Апротекс

Апротекс – polyvalent inhibitor of proteases of plasma with anti-fibrinolitic, anti-proteolytic, haemo static action.

Form of release and structure

Dosage forms:

• lyophilisate for preparation of solution for intravenous (in/in) introductions: the lyophilized powder of almost white or white color (in bottles: in a cardboard pack of 1, 5 or 10 bottles; for hospitals – in a cardboard box of 30, 50, 85 or 100 bottles);
• solution for infusions: the transparent slightly painted or colourless liquid (in glass transparent bottles: on 10 ml – in a cardboard pack of 1, 5, 10 or 25 bottles; on 50 ml – in a cardboard pack of 1 or 5 bottles).

1 bottle contains:

• active ingredient: Aprotininum – 10 000 anti-tryptic units (ATRE) or 100 000 ATRE;
• auxiliary components: lactose, sodium hydroxide.

1 ml of solution contains:

• active ingredient: Aprotininum – 10 000 kallikrein of the inactivating units (KIU);
• auxiliary components: sodium chloride, water for injections.

Indications to use

• acute pancreatitis, exacerbation of chronic pancreatitis, prevention of postoperative pancreatitis, pancreatonecrosis;
• prevention of embolisms at polyinjuries and after operation;
• hyper fibrinolitic bleedings in posttraumatic, postoperative (especially after lung, prostate operation) the period, at a polymenorrhea, before childbirth, in time and after them, at an embolism amniotic waters;
• complications of thrombolytic therapy;
• the coagulopathy which is characterized by a secondary hyper fibrinolysis;
• prevention of bleedings at surgical intervention on open heart using the cardiopulmonary bypass;
• traumatic, endotoxic or hemolitic shock (treatment and prevention of development);
• prevention of postoperative parotitis.

Contraindications

• I and III trimesters of pregnancy;
• syndrome of the disseminated intravascular blood coagulation (IDCS) (except a coagulopathy phase);
• breastfeeding;
• hypersensitivity to protein of cattle;
• individual intolerance of components of drug.

With care it is recommended to appoint Aproteks to patients with allergic reactions in the anamnesis, at the cardiopulmonary shunting operations, a blood circulation stop when carrying out operation using the cardiopulmonary bypass, the deep hypothermia preceding therapy by Aprotininum in case of reception of muscle relaxants in 2-3 days prior to administration of drug, in the II trimester of pregnancy (only according to vital indications).

Route of administration and dosage

Lyophilisate and solution enter in/in struyno (slowly, up to 5 ml a minute) or kapelno and intraperitoneally. During Aproteks's use the patient has to be in horizontal position.

Lyophilisate
For preparation of solution from lyophilisate with a dosage of 10 000 ATRE add 2 ml of isotonic solution of sodium chloride to contents of 1 bottle, with a dosage of 100 000 ATRE – 20 ml.

The recommended daily mode of dosing:

• bleedings: an initial dose – 300 000 ATRE, then in/in struyno every 4 hour on 140 000 ATRE before normalization of a hemostasis;
• acute pancreatitis: in/in struyno (slowly) – 200 000-300 000 ATRE once, then in/in kapelno – 200 000-300 000 ATRE a day. Treatment is continued before normalization of laboratory indicators and a clinical condition of the patient;
• prevention of postoperative pancreatitis: in/in struyno – 200 000 ATRE;
• depressed cases: an initial dose – 200 000-300 000 ATRE, then in/in struyno on 140 000 ATRE every 4 hour;
• the coagulopathy which is defined by a secondary hyper fibrinolysis: on 750 000 ATRE above;
• prevention of a fatty embolism: in/in (slowly) – 200 000 ATRE daily.

At a pancreatonecrosis with the exudate in an abdominal cavity containing enzymes in addition to in introduction of Aproteks it is possible to appoint intraperitoneally.

Besides, solution of lyophilisate is applied locally at treatment of long insignificant bleedings. For this purpose the gauze napkin impregnated with solution (75 000 ATRE) is put to the place of bleeding.

At disturbances of a hemostasis at children drug is appointed from calculation for 15 000 ATRE to 1 kg of weight of the child a day.

