Oktreotid Fsintez

General characteristics. Structure:

Active ingredient: 0,05 mg, 0,1 mg or 0,3 mg of an okreotid of acetate (in terms of окреотид).

Excipients: sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. Oktreotid – synthetic octapeptide, derivative natural hormone of somatostatin, has pharmacological effects, similar to it, but with considerably bigger duration of action. Oktreotid suppresses as patholologically hypersecretion of the growth hormone (GH), and caused by arginine, an exercise stress and an insulin hypoglycemia. Drug suppresses secretion of serotonin, gastrin, insulin and glucagon and other peptides produced in gastro-entero-pankreoticheskoy to endocrine system.

At patients to whom pancreas operations are performed use of an oktreotid during operation and after it reduces the frequency of typical postoperative complications (acute postoperative pancreatitis, pancreatic fistulas, abscesses, sepsis).

At bleedings from varicose expanded veins of a p*-98/ishchevod and a stomach at patients with cirrhosis use of an oktreotid as a part of complex therapy leads to an effective stop of bleeding, prevention of early repeated bleeding and improvement of survival. The mechanism of action of an oktreotid is connected with reduction of an organ blood-groove by means of suppression of vasoactive hormones (vasoactive intestinal peptide, a glucagon).

Pharmacokinetics. After hypodermic introduction октреотид it is quickly and completely soaked up. It is known that the maximum concentration of drug 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 most part of drug is removed by intestines, about a third of the entered oktreotid is removed in an invariable look by kidneys. An elimination half-life (T1/2) after hypodermic (п / to) injections about 100 min. After intravenous (in/in) introductions removal of drug is carried out in two phases. At elderly patients the clearance decreases, the elimination half-life increases. At a heavy renal failure the clearance decreases twice.

Indications to use:

• prevention and treatment of complications after pancreas operations and a gastroduodenal zone;
• as a part of complex therapy for a stop of bleedings and prevention of repeated bleeding from varicose expanded veins of a gullet at patients with cirrhosis;
• treatment of acute pancreatitis;
• stop of bleedings at a peptic ulcer of a stomach and a 12-perstny gut.

Route of administration and doses:

At treatment of acute pancreatitis Oktreotid Fsintez is entered п / to in a dose of 100 mkg of 3 times/days within 5-7 days. Appointment to 1200 mkg/days is possible, selection of a dose is based on definition of concentration of amylase, a lipase, inflammatory cytokines of blood.

For prevention of complications after pancreas operations Oktreotida Fsintez 100 mkg enter the first dose п / to for 1 h to a laparotomy; then after operation enter п / to on 100 mkg of 3-4 times/days for 7 next days.

For a bleeding stop from varicose expanded veins of a gullet the drug is administered in/in in a dose of 25 mkg/h in the form of long infusions within 5 days.

For a stop of bleedings at a peptic ulcer of a stomach and a 12-perstny gut Oktreotid Fsintez in a look in/in infusions in a dose is recommended to enter 25 mkg/hour within 5 days.

Patients of advanced age have no need for a dose decline Oktreotida Fsintez.

With a renal failure correction of the mode of dosing of an oktreotid is not required from patients.

At patients with an abnormal liver function correction of a maintenance dose since patients with cirrhosis have data on increase in T1/2 of an oktreotid is recommended.

Experience of use of an oktreotid for children is very limited.

Rules of preparation and administration of solution. For reduction of the phenomena of discomfort in an injection site, solution Oktreotida Fsintez before introduction has to have room temperature. At п / to administration of drug it is necessary to avoid several injections to the same place through short intervals of time. Ampoules with drug should be opened just before introduction, the unused amount of solution should be destroyed.

At in introduction it is necessary to examine attentively solution regarding transparency, existence of particles, a deposit, discoloration. It is impossible to use drug if it is muddy, contains particles, a deposit. Oktreotid Fsintez within 24 hours keeps physical and chemical stability in sterile 0,9% chloride sodium solution at a temperature from 8 to 25 °C. In order to avoid microbic pollution divorced solutions should be used right after preparation. If solution is not used at once, it should be stored at a temperature from 2 to 8 °C up to its use. Before use solution should be taken at the room temperature.

The general time between cultivation, storage in the refrigerator and the end of administration of solution should not exceed 24 h. If necessary in/in introductions contents of one ampoules, containing 500 mkg of an oktreotid, have to be divorced in 60 ml of 0,9% of solution of sodium of chloride, the prepared solution should be entered in/in kapelno. Infusions are repeated with a necessary frequency according to the recommended treatment duration. Oktreotid it is also possible to enter also in lower concentration.

Features of use:

Use during pregnancy and a lactation. Adequate and controlled researches were not conducted. Use during pregnancy and in the period of a lactation only according to absolute indications, taking into account a ratio risk/advantage i.e. when the estimated advantage for mother exceeds estimated risk for a fruit or the baby.

