Traxsara - instructions for use, doses, side effects, contraindications

Pharmacodynamics:Antifibrinolytic agent, is a competitive (at high concentrations-uncompetitive) inhibitor of plasminogen activation and its conversion into plasmin. It has local and systemic hemostatic as well as anti-allergic and anti-inflammatory effects due to inhibition of the formation of kinins and other active peptides involved in allergic and inflammatory reactions. Has a local and systemic hemostatic effect in bleeding associated with increased fibrinolysis (platelet pathology, menorrhagia). Also tranexamic acid by suppressing the formation of kinins and other active peptides involved in allergic and inflammatory reactions, has anti-allergic and anti-inflammatory effects.

Tranexamic acid at a concentration of 1 mg / ml does not aggregate platelets in vitro, at concentrations up to 10 mg / ml of blood does not affect the platelet count, clotting time or various coagulation factors in whole blood or nitrate blood in a healthy person.On the other hand, ganexamic acid, both at a concentration of 1 mg / ml blood, and 10 mg / ml blood, prolongs thrombin time.

Pharmacokinetics:

It is distributed in tissues relatively evenly (with the exception of cerebrospinal fluid, where the concentration is 1/10 of the plasma one). Penetrates through the placental barrier (the concentration in the cord blood after administration to a woman at a dose of 10 mg / kg can be quite high, about 30 μg / ml fetal serum) and the blood-brain barrier (BBB). is excreted in breast milk (reaching approximately 1% of the concentration in the mother plasma). It is found in seminal fluid, where it reduces fibrinolytic activity, but does not affect the migration of spermatozoa. Transksamic acid diffuses rapidly into the joint fluid and through the synovial membrane, in the joint fluid is found at the same concentration as in the blood serum. The biological half-life of the joint fluid is about 3 hours. The initial volume of distribution V_d - 9-12 liters. Binding to plasma proteins (profibrinolysin) is less than 3%.

In blood, about 3% is associated with a protein (plasminogen). The total renal clearance is equal to the plasma clearance.

Antifibrinolytic concentration in various tissues persists for 17 hours in plasma - up to 7-8 hours.

Metabolized to a small extent. The iodine area of the "concentration / time" curve AUC has a three-phase form with T_1/2 in the terminal phase - 2 hours. The total renal clearance is equal to the plasma clearance (7 l / h). It is excreted by the kidneys (the main way is glomerular filtration), more than 95% unchanged during the first 12 hours. After intravenous administration at a dose of 10 mg / kg for 24 hours by glomerular filtration, about 90% of tranexamic acid is excreted. Two metabolites of tranexamic acid have been identified: N-acetylated and deaminated derivatives. In case of violations of kidney function, there is a risk of cumulation of tranexamic acid.

Indications:

It is distributed in tissues relatively evenly (with the exception of cerebrospinal fluid, where the concentration is 1/10 of the plasma one). Penetrates through the placental barrier (the concentration in the cord blood after administration to a woman at a dose of 10 mg / kg can be quite high, about 30 μg / ml fetal serum) and the blood-brain barrier (BBB). is excreted in breast milk (reaching approximately 1% of the concentration in the mother plasma).It is found in seminal fluid, where it reduces fibrinolytic activity, but does not affect the migration of spermatozoa. Transksamic acid diffuses rapidly into the joint fluid and through the synovial membrane, in the joint fluid is found at the same concentration as in the blood serum. The biological half-life of the joint fluid is about 3 hours. The initial volume of distribution V_d - 9-12 liters. Binding to plasma proteins (profibrinolysin) is less than 3%.

In blood, about 3% is associated with a protein (plasminogen). The total renal clearance is equal to the plasma clearance.

Antifibrinolytic concentration in various tissues persists for 17 hours in plasma - up to 7-8 hours.

Metabolized to a small extent. The iodine area of the "concentration / time" curve AUC has a three-phase form with T_1/2 in the terminal phase - 2 hours. The total renal clearance is equal to the plasma clearance (7 l / h). It is excreted by the kidneys (the main way is glomerular filtration), more than 95% unchanged during the first 12 hours. After intravenous administration at a dose of 10 mg / kg for 24 hours by glomerular filtration, about 90% of tranexamic acid is excreted. Two metabolites of tranexamic acid have been identified: N-acetylated and deaminated derivatives.In case of violations of kidney function, there is a risk of cumulation of tranexamic acid.

