Fibrinolysis inhibitors: drugs, mechanism of action, indications

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Fibrinolysis inhibitors: drugs, mechanism of action, indications
Fibrinolysis inhibitors: drugs, mechanism of action, indications

Video: Fibrinolysis inhibitors: drugs, mechanism of action, indications

Video: Fibrinolysis inhibitors: drugs, mechanism of action, indications
Video: Йошкар-Ола 2024, December
Anonim

The word "fibrinolysis" in Greek means "decomposition" or "dissolution". This process of splitting blood clots and thrombi, which is part of homeostasis and is accompanied by clotting. For a person, this is a natural protective reaction of the body. It prevents thrombosis and promotes cell recovery after heavy blood loss. Fibrinolysis inhibitors are a group of drugs that have a hemostatic effect.

What is this

Fibrinolysis inhibitors stop bleeding in various pathological conditions of the patient. Actively used during and after surgery. With the help of the fibrinolysis procedure, blood clots are dissolved, blood clots are broken down, blockage of blood vessels is prevented. Fibrinolysis helps restore blood vessels after blood loss ends. The process proceeds according to the internal and external mechanism. In the first case, plasma activators, erythrocytes, platelets, and leukocytes are responsible for regeneration. Thanks to an internal mechanism, the vessels are cleared of fibrin formed during blood clotting. In the second case, tissue activators are involved in the recovery process. These include plasminogen and urokinase.

fibrinolysis inhibitors
fibrinolysis inhibitors

In the body, the processes of fibrinolysis and blood coagulation are in harmony. If a person has an active sympathetic nervous system, adrenaline and norepinephrine enter the bloodstream, that is, external and internal mechanisms are triggered that stimulate fibrinolysis. If the tone of the parasympathetic nervous system increases, blood clotting accelerates. In a he althy person, there is a balance between coagulability and fibrinolysis, its liquefaction. If this connection is broken, blood clots or a dangerous disease such as hemophilia occur. Fibrinolysis inhibitor drugs are designed to break down clots and help the body if the balance between the two processes has been disturbed. The use of these substances is allowed only on the recommendation of the attending physician.

Properties

Fibrinolysis inhibitors inhibit the process of blood thinning. They prevent the formation of acids and plasminogen-activating enzyme. Inhibitors are designed to stop bleeding in various pathological conditions, as well as during surgery. In the process of fibrinolysis, proteolytic proteins are involved, which inhibit blood thinning, but improve its coagulability. Plasminconsidered the main catalyst in fibrinolysis. On the contrary, it decomposes fibrin. Inhibitors reduce plasminogen activity.

amben instructions for use injections
amben instructions for use injections

How they work

Fibrinolysis inhibitors are hemostatics. They have the ability to inhibit fibrinolysis, block the action of plasmin and plasminogen activators. The group of inhibitors include aminocaproic acid and aprotinin. The drugs block plasminogens, do not allow the formed clots to collapse. Aminocaproic acid increases the level of plasmin, inhibits the secretion of urokinase. If bleeding occurs, the acid normalizes fibrinogen levels. The substance is rapidly absorbed in the gastrointestinal tract. The acid reaches its maximum concentration in the blood within two hours after ingestion. If the drug is taken orally, approximately sixty percent is excreted from the body by the kidneys. The mechanism of action of fibrinolysis inhibitors is simple: hemostatics block plasminogen, inhibit the process of blood splitting. In pathological conditions, high fibrinolysis causes severe, sometimes fatal bleeding. They arise due to injuries of internal organs, an overdose of coagulants. Inhibitors perform an important function: they quickly stop blood loss.

fibrinolysis inhibitor drugs
fibrinolysis inhibitor drugs

Indications for use

When are fibrinolysis inhibitors prescribed? The indications for the use of these drugs are as follows:

  • Excessive bleeding associated with high fibrinolytic activity of the blood.
  • Blood loss after surgery (lung, thyroid and pancreas surgery, prostate removal)
  • Placental abruption. The presence of a dead fetus in the uterus for a long time.
  • Cirrhosis of the liver, kidney disease.
  • Pancreatitis.
  • Stomach and duodenal ulcer.
  • Sepsis.

