Sartans for arterial hypertension - a list of drugs, classification by generation and mechanism of action. The mechanism of action of sartans on the body, indications and contraindications for the use of sartans classification by generation

Drugs that block angiotensin II receptors, lowering blood pressure, are called sartans. They are distinguished by good tolerability and effectiveness in the treatment of hypertension. These drugs are prescribed for concomitant metabolic syndrome, kidney damage, myocardial hypertrophy and circulatory failure.

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Mechanism of action

Low oxygen supply to the kidneys (hypotension, hypoxia) leads to the formation of an enzyme - renin. With its help, angiotensinogen passes into angiotensin 1. It also does not cause vasoconstriction, but only after conversion into angiotensin 2 provokes hypertension.

Sufficiently well-known drugs for the treatment of high blood pressure inhibit precisely the latter reaction. They are often prescribed to patients in the form of Capoten. These are the so-called.

But some patients have no reaction to this group of medicines. Such stability is explained by the fact that in addition to the angiotensin-converting enzyme itself, there are a number of other compounds involved in such reactions.

Therefore, the appearance of receptor blockers for such an active vasoconstrictor as angiotensin 2 helps to solve several problems at once in the treatment of hypertension.

Effects on the heart, kidneys

A feature of medicines from the sartans group is the ability to protect internal organs. They have a cardio- and nephroprotective effect, increase tissue sensitivity to insulin, which has a positive effect on patients with diabetes, and also reduce progression.

When taking these drugs, the risk of occurrence decreases, especially decreases. Patients are less likely to experience complications, sartans soften the manifestations of circulatory failure.

Nephropathy often complicates hypertension and diabetes mellitus. In this case, the body loses protein in the urine. One of the clinical effects of sartans is to slow down proteinuria with a simultaneous increase in glomerular filtration rate.

Classification of sartans

The distribution of drugs within the group is carried out according to the active substance. Medicines can be based on:

  • losartan (Lorista,);
  • (Teveten);
  • valsartan (Valsacor, Diocor Solo);
  • irbesartan (Aprovel);
  • candesartana (Casark);
  • telmisartan (Micardis, Prytor);
  • olmesartan (Olmesar).

Such a good representation of sartans in the pharmacy network is due to the fact that they are gaining more and more popularity among doctors and patients with hypertension.

Indications for use

The main disease in which sartans are used is hypertension. But besides this, there are accompanying indications for the appointment:

  • kidney disease in patients with hypertension and diabetes;
  • chronic circulatory failure, especially in the presence of contraindications to ACE inhibitors (for example, cough);
  • blood flow disorders in the cerebral vessels (transient attacks) in hypertension and myocardial hypertrophy;
  • acute period of infarction with dysfunction of the left ventricle.

Watch the video about the appointment of sartans for hypertension and their action:

Additional effects

If we conduct a comparative analysis between the main antihypertensive drugs and sartans, we can find the undoubted advantages of the latter. These include:

  • good tolerance, as they do not affect the exchange of bradykinin. This means that dry cough and angioedema do not develop;
  • prolonged and stable lowering of blood pressure;
  • inhibit the main and additional effects of angiotensin 2;
  • do not increase the content of uric acid, sugar and cholesterol;
  • reduce mortality from;
  • protect brain cells, improve memory and mental activity in the elderly;
  • improve potency;
  • strengthen the wall of the aorta in patients with;
  • improve carbohydrate and fat metabolism, can be used in obese patients;
  • prescribed with a weak effectiveness of ACE inhibitors or their intolerance.

Contraindications

Despite the relative safety, the appointment of sartans can only be carried out by a doctor, they are not recommended for:

  • hypersensitivity to any of the components of the drug;
  • impaired liver function, cirrhosis and bile stasis;
  • insufficiency of kidney function requiring hemodialysis;
  • pregnancy and lactation.

Side effects when taking

The drugs are distinguished by rare side effects in the form of dizziness and nausea, abdominal pain. In patients with myocardial infarction, a headache was also noted, hypotension occurs when standing up (), asthenia.

With dehydration or forced excretion of fluid in patients taking sartans, blood pressure may drop significantly. Therefore, in such cases, before starting treatment, it is necessary to restore the volume of circulating blood and the concentration of sodium.

Combined with diuretics

When used together with diuretics, their strength increases, and sartans reduce the loss of potassium caused by. The most common is the combination with 12.5 mg of hydrochlorothiazide.

Preparations of this composition are:

It is considered one of the most modern Valsartan for pressure. The antihypertensive agent may be in the form of tablets and capsules. The medicine helps even those patients who develop a cough after conventional drugs for pressure.

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  • The need for treatment of renal hypertension is due to symptoms that seriously impair the quality of life. Tablets and drugs, as well as folk medicines, will help in the treatment of hypertension with stenosis of the renal arteries, with renal failure.
  • In the treatment of hypertension, some drugs include the substance eprosartan, the use of which helps to normalize blood pressure. The influence is taken as a basis in such a drug as Teveten. There are analogues with a similar effect.
  • Which drug to normalize pressure to choose: "Valsartan" or "Losartan"? To determine which one is more effective, you need to compare the characteristics of these drugs. The patient can study the instructions attached to the medications, however, the selection of a medicine for the treatment of hypertension should be handled by a specialized physician. Medicines are prescribed only on the basis of the results of a diagnostic examination, which the patient must undergo before starting the therapeutic course.

    General information about "Valsartan" and "Losartan"

    "Valsartan"

    With a decrease in blood pressure, Valsartan and Losartan show high efficiency. To choose which is better, you need to familiarize yourself with the characteristics of each of them.

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    The action of the pharmaceutical agent is aimed at stabilizing blood pressure. The drug belongs to the ARB group. The active components of "Valsartan" do not affect the blood levels of cholesterol, glucose and uric acid. They reduce the enlarged myocardium against the background of hypertension. After discontinuation, the withdrawal syndrome does not appear, which means that a gradual reduction in dosage is not required. In patients with chronic heart failure, the drug reduces the severity of edema, eliminates increased stimulation of the RAAS and prevents pathological cell growth. It is produced in the form of tablets, which contain as an active substance - valsartan and such additional components as:

    • aerosil;
    • food emulsifier;
    • dye;
    • croscaramellose sodium.

    "Losartan"

    Taking the drug contributes to a gradual decrease in pressure.

    The drug, which is a specific ARB, is intended for oral administration. Produced in tablets that contain losartan - the active substance and auxiliary components:

    • croscarmellose sodium;
    • food emulsifier E572;
    • calcium hydrogen phosphate dihydrate;
    • talc;
    • aerosil.

    Losartan reduces peripheral vascular resistance, blood pressure and afterload. The drug reduces the concentration of adrenal hormones in the blood plasma, has a diuretic effect and reduces pressure in the pulmonary circulation. "Losartan" is characterized by a long action and does not have a serious effect on the heart rate.

    Indications and contraindications

    Taking "Valsartan" is recommended for hypertension, acute myocardial infarction, chronic heart failure, as well as arterial hypertension associated with pathologies of organs that are actively involved in the regulation of blood pressure. It is contraindicated to use "Valsartan" to normalize pressure in the following cases:

    • children's age up to 18 years;
    • the period of bearing a child and GV;
    • liver dysfunction;
    • hypersensitivity to the components of the tablets.

    "Losartan" is prescribed to patients with arterial hypertension, impaired functioning of the heart muscle and to reduce the risk of stroke in a hypertensive crisis. It is contraindicated to use a medicine for the treatment of hypertension with hypersensitivity to substances from the composition of Losartan. It is not recommended to drink pills for pregnant women and nursing mothers, as well as for small children.

