Producer: CJSC Generium Russia
Code of automatic telephone exchange: B02BD08
Release form: Liquid dosage forms. Lyophilisate for solution preparation.
General characteristics. Structure:
Active ingredient: 1,2 mg, 2,4 mg or 4,8 mg of an eptakog alpha (activated).
Excipients: sodium chloride, Calcii chloridum dihydrate, glycylglycine, polysorbate-80, Mannitolum.
Solvent: water for injections.
Эптаког an alpha [activated] - the recombinant factor of coagulation of VIIA received by method of genetic engineering from cells of kidneys of hamsters (VNK-cell). Molecular weight approximately makes 50000 дальтон.
Pharmacodynamics. The mechanism of action consists in linkng of blood-coagulation factors of VIIA with the released fabric factor in a damage zone. The formed complex stimulates transition of blood-coagulation factors of IX and X in the active IHa form and Xa. Then the blood-coagulation factors of Xa start initial processes of transformation of a prothrombin (II) into thrombin. Thrombin provides with way of transformation of fibrinogen to fibrin formation of a haemo static stopper, and also promotes activation of thrombocytes and blood-coagulation factors of Vi VIII in a damage zone. In pharmacological doses эптаког the alpha [activated] directly without participation of a fabric factor transfers blood-coagulation factors of X to the active Xa form on surfaces of the activated thrombocytes in a damage zone that leads to formation of large amounts of thrombin from a prothrombin.
Thus, the pharmakodinamichesky effect of recombinant blood-coagulation factors of VIIA consists in the strengthened local formation of blood-coagulation factors of Xa with the subsequent acceleration of synthesis in the cascade of enzymatic reactions of coagulant system of blood of thrombin and fibrin. At use of an eptakog an alpha [activated] it is impossible to exclude completely risk of system activation of a blood coagulation at the patients having the diseases contributing to development of the IDCS.
Pharmacokinetics. According to literature the elimination half-life of recombinant blood-coagulation factors of VIIA at adults makes 2-2,5 hours, at children the elimination half-life is shorter. The average clearance of recombinant blood-coagulation factors of VIIA makes 31,8 ml/hour/kg, the clearance at children is higher on average twice.
Indications to use:
For a stop of bleedings and prevention of their development when carrying out surgical interventions and invasive procedures in patients with
- hemophilia (hereditary or acquired) with a high caption of inhibitor to VIIIILI IX blood-coagulation factors;
- inborn deficit of blood-coagulation factors of VII;
- Glantsman's thrombasthenia in the presence of antibodies to glycoproteins of IIb-IIIa and a refrakternost (in the present or the past) to transfusions of a platelet concentrate.
Route of administration and doses:
Inhibitory hemophilia And or In or the acquired hemophilia. At development of bleeding it is necessary to enter Koagil-VII as soon as possible. The dose is selected individually. The drug is administered intravenously bolyusno (within 2-5 minutes). Usually initial dose makes 90 mkg/kg. After the first injection it is possible to repeat administration of drug each 2-3 hours before achievement of a hemostasis. In the presence of indications for treatment continuation intervals between administrations of drug can be consistently increased up to 4, 6, 8 or 12 hours by the entire period of treatment. Duration of treatment and an interval between administrations of drug are defined by weight of bleeding, and also the nature of invasive interventions or surgery.
Bleedings easy and moderate severity (including out-patient treatment). An initial dose - 90 mkg/kg. For providing a hemostasis enter 1-3 doses of drug with 3-hour intervals to a bleeding stop. For maintenance of effect enter one more dose. The mode of single introduction of a dose at the rate of 270 mkg on body weight kg is possible. Duration of out-patient treatment should not exceed 24 hours. Early administration of drug allows to control effectively bleedings easy and moderately severe in joints, muscles, skin and mucous membranes.
