Tranexam
Active material: Tranexamic acid
When ATH: B02AA02
CCF: Hemostatic drug. An inhibitor of fibrinolysis – inhibitor of plasminogen to plasmin is transition
ICD-10 codes (testimony): C25, C61, D66, D67, D69.3, J02, J03, J04, K12, K25.0, K26.0, L20.8, L23, L24, L50, N93, O72, R58, T78.3, T81.0, T88.7, Z29.2
When CSF: 20.01.02.02
Manufacturer: MIR-PHARM LTD (Russia)
Pharmaceutical form, composition and packaging
Pills, coated (film) white, lenticular.
| 1 tab. | |
| tranexamic acid | 250 mg |
Excipients: microcrystalline cellulose, hydroksypropyltsellyuloza, sodium carboxymethyl starch (sodium starch glycolate), talc, calcium stearate, colloidal silicon dioxide (aэrosyl).
The composition of the shell: gipromelloza, Titanium dioxide, talc, polyethylene glycol 6000.
10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.
The solution for the on / in the clear or almost clear, colorless or light-brown tint.
| 1 ml | 1 amp. | |
| tranexamic acid | 50 mg | 250 mg |
Excipients: water d / and.
5 ml – ampoule (5) – packings Valium planimetric (2) – packs cardboard.
Pharmacological action
Hemostatic drug. An inhibitor of fibrinolysis. Specifically inhibits the activation of plasminogen and its conversion into plasmin. It has local and systemic hemostatic effect of bleeding, associated with increased fibrinolysis (pathology of platelets, menorragii).
By suppressing the formation of kinins and other active peptides, involved in allergic and inflammatory reactions, It has anti-allergic and anti-inflammatory action.
In experimental studies confirmed the site of analgesic activity of tranexamic acid, and potentiating effect on the analgesic activity of opioid analgesics.
Pharmacokinetics
Absorption
When administered at a dose of 0.5-2 g absorbed 30-50% product. When administered in doses 0.5, 1 and 2 Mr time to reach Cmax – 3 no, and is 5, 8 and 15 ug / ml, respectively.
Distribution
Plasma protein binding (plasminogen) – less 3%.
Distributed relatively evenly in the tissue (except cerebrospinal fluid, wherein the concentration of 1/10 from plasma). It penetrates through the placental barrier and the blood-brain barrier, excreted in breast milk (reaching approximately 1% the concentration in maternal plasma). Found in seminal fluid, which reduces the fibrinolytic activity, but has no effect on the migration of spermatozoa. Initial Vd – 9-12 l. Antifibrinolytic concentration in various tissues retained for 17 no, plasma – to 7-8 no.
Metabolism and excretion
It is metabolized to a minor extent. Identified 2 metabolite traneksamovoy kislotы: N-acetylated and deaminated derivatives. AUC curve has the shape of a three-phase to the T1/2 in the final phase – 3 no. The total renal clearance is plasma (7 l /). Report the news (the basic way – glomerular filtration), more 95% as unchanged during the first 12 no.
Pharmacokinetics in special clinical situations:
If the kidney function there is a risk of cumulation of tranexamic acid.
Testimony
- Bleeding or risk of bleeding against the backdrop of generalized enhance fibrinolysis (bleeding during surgery and in the postoperative period, postpartum hemorrhage, manual removal of placenta, chorionic detachment, Bleeding during pregnancy, malignancies, pancreatic and prostate, hemophilia, hemorrhagic complications of fibrinolytic therapy, trombotsitopenicheskaya purpura, leukemia, liver disease, predshestvuyushtaya therapy streptokinazoy);
- Bleeding or risk of bleeding against the backdrop of strengthening local fibrinolysis (Uterine, Nasal, gastrointestinal bleeding, hematuria, bleeding after prostatectomy, conization of cervical carcinoma over, tooth extraction in patients with bleeding diathesis);
- Hereditary angioedema (Pill);
- Allergic diseases, incl. eczema, allergic dermatitis, hives, drug and toxic rash (Pill);
- Inflammatory diseases of the oral cavity and pharynx, in t.ch.tonzillit, pharyngitis, laringit, stomatitis, aphthae oral mucosa (Pill);
- Surgery on the bladder (for a solution);
- Surgical procedures in the systemic inflammatory response, incl. sepsis, peritonitis, pankreonekroz, heavy and moderate preeclampsia, the shock of various etiologies (for a solution).