    What's better?


    The antihypertensive effect occurs during treatment with both Valsartan and Losartan.

    What is the difference between the drugs? First of all, it should be noted that "Valsartan" in comparison with "Losartan" does not contain water-soluble substances and does not need biotransformation during the initial passage through the liver. In addition, a persistent decrease in blood pressure from the beginning of treatment with Valsartan occurs after 2-4 weeks, and the maximum antihypertensive effect of Losartan appears after 3-6 weeks. It is difficult to determine which medicine is better, because each organism reacts differently to medicinal substances entering it.

    The mechanism of action of drugs is to suppress the activity of the renin-angiotensin-aldosterone system, which has a positive effect on human health.

    Sartans are not inferior in effectiveness to well-known drugs for high blood pressure, practically do not cause side effects, relieve symptoms of hypertension, and have a protective effect on the cardiovascular system, kidneys and brain. Also, such drugs are called angiotensin-II receptor blockers or angiotensin receptor antagonists.

    If we compare all drugs for arterial hypertension, sartans are considered the most effective drugs, while their price is quite affordable. As medical practice shows, many patients take sartans stably for several years.

    This is due to the fact that such drugs for high blood pressure, which include Eprosartan and other drugs, cause a minimum of side effects.

    Including in patients, they do not experience a reaction in the form of a dry cough, which often occurs while taking ACE inhibitors. As for the claim that drugs can cause cancer, this issue is under scrutiny.

    Sartans and treatment of arterial hypertension

    Initially, sartans were developed as a medicine for high blood pressure. Studies have shown that drugs such as Eprosartan and others can lower blood pressure as effectively as the main types of drugs for hypertension.

    Angiotensin-II receptor blockers are taken once a day, these medications smoothly lower blood pressure readings throughout the day.

    The effectiveness of the drugs directly depends on the degree of activity of the renin-angiotensin system. The most effective is the treatment of patients who have a high activity of renin in the blood plasma. To identify these indicators, the patient is prescribed a blood test.

    Eprosartan and other sartans, the prices of which are comparable to similar drugs in terms of the target effect, lower blood pressure for a long period (on average, over 24 hours).

    A persistent therapeutic effect can be seen after two to four weeks of continuous treatment, which is significantly enhanced by the eighth week of therapy.

    Benefits of drugs

    In general, a drug of this group has quite positive reviews from doctors and patients. Sartans have numerous advantages over traditional preparations.

    1. With prolonged use of the drug for more than two years, the drug does not cause dependence and addiction. If you abruptly stop taking the medicine, this does not provoke a sharp increase in blood pressure.
    2. If a person has normal blood pressure, sartans do not lead to an even greater decrease in indicators.
    3. Angiotensin-II receptor blockers are better tolerated by patients and practically do not cause side effects.

    In addition to the main function of lowering blood pressure, the drugs have a beneficial effect on the functioning of the kidneys if the patient has diabetic nephropathy. Sartans also contribute to the regression of left ventricular hypertrophy and improve performance in people with heart failure.

    For a better therapeutic effect, angiotensin-II receptor blockers are recommended to be taken in combination with diuretic drugs in the form of Dichlothiazide or Indapamide, this enhances the effect of the drug by one and a half times. As for thiazide diuretics, they have not only an amplifying, but also a lengthening effect of blockers.

    Additionally, sartans have the following clinical effect:

    • The cells of the nervous system are protected. The drug protects the brain in hypertension, reduces the risk of stroke. Since the drug acts directly on brain receptors, it is often recommended to patients with normal blood pressure, who are at high risk of vascular catastrophe in the brain.
    • Due to the antiarrhythmic effect in patients, the risk of paroxysmal atrial fibrillation is reduced.
    • With the help of a metabolic effect with regular use of the drug, the risk of developing type 2 diabetes is reduced. In the presence of such a disease, the patient's condition is quickly corrected by reducing tissue insulin resistance.

    When using drugs in a patient, lipid metabolism improves, cholesterol and triglyceride levels decrease. Sartans help to reduce the amount of uric acid in the blood, which is necessary in case of long-term treatment with diuretics. In the presence of connective tissue disease, the walls of the aorta are strengthened and their rupture is prevented. In patients with Duchenne myodystrophy, the condition of muscle tissues improves.

    The price of medicines depends on the manufacturer and duration of action of the medicine. Losartan and Valsartan are considered the cheapest options, but they have a shorter duration of action, so they require more frequent use.

    Classification of drugs

    Sartans are classified according to their chemical composition and effects on the body. Depending on whether the drug has an active metabolite, drugs are divided into so-called prodrugs and active substances.

    According to the chemical composition, sartans are divided into four groups:

    1. Candesartan, Irbesartan and Losartan are tetrazole biphenyl derivatives;
    2. Telmisartan is a non-biphenyl derivative of tetrazole;
    3. Eprosartan is a non-biphenyl netetrazole;
    4. Valsartan is considered a non-cyclic compound.

    In modern times, there are a large number of drugs in this group that can be purchased at a pharmacy without presenting a doctor's prescription, including Eprosartan, Losartan, Valsartan, Irbesartan, Candesartan, Telmisartan, Olmesartan, Azilsartan.

    Additionally, in specialized stores, you can purchase a ready-made combination of sartans with calcium antagonists, diuretics, renin secretion antagonist aliskiren.

    Instructions for use of the drug

    The doctor prescribes the medication individually, after a complete examination. The dosage is compiled according to the information that displays the instructions for the use of the drug. It is important to take the medicine every day to avoid missing it.

    The doctor prescribes an angiotensin-II receptor blocker for:

    • heart failure;
    • Postponed myocardial infarction;
    • diabetic nephropathy;
    • Proteinuria, microalbuminuria;
    • Hypertrophy of the left ventricle of the heart;
    • atrial fibrillation;
    • metabolic syndrome;
    • Intolerance to ACE inhibitors.

    According to the instructions for use, unlike ACE inhibitors, sartans do not increase the level of protein in the blood, which often leads to an inflammatory reaction. Due to this, the drug does not have such side effects as angioedema and cough.

    In addition to the fact that Eprosartan and other drugs reduce blood pressure in arterial hypertension, they additionally have a positive effect on other internal organs:

    1. The hypertrophy of the mass of the left ventricle of the heart decreases;
    2. Improves diastolic function;
    3. Reduced ventricular arrhythmia;
    4. Reduced excretion of protein through the urine;
    5. The blood flow in the kidneys increases, while the glomerular filtration rate does not decrease.
    6. Does not affect the levels of sugar, cholesterol and purines in the blood;
    7. Tissue sensitivity to insulin increases, thereby reducing insulin resistance.

    Researchers have conducted many experiments on the effectiveness of the drug in the treatment of hypertension and the presence of benefits. Patients with impaired functioning of the cardiovascular system took part in the experiments, due to which it was possible to test the mechanism of the drugs in practice and prove the high effectiveness of the drug.

    At the moment, studies are underway to determine whether sartans are really capable of provoking cancer.

    Sartans with diuretics

    Such a combination effectively relieves hypertension, and angiotensin-II receptor blockers, when using diuretics, have a uniform and long-term effect on the body.

    There is a certain list of drugs that contain a certain amount of sartans and diuretics.

    • The composition of Atacand plus includes 16 mg of Candesartan and 12.5 mg of Hydrochlorothiazide;
    • Co-diovan contains 80 mg of Valsartan and 12.5 mg of Hydrochlorothiazide;
    • The drug Lorista H / ND contains 12.5 mg of Hydrochlorothiazide img Losartan;
    • Mikardis Plus contains 80 mg of Telmisartan and 12.5 mg of Hydrochlorothiazide;
    • The composition of Teveten plus includes Eprosartan in the amount of 600 mg and 12.5 mg of Hydrochlorothiazide.