At patients with a diabetes mellitus of 1 type (receiving insulin), Oktreotid Fsintez can reduce the need for insulin. At patients without disturbance of carbohydrate metabolism and patients with a diabetes mellitus administration of drug can lead 2 types to a postprandialny glycemia. Patients with a diabetes mellitus against the background of antidiabetic therapy are recommended to carry out control of concentration of glucose to blood.

At some patients октреотид can change absorption of fats in intestines. Against the background of use of an oktreotid decrease in content of cyanocobalamine (B12 vitamin) and an aberration of indicators of the test of absorption of cyanocobalamine (the test of Shilling) is noted.

At patients with deficit of B12 vitamin in the anamnesis at use of an oktreotid it is recommended to control the content of cyanocobalamine.

If against the background of use of an oktreotid bradycardia develops, it is necessary to lower doses of beta adrenoblockers, blockers of the "slow" calcium channels or drugs influencing water and electrolytic balance.

Before purpose of an oktreotid patients have to undergo initial ultrasonography of a gall bladder. If stones in a gall bladder are revealed before an initiation of treatment, the issue of use Oktreotida Fsintez is resolved individually, depending on a ratio of potential medical effect of drug and the possible risk factors connected with existence of stones in a gall bladder.

During treatment oktreotidy. it is necessary to carry out ultrasonography of a gall bladder, with an interval of 6-12 months.

Maintaining patients at whom stones of a gall bladder are formed in the course of treatment oktreotidy.
a) Asymptomatic stones of a gall bladder. Use of an oktreotid can be stopped or continued - according to ratio assessment advantage/risk. Anyway no other measures, except continuation of carrying out surveys are required, having made them, if necessary, more frequent.
b) Stones of a gall bladder with clinical symptomatology. Use of an oktreotid can be stopped or continued - according to ratio assessment advantage/risk. Anyway the patient should be treated as well as in other cases of cholelithiasis with clinical manifestations.

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

Correction of the mode of dosing of at the same time applied diuretics, beta adrenoblockers, blockers of "slow" calcium channels, insulin, peroral hypoglycemic means, a glucagon is necessary.

Influence on ability to driving and other vehicles, for work with the moving mechanisms: today there are no data on influence of an oktreotid on ability to drive the car and to work with mechanisms.

Side effects:

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.).

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 oktreotidy can lead to development of disturbances of absorption (malabsorption). In rare instances the phenomena reminding acute intestinal impassability can be noted: the progressing abdominal distention, the expressed pain in epigastric area, tension of an abdominal wall.

Long use of an oktreotid can lead to formation of stones in a gall bladder. Separate cases of an acute hepatitis without cholestasia (normalization of indicators of transaminases after cancellation of an oktreotid), and also hyperbilirubinemias in combination with increase in activity of an alkaline phosphatase, gamma глютамилтрансферазы, etc. transaminases are known. There are separate messages on exceptional cases of acute pancreatitis which developed during the first hours or days of use of an oktreotid.

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

From a metabolism: disturbance of tolerance to glucose after meal (октреотид has overwhelming effect on formation of GR, glucagon and insulin), a hypoglycemia is possible; in rare instances at prolonged treatment development of a persistent hyperglycemia is possible.

Others: seldom - allergic reactions, an allopecia; in some cases – anaphylactic reactions.

Interaction with other medicines:

Oktreotid reduces cyclosporine absorption, slows down absorption of Cimetidinum. Correction of doses of at the same time applied diuretics, beta adrenoblockers, blockers of "slow" calcium channels, insulin, peroral hypoglycemic drugs is necessary.

At simultaneous use Oktreotida Fsintez and a bromkriptina bioavailability of the last raises.

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 drug components.

With care:

- diabetes mellitus,
- cholelithiasis.

Overdose:

It is known that introduction of an oktreotid in a dose to 2000 mkg in a look п / to an injection 3 times within several months was transferred well. The maximum single dose at in bolyusny introduction to the adult patient made 1000 mkg. At the same time such symptoms as decrease in heart rate, "inflows" of blood to the person, abdominal pain of spastic character, diarrhea, nausea, feeling of emptiness in a stomach were noted. All these symptoms were resolved within 24 hours from the moment of administration of drug. To one patient by mistake the method of long infusion entered an excess dose of an oktreotid of 250 mkg/h (instead of 25 mkg/h) that was not followed by side effects. At acute overdose any life-threatening reactions were not noted.

Treatment: symptomatic therapy.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. Not to freeze. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and hypodermic administration of 50 mkg/ml, 100 mkg/ml, 300 mkg/ml. On 1 ml in ampoules of neutral glass; use of ampoules with a tension ring for opening or a break point is possible. On 5 ampoules in a blister strip packaging from a film polyvinyl chloride. 1 or 2 blister strip packagings, a knife for opening of ampoules or the scarificator ampoule, place the application instruction in a cardboard pack. When packaging solution or in ampoules with a break point the knife or the scarificator ampoule do not put in the ampoules having a tension ring for opening.