Стабизол® GEK of 6%

General characteristics. Structure:

Active ingredient: Gidroksietilkrakhmal (GEK 450/0,7) - 60,00 g

Excipients: sodium chloride, water for injections

Theoretical osmolarity: ~ 300 ¼Äß¼«½ý/l

Colloid osmotic pressure: ~ 24 Mbar = 18 mm of mercury.

Value рН: 4,0-7,0

Pharmacological properties:

Pharmacodynamics. Стабизол® GEK of 6% are 6% isotonic solution of a hydroxyethyl derivative product of partial hydrolysis of wax-like corn starch - hydroxyethylstarch (GEK) with an average molecular weight of 450 000 дальтон and extent of substitution 0,7 ± 0,05.

Drug possesses the volemichesky action within 85-100% of the entered volume remaining within 6-8 hours that is caused by ability to connect and hold water, and increase in the volume of the circulating blood (VCB) at the same time is almost equivalent to the entered drug volume.

Physical and chemical parameters of hydroxyethylstarch provide high performance at a hypovolemia and shock, and also when using for therapeutic cultivation of blood (hemodilution) due to normalization of the central and peripheral hemodynamics, microcirculation, improvement of delivery and consumption of oxygen by bodies and fabrics, normalization of permeability of a vascular wall, decrease in local inflammatory reaction, activation of an immune response, mobilization of uniform elements of blood, physiological deposition and their involvement in active metabolism against the background of moderate hemodilution. Besides, drug improves rheological properties of blood and microcirculation, and also a cerebral and fetoplacental blood stream due to decrease in indicators of a hematocrit, and also reduces viscosity of plasma, reduces aggregation of thrombocytes and interferes with aggregation of erythrocytes.

Pharmacokinetics. Elimination of the drug Stabizol® of GEK of 6% results from its disintegration and removal through kidneys. The elimination half-life of the drug Stabizol® of GEK of 6% makes in two-chamber pharmacokinetic model for an alpha phase of 7,9 hours and for a beta phase — 126 hours.

Indications to use:

• prevention and treatment of a hypovolemia and shock at operations, acute blood losses, injuries, infectious diseases and burns;
• therapeutic hemodilution.

Route of administration and doses:

Стабизол® GEK of 6% is appointed in the form of intravenous infusions.

The daily dose and rate of administering depend on the sizes of blood loss and value of an indicator of a hematocrit.

Considering possible anaphylactic reactions, the first 10-20 ml should be entered slowly and at careful observation of a condition of the patient.
Duration of therapy depends on duration and expressiveness of a hypovolemia. At use of drug for hemodilution usually work according to schemes of multi-day therapy.

Daily dose

At substitution of volume of blood the average daily dose makes, as a rule, 250 - 1000 ml. Exceeding of a dosage of 20 ml/kg of weight is only in exceptional cases allowed bodies/days. The total quantity equal of 300 g (5 l) of GEK on a course of treatment (at reusable introduction), it is not necessary to exceed.

At use of the drug Stabizol® of GEK of 6% for hemodilution within several days in a row the daily dose usually makes 500 ml. The general dose making 5 l can be exceeded only in exceptional cases, at the same time the dose can be distributed for the term of treatment by duration up to four weeks.

Rate of administering

In the absence of critical emergency situation the recommended introduction duration - not less than 30 minutes on 500 ml of the drug Stabizol® of GEK of 6%. Data on use for children aged up to 10 years are not available, it is not recommended to use drug at this group of patients.

Features of use:

Emergency measures of the help at emergence of reactions of intolerance:
To stop infusion, a cannula to leave in a vein.

I. Skin reactions                           Antihistaminic drugs
II. Tachycardia, falling                    Antihistaminic drugs and
arterial pressure,                 glucocorticosteroids
 nausea, vomiting.                                (100 mg of Prednisolonum intravenously).
III. Shock, bronchospasm                       1. Epinephrinum (adrenaline) of 0,05 - 0,1 mg
                                                            slowly intravenously.
                                                           2. Glucocorticosteroids (1000 mg
                                                           Prednisolonum in/in).
IV. Cardiac standstill and/or           3. Carrying out resuscitation
breath                                             of the actions hosted
                                                            in such cases.

It is necessary to consider risk of an overload of blood circulation at introduction of too high dose at too high rate of administering.

Treatment should be carried out under control of volume of the circulating blood, the maintenance of ions, leukocytes, thrombocytes, hemoglobin, indicators of a blood coagulation, function of kidneys.

At the beginning of therapy it is required to carry out control of content of creatinine in blood serum. At extreme values of content of creatinine (1,2-2 mg/dl or 106-177 µmol/l - the compensated renal failure) it is necessary to weigh carefully an opportunity and need of performing therapy and it is obligatory to exercise frequent control of liquid balance. It must be kept in mind that hydroxyethylstarch can exert impact on kliniko-chemical indicators (glucose, protein, SOE, fatty acids, cholesterol, a sorbitdegidrogenaza, specific weight of urine).