Bleedings of heavy degree. The dose of drug makes 90 mkg/kg and can be entered at a transportation stage into clinic. The further scheme of treatment depends on type and weight of bleeding. The drug is administered each two hours to a bleeding stop. In the presence of indications for therapy continuation intervals between administrations of drug can be increased till 3 o'clock within 1-2 days. In the subsequent, intervals between administrations of drug can be increased up to 4, 6, 8 or 12 hours by the entire period of treatment. Depending on indications duration of treatment can make 2-3 weeks and more.
Invasive interventions / surgeries. Just before intervention or operation the dose is entered. 90 mkg/kg. The second dose is entered in 2 hours, and then the drug is administered with 2-3 hour intervals for the first 24-48 hours. At big operations treatment continues 6-7 days with 2-4 hour intervals between introduction of doses. When performing treatment for the next 2 weeks intervals between administrations of drug can be increased till 6-8 o'clock. The general duration of use of drug can make 2-3 weeks.
Deficit of a factor of VII. The recommended doses for a stop of bleedings and prevention of their development at surgeries or invasive interventions make 15-30 mkg/kg of body weight. The drug is administered each 4-6 hours before achievement of a hemostasis.
Glantsman's thrombasthenia. The dose for control of bleedings and prevention of bleedings when carrying out surgeries or invasive interventions makes 90 mkg (80-120 mkg) / body weight kg. The drug is administered each 2 hours. Providing a resistant hemostasis requires not less than three doses. The main method of treatment of patients with Glantsman's thrombasthenia without refrakternost is use of a platelet concentrate.
Rules of preparation of injection solutions:
1. Heat bottles with the drug Koagil-VII (lyophilisate) and ampoules with water for injections to room temperature (but not higher than 37 ° C), for example: having taken a bottle and an ampoule at itself in hands.
2. Remove a protective cap from a bottle.
3. Process a rubber bung of a bottle and a neck of an ampoule spirit tampons. Let's them dry before use.
4. Open the blister packaging of the syringe, having unbent a paper covering to the middle.
5. Open the blister packaging of a needle, having unbent a paper covering to the middle.
6. Put on a sterile needle the syringe, without taking out it from a protective cap. You watch that the tip of the syringe did not adjoin to a hand or other surface. Postpone the syringe with a needle until the following manipulation.
7. Open an ampoule with water for injections.
8. Remove a protective cap from a needle.
9. Gather in the syringe the following amount of water for injections:
· for a bottle with a dosage of 1,2 mg – 2 ml;
· for a bottle with a dosage of 2,4 mg – 4 ml;
· for a bottle with a dosage of 4,8 mg – 8 ml.
(ml are equal to cm3 on the syringe)
10. Enter the necessary volume of water for injections through the same needle into a bottle with a necessary dosage of the drug Koagil-VII, slowly pressing a piston rod. You keep the syringe in slightly inclined state in a downward direction. The stream of water should not get directly on lyophilisate as it can cause "foaming".
11. Carefully rotate a bottle until all substance is dissolved. Do not stir up a bottle. Make sure that powder was completely dissolved.
12. Keeping a bottle in the turned state ("upside down"), gather from it solution in the syringe, having slowly and smoothly delayed the piston. Make sure that all contents of a bottle are gathered in the syringe.
13. Without changing position of the piston, remove a needle from the syringe. Let out the air from the syringe.
14. Open the blister packaging with the injection filter.
15. Put on the injection filter the syringe. You watch that there was no contact of a hand or other surface with parts of the injection filter into which the syringe and system for intravenous injection is inserted.
16. Attach the syringe with the injection filter to the enclosed system for intravenous injection, having turned the injection filter clockwise against the stop. Let out the air from the syringe with the attached injection filter and system for intravenous injection. Enter solution intravenously struyno (bolyusno) within 2-5 minutes.
If the patient needs to enter more than one bottle, prepare solution in each bottle by means of the enclosed solvent (water for injections), and then connect solutions in larger syringe it (is not applied) and administer the drug regularly.
It is recommended to use the drug Koagil-VII at once after cultivation.
Features of use:
Patients with the increased risk of development of the IDCS are subject to strict observation of a clinical state and indicators of a koagulogramma.