    As practice and numerous positive patient reviews show, all these drugs included in the list help well with arterial hypertension, have a protective effect on internal organs, and reduce the risk of stroke, myocardial infarction, and kidney failure.

    All these drugs are considered safe, as they have practically no side effects. Meanwhile, it is important to understand that the therapeutic effect is usually not immediately visible. It is possible to objectively assess whether the drug helps with high blood pressure only after four weeks of continuous treatment. If this is not taken into account, the doctor may rush and prescribe a new drug with a stronger effect, which will negatively affect the patient's health.

    The effect of the drug on the heart muscle

    With a decrease in blood pressure while taking sartans, the patient's heart rate does not increase. A particular positive effect can be observed when blocking the activity of the renin-angiotensin-aldosterone system in the vascular walls and the myocardial region. This protects against hypertrophy of the blood vessels and the heart.

    This feature of the drugs is especially useful if the patient has hypertensive cardiomyopathy, coronary disease, cardiosclerosis. Additionally, sartans reduce atherosclerotic lesions of the heart vessels.

    The effect of the drug on the kidneys

    As you know, in arterial hypertension, the kidneys act as a target organ. Sartans, in turn, help to reduce protein excretion in the urine in people with kidney damage in diabetes mellitus and hypertension. Meanwhile, it is important to consider that in the presence of unilateral renal artery stenosis, angiotensin II receptor blockers often increase plasma creatinine levels and cause acute renal failure.

    Due to the fact that the drugs inhibit the reverse absorption of sodium in the proximal tubule, inhibit the synthesis and release of aldosterone, the body gets rid of salt through the urine. This mechanism in turn causes a certain diuretic effect.

    1. Compared with sartans, the use of ACE inhibitors has a side effect in the form of a dry cough. This symptom sometimes becomes so severe that patients have to stop using the medicine.
    2. Sometimes the patient develops angioedema.
    3. Also, specific kidney complications include a sharp decrease in glomerular filtration rate, which causes an increase in potassium and creatinine in the blood. The risk of developing complications is especially high in patients with atherosclerosis of the renal arteries, congestive heart failure, hypotension and a decrease in blood circulation.

    In this case, sartans act as the main drug, which slowly reduces the glomerular filtration rate of the kidneys. Due to this, the amount of creatinine in the blood does not increase. Additionally, the medicine does not allow the development of nephrosclerosis.

    Presence of side effects and contraindications

    The drugs have a therapeutic effect similar to placebo, therefore they have a minimum of side effects and are well tolerated, compared with ACE inhibitors. Sartans do not cause a dry cough, and the risk of angioedema is minimal.

    But it must be taken into account that angiotensin II receptor blockers in some cases are able to quickly reduce blood pressure due to the activity of renin in the blood plasma. With bilateral narrowing of the renal arteries in a patient, the work of the kidneys may be disrupted. Sartans are not approved for use during pregnancy, as this adversely affects the development of the fetus.

    Despite the presence of undesirable effects, Eprosartan and other sartans are classified as drugs that are well tolerated and rarely cause adverse reactions in the treatment of high blood pressure. The drug is well combined with other drugs against hypertension, the best therapeutic effect is observed during the additional use of diuretic drugs.

    Also today, the disputes of scientists about the advisability of using sartans do not fade away, given the fact that these drugs can provoke cancer in a certain situation.

    Sartans and cancer

    Since the angiotensin receptor blockers Eprosartan and others use the mechanism of action of the angiotensin-renin system, angiotensin type 1 and type 2 receptors are involved in the process. These substances are responsible for the regulation of cell proliferation and tumor development, which provoke cancer.

    Numerous scientific studies have been conducted to find out whether the risk that patients taking sartans regularly may develop cancer is really high. As the experiment showed, in patients taking angiotensin receptor blockers, the risk of developing oncology became higher compared to those people who did not take the medicine. Meanwhile, oncological disease with the same risk leads to death both after taking the drug and without it.

    Despite the findings, doctors still cannot accurately answer the question of whether Eprosartan and other sartans provoke cancer. The fact is that due to the lack of complete data on the involvement of each drug in oncological diseases, doctors cannot claim that sartans cause cancer. Today, research on this topic is actively ongoing, and researchers are very ambiguous on this issue.

    Thus, the question remains open, despite such a cancer-provoking effect, doctors consider sartans to be a really effective medicine that can become an analogue of traditional drugs for hypertension.

    However, there are certain angiotensin receptor blockers that help treat cancer. In particular, this applies to lung and pancreatic cancer. Also, some types of drugs are used during chemotherapy in hypertensive patients who have cancer of the pancreas, esophagus and stomach. An interesting video in this article will sum up the discussion about sartans.

    Sartans: action, use, list of drugs, indications and contraindications

    Scientists have reliably identified all the risk factors leading to the development of pathology of the heart and blood vessels several decades ago. Moreover, this pathology plays an important role in young people. The sequence of development of processes in a patient with risk factors from the moment of their occurrence to the development of terminal heart failure is called the cardiovascular continuum. In the latter, in turn, the so-called "hypertensive cascade" is of great importance - a chain of processes in the body of a patient suffering from hypertension, which is a risk factor for the occurrence of more serious diseases (stroke, heart attack, heart failure, etc.). Among the processes that can be influenced are those that are regulated by angiotensin II, the blockers of which are the sartans discussed below.

    So, if it was not possible to prevent the development of heart diseases by preventive measures, the development of more severe heart diseases should be “delayed” in the early stages. That is why patients with hypertension should carefully monitor blood pressure numbers (including by taking medications) in order to prevent left ventricular systolic dysfunction and the resulting adverse consequences.

    The mechanism of action of sartans - angiotensin II receptor blockers

    It is possible to break the pathological chain of processes occurring in the human body with arterial hypertension by influencing one or another link of pathogenesis. So, it has long been known that the cause of hypertension is an increased tone of the arteries, because, according to all the laws of hemodynamics, fluid enters a narrower vessel under greater pressure than a wide one. The renin-aldosterone-angiotensin system (RAAS) plays a leading role in the regulation of vascular tone. Without delving into the mechanisms of biochemistry, it is enough to mention that the angiotensin-converting enzyme promotes the formation of angiotensin II, and the latter, acting on receptors in the vascular wall, increases its tension, which results in arterial hypertension.

    Based on the foregoing, there are two important groups of drugs that affect the RAAS - angiotensin-converting enzyme inhibitors (ACE inhibitors) and angiotensin II receptor blockers (ARBs, or sartans).

    The first group - ACE inhibitors include drugs such as enalapril, lisinopril, captopril and many others.

    To the second - sartans, the drugs discussed in detail below are losartan, valsartan, telmisartan and others.

    So, sartans block receptors for angiotensin II, thereby normalizing increased vascular tone. As a result, the load on the heart muscle is reduced, because now it is much easier for the heart to "push" blood into the vessels, and blood pressure returns to normal.

    the effect of various antihypertensive drugs on the RAAS

    In addition, sartans, as well as ACE inhibitors, contribute to an organoprotective effect, that is, they “protect” the retina of the eyes, the inner wall of blood vessels (the intima, the integrity of which is extremely important at high cholesterol levels and in atherosclerosis), the heart muscle itself, the brain and kidneys from the adverse effects of high blood pressure.