Contraindications:Hypersensitivity to tranexamic acid or other components of the drug. Patients with an anamnesis and a risk of developing thrombosis with the impossibility of simultaneous treatment with anticoagulants, active thromboembolic disease, incl. deep vein thrombosis, pulmonary embolism, cerebral thrombosis, acquired color vision disorder, subarachnoid hemorrhage (risk of edema and cerebral infarction), hematuria caused by renal parenchyma diseases, concurrent treatment with coagulation factor IX or anti-inhibitory coagulant complex.

Pediatric Use

There is no clinical experience with tranexamic acid in patients under 15 years of age with menorrhagia.

Clinical experience in children younger than 2 years is limited, so tranexamic acid It should be used in this category of patients only if the potential benefit exceeds the risk. The use of antifibrinolytic drugs in newborns and children younger than 2 years remains discrete,because the bleeding in these patients is largely due to the immaturity of the coagulation system than fibrinolysis.

Published data on the efficacy and safety of tranexamic acid did not allow a definitive conclusion about the benefits of the use of tranexamic acid in infants, children up to 2 years. Due to the physiological characteristics of newborns and infants (immature blood-brain barrier and function nochek) there is a potential risk of seizures against application of tranexamic acid.

Carefully:

Renal failure (risk of cumulation), bleeding from the upper urinary tract (a risk of secondary mechanical obstruction of blood clot), patients with a high risk of thrombosis (thromboembolic events in a history or family history of thromboembolism), disseminated intravascular coagulation (DIC).

Pregnancy and lactation:

There are no adequate and strictly controlled studies of the use of tranexamic acid preparations in pregnant women. In cord blood tranexamic acid is contained in concentrations close to the parent. Tranexamic acid penetrates the placental barrier and is excreted in breast milk (reaching approximately 1% of the concentration in the mother's plasma).

Tranexamic acid is used in pregnancy according to indications with mandatory consideration of contraindications.

When using tranexamic acid, breastfeeding should be abolished.

Dosing and Administration:

Intravenous (IV) drip, slowly stream.

In generalized fibrinolysis, 15 mg / kg body weight every 6-8 hours at a rate of 1 ml / min.

When used in cardiac surgery, in operations under extracorporeal circulation, tranexamic acid is used during the induction of anesthesia before sternotomy at a dose of 15 mg / kg. then intraoperatively at a dose of 4.5 mg / kg / h. of which

0.6 mg / kg - by introducing into the primary filling volume of the artificial circulation apparatus (AIC).

With local fibrinolysis, 250-500 mg 2-3 times a day. When prostatectomy or bladder surgery - 1 g during surgery, then on

1 g every 8 hours for 3 days, then switch to oral administration in the dosage form of "tablet" until the disappearance of the macrohematuria.

At a high risk of bleeding, with a syndrome of systemic inflammatory reaction - 10-11 mg / kg for 20-30 minutes before the intervention.

Patients with coagulopathies, before the extraction of the tooth are administered at a dose of 10 mg / kg, after the extraction of the tooth, they switch to the oral dosage form of the "tablet".

Mode of administration

A solution of tranexamic acid (TC) is intended for intravenous administration (intravenous injection and infusion). The recommended rate of administration is 50 mg / min:

- for undiluted TC solution (50 mg / ml) - 1 ml / min;

- for diluted to 1% (10 mg / ml) solution of TK - 5 ml / min;

- for diluted to 2% (20 mg / ml) - solution of TC - 2.5 ml / min.

In cardiosurgery in adults, the loading dose is administered before surgery followed by extended infusion during surgery. It is recommended that the rate of prolonged infusion is 4.5 mg / kg of patient body weight per hour. For a patient with a body weight of 100 kg, an undiluted TC solution (50 mg / ml) is injected at a rate of 45 ml / h: and diluted to

2 % (20 mg / ml) rp TK is administered at a rate of 22.5 ml / h.

Rapid intravenous administration may cause dizziness and / or hypotension (lowering blood pressure).

To dilute the preparation of Traxar, a solution for intravenous administration, the following solutions can be used:

- 0.9% solution of sodium chloride

- 5% glucose solution

- dextran 40

- dextran 70

- Ringer's solution.

Required volume of the preparation of Traxar. solution for intravenous administration can be added to the selected infusion solution to achieve final concentrations of 1 or 2 g in 100 ml (10 or 20 mg / ml 1% or 2%). The dilute solution follows use immediately after preparation. If it is necessary to store the prepared solution, it should be stored at 2-8 ° C for no more than 24 hours. The solution not used within 24 hours must be disposed of.

Side effects:

From the digestive system: anorexia, nausea, vomiting, heartburn, diarrhea.

