- What are anticoagulants, farm. the effect
- Indirect anticoagulants
- What it is?
- Contraindications for use
- Pathological anticoagulants
- Anticoagulant preparations: description and list of drugs of direct and indirect action
- What it is?
- New generation oral anticoagulants
- History of discovery
- The price of anticoagulants
Anticoagulants – what is it? These substances are divided into pathological and physiological. The latter are present in plasma in normal, the first are detected subject to the presence of the disease in humans. Natural or natural anticoagulants are divided into primary ones, which the body produces independently, they enter the bloodstream, and secondary ones, which are formed during the breakdown of coagulation factors due to the formation and dissolution of fibrin.
It is described above what anticoagulants are and now it is necessary to understand their types and groups. As a rule, natural primary anticoagulants are divided into:
- fibrin self-assembly inhibitors.
If a person has a decrease in the level of these anticoagulants, there is a likelihood of developing thrombosis. This group includes:
- Heparin. It is synthesized in mast cells and belongs to the class of polysaccharides. It is in a large volume in the liver, lungs. With the growth of this substance, blood coagulation decreases at all stages, which occurs due to the suppression of a number of platelet functions.
- Protein C. It is produced by the cells of the liver parenchyma, is in the blood in an inactive state. Thrombin leads to activity.
- Antithrombin III. Refers to alpha2-glycoproteins, is synthesized in the liver. It is able to reduce the activity of certain activated coagulation factors and thrombin, but does not affect non-activated ones.
- Protein S. It is synthesized by the parenchyma of the liver and endothelial cells, depending on vitamin K.
- Contact, lipid inhibitor.
Thanks to the process of blood coagulation, the body itself ensured that the thrombus does not go beyond the limits of the affected vessel. One milliliter of blood can contribute to coagulation of all fibrinogen in the body.
Due to its movement, the blood maintains a liquid state, as well as due to natural coagulants. Natural coagulants are produced in tissues and then enter the bloodstream, where blood clotting is prevented.
These anticoagulants include:
- Antithrombin III;
- Alpha-2 macroglobulin.
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What are anticoagulants, farm. the effect
The most formidable complication of anticoagulant treatment is hemorrhage in the internal organs: mouth, nasopharynx, intestines, stomach, joints and muscles. Blood may appear in the urine. To prevent these complications, it is necessary to control the blood picture of the patient receiving anticoagulants, and also to monitor his condition as a whole.
Anticoagulants are blood thinners, in addition, they reduce the risk of other thromboses that may appear in the future. There are direct and indirect anticoagulants.
With an overdose of drugs of indirect action, bleeding may begin.
When combined with warfarin with aspirin or other non-steroidal anti-inflammatory drugs (Simvastin, Heparin, etc.), the anticoagulant effect is enhanced.
And vitamin K, laxatives or Paracetamol will weaken the effect of Warfarin.
Side effects when taking:
- Fever, headache;
- Skin necrosis;
- Impaired renal function;
- Nausea, diarrhea, vomiting;
- Itching, abdominal pain;
Before you start taking anticoagulants, you should consult a specialist for contraindications and side effects
Heparin. This drug is the most common direct-acting anticoagulant. No less popular are medicines based on it. Heparin prevents platelets from sticking together, enhances blood flow to the kidneys and heart muscle. However, the possibility of the formation of blood clots with heparin administration should not be ruled out, since it interacts with plasma proteins and macrophages.
Taking the drug can reduce blood pressure, has an anti-sclerotic effect, increases the permeability of the vascular wall, and prevents smooth muscle cells from carrying out proliferative processes. Heparin also has an inhibitory effect on the immune system, enhances diuresis and the development of osteoporosis. This substance was first obtained from the liver, which follows from its name.
If the drug is used to prevent thrombosis, then it is administered subcutaneously. In emergency cases, heparin is administered intravenously. You can also use gels and ointments, which contain Heparin. They have an antithrombotic effect, contribute to a decrease in the inflammatory response. It is applied to the skin with a thin layer, gently rubbing.
Lyoton, Hepatrombin, Heparin ointment – these are the three main drugs that are used for topical treatment of thrombosis and thrombophlebitis.
