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

Tranexamic acid is an antifibrinolytic agent that specifically inhibits the activation of the profibrinolysin (plasminogen) and its conversion to fibrinolysin (plasmin). Has local and systemic hemostatic effect in bleeding associated with increased fibrinolysis, as well as anti-inflammatory, antiallergic, anti-infective and antitumor actions by suppressing the formation of kinins and other active peptides involved in allergic and inflammatory reactions. The experiment confirms the own analgesic activity of tranexamic acid, as well as the over-lunar potentiating effect on the analgesic activity of opiates.

Pharmacokinetics:

It is distributed in tissues relatively evenly (except for cerebrospinal fluid, where the concentration is 1/10 of the plasma one); penetrates the placental and blood-brain barrier, into breast milk (about 1% of the concentration in the mother's 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. The connection with plasma proteins (profibrinolysin) is less than 3%. In blood, about 3% is associated with a protein (plasminogen).

The concentration in the cerebrospinal fluid is 1/10 of the plasma one. 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.

Metabolizes a small part. The concentration-time curve has a three-phase form with a half-life in the terminal phase of 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. Two metabolites of tranexamic acid have been identified: N-acetylated and deaminated derivatives. With impaired renal function, there is a risk of cumulation of tranexamic acid.

Indications:

Bleeding or risk of bleeding against the background of increased fibrinolysis, as generalized (bleeding during surgery and in the postoperative period, postpartum hemorrhages, 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 therapy with streptokinase) and local (uterine, cone cervical carcinoma, nasal, pulmonary, gastrointestinal bleeding, hematuria , bleeding after prostatectomy, extraction of the tooth in patients with hemorrhagic diathesis). Operative interventions on the bladder. Surgical manipulations with a systemic inflammatory reaction (sepsis, peritonitis, pancreonecrosis, severe and moderate severity of gestosis, shock of various etiologies and other critical conditions).

Contraindications:Hypersensitivity to the drug, subarachnoid hemorrhage.

Carefully:

Thrombohemorrhagic complications (in combination with heparin and indirect anticoagulants), thrombosis (deep vein thrombophlebitis, thromboembolic syndrome, myocardial infarction), color vision disorders, hematuria from the upper urinary tract (blood clot obstruction possible), renal failure (possible cumulation).

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, the administration of the drug in a dose of 250-500 mg 2-3 times a day is recommended.

When prostatectomy or surgery on the bladder is administered during the operation, 1 g, then 1 g every 8 hours for 3 days, after which they switch to the inside of the tablet form until the disappearance of the macrohematuria.

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 intake of the tablet form of the preparation is prescribed. In case of 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 prescribed; at a creatinine concentration of 250-500 μmol / l administered at 10 mg / kg once a day; with a creatinine concentration of more than 500 μmol / l administered at 5 mg / kg 1 time per day.

Side effects:Allergic reactions (rash, itchy skin, urticaria),dyspeptic phenomena (anorexia, nausea, vomiting, heartburn, diarrhea), dizziness, weakness, drowsiness, tachycardia, chest pain, hypotension (with rapid intravenous injection), impaired color vision, blurred vision; thrombosis or thromboembolism (the risk of development is minimal).

Interaction:

Pharmaceutically incompatible with blood products, solutions containing penicillin, urokinase, hypertensive drugs (norepinephrine, deoxyepinefrin hydrochloride, metarmine bitartrate), tetracyclines, dipyridamole, diazepam. Hemostatic drugs, hemocoagulase potentiate the activation of thrombosis.

Special instructions:When combined with hemostatic drugs and hemocoagulase, thrombus formation can be activated. Before and during the treatment it is necessary to conduct an examination of the oculist (visual acuity, color vision, eye fundus).

Form release / dosage:Ampoules 50 mg / ml.

Packaging:

For 5 ml of the drug in a vial of neutral glass, 5 ampoules per contour cell pack of PVC film and aluminum foil.

For 1 or 2 contour squares, together with the instructions for use, will prevent the cardboard package from being inserted.

For 20, 50 or 100 contour mesh packages, respectively, with 10, 25 and 50 instructions for use are placed in boxes of cardboard or in boxes of corrugated cardboard (for inpatient).

Storage conditions:

At a temperature not higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001709/07

Date of registration:26.07.2007

The owner of the registration certificate:NIZHFARM, JSC NIZHFARM, JSC Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Tranexam® (Tranexam®)