Pharmacological properties

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

Pharmacokinetics. Later in/in introductions Aprotininum is quickly distributed in extracellular space, quickly collects in a liver and is removed from an organism by kidneys during 48 h. Disintegration of a molecule of Aprotininum to inactive particles happens due to lizosomalny activity of kidneys. Decomposition products are excreted with urine.

Indication

Bleeding owing to activization of a fibrinolysis.

Use

Drug kontriven is administered in a look in/in an injection (slowly) or in in drop infusion, parting in 300–500 ml of isotonic solution of sodium of chloride. at administration of medicament of the patient has to be in a prone position. for determination of possible hypersensitivity to medicament in 10 min. prior to its introduction it is recommended to enter a test dose in number of 1 ml of medicament (10,000 Kia of Aprotininum).

it is impossible to use.

If during administration of medicament in/in or in the form of infusion reactions of hypersensitivity or intolerance arise, administration of medicament should be stopped immediately.

In bleeding:

makes 500,000 KIE (50 ml of drug) in/in slowly (the maximum speed — 5 ml/min.).

For preservation of the reached level of concentration of medicament in blood introduction is continued in the form of long drop infusion (200,000 KIE each 4 h).

to Children at the age of 6–15 years the daily dose makes 20,000 KIE on kg/body weight.

For patients of advanced age of special instructions.

Cannot use medicament if turbidity of contents of an ampoule is revealed. After opening of an ampoule, solution needs to be used immediately.

Contraindication

Hypersensitivity to Aprotininum; IDCS, і pregnancy trimester.

Side effects

At medicament use (most often at repeated courses of therapy) can arise anaphylactic or anaphylactoid reactions.

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

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

Special instructions

can use Drug only in the conditions of a hospital. for identification of possible hypersensitivity to medicament before introduction of its full dose (not less than in 10 min.) it is recommended to enter a test dose (see use). antihistaminic medicaments are recommended to patients with the increased risk of development of allergic reactions before use of a kontriven. at emergence of allergic or anaphylactic reactions the administration of medicament should be stopped and carried out immediately the corresponding therapy.

for patients to whom Aprotininum was entered in 15 days — 6 months prior to the beginning of the carried-out treatment. In the presence of atopic diathesis the administration of medicament can cause pseudo-allergic reaction in this connection patients should administer the medicament at 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 medicament can cause allergic (anaphylactic) reaction even in case the test dose of such reaction did not cause. Just before administration of medicament such patients are recommended in/in to enter medicines, the blocking N ₁ — and N ₂ - histamine receptors (for example Cimetidinum).

Incompatibility. Kontriven it is not necessary to mix with other medicines, including with β-laktamny antibiotics, a dextran, corticosteroids, medicaments of parenteral nutrition (see INTERACTIONS).

Use during pregnancy and feeding by a breast. Use of medicament in II or III trimester of pregnancy and during feeding by a breast perhaps only if the expected advantage for mother exceeds potential risk for the fruit/child.

.

Children. See USE. Experience of use of medicament for children under 6 years insufficient.

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

Interaction

Drug should not be mixed with other medicines, including (are incompatible) with β-laktamny antibiotics. administration of medicament together with the solutions containing a dextran with gks, the solutions for parenteral nutrition containing amino acids and lipids is forbidden.

Depending on a dose Kontriven reduces activity of streptokinase and an urokinase. Can suppress activity of nonspecific cholinesterase of blood serum. At patients with reduced activity of nonspecific cholinesterase at simultaneous use of Aprotininum and succinylcholine of chloride the developing of an apnoea is possible that is caused by a muscular relaxation. Administration of medicament in heparinized blood increases time of coagulation of whole blood.

Overdose

. antidote does not exist.

Storage conditions

B the dry, protected from light place at a temperature of 2-8 s.

Translation of the instruction Mose