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Oktrestatin

Oktrestatin (Octrestatin)

international and chemical name: oktreotid;

Main physical and chemical characteristics: inodorous transparent colourless liquid;

Structure okterotid (in the form of free to peptide) 5,0 mg or 10,0 mg in an ampoule;

other components: sodium chloride, water for injections.

Form of release of medicine. Solution for injections.

Farmakoterapevtichesky group. Somatostatin. ATC H01CB02 code.

Effect of the medicine.

Pharmacodynamics.

Oktrestatin represents synthetic oktopeptid which is to derivatives of natural hormone of somatostatin, it has similar pharmacological effects, but at the same time duration of its action considerably big. Drug suppresses patholologically growth hormone hypersecretion, and also peptides and serotonin which are formed in gastro-entero-pankreatichii to endocrine system.

At patients to whom operations of a pas to a pancreas are performed of Oktrestatin's use during operation and after it reduces the frequency of typical postoperative complications, for example: pancreatic fistulas, abscesses, sepsis, acute postoperative pancreatitis and others.

Pharmacokinetics.

After hypodermic introduction oktreotid quickly and completely the blood channel gets. The maximum concentration of drug in plasma is reached within 30 minutes.

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 general clearance makes 160 ml/min. About 32% are brought in an invariable look by kidneys. The elimination half-life (T1/2) after a subcutaneous injection of drug makes 100 minutes. After intravenous administration removal of drug is carried out in two phases: T1/2 - 10 and 90 minutes respectively. At elderly patients the clearance decreases, and T1/2 increases. At a heavy renal failure the clearance decreases twice.

Indications to use.

Prevention and treatment of complications after operations on abdominal organs.

Stop of bleeding and prevention repeated bleedings from varicose expanded veins of a gullet at patients on cirrhosis.

Treatment of acute pancreatitis.

Stop of ulcer bleedings.

Way of use and dose.

For treatment of acute pancreatitis drug to be taken away subcutaneously in a dose of 100 mkg 3 times a day within 5 days. Appointment to 1200 mkg a day with use of an intravenous way of introduction is possible.

For prevention of complications after pancreas operations the first dose of 100 mkg is entered subcutaneously in 1 hour prior to a laparotomy; then after operation enter subcutaneously 100 mkg 3 times a day within 7 consecutive days.

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

For a stop of ulcer bleedings enter in/in in a dose of 25 mkg/hour in the form of infusions within 5 days.

Side effect.

From a digestive tract, a pancreas, liver and gall bladder: are possible - anorexia, nausea, vomiting, spastic abdominal pains, feeling abdominal distention, excessive gas generations, liquid emptying, diarrhea and a steatorrhea. Though allocation to fat with a stake can increase, there are no instructions on the fact that oktreotidy absorption (malabsorption) can lead long-term treatment to development of disturbances. In isolated cases the phenomena can be noted that remind acute intestinal impassability.

Separate cases of an acute hepatitis without cholestasia, and also hyperbilirubinemias in connection with increase in activity of an alkaline phosphatase, gamma glyutamiltransferazy and, in menshy are known to a step, other transaminases.

Long-term use of an oktreotid can lead to formation of concrements in a gall bladder.

In foreign sources it is reported about isolated cases of acute pancreatitis that developed in the first hour or day of use and disappeared after cancellation of an oktreotid (Sandostatin).

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

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

Local reactions: in the place of an injection pain, feeling an itch or burning, reddening and a swelling are possible (such phenomena ordinary pass within 15 minutes).

Others: allergic reactions, alopecia.

Contraindications. Hypersensitivity to drug components Oktrestatin.

Overdose.

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

Symptomatic treatment.

Features of use.

Oktrestatin it is necessary to apply with care at patients that have a zhelchekamenny illness and a diabetes mellitus, and also women in the period have pregnancies and lactations.

At patients with a diabetes mellitus who receive insulin oktreotid can reduce need for insulin.

If stones in a gall bladder are revealed before an initiation of treatment, the issue about uses of an oktreotid is resolved individually, depending on the comparison of potential medical effect of drug and possible risk factors connected with existence of stones in a gall bladder.

Side effects from a digestive tract can be lowered if to do injections of an oktreotid in intervals between receptions of food or before going to bed.

For decrease in 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 in those the place through short intervals of time.

Pregnancy and lactation. The adequate and controlled researches for the person were not conducted. Use during pregnancy and in the period of a lactation only on absolute measures, taking into account comparison risk/advantage that is when the predicted advantage for mother exceeds preseen risk for a fruit. Category of action on a germ B.

Interaction with other medicines. Oktreostatin reduces absorption of Cimetidinum, cyclosporine.

It is necessary correction of doses of at the same time applied diuretics, b-adrenoblockers, antagonists of calcium, insulin, peroral gipoglikemichny drugs.

At simultaneous use of an oktreotid and bromkriptin bioavailability of the last increases.

Drugs that are metabolized by enzymes of system of P450 cytochrome and have the narrow therapeutic range of doses, it is necessary to appoint with care.

Conditions and periods of storage.

TO STORE IN THE PLACE, UNAVAILABLE TO CHILDREN.

To store in the place protected from light at a temperature from 8 °C to 20 °C.

Period of storage - 2 years.

 
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