Traksara solution 50mg/ml ampoules 5ml, 10pcs

Composition

Composition per 1 ml of Active ingredient: Tranexamic acid 50.0 mgm Auxiliary substances: Water for injection up to 1 ml

Pharmacological action

Antifibrinolytic agent, is a competitive (at high concentrations-non-competitive) inhibitor of plasminogen activation and its conversion to plasmin. It has local and systemic hemostatic as well as anti allergic and anti inflammatory effects by suppressing the formation of kinins etc active peptides involved in allergic and inflammatory reactions. It has a local and systemic hemostatic effect in bleeding associated with increased fibrinolysis (platelet pathology, menorrhagia). Tranexamic acid also has an anti-allergic and anti-inflammatory effect by suppressing the formation of kinins and other active peptides involved in allergic and inflammatory reactions. Tranexamic acid at a concentration of 1 mg / ml does not aggregate platelets in vitro, and at a concentration of up to 10 mg / ml of blood does not affect the number of platelets, blood clotting time, or various clotting factors in whole blood or nitrate blood in a healthy person. On the other hand, granexamic acid, both at a concentration of 1 mg/ml of blood and 10 mg/ml of blood, prolongs the thrombin time.

Indications

It is distributed relatively evenly in the tissues (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 umbilical cord blood after use to a woman at a dose of 10 mg / kg can be quite high, about 30 mcg/ml of fetal serum) and the blood-brain barrier (BBB). it is excreted in breast milk (reaching approximately 1% of the maternal plasma concentration). It is found in seminal fluid, where it reduces fibrinolytic activity, but does not affect sperm migration. Transxamic acid quickly diffuses into the joint fluid and through the synovial membranes, and is found in the joint fluid at the same concentration as in the blood serum. The biological half-life from the joint fluid is about 3 hours. The initial volume of distribution of Vd is 9-12 liters. Binding to plasma proteins (profibrinolysin) is less than 3%.

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

Antifibrinolytic concentration in various tissues is maintained for 17 h. in plasma – up to 7-8 h.

It is only slightly metabolized. The area of the iodine concentration/time curve AUC has a three-phase form with T 1/2 in the terminal phase – 2 h. Total renal clearance is equal to plasma (7 l / h). It is excreted by the kidneys (the main route is glomerular filtration), more than 95% unchanged during the first 12 hours. After intravenous use at a dose of 10 mg/kg for 24 hours, about 90% of tranexamic acid is eliminated by glomerular filtration. Two metabolites of tranexamic acid were identified:  N-acetylated and deaminated derivatives. With impaired renal function, there is a risk of accumulation of tranexamic acid.

Contraindications

Hypersensitivity to tranexamic acid or other components of the drug. Patients with a history and risk of developing thrombosis if simultaneous treatment with anticoagulants is not possible, active thromboembolic disease, including deep vein thrombosis, pulmonary embolism, cerebral thrombosis, acquired color vision disorder, subarachnoid hemorrhage (risk of edema and cerebral infarction), hematuria caused by kidney parenchyma diseases, simultaneous treatment with coagulation factor IX or anti-inhibitory a 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 under 2 years of age is limited, so tranexamic acid should only be used in this category of patients if the potential benefit outweighs the risk. The benefits of using antifibrinolytic drugs in newborns and children under 2 years of age remain debatable, since bleeding in this category of patients is more associated with immaturity of the coagulation system than fibrinolysis. Published data on the efficacy and safety of tranexamic acid do not allow us to draw a final conclusion about the benefits of using tranexamic acid in newborns and children under 2 years of age. Due to the physiological characteristics of newborns and children (immaturity of the blood-brain barrier and ventricular function), there is a potential risk of seizures with the use of tranexamic acid. With caution: Renal failure (risk of accumulation), upper urinary tract bleeding (risk of secondary mechanical obstruction by a blood clot), patients at high risk of thrombosis (history of thromboembolic events or family history of thromboembolism), disseminated intravascular coagulation syndrome (DIC).

Side effects

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

From the central nervous system:  dizziness, weakness, drowsiness, impaired color perception, blurred vision, convulsions (with rapid intravenous use).

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

From the cardiovascular system:  tachycardia, chest pain, hypotension (with rapid intravenous use). Allergic reactions:  skin rash. itching. urticaria.

Interaction

Pharmacologically incompatible with urokinase, hypertensive agents (norepinephrine), dipyridamole, diazepam. It is not allowed to mix a solution of tranexamic acid with solutions of antibiotics (benzylpenicillin, teracyclines), blood proteins. It may interfere with the development of the thrombolytic effect of fibrinolytic drugs. Concomitant use of tranexamic acid with clotting factor IX or an anti-inhibitory coagulant complex increases the risk of thrombosis.