    Add to high blood pressure and atherosclerosis increased blood viscosity, diabetes and poor lifestyle - in a large percentage of cases, you can get an acute heart attack or stroke at a fairly young age. Therefore, not only to correct the level of blood pressure, but also to prevent such complications, sartans should be used if the doctor has determined the patient's indications for taking them.

    Video: honey. animation about angiotensin II and high blood pressure

    When should you take sartans?

    Based on the foregoing, the following diseases act as indications for taking angiotensin receptor blockers:

    • Arterial hypertension, especially in combination with left ventricular hypertrophy. The excellent hypotensive effect of sartans is due to their effect on the pathogenetic processes occurring in the body of a patient with hypertension. However, patients should take into account that the optimal effect develops after a couple of weeks from the start of daily intake, but nevertheless, it persists throughout the entire period of treatment.
    • Chronic heart failure. According to the cardiovascular continuum mentioned at the beginning, all pathological processes in the heart and blood vessels, as well as in the neurohumoral systems that regulate them, sooner or later lead to the fact that the heart cannot cope with the increased load, and the heart muscle simply wears out. In order to stop pathological mechanisms in the early stages, there are ACE inhibitors and sartans. In addition, multicenter clinical studies have shown that ACE inhibitors, sartans, and beta-blockers significantly reduce the rate of progression of CHF, as well as reduce the risk of heart attack and stroke to a minimum.
    • Nephropathy. The use of sartans is justified in patients with kidney pathology, which caused or resulted from hypertension.
    • Cardiovascular pathology in patients with type 2 diabetes mellitus. The constant intake of sartans contributes to better utilization of glucose by body tissues due to a decrease in insulin resistance. This metabolic effect contributes to the normalization of blood glucose levels.
    • Cardiovascular pathology in patients with dyslipidemia. This indication is determined by the fact that sartans normalize blood cholesterol levels in patients with high cholesterol levels, as well as with an imbalance between very low, low and high density lipoprotein cholesterol (VLDL cholesterol, LDL cholesterol, HDL cholesterol). Recall that "bad" cholesterol is found in very low and low density lipoproteins, and "good" - in high density lipoproteins.

    Are there any advantages to sartans?

    After receiving synthetic drugs that block angiotensin receptors, scientists have solved some problems that arise in the practical use of antihypertensive drugs of other groups by doctors.

    So, in particular, ACE inhibitors (prestarium, noliprel, enam, lisinopril, diroton), which are quite effective and safe, moreover, in a sense, even “useful” drugs, are very often poorly tolerated by patients due to a pronounced side effect in dry compulsive cough. Sartans do not show such effects.

    Beta-blockers (egilok, metoprolol, concor, coronal, bisoprolol) and calcium channel antagonists (verapamil, diltiazem) significantly affect the heart rate, slowing it down, therefore, it is preferable to prescribe ARBs to patients with hypertension and rhythm disturbances such as bradycardia and / or bradyarrhythmia . The latter do not affect the conduction in the heart and the heart rate. In addition, sartans do not affect potassium metabolism in the body, which, again, does not cause conduction disturbances in the heart.

    An important advantage of sartans is the possibility of prescribing them to men who are sexually active, since sartans do not cause potency and erectile dysfunction, unlike outdated beta-blockers (anaprilin, obzidan), which are often taken by patients on their own, because they “help”.

    Despite all these advantages of such modern drugs as ARBs, all indications and features of a combination of drugs should be determined only by a doctor, taking into account the clinical picture and the results of the examination of a particular patient.

    Contraindications

    Contraindications to the use of sartans are individual intolerance to drugs of this group, pregnancy, children under 18 years of age, severe violations of the liver and kidneys (liver and kidney failure), aldosteronism, severe violations of the electrolyte composition of the blood (potassium, sodium), stenosis of the renal arteries, condition after a kidney transplant. In this regard, taking drugs should be started only after consultation with a general practitioner or cardiologist in order to avoid undesirable effects.

    Are side effects possible?

    As with any drug, a drug from this group may also have side effects. However, the frequency of their occurrence is negligible and occurs with a frequency of slightly more or less than 1%. These include:

    1. Weakness, dizziness, orthostatic hypotension (with a sharp adoption of a vertical body position), increased fatigue and other signs of asthenia,
    2. Pain in the chest, in the muscles and joints of the extremities,
    3. Abdominal pain, nausea, heartburn, constipation, dyspepsia.
    4. Allergic reactions, swelling of the mucous membrane of the nasal passages, dry cough, redness of the skin, pruritus.

    Are there better drugs among sartans?

    According to the classification of angiotensin receptor antagonists, four groups of these drugs are distinguished.

    This is based on the chemical structure of the molecule based on:

    • biphenyl derivative of tetrazole (losartan, irbesartan, candesartan),
    • A non-biphenyl derivative of tetrazole (telmisartan),
    • Non-biphenyl netetrazole (eprosartan),
    • Non-cyclic compound (valsartan).

    Despite the fact that sartans in themselves are an innovative solution in cardiology, among them, drugs of the latest (second) generation can also be distinguished, significantly superior to previous sartans in a number of pharmacological and pharmacodynamic properties and end effects. To date, this drug is telmisartan (trade name in Russia - "Micardis"). This medicine can rightly be called the best among the best.

    List of sartans, their comparative characteristics

    Can sartans be taken with other medications?

    Often, patients with hypertension have some other comorbidities that require the appointment of combined drugs. For example, patients with rhythm disturbances can receive antiarrhythmics, beta-blockers and angiotensin antagonist inhibitors at the same time, and patients with angina pectoris can also receive nitrates. In addition, all patients with cardiac pathology are shown to take antiplatelet agents (aspirin-cardio, thromboAss, acecardol, etc.). Therefore, patients receiving the listed drugs and not only them should not be afraid of taking them together, since sartans are fully compatible with other cardiac drugs.

    Of the clearly undesirable combination, only the combination of sartans and ACE inhibitors can be noted, because their mechanism of action is almost the same. Such a combination is not something that is contraindicated, rather, it is meaningless.

    In conclusion, it should be noted that, no matter how attractive the clinical effects of this or that drug, including sartans, may seem, first of all, you should consult your doctor. Again, treatment started at the wrong time is sometimes fraught with a threat to health and life, and vice versa, self-treatment, coupled with self-diagnosis, can also cause irreparable harm to the patient.

    Sartans for arterial hypertension - a list of drugs, classification by generation and mechanism of action

    A deep study of the pathological conditions of the cardiovascular system has made it possible to create receptor blockers for the angiotensin II provoking high blood pressure, known to patients as sartans for arterial hypertension. The main purpose of such drugs is to correct blood pressure, each jump of which brings the onset of serious problems with the heart, kidneys and brain vessels closer.

    What are sartans for arterial hypertension

    Sartans belong to a group of inexpensive drugs that lower blood pressure. In individuals predisposed to hypertension, these drugs become an essential component of a stable life, greatly improving the prospects for longevity. The composition of the drug contains components that have a corrective effect on pressure throughout the day, they prevent the onset of hypertensive attacks and prevent the disease.

    Indications for appointment

    The main indication for the use of sartans is hypertension. They are especially indicated for people who acutely tolerate therapy with beta-blockers, because they do not affect the metabolic processes in the body. In patients with heart failure, sartans are prescribed as a drug that slows down the mechanisms that lead to myocardial and left ventricular dysfunction. In neuropathy, they protect the kidneys and counteract the loss of protein in the body.

    In addition to the main indications for use, there are additional factors confirming the benefits of sartans. These include the following effects:

    Means for the treatment of hypertension!