Dosage regimen
At generalized fibrinolysis the drug is administered in / drip in a single dose 15 mg / kg of body weight every 6- 8 no, introduction rate 1 ml / min.
At Local fibrinolysis introducing drug / in a single dose 250-500 mg oral dose or 1.0-1.5 g 2-3 times / day.
At prostatectomy or bladder surgery introduced in / during operation 1 g, then 1 g every 8 h for 3 days, then go to the reception to the disappearance of gross hematuria inside.
At high risk of bleeding, systemic inflammatory response introduced in / dose 10-11 mg / kg 20-30 minutes prior to the intervention.
Patients with coagulopathies prior to extraction of the tooth is introduced in / dose 10 mg / kg body weight, After estraktsii tooth prescribed oral dose 25 mg / kg 3-4 times / day for 6-8 days.
At profuse uterine bleeding administered orally at a dose 1.0-1.5 g 3-4 times / day for 3-4 days.
At repeated nosebleeds drug prescribed oral dose 1 g 3 times / day for 7 days.
After cervical conization surgery administered orally at a dose 1.5 g 3 times / day for 12-14 days.
At hereditary angioedema appointed interior 1-1.5 g 2-3 times / day continuously or intermittently depending on the presence of prodromal symptoms.
Patients with impaired renal function necessary correction mode.
| The concentration of creatinine in the blood | The dose of oral Traneksama | Traneksama dose for i / v administration |
| 120-250 mmol / l | 15 mg / kg 2 times / day | 10 mg / kg 2 times / day |
| 250-500 mmol / l | 15 mg / kg 1 time / day | 10 mg / kg 1 times / day |
| >500 mmol / l | 7.5 mg / kg 1 time / day | 5 mg / kg 1 time / day |
Side effect
From the digestive system: anorexia, nausea, vomiting, heartburn, diarrhea.
CNS: dizziness, weakness, drowsiness, violation of color, blurred vision.
From the blood coagulation system: rarely – thrombosis, thromboembolism.
Cardio-vascular system: tachycardia, chest pain, hypotension (With the rapid on / in a).
Allergic reactions: skin rash, itch, hives.
Contraindications
- Subarachnoid hemorrhage;
- Hypersensitivity to the drug.
C caution should be prescribed the drug for thrombosis (incl. thrombosis of cerebral vessels, myocardial infarction, deep vein thrombophlebitis, thromboembolic syndrome) or the threat of their development, thrombohemorrhagic complications (in combination therapy with heparin and indirect anticoagulants), breach of color vision, haematuria from the upper urinary tract (vozmozhna obstruction krovyanыm sgustkom), renal failure (because of the increased risk of cumulation).
Pregnancy and lactation
It is used during pregnancy if indicated with the obligatory account contraindications, tranexamic acid crosses the placental barrier and is excreted in breast milk (reaching approximately 1% the concentration in maternal plasma).
Cautions
Before and during treatment is necessary to conduct inspections ophthalmologist for visual acuity, tsvetovospriyatiya, the state of the fundus.
Overdose
Data on overdose are not provided.
Drug Interactions
In a joint application with hemostatic drugs and gemokoagulazoy possible activation of thrombosis.
The solution for the on / in a pharmaceutically compatible with blood, solutions, soderjaşçïmï penicillin, urokinase, hypertensive agents (norepinephrine, dezoksiepinefrinom gidroxloridom, metarminom ʙitartratom), Tetracycline, dipiridamolom, diazepamom.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored in a dry, inaccessible to children at temperature not exceeding 25 ° C. Shelf life - 3 year. Do not use after the expiry date, on the package.
