Tranexam, 30 pcs., 250 mg, film-coated tablets

Nosological classification (ICD-10)

• D68.0 Von Willebrand disease
• D69.9 Hemorrhagic condition, unspecified
• J02 Acute pharyngitis
• J03 Acute tonsillitis [tonsillitis]
• J31.2 Chronic pharyngitis
• J35.0 Chronic tonsillitis
• K12 Stomatitis and related lesions
• K12.0 Recurrent oral aphthae
• K76.9 Liver disease, unspecified
• K92.2 Gastrointestinal bleeding, unspecified
• L20 Atopic dermatitis
• L27.0 Generalized skin rash caused by drugs and medications
• L27.1 Localized skin rash caused by drugs and medications
• L30.9 Dermatitis, unspecified
• L50 Urticaria
• N93.9 Abnormal uterine and vaginal bleeding, unspecified
• O20 Bleeding in early pregnancy
• O46 Antepartum haemorrhage, not elsewhere classified
• O72.2 Late or secondary postpartum hemorrhage
• O83.2 Childbirth with other obstetric manipulations [manual techniques]
• R04.0 Nosebleed
• R21 Rash and other nonspecific skin eruptions
• R31 Nonspecific hematuria
• R58 Bleeding, not elsewhere classified
• T78.3 Angioedema
• T78.4 Allergy, unspecified
• T81.0 Bleeding and hematoma complicating the procedure, not elsewhere classified
• Z100* CLASS XXII Surgical practice

Compound

Pharmacodynamics

Tranexamic acid is an antifibrinolytic agent that specifically inhibits the activation of profibrinolysin (plasminogen) and its conversion to fibrinolysin (plasmin). It has local and systemic hemostatic effects in bleeding associated with increased fibrinolysis (platelet pathology, menorrhagia), as well as anti-inflammatory, anti-allergic, anti-infective and anti-tumor effects due to the suppression of the formation of kinins and other active peptides involved in allergic and inflammatory reactions. The experiment confirmed the intrinsic analgesic activity of tranexamic acid, as well as the potentiating effect on the analgesic activity of opiates.

Pharmacokinetics

Absorption after oral administration of doses in the range of 0.5–2 g is 30–50%. Tmax when taken orally 0.5; 1 and 2 g - 3 hours, Cmax - 5; 8 and 15 μg/ml, respectively. Plasma protein binding (profibrinolysine) - less than 3%.

Distributed relatively evenly in tissues (with the exception of cerebrospinal fluid, where the concentration is 1/10 of the plasma concentration); penetrates the placental barrier into breast milk (about 1% of the concentration in maternal plasma). It is found in seminal fluid, where it reduces fibrinolytic activity, but does not affect sperm migration. The initial volume of distribution is 9–12 l. Antifibrinolytic concentration in various tissues lasts 17 hours, in plasma - up to 7-8 hours.

A small part is metabolized. The AUC curve has a three-phase shape with T1/2 in the final phase - 3 hours (for solution for intravenous administration - 2 hours). Total renal clearance is equal to plasma (7 l/h). Excreted by the kidneys (the main route 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. In case of impaired renal function, there is a risk of accumulation of tranexamic acid.

Indications of the drug Tranexam®

Pills

bleeding or risk of bleeding due to:

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

- increased generalized fibrinolysis (malignant neoplasms of the pancreas and prostate glands, operations on the chest organs, postpartum hemorrhage, manual separation of the placenta, leukemia, liver diseases);

bleeding during pregnancy;

hereditary angioedema, allergic diseases (eczema, allergic dermatitis, urticaria, drug and toxic rashes);

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

Solution for intravenous administration

bleeding or the risk of bleeding against the background of increased fibrinolysis, as generalized (bleeding during operations and in the postoperative period, postpartum hemorrhage, manual separation of the placenta, chorionic detachment, bleeding during pregnancy, malignant neoplasms of the pancreas and prostate glands, hemophilia, hemorrhagic complications of fibrinolytic therapy, thrombocytopenic purpura, leukemia, liver disease, previous therapy with streptokinase), and local (uterine bleeding, after conization of the cervix for carcinoma, nasal, pulmonary, gastrointestinal, hematuria, bleeding after prostatectomy, tooth extraction in patients with hemorrhagic diathesis);

surgical interventions on the bladder;

surgical manipulations for systemic inflammatory reactions (sepsis, peritonitis, pancreatic necrosis, severe and moderate gestosis, shock of various etiologies and other critical conditions).

Tranexam®

Tranexamic acid solution is administered intravenously very slowly; tranexamic acid cannot be administered intramuscularly.