However, during the use of Heparin-based drugs, it should be borne in mind that the risk of bleeding increases, since the process of thrombosis is inhibited, and the permeability of the vascular wall increases.
Low molecular weight heparins. Drugs that are called low molecular weight heparins are characterized by high bioavailability and sufficient activity against blood clots. They last longer than regular heparins, and the risk of bleeding is lower.
Low molecular weight heparins are rapidly absorbed and stored in the blood for a long time. They interfere with the production of thrombin, but do not make the vascular wall excessively permeable. The use of drugs of this group makes it possible to improve blood flow, increase blood supply to internal organs, and normalize their performance.
The use of low molecular weight heparins is not associated with a high risk of complications, so they displace conventional heparin from modern medical practice. The drugs are injected under the skin into the lateral surface of the abdominal wall.
Representatives of low molecular weight heparins are:
Fragmin. The drug is available in the form of a solution that weakly affects primary hemostasis and platelet adhesion processes. The drug is administered only intravenously, intramuscular use is prohibited. It is prescribed to patients in the early postoperative period, provided that there is a risk of developing bleeding or if there are pronounced platelet dysfunctions.
Klivarin. This is a drug that is a direct anticoagulant. It does not allow blood to clot, thereby preventing the development of thromboembolism.
Clexane. This drug prevents the formation of blood clots, and also helps relieve the inflammatory reaction. It is not combined with other drugs that affect hemostasis.
Fraxiparin. This drug prevents blood from clotting and promotes resorption of blood clots. After its introduction, bruises and nodules form at the injection site. After a few days, they dissolve on their own. If at the initial stage of therapy the patient was given too large a dose, this can provoke the development of bleeding and thrombocytopenia, but in the future these side effects will be eliminated.
Vesel Douay F. This drug has a natural basis, as it is obtained from the intestinal mucosa of animals. It is used to reduce the level of fibrinogen in the blood, for resorption of thrombotic masses. For prophylactic purposes, it is used if there is a risk of blood clots in the veins and arteries.
Preparations related to low molecular weight heparins require strict adherence to the instructions. Their independent appointment and use is unacceptable.
Thrombin Inhibitors. Thrombin inhibitors include the drug Hirudin. It contains a component that is present in leech saliva. The drug begins to act in the blood, directly inhibiting the production of thrombin.
There are also drugs that contain a synthetic protein similar to that which was isolated from leech saliva. These medicines are called Girugen and Girulog. These are new drugs that have several advantages over heparins. They last longer, so scientists today are engaged in the creation of these medicines in tablet form. In practice, Girugen is rarely used, since the drug has a high cost.
Lepirudin is a drug that is used to prevent thrombosis and thromboembolism. It inhibits the production of thrombin, refers to direct anticoagulants. Thanks to the use of Lepirudin, it is possible to reduce the risks of developing myocardial infarction, as well as to refuse surgical intervention for patients with exertional angina.
Indirect anticoagulants include drugs such as:
Phenylin. This drug is well absorbed and distributed in the body, quickly penetrates all histohematological barriers and concentrates in the right place. Phenylin is considered one of the most effective drugs from the group of indirect anticoagulants. Its use allows to improve the rheological properties of blood, normalize its ability to coagulate. The treatment carried out by Fenilin allows you to eliminate convulsions, improve the general well-being of the patient. However, the drug is rarely prescribed, since its administration is associated with a risk of developing many side effects.
Neodicumarin. This drug interferes with the formation of blood clots. The therapeutic effect develops as the drug accumulates in the body. Its use allows to reduce blood coagulability, increase the permeability of the vascular wall. You need to take the drug strictly at a certain time, without violating the dosage regimen.
Warfarin. This is the most commonly used anticoagulant, which prevents the development of coagulation factors in the liver, thereby preventing platelets from clotting. Warfarin has a quick healing effect. When the drug is completed, its side effects will also quickly be stopped.
Anticoagulant drugs inhibit the activity of the blood coagulation system, preventing the formation of new blood clots, or destroying existing ones. This group of drugs has been widely used in all branches of medicine.
Thanks to these drugs, surgical mortality in the postoperative period has significantly decreased.
