Fibrinolysis inhibitors: drugs, mechanism of action, indications

The word "fibrinolysis" in Greek means "decomposition" or "dissolution". This process of splitting blood clots and blood clots, which is part of homeostasis and is accompanied by coagulation. For humans, this is a natural defensive reaction of the body. It prevents thrombosis and helps restore cells after heavy blood loss. Fibrinolysis inhibitors are a group of drugs that have a hemostatic effect.

What is it

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 dissolve, blood clots break down, and clogging 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, red blood cells, platelets, white blood cells are responsible for the regeneration. Thanks to the internal mechanism, the vessels are cleaned of fibrin formed during blood coagulation. In the second case, tissue activators are involved in the recovery process. These include plasminogen and urokinase.

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 that stimulate fibrinolysis are triggered. If the tone of the parasympathetic nervous system rises, blood coagulation accelerates. A healthy person has a balance between coagulation and fibrinolysis, its dilution. 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. Use of these substances is allowed only on the recommendation of your doctor.

The properties

Fibrinolysis inhibitors inhibit the blood thinning process. They inhibit 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 that inhibit blood thinning, but improve its coagulability. Plasmin is considered the main catalyst in fibrinolysis. On the contrary, it decomposes fibrin. Inhibitors reduce plasminogen activity.

Amben injections instructions

How do they act

Fibrinolysis inhibitors are hemostatic. 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 plasminogen, 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 the fibrinogen level. The substance is rapidly absorbed in the gastrointestinal tract. Acid reaches its maximum concentration in the blood within two hours after administration. If taken orally, approximately sixty percent is excreted 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 becomes the cause of 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 inhibitors drugs

Indications for use

In what cases are fibrinolysis inhibitors prescribed? Indications for the use of these drugs are as follows:

  • Heavy bleeding associated with high fibrinolytic activity of the blood.
  • Blood loss after surgery (surgery on the lungs, thyroid and pancreas, removal of the prostate)
  • Detachment of the placenta. Finding a dead fetus in the uterus for a long time.
  • Cirrhosis of the liver, kidney disease.
  • Pancreatitis
  • Gastric and duodenal ulcer.
  • Sepsis.

Inhibitors are taken as tablets or intravenously.

fibrinolysis inhibitors mechanism of action

Contraindications

Strictly following the instructions for the use of Amben injections and other inhibitors, as well as the dosage prescribed by the doctor, will help to avoid pronounced 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. Inhibitors should not be prescribed 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 disease. It is important to monitor the patient's condition during the entire therapeutic period and check the content of fibrinogen in the blood.

Aminocaproic acid solution, like other drugs inhibitors, have side effects. They occur if the patient is prescribed the usual dose, as well as with impaired renal function. Side effects of taking inhibitors include allergic reactions, inflammation of the airways, skin rash, nasal congestion, ringing in the ears, burning eyes and redness, nausea, diarrhea, fluctuations in blood pressure, dizziness, weakness, and heart rhythm disturbances. You can not take aprotinin and aminocaproic acid at the same time. This leads to blood clots.

fibrinolysis inhibitors indications

Drug List

Drugs are prescribed by the attending physician in case of bleeding, for prophylaxis, after surgery, including operations on organs that have many tissue fibrinolysis activators. For example, aminocaproic acid is taken orally at fifteen grams per day, sharing techniques. A five percent solution of 100 ml is administered 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 the pharmacological effect. Each medicine has its own. Substances of this group are opposed to fibrinolytics. Inhibitors stop bleeding and stabilize fibrin. To the group of such drugs include tranexanoic and aminocaproic acid, paraaminomethylbenzoic acid. Aprotinin belongs to the natural inhibitors of trypsin and plasmin. Thanks to them, the level of proteases in the blood and tissues decreases, inflammation in the pancreas is removed. These drugs are recommended for bleeding that causes surgery, trauma, childbirth, as well as complications after thrombolytic therapy. Fibrinolysis inhibitors include Amben, Gordoks, Kontrikal 10000, Aprotex, Aerus, Gumbiks, Ingitril, Pamba, Restikam, Traneksam, Exazil, "Traskolan" and others.

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 crystalline powder. It has no taste, odor and color, it is well soluble in water. Do not use with hypersensitivity during pregnancy. It 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 the use of Amben injections say that they are also prescribed for bleeding (postoperative, uterine, gastrointestinal, nasal), leukemia, sepsis.

fibrinolysis inhibitors classification

Tranexam

This is a hemostatic drug for the conversion of plasminogen to plasmin. It does not allow the formation of kinins, which cause inflammation and allergies. It stops blood loss during pathologies, acts as an analgesic. It is prescribed for the risk of bleeding against the background of increased fibrinolysis, with malignant neoplasms, inflammatory processes, allergic diseases. Dosage is set individually. The drug has contraindications and side effects from the cardiovascular, digestive, coagulation system, as well as the central nervous system. It can not be used if the patient has an increased sensitivity to the composition of the drug.


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