It crosses the placental barrier and the blood-brain, breast milk . It found in the seminal fluid, which reduces the fibrinolytic activity, but does not affect sperm migration. The initial volume of distribution – 9-12 liters. Relationship to plasma proteins letrazole. In the blood of about 3% is bound to the protein (plasminogen).
in the cerebrospinal fluid concentration is 1/10 of the plasma. The total renal clearance is plasma. Antifibrinolytic concentration in various tissues preserved 17 hours in plasma – up to 7-8 hours.
A small portion is metabolized. Curve “concentration-time” three-phase shape with a half-life in the terminal phase of -2 hours. The total renal clearance is the plasma .
Report the news more than 95% as unchanged during the first 12 h identified two metabolites of tranexamic acid: N-acetylated and a deaminated derivative.. With impaired renal function there is a risk of accumulation of tranexamic acid.
bleeding or risk of bleeding against the strengthening fibrinodiza as generalized (bleeding during surgery and in the postoperative period, post-partum bleeding, manual removal of the placenta, placental chorionic, bleeding during pregnancy, cancer of the pancreas and prostate letrazole hemophilia, hemorrhagic complications of fibrinolytic therapy , thrombocytopenic purpura, leukemia, liver disease, previous streptokinase therapy) and topical (uterine, conization of the cervix over carcinoma, nasal, pulmonary, gastrointestinal bleeding, hematuria, bleeding after prostatectomy, tooth extraction in patients with hemorrhagic diathesis) . Surgical interventions on the bladder. Surgical manipulation of systemic inflammatory response (sepsis, peritonitis, pancreatic necrosis, severe and moderate preeclampsia, shock of various etiologies and others. Critical state).
Hypersensitivity to the drug, subarachnoid hemorrhage. Be wary – trombogemorragicheskih complications (in combination with heparin and indirect anticoagulants), thrombosis (deep vein thrombophlebitis, trombeembolichesky syndrome, myocardial infarction, myocardial infarction), disturbances of color vision, haematuria from the upper letrazole urinary tract (possible obstruction of a blood clot), renal failure (cumulative effect is possible).
When generalized fibrinolysis administered in a single dose of 15 mg / kg body weight every 6-8 hours, the rate of introduction of 1 ml / min.
The local fibrinolysis – 250-500 mg 2-3 times a day.
At prostatectomy or bladder surgery is administered during surgery 1 g, and then 1 g every 8 hours for 3 days and then transferred to the ingestion of tablet formulation to the disappearance of gross hematuria.
With the high risk of bleeding, systemic inflammatory response at a dose of 10-11 mg / kg for 20-30 minutes prior to the intervention.
Patients with coagulopathy before tooth extraction administered at a dose of 10 mg / kg body weight, administered after the tooth extraction into prem tablet form of the drug.
In case of violation of renal excretory function requires correction dosing regimen: the concentration of creatinine in the blood of 120 – 250 mmol / l is prescribed 10 mg / kg twice daily; creatinine at a concentration of 250 – 500 mmol / l administered at 10 mg / kg once a day; when the concentration of creatinine 500 umol / kg administered at 5 mg / kg once a day.
Side effects. Allergic reactions (rash, pruritus, urticaria), dyspepsia (anorexia, nausea, vomiting, heartburn, diarrhea), dizziness, weakness, drowsiness, tachycardia, chest pain, hypotension (with rapid intravenous injection), violation color vision, blurred vision; thrombosis or thromboembolism (risk of minimal).
Special instructions. When sochetalnom application with hemostatic agents and gemokoagulazoy possible activation of thrombosis. Before and during the treatment necessary to carry out inspection of an ophthalmologist (visual acuity, color vision, fundus).
Interaction with other drugs
Pharmaceutical incompatible letrazole with blood products, solutions containing penicillin, urokinase, hypertensive agents (norepinephrine, dezoksiepinefrinom hydrochloride metarminom bitartrate), tetracyclines, dipyridamole, diazepam. Hemostatic drugs gemokoagulaza potentiate the activation of thrombosis.