At use of the drug Koagil-VII in house conditions the patients or persons who are carrying out care of them have to report to the attending physician or in clinic about each case of use. If bleeding does not manage to be stopped, hospitalization is obligatory. Duration of out-patient therapy should not exceed 24 hours.
At patients with deficit of blood-coagulation factors of Viisleduyet to control a prothrombin time and activity of blood-coagulation factors of VII before administration of the drug Koagil-VII. If activity of blood-coagulation factors of VIIA does not reach the expected level or bleeding proceeds, despite use of drug in the recommended doses, it is possible to assume antibody formation. In this case it is necessary to carry out the analysis on existence of antibodies.
Patients who have a risk of development of venous thrombosis caused by associated diseases, existence of thrombosis in the anamnesis, an immobilization in the postoperative period or vein catheterization need careful observation.
Before use it is necessary to check solution for transparency and existence of inclusions. In the presence of inclusions solution cannot be used.
In rare instances can be observed: a fever, fever, pain (including in the place of injections), a headache, nausea, vomiting, weakness, the increased sweating, allergic reactions (skin rash, an itch, reddening of integuments), reduction of number of thrombocytes and decrease in level of fibrinogen, increase in level of a prothrombin, alaninaminotranspherase, an alkaline phosphatase, lactate dehydrogenase, D-dimera.
In some cases can preferential be observed at patients with tendency to development
- arterial thrombosis: disturbances of cerebrovascular blood circulation (heart attack of a brain and ischemia of a brain), stenocardia, myocardial infarction, intestines heart attack.
- venous thrombosis: thrombophlebitis, deep vein thrombosis and their complications, thromboembolism of a pulmonary artery.
Separate cases of emergence of antibodies to a factor of VII after use of an eptakog an alpha of the [activated] at patients with deficit factor of VII are described. This patient poured human plasma and / or a plasma factor of VII earlier.
Interaction with other medicines:
It is not necessary to enter at the same time the concentrates of a prothrombin complex (activated or not activated) and Koagil-VII. Antifibrinolitiki snizhayutintraoperatsionny blood loss at patients with hemophilia, especially at orthopedic operations and operations on fabrics with high fibrinolitic activity, for example, in an oral cavity. However the possibility of the combined use of antifibrinolitik and the drug Koagil-VIINE was studied. It is not necessary to enter in one syringe with any other drugs.
Hypersensitivity to proteins of mice, hamsters or cows, and also to active component of drug and excipients.
It is applied with care. At the smashed wounds, widespread atherosclerosis, trombotichesky complications, sepsis, recently undergone surgeries in connection with potential risk of development of trombotichesky complications or a syndrome of the disseminated intravascular coagulation (DIC). Use of the drug Koagil-VII for pregnant women and the feeding women should be limited to strict indications.
At exceeding of the recommended dose at 10-20 times the risk of development of arterial and/or venous thrombosis increases. In this regard careful dynamic control of a clinical state and indicators of a koagulogramma is necessary.
At a temperature from 2 °C up to 8 °s.ne to freeze. To store in the places unavailable to children. A drug period of validity - 2 years, solvent – 4 years. Not to use after the term specified on packaging. Issue conditions from drugstores - according to the recipe of the doctor.
According to the recipe
Lyophilisate for preparation of solution for intravenous administration of 1,2 mg, 2,4 mg or 4,8 mg in the glass bottles corked by rubber bungs with a running in caps aluminum-plastic with control of the first opening. On 5 ml of water for injections - solvent in ampoules glass with a ring or a point of a break. 1 bottle with drug and 1 ampoule (for dosages of 1,2 mg or 2,4 mg) or 2 ampoules (for a dosage of 4,8 mg) with solvent complete with account medical materials: the syringe, a needle for cultivation, a catheter for peripheral veins, the filter injection, 2 napkins spirit and the application instruction in a pack from a cardboard. Each component of account medical materials is placed in the sterile one-time packaging consisting of a film polyvinyl chloride and the paper laminated. On joints of a cover and a bottom with front and back sides of a pack paste unmarked self-adhesive labels for control of the first opening.