27 l/kg.

The elimination half-life (T1/2) after п / to introduction of an oktreotid makes 100 min. After intravenous (in/in) introductions removal of an oktreotid is carried out in 2 phases, with T1/2 - 10 and 90 min., respectively. The most part of an oktreotid is removed through intestines, about 32% are removed in an invariable look by kidneys.

The general clearance makes 160 ml/min. At elderly patients the clearance decreases, and T1/2 increases. At a heavy chronic renal failure the clearance decreases twice.

Indications to use:

- treatment of acute pancreatitis;
- a stop of bleedings at a peptic ulcer of a stomach and a 12-perstny gut;
- a stop of bleeding and prevention of repeated bleeding from varicose expanded veins of a gullet at patients with cirrhosis;
- prevention and treatment of complications after abdominal organs operations

Route of administration and doses:

The drug is administered in/in kapelno, subcutaneously.

For treatment of acute pancreatitis the drug is administered п / to in a dose of 100 mkg of 3 times/days within 5 days. Appointment to 1200 mkg/days with use of an intravenous way of introduction is possible.

For a stop of ulcer bleedings enter in/in in a dose of 25 - 50 mkg/h in the form of intravenous infusions within 5 days.

For a bleeding stop from varicose expanded veins of a gullet enter in/in in a dose of 25-50 mkg/h in the form of long intravenous infusions within 5 days. Patients of advanced age have no need for Oktreotid dose decline.

For prevention of complications after pancreas operations the first dose of 100-200 mkg is entered п / to for 1-2 h to a laparotomy; then after operation enter п / to on 100-200 mkg of 3 times/days for 5-7 consecutive days.

Features of use:

At the patients with a diabetes mellitus receiving insulin, Oktreotid can reduce the need for insulin.

If stones in a gall bladder are revealed before an initiation of treatment, the issue of Oktreotid's use is resolved individually, depending on a ratio of potential medical effect of drug and possible risk factors, the stones connected with existence in a gall bladder.

Side effects from a GIT can be reduced if to do Oktreotid's injections in intervals between meals or before going to bed.

For reduction of the phenomena of discomfort in the place of an injection it is recommended to bring drug solution before introduction to room temperature and to administer the smaller volume of the drug. It is necessary to avoid several injections to the same place through short intervals of time.

Use during pregnancy and breastfeeding. Use of an oktreotid at pregnancy was not studied. Oktreotid it is necessary to apply at pregnancy only if the estimated advantage for mother exceeds potential risk for a fruit.

It is unknown whether drug gets to breast milk therefore at use of drug in the period of a lactation it is necessary to refuse breastfeeding.

Influence on ability to manage vehicles and other mechanisms. Some side effects of an oktreotid can negatively influence ability to manage the vehicles and other mechanisms demanding the increased concentration of attention and speed of speed of psychomotor reactions.

Side effects:

From a GIT, a pancreas, liver and gall bladder: are possible – anorexia, nausea, vomiting, spastic abdominal pains, feeling of abdominal distention, excess gas generation, a liquid chair, diarrhea and a steatorrhea. Though release of fat with a stake can increase, there are no instructions on the fact that prolonged treatment by Oktreotid can lead to development of disturbances of absorption (malabsorption). In rare instances the phenomena reminding acute intestinal impassability can be noted.

Separate cases of an acute hepatitis without cholestasia, and also hyperbilirubinemias in combination with increase in activity of an alkaline phosphatase, gamma глутамилтрансферазы and, to a lesser extent, other transaminases are known.

Long use of Oktreotid can lead to formation of stones in a gall bladder.

From cardiovascular system: in some cases – arrhythmia, bradycardia.

From carbohydrate metabolism: disturbance of tolerance to glucose after meal (it is caused by suppression by insulin secretion drug), a hypoglycemia is possible; in rare instances at prolonged treatment development of a persistent hyperglycemia is possible.

Local reactions: in the place of an injection pain, feeling of an itch or burning, redness and a swelling are possible (usually pass within 15 min.).

Others: allergic reactions, alopecia.

Interaction with other medicines:

Oktreotid reduces cyclosporine absorption, slows down absorption of Cimetidinum.

Correction of the mode of dosing of at the same time applied diretik, beta adrenoblockers, blockers of "slow" calcium channels, insulin, peroral hypoglycemic drugs is necessary.

At simultaneous use of Oktreotid and Bromocriptinum bioavailability of the last increases.

It is necessary to appoint the drugs which are metabolized enzymes of system of P450 cytochrome and having the narrow therapeutic range of doses with care.

Contraindications:

Hypersensitivity to an oktreotid or other components of drug. Children's age up to 18 years.

With care. Cholelithiasis (cholelithiasis), diabetes mellitus, pregnancy, lactation period.

Overdose:

The following symptoms are possible: a short-term urezheniye of heart rate, feeling of "inflow" of blood to the person, spastic abdominal pains, diarrhea, nausea, feeling of emptiness in a stomach.

Symptomatic treatment.

Storage conditions:

In the place protected from light at a temperature from 8 to 25 °C, in places unavailable to children. Period of validity of 5 years.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and hypodermic administration 50, 100 mkg/ml.

On 1 ml in ampoules from colourless glass with color marking in the form of two green strips or in the ampoules of dark glass having a tension ring for opening or an ampoule with a break point.

On 5 ampoules in a blister strip packaging from a film polyvinyl chloride.

1 or 2 blister strip packagings with the application instruction place in a pack from a cardboard bandbox.