Indirect anticoagulants are used to prevent and treat thrombosis and thromboembolism in the following conditions:
after surgical interventions on the heart and blood vessels;
TELA – with thromboembolism of the pulmonary artery;
with aneurysm of the left ventricle;
with obliterating thromboangiitis;
with obliterating endarteritis.
Contraindications to the use of drugs of this group are:
other diseases accompanied;
increased vascular permeability;
severe impaired renal and hepatic function;
myocardial infarction, accompanied by high blood pressure;
period of pregnancy;
you should not take these drugs in the period (2 days before the planned start, their medicine is canceled) and in the early postpartum period;
prescribed with caution to patients of advanced and senile age.
Unlike direct-acting anticoagulants, the effect of drugs of this group does not appear immediately, but as the active substance accumulates in organs and tissues, that is, slowly. They act, on the contrary, for a longer time. The speed, strength and degree of cumulation (accumulation) of different drugs in this class varies.
They are used exclusively orally or orally. Intramuscularly, intravenously or subcutaneously, they cannot be used.
Discontinue therapy with indirect anticoagulants should not be done immediately, but gradually – slowly reducing the dose and increasing the time between doses (up to 1 time per day or even every other day). Abrupt drug withdrawal can lead to a sudden compensatory increase in the level of prothrombin in the blood, which will cause thrombosis.
With an overdose of drugs of this group or their prolonged use, they can become a cause, moreover, it will be associated not only with a decrease in blood coagulation, but also with an increase in the permeability of the capillary wall. Less commonly, in this situation, bleeding from the oral cavity and nasopharynx, gastrointestinal bleeding, hemorrhages in the muscles and cavity of the joints develop, and also micro- or macrohematuria appears.
To avoid the development of the complications described above, it is necessary to carefully monitor the patient’s condition and laboratory indicators of blood coagulation during treatment with indirect anticoagulants. Once every 2-3 days, and in some cases more often, prothrombin time should be determined and urine examined for the presence of red blood cells (hematuria, i.e. the presence of blood in the urine, is one of the first signs of an overdose of the drug).
Salicylates (in particular, acetylsalicylic acid) should not be prescribed simultaneously with these medicines, since they help increase the concentration of free anticoagulant in the blood.
There are actually few drugs of the indirect anticoagulant group. These are neodicumarin, acenocoumarol, warfarin and phenindione. Let us consider each of them in more detail.
When taken orally, it is absorbed relatively quickly, the half-life is 2,5 hours, it is excreted in the urine not in its original form, but in the form of metabolic products.
The expected effect of the drug begins to appear 2-3 hours after its administration, reaches a maximum in the period of 12-30 hours and lasts another two days after discontinuation of the drug.
It is used alone or in addition to heparin therapy.
Release form – tablets.
Dose according to the scheme, the maximum daily dose is 0,9 g. The dose is selected depending on the indicators of prothrombin time.
It is well absorbed when taken orally. It has a cumulative effect (that is, it acts when a sufficient amount is collected in the tissues). The maximum effect is observed 24-48 hours after the start of treatment with this drug. After cancellation, its normal level of prothrombin is determined after 48-96 hours.
Take inside. On the first day, the recommended dose is 8-16 mg, in the future, the dosage of the drug depends on the values of prothrombin. As a rule, the maintenance dose is 1-6 mg per day. An increased sensitivity of the patient’s body to this drug is possible. In case of allergic reactions, it must be canceled.
A decrease in blood coagulation ability is noted 8-10 hours after taking the drug, reaches a maximum in about a day. It has a pronounced cumulative effect.
The initial dose in the first 2 days is 0,03-0,05 g three times a day. Further dosages of the drug are selected individually depending on blood parameters: the prothrombin index should not be less than 40-50%. The maximum single dose is 0,05 g, daily – 200 mg.
Against the background of phenylin treatment, it is possible to stain the skin and change the color of urine. If these symptoms occur, replace phenindione with another anticoagulant.
In the gastrointestinal tract is completely absorbed. The half-life is 40 hours. The anticoagulant effect begins 3-5 days after the start of treatment and lasts for 3-5 days after discontinuation of the drug.
It is produced in tablets. Treatment begins with 10 mg once a day, after 1 days the dosage is reduced by 2-1,5 times – up to 2-5 mg per day. The therapy is carried out under the control of an INR blood count (international normalized ratio). In individual clinical situations, for example, in preparation for surgical treatment, the recommended dosages of the drug vary and are determined individually.
Blood clotting drugs are called coagulants. They have their own characteristics in use, have a positive effect on the body, can prevent and stop bleeding. Modern pharmacological companies produce a wide variety of drugs that can cope with the problem optimally quickly.
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:
thrombosis of the inferior vena cava;
blood clots of hemorrhoidal veins;
injuries of various etiologies;
Anticoagulants are used in almost all cases where there is a risk of a blood clot, with cardiological diseases and diseases of the vessels of the extremities.
In cardiology, they are prescribed for:
congestive heart failure;
the presence of mechanical heart valves;
parietal thrombosis of the heart cavities;
large focal myocardial infarction.
In other cases, anticoagulants are intended to prevent thrombosis:
prolonged stay in bed after surgery;
blood loss (over 500 ml);
prevention of reocclusion after angioplasty.
What does it mean by itself and what methods and methods are used you can learn from our article.
If you are prescribed the drug Vazobral, the instructions for use are required to be studied. All that is about the medicine is contraindications, reviews, analogues.
Before you start taking anticoagulants, a number of studies are prescribed to the patient.
He must pass a general blood test, a general urine test, a Nechiporenko urine test, fecal occult blood test, a biochemical blood test, as well as a coagulogram and an ultrasound examination of the kidneys.
Anticoagulants are contraindicated in the following diseases:
peptic ulcer of the gastrointestinal tract;
vitamin K hypovitaminosis;
renal or hepatic insufficiency;
high blood pressure (above 180/100);
In medical practice, antiplatelet agents are used in parallel with other anticoagulants for example with heparin.
To obtain the desired effect, the dosage of the drug, and the drug itself, is chosen so as to level or, on the contrary, enhance the effect of another anticoagulant drug.
The onset of action of antiplatelet agents occurs later than in simple anticoagulants, especially of direct action. After the cancellation of such drugs, they are still not excreted for some time and continue to act.
Titration (gradual selection of doses) of Warfarin for maintenance therapy goes through two stages: the actual selection of the dose and long-term treatment with maintenance doses. Today, all patients, depending on the sensitivity to the drug, are divided into three groups.
Highly sensitive to warfarin. They quickly (in a few days) from the start of taking the drug achieve therapeutic target values of INR. Further attempts to increase the dose lead to high risks of bleeding.
Individuals with normal sensitivity reach the INR target numbers on average after a week from the start of therapy.
Patients with reduced sensitivity to Warfarin, even at high doses for two to three weeks, do not give an adequate INR response.
These features of the bioavailability of Warfarin in different patients may require more careful (frequent) laboratory monitoring of INR during the treatment period, linking patients to laboratories. The patient can maintain relative freedom of movement and life by acquiring a simple Koaguchek apparatus, which works similarly to a glucometer using test strips. True, the price tag for the device itself is about 30000 rubles, and consumables (a set of test strips) will cost six to seven thousand.
Today, a new generation of anticoagulants that successfully replace Warfarin in many situations (cardiology, prophylaxis and treatment of deep vein thrombosis of the extremities, pulmonary embolism, in the treatment and prevention of strokes) allows us to get away from the control problem of INR.
This drug is the most common direct-acting anticoagulant. No less popular are medicines based on it. Heparin does not allow platelets to stick together, increases 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 development, as well as to refuse surgical intervention for patients with exertional angina.
Indirect anticoagulants include drugs such as:
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, to 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 coagulation, 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.
Anticoagulants are prescribed in the following cases:
Mitral valve disease.
Thrombosis in the acute stage.
Thromboangiitis and endarteritis obliterans.
If a person takes anticoagulants without medical supervision, then this carries a risk of developing serious complications, up to hemorrhagic hemorrhages in the brain. If the patient has a predisposition to bleeding, then for his treatment should use antiplatelet drugs, which differ in a gentle effect on the body and do not cause such complications.