What it is?
Anticoagulants are substances or drugs that suppress the activity of the blood coagulation system and also prevent blood clots.
Preparations of this series are used in all areas of medicine. However, anticoagulants are most prevalent in cardiology and surgery. In the course of any, even minor surgical interventions, the integrity of body tissues is violated. In this case, the hemostatic system is activated, which is characterized by increased thrombosis.
The lack of correction of this condition can lead to the development of acute disorders of the cerebral and coronary circulation, as well as thromboembolism of the branches of the pulmonary artery.
In cardiological practice, the use of anticoagulants becomes especially important in the post-infarction period, with arrhythmias, as well as heart failure.
Anticoagulants are prescribed for life to patients who have undergone stenting, or coronary artery bypass grafting.
Modern anticoagulants can affect the blood coagulation system, reducing its activity.
This leads to a decrease in blood viscosity and the likelihood of blood clots.
The mechanism of action of anticoagulants depends on the class of drugs to which they belong.
For a better understanding, classifications have been created in which the points of action of specific groups of drugs are indicated.
Classification of anticoagulants begins with the separation of drugs according to the mechanism of action. Allocate drugs that directly affect blood coagulation factors – they are also called direct.
Indirect drugs include drugs that affect the metabolic processes of the liver, reducing the synthesis of vitamin K. The latter is an important factor in the conversion of prothrombin to thrombin (platelet lance of hemostasis).
The main classes are distinguished among direct-acting and indirect-acting anticoagulants:
- Heparins – Antithrombin III, Heparin, Sulodexide, Enoxyparin.
- Antagonists of vitamin K – Warfarin, Acenocumarol, Fenindion.
- Thrombolytics – Streptokinase, Fibrinolysin, Tenecteplase, Alteplase, Urokinase, Protein C, Anchord.
- Direct inhibitors of factor Xa are Darexaban, Rivaroxaba, Apixaban, Betrixaban, Endoxaban.
- Antiplatelet agents – clopidogrel, acetylsalicylic acid, indobufen, ticagrelor, dipyridamod, abciximab, ticlopidine.
- Direct thrombin inhibitors are Bivalirudin, Lepirudin, Dabigatran, Xymelanatran, Desirudin, Melanatran, Argatroban.
- Other antithrombotic agents – Fondaparinux, Defibrotide, dermatan sulfate.
Many patients with a history of atrial fibrillation, ischemia or myocardial infarction, transient ischemic brain attack, prefer to carry with them a tablet anticoagulant that can be drunk quickly.
Those people who have a high risk of developing cardiovascular events, it is better to ask your doctor what these new oral anticoagulants are, and which is better to always have with you. The drug may vary (depending on the patient’s health status). Usually it is Dabigatran, Apiksaban, Eparin.
In turn, direct-acting drugs are divided into the following subcategories:
- heparins, as well as their derivatives;
- low molecular weight heparins;
- sodium hydrogen citrate;
- danaparo >
The list of anticoagulant drugs with an indirect mechanism of action can also be divided into subcategories:
- monocoumarins (obtained from oxmarin);
Contraindications for use
Contraindications for taking anticoagulants:
Hemorrhoids, which is complicated by the release of blood.
Hepatitis and fibrotic change in the liver of a chronic course.
Hepatic and renal failure.
Pericarditis and endocarditis.
An acute shortage in the body of ascorbic acid and vitamin K.
Cavernous pulmonary tuberculosis.
The presence in the body of a malignant tumor.
Aneurysm of the brain.
Myocardial infarction with high blood pressure.
Anticoagulants are not prescribed for pregnant women, nursing mothers, women during menstrual bleeding, and also immediately after childbirth. The use of this group of drugs is not recommended for older people.
The clinical use of anticoagulants is recommended for the following diseases:
- Pulmonary and myocardial infarction;
- Stroke embolic and thrombotic (except hemorrhagic);
- Phlebothrombosis and thrombophlebitis;
- Vascular embolism of various internal organs.
As a prophylaxis, you can use it with:
- Atherosclerosis of the coronary arteries, cerebral vessels and peripheral arteries;
- Heart defects rheumatic mitral;
- Postoperative period to prevent blood clots.