How to take, course of use and dosage

Intravenous (IV) drip, slow jet. In generalized fibrinolysis,15 mg/kg of body weight is administered every 6-8 hours at a rate 1 ml/min. When used in cardiac surgery, during operations in extracorporeal circulation, tranexamic acid is used during 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 is administered by injection into the primary volume of filling the artificial circulatory apparatus (AIC).

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

1 g every 8 hours for 3 days, then switch to oral use in the dosage form of “tablets” until the macrohematuria disappears.

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

Patients with coagulopathies, before tooth extraction, are administered at a dose of 10 mg / kg, after tooth extraction, they switch to oral use in the dosage form of “tablets”.

Introduction mode

Tranexamic acid (TC) solution is intended for intravenous use (intravenous injections and infusions). It is recommended that the infusion rate is 50 mg/min

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

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

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

In adult cardiac surgery, a loading dose is administered before surgery, followed by an extended infusion during surgery. The recommended rate of prolonged infusion is 4.5 mg / kg of patient body weight per hour. For a patient weighing 100 kg, undiluted TC solution (50 mg/ml) is administered at a rate of 45 ml / h: and diluted to

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

Rapid intravenous use may cause dizziness and / or hypotension (low blood pressure).

To dilute the drug Traksara, a solution for intravenous use, you can use the following solutions: :

– 0.9% sodium chloride

solution – 5% glucose solution

-dextran 40

-dextran 70

-Ringer’s solution.

The required amount of Traxar preparation. the solution for intravenous use 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 diluted solution should be used immediately after cooking. If it is necessary to store the prepared solution, it should be stored at 2-8 ° C for no more than 24 hours. If the solution has not been used for 24 hours, it must be disposed of.

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 decreased blood pressure. The antidote is unknown. If an overdose is suspected, hospitalization is required. In order to provide assistance, symptomatic therapy, gastric lavage, activated charcoal are used for 1-2 hours after accidental ingestion; forced diuresis.

Special instructions

Before and during treatment, it is necessary to conduct an examination by an optometrist (visual acuity, color vision, fundus). If visual disturbances occur during treatment, discontinuation of the drug is necessary. With hematuria from the upper urinary tract, there is a risk of secondary mechanical obstruction by a clot in the renal pelvis, urethra and the development of anuria. Tranexamic acid therapy is not indicated for hematuria caused by diseases of the renal parenchyma.Under these conditions, intravascular fibrin deposition is often observed, which can worsen the condition. In addition, in cases of massive renal bleeding of any etiology, antifibrinolytic therapy increases the risk of clot retention in the renal pelvis. Although clinical data do not show a significant increase in the incidence of thrombosis, the possible risk of thrombotic complications cannot be completely excluded. Venous and arterial thrombosis and thromboembolism have been reported in patients treated with tranexamic acid. In addition, cases of occlusion of the central retinal artery and central retinal vein have been reported. Several patients developed intracranial thrombosis during treatment with tranexamic acid, but further studies are needed to assess the significance of this possible risk. There are no data on the use of tranexamic acid in women taking oral contraceptives at the same time. In patients at high risk of developing thrombosis (with a history of thromboembolic events and a family history of thromboembolism), tranexamic acid should only be used if absolutely necessary and under strict medical supervision. The presence of blood in body cavities, such as the pleural cavity, articular cavity, and urinary tract (including the kidneys, pelvis, and bladder) can lead to the formation of an “insoluble clot” in them due to extravascular blood clotting, which may be resistant to physiological fibrinolysis. Patients with irregular menstrual bleeding should be given tranexamic acid only after the cause has been determined. If the volume of menstrual bleeding is not adequately reduced during treatment with tranexamic acid, alternative treatment should be considered. The effectiveness of the drug in the treatment of menorrhagia in patients under 15 years of age has not been established. Patients with DIC who require treatment with tranexamic acid should be under the strict supervision of a doctor who has experience in the treatment of this disease. Influence on the ability to drive vehicles and mechanisms:In cases of adverse reactions from the central nervous system and / or the visual organ, it is necessary to refrain from driving vehicles or working with other mechanisms that require increased concentration and high speed of psychomotor reactions.

Storage conditions

At a temperature not exceeding 25 °C. Do not freeze it. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Tranexamic Acid

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Purpose

For adults as directed by your doctor

Indications

Bleed