Convulsions

Cases of seizures have been described that have been associated with the use of tranexamic acid. In patients undergoing coronary artery bypass surgery, seizures, in most cases, developed when tranexamic acid was used in high doses. When using the drug in recommended doses, the frequency of seizures after

surgery was the same as in patients who did not receive tranexamic acid.

Visual impairment

When using tranexamic acid, visual impairment may develop, including impaired color perception. Before starting and during long-term treatment with tranexamic acid, it is necessary to conduct an examination by an ophthalmologist (visual acuity, color vision, fundus). If visual impairment occurs during treatment, discontinuation of the drug is necessary.

Hematuria

Tranexamic acid preparations should be used with caution in hematuria caused by diseases of the renal parenchyma, since intravascular fibrin deposition is often observed in these conditions, which can aggravate renal damage. In addition, in cases of massive bleeding of any etiology from the upper urinary tract, antifibrinolytic therapy increases the risk of blood clots in the renal pelvis and/or ureter and, accordingly, secondary mechanical obstruction of the urinary tract and the development of anuria.

Thromboembolic events

Before using tranexamic acid, possible risk factors for thromboembolic events should be taken into account. In patients with a history of thromboembolic disease or in patients with an increased incidence of thromboembolic events in the family history (patients at high risk of thrombophilia), tranexamic acid injection should only be prescribed for strict medical indications after consultation with a hemostasis specialist. The use of the drug in such patients should be carried out under close medical supervision.

Tranexamic acid should be used with caution in patients receiving oral contraceptives due to the increased risk of thrombosis.

The effectiveness and safety of tranexamic acid preparations in the treatment of menorrhagia in patients under 16 years of age have not been established.

Disseminated intravascular coagulation syndrome (DIC syndrome)

The use of tranexamic acid in patients with DIC is contraindicated in most cases. Tranexamic acid can be prescribed to such patients only if the patient has symptoms of predominant activation of the fibrinolytic system with acute severe bleeding. In such acute cases, a single dose of tranexamic acid 1 g is often sufficient to stop bleeding. The prescription of tranexamic acid for disseminated intravascular coagulation should be made only if appropriate laboratory data are available and after evaluation of these data by a specialist.

Due to the lack of adequate clinical studies, the simultaneous use of tranexamic acid preparations with anticoagulants should be carried out under the careful supervision of a specialist experienced in the treatment of blood clotting disorders.

Side effects

Pills

Nausea, vomiting, heartburn, diarrhea, rash, itching, decreased appetite, drowsiness, and dizziness may occur. Color vision disturbance may occur; rarely - thrombosis, thromboembolism.

Solution for intravenous administration

Allergic reactions (rash, skin itching, urticaria), dyspeptic symptoms (anorexia, nausea, vomiting, heartburn, diarrhea), dizziness, weakness, drowsiness, tachycardia, chest pain, hypotension (with rapid intravenous administration), color disturbance vision, blurred vision; thrombosis or thromboembolism (the risk of development is minimal).

Contraindications and side effects

Tablets and injection solution should not be used if you have an individual intolerance to the active substance or auxiliary components. There is also an absolute contraindication for use in the case of diagnosed subarachnoid bleeding.

Tranexam is used with caution in the presence of thrombosis or an increased risk of its development, as well as in thrombohemorrhagic complications, in the case of renal failure, impaired color discrimination and hematuria.

During a course of therapy using Tranexam tablets and injections, the following side effects are possible:

• allergic manifestations;
• dizziness;
• weakness;
• increased drowsiness;
• tachycardia;
• dyspepsia;
• decreased blood pressure;
• chest pain;
• violation of color discrimination;
• thrombosis;
• thromboembolism, etc.

Directions for use and doses

Pills

Inside.

For local fibrinolysis, 1000–1500 mg is prescribed 2–3 times a day.

For profuse uterine bleeding, 1000–1500 mg is prescribed 3–4 times a day for 3–4 days.

For bleeding due to von Willebrand disease and other coagulopathies - 1000–1500 mg 3–4 times a day. The duration of treatment is 3–10 days.

After cervical conization surgery, 1500 mg is prescribed 3 times a day for 12–14 days.

For nosebleeds, 1000 mg is prescribed 3 times a day for 7 days.

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

For bleeding during pregnancy - 250-500 mg 3-4 times a day until bleeding stops completely. The average duration of treatment is 7 days.

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

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

For generalized fibrinolysis, therapy begins with parenteral (iv) administration of the drug Tranexam®, followed by switching to oral administration of 1000–1500 mg 2–3 times a day.