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    • the ability to lower cholesterol;
    • reducing the risk of Alzheimer's disease;
    • strengthening the aortic wall, which serves as additional protection against the effects of hypertension.

    Mechanism of action

    With oxygen starvation and a decrease in blood pressure, a special substance begins to form in the kidneys - renin, which transforms angiotensinogen into angiotensin I. Further, angiotensin I, under the influence of special enzymes, converts angiotensin II, which, by binding to receptors sensitive to this compound, causes hypertension. The drugs act on these receptors, preventing hypertensive tendencies.

    Benefits of drugs

    Due to the high efficiency in the treatment of hypertensive crises, sartans have occupied an independent niche and are considered as an alternative to ACE inhibitors (angiotensin-converting enzyme inhibitors), which previously prevailed in the practice of preventing and treating various stages of hypertension. Proven benefits include:

    • improvement of symptoms in patients with heart metabolic insufficiency;
    • reducing the risk of stroke, atherosclerosis;
    • reducing the likelihood of an attack of atrial fibrillation;
    • effective and prolonged blocking of the action of angiotensin II;
    • lack of accumulation in the body of bradykinin (which provokes a dry cough);
    • well tolerated by the elderly;
    • no negative effect on sexual functions.

    Classification

    There are a lot of trade names of sartans. According to the chemical composition and, as a result, the effect on the human body, drugs are divided into four groups:

    • Biphenyl derivatives of tetrazole: Losartan, Irbesartan, Candesartan.
    • Non-biphenyl derivatives of tetrazole: Telmisartan.
    • Non-biphenyl netetrazoles: Eprosartan.
    • Non-cyclic compounds: Valsartan.

    List of drugs

    The use of sartans has found wide demand in medicine, practicing various methods of therapy for high blood pressure. A list of known and used remedies for secondary hypertension includes:

    • Losartan: Renicard, Lotor, Presartan, Lorista, Losacor, Losarel, Cozaar, Lozap.
    • Valsartan: Tareg, Nortivan, Tantordio, Valsakor, Diovan.
    • Eprosartan: Teveten.
    • Irbesartan: Firmasta, Ibertan, Aprovel, Irsar.
    • Telmisartan: Prytor, Micardis.
    • Olmesartan: Olimestra, Cardosal.
    • Kandesartan: Ordiss, Kandesar, Hyposart.
    • Azilsartan: Edarbi.

    Sartans of the latest generation

    The first generation includes those drugs that act exclusively on the hormonal system responsible for blood pressure (RAAS) through the blocking of sensitive AT 1 receptors. Second-generation sartans are bifunctional: they suppress undesirable manifestations of RAAS and have a positive effect on pathogenetic algorithms for lipid and carbohydrate metabolic disorders, as well as on inflammation (non-infectious) and obesity. Experts confidently assert that the future of antagonist sartans belongs to the second generation.

    Instructions for use

    Angiotensin receptor blockers have appeared on the market relatively recently. They should be taken as prescribed by a doctor in a dosage that depends on the individual characteristics of the patient. Drugs are used once a day, act for hours. The persistent effect of sartans manifests itself after 4-6 weeks from the moment of treatment. Medications relieve spasms of the vascular wall in symptomatic renal hypertension; they can be prescribed as part of complex therapy for resistant hypertension.

    Telmisartan

    A popular drug that is part of the angiotensin receptor blockers group is Telmisartan. Indications for the use of this antagonist are the prevention of cardiovascular diseases and the treatment of essential hypertension, it reduces the hypertrophy of cardiocytes, reduces the level of triglycerides. Tablets are taken orally, regardless of food intake, in elderly patients and in liver failure, dose adjustment of the drug is not carried out.

    The recommended dosage is 40 mg per day, sometimes it can be reduced to 20 mg (renal failure) or increased to 80 (if systolic pressure does not drop stubbornly). Telmisartan is well combined with thiazide diuretics. The course of treatment lasts approximately 4-8 weeks. At the beginning of therapy, blood pressure should be monitored.

    Losartan

    Doctors prescribe angiotensin receptor antagonists for hypertension and for its prevention. The most common sartan is Losartan. It is a tablet preparation taken from a dose of 100 mg. This amount provides a stable hypotensive effect. Film-coated tablets are taken once a day. If the effect is insufficient, the dose can be increased to two tablets per day.

    Contraindications to the use of sartans and side effects

    When using sartans for arterial hypertension, doctors note their good tolerance and the absence of specific side effects compared to other groups of drugs. Possible manifestations of a negative nature, according to reviews, are an allergic reaction, headache, dizziness, insomnia. Rarely noted fever, cough, sore throat, runny nose.

    In some cases, pressure sartans can cause nausea, vomiting, constipation, and myalgia. Contraindications for the use of medicines are:

    • pregnancy, breastfeeding, childhood due to lack of data on efficacy and safety;
    • renal failure, stenosis of renal vessels, kidney disease, nephropathy;
    • individual intolerance or hypersensitivity to the components.

    Sartans and cancer

    Scientists have found that angiotensin hyperactivity provokes the occurrence of malignant tumors. Sartans are angiotensin receptor blockers, therefore they suppress and prevent the development of many types of cancer in patients with high blood pressure and even diabetes. Sometimes drugs can be used during chemotherapy for already detected malignant neoplasms - they enhance drug delivery by unpacking tumor vessels. Sartans show activity in preventing the following types of cancer:

    • glioma;
    • colorectal cancer;
    • tumors of the stomach, lungs, bladder, prostate, pancreas;
    • cancer of the endometrium, ovaries.

    An effective combination of drugs from different groups

    Often, patients with arterial hypertension have comorbidities that require the appointment of combined drugs. In this regard, you should be aware of the compatibility of medicines with prescribed sartans:

    • The combination of sartans with ACE inhibitors is undesirable due to the same mechanism of action.
    • The appointment of diuretics (diuretics), drugs with ethanol, antihypertensive drugs may enhance the hypotensive effect.
    • Non-steroidal anti-inflammatory drugs, estrogens, sympathomimetics weaken their effectiveness.
    • Potassium-sparing diuretics and potassium-containing drugs can lead to hyperkalemia.
    • Lithium preparations lead to an increase in the concentration of lithium in the blood, increase the risk of toxic effects.
    • Warfarin reduces the concentration of sartans, increases prothrombin time.

    Video

    The information presented in the article is for informational purposes only. The materials of the article do not call for self-treatment. Only a qualified doctor can make a diagnosis and give recommendations for treatment based on the individual characteristics of a particular patient.

    Sartans are a new generation of drugs that are used to lower blood pressure in hypertension. The first versions of these types of drugs were synthesized in the early 90s of the last century.

    The mechanism of action of drugs is to suppress the activity of the renin-angiotensin-aldosterone system, which has a positive effect on human health.

    Sartans are not inferior in effectiveness to well-known drugs for high blood pressure, practically do not cause side effects, relieve symptoms of hypertension, and have a protective effect on the cardiovascular system, kidneys and brain. Also, such drugs are called angiotensin-II receptor blockers or angiotensin receptor antagonists.

    If we compare all drugs for arterial hypertension, sartans are considered the most effective drugs, while their price is quite affordable. As medical practice shows, many patients take sartans stably for several years.

    This is due to the fact that such drugs for high blood pressure, which include Eprosartan and other drugs, cause a minimum of side effects.

    Including in patients, they do not experience a reaction in the form of a dry cough, which often occurs while taking ACE inhibitors. As for the claim that drugs can cause cancer, this issue is under scrutiny.

