Active substanceTranexamic acidTranexamic acid
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  • Dosage form: & nbspsolution for intravenous administration
    Composition:

    5 ml of solution contains:

    Active substance: tranexamic acid .... 250 mg or 500 mg;

    Excipients: water for injection up to 5 ml.

    Description:A clear, colorless solution.
    Pharmacotherapeutic group:Hemostatic agent. The inhibitor of fibrinolysis is an inhibitor of the transition of plasminogen to plasmin.
    ATX: & nbsp

    B.02.A.A   Amino acids

    B.02.A.A.02   Tranexamic acid

    Pharmacodynamics:Hemostatic drug. Inhibitor of fibrinolysis. Inhibits the activation of plasminogen, and at high concentrations it is a noncompetitive plasmin inhibitor. Has a local and systemic hemostatic effect in bleeding associated with increased fibrinolysis (platelet pathology, menorrhagia). By suppressing the formation of kinins and other active peptides involved in allergic and inflammatory reactions, it has anti-allergic and anti-inflammatory effects. In experimental studies, the own analgesic activity of tranexamic acid has been confirmed, as well as a potentiating effect on the analgesic activity of opioid analgesics.
    Pharmacokinetics:
    The connection with plasma proteins (profibrinolysin) is less than 3%.
    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 and the blood-brain barrier, 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. The initial volume of distribution is 9-12 liters. Antifibrinolytic concentration in various tissues persists for 17 hours, in plasma - up to 7-8 hours.

    Metabolized to a small extent. Curve AUC (the area under the concentration-time curve) has a three-phase shape with T1/2 (half-life) in the final phase - 3 hours. The total renal clearance is equal to the plasma clearance (7 l / h). More than 95% is excreted by the kidneys unchanged during the first 12 hours (the main way is glomerular filtration). Identified 2 metabolites of tranexamic acid: N-acetylated and deaminated derivatives.

    Pharmacokinetics in special clinical cases:

    With impaired renal function, there is a risk of cumulation of tranexamic acid.

    Indications:

    Indications for use in adults.

    1 Bleeding or risk of bleeding with a background of increased fibrinolysis, as generalized (bleeding during surgery and inpostoperative period, postpartum hemorrhage, manual detachment, chorion detachment, bleeding during pregnancy, malignant neoplasms of the pancreas and prostate gland, hemophilia, hemorrhagic complications of fibrinolytic therapy, thrombocytopenic purpura, leukemia, liver disease, previous streptokinase therapy) and local (uterine, conization of the cervix for cervical cancer, nasal, pulmonary, gastrointestinal bleeding, hematuria, bleeding after prostatectomy, extraction of the tooth in patients with hemorrhagic diathesis).

    2 Operative interventions on the bladder.

    3 Surgical manipulations with a systemic inflammatory reaction (sepsis, peritonitis, pancreatic necrosis, severe and moderate severity of gestosis, shock of various etiologies and other critical conditions).

    Indications for use in children's practice.

    4 Uterine bleeding puberty, bleeding from the upper divisions of the gastrointestinal tract, nasal bleeding, pulmonary hemorrhage, including in patients with cystic fibrosis, bleeding after tonsillectomy.

    5 Hereditary angioedema.

    6 Prevention and treatment of bleeding during surgery, surgery for congenital heart disease, spinal surgery, liver transplantation.

    7 Menorrhagia in women with coagulopathies, including with von Willebrand's disease, deficiency of clotting factors VII, X, XI.

    8 Bleeding from the upper gastrointestinal tract, nasal bleeding, dental procedures, including surgical manipulations with labial or gingival hematomas in patients with coagulopathies.

    Surgical treatment of patients with hemorrhagic disorders.

