Antithrombin III human

Antithrombin III human – antithrombin III drug, anticoagulant of direct action.

Form of release and structure

Dosage form – lyophilisate for preparation of solution for infusions: the friable firm mass or powder of pale green or pale yellow color (on 500 international units (IU) in bottles, in a cardboard box 1 bottle and a set for dissolution and introduction: 1 bottles of solvent (10 ml), needle filter, one-time needle, needle adapter, needle - "butterfly", airwater needle; on 1000 ME in bottles, in a cardboard box 1 bottle and a set for dissolution and introduction: 1 bottles of solvent (20 ml), needle filter, one-time needle, needle adapter, needle - "butterfly", airwater needle).

Active agent of Antithrombin III human – antithrombin III, in 1 ml of ready solution – 50 ME (1 ME solutions it is equivalent to activity of antithrombin III in 1 ml of normal fresh plasma of the person), crude protein – 20-50 mg.

Auxiliary components: Tris (hydroxymethyl) aminomethane, sodium chloride, Dextrosums monohydrate, citrate sodium dihydrate.

Solvent: water for injections.

Indications to use

Use of Antithrombin III human is shown to patients with the inborn or acquired insufficiency of antithrombin III in a blood plasma. The acquired insufficiency of antithrombin can be a consequence of various clinical disturbances, including the increased consumption or loss of protein, antithrombin synthesis disturbance.

Drug is appointed for prevention of trombotichesky and tromboembolic episodes by the patient with activity of antithrombin in plasma by less than 70% of the established norm.

Indications for introduction:

• surgeries at patients with inborn insufficiency of antithrombin III;
• the period pregnancy and childbirth at patients with inborn insufficiency of antithrombin III;
• thrombosis at patients with inflammatory diseases of a bladder or a nephrotic syndrome, or risk of its development;
• syndrome of the disseminated intravascular blood coagulation or risk of its development at the septic complications, the combined injury, a preeclampsia, shock and other states connected with an acute consumption coagulopathy;
• surgical intervention or bleeding at a heavy liver failure, especially at the patients who are on therapy by concentrates of factors of coagulation;
• absence or insufficient answer to heparin.

Contraindications

• the instruction in the anamnesis on heparin - the induced thrombocytopenia;
• age up to 6 years;
• hypersensitivity to drug components.

During pregnancy and breastfeeding human it is possible to appoint Antithrombin III only according to vital indications.

Route of administration and dosage

Lyophilisate is intended for intravenous (in/in) drop introductions.

Infusion solution is prepared before direct introduction, using the set enclosed for dissolution and introduction and strictly following rules of an asepsis and antiseptics. Heating still the closed bottle with solvent up to the temperature is not above 37 °C, having exempted bottles with lyophilisate and solvent from protective covers, rubber bungs on each of bottles should be disinfected. Having exempted since one end from a protective cap a needle adapter, to pierce a needle a bottle stopper with solvent. Without touching a needle, to remove a protective cap from other its end. Then, having turned a bottle with solvent, the free end of a needle it is necessary to pierce a rubber bung of a bottle with lyophilisate and under the influence of vacuum solvent will come to a bottle with lyophilisate. After removal of a needle from a bottle with drug easy rotation or rocking it is necessary to accelerate lyophilisate dissolution. For sedimentation of the formed foam after full dissolution of drug the stopper of a bottle is pierced an airwater needle and then deleted. The intake of the prepared solution is made by the one-time sterile syringe with the put-on needle filter. Having visually investigated solution and having convinced of lack of a turbidity or foreign inclusions, it is necessary to change a needle filter for a needle - "butterfly". Then it is necessary slowly in/in to enter solution, without exceeding the most admissible rate of administering – 5 ml a minute. Unused solution needs to be utilized according to the established rules.

The doctor with experience of therapy of insufficiency of antithrombin has to carry out purpose of drug and treatment.

The dose at inborn insufficiency is chosen for each patient individually, taking into account the family anamnesis of rather thromboembolic states, results of laboratory researches and the existing clinical risk factors.