Solution for infusions
The recommended dosing:

• the bleedings and hemorrhages connected with a hyper fibrinolysis: in/in kapelno – 100 000-200 000 KIE, at intensive bleeding – to 500 000 KIE;
• exacerbation of chronic pancreatitis: once 25 000 KIE an hour, a course of treatment – 3-6 days. The maximum daily dose – 50 000 KIE;
• acute pancreatitis: an initial dose – 500 000-1 000 000 KIE, further it is necessary to reduce gradually within 2-6 days a dose to 50 000-300 000 KIE, treatment is continued before total disappearance of a fermental toxaemia;
• coagulopathy in combination with a secondary hyper fibrinolysis: 1 000 000 KIE above;
• prevention of bleedings at surgery (to, in time and after intervention): in/in struyno or kapelno – 200 000-400 000 KIE in the first days, then on 100 000 KIE during the next two days;
• obstetric practice: an initial dose – 1 000 000 KIE, then on 200 000 KIE each hour until a full stop of bleeding. Topical administration by means of the tampons impregnated with drug in concentration of 100 000 KIE is at the same time shown, they should be put to the bleeding center;
• postoperative period, prevention of injury of a pancreas: an initial dose – 200 000 KIE, then on 100 000 KIE every 6 hours within two days after operation;
• disturbance of a hemostasis at children: from calculation for 20 000 KIE on 1 kg of body weight.

At an acute necrosis of a pancreas with a fermental exudate in an abdominal cavity, against the background of in addition enter solution into uses of Aprotininum by the patient intraabdominalno.

Side effects

• alimentary system: against the background of bystry introduction – nausea and vomiting of passing character;
• cardiovascular system: tachycardia, lowering of arterial pressure; against the background of high (6 000 000 - 9 000 000 ATRE, or 8 000 000-12 000 000 KIE) Aprotininum doses – increase in risk of development of a myocardial infarction at repeated shunting of coronary vessels;
• allergic reactions: skin itch, small tortoiseshell, conjunctivitis, rhinitis, bronchospasm, anaphylaxis, acute anaphylaxis;
• nervous system: confusion of consciousness, hallucination, psychotic reactions;
• local reactions: at long therapy – thrombophlebitis in the place of an injection;
• others: mialgiya.

Special instructions

Because of big risk of an anaphylaxis Aproteks's use is recommended to be begun after test for hypersensitivity definition. For this purpose the sick 1 ml (10 000 KIE) of Aprotininum needs in/in to enter. At absence within 10 minutes after introduction of a trial dose of signs of allergic reaction it is possible to start introduction of a therapeutic dose, otherwise – use of Aprotininum is forbidden.

In need of purpose of drug patients with the increased risk of development of allergic reactions should enter antihistamines previously. At emergence of symptoms of an allergy introduction of Aprotininum is cancelled immediately. Previous (during from 2 to 24 weeks) therapy by drug increases risk of development of allergic reactions.

At a trombogemorragichesky syndrome drug can be used only after elimination of all disturbances of a blood coagulation against the background of simultaneous preventive purpose of heparin.

Because of risk of development of a renal failure and a lethal outcome with extra care it is necessary to apply Aproteks at a blood circulation stop during operation with use of the cardiopulmonary bypass. When using extracorporal blood circulation in the course of heart operation at the patients receiving high doses of Aprotininum it is necessary to support time of the activated coagulability of blood at the level of higher than 750 seconds. Level of heparin is measured by titrating geparino-prothrombin test.

Influence of drug on ability of the patient to control of vehicles and mechanisms is not established.

Medicinal interaction

Апротекс suppresses action of an urokinase, Streptokinasa, alteplaza and other fibrinolitic means.

Exponentiates effect of heparin, at addition of Aprotininum to a heparinized blood time of coagulation of whole blood increases.

Simultaneous use with drugs of a dextran causes mutual strengthening of action.

Pharmaceutical we will combine only with solutions of electrolytes and Dextrosums.

Terms and storage conditions

To protect from children.

To store at a temperature up to 25 °C, lyophilisate – in the place protected from light.

Period of validity: lyophilisate – 3 years, solution – 2 years.