    Contraindications:-Subarachnoid hemorrhage;
    -Increased sensitivity to the components of the drug;
    - simultaneous use with prothrombin complex preparations (coagulation factors II, VII, IX and X in combination) or anti-inhibitory coagulant complex;
    - Venous or arterial thrombosis (deep vein thrombosis of the legs, pulmonary embolism, thrombosis of the intracranial vessels, etc.), except for cases when simultaneous therapy with anticoagulants is possible.
    Carefully:With caution should prescribe the drug for thrombosis (including with thrombosis of the vessels of the brain,myocardial infarction, deep vein thrombophlebitis, thromboembolic syndrome), or with the threat of their development, thrombohemorrhagic complications (in combination therapy with heparin, and indirect anticoagulants), impaired color vision, hematuria from the upper urinary tract (possible blood clot obstruction), renal failure due to the increased risk of cumulation), thromboembolic complications in the history (including in the family).
    Pregnancy and lactation:
    In preclinical studies tranexamic acid had no teratogenic effect. Adequate and strictly controlled studies of the efficacy and safety of tranexamic acid drugs in pregnant women have not been conducted. Tranexamic acid penetrates the placenta and can be contained in cord blood in a concentration close to the mother's. Because studies of reproductive function in animals do not always allow predicting reactions in humans, tranexamic acid should be used during pregnancy only in case of emergency. Tranexamic acid penetrates into breast milk (the concentration of the drug in milk is about 1% of the concentration in the blood plasma of the mother). Development of antifibrinolytic effect in an infant is unlikely, nevertheless, caution should be used against the background of the use of tranexamic acid.
    Dosing and Administration:
    Intravenous (drip, jet).
    When generalized fibrinolysis is administered in a single dose of 15 mg / kg body weight every 6-8 hours, the rate of administration is 1 ml / min.
    With local fibrinolysis, 250-500 mg 2-3 times a day.
    In prostatectomy or bladder surgery, 1 g is injected during the operation, then 1 g every 8 hours for 3 days, then go to the inside of the tablet form until the macrohematuria disappears.
    With a high risk of bleeding, with a systemic inflammatory reaction at a dose of 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 of body weight, after extraction of the tooth, the tablet form of the preparation is ingested. In the case of a violation of the excretory function of the kidneys, correction of the dosing regimen is necessary: ​​at a creatinine concentration of 120-250 μmol / l, 10 mg / kg 2 times a day are administered; at concentrationCreatinine 250-500 μmol / l administered at 10 mg / kg once a day; at a creatinine concentration of more than 500 μmol / L administered at 5 mg / kg once a day.
    The way of application and dose in children's practice.
    Uterine bleeding pubertal period: depending on the volume of bleeding and the general condition of the patient, inject 0.5-1 g 3-4 times a day from the 1st to the 4th day of menstruation.
    Bleeding from the upper sections of the gastrointestinal tract: 10-15 mg / kg body weight of the patient.
    Nasal bleeding: 1 g 3 times a day for 10 days after bleeding. Pulmonary bleeding, including in patients with cystic fibrosis: 1 g 3-4 times a day until the complete cessation of hemoptysis.