Initial dose at inborn insufficiency usually appoint from calculation on 30-50 ME to 1 kg of weight. Further the single dose, frequency rate of introduction and duration of treatment are adapted to indicators of biochemical researches and a clinical condition of the patient.

The dose, frequency of introduction and the period of replacement therapy for each patient with the acquired insufficiency are defined on the basis of biochemical indicators of level of antithrombin in plasma, considering the diagnosis of a basic disease, the available signs of the increased metabolism of antithrombin and severity of a clinical state.

Proceeding from empirical data, when calculating a necessary dose use compliance in which for increase in activity of antithrombin in plasma of the person approximately for 2% it is necessary to enter on 1 ME antithrombins on 1 kg of body weight.

For definition of an initial dose of drug (ME) it is necessary to increase the nominal body weight of the patient by a difference between the target and initial objective of activity of antithrombin (which are expressed as a percentage) and to increase on 0,5.

Initial target activity of antithrombin has to be the established pathology, sufficient for achievement of target activity of antithrombin at replacement therapy. For maintenance of effective level it is necessary to take laboratory measurements of activity of antithrombin not less than 2 times a day, it is desirable – just before the following administration of drug. At the increased antithrombin metabolism the dose should be adjusted.

Activity of antithrombin throughout a course of therapy should be maintained at the level of higher than 80% (normal activity of antithrombin at adults – 80-120%) in the absence of need for maintenance of other effective level connected with clinical features.

Side effects

• cardiovascular systems: lowering of arterial pressure (ABP), tachycardia, reddening of integuments;
• alimentary system: nausea, vomiting;
• immune system: skin rash, allergic reactions (including hypersensitivity), a Quincke's disease, a heavy anaphylaxis (including shock), a generalized small tortoiseshell;
• nervous system: concern, a headache, feeling of a pricking in a body;
• respiratory system: goose breathing;
• laboratory and tool indicators: decrease in maintenance of thrombocytes twice or quantity of thrombocytes less than 100 000/mkl;
• general reactions: drowsiness, a fever, constraint in breasts, heparin - the induced thrombocytopenia with antibodies (type II), fever;
• local reactions: burning and a pricking in an injection site.

Special instructions

Because of risk of development of allergic reactions and hypersensitivity during the entire period of infusion it is necessary to watch a condition of the patient carefully. Prior to treatment of patients it is necessary to inform on possible development of early symptoms of reactions of hypersensitivity which a generalized small tortoiseshell, decrease in the ABP, feeling of constraint in a breast, goose breathing, an anaphylaxis, and about need of the immediate message to the doctor in case of their emergence treats.

Use of drug has to be carried out in the presence of means of antishock therapy.

At in administration of the drug made of a blood plasma or blood of the person infection with the casing-free virus, such as B19 parvovirus constituting serious danger to patients with an immunodeficiency or increased by an erythrogenesis (including hemolitic anemia) and pregnant women (risk of infection of a fruit) is possible.

The patient should be vaccinated against the hepatitises A and B at regular or repeated purpose of the drugs of antithrombin received from plasma of the person.

The specific patient needs carrying out registration of number of a series and the name of each entered Antithrombin III human.

From first minutes after the beginning of administration of antithrombin at combined use with heparin it is necessary to control often and regularly extent of anti-coagulation for the purpose of dose adjustment of heparin and prevention of excess decrease in coagulability of blood. Also because of the existing risk of decrease in level of antithrombin against the background of prolonged use of unfractionated heparin daily measurement of level of antithrombin and correction of an individual dose if necessary is required.

Antithrombin does not influence ability of the patient to control of vehicles and mechanisms.

Medicinal interaction

At simultaneous use of replacement therapy by antithrombin with heparin in therapeutic doses:

• the risk of bleeding increases;
• effect of antithrombin amplifies;
• metabolism of antithrombin accelerates, causing essential decrease _{in T1/2} of antithrombin.

Therefore at the increased risk of bleeding combined use of heparin and antithrombin should be accompanied with careful control of a clinical condition of the patient and his biochemical data.

It is impossible to mix Antithrombin III human with other medicines.

Terms and storage conditions

To protect from children.

Not to freeze, store at a temperature of 2-8 °C.

Period of validity – 3 years.