Tranexam: contraindication, drug interactions

Composition, release form

"Tranexam" is a drug with anti-inflammatory, antiallergic and hemostatic effects. Contains tranexamic acid (active ingredient) and additional components, including calcium stearate, talc, silicon dioxide and others.

"Tranexam" is produced in the form of tablets and solutions for intravenous injection. Tablets are sold in packs of 10, 10, 30 and 50 pieces. Ampoules with a volume of 50 ml each are packaged in 5 or 10 pieces.

The drug is released only with a prescription. Store under standard conditions (temperature no higher than 30 degrees). The shelf life of the injection solution and tablets is the same and is 3 years from the date of production.

Indications for the use of Tranexam tablets and solution

The drug is prescribed for bleeding or increased risk of bleeding. They can be associated with various factors, so there are quite a few indications for the use of Tranexam tablets:

• bleeding during pregnancy;
• uterine;
• nasal;
• internal bleeding in the gastrointestinal tract;
• dental;
• stomatitis;
• laryngitis;
• pharyngitis;
• tonsillitis;
• hematuria;
• hereditary angioedema;
• allergic diseases (including rash, skin irritation, urticaria, allergic dermatitis, eczema).

Solutions for intravenous administration are indicated for use against the background of the following pathologies:

• risks of bleeding due to fibrinolysis of various nature;
• consequences of bladder surgery;
• consequences of operations in the presence of systemic inflammation (peritonitis, sepsis, gestosis, shock conditions and others).

Tranexam

Tranexam (tranexamic acid) is a hemostatic drug. Used to treat and prevent blood loss due to decreased blood clotting. The use of blood components and products is associated with an increased risk of developing certain complications: bacterial infection, allergies, so-called. "massive transfusion syndrome." In this regard, the issue of finding safer and more reliable blood-saving technologies is relevant. The process of hemostasis starts immediately from the moment of traumatic damage to the vessel, and ends with the formation of a hemostatic plug in the form of a platelet-fibrin mesh. The latter acts as a mechanical barrier to further blood loss. An imbalance of the hemostatic mechanism has two extremes as a consequence: excessive blood loss and increased thrombus formation. Today, doctors have a number of hemostatic drugs in their arsenal - direct and indirect coagulants, synthetic and animal fibrinolysis inhibitors - each of which, however, has its own limitations for use. Of particular interest in terms of hemostatic and blood-saving technology is Tranexam, a drug based on tranexamic acid. It is an antifibrinolytic that suppresses the activation of the plasmin precursor proenzyme, plasminogen. The medical literature provided data that Tranexam is two orders of magnitude superior to aminocaproic acid in its antifibrinolytic activity in vitro and by an order of magnitude in vivo.

The antifibrinolytic properties of tranexamic acid were discovered in 1962 by the Japanese scientist Okamoto. Then clinical studies were conducted, which proved that pharmacotherapy with Tranexam significantly reduces the amount of blood loss and significantly reduces the need for donor blood products - fresh frozen plasma and red blood cells. In addition, interpretation of coagulogram parameters confirmed a decrease in the severity of excess fibrinolysis. Today Tranexam is a first-line hemostatic agent with a high safety profile and is effective in the treatment and prevention of massive blood loss. Reduces the amount of bleeding after surgery by 30-40%. Reduces the need for blood transfusion by half. Does not increase the risk of thromboembolic complications. Has a systemic anti-inflammatory effect. It is more effective and safe than aminocaproic acid preparations and aprotinin. Has half a century of experience and a solid evidence base in various areas of medicine, including hematology, cardiac anesthesiology, traumatology, obstetrics and gynecology, urology, gastroenterology, oncology, otorhinolaryngology. In case of massive uterine bleeding, it has proven advantages in comparison with non-steroidal anti-inflammatory drugs and etamsylate.

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.