With the development of some diseases in the plasma, powerful immune clotting inhibitors sometimes accumulate, which are specific antibodies, for example, lupus anticoagulant. They indicate a particular factor. These antibodies can be produced to combat any manifestation of blood coagulation, but according to statistics, as a rule, these are factor VII, IX inhibitors.
Anticoagulant preparations: description and list of drugs of direct and indirect action
These are drugs that affect the function of blood coagulation, used to reduce the likelihood of a blood clot in the body. Due to blockage in the vessels or organs, the following can develop:
- ischemic stroke;
- gangrene of limbs;
- vascular inflammation;
- heart ischemia;
Direct and indirect anticoagulants, which help to monitor blood coagulation processes, are distinguished by the mechanism of action. Often they are used to treat varicose veins, the treatment of autoimmune diseases. Anticoagulants have certain pharmacological properties and rules for admission, so they can only be prescribed by a doctor who is familiar with the patient’s medical history.
Direct-acting anticoagulants are absorbed quickly and their duration is not more than a day before re-administration or application.
Indirect anticoagulants accumulate in the blood, creating a cumulative effect.
They can not be canceled immediately, as this can contribute to thrombosis. When taken, they gradually reduce the dosage.
Direct anticoagulants of local action:
- Heparin ointment;
- Lyoton gel;
Anticoagulants for intravenous or intradermal administration:
- Warfarin Nycomed in tab .;
- Phenylin in tab.
Various vascular diseases lead to the formation of blood clots. This leads to very dangerous consequences, since, for example, a heart attack or stroke can form.
To thin the blood, the doctor may prescribe medications that help reduce blood coagulation. They are called anticoagulants and are used to prevent blood clots from forming in the body. They help block the formation of fibrin.
Most often they are used in situations when blood clotting is increased in the body.
It can arise due to problems such as:
- Varicose veins or phlebitis;
- Blood clots of the inferior vena cava;
- Blood clots hemorrhoidal veins;
- Myocardial infarction;
- Artery injury in the presence of atherosclerosis;
- Shock, trauma or sepsis can also lead to blood clots.
Anticoagulants are also used to improve the state of blood coagulation. If you used Aspirin before, now doctors have left this technique, because there are much more effective drugs.
What it is?
To avoid the occurrence of blood clots as dangerous blood clots, in the classification of drugs there is a pharmacological group called anticoagulants – the list of drugs is presented in any medical reference book.
Such medications provide control of blood viscosity, prevent a number of pathological processes, and successfully treat certain diseases of the hematopoiesis system.
In order for the recovery to be final, the first step is to identify and remove the coagulation factors.
These are representatives of a separate pharmacological group, produced in the form of tablets and injections, which are designed to reduce blood viscosity, prevent thrombosis, prevent stroke, in the complex treatment of myocardial infarction.
Such medications not only productively reduce the coagulation of systemic blood flow, but also maintain the elasticity of the vascular walls.
With increased platelet activity, anticoagulants block the formation of fibrin, which is appropriate for the successful treatment of thrombosis.
Anticoagulants are used not only for the successful prevention of thromboembolism, this appointment is suitable for increased thrombin activity and the potential threat of the formation of blood clots in the vascular walls that are dangerous for systemic blood flow. The platelet concentration is gradually reduced, the blood acquires an acceptable flow rate, the disease recedes. The list of drugs approved for use is extensive, and their specialists prescribe for:
- liver disease;
- vein thrombosis;
- vascular disease;
- thrombosis of the inferior vena cava;
- blood clots of hemorrhoidal veins;
- injuries of various etiologies;
- varicose veins.
There are quite a few contraindications to the use of anticoagulants, so be sure to check with your doctor the advisability of taking the funds.
Cannot be used with:
- Peptic ulcer;
- Parenchymal diseases of the liver and kidneys;
- Septic endocarditis;
- Increased vascular permeability;
- With increased pressure with myocardial infarction;
- Oncological diseases;
- Acute aneurysm of the heart;
- Allergic diseases;
- Diathesis hemorrhagic;
With caution during menstruation in women. Not recommended for nursing mothers.