What drugs are used for anticoagulant therapy?
Contraindications for taking anticoagulants:
The presence in the body of a malignant tumor.
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.
Among the side effects of taking anticoagulants, the following can be distinguished:
Skin rashes and skin itching.
Disorders in the work of the kidneys.
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.
Antiplatelet agents are drugs that are designed to reduce blood coagulation due to the fact that they do not allow platelets to stick together. They are prescribed together with anticoagulants in order to enhance the therapeutic effect in terms of preventing the formation of blood clots.
Antiplatelet agents allow you to expand the lumen of blood vessels, relieve pain and inflammation.
The most common anticoagulants include:
Aspirin. The drug is available in tablet form, so it can be taken at home. The drug has a vasodilating effect, does not allow platelets to stick together, prevents the formation of blood clots.
Ticlopidine. This drug prevents platelet adhesion, prolongs bleeding time, improves blood circulation in small vessels. It is prescribed for coronary heart disease, myocardial infarction, and cerebrovascular disease. The purpose of the therapy is to prevent the formation of blood clots.
Tirofiban . This drug is often prescribed in a comprehensive treatment regimen in conjunction with Heparin, which helps to more effectively inhibit the formation of blood clots.
Dipyridamole. This drug helps to expand the lumen of the coronary vessels, dilutes blood, improves nutrition of the heart muscle and brain, and helps to lower blood pressure.
Education: In 2013, the Kursk State Medical University was graduated and a diploma in General Medicine was received. After 2 years, residency in the specialty “Oncology” was completed. In 2016, postgraduate studies were held at the N.I. Pirogov National Medical and Surgical Center.
Cardiovascular diseases occupy a leading position among pathologies leading to disability and early mortality among the population. It is for this reason that modern pharmacology pays special attention to drugs aimed at diluting blood and preventing the formation of blood clots in blood vessels and arteries.
Indirect anticoagulants disrupt the production of substances responsible for blood coagulation. Such funds begin to act in a few days, as they have a cumulative effect, and the duration of their action is from 5 days to 15 days.
to prevent the formation of blood clots or to limit their localization during various surgical interventions, in particular, on the heart and blood vessels;
in case of progressive and acute;
with embolism and and peripheral arteries, eyes, pulmonary arteries;
with disseminated intravascular coagulation;
in order to prevent blood coagulation with a number of laboratory examinations;
to maintain reduced blood coagulation during or in cardiopulmonary bypass.
begin to act immediately after use (which is much more effective than taking Warfarin, the effect of which appears only after a week, and for the prevention of venous thrombosis it takes a very long time);
have specific antidotes (which gives a positive effect in the treatment of acute ischemic stroke);
have a fixed dosage, which does not need to be specially selected and constantly adjusted;
food intake does not affect the dosage of the drug;
there is no need for regular blood control.
Gangrene of limbs;
gangrene of limbs;
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Features of the use of “Heparin”
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.
Since these drugs reduce blood coagulation, you can not lower or increase the dosage yourself, as well as reduce the time of administration. Medicines are used according to the schedule prescribed by the doctor.
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.
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:
Anticoagulants for intravenous or intradermal administration:
Warfarin Nycomed in tab .;
Phenylin in tab.
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:
Parenchymal diseases of the liver and kidneys;
Increased vascular permeability;
With increased pressure with myocardial infarction;
Acute aneurysm of the heart;
With caution during menstruation in women. Not recommended for nursing mothers.
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:
Impaired renal function;
Nausea, diarrhea, vomiting;
Itching, abdominal pain;
Before you start taking anticoagulants, you should consult a specialist for contraindications and side effects
Depending on the anticoagulant group, it affects the synthesis of certain substances in the body that are responsible for blood viscosity and its ability to thrombus formation.
There are direct and indirect anticoagulants . Anticoagulants can be in the form of tablets, so in injections and ointments.
Some anticoagulants are able to act not only in vivo, that is, directly in the body, but also in vitro – to show their abilities in a test tube with blood.
Therefore, treatment with heparin does not exclude the possibility of a blood clot. It should also be borne in mind that a thrombus on an atherosclerotic plaque is not sensitive to heparin.
There are also low molecular weight heparins: enoxaparin sodium, deltaparin sodium, nadroparin calcium.
Along with the fact that they have a high antithrombotic effect due to the high bioavailability (99%), such substances are less likely to cause hemorrhoidal complications. This is due to the fact that low molecular weight heparin molecules do not interact with von Willebrand factor.
Scientists tried to recreate synthetic hirudin – a substance that is in the saliva of leeches and has a direct anticoagulant effect that lasts about two hours.
But the attempts were unsuccessful. However, lepirudin, a recombinant derivative of hirudin, was created.
Danaparoid – a mixture of glycosaminoglycans, which also has an anticoagulant effect. The substance is synthesized from the mucous membrane of the intestines of a pig.
Preparations representing oral anticoagulants and direct-acting ointments:
Indirect preparations of this type of anticoagulant are used to reduce blood coagulation During a long time.
One of the subgroups of these drugs has its effect due to a decrease in the liver of K-dependent factors (vitamin K antagonists). This includes factors such as: prothrombin II, VII, X and IX. A decrease in the level of these factors leads to a decrease in the level of thrombin.
Another subgroup of indirect anticoagulants has the ability to reduce the formation of proteins of the anticoagulant system (proteins S and C). The peculiarity of this method is that the effect on protein occurs faster than on K-dependent factors.
And therefore, these drugs are used if necessary urgent anticoagulant effect.
The main representatives of anticoagulants of indirect action:
Ethyl biscum acetate.
Anticoagulants are contraindicated in people suffering from the following diseases:
Peptic ulcer of the duodenum and stomach;
Renal and hepatic insufficiency;
Liver fibrosis and chronic hepatitis;
Vitamin C and K deficiency;
Cavernous pulmonary tuberculosis;
Pericarditis and endocarditis;
Myocardial infarction with hypertension;
Anticoagulants can not be taken during menstruation, pregnancy, lactation, in the early postpartum period, the elderly.
Complications of therapy – bleeding from internal organs:
Hemorrhages in joints and muscles;
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To prevent the development of dangerous consequences, it is necessary to monitor the patient’s condition and monitor blood counts.
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The complex effect of plant components of the drug Detonic on the walls of blood vessels and the autonomic nervous system contribute to a rapid decrease in blood pressure. In addition, this drug prevents the development of atherosclerosis, thanks to the unique components that are involved in the synthesis of lecithin, an amino acid that regulates cholesterol metabolism and prevents the formation of atherosclerotic plaques.
Detonic not addictive and withdrawal syndrome, since all components of the product are natural.
Detailed information about Detonic is located on the manufacturer’s page www.detonicnd.com.
They act directly on thrombin, reducing its activity. These drugs are prothrombin deactivators, thrombin inhibitors and inhibit thrombus formation. In order to prevent internal bleeding, it is necessary to control the parameters of the coagulation system.
Direct anticoagulants quickly enter the body, are absorbed in the digestive tract and reach the liver, have a therapeutic effect and are excreted in the urine.
They are divided into the following groups:
Low molecular weight heparin;
The most common clotting inhibitor is Heparin. This is a direct-acting anticoagulant drug.
It is administered intravenously, intramuscularly and under the skin, and is also used as an ointment as a local remedy.
Antithrombotic drugs of local action have not very high efficiency and low permeability in the tissue. Used to treat hemorrhoids, varicose veins, bruises.
Heparins for subcutaneous and intravenous administration are coagulation-reducing drugs that are individually selected and are not replaced by one another in the treatment process, since they are not equivalent in effect.
The activity of these drugs reaches a maximum after about 3 hours, and the duration of action is hours. These heparins block thrombin, reduce the activity of plasma and tissue factors, prevent the formation of fibrin filaments and prevent platelet adhesion.
For the prevention of thrombosis and thromboembolism, Reviparin and Heparin are prescribed.