    Sartans and treatment of arterial hypertension

    Initially, sartans were developed as a medicine for high blood pressure. Studies have shown that drugs such as Eprosartan and others can lower blood pressure as effectively as the main types of drugs for hypertension.

    Angiotensin-II receptor blockers are taken once a day, these medications smoothly lower blood pressure readings throughout the day.

    The effectiveness of the drugs directly depends on the degree of activity of the renin-angiotensin system. The most effective is the treatment of patients who have a high activity of renin in the blood plasma. To identify these indicators, the patient is prescribed a blood test.

    Eprosartan and other sartans, the prices of which are comparable to similar drugs in terms of the target effect, lower blood pressure for a long period (on average, over 24 hours).

    A persistent therapeutic effect can be seen after two to four weeks of continuous treatment, which is significantly enhanced by the eighth week of therapy.

    Benefits of drugs

    In general, a drug of this group has quite positive reviews from doctors and patients. Sartans have numerous advantages over traditional preparations.

    1. With prolonged use of the drug for more than two years, the drug does not cause dependence and addiction. If you abruptly stop taking the medicine, this does not provoke a sharp increase in blood pressure.
    2. If a person has normal blood pressure, sartans do not lead to an even greater decrease in indicators.
    3. Angiotensin-II receptor blockers are better tolerated by patients and practically do not cause side effects.

    In addition to the main function of lowering blood pressure, the drugs have a beneficial effect on the functioning of the kidneys if the patient has diabetic nephropathy. Sartans also contribute to the regression of left ventricular hypertrophy and improve performance in people with heart failure.

    For a better therapeutic effect, angiotensin-II receptor blockers are recommended to be taken in combination with diuretic drugs in the form of Dichlothiazide or Indapamide, this enhances the effect of the drug by one and a half times. As for thiazide diuretics, they have not only an amplifying, but also a lengthening effect of blockers.

    Additionally, sartans have the following clinical effect:

    • The cells of the nervous system are protected. The drug protects the brain in hypertension, reduces the risk of stroke. Since the drug acts directly on brain receptors, it is often recommended to patients with normal blood pressure, who are at high risk of vascular catastrophe in the brain.
    • Due to the antiarrhythmic effect in patients, the risk of paroxysmal atrial fibrillation is reduced.
    • With the help of a metabolic effect with regular use of the drug, the risk of developing type 2 diabetes is reduced. In the presence of such a disease, the patient's condition is quickly corrected by reducing tissue insulin resistance.

    When using drugs in a patient, lipid metabolism improves, cholesterol and triglyceride levels decrease. Sartans help to reduce the amount of uric acid in the blood, which is necessary in case of long-term treatment with diuretics. In the presence of connective tissue disease, the walls of the aorta are strengthened and their rupture is prevented. In patients with Duchenne myodystrophy, the condition of muscle tissues improves.

    The price of medicines depends on the manufacturer and duration of action of the medicine. Losartan and Valsartan are considered the cheapest options, but they have a shorter duration of action, so they require more frequent use.

    Classification of drugs

    Sartans are classified according to their chemical composition and effects on the body. Depending on whether the drug has an active metabolite, drugs are divided into so-called prodrugs and active substances.

    According to the chemical composition, sartans are divided into four groups:

    1. Candesartan, Irbesartan and Losartan are tetrazole biphenyl derivatives;
    2. Telmisartan is a non-biphenyl derivative of tetrazole;
    3. Eprosartan is a non-biphenyl netetrazole;
    4. Valsartan is considered a non-cyclic compound.

    In modern times, there are a large number of drugs in this group that can be purchased at a pharmacy without presenting a doctor's prescription, including Eprosartan, Losartan, Valsartan, Irbesartan, Candesartan, Telmisartan, Olmesartan, Azilsartan.

    Additionally, in specialized stores, you can purchase a ready-made combination of sartans with calcium antagonists, diuretics, renin secretion antagonist aliskiren.

    Instructions for use of the drug

    The doctor prescribes the medication individually, after a complete examination. The dosage is compiled according to the information that displays the instructions for the use of the drug. It is important to take the medicine every day to avoid missing it.

    The doctor prescribes an angiotensin-II receptor blocker for:

    • heart failure;
    • Postponed myocardial infarction;
    • diabetic nephropathy;
    • Proteinuria, microalbuminuria;
    • Hypertrophy of the left ventricle of the heart;
    • atrial fibrillation;
    • metabolic syndrome;
    • Intolerance to ACE inhibitors.

    According to the instructions for use, unlike ACE inhibitors, sartans do not increase the level of protein in the blood, which often leads to an inflammatory reaction. Due to this, the drug does not have such side effects as angioedema and cough.

    In addition to the fact that Eprosartan and other drugs reduce blood pressure in arterial hypertension, they additionally have a positive effect on other internal organs:

    1. The hypertrophy of the mass of the left ventricle of the heart decreases;
    2. Improves diastolic function;
    3. Reduced ventricular arrhythmia;
    4. Reduced excretion of protein through the urine;
    5. The blood flow in the kidneys increases, while the glomerular filtration rate does not decrease.
    6. Does not affect the levels of sugar, cholesterol and purines in the blood;
    7. Tissue sensitivity to insulin increases, thereby reducing insulin resistance.

    Researchers have conducted many experiments on the effectiveness of the drug in the treatment of hypertension and the presence of benefits. Patients with impaired functioning of the cardiovascular system took part in the experiments, due to which it was possible to test the mechanism of the drugs in practice and prove the high effectiveness of the drug.

    At the moment, studies are underway to determine whether sartans are really capable of provoking cancer.

    Sartans with diuretics

    Such a combination effectively relieves hypertension, and angiotensin-II receptor blockers, when using diuretics, have a uniform and long-term effect on the body.

    There is a certain list of drugs that contain a certain amount of sartans and diuretics.

    • The composition of Atacand plus includes 16 mg of Candesartan and 12.5 mg of Hydrochlorothiazide;
    • Co-diovan contains 80 mg of Valsartan and 12.5 mg of Hydrochlorothiazide;
    • The drug Lorista H / ND contains 12.5 mg of Hydrochlorothiazide and 50-100 mg of Losartan;
    • Mikardis Plus contains 80 mg of Telmisartan and 12.5 mg of Hydrochlorothiazide;
    • The composition of Teveten plus includes Eprosartan in the amount of 600 mg and 12.5 mg of Hydrochlorothiazide.

    As practice and numerous positive patient reviews show, all these drugs included in the list help well with arterial hypertension, have a protective effect on internal organs, and reduce the risk of stroke, myocardial infarction, and kidney failure.

    All these drugs are considered safe, as they have practically no side effects. Meanwhile, it is important to understand that the therapeutic effect is usually not immediately visible. It is possible to objectively assess whether the drug helps with high blood pressure only after four weeks of continuous treatment. If this is not taken into account, the doctor may rush and prescribe a new drug with a stronger effect, which will negatively affect the patient's health.

    The effect of the drug on the heart muscle

    With a decrease in blood pressure while taking sartans, the patient's heart rate does not increase. A particular positive effect can be observed when blocking the activity of the renin-angiotensin-aldosterone system in the vascular walls and the myocardial region. This protects against hypertrophy of the blood vessels and the heart.

    This feature of the drugs is especially useful if the patient has hypertensive cardiomyopathy, coronary disease, cardiosclerosis. Additionally, sartans reduce atherosclerotic lesions of the heart vessels.

    The effect of the drug on the kidneys

    As you know, in arterial hypertension, the kidneys act as a target organ. Sartans, in turn, help to reduce protein excretion in the urine in people with kidney damage in diabetes mellitus and hypertension. Meanwhile, it is important to consider that in the presence of unilateral renal artery stenosis, angiotensin II receptor blockers often increase plasma creatinine levels and cause acute renal failure.