New generation oral anticoagulants
Drugs that can slow down the work of the human blood-clotting system are called anticoagulants.
Their action is due to inhibition of the metabolism of those substances that are responsible for the production of thrombin and other components capable of forming a blood clot in a vessel.
They are used for many diseases, during which the risk of blood clot formation in the venous system of the lower extremities, the vascular system of the heart and lungs increases.
History of discovery
The history of anticoagulants began at the beginning of the twentieth century. In the fifties of the last century, a medicine capable of thinning blood, with the active substance coumarin, has already arrived in the world of medicine.
The first patented anticoagulant was Warfarin (WARFARIN) and it was intended solely for bullying rats, since the drug was considered extremely toxic to humans.
Nevertheless, the increasing unsuccessful suicide attempts by Warfarin forced scientists to change their mind about its danger to humans.
So in 1955, Warfarin began to be prescribed to patients after myocardial infarction. To this day, Warfarin takes 11th place among the most popular anticoagulants of our time.
But pharmaceutical progress does not stand still. The development of the best and effective anticoagulant has been conducted and continues to be conducted, with a minimum number of contraindications and side effects, with no need to control INR and others.
Over the past twenty years, new generation anticoagulant drugs have appeared.
Consider their mechanism of action, and the main differences in comparison with their predecessors.
First of all, in the synthesis of new drugs, scientists are trying to achieve the following improvements:
- universality, that is, the ability to take one drug for different diseases;
- the presence of an oral form;
- increased controllability of hypocoagulation, reduction to a minimum of additional control;
- lack of need for dose adjustment;
- expanding the range of potential patients for whom taking this medicine is necessary, but has been contraindicated;
- the possibility of taking anticoagulant in children.
Some new oral anticoagulants have a completely unique effect on the blood coagulation system.
And also affect other coagulation factors, unlike other drugs.
For example, newly synthesized substances interact with the P2Y12 platelet ADP receptor, inhibit factor FXa, Xa, are IgG class immunoglobulins, and so on.
NOA (new oral anticoagulants) have several advantages over their predecessors. Depending on the drug and its group, there are the following positive innovations:
- reduced likelihood of intracranial and fatal bleeding;
- the frequency of embolism is not higher in predecessors, and sometimes even lower;
- the possibility of relatively safe administration of NOA if warfarin is prohibited;
- rapid onset and termination (about two hours);
- reversible inhibition of free thrombin-linked factor and thrombin itself;
- lack of interaction with edecalcin and GLA protein;
- low impact of food and other drugs;
- short half-life (about 5-16 hours).
However, there are a number of disadvantages of modern anticoagulants, such as:
- The need for regular intake of some NLA. Some old anticoagulants allowed to skip several doses, because they had a long-term effect, which did not entail a sharp change in blood counts.
- Lack of validated tests for emergency discontinuation of anticoagulant therapy or for monitoring adherence to therapy.
- The presence of a large number of tests for each of the new anticoagulants.
- Intolerance of some new drugs in patients who took similar anticoagulants of the older generation without side effects.
- Perhaps an increased risk of gastrointestinal bleeding.
- High price.
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New indirect anticoagulants in one way or another affect the metabolism of vitamin K.
All anticoagulants of this type are divided into two groups: monocoumarins and dicumarins.
At one time, such drugs as Warfarin, Sinkumar, Dikumarin, Neodikumarin and others were developed and released.
The use of such drugs has a large number of contraindications and additional, often uncomfortable, tests and a diet.
Anyone taking indirect anticoagulants should:
- Calculate your daily vitamin K intake
- regularly monitor INR;
- be able to change the level of hypocoagulation in intercurrent diseases;
- monitor the possible sharp appearance of symptoms of internal bleeding, in which immediately consult a doctor and switch to another group of anticoagulants in the near future.
But anticoagulants are not strictly divided into drugs of direct and non-direct action. There are several groups of substances that have the ability to dilute, in one way or another, blood. For example, enzymatic anticoagulants, platelet aggregation inhibitors, and others.
So the new Brilint antiplatelet agent appeared on the market. The active substance is ticagrelor. The representative of the class of cyclopentyltriazolopyrimidines is a reversible P2U receptor antagonist.