Tranexamic acid (TXA) has been widely used for several decades in obstetric practice, as well as in other areas of medicine for the treatment of bleeding. The mechanism of action of the drug is associated with inhibition of fibrinolysis: TXA blocks the binding of plasmin to fibrin and disrupts the activation of tissue plasminogen activator 1. The use of TXA is especially effective in the first 3 hours from the onset of bleeding against the background of the predominant pathogenetic role of tissue plasminogen activator. The antifibrinolytic effect of the drug remains the reason for some caution among doctors regarding the risk of thrombotic complications. A meta-analysis of 216 studies performed between 1976 and 2020 was published in the journal JAMA Surgery. Only parenteral administration of the drug was analyzed. In total, the analysis included data from 125,550 patients. The analysis showed that the use of tranexamic acid (even at high doses) was not associated with an increased risk of thrombotic complications such as venous thromboembolism, myocardial infarction, ischemic stroke, or coronary or cerebral ischemia.

The overall incidence of these thrombotic complications was 2.1% in the TXA group and 2% in the control group (placebo or no therapy). In patients with a previous history of venous thromboembolism, tranexamic acid also did not increase the risk of thrombotic complications.

The use of tranexamic acid was associated with a reduction in all-cause and bleeding-related mortality.

Very heterogeneous studies were included in the meta-analysis. In a subgroup analysis, there was no clear benefit from tranexamic acid for patients with hemorrhagic stroke or traumatic central nervous system injury in this meta-analysis, which requires separate studies.

The authors conclude that tranexamic acid is an effective and safe drug that can be used in the complex treatment of bleeding. The place of tranexamic acid in neurological practice requires study.

Based on materials:

Taeuber I, Weibel S, Herrmann E, et al. Association of Intravenous Tranexamic Acid With Thromboembolic Events and Mortality: A Systematic Review, Meta-analysis, and Meta-regression. JAMA Surg. Published online April 14, 2021. doi:10.1001/jamasurg.2021.0884

https://jamanetwork.com/

Text: Shakhmatova O.O.

"Tranexam": instructions for use

The dosage, duration of therapy and frequency of doses is determined by the doctor. It depends on the age, diagnosis and general condition of the patient. For example, in the presence of a pathology such as local fibrinolysis, the use of 1000 to 1500 mg of the drug 2 or 3 times a day is indicated.

A similar dosage is established for the treatment of uterine bleeding, but in this case the frequency of administration is 3-4 times. After cervical surgery, the dosage regimen is the same, duration is up to 14 days.

The solution is given intravenously - through a dropper or infusion. The dosage is also determined by the doctor.

Uterine bleeding

Uterine cancer

Cervical cancer

6542 January 27

IMPORTANT!

The information in this section cannot be used for self-diagnosis and self-treatment.
In case of pain or other exacerbation of the disease, diagnostic tests should be prescribed only by the attending physician. To make a diagnosis and properly prescribe treatment, you should contact your doctor. Uterine bleeding: causes of occurrence, what diseases it occurs with, diagnosis and treatment methods.

Definition

Every woman and girl can experience abnormal uterine bleeding. They are a signal of dysfunction of the reproductive, endocrine or nervous systems. This condition usually occurs suddenly, so it is necessary to clearly understand what to do if abnormal uterine bleeding develops.

The uterus is an organ of the female reproductive system, consisting of three layers: internal (endometrium), middle muscular (myometrium) and external (perimetry), which is adipose tissue surrounding the outside of the uterus.

The uterus, like other organs of the female reproductive system, undergoes significant changes during the menstrual cycle, which, in turn, is associated with the maturation of eggs in the ovaries.

The germ cells (cells that are the precursors of the egg) laid down during the intrauterine development of the female fetus are activated and enter into the process of further development every month, but not all at once, but in a strictly defined quantity (about 20–30 cells), while fully maturing only one cell. It leaves the ovary, enters the fallopian tube, through which it gradually moves towards the uterus. If the egg has been successfully fertilized by a sperm, then a zygote is formed - the first cell of the future embryo, which begins to divide and, reaching the uterine cavity, is fixed (implanted) on the surface of the endometrium. If fertilization does not occur, then the egg does not remain in the uterine cavity and is subsequently excreted along with normal menstrual flow. In the process of implantation, the most important role is played by the epithelium lining the uterine cavity from the inside - the endometrium. From the beginning of the menstrual cycle, it grows, thickens and reaches its maximum thickness at the time of ovulation. Next, the endometrium is loosened, which is necessary for successful implantation. If implantation does not occur, then before the start of a new menstruation, endometrial rejection begins, which is preceded by spasm of the uterine arteries. It is the spasm of the uterine arteries that causes the development of pain during the premenstrual period. Next, the arteries relax and become fragile, which leads to the development of bleeding under the endometrium with its further rejection.

