Конфумин®

General characteristics. Structure:

Active ingredient: 150 g of sodium of a fumarat.

Excipients: water for injections.

Pharmacological properties:

Pharmacodynamics. Pharmacological active component of Konfumin is the fumarating sodium. Fumarates sodium – an antigipoksant who activates adaptation of a cell to a lack of oxygen. Its action is caused by participation in reactions of reversible oxidation and recovery in a tricarbonic acid cycle. In the course of these reactions there is an ATP synthesis necessary for maintenance of functions of cells of an organism at a hypoxia. At deficit of oxygen the pool of substrates of oxidation including ions of a fumarat it is exhausted, and replenishment in its exogenous way (introduction as a part of drug Konfumin) promotes increase in reserve power of the systems of tissue respiration allowing cells to synthesize ATP in the conditions of a hypoxia. These reactions provide the mechanism of anti-hypoxemic effect of drug Konfumin.

Maintenance of processes of oxidizing metabolism in fabrics at oxygen insufficiency interferes with education and accumulation of nedookislenny products of exchange, reducing thereby, an acidemia. Along with metabolic alkalization Konfumin promotes easing or elimination of an acidemia and by chemical neutralization of acid products of metabolism. Fumarates sodium – the salt formed by the strong basis and weak acid. At Konfumin's introduction to a circulatory bed of the fumarating sodium is exposed to hydrolysis with formation of fumaric acid and the strong basis (NaOH). The last is spent for neutralization of acid products of exchange, and fumaric acid is used for ATP synthesis.

The beneficial effect of Konfumin on oxidizing metabolism in fabrics allows to improve in the conditions of a hypoxia a functional condition of vitals, including, and hearts. Drug maintains sokratitelny ability of a myocardium, possesses cardiotonic action.

Konfumin's use promotes decrease in blood of concentration of products of peroxide oxidation of lipids that testifies to its antioxidant properties. Drug Konfumin is a hypertonic salt solution of a fumarat of sodium and its introduction to a circulatory bed leads to mobilization of endogenous liquid with increase in intravascular volume, providing volemichesky effect of drug. Konfumin's ability to increase the volume of the circulating blood along with its positive influence on cardiac effeciency, defines hemodynamic effect of drug (increase in stroke and minute output of heart, increase in the ABP and so forth). These properties of Konfumin allow to use it as means of a low-volume volyumokorrektion.

Pharmacokinetics. At Konfumin's infusion, entered into an organism exogenous fumarating completely on chemical structure it is identical to an endogenous fumarat. Therefore, when determining content of substrate in cells it is impossible to identify the component which arrived from the outside. Besides, it is known that fumarating it is capable to turn into succinate, malate, oxaloacetate (tricarbonic acid cycle), and also into aspartate (an ornitinovy cycle) and other metabolites.

In experiments with use of a tracer technique it was established that at introduction in cells of bodies other substrates of oxidation decided afterwards on a radioactive label by an animal of a marked fumarat. Therefore, in an organism high-mobile mechanisms of utilization of a fumarat work. Thus, after Konfumin's infusions fumarating completely it is metabolized. Being giperosmolyarny, Konfumin contains osmotically active component – sodium ions. Maintenance of an osmotic and ionic homeostasis at Konfumin's introduction is provided employment kidneys.

The mechanism of excretion of ions of sodium from an organism is well-known and is provided took away -
cheniye of renal filtering, diuresis and salurez.

Indications to use:

Hypoxemic conditions of various etiology at a hypovolemia (blood loss, shock, injuries, burns, intoxications, etc.).

Route of administration and doses:

Konfumin is recommended to use as a component in schemes of infusion-transfusion therapy of hypovolemic states. The dose and rate of administering of drug should be chosen according to indications and a condition of the patient.

