Instructions Hemotran solution for injection 100 mg/ml ampoule 5 ml No. 5
Composition
active ingredient: 1 ml of solution contains tranexamic acid, calculated as 100% dry matter, 50 mg or 100 mg;
excipient: water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: transparent colorless or light brown solution.
Pharmacotherapeutic group
Antihemorrhagic agents. Fibrinolysis inhibitors.
ATX code B02A A02.
Pharmacological properties
Pharmacodynamics
Hemotran® is an antifibrinolytic agent. Tranexamic acid competitively inhibits the activation of plasminogen and its conversion to plasmin. It has a hemostatic effect in bleeding associated with increased fibrinolysis, as well as anti-allergic and anti-inflammatory effects by inhibiting the formation of kinins and other active peptides involved in allergic and inflammatory reactions.
Pharmacokinetics
After intravenous administration of a 1 g dose, the concentration-time curve shows three-exponential kinetics with a mean terminal elimination half-life of approximately 2 hours. The initial volume of distribution is approximately 9-12 l. Excreted in the urine. Excreted by the kidneys by glomerular filtration. The total renal excretion rate is equivalent to the total plasma clearance (110-116 ml/min). More than 95% of the administered dose is excreted in the urine unchanged. Tranexamic acid is excreted approximately 90% within 24 hours after intravenous administration of the drug at a dose of 10 mg/kg body weight. Tranexamic acid crosses the placental barrier. The concentration in umbilical cord blood after intravenous administration of the drug at a dose of 10 mg/kg body weight in pregnant women is approximately 30 mg/l. Tranexamic acid rapidly penetrates into the synovial fluid and synovial membrane. In the synovial fluid, it reaches the same concentration level as in the blood serum. The half-life of tranexamic acid fluid is about 3 hours. The concentration of tranexamic acid in the blood is lower than in other tissues. In breast milk, the concentration is about 1/100 of the peak concentration in the blood serum. The concentration of tranexamic acid in the cerebrospinal fluid is about 1/10 of the plasma concentration, in the intraocular fluid - about 1/10 of the plasma concentration.
Indication
Bleeding or risk of bleeding with increased fibrinolysis, both generalized (bleeding during prostate surgery and in the postoperative period, hemorrhagic complications of fibrinolytic therapy) and local (uterine, gastrointestinal bleeding, bleeding after prostatectomy, tonsillectomy, conization of the cervix, tooth extraction in patients with hemophilia).
Contraindication
Hypersensitivity to tranexamic acid and components of the drug. History of thromboembolic diseases, high risk of thrombosis, severe renal failure, macroscopic hematuria, myocardial infarction, subarachnoid hemorrhage, coagulopathy due to diffuse intravascular coagulation (DIC) without significant activation of fibrinolysis, color vision impairment.
Interaction with other medicinal products and other types of interactions
The drug can be used with isotonic sodium chloride and glucose solution, 20% fructose solution, 10% invertase solution, dextran 40 or 70, Ringer's solution. The drug should be used with caution in combination with heparin in patients with blood clotting disorders.
Heparins can be added to intravenous drip administration.
Concomitant therapy with chlorpromazine and tranexamic acid in patients with subarachnoid hemorrhage may lead to cerebral vasospasm and cerebral ischemia, and a decrease in cerebral blood flow is also possible.
The drug is incompatible with urokinase, norepinephrine bitartrate, desoxyepinephrine hydrochloride, dipyridamole, diazepam.
Use with caution in patients receiving antifibrinolytic therapy.
When used simultaneously with estrogens, the risk of blood clots increases.
Application features
Intravenous injections should be administered slowly. Tranexamic acid should not be administered intramuscularly.
Rapid intravenous administration may cause dizziness and hypotension. To avoid hypotension, the drug should be administered slowly and at a rate of no more than 1 mg per minute.