    Due to the fact that the drugs inhibit the reverse absorption of sodium in the proximal tubule, inhibit the synthesis and release of aldosterone, the body gets rid of salt through the urine. This mechanism in turn causes a certain diuretic effect.

    1. Compared with sartans, the use of ACE inhibitors has a side effect in the form of a dry cough. This symptom sometimes becomes so severe that patients have to stop using the medicine.
    2. Sometimes the patient develops angioedema.
    3. Also, specific kidney complications include a sharp decrease in glomerular filtration rate, which causes an increase in potassium and creatinine in the blood. The risk of developing complications is especially high in patients with atherosclerosis of the renal arteries, congestive heart failure, hypotension and a decrease in blood circulation.

    In this case, sartans act as the main drug, which slowly reduces the glomerular filtration rate of the kidneys. Due to this, the amount of creatinine in the blood does not increase. Additionally, the medicine does not allow the development of nephrosclerosis.

    Presence of side effects and contraindications

    The drugs have a therapeutic effect similar to placebo, therefore they have a minimum of side effects and are well tolerated, compared with ACE inhibitors. Sartans do not cause a dry cough, and the risk of angioedema is minimal.

    But it must be taken into account that angiotensin II receptor blockers in some cases are able to quickly reduce blood pressure due to the activity of renin in the blood plasma. With bilateral narrowing of the renal arteries in a patient, the work of the kidneys may be disrupted. Sartans are not approved for use during pregnancy, as this adversely affects the development of the fetus.

    Despite the presence of undesirable effects, Eprosartan and other sartans are classified as drugs that are well tolerated and rarely cause adverse reactions in the treatment of high blood pressure. The drug is well combined with other drugs against hypertension, the best therapeutic effect is observed during the additional use of diuretic drugs.

    Also today, the disputes of scientists about the advisability of using sartans do not fade away, given the fact that these drugs can provoke cancer in a certain situation.

    Sartans and cancer

    Since the angiotensin receptor blockers Eprosartan and others use the mechanism of action of the angiotensin-renin system, angiotensin type 1 and type 2 receptors are involved in the process. These substances are responsible for the regulation of cell proliferation and tumor development, which provoke cancer.

    Numerous scientific studies have been conducted to find out whether the risk that patients taking sartans regularly may develop cancer is really high. As the experiment showed, in patients taking angiotensin receptor blockers, the risk of developing oncology became higher compared to those people who did not take the medicine. Meanwhile, oncological disease with the same risk leads to death both after taking the drug and without it.

    Despite the findings, doctors still cannot accurately answer the question of whether Eprosartan and other sartans provoke cancer. The fact is that due to the lack of complete data on the involvement of each drug in oncological diseases, doctors cannot claim that sartans cause cancer. Today, research on this topic is actively ongoing, and researchers are very ambiguous on this issue.

    Thus, the question remains open, despite such a cancer-provoking effect, doctors consider sartans to be a really effective medicine that can become an analogue of traditional drugs for hypertension.

    However, there are certain angiotensin receptor blockers that help treat cancer. In particular, this applies to lung and pancreatic cancer. Also, some types of drugs are used during chemotherapy in hypertensive patients who have cancer of the pancreas, esophagus and stomach. An interesting video in this article will sum up the discussion about sartans.

    Against the background of a decrease in blood pressure and hypoxia, renin is formed in the kidneys. This substance promotes the conversion of inactive angiotensinogen to angiotensin. The action of sartans in arterial hypertension is directed to this reaction.

    The following classification of sartans is recognized by specialists (taking into account the chemical structure):

    • medicines of a biphenyl derivative of tetrazole (Losartan, Candesartan);
    • medicines of a non-biphenyl derivative of tetrazole (Telmisartan);
    • non-biphenyl non-tetrazoles (Eprosartan);
    • medicines of a non-cyclic compound (Valsartan).

    A separate group includes combined sartans with calcium antagonists and diuretics. Rasilez is taken for high blood pressure at the dosage prescribed by the doctor. If the medication is taken for the first time, a hypotensive reaction is not observed. Dry cough is less common in patients taking Rasilez with Ramipril.

    Against the background of the complex administration of Rasilez and Amlodipine, the frequency of peripheral edema decreases. Monotherapy with Rasilez in current diabetes mellitus can effectively and safely reduce blood pressure.

    Patients who suffer from hypertension and CHF receive standard treatment with Rasilez. Against the background of taking this medication, unwanted reactions may develop, which are temporary.

    Rasilez is contraindicated for drinking in severe violations of kidney function, nephrotic syndrome, RG.

    With a lack of oxygen in the body and a decrease in blood pressure, renin is produced. This is a special element due to which inactive angiotensinogen is converted to angiotensin I, and this in turn is converted to angiotensin II due to the action of angiotensin-converting enzyme. It is ACE inhibitors that have an effect on such a reaction.

    Transformed angiotensin II is a very active substance. It is able to rapidly increase pressure and maintain its stable performance due to interaction with receptors.

    This allows the use of sartans in arterial hypertension and influence the receptors, due to which the therapeutic effect of the drug is observed.

    Suppress inflammation - one of the causes of aging

    With age, the level of systemic inflammation in the body increases, which is also one of the causes of aging and the development of many age-related diseases. One of the indicators of increased inflammatory processes in the body is an analysis of C-reactive protein.

    Its high rates reflect the processes of inflammation. Studies have shown that angiotensin II increases C-reactive protein.

    But sartans are blockers of angiotensin II receptors (AT1 receptors).

    Classification of drugs

    The cost of drugs depends on the manufacturer, duration of action. When using the cheapest medicines, the patient must understand that they need to be drunk more often, since they have a short effect.

    Preparations are divided according to composition and effect. Doctors divide them into prodrugs and active substances, based on the presence of an active metabolite. According to the chemical composition, sartans are:


    Without a prescription, all these funds can be purchased at specialized points. In addition, pharmacies offer ready-made combinations.

    Sartans are classified according to their chemical composition and effects on the body. Depending on whether the drug has an active metabolite, drugs are divided into so-called prodrugs and active substances.

    According to the chemical composition, sartans are divided into four groups:

    1. Candesartan, Irbesartan and Losartan are tetrazole biphenyl derivatives;
    2. Telmisartan is a non-biphenyl derivative of tetrazole;
    3. Eprosartan is a non-biphenyl netetrazole;
    4. Valsartan is considered a non-cyclic compound.

    In modern times, there are a large number of drugs in this group that can be purchased at a pharmacy without presenting a doctor's prescription, including Eprosartan, Losartan, Valsartan, Irbesartan, Candesartan, Telmisartan, Olmesartan, Azilsartan.

    Additionally, in specialized stores, you can purchase a ready-made combination of sartans with calcium antagonists, diuretics, renin secretion antagonist aliskiren.

    The classification of sartans is carried out according to the effect on the body and chemical composition. The presence or absence of a metabolite in a drug separates it into active substances and prodrugs.

    According to the chemical composition, the division is carried out into 4 groups:

    • biphenyl derivatives of tetrazole (Irbesartan, Candesartan, Losartan);
    • non-biphenyl derivatives of tetrazole as Telmisartan;
    • non-biphenyl netetrazole of the Eprosartan type;
    • non-cyclic compounds in the form .

    Today, this group represents a huge number of drugs that are available with or without a prescription. Therefore, their cost may vary. On average, prices correspond to the price segment of drugs with similar effects.