At blood loss and shock (hemorrhagic, traumatic, septic, etc.) for elimination of metabolic disturbances 100 ml (single dose) of Konfumin intravenously kapelno against the background of basic infusion-transfusion therapy enter. If repeated administrations of blood-substituting solutions are required, they can be also combined with Konfumin's infusions, the interval between administration of drug has to be not less than 6 hours, the daily dose should not exceed 300 ml.

When using Konfumin's not only as an antigipoksant, but also as means of a low-volume hyperosmotic volyumokorrektion, the dose of drug is calculated taking into account the body weight of the patient, the drug needs to be administered struyno or kapelno in a dose of 2,2-2,4 ml/kg with simultaneous infusion of colloid, and then and crystalloid solutions by the standard technique.

Features of use:

Use at pregnancy and during feeding by a breast. There is no clinical experience of use of Konfumin for women during pregnancy and a lactation. However, teratogenic and embriotoksichesky action of a fumarat is studied in animal experiments. It is established that drug does not influence negatively emergence and the course of pregnancy and does not possess teratogenic and embriotoksichesky action. At the same time, if there is a need of use of Konfumin for pregnant women and the feeding women, it is necessary to estimate carefully possible risk and effect of use of drug for this category of patients.

In the early post-infusional period at patients after Konfumin's introduction it is necessary to control a condition of electrolytic structure of a blood plasma (concentration of potassium ions, sodium).

In exceptional cases individuals can have allergic reactions of various type up to the anaphylactic or anaphylactoid phenomena. It is necessary to stop immediately administration of drug and to hold the standard urgent events.

At high rate of administering of drug emergence of burning sensation and morbidity on the course of a vein to which drug infusion is carried out is possible. Any negative effects on ability of driving are noted.

Data on safety of use in preclinical trials. It is experimentally established that drug Konfumin is almost not toxic. Acute toxicity of a fumarat of sodium does not exceed acute toxicity of sodium chloride. Konfumin does not collect in bodies and fabrics at prolonged use in a therapeutic dose. Having medical effect, he does not give adverse side effects as during its biotransformation toxic products are not formed.

The fumarating sodium is not among carcinogens. It is established what the fumarating sodium increases resistance of an organism to various supernormal influences (physical overworks, a lack of oxygen, a hypercapnia, cold influences, etc.), t. е is a universal adaptogen.

Side effects:

Side effect of drug is not revealed.

Interaction with other medicines:

Konfumin is allowed to enter in combination with colloid environments (on the basis of a dextran, gelatin, hydroxyethylstarch, polyethyleneglycol, etc.) and crystalloid solutions (normal saline solution of sodium chloride, Ringer's solution, лактасоль, disalt, Acesolum, etc.). Konfumin's use in schemes of treatment assumes a possibility of administration of drug together with transfusion of donor blood, the erythrocontaining environments, plasma and other blood preparations.

Konfumin's use does not interfere also with use of usually applied medicines from among the anesthetizing drugs, barbiturates, tranquilizers, hormones, inhibitors of proteases (Contrykal, Gordoxum). At combined use of Konfumin with other drugs visually to control compatibility.

Contraindications:

The morbid conditions which are followed by a hypernatremia and hyper osmolarity of a blood plasma, hypersensitivity, children's age.

Overdose:

At use of excess doses drug causes short-term excitement, for
to which the oppression disappearing within 3-5 hours follows.

Treatment: drug withdrawal, performing symptomatic therapy.

Storage conditions:

To store in dry, unavailable to children, the place at a temperature from 0 to 25 °C. Freezing of drug at transportation is allowed. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Solution for infusions on 50 or 100 ml in containers polymeric for infusion solutions of single use from polyvinylchloride or from the polyolefin film. Each container is packed into a secondary package of the application instruction applied on it. The secondary package is made of polypropylene. Containers in secondary packaging place in a transport container (boxes from corrugated fibreboard). Containers from the polyolefin film can be packed into a transport container (boxes from corrugated fibreboard) without secondary package (for hospitals). With containers put application instructions in the quantity equal to the number of containers in a box.