At the depressed cases caused, mainly, by loss of water and electrolytes (severe vomiting, diarrhea, burns) after initial treatment using the drug Stabizol® of GEK of 6% further treatment by means of the balanced solution of electrolytes is recommended.

During treatment by the drug Stabizol® of GEK of 6% it is necessary to watch that the patient received enough liquid.

The raised doses of the drug Stabizol® of GEK of 6% cause effect of fluidifying and lead to decrease in a hematocrit, and also to decrease in concentration of hemoglobin and a protein of plasma. Values of hemoglobin are lower than 10 g/dl and a hematocrit lower than 27% are considered as critical. At indicators of crude protein <5,0 g/dl, administration of albumine is shown. At losses of blood over 20-25% of the circulating volume of blood obligatory additional introduction of a packed red cells is shown.

At treatment of patients whose blood group is not established it must be kept in mind that introduction of large volumes of GEK can complicate interpretation of results of an agglutination test.

Side effects:

Anaphylactic reactions to hydroxyethylstarch (in terms of the entered quantity of units of infusion solution - about 0,085%). Such reactions are shown in most cases in the form of vomiting, slight increase of temperature, a fever, an itch and a small tortoiseshell. Increase in a submandibular and parotid sialaden, a grippopodobny syndrome (a headache, muscle pain, peripheral hypostases) were observed.

The reactions of intolerance which are followed by shock and life-threatening symptoms (sometimes up to a cardiac standstill and an apnoea) are exclusively rare (in terms of the entered quantity of units of infusion solution – about 0,006%).

At introduction in high doses - the raised bleeding.

At emergence of reaction of intolerance introduction has to be immediately stopped. All necessary emergency measures of the help are at the same time undertaken (see also section "Special Instructions").

Activity of amylase after administration of the drug Stabizol® of GEK of 6% considerably increases in serum, however in 3-5 days returns to normal again. Diagnostic or therapeutic actions are not required.

Gidroksietilkrakhmal at his prolonged use can cause the itch which is badly giving in to stopping which, under certain conditions, can also develop only upon termination of treatment and keep for months.

Interaction with other medicines:

In need of mixing with other medicines (M) the full asepsis has to be observed; when mixing with other medicines in one container or in one system the phenomena of pharmaceutical incompatibility can be observed (it is necessary to be convinced of compatibility of HP). Gidroksietilkrakhmal at simultaneous use with aminoglikozidny antibiotics can increase their nephrotoxicity.

Contraindications:

• hypersensitivity to drug components (including to starch);
• overhydratation;
• hypervolemia;
• hypopotassemia;
• hypernatremia;
• hyperchloremia;
• heart failure in a decompensation stage;
• a renal failure with an oliguria or an anury (creatinine> of 2 mg/dl or, respectively, 177 microns/l).
• fluid lungs (including cardiogenic);
• intracranial bleeding;
• the expressed disturbances of coagulant system of blood (including heavy hemorrhagic diathesis, hypocoagulation);
• hemodialysis;
• dehydration (in need of correction of electrolytic exchange);
• intracranial hypertensia.

With care:
• the compensated chronic heart, liver and renal failure;
• hemorrhagic diathesis;
• children's age up to 10 years;
• chronic diseases of a liver;
• angiohemophilia;
• hypofibrinogenemia.

Use at pregnancy and a lactation

Though it is established that Stabizol® of GEK of 6% has no embriotoksichesky and teratogenic effect, use of drug in the 1st trimester of pregnancy is contraindicated. In the 2 and 3 trimesters of pregnancy of Stabizol® of GEK of 6% it is possible to apply only if the estimated advantage for mother exceeds possible risk for a fruit.

It is unknown whether Stabizol® of GEK of 6% with breast milk therefore women should show care at purpose of this drug in the period of a lactation is allocated. In need of use of drug in the period of a lactation it is recommended to stop breastfeeding.

Overdose:

At introduction of high doses of the drug Stabizol® of GEK of 6% increase in tendency to bleedings is not excluded.

Treatment: symptomatic.

Storage conditions:

To store at a temperature not above 25 °C. Not to freeze!

To store medicine in the place, unavailable to children!

Period of validity of 5 years in original packaging. To use only transparent or poorly opalescent (no more than light yellow color) solutions in the unimpaired bottles. Not to apply after expiry date.

Issue conditions:

According to the recipe

Packaging:

Solution for infusions of 6%.

On 250 or 500 ml in bottles from colourless transparent glass like II (Evr. T.), closed a brombutilovy rubber stopper like I (Evr. T.) for piercing and a plastic cover under an aluminum running in with the plastic holder strengthened on a bottle.

On 10 bottles in a cardboard box with the application instruction (for hospitals).