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

Antifibrinolytic agent. Tranexamic acid specifically inhibits the activation of profibrinolysin (plasminogen) and its conversion to fibrinolysin (plasmin). 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.

Pharmacokinetics:

Absorption at oral intake of doses in the range of 0.5-2 g is 30-50%. The time of maximum concentration with oral intake of 0.5, 1 and 2 g is 3 hours, the maximum concentration is 5, 8 and 15 μg / ml, respectively.The connection with plasma proteins (profibrinolysin) is less than 3%.

It is distributed in tissues relatively evenly (except for cerebrospinal fluid, where the concentration is 1/10 of the plasma one); penetrates the placental 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. Antifibrinolytic concentration in various tissues persists for 17 hours, in plasma - up to 7-8 hours.

Metabolizes a small part. The curve of the area under the curve has a three-phase form with a half-life in the final phase of 3 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 derivative. With impaired renal function, there is a risk of cumulation of tranexamic acid.

Indications:

Bleeding or risk of bleeding in the background:

- strengthening local fibrinolysis (uterine,including von Willebrand disease and other coagulopathies, nasal, gastrointestinal bleeding, hematuria, bleeding after prostatectomy, conization of the cervix for cancer, extraction of the tooth in patients with hemorrhagic diathesis);

- strengthening of generalized fibrinolysis (malignant neoplasms of the pancreas and prostate gland, operations on the thoracic organs, postpartum haemorrhages, manual detachment, leukemia, liver disease).

Bleeding during pregnancy.

Hereditary angioedema, allergic diseases (eczema, allergic dermatitis, urticaria, drug and toxic rash).

Inflammatory diseases (tonsillitis, pharyngitis, laryngitis, stomatitis, aphthae of the oral mucosa).

Contraindications:

Hypersensitivity to the drug, subarachnoid hemorrhage.

Carefully:

Carefully the drug is prescribed for thrombosis (thrombosis of the cerebral vessels, myocardial infarction, thrombophlebitis) or the threat of their development, with thrombohemorrhagic complications (in combination with heparin and indirect anticoagulants), violation of color vision,hematuria from the upper parts of the urinary tract (possible obstruction by a blood clot), renal insufficiency (cumulation possible).

Dosing and Administration:

Inside.

With local fibrinolysis appoint 1000-1500 mg 2-3 times a day.

With profuse uterine bleeding appoint 1000-1500 mg 3-4 times a day for 3-4 days.

When bleeding against the background of Willebrand disease and other coagulopathies 1000-1500 mg 3-4 times a day. The duration of the course of treatment is 3-10 days.

After the operation, conization of the cervix is prescribed 1500 mg 3 times a day for 12-14 days.

With nasal bleeding appoint 1000 mg 3 times a day for 7 days.

Patients with coagulopathies after extraction of the tooth are prescribed 1000-1500 mg 3-4 times a day for 6-8 days.

When bleeding during pregnancy 250-500 mg 3-4 times a day until the complete stop of bleeding. The average duration of the course of treatment is 7 days.

When hereditary angioedema is prescribed, 1000-1500 mg 2-3 times a day, continuously or intermittently, depending on the presence of prodromal symptoms.

With symptoms of allergy and inflammation, 1000-1500 mg 2-3 times a day for 3-9 days, depending on the severity of the condition.

With generalized fibrinolysis, therapy is started with parenteral (intravenous) administration of Tranexam followed by a transition to oral administration of 1000-1500 mg 2-3 times a day.

In case of disturbance of the excretory function of the kidneys, correction of the dosing regimen is necessary: at a creatinine concentration of 120-250 μmol / l, 1000 mg 2 times a day is prescribed; at a creatinine concentration of 250-500 μmol / l, 1000 mg once a day is prescribed; at a creatinine concentration of more than 500 μmol / l, 500 mg once a day are prescribed.

Side effects:

When taking the drug, nausea, vomiting, heartburn, diarrhea, rash, itching, loss of appetite, drowsiness, dizziness may occur. There may be a violation of color perception; rarely - thrombosis, thromboembolism.

Interaction:

When combined with hemostatic drugs and hemocoagulase, thrombus formation can be activated.

Special instructions:

Before and during the treatment it is necessary to conduct an examination of the oculist for visual acuity, color perception, and the condition of the fundus.

In studies on animals, teratogenic and embryotoxic effects were not detected.

Form release / dosage:Tablets, film-coated, 250 mg.

Packaging:For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered. 1, 2, 3, 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LS-001070

Date of registration:15.02.2010

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

Manufacturer: & nbsp

OBNINSKAYA CHEMICAL - PHARMACEUTICAL COMPANY, CJSC Russia

Information update date: & nbsp31.08.2015

Illustrated instructions

Instructions

Tranexam® (Tranexam®)