Inhibitors are taken as tablets or intravenously.

fibrinolysis inhibitors mechanism of action
fibrinolysis inhibitors mechanism of action

Contraindications

Strict adherence to the instructions for the use of Amben injections and other inhibitors, as well as the dosage prescribed by the doctor, will help to avoid severe side effects and other problems. It should be noted that each drug has its own characteristics. For example, aminocaproic acid is not toxic to humans. If the dose is set small, then the patient will not notice any negative manifestations. It is forbidden to prescribe inhibitors to people with a tendency to embolism and thrombosis, patients with impaired renal and hepatic function, during pregnancy. Caution fibrinolysis drug is used in the pathology of cerebral circulation, cardiovascular diseases. It is important to monitor the patient's condition throughout the entire therapeutic period and check the fibrinogen content in the blood.

Aminocaproic acid solution, like other inhibitor drugs, have side effects. They appear if the patient is prescribed the usual doses, as well as in violation of kidney function. Side effects of taking inhibitors include allergic reactions, inflammationrespiratory tract, skin rash, nasal congestion, ringing in the ears, burning eyes and redness, nausea, diarrhea, fluctuations in blood pressure, dizziness, weakness, heart rhythm disturbances. You can not simultaneously take aprotinin and aminocaproic acid. This leads to the formation of blood clots.

fibrinolysis inhibitors indications
fibrinolysis inhibitors indications

Drug list

Drugs are prescribed by the attending physician in case of bleeding, for prevention, after surgery, including operations on organs that have many tissue fibrinolysis activators. For example, aminocaproic acid is taken orally at fifteen grams per day, dividing the doses. A 5% solution of 100 ml is injected dropwise. The dose is set individually. The course of treatment with inhibitors is from six days to four weeks.

The classification of fibrinolysis inhibitors is based on pharmacological action. Each medicine has its own. Substances of this group are opposed to fibrinolytics. Inhibitors stop bleeding and stabilize fibrin. The group of such drugs includes tranexanoic and aminocaproic acids, paraaminomethylbenzoic acid. Aprotinin is a natural inhibitor of trypsin and plasmin. Thanks to them, the level of proteases in the blood and tissues decreases, inflammation in the pancreas is relieved. These drugs are recommended for bleeding caused by surgery, trauma, childbirth, and complications from thrombolytic therapy. The drugs inhibitors of fibrinolysis include "Amben","Gordox", "Kontrykal 10000", "Aproteks", "Aerus", "Gumbix", "Ingitril", "Pamba", "Resticam", "Tranexam", "Exacil", "Traskolan" and others.

aminocaproic acid solution
aminocaproic acid solution

Aminocaproic acid

Like other inhibitors, it is used for bleeding and diseases of internal organs. The drug is available in the form of a crystalline powder. It has no taste, smell and color, it dissolves well in water. Do not use with hypersensitivity, during pregnancy. Has a number of side effects.

Aprotinin

Broad spectrum inhibitor. It is prescribed for heavy blood loss, pancreatitis, postoperative, post-traumatic bleeding, angioedema, shock after burns, injuries, intoxication, for the prevention of embolism, as an additional therapy. The instructions for use of Amben injections say that they are also prescribed for bleeding (postoperative, uterine, gastrointestinal, nasal), leukemia, sepsis.

fibrinolysis inhibitors classification
fibrinolysis inhibitors classification

Tranexam

This is a hemostatic drug converting plasminogen to plasmin. Does not allow the formation of kinins, which cause inflammation and allergies. Stops blood loss in pathologies, acts as an analgesic. It is prescribed at the risk of bleeding against the background of enhanced fibrinolysis, with malignant neoplasms, inflammatory processes, allergicdiseases. The dosage is set individually. The drug has contraindications and side effects on the part of the cardiovascular, digestive, coagulation systems, as well as the central nervous system. Do not use if the patient has hypersensitivity to the composition of the drug.

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