In patients with disseminated intravascular coagulation (DIC), treatment should be restricted to those with predominant activation of the fibrinolytic system with acute bleeding. Typically, the hematological profile is similar to the following: shortened euglobulin fibrinolytic activity time; prolonged prothrombin time; decreased plasma fibrinogen, factors V and VIII, plasminogen, and a2-macroglobulin; normal plasma levels of P and P-complex, i.e. factors II (prothrombin), VIII, and X; elevated plasma levels of fibrinogen degradation products; and platelet count. The above assumes that the underlying disease does not modify the various elements of this profile. In such acute cases, a single dose of 1.0 g of tranexamic acid is often sufficient to control bleeding. With normal renal function, fibrinolytic activity in the blood will be reduced by approximately 4 hours. Patients with thrombohemorrhagic complications should not use the drug simultaneously with anticoagulants (heparin) to prevent further fibrin deposition. The use of Hemotran® in DIC should only be considered when hematological laboratory facilities and experience are available.
During treatment, observation by an ophthalmologist is necessary for several days, including checking visual acuity, visual fields, and color vision, and examining the fundus.
Tranexamic acid should be used with caution in patients taking oral contraceptives, as the risk of thrombosis is increased.
Convulsions have been reported with the use of tranexamic acid. Most of these cases have been reported after high-dose intravenous tranexamic acid during coronary artery bypass grafting (CABG). At the recommended low doses of tranexamic acid, the incidence of postoperative seizures is similar to that in patients not receiving tranexamic acid.
Use during pregnancy or breastfeeding
Application is possible only in case of urgent need.
Although there is no evidence of teratogenic or other adverse effects during pregnancy, when prescribing the drug, it is necessary to constantly monitor the patient's health. Since tranexamic acid penetrates into breast milk in an amount of approximately 1% of the concentration of the drug in the mother's plasma, an antifibrinolytic effect in the infant is unlikely, but if necessary, breastfeeding is recommended to be discontinued.
Ability to influence reaction speed when driving vehicles or other mechanisms
In cases of adverse reactions from the central nervous system and/or organs of vision, you should refrain from driving or operating other mechanisms.
Method of administration and doses
Administer intravenously (drip, jet).
The dosage regimen is individual, depending on the clinical situation.
In case of generalized fibrinolysis, administer a single dose of 15 mg/kg of body weight every 6-8 hours, the rate of administration is 1 ml/min.
For local fibrinolysis, it is recommended to use the drug at a dose of 200-500 mg 2-3 times a day.
For prostatectomy, administer 1 g during surgery, then 1 g every 8 hours for 3 days, then switch to taking the tablet form of tranexamic acid until the macrohematuria disappears.
If there is a high risk of bleeding, in the presence of a systemic inflammatory reaction, it is recommended to use the drug at a dose of 10-11 mg/kg 20-30 minutes before the intervention.
Patients with coagulopathy should be administered the drug at a dose of 10 mg/kg of body weight before tooth extraction, and after tooth extraction, oral tablet form of tranexamic acid should be prescribed.
In cases of impaired renal excretory function, correction of the dosage regimen is necessary: at a creatinine concentration in the blood of 120-250 μmol/l, prescribe 10 mg/kg 2 times a day; at a concentration of 250-500 μmol/l - 10 mg/kg 1 time a day; at a concentration of more than 500 μmol/l - 5 mg/kg 1 time a day.
Children: Single dose is 10 mg/kg, administered twice daily.
Elderly patients: In the absence of renal dysfunction, dose adjustment is not required.
Children
Used in pediatric practice.
Overdose
Nausea, vomiting, orthostatic symptoms, and hypotension may occur.
Treatment: symptomatic therapy, forced diuresis, maintenance of water-salt balance.
Adverse reactions
On the part of the digestive tract: nausea, vomiting, diarrhea, feeling of discomfort in the stomach and intestines.
Nervous system: convulsions, dizziness.
Cardiovascular system: arterial hypotension (especially after rapid intravenous administration), orthostatic hypotension, thromboembolism, deep vein thrombosis, pulmonary embolism, cerebral thrombosis.
From the urinary system: acute necrosis of the renal cortex.
On the part of the organs of vision: visual impairment, chromatopsia.
Hypersensitivity reactions, including anaphylaxis, skin rashes, are possible.
Expiration date
2 years.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging
5 ml in an ampoule. 5 ampoules in a blister. 1 or 2 blisters in a pack.
Vacation category
According to the recipe.
Producer
PJSC "Farmak".
Location of the manufacturer and address of its place of business
Ukraine, 04080, Kyiv, Frunze St., 74.