From the side of the central nervous system: dizziness, weakness, drowsiness, violation of color perception, blurred vision, convulsions (with rapid intravenous injection).

From the coagulation system of the blood: thrombosis, thromboembolism (the risk of development is minimal).

From the cardiovascular system: tachycardia, pain in the chest, arterial hypotension (with rapid on / in the introduction). Allergic reactions: skin rash. itching. hives.

Overdose:

There are limited data on overdose cases. One case of overdose (37 g) has been reported.

Symptoms of overdose may include dizziness, headache, nausea, vomiting, diarrhea, orthostatic symptoms, and lowering blood pressure. The antidote is unknown. If you suspect an overdose, hospitalization is necessary. With the aim of providing relief, symptomatic therapy, gastric lavage, Activated carbon within 1-2 hours after accidental ingestion; forced diuresis.

Interaction:Pharmaceutically incompatible with urokinase, hypertensive drugs (norepinephrine), dipyridamole, diazepam.

It is not allowed to mix a solution of tranexamic acid with solutions of antibiotics (benzylpenicillin, teracyclines), blood proteins.

May interfere with the development of the thrombolytic effect of fibrinolytic drugs.

Simultaneous use of tranexamic acid with coagulation factor IX or anti-inhibitory coagulant complex increases the risk of developing thrombosis.

Special instructions:

Before and during the treatment it is necessary to conduct an examination of the oculist (visual acuity, color vision, eye fundus).

When there are visual impairments on the background of treatment, it is necessary to cancel the drug.With hematuria from the upper parts of the urinary tract, there is a risk of secondary mechanical obstruction of the clot in the renal pelvis, urethra and the development of anuria. Tranexamic acid therapy is not indicated in hematuria caused by diseases of the kidney parenchyma. Under these conditions, intravascular precipitation of fibrin is often observed, which can aggravate the condition. In addition, in cases of massive renal bleeding of any etiology, antifibrinolytic therapy increases the risk of retention of the clot in the renal pelvis.

Although the clinical data do not show a significant increase in the incidence of thrombosis, a possible risk of thrombotic complications can not be completely ruled out. There have been reports of cases of venous and arterial thrombosis and thromboembolism in patients receiving tranexamic acid. In addition, cases of occlusion of the central artery of the retina and the central vein of the retina have been reported. Several patients developed intracranial thrombosis on the background of treatment with tranexamic acid, but further studies are needed to assess the significance of this potential risk.

There are no data on the use of tranexamic acid in women taking concurrent oral contraceptives.

In patients with a high risk of thrombosis (thromboembolic events and anamnesis, cases of thromboembolism in a family history) tranexamic acid should be used only in case of emergency and under strict medical supervision. The presence of blood in the body cavities, for example, the pleural cavity, articular cavity and urinary tract (including the kidneys, small pelvis, bladder) can lead to the formation of an "insoluble clot" due to extravascular coagulation, which can be resistant to physiological fibrinolysis. Patients with irregular menstrual bleeding should be administered tranexamic acid only after establishing the cause. If the amount of menstrual bleeding is inadequately reduced with treatment with tranexamic acid, alternative treatment should be considered.

The effectiveness of the drug in the treatment of menorrhagia in patients younger than 15 years is not established.

Patients with DIC syndrome who need treatment with tranexamic acid should be under strict medical supervision,who has experience in the treatment of this disease.

Effect on the ability to drive transp. cf. and fur:

In cases of adverse reactions from the CNS and / or the organ of vision, one should refrain from driving vehicles or working with other mechanisms that require an increased concentration and a high rate of psychomotor reactions.

Form release / dosage:

Solution for intravenous administration 50 mg / ml.

Packaging:

5 ml in neutral glass ampoules with a capacity of 5 ml.

5 ampoules per box or a pack of cardboard with partitions or a loose leaf of paper paste.

5 ampoules per circuit cell packaging made of non-vinyl chloride film and aluminum foil printed lacquered or foil-free. 1 or 2 contour squares but 5 ampoules per pack of cardboard. In each box or pack, the instructions for use and the opener for opening ampoules or the ampoule scarifier are put. When using ampoules with incisions or a ring of fracture, a scarifier ampoule or a knife for opening ampoules is not inserted. For 10 or 20 ml in bottles of colorless glass, hermetically sealed with rubber stoppers, with capping aluminum or aluminoplastic caps.To 1 bottle together with instructions for use in a pack of cardboard.

Storage conditions:At a temperature of no higher than 25 ° C. Do not freeze. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002926

Date of registration:24.03.2015

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp20.09.2015

Illustrated instructions

Instructions

Traxara (Traksara)