KONTRIVEN

General characteristics. Structure:

Active ingredient: Aprotininum – 10 000 KIE in 1 ml of drug;

excipients: sodium chloride; water for injections.

Main physical and chemical properties: transparent, colourless or with a yellowish shade liquid.

Pharmacological properties:

Pharmacodynamics. Aprotininum inhibits activity of proteases – proteolytic enzymes which accelerate the proteolysis and products of their disintegration – polypeptides. Slows down effect of plasmin, trypsin, plasma and fabric kallikrein that causes a possibility of its therapeutic effect and use as an antifibrinolitik, and also for prevention and treatment of other fermental systems.

Pharmacokinetics. After intravenous administration Aprotininum is quickly distributed in extracellular space, quickly collects in a liver and is brought out of an organism by kidneys within 48 hours. Disintegration of a molecule of Aprotininum to inactive particles happens due to lizosomalny activity of kidneys. Decomposition products are excreted with urine.

Indications to use:

Bleedings owing to activation of a fibrinolysis.

Route of administration and doses:

The drug is administered in the form of an intravenous injection (slowly) or intravenous drop  infusion, parting in 300-500 ml of isotonic solution of sodium of chloride. At administration of drug of the patient has to be in a prone position. For definition of possible hypersensitivity to drug in 10 minutes prior to its introduction it is recommended to enter a test dose in number of 1 ml of drug ( 10 000 KIE of Aprotininum).

If allergic reaction to a test dose, drug is defined it is impossible to use.

If during administration of drug intravenously or in the form of infusion there are reactions of hypersensitivity or intolerance, administration of drug should be stopped immediately.

At bleedings:

To adults and children 15 years an initial dose are more senior makes 500 000 KIE (50 ml of drug) intravenously slowly (the maximum speed - 5 ml/min.).

For preservation of the reached level of concentration of drug in blood introduction is continued in the form of long drop infusion ( to 200 000 KIE there are each 4 hours).

To children aged from 6 up to 15 years the daily dose makes 20 000 KIE on kilogram of body weight.

To elderly patients: there are no special instructions.

It is impossible to use drug if viyavleno opacification of contents of an ampoule. After opening of an ampoule not обходимо immediately to apply solution.

Features of use:

Drug can be used only in the conditions of a hospital. For detection of possible hypersensitivity to drug, before introduction of its full dose (not less than in 10 minutes), it is recommended to enter a test dose (see the section "Route of Administration and Doses"). Antihistaminic drugs are recommended to patients with the increased risk of development of allergic reactions before Kontriven's use. At emergence of allergic reactions and anaphylactic symptoms administration of drug it is necessary to stop immediately and provet the corresponding therapy.

The risk of development of reactions of hypersensitivity or intolerance is especially high for patients to whom Aprotininum was entered in 15 days – 6 months prior to the carried-out treatment. In the presence of allergic diathesis administration of drug can cause pseudo-allergic reaction in this connection to administer the drug to patients of a sleduyetpra careful control and obligatory use of a test dose. At the same time it is necessary to remember that introduction of a full dose of drug can cause allergic (anaphylactic) reaction even if the test dose of such reaction did not cause. Just before administration of drug such patients are recommended to enter intravenously the medicines blocking _N1-and _H2-histamine receptors (for example, Cimetidinum).

Ability to influence speed of response at control of motor transport or work with other mechanisms. It was not studied.

Side effects:

At drug use (most often at repeated courses of therapy) there can be anaphylactic or anaphylactoid reactions.

In certain cases at introduction of the first dose of drug anaphylactic reaction was revealed. Symptoms of anaphylactic or anaphylactoid reactions can vary from skin rash, an itch, an asthma, nausea, tachycardia before development of an acute anaphylaxis (that is followed by a circulatory unefficiency) that in certain cases can lead to the death of the patient.

At emergence of allergic reactions administration of drug should be stopped immediately and if necessary to carry out an intensive care (administration of adrenaline, additional liquid, corticosteroids).

Interaction with other medicines:

Drug should not be mixed with other medicines, including antibiotics (are incompatible) with a beta laktamnymi. Administration of drug together with the solutions containing a dextran with corticosteroids, solutions for parenteral food, the containing amino acids and lipids is forbidden.

Depending on a dose Kontriven lowers activity of Streptokinasa and urokinase. Can suppress activity of nonspecific cholinesterase of blood serum. At patients with hypoactivity of nonspecific cholinesterase at simultaneous use of an aprotininaa of succinylcholine developing of an apnoea is possible that is caused by a muscular relaxation. Administration of drug in a heparinized blood increases time of turning of whole blood.

Contraindications:

Hypersensitivity to Aprotininum. The disseminated intravascular blood coagulation (IDCS), І a pregnancy trimester.

Overdose:

It was not observed. The antidote does not exist.

Storage conditions:

Хранитьв the dry, protected from light place at  a temperature from 2 °C to 8 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 5 ml (10 000 KIE) in an ampoule. On 5 ampoules in a pack.