    Sartans inhibit the development of vascular atherosclerosis

    Atherosclerosis is a process that affects blood vessels and the heart with the development of deadly diseases: heart attack and brain stroke. And death from cardiovascular disease is the main cause of death in old age. Thus, atherosclerosis is the #1 killer of people.

    As a result of atherosclerosis, the vessels are "clogged" with atherosclerotic plaques, which worsens or even completely blocks the blood flow through them. The main cause of atherosclerosis is most likely damage to the integrity of the vascular endothelium due to inflammation, advanced glycation end products, high blood pressure, and possibly high levels of homocysteine.

    Studies have shown that sartans can slow down the development of atherosclerosis. So valsartan can increase the stability of atherosclerotic plaque together with some other drugs.

    Telmisartan suppresses vascular inflammation caused by homocysteine ​​through a binary mechanism involving PPARδ activation and inhibition of NF-kb (nuclear factor "kappa-bi" - a universal transcription factor that controls the expression of immune response genes).

    Telmisartan protects the vessels by modulating vascular endothelial function through the activation of AMPK (5′ adenosine monophosphate-activated protein kinase is an enzyme that plays an important role in cellular energy homeostasis).

    Sartans and treatment of arterial hypertension

    Initially, sartans were developed as a medicine for high blood pressure. Studies have shown that drugs such as Eprosartan and others can lower blood pressure as effectively as the main types of drugs for hypertension.

    Angiotensin-II receptor blockers are taken once a day, these medications smoothly lower blood pressure readings throughout the day.

    The effectiveness of the drugs directly depends on the degree of activity of the renin-angiotensin system. The most effective is the treatment of patients who have a high activity of renin in the blood plasma. To identify these indicators, the patient is prescribed a blood test.

    Eprosartan and other sartans, the prices of which are comparable to similar drugs in terms of the target effect, lower blood pressure for a long period (on average, over 24 hours).

    A persistent therapeutic effect can be seen after two to four weeks of continuous treatment, which is significantly enhanced by the eighth week of therapy.

    Hyperactivity of angiotensin II provokes many types of cancer. And sartans are blockers of angiotensin II receptors (AT1 receptors). Studies have shown the properties of sartans to prevent and sometimes even help treat many types of cancer in patients with high blood pressure.

    Sartans enhance drug delivery in chemotherapy by unpacking tumor vessels. This is important for enhancing the effect of chemotherapy in cancer - especially in pancreatic cancer!!!

    • http://www.ncbi.nlm.nih.gov/pubmed/24717824

    Medication use

    Aprovel is taken as prescribed by a doctor, since its effect is aimed at blocking the effect of angiotensin 2. While taking Aprovel, the concentration of potassium ion in the blood serum is normalized. The hypotensive effect of the drug develops over 1-2 weeks, and the maximum effect is observed within 6 weeks.

    After taking it, the active ingredient is rapidly absorbed from the gastrointestinal tract. A high concentration of irbesartan in plasma occurs in women.

    But scientists did not reveal differences in the value of T1 / 2 and the accumulation of irbesartan. Dosage adjustments are not required for patients.


    Studies have shown that the values ​​of Cmax and AUC of irbesartan are several times higher in patients older than 65 years than in young patients. For elderly patients, the dosage of sartans is not required.

    In patients with impaired renal function and patients undergoing hemodialysis, the pharmacokinetics of irbesartan do not change. The substance is not excreted from the body during hemodialysis.

    Atacand is an antagonist that effectively acts on AT1 receptors. The effectiveness of this medication does not depend on the gender and age of the patient.

    Candesartan is an oral medicine that is excreted from the patient's body in the bile and urine.

    Product effectiveness

    These drugs are combined with almost any drugs to combat AD, but the most effective treatment is seen when taken in conjunction with calcium antagonists or diuretics. Pharmacies sell angiotensin receptor antagonists (ARA or sartans) in combination with hydrochlorothiazides diuretics.

    Such combined preparations meet a number of important requirements:

    • during the use of combined treatment, the effectiveness is markedly increased. This is achieved through the use of various mechanisms and the impact on certain links of pathogenesis;
    • side effects are minimized. This is possible by reducing the dose of various components.

    As you know, in arterial hypertension, the kidneys act as a target organ. Sartans, in turn, help to reduce protein excretion in the urine in people with kidney damage in diabetes mellitus and hypertension.

    Meanwhile, it is important to consider that in the presence of unilateral renal artery stenosis, angiotensin II receptor blockers often increase plasma creatinine levels and cause acute renal failure.

    Due to the fact that the drugs inhibit the reverse absorption of sodium in the proximal tubule, inhibit the synthesis and release of aldosterone, the body gets rid of salt through the urine. This mechanism in turn causes a certain diuretic effect.

    1. Compared with sartans, the use of ACE inhibitors has a side effect in the form of a dry cough. This symptom sometimes becomes so severe that patients have to stop using the medicine.
    2. Sometimes the patient develops angioedema.
    3. Also, specific kidney complications include a sharp decrease in glomerular filtration rate, which causes an increase in potassium and creatinine in the blood. The risk of developing complications is especially high in patients with atherosclerosis of the renal arteries, congestive heart failure, hypotension and a decrease in blood circulation.

    In this case, sartans act as the main drug, which slowly reduces the glomerular filtration rate of the kidneys. Due to this, the amount of creatinine in the blood does not increase. Additionally, the medicine does not allow the development of nephrosclerosis.

    Sartans are medicines for high blood pressure. The main mechanism of their action is the blockade of angiotensin II receptors (AT1 receptors). These receptors bind to the hormone angiotensin II and increase blood pressure, as well as stimulate a number of negative processes in the body that contribute to poor health and shortened life expectancy.

    Sartans are synthetic drugs that block angiotensin receptors.

    With hypertension, the kidneys take over.

    Thanks to sartans, the amount of protein in the urine is reduced in people with kidney disease.

    However, if unilateral stenosis of the renal artery is observed, the plasma creatinine level rises, as a result of which acute renal failure develops.

    The drugs of this group have the ability to inhibit sodium reabsorption, inhibit the release of aldosterone and inhibit synthesis. All this relieves the body of salt. Thus, the diuretic property of medicines is manifested.

    Instructions for use of the drug

    It is known for certain that in patients with severe arterial hypertension, the use of drugs with irbesartan effectively lowers blood pressure as effectively as ACE inhibitor enalapril.

    Doctors recommend taking a combination of antihypertensive drugs immediately before starting therapy, or as soon as possible during it, if patients with cardiovascular disease have systolic blood pressure equal to more than 160 millimeters of mercury.

    The doctor prescribes the medication individually, after a complete examination. The dosage is compiled according to the information that displays the instructions for the use of the drug. It is important to take the medicine every day to avoid missing it.

    The doctor prescribes an angiotensin-II receptor blocker for:

    • heart failure;
    • Postponed myocardial infarction;
    • diabetic nephropathy;
    • Proteinuria, microalbuminuria;
    • Hypertrophy of the left ventricle of the heart;
    • atrial fibrillation;
    • metabolic syndrome;
    • Intolerance to ACE inhibitors.

    According to the instructions for use, unlike ACE inhibitors, sartans do not increase the level of protein in the blood, which often leads to an inflammatory reaction. Due to this, the drug does not have such side effects as angioedema and cough.

    In addition to the fact that Eprosartan and other drugs reduce blood pressure in arterial hypertension, they additionally have a positive effect on other internal organs:

    1. The hypertrophy of the mass of the left ventricle of the heart decreases;
    2. Improves diastolic function;
    3. Reduced