Thus, it is the rejected endometrium that is the main component of the discharge from the uterine cavity during uterine bleeding.
Types of Uterine Bleeding
All uterine bleeding can be divided into normal menstrual bleeding and abnormal uterine bleeding. Normal menstrual bleeding is characterized by frequency of occurrence, a certain duration of the menstruation itself (on average from 3 to 7 days) and a small loss of blood (usually about 40-60 ml).

Bleeding that differs in its characteristics from those listed above is considered abnormal in women who have reached reproductive age.

These bleedings are excessive in duration (more than 7 days), volume of blood loss (more than 80 ml), and frequency (including intermenstrual bleeding).

Separately, abnormal bleeding of the pubertal, perimenopausal and postmenopausal periods is distinguished, which is associated with the peculiarities of the functioning of the reproductive and neuroendocrine systems during these age periods.

Possible causes of abnormal uterine bleeding

Identification of the causes of abnormal uterine bleeding formed the basis of the PALM-COEIN classification, widespread throughout the world (many domestic gynecologists also use this classification, indicating this abbreviation in the diagnosis). In accordance with it, the causes of uterine bleeding are divided into organic (structural, accessible to visualization and detection by ultrasound, MRI, etc.) diseases of the female reproductive system and functional, caused by impaired functioning of the reproductive system in the absence of visible changes, as well as those arising from -for disorders of the endocrine system, blood coagulation system, etc.

What diseases cause abnormal uterine bleeding

What diseases are hidden under the abbreviation PALM-COEIN?

• Polyp (polyp) – the presence of polyps, i.e. formations, often benign;

• Adenomyosis (adenomyosis) is a type of endometriosis in which the endometrium grows deep into the wall of the uterus;
• Leiomyoma (leiomyoma, or myoma) is a benign tumor that develops from myometrial tissue;
• Malignancy (malignancy) – malignant (oncological) processes developing from uterine tissue;
• Hyperplasia (hyperplasia) – excessive growth of the endometrium;
• Coagulopathy (coagulopathy) – disorders of the blood coagulation system (for example, hemophilia, von Willebrand disease, etc.), manifested by a tendency to bleeding of various locations (not only uterine bleeding, but also nasal, post-injection, etc.);
• Ovulatory dysfunction (ovulatory dysfunction) – disruption of the functioning of the ovaries, leading to certain changes in the process of egg maturation;
• Endometrial (endometrial dysfunction) – disruption of the functioning of the endometrium in the absence of its visible changes;
• Iatrogenic (iatrogenic cause) – uterine bleeding as a complication in the process of treating a particular disease;
• Not yet classified (not yet classified cause) - other rare or unknown causes of uterine bleeding.

Which doctors should I contact if abnormal uterine bleeding occurs?
Emergency treatment of abnormal uterine bleeding is carried out by an obstetrician-gynecologist. After the bleeding has stopped, the gynecologist continues to care for such a patient, often together with an endocrinologist and mammologist. If abnormalities in the blood coagulation system are detected, the patient is sent for a mandatory consultation with a hematologist (a doctor specializing in blood diseases).

Diagnosis and examination of abnormal uterine bleeding

Diagnosis of the cause of abnormal uterine bleeding begins with a detailed interview of the patient in order to identify risk factors for a particular disease and clarify the circumstances of the development of bleeding. The dates of the last normal menstruation must be specified, and pregnancy is excluded (in the laboratory) using a blood test for hCG (human chorionic gonadotropin).

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.