    Tonsillectomy: intravenously before the surgical operation 10-15 mg / kg, and after the operation - inside 1 g 3 times a day for 5 days.
    Hereditary angioedema: 1-1.5 g orally 2-3 times a day or intravenously drip 15 mg / kg of body weight under the control of the blood coagulation system. For the prevention and treatment of bleeding during surgery: 10 mg / kg body weight.
    Dental procedures: inside 10 mg / kg of body weight after extraction of the tooth, rinsing of the oral cavity with tranexamic acid can also be used. Surgery of congenital heart disease:
    1) a loading dose of 10 mg / kg, followed by infusion of the drug at a dose of 1 mg / kg / h;
    2) 10 mg / kg of the drug is injected into the circulatory system;
    3) The patient receives 10 mg / kg after the administration of protamine.
    Spinal surgery, liver transplantation: 20 mg / kg body weight with cutaneous incision followed by infusion of 1 mg / kg / h, 20 mg / kg every 6-8 hours in the postoperative period.
    Menorrhagia in women with coagulopathy, including with von Willebrand's disease, deficiency of blood coagulation factors VII, X and XI: 15-20 mg / kg body weight 3-4 times a day with the onset of bleeding before it stops (1-1.5 g 3 times a day). Bleeding from the upper gastrointestinal tract in patients with coagulopathy: 10 mg / kg body weight 3-6 times a day intravenously. With erosive gastritis: 10 mg / kg body weight 3-4 times a day is injected into the nasogastric tube to stop bleeding.
    Nasal bleeding in patients with coagulopathies: 15-20 mg / kg or locally (wetted tourniquet).
    Dental procedures in patients with coagulopathies: inside 15-20 mg / kg of body weight before the operation and after tooth extraction, then 3 times a day for 8-10 days. You can rinse your mouth for 2 minutes 4 times a day for 2 days.To treat the bleeding that continues after tooth extraction, inject bleeding at a dose of 20 mg / kg intravenously, and after performing local hemostasis, 10 mg / kg orally every 6 hours for several days.
    In the formation of labial or gingival hematomas for the implementation of hemostasis is administered at a rate of 7.5-10 mg / kg every 6 hours.
    In manipulations requiring a gingival incision or local exposure to bones, it is advisable to use continuous infusion at a dose of 1.5 mg / kg / h. Surgical treatment of patients with hemorrhagic disorders: 10 mg / kg of body weight are administered 3 times a day intravenously immediately before and after the operation. Orally 15-20 mg / kg body weight 3 times a day after surgery, when the patient can take the pill within 7-10 days.
    In the endoprosthesis of the knee joint, an additional dose is applied immediately before the removal of the hemostatic tourniquet.
    In operations in the lower urinary tract, a dose of 2 g is administered 3 times a day on the day of the operation and on the first day after the operation, along with irrigation of the bladder.
    In small operations, the drug can be used only inward 2 hours before the operation and within one week after the operation.

    Side effects:On the part of 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.
    From the coagulation system: rarely - thrombosis, thromboembolism.
    From the cardiovascular system: tachycardia, pain in the chest, arterial hypotension (with rapid intravenous administration).
    Allergic reactions: rash, itchy skin, hives.
    Overdose:Symptoms: nausea, vomiting, diarrhea; orthostatic hypotension; arterial or venous thromboembolism; impaired vision; change in mental status; myoclonus, rash.
    Interaction:Pharmaceutically incompatible with urokinase, hypertensive drugs (norepinephrine), dipyridamole, diazepam.
    With simultaneous use with hemostatic drugs and hemocoagulase, activation of thrombosis is possible.
    In solution tranexamic acid reacts (can not be mixed) with antibiotics (benzylpenicillin, tetracyclines), blood proteins.
    Special instructions:Before and during the treatment it is necessary to consult the ophthalmologist (determining the visual acuity,color vision, condition of the fundus). When hematuria can cause the formation of a thrombus and obstruction of the ureters. Tryxaminat should not be used during work drivers of vehicles and people whose profession is associated with increased concentration of attention.
    Form release / dosage:Solution for intravenous administration 50 mg / ml, 100 mg / ml.
    Packaging:For 5 ml of the drug in ampoules of colorless transparent glass of USP type 1 with a notch for the fracture in the upper part of the ampoule, which is designated as a blue band. For 10 ampoules are placed in a plastic tray with uncoated cells. 1 plastic pallet together with instructions for use are placed in a cardboard pack.
    Storage conditions:In a dry, dark place at a temperature of 8 ° C to 25 ° C. Keep out of the reach of children.
    Shelf life:3 years.
    Do not use after the time specified on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-006725/10
    Date of registration:16.07.2010
    The owner of the registration certificate:Hilton Pharma (Pvt) Ltd.Hilton Pharma (Pvt) Ltd. Pakistan
    Manufacturer: & nbsp
    Representation: & nbspHilton Pharma (Pvt) Ltd.Hilton Pharma (Pvt) Ltd.Pakistan
    Information update date: & nbsp20.09.2015
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