The following drugs are referred to new indirect anticoagulants.
New anticoagulant direct thrombin inhibitor. Dabigatran etexilate is a low molecular weight precursor to the active form of dabigatran. The substance inhibits free thrombin, fibrin-binding thrombin and platelet aggregation.
Most often used to prevent venous thromboembolism, in particular, after joint replacement.
In pharmacies you can find a medicine with the active substance dabigatran – Pradax. Available in the form of capsules, containing dabigatran etexilate 150 mg in one capsule.
Highly selective factor Xa inhibitor. Rivaroxaban is able to dose-dependently increase APTT and the result of HepTest. The bioavailability of the drug is about 100%. It does not require monitoring of blood parameters. The variation coefficient of individual variability is 30–40%.
One of the brightest representatives of the drug containing rivaroxaban is Xarelto. Available in tablets of 10 mg of active substance in each.
The drug can be prescribed to patients for whom vitamin K antagonists are contraindicated.
Compared with acetylsalicylic acid, it has a low probability of embolism. Apixaban selectively inhibits coagulation factor FXa. It is mainly prescribed after planned knee or hip arthroplasty.
Available under the name Elikvis. It has an oral form.
The drug belongs to the latest class of fast-acting factor Xa inhibitors. As a result of clinical studies, it was found that Edoxaban has the same opportunity to prevent the formation of blood clots with Warfarin.
And at the same time, it has a significantly lower probability of bleeding.
It should be used with caution in elderly patients, with a significant deviation of weight from normal, with impaired renal function, diseases associated with improper function of the circulatory system.
One of the features of many new anticoagulants is their speed and rapid half-life. This suggests that it is necessary to be extremely careful in observing the regimen of taking the tablets. Since even skipping one tablet can lead to complications.
For bleeding that occurs, as a result of therapy with some anticoagulants, there is a specific treatment.
For example, when bleeding due to Rivaroxaban, the patient is prescribed a prothrombin concentrate or freshly frozen plasma. In case of blood loss due to Dabigatran, hemodialysis is carried out, recombinant FVIIa.
The development of new anticoagulants continues to this day. Problems with side effects such as bleeding are still not resolved.
Even some new drugs require control.
The number of contraindications, although reduced, but not completely eliminated. Some drugs still have slightly increased toxicity.
Therefore, scientists continue to search for a universal remedy with high bioavailability, lack of tolerance, absolute safety and intellectual regulation of the level of prothrombin in the blood, depending on other factors influencing it.
Nevertheless, new drugs, in comparison with drugs of the last century, have very noticeable positive differences, which speaks of the titanic work of scientists.
Blood-thinning drugs that prevent blood clots have become an indispensable tool to prevent ischemia, arrhythmia, heart attack, thrombosis, etc. Many effective drugs have a number of unpleasant side effects, so the developers continue to improve this group of medicines. New oral anticoagulants should become a universal remedy that will be allowed for children to take during pregnancy. Modern drugs have the following positive aspects:
- they are allowed to people to whom warfarin is contraindicated;
- reduced risk of bleeding;
- dilute blood 2 hours after administration, but the action quickly ends;
- the effect of consumed food and other means is reduced;
- inhibition is reversible.
Specialists are constantly working on improving drugs for thinning the blood of a new generation, but they still have a number of negative properties, which include:
- reception of old options could be skipped, new ones require strictly regular use;
- there is a risk of bleeding in the digestive tract;
- for the appointment of funds, it is necessary to conduct many analyzes;
- some patients who did not have problems with old drugs experience intolerance to new anticoagulants.
The price of anticoagulants
The anticoagulant agent has a strong effect, which, without medical supervision, can lead to profuse internal bleeding. Therefore, you can’t buy this tool in the online store. The exception is the electronic representation of pharmacies. Blood thinning and thrombotic drugs have different costs. The drug catalog offers a wide variety of derivatives. Below is a list of popular medicines that can be ordered inexpensively:
- Warfarin, 100 tablets – the price is from 100 rubles;
- Curantil – price from 345 p.;
- Detralex – price from 640 r.;
- Antithrombin, 75 mg capsules – price from 225 r.
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