In case of impaired renal excretory function, correction of the dosage regimen is necessary: ​​if the concentration of creatinine in the blood is 120–250 µmol/l, 1000 mg is prescribed 2 times a day; if the creatinine concentration is 250–500 µmol/l, 1000 mg is prescribed once a day; if the creatinine concentration is more than 500 µmol/l, 500 mg is prescribed once a day.

Solution for intravenous administration

IV (drip, stream).

For generalized fibrinolysis, a single dose of 15 mg/kg is administered every 6–8 hours, the injection rate is 1 ml/min.

For local fibrinolysis, it is recommended to administer the drug at a dose of 250–500 mg 2–3 times a day.

For prostatectomy or bladder surgery, 1 g is administered during surgery, then 1 g every 8 hours for 3 days, after which they switch to oral tablet form until gross hematuria disappears.

With a high risk of bleeding, with a systemic inflammatory reaction - at a dose of 10-11 mg/kg 20-30 minutes before the intervention.

Patients with coagulopathies are administered a dose of 10 mg/kg before tooth extraction; after tooth extraction, oral tablet form of the drug is prescribed.

In case of impaired renal excretory function, it is necessary to adjust the dosage regimen depending on the concentration of creatinine in the blood: if the concentration of creatinine in the blood is 120–250 µmol/l, 10 mg/kg is prescribed 2 times a day; at 250–500 µmol/l - 10 mg/kg 1 time per day; at >500 µmol/kg - 5 mg/kg 1 time per day.

Tranexam tablets: special instructions

Regardless of the diagnosis and age of the patient, before starting a course of therapy, an appointment with an ophthalmologist is indicated, who must conduct standard examinations:

• color perception;
• determination of visual acuity;
• fundus examination.

Tranexam is often used to treat heavy bleeding during menstruation. Moreover, in these cases, doctors prescribe the drug only in tablets. You need to take 3-4 pieces one at a time. per day for no more than 4 days.

Also, tablets are used to stop uterine bleeding of various natures. But only a doctor can prescribe an appointment - self-medication in this case is excluded.

During pregnancy and lactation, the drug can be prescribed only in the presence of bleeding. The active ingredient passes freely into breast milk, so the product can only be used in a limited dosage of up to 500 mg per day. In this case, the duration of the course is no more than 7 days.

Attention!

Drinking alcohol during the course of therapy is excluded.

Release form

Film-coated tablets, 250 mg, 500 mg. In a blister pack made of PVC film and printed varnished aluminum foil, 10 pcs. 1, 2, 3, 5 blister packs in a cardboard pack.

Solution for intravenous administration, 50 mg/ml. In neutral glass ampoules, 5 ml. In blister packs made of PVC film and aluminum foil, 5 pcs. 1 or 2 blister packs in a cardboard pack. 20, 50 or 100 blister packs in cardboard boxes or corrugated cardboard boxes (for hospital use).

Analogues and prices

Tranexam can be purchased at a pharmacy. Price 10 tablets with a dosage of 250 mg - from 250 rubles. The cost of 10 ampoules (5 ml each) of the product is from 220 rubles.

The drug has several analogues:

1. Dicynone. Widely used in veterinary practice. The medication has no contraindications for pregnant animals and kittens. May cause vomiting and allergic reactions. Pharmaceutically incompatible (in the same syringe) with other drugs. Price 10 ampoules (2 ml each) - from 130 rubles. The average cost of tablets (100 pieces, 250 mg each) is 360 rubles.
2. Vikasol. This is a synthetic analogue of vitamin K. It is used with caution in the treatment of animals with liver pathologies and pregnant cats. The cost of a package of tablets (20 pieces of 15 mg each) is from 40 rubles, a solution of 1% (10 ampoules of 1 ml each) is from 45 rubles.
3. Etamzilat. Effective for deep cuts and heavy bleeding due to injury. Taking the medication minimizes the risk of internal hemorrhages in the postoperative period. Does not have a vasoconstrictor effect. The product should not be used for thrombosis. Etamsylate may cause allergic reactions. The average cost of an injection solution (10 ampoules of 2 ml each) is 80 rubles. The price of tablets (100 pieces, 250 mg each) is from 350 rubles.
4. Capramin. It is a hemostatic fluid. A sterile swab is moistened with the medication and applied to the wound for several minutes. Convenient to use for scratches, shallow cuts, abrasions. The cost of a bottle (30 ml) is from 130 rubles.

Tranexam is a popular drug for stopping bleeding in animals, which is not inferior in effectiveness to analogues. However, the price of the medicine is higher than that of similar drugs.

The medicine may cause side effects, so before giving it to your cat, you should consult your doctor. To determine the exact dosage of tablets or to administer the solution intravenously, you should also contact your veterinarian.