This anticoagulant is used in laboratory practice. It is added to tubes to prevent blood clotting. It is used to preserve blood and its components.
They have an effect on the biosynthesis of side enzymes of the coagulation system. They do not inhibit the activity of thrombin, but completely destroy it.
In addition to anticoagulant effects, drugs of this group have a relaxing effect on smooth muscles, stimulate the blood supply to the myocardium, remove urate from the body and have a hypocholesterolemic effect.
“Indirect” anticoagulants are prescribed in the treatment and prevention of thrombosis. They are used exclusively inside. The form of tablets is used for a long time in an outpatient setting. Abrupt withdrawal leads to an increase in prothrombin and thrombosis.
Coumarin is naturally found in plants (sweet clover, bison) in the form of sugars. In the treatment of thrombosis, dicumarin was first used – its derivative isolated from clover in the 20s of the last century.
Derivatives Indan -1,3-Dion
Representative – Fenilin. This oral drug is available in tablets. The action begins 8 hours after administration, and the maximum effectiveness occurs a day later. When taking urine, it is necessary to check the urine for blood, as well as to monitor the prothrombin index.
“Indirect” drugs include:
Warfarin (thrombin inhibitors) cannot be taken with certain liver and kidney diseases, thrombocytopenia, with a tendency to bleeding and acute bleeding, during pregnancy, with DIC, congenital deficiency of S and C proteins, lactase deficiency, if glucose and galactose absorption are impaired.
The main disadvantage of Warfarin is an increased risk of bleeding (nasal, gastrointestinal and others).
Medicines based on coumarin derivatives.
Medicines, derivatives of Indandion.
The latter proved poorly in clinical trials, because the result is unstable, there is a risk of an allergic reaction. Therefore, coumarin-like drugs have become the most optimal option. The most famous coumarin medication is Warfarin. The following indications for its use are distinguished:
prevention of thromboembolism;
mechanical prosthetics of the heart valve;
acute venous thrombosis.
The postoperative period.
Conditions after acute cerebrovascular accident.
branches of the pulmonary artery.
, and .
light bruises on the skin;
the appearance of blood in the urine or feces;
hematomas in the neck;
an overdose of anticoagulants;
hemorrhagic syndrome with hypoprothrombinemia, which is provoked by a deterioration in the process of liver functioning;
long-term treatment with antibiotics, which have an extensive spectrum of action;
long-term therapy with sulfonamides;
prior to major surgical interventions to eliminate the high risk of bleeding.
erosive and ulcerative lesions of the gastrointestinal tract, which are accompanied by a risk of bleeding;
severe renal impairment, including the development of renal failure;
the appearance of C or K-vitamin deficiency;
chronic hepatitis, cirrhosis of the liver, as well as other serious diseases that are accompanied by a violation of biliary function;
detection of blood impurities in the cerebrospinal fluid;
period of pregnancy (this contraindication is due to the risk of postpartum hemorrhage).
Direct action (e.g., heparin). They act quickly, their effect is associated with a direct effect on the blood coagulation system through the formation of complexes with different coagulation factors and inhibition of the three coagulation phases.
Indirect action (vitamin K antagonists). They act for a long time, but after a latent (“silent”) period they stop the activation of the enzyme involved in the conversion of vitamin K, thereby stopping the production of vitamin-dependent plasma coagulation factors (II, VII, IX, X).
Aspirin is the most popular all over the world, however, among allergy sufferers, a reaction to this substance is very common;
Dipyridamole – dilates blood vessels;
Ticlopidine – used for coronary heart disease, heart attack, as well as for the prevention of thrombosis;
Tirofiban – prevents platelet adhesion;
Eptifibatide – has a blocking effect on platelet adhesion.
bleeding of any localization;
increased vascular permeability;
oncological pathology or;
anemia – hypo-and;
acute aneurysm of the heart;
pronounced and renal;
unfractionated heparin preparations (Heparin);
drugs of low molecular weight heparin (Nadroparin, Enoxaparin, Dalteparin and others);
heparinoids (Sulodexide, Pentosan polysulfate);
direct thrombin inhibitors – hirudin preparations.
Overdose with indirect anticoagulants
The mechanism of action of anticoagulants is determined by the destruction of fibrin in the body, which contributes to the formation of blood clots. Due to direct or indirect exposure, they prevent its development.
Pathological processes of the liver.
Urolithiasis of the kidneys, bladder.
Some chronic diseases.
Respiratory failure – tuberculosis, asthma.
Deficiency of ascorbic acid and vitamin K.
Women during pregnancy and lactation.
Pathological blood processes characterized by a violation of homeostasis.
Aneurysms of the cerebral artery and aorta.
Also, anticoagulants should not be used for intoxication, pathologies of the pancreas.
If you do not follow the medical recommendations and instructions for the use of the drug, it can provoke side effects, which are expressed by dizziness, nausea, vomiting, headache. The primary symptoms are more often allergic reactions, fever, bloating, pain in the epigastric region.
In severe cases, impaired renal function, hair loss, diarrhea, necrotic lesions of the skin. Some people may experience itching, rash, and redness.
If these symptoms begin to manifest, you should stop taking the drug and seek help from a medical professional.
According to statistics, various thromboembolic complications (pulmonary embolism, deep vein thrombosis) occupy one of the leading places in the mortality structure of the Russian population. In medicine, for the treatment of such conditions, anticoagulants are used – substances that prevent the formation of thin filaments of fibrin under the influence of coagulation factors, inhibit the growth of an already formed thrombus and increase the activity of internal fibrinolytic (aimed at dissolving the thrombus) enzymes.
Classification of drugs
Currently, the classification of anticoagulants is based on the points of application of their effects in the body. Allocate drugs:
Direct action (e.g., heparin). They act quickly, their effect is associated with a direct effect on the blood coagulation system through the formation of complexes with different coagulation factors and inhibition of the three coagulation phases.
Indirect action (vitamin K antagonists). They act for a long time, but after a latent (“silent”) period they stop the activation of the enzyme involved in the conversion of vitamin K, thereby stopping the production of vitamin-dependent plasma coagulation factors (II, VII, IX, X).
Unfractionated heparin (UFH) is a naturally occurring substance derived from the organs of domestic animals. The mechanism of its action is based on the ability to bind to antithrombin and thereby increase its ability to inactivate coagulation factors IIa, IXa, Xa, XIa, XIIa. Thrombin (factor IIa) is particularly sensitive to the effects of the heparin-antithrombin complex.
The action of heparin is carried out exclusively with parenteral administration: after intravenous administration, the activity manifests itself immediately, with subcutaneous administration – after 20-60 minutes with bioavailability of 10-40% (that is, only this percentage of the substance reaches the systemic circulation). Due to the fact that unfractionated heparin binds to plasma proteins, this drug often exhibits an unpredictable anticoagulant effect. To create and maintain the necessary therapeutic concentration of heparin in the blood, continuous intravenous administration or regular subcutaneous injections, taking into account bioavailability, are necessary. To control treatment, it is necessary to determine the activated partial thromboplastin time (APTT), the indicators of which should remain within 1,5-2,3 of the control value.
Low molecular weight heparins (NMH) – chemically or enzymatically treated unfractionated heparin. The mechanism of action is similar to UFH, but NMH is significantly more active with respect to coagulation factor Xa than thrombin. With intravenous administration, maximum activity appears after 5 minutes, with subcutaneous administration – after 3-4 hours with bioavailability of more than 90%, therefore, to maintain a stable level of anticoagulant plasma activity, it is not necessary to carry out continuous intravenous infusion, unlike UFH. Dosage of the drug is carried out individually under the control of anti-Xa blood activity.
Fondaparinux sodium is a drug that selectively deactivates coagulation factor Xa. The bioavailability of the substance with subcutaneous administration is 100%, and the activity is maintained for 17-21 hours, therefore, to achieve a therapeutic concentration, a single subcutaneous injection is sufficient.
Bivalirudin is a substance that directly inhibits the activity of thrombin, the only drug of similar effect registered in Russia for parenteral administration. Its action is directed not only at the thrombin circulating in the blood, but also at the thrombin inside the formed thrombus. The drug is administered exclusively intravenously, and its activity time is only 25 minutes. The prescribed doses are fixed and do not require monitoring of blood coagulation.
New oral anticoagulants (dabigatran, apixaban, rivaroxaban) are aimed at the selective inhibition of any coagulation factor.
Their effectiveness and safety has been proven by large-scale studies, and laboratory use is not required for use.
Dabigatran etexilate in the body is converted into the active substance dabigatran, acts on thrombin, is excreted by the kidneys in 80% and causes digestive upset in 10% of cases. Apixaban and rivaroxaban initially belong to active drugs that do not need transformation after receipt, act on the Xa coagulation factor. Average oral bioavailability is more than 50%, and fasting rivaroxaban increases it to almost 100%. The drugs do not cause intolerance from the gastrointestinal tract.
Vitamin K antagonists (AVKs) are drugs that block the transition of vitamin K to the active form, which is required for the formation of prothrombin, VII, IX, and X coagulation factors in the liver. The actions of drugs of this group are associated with the removal of functioning prothrombin from blood serum. AVK is used orally in tablets, while their bioavailability is more than 90%. Warfarin is the drug of choice due to the most stable anticoagulant effect. Difficulties in the selection of dosages of drugs are possible: their precise regulation by the international normalized ratio (INR) is required, and the effect of the first dose appears only 5 days after use. An overdose of AVK is treated with vitamin K, an antidote.
Indications, contraindications and side effects
Indications, contraindications and side effects of direct anticoagulants. presented in the table:
1. Initial treatment of acute coronary syndrome (myocardial infarction, unstable form of angina pectoris).
2. Prevention and therapy of deep vein thrombosis and pulmonary embolism.
3. Prevention and treatment of complications in the presence of artificial heart valves, intravascular manipulations, hemodialysis, cardiopulmonary bypass.
4. Prevention of thrombosis of intravascular catheters
2. Thrombocytopenia less than 100 * 10 9/L.
3. An immune form of thrombocytopenia, as a complication of heparin therapy in history.
4. Uncontrolled active bleeding (except associated with DIC).
5. Alleged intracranial bleeding
headache, fever, chills;
increase in AlAT, AsAT;
Low molecular weight heparins
The same as unfractionated heparin
The same as unfractionated heparin, as well as allergy to pork products
increase in AlAT, AsAT;
local reactions with subcutaneous injection
1. Early treatment of acute coronary syndrome (myocardial infarction, unstable angina).
2. Prevention and therapy of deep vein thrombosis and pulmonary thromboembolism.
3. Therapy of thrombosis of the saphenous veins of the lower extremities
2. Hemorrhagic diathesis.
4. Active bleeding.
5. Bacterial endocarditis
Bleeding allergic reactions;
increase in AlAT, AsAT;
local reactions with subcutaneous injection
1. Percutaneous coronary intervention (PCI), including in the complex of primary procedures for acute coronary syndrome with ST segment elevation.
2. Therapy of immune thrombocytopenia as complications of heparin therapy
1. Allergy or hypersensitivity.
2. Hemorrhagic diathesis.
3. Severe renal failure.
4. Severe active bleeding.
5. Subacute bacterial endocarditis.
6. Age to 18 years.
7. Severe arterial hypertension
Bleeding allergic reactions
New oral anticoagulants (dabigatran, apixaban, rivaroxaban)
1. Prevention of deep vein thrombosis and pulmonary thromboembolism with planned hip and knee arthroplasty.
2. Prevention of strokes and thromboembolism with atrial fibrillation
2. Ongoing bleeding.
2. Hemorrhagic diathesis.
4. A history of hemorrhagic stroke.
5. Severe renal and hepatic failure.
6. Pregnancy and lactation.
7. Age to 18 years
increase in AlAT and AsAT;
dyspepsia (in dabigatran etexilate)
Indications for the appointment of vitamin K antagonists are:
prevention and therapy of venous thrombosis and pulmonary thromboembolism;
therapy of thromboembolic events in patients at high risk (in the presence of artificial valves, atrial fibrillation);
prevention of coronary complications in coronary heart disease;
prevention of thrombotic events with antiphospholip >
Clearing or washing the stomach a few hours after taking the drugs does not make any sense.
The patient is given activated carbon for intestinal absorption.
In the case of an overdose of “warfarin” or its analogs inside, “Cholestyramine” is prescribed.
The patient is placed in anti-traumatic conditions to avoid the emergence of new hematomas and hemorrhages.
With significant blood loss, blood transfusions of blood or plasma, sometimes whole blood, are performed. Erythrocyte mass, cryoprecipitate, prothrombin complex are effective in use.
Assigned to “Fitomenadion”, preparations based on vitamin K.
If there is no need to prescribe antiplatelet therapy, the drug Fitomenadion is prescribed a course of treatment, and not as a first aid.
Aspirin is the most common antiplatelet agent. An effective blood thinner, vasodilator and thrombus formation;
Tirofiban – interferes with the adhesion of platelets;
Eptifibatitis – inhibits platelet adhesion;
Dipyridamole is a vasodilator;
Ticlopidine – used for heart attacks, cardiac ischemia and for the prevention of thrombosis.
May be pathological and physiological. Pathological in some diseases appear in the blood. Physiological are normally found in plasma.
Physiological anticoagulants are divided into primary and secondary. The former are independently synthesized by the body and are constantly present in the blood. Secondary appear during the splitting of coagulation factors in the formation and dissolution of fibrin.
Inhibitors of the fibrin self-assembly process.
With a decrease in the level of primary physiological anticoagulants in the blood, there is a risk of thrombosis.
Formed in the process of blood coagulation. They also appear during the breakdown of coagulation factors and the dissolution of fibrin clots.
Secondary anticoagulants – what is it:
Antithrombin I, IX;
Meta-factors Va, XIa.
With the development of a number of diseases in the plasma, strong immune coagulation inhibitors can accumulate, which are specific antibodies, such as lupus anticoagulant.
These antibodies indicate a specific factor, they can be produced to combat the manifestations of blood coagulation, however, according to statistics, these are factor VII, IX inhibitors.
Sometimes, with a number of autoimmune processes in the blood and paraproteinemia, pathological proteins with antithrombin or inhibitory effects can accumulate.
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.
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 >To understand what these anticoagulants are, you can only understand the mechanism of action of these substances. In the human body, there are both coagulation and anticoagulation systems. The former are responsible for the formation of thrombotic masses in violation of the integrity of the vascular structures . The second prevents excessive activity of the blood coagulation system, and is also responsible for the timely splitting of existing blood clots.
Natural anticoagulants are divided into primary and secondary. Primary factors constantly circulate in the vascular bed and prevent the uncontrolled formation of blood clots. They are also divided into several subcategories.
Fibrin creation inhibitors – interfere with the conversion of fibrinogen to fibrin.
Antithromboplastic substances have an antiprotrobinase effect.
Antithrombin – structures that bind thrombin.
Primary blood anticoagulant drugs are:
placental anticoagulant – is produced only with a formed placenta;
autoantibodies produced by active coagulation factors;
fibrin assembly inhibitor;
Secondary factors are formed during the destruction of blood clots:
fibrin pept >Despite the variety of natural blood factors, the balance between coagulation and anticoagulation systems is not always achieved. Inadequate activity of natural anticoagulants and excessive activity of the blood coagulation system can lead to increased thrombosis . In this case, there is a need for the use of anticoagulant drugs.
They can be physiological and pathological. Physiological anticoagulants are normally present in plasma. Pathological appear in the blood with some diseases.
Physiological anticoagulants are divided into primary and secondary. Primary are synthesized by the body independently and are constantly in the blood. Secondary are formed during the cleavage of coagulation factors during the formation of fibrin and its dissolution.
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:
Heparin-based drugs of direct action
Adherents of treatment with alternative methods are used to prevent grass thrombosis with a blood-thinning effect. The list of such plants is quite long:
chicory and others.
Before being treated with herbs, it is advisable to consult a doctor: not all plants can be useful.
Red clover is used in folk medicine as a means of improving blood flow
Blood coagulation is a combination of physiological and biochemical processes aimed at stopping bleeding that has begun earlier. This is a protective reaction of the body, preventing massive blood loss.
Blood coagulation proceeds in 2 stages:
Three structures take part in this complex physiological process: the vascular wall, central nervous system, and platelets. When the vessel wall is damaged and bleeding begins, the smooth muscles located in it around the perforation site are compressed, and the vessels are spasmodic. The nature of this event is reflexive, that is, it occurs involuntarily, after the corresponding signal of the nervous system.
The next step is the adhesion (adhesion) of platelets to the site of damage to the vascular wall and their aggregation (gluing) together. After 2-3 minutes, the bleeding stops, since the site of damage is clogged by a blood clot. However, this blood clot is still loose, and the blood plasma at the site of damage is still liquid, so under certain conditions, bleeding can develop with renewed vigor.
When traces of thrombin appear in the area of damage to the vessel wall, a cascade of reactions of interaction of tissue coagulation factors with blood starts, another factor appears – thromboplastin, which interacts with a specific substance prothrombin to form active thrombin. This reaction also occurs with the participation of calcium salts. Thrombin interacts with fibrinogen and fibrin is formed, which is an insoluble substance – its filaments precipitate.
The next stage is the compression, or retraction, of a blood clot, which is achieved by compaction, compression of it, as a result of which transparent, liquid blood serum is separated. And the last stage is the dissolution or lysis of a previously formed thrombus. During this process, many substances interact with each other, and the result is the appearance in the blood of the enzyme fibrinolysin, which destroys the filaments of fibrin and turns it into fibrinogen.
For a better understanding, classifications have been created in which the points of action of specific groups of drugs are indicated.
The choice of group and drug depends on the health status of a particular patient, his pathology and the state of the blood coagulation system . For this, there is a coagulogram that displays the functional activity of the blood system before, during and after the use of drugs.
After surgery, non-fractional heparin is reintroduced after 4 hours. Acceptance of indirect antiplatelet agents can be returned after two days, after monitoring the state of the blood with the help of laboratory tests.
ulcerative diseases of the gastrointestinal tract;
I term and last month of pregnancy;
high creatinine level.
fast onset of action;
relatively short half-life;
the presence of specific antidote agents (may be useful in the treatment of acute ischemic strokes, as well as to eliminate post-stroke negative symptoms);
lack of direct effect of dietary supplements on the daily dose of the drug;
lack of need for regular laboratory monitoring of blood.
The most common side effect that occurs after taking PAP is an increased risk of bleeding. But the perceived threat of severe bleeding is relatively small compared to the benefits that direct anticoagulants provide.
Additional effective direct anticoagulant mechanisms include platelet deactivation and a decrease in blood coagulation activity. The half-life of this group of drugs is 7-14 hours, the time of occurrence of the therapeutic effect ranges from one to four hours. Direct anticoagulants accumulate in the liver with the formation of active metabolites and are excreted in the urine.
Two types of heparins are also used as anticoagulants – non-fractional (UFH) and low molecular weight (NMH). Low-fraction heparin has been used to prevent and treat mild thrombosis for several decades. The disadvantages of UFH are that it has a variable anticoagulant effect, as well as limited bioavailability. Low molecular weight heparin is obtained from low molecular weight by depolymerization.
Low molecular weight heparin has a specific molecular weight distribution, which determines its anticoagulant activity and duration of action. The advantage of LMWH is that you can easily calculate the required dosage, as well as not be afraid of severe side effects. For these reasons, it is the low molecular weight subspecies of heparin that is used in most hospitals in the world.
As an anticoagulant, a heparin solution is used.
Consistency and regularity is essential for effective treatment with direct anticoagulants. Since this type of drug has a short half-life, patients who miss a dose intentionally or accidentally are at risk of thrombosis or inadequate coagulation. Given that the positive effect of taking PAP quickly disappears when the drug is discontinued, it is extremely important to follow the schedule prescribed by the doctor.
Treatment with a combination of different anticoagulants is contraindicated in:
diseases accompanied by a decrease in blood coagulability;
impaired liver and kidney function;
It is also necessary to urgently interrupt combination therapy when blood appears in the urine.
On the basis of heparin, local anticoagulants were created, drugs reduce the ability to form blood clots, increase capillary strength, eliminate pain, swelling, and nourish tissues.
Venolife – the composition of the gel and ointment includes components that contribute to the absorption of heparin, increased blood flow, and decreased vascular permeability.
Venitan – ointment, cream and gel are composed of heparin and escin. After applying Venitana, blood flow improves, the venous mesh becomes less noticeable, the risk of trophic ulcers, thrombophlebitis decreases.
Hepatrombin – ointment and gel inhibit the formation of blood clots, provide anti-inflammatory and moderate analgesic effect.
Venosan – a multicomponent gel prevents the penetration of exudate into the tissue, the process of adhesion and attachment of platelets to the vascular wall.
Lyoton 1000 gel – additionally contains a component of plant origin escin, which improves the tone of blood vessels and muscles, reduces inflammation and pain.
Reception of anticoagulants intravenously and subcutaneously is prescribed for inflammation of the vascular wall, thrombophlebitis, blood clots in the veins and arteries, for the prevention of thromboembolic complications in old age.
Fragmin – a drug based on low molecular weight heparin, inhibits thrombin activity, slightly affects blood flow. Therapy lasts until normal prothrombin levels are reached.
Fraxiparin – recommended for use in thrombosis of superficial and deep veins. In addition to the main effect, the drug reduces the amount of cholesterol and improves blood circulation. Fraxiparin, which is a direct anticoagulant, is prescribed to pregnant women with high blood coagulability to prevent violations in the placental blood flow, the risk of abortion.
Clexane is a long-acting agent with high anticoagulant activity for the treatment of varicose veins, thrombophlebitis, thrombosis. The drug has virtually no effect on the initial stage of the formation of a blood clot.
Calcium nadroparin – is intended for the treatment of venous thrombosis.
Direct thrombin inhibitors are commonly used to prevent venous thromboembolism, stroke, and venous thrombosis of the lower extremities. New anticoagulants based on dabigatran etexilate are now being used.
Pradaxa – can be used for life-long therapy. The active component of the drug affects thrombin and platelet aggregation. The use of the drug in acute venous thrombosis helps to reduce the risk of relapse and death.
Piyavit – a biologically active supplement based on hirudin slows down hemocoagulation, interferes with the connection of platelets, dissolves blood clots, has moderate analgesic and anti-inflammatory properties. The dietary supplement is effective for varicose veins, thrombophlebitis, trophic ulcers. Piyavit is available in the form of capsules, ointments, spray.
Indirect anticoagulants can be used from several weeks to several months. To prevent bleeding, a blood condition is evaluated every four weeks of treatment. The action of the drug in tablets develops slowly, but the tablet form is convenient to use at home.
Phenylin – disrupts the formation of fibrinogen, prothrombin, coagulation inhibitors in the liver, the concentration of which decreases after eight hours of administration. The drug is indicated for the treatment and prevention of thrombophlebitis, thrombosis in the postoperative period.
Warfarin – refers to safe medicines for long-term anticoagulant therapy under constant monitoring. Undesirable effects in the form of small hematomas, bleeding gums, nausea, decreased performance, allergic rashes rarely occur.
After a dose reduction or withdrawal, they quickly disappear. The use of the drug helps to reduce the number of thromboembolic disorders, heart attack, stroke.
The action after the first dose lasts 2-3 days. During the treatment period, foods with a high content of vitamin K should not be used: cabbage, parsley, kiwi, olive oil, peas, soy. Indications for use:
Prevention of complications after myocardial infarction.
On the first day of treatment of acute thrombosis, Warfarin can be used in combination with heparins.
Anticoagulants inhibit the formation of fibrin thrombi. They are classified for direct and indirect anticoagulants actions.
Direct-acting anticoagulants inactivate circulating in the blood coagulation factors effective in study in vitro and in v » lvo , used for blood preservation, treatment and prevention of thromboembolic diseases and complications.
Indirect anticoagulants (oral) are antagonists vitamin k and violate addictive this vitamin activation factors coagulation in the liver, only effective ” in live , apply with therapeutic purpose.
DIRECT ACTION ANTICAGULANTS (THROMBINE INHIBITORS)
Direct-acting anticoagulants reduce thrombin enzymatic activity (coagulation factor IIa) in blood. Distinguish two groups anticoagulants depending on thrombin inhibition mechanism. The first group is selective, specific inhibitors independent from antithrombin III (β-hirudin oligopeptides, argatroban). They neutralize thrombin, blocking its active center. Another the group is heparin -activator antithrombin 111.
HIRUDIN -polypeptide (65-66 amino acids) leech saliva (Hirudo doctors — nalis ) with a molecular weight of about 7kDa. Currently hirudin obtained by genetic engineering. Hirudin selectively and reversibly inhibits thrombin, forming with its the active center is a stable complex, does not affect other coagulation factors blood.
Next Generation Oral Anticoagulants (PLA)
Anticoagulants are irreplaceable drugs used in the treatment of many pathologies, such as thrombosis, arrhythmias, heart attacks, ischemia and others.
However, drugs that have proven effective have many side effects. . Development continues, and new anticoagulants sometimes appear on the market.
New generation blood thinners have the following benefits:
The action of the drug quickly occurs and stops;
When taken, the risk of bleeding is reduced;
Drugs are indicated for patients who should not take Warfarin;
Inhibition of thrombin-linked factor and thrombin is reversible;
The effect of consumed food, as well as other drugs, is reduced.
However, new drugs have disadvantages:
It is necessary to take it regularly, while taking old drugs can be skipped because of the long action;
A lot of tests;
Intolerance by some patients who could take old pills without side effects;
Risk of bleeding in the gastrointestinal tract.
The list of new generation drugs is small.
The new drugs Rivaroxaban, Apixaban and Dabigatran may be an alternative in case of atrial fibrillation. Their advantage is the lack of the need to constantly donate blood during administration, they do not interact with other drugs.
However, PLA are equally effective at no higher risk of bleeding.
New anticoagulants for oral administration are: Rivoraxoban and Elivix. When using them, you do not need to adhere to a diet and control blood coagulation indicators.
Rivoraxoban – slows the stop of the process of thrombosis by suppressing the prothrombin activator. Rivoraxoban is completely absorbed, begins to act two hours after administration.
Elivix is a direct-acting drug that inhibits the activity of thrombin and other coagulation factors.
New oral anticoagulants are prescribed for acute thrombotic occlusion to prevent thromboembolism after surgery.
Medicines reduce the likelihood of bleeding, are toxic to the liver, and in rare cases cause dyspepsia. The drugs are officially registered in Russia.
To prevent the formation of pathological blood clots, to avoid thromboembolic syndrome, experts prescribe anticoagulants after diagnosing vascular pathology. When choosing a drug, the pharmacokinetic properties and severity of the disease are taken into account.
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.
Anticoagulants are irreplaceable medicines in the treatment of pathologies of the heart and blood vessels. They can not be taken on their own.
During treatment, regular laboratory monitoring is needed.
It is very important not to confuse anticoagulants and antiplatelet agents with thrombolytic agents. The difference is that anticoagulants do not destroy a blood clot, but only slow down or prevent its development.
These are antithrombotic drugs and substances that prevent the formation of blockages in the bloodstream. They provide blood with an optimal fluid state, fluidity, provided that the integrity of the vessels. These substances are divided into several groups according to the formation factor: inside the body or synthetic medicines.
The use of antiplatelet drugs allows not only to normalize the rheological standards of blood, but also to improve the general condition of the patient and prevent the possibility of the development of serious diseases.
Careful attention to the use of anticoagulants, the choice of dosage and monitoring of the patient’s condition will help reduce the risk of complications and achieve success. Professionals who use this group of drugs in their practice need to improve their knowledge and strictly follow international medical recommendations.
Anticoagulants are indispensable drugs for the treatment of cardiovascular pathologies. You cannot take them yourself. They have many contraindications and side effects, and uncontrolled intake of these drugs can lead to bleeding, including hidden bleeding. Prescribe them and determine the dosage should be a doctor who is able to take into account all the features of the course of the disease and possible risks. During treatment, regular laboratory monitoring is needed.
It is important not to confuse anticoagulants and antiplatelet agents with thrombolytic agents. The main difference is that the former cannot destroy a blood clot, but only prevent or slow its development. Thrombolytics are drugs for intravascular administration that dissolve blood clots.
In one case, it is indicated that chicory along with greens should be removed from the diet, and chicory is named in the list of natural remedies (coagulants). So how to understand, can it be taken in parallel with warfarin or not?
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.
Anticoagulants are substances or drugs that inhibit 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.
That is why it is extremely important to conduct adequate anticoagulant therapy in the postoperative period. .
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.
There are clear indications and contraindications for the appointment of antithrombotic drugs. They should be taken only as prescribed by the attending physician under the strict supervision of the coagulogram.
Despite the existing contraindications and possible side effects, you should not be afraid of taking these drugs. Their use can prevent the development of serious complications and even save a person’s life.
Almost all patients suffering from heart disease should take special blood thinning medications. All these drugs can be divided into 2 main types: direct-acting anticoagulants and vitamin K antagonists (indirect effect). How to understand what is the difference between these subspecies and what is the mechanism of their effect on the body?
The balance between hemocoagulation and anticoagulation systems is a prerequisite for the normal functioning of the body. The balance is disturbed by various diseases, functional disorders of the liver, genetic pathologies, atherosclerosis.
With increased coagulation activity, blood viscosity increases and its movement in the vessels slows down. As a result, inflammatory processes in the vascular wall, varicose veins, thromboembolism, and heart attack develop. Thick blood disturbs cerebral circulation, complicates pregnancy, and can cause fetal death.
Direct and indirect anticoagulants are intended to inhibit coagulation. The drugs support optimal blood flow, block the formation of thrombotic masses on the vascular walls.
In addition, anticoagulant drugs reduce the fragility of the capillary network and cholesterol, dilate blood vessels.
Blood clotting agents are also called hemostatics. Their action is direct and indirect, the activity in the body also varies. Certain drugs manifest it exclusively within the body. Medicines differ in the specificity of their effects.
The inclusion of the biological components of the blood coagulation system is inherent in the group of direct coagulants. In this series are drugs that are intended exclusively for local use. Some drugs are injected into the blood only. There are direct contraindications to therapy.
high blood clots in humans;
increased blood clotting history.
A group of drugs based on vitamin K is made up of coagulants with indirect action. Some drugs with hormonal properties are also included in it. Reception of such drugs is carried out inside. It can be tablets or injections.
Any remedies that affect the blood system are prescribed by the doctor. Medicines are used only under his control, so you can not self-medicate.
How to increase blood coagulation? Fibrinogen is often prescribed to patients. It is sold in vials that contain a porous mass. A medication is prescribed to carry out systemic effects on the body. It can be obtained from the blood plasma of a donor. After administration, the active component of the agent can turn into fibrin, which forms blood clots.
The medicine Fibrinogen is used for prompt exposure to the body and emergency treatment. The maximum degree of effectiveness is visible with a lack of substance in the body, if massive bleeding is observed. We are talking about placental abruption, with afibrinogenemia.
To increase blood coagulation, the drug is mainly prescribed in a vein. Local use as a film, which is applied to a bleeding surface area, is not ruled out. Before use, the composition is dissolved in 250-500 ml of water to perform an injection. Patients are shown drip or jet intravenous administration at a slow pace.
Some products also have anticoagulant activity.
Large volumes of liquid – water, compote, tea.
Flaxseed oil and low-fat fish.
Cranberry drinks from other dark berries.
Iodine-containing products – seaweed.
Unfortunately, the use of these products does not fully support the hemostatic system at an appropriate level.
However, such properties must be remembered by people who take anticoagulant drugs – an excess of their use can cause internal and external bleeding .
If necessary, a medicine that can be purchased at pharmacy points in the form of tablets or as a solution in ampoules allows you to increase blood coagulation. The drug is an indirect coagulant. This is an analogue of vitamin K, which has a synthetic origin. It is water soluble. With its help, it is possible to improve the process associated with the formation of fibrin thrombi. In medicine, the drug is designated as vitamin K3.
It is possible to obtain a pharmacological effect thanks not to Vikasol himself, but to vitamins that are synthesized from it. These are compounds K1, K2. For this reason, the result is noticeable after 12-24 hours. If the drug is administered intravenously, the effect is observed after half an hour. Intramuscular use allows you to see a positive effect after 2-3 hours. The need for these vitamins is noted in the synthesis of prothrombin, proconvertin and other factors of the liver.
The medication is prescribed with an excessive reduction of the prothrombin index or with pronounced K-vitamin deficiency. The elimination of the last deviation is carried out when it is provoked by a replacement blood transfusion or bleeding from parenchymal organs. Other reasons:
prolonged use of vitamin K antagonists;
conducting long-term therapy involving antibacterial drugs with a wide spectrum of action;
the use of sulfonamides;
prevention of hemorrhagic disease in infants;
prolonged diarrhea in childhood;
pregnancy in a woman who suffers from epilepsy, tuberculosis and receives symptomatic therapy;
an overdose of anticoagulants with indirect action;
hepatitis, jaundice, wounds, bleeding;
preparation for surgery, postoperative period.
The effectiveness of therapy with the drug Vikasol is sometimes weakened if the antagonists of the drug are simultaneously prescribed to the patient. These are NSAIDs, indirect anticoagulants included in the neodicumarin group, PASK, aspirin. Treatment with the drug is carried out in strict accordance with the doctor’s instructions, as well as the instructions. Vikasol can provoke the development of side effects. For example, hemolysis of red blood cells, when the drug is administered intravenously.
The essence of anticoagulant treatment
Anticoagulant therapy is an effective method of combating varicose veins, deep vein thrombosis, pulmonary embolism, heart attacks and strokes. The active substances of anticoagulants perfectly thin the blood and prevent its coagulation, due to which a therapeutic and preventive effect is achieved.
How to determine the effectiveness of taking anticoagulants?
INR (International Normalized Ratio) is an indicator of blood coagulability, which is examined before prescribing warfarin and as a control of the effectiveness of therapy, as well as to adjust dosages and assess the risks of treatment complications. This is a derivative of prothrombin time (for which blood coagulates), as well as IPT (prothrombin index), which normally is 95-105%.
INR is the ratio of the patient’s prothrombin time to standard prothrombin time. The more INR, the worse the blood coagulation.
The norm of INR is 0,85-1,25. During warfarin therapy, INR 2-3 should be achieved.
INR is checked before taking warfarin, then for 2-5 days. On average, it takes up to 2 days to select the dose of the drug and stabilize the INR within the target numbers (3-10). Further control is carried out once every 2-4 weeks.
If the INR is less than 2 – the dose of warfarin is insufficient, it is increased by 2,5 mg (1 tablet per week) by monitoring the INR every week until it reaches 2-3.
If the INR is more than 3, then the dose of the drug is reduced (1 tablet 2, 5 mg per week). INR monitoring is carried out one week after a dose reduction.
If INR 3,51-4, 5 reduce the dose by 1 tablet. INR is monitored after 3 days.
If INR 4,51-6 reduce the dose by 1 tablet with INR control every other day.
With an INR greater than 6, warfarin is canceled.
In general, anticoagulants are drugs with many pitfalls. The main ones are the risks of spontaneous bleeding (including hidden) and brain accidents that can lead to death. In this regard, anticoagulant drugs should be taken only as directed and under the supervision of a doctor, taking into account all the circumstances of the disease, the risks of this patient and laboratory monitoring data, which should be thorough and regular.
Drugs from the group of anticoagulants are prescribed for the prevention and treatment of thrombosis provoked by the following pathological conditions:
development of aneurysm of the left ventricle;
heart or vascular surgery;
thrombophlebitis of superficial veins on the legs;
Often, blood clots appear in the deep veins on the legs, causing redness and swelling of the lower extremities. However, this is not the biggest nuisance associated with the formation of a blood clot. It is much more dangerous when a separated blood clot with a blood stream enters the lungs. In this case, pulmonary embolism develops.
Another indication for the use of anticoagulants is to prevent the development of thrombosis in the vessels of the heart. This is especially true for people suffering from cardiac arrhythmias, i.e. atrial fibrillation. Finally, a detached fragment of a blood clot can enter the brain vessels, causing the development of a stroke. Correctly selected blood thinners also save from such severe consequences.
A key disadvantage of this therapy is that it increases the risk of bleeding. Moreover, bleeding can develop not only on the skin (where they can be noticed in a timely manner), but also in the gastrointestinal tract or in the brain (which jeopardizes the patient’s life). Particularly at risk are patients who take anticoagulants in high doses or take drugs that increase the effect of anticoagulants in parallel.
In this regard, patients prone to bleeding, suffering from uncontrolled hypertension or having reached the age of 75 years cannot take anticoagulants due to the high probability of bleeding.
Another disadvantage of this group of drugs is their cost. The cheapest means are warfarin-based medicines. However, their administration requires regular laboratory tests to evaluate the effect of the drug on the blood. And heparin-based products are usually used only in a hospital setting.
Finally, specific side effects of certain anticoagulants can also be attributed to disadvantages. For example, heparin-based agents provoke thrombocytopenia, and medicines with warfarin cause skin problems, up to tissue necrosis. In addition, any anticoagulant can provoke a severe allergic reaction or even anaphylactic shock in patients prone to them.
a patient not taking indirect anticoagulants has an INR of less than 1,0;
in a patient taking Warfarin and its analogues, the INR indicator fluctuates at a level of 2,0-3,0 (these indicators are a warning about the possible development of bleeding);
an INR indicator in the range of 1,0–2,0 indicates that the patient is at risk of ischemic stroke;
in the case of INR greater than 4,0, the risk of blood clotting, and hence the development of hemorrhagic stroke, is highest.
But the effectiveness of taking direct anticoagulants is impossible to evaluate and this becomes a serious problem for doctors who prescribe such drugs. For example, the need to evaluate anticoagulant action occurs when patients are admitted in an unconscious state. And if there is no information on taking direct anticoagulants in the medical record of such a patient, it is quite difficult to identify them in the body. The introduction of anticoagulants in this case can easily provoke an overdose.
Direct and indirect anticoagulants are used to prevent the development of thromboembolism, acute venous thrombosis in the case of mechanical prosthetic heart valves and the development of atrial fibrillation.
The main diseases, the development of which is assigned to anticoagulants of direct and indirect action, have the following division into groups:
Arterial system thrombosis:
stroke with manifestations of ischemia;
traumatic damage to the arteries against atherosclerosis.
development of sepsis.
Acute vein thrombosis:
thrombosis on the background of varicose veins;
thrombosis of hemorrhoidal venous plexuses;
clotting in the inferior vena cava.
What are anticoagulants, and what is the list of indications? This is a drug with the opposite effect of thrombosis. It is mainly used for diseases of the cardiovascular system:
Coronary heart disease.
Impaired blood vessel function.
Chronic pathology of the heart and blood vessels.
The presence of artificial valves.
In addition to treatment, drugs are prescribed for preventive purposes of the above diseases, in the postoperative period to prevent blood clots. They are applied individually, under the supervision of a physician.
Warfarin is a true old-timer in the pharmaceutical market
Until the end of 2010, the vitamin K antagonist (warfarin) was the only oral anticoagulant approved by the world health organization for the prevention of thromboembolic complications in patients with non-valve atrial fibrillation and the treatment of venous thromboembolism. For half a century, pharmacists have studied in detail the effectiveness of the drug, and also clearly identified the shortcomings and side effects.
The most common include:
narrow therapeutic window (for poisoning, it is enough to drink a minimum number of tablets);
interaction with foods rich in vitamin K (taking tablets in combination with daily consumption of green vegetables can lead to hyperkalemia);
delayed anticoagulant effect (this means that several weeks must elapse between the initiation of therapy and the first results). For the prevention of venous thrombosis, this period is too long;
the need for frequent monitoring of blood status and dose adjustment;
the possibility of bruising and bleeding.
A person who does not take indirect anticoagulants will have an INR slightly below 1.
A patient taking warfarin will have an INR between 2,0 and 3,0. Having seen such high rates, doctors will be ready for sudden bleeding to occur.
An INR between 1 and 2 indicates that the patient may be at risk of developing ischemic stroke.
With INR 4 and above, there is the greatest risk of blood clotting and the development of hemorrhagic stroke.
An INR blood test is indicative of indirect anticoagulant therapy
But a blood test for INR will not give objective indicators if the patient takes direct anticoagulants. The biggest problem with the latest direct anticoagulants is the lack of a reliable way to evaluate their effectiveness. Doctors can find out the time to stop the bleeding, but there is no indicator that would evaluate the presence of anticoagulant effects.
What you need to know
Patients who are prescribed oral anticoagulants should know that they have a large number of contraindications and side effects. When taking these medicines, you need to follow a diet and take additional blood tests. It is important to calculate the daily dose of vitamin K, since anticoagulants disrupt its metabolism;
Can two types of anticoagulants be combined?
As can be understood from the above, anticoagulants are a real salvation of a person in case of angina pectoris, heart attacks, vascular embolism, with varicose veins or thrombophlebitis. Moreover, in the case of an acute condition, direct-acting drugs are prescribed, which give an immediate effect. If therapy yields a positive result, after a few days the treatment is supplemented with indirect drugs.
In addition, combinations of these drugs are prescribed for patients to prepare for blood transfusion, for operations on vessels and the heart, as well as to prevent thrombosis. True, specialists should constantly monitor the patient’s condition, in particular, check the rate of blood coagulation, the presence of sediment in the urine, as well as the level of prothrombin.
Anticoagulants generally inhibit the appearance of fibrin strands; they prevent thrombosis, help to stop the growth of blood clots that have already arisen, and increase the effect on endogenous fibrinolytic enzymes on blood clots.
Anticoagulants are divided into 2 groups: a) direct anticoagulants – fast acting (sodium heparin, calcium nadroparin, enoxaparin sodium, etc.), effective in vitro and in vivo ; b) indirect antacoagulants (vitamin K antagonists) – long-acting (warfarin, phenindione, acenocoumarol, etc.), act only in vivo and after a latent period.
The anticoagulant effect of heparin is associated with a direct effect on the blood coagulation system due to the formation of complexes with many hemocoagulation factors and is manifested in the inhibition of the coagulation phases I, II and III. Heparin itself is activated only in the presence of antithrombin III.
Indirect anticoagulants – derivatives of oxycoumarin, indandion, competitively inhibit vitamin K reductase, which inhibits the activation of the latter in the body and stops the synthesis of K-vitamin-dependent plasma hemostasis factors – II, VII, IX, X.
Overdose with indirect anticoagulants
Doctors are concerned that so far no antidote has been developed that can quickly and effectively normalize the condition of a patient who has an overdose from taking anticoagulants. If bleeding occurs, doctors administer a prothrombin complex concentrate, freshly frozen plasma, and Fitonadion (a form of vitamin K) to the patient. Take care!
There is a normalization of the internal balance of the body. The blood flow through the vessels has no obstacles and restrictions, and thrombosis is at the right level. When the balance of the functioning of systems is disturbed in favor of enhancing blood coagulation, conditions appear that can lead to excessive clot formation. Indirect anticoagulants are one of the groups of drugs used to restore internal disorders.
Despite all of the above advantages, doctors are still concerned about the lack of specific antidotes for use in case an overdose occurs. To prevent such a serious condition, doctors adhere to the following rules:
reduce the dose of epobaxan after 7 days of use;
xalerto requires a dose reduction after a course of 21 days.
At the moment, when life-threatening bleeding occurs, including those caused by indirect anticoagulants, freshly frozen plasma, a prothrombin complex concentrate, and Fitonadion are administered to the patient.
Phytonadione is one of the few antidotes to anticoagulants
The pharmacology and mechanism of action of each antidote are different. Different anticoagulants will require different doses and strategies for administering antidotes. The duration of the course and dosage of antidotes is calculated depending on how the patient responds to the drugs already administered (there are cases when some antidotes not only stop bleeding, but also activate platelet aggregation).
Anticoagulants – this is one of the groups of drugs that affect the blood coagulation system, preventing the formation of blood clots in blood vessels. Depending on the mechanism of action, these drugs are usually divided into 2 subgroups: direct and indirect anticoagulants. Below we will talk about the first group of anticoagulants – direct action.
What are anticoagulants? This is a specific group of drugs that has an anticoagulant effect. The drug is able to prevent the formation of blood clots, is aimed at normalizing blood flow and maintaining blood function. Depending on the therapeutic effect, it is divided into types and classifications. It is used under the supervision of a medical professional.
A variety of anticoagulants
According to the therapeutic effect, anticoagulants are divided into several types:
Natural – they include pathological and physiological agents. The former arise in the blood of a person with the development of the disease, the latter are part of the plasma and are divided into primary and secondary. Primary independently, in a certain amount produced by the body, secondary to the destruction of fibrin.
Primary natural anticoagulants: what is it and the names belonging to this group are distributed more often according to classifications. They are usually divided into antithromboplastins, antitrobins and fibrin self-reproduction inhibitors.
If a lack of primary anticoagulants appears in the body, the chance of blood clots and the development of vascular diseases increases significantly.
Popular representatives of this group of drugs are Heparin, Protein C, Lipid and Contact inhibitors, Protein S and others.
Heparin is produced in the body by mast cells, mainly its accumulation is in the liver and lungs. High amounts help prevent clotting, blood clots.
Protein C is formed by parenchymal cells of the liver, is found in the blood in a weak form. Thanks to thrombin, it becomes active.
Protein S is produced by the liver, endothelium. Its amount directly depends on the content of vitamin K.
Secondary physiological – are synthesized in the process of blood coagulation and destruction of fibrin. Effective representatives are Antithrombin 1 and 9, Febrinopept >
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.
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.
The name of the anticoagulant is from the list of drugs
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Anticoagulants are drugs that prevent the formation of blood clots in blood vessels. This group includes 2 subgroups of drugs: anticoagulants of direct and indirect action. We already talked about earlier. In the same article, we briefly described the principle of the normal functioning of the blood coagulation system.
In order to better understand the mechanisms of action of anticoagulants of indirect action, we strongly recommend that the reader familiarize themselves with the information available there, with what is normal, knowing this, it will be easier for you to navigate what phases of coagulation are affected by the drugs described below and what are their effects.
An 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.
In a healthy human body, the coagulation and anticoagulation systems of the blood are in dynamic equilibrium. At the same time, blood flow through the vessels is not impeded, and there is no excessive thrombosis, both with open bleeding and inside the vascular bed.
If this balance is disturbed, conditions are created for thrombosis of small or large vessels or even the development of disseminated intravascular coagulation syndrome, in which multiple blood clots can lead to rapid death.
However, a number of clinical situations lead to the fact that blood clots form out of place and out of time, clogging veins and arteries of different calibers.
Editor-in-chief of the Detonic online magazine, cardiologist Yakovenko-Plahotnaya Tatyana. Author of more than 950 scientific articles, including in foreign medical journals. He has been working as a cardiologist in a clinical hospital for over 12 years. He owns modern methods of diagnosis and treatment of cardiovascular diseases and implements them in his professional activities. For example, it uses methods of resuscitation of the heart, decoding of ECG, functional tests, cyclic ergometry and knows echocardiography very well.
For 10 years, she has been an active participant in numerous medical symposia and workshops for doctors - families, therapists and cardiologists. He has many publications on a healthy lifestyle, diagnosis and treatment of heart and vascular diseases.
He regularly monitors new publications of European and American cardiology journals, writes scientific articles, prepares reports at scientific conferences and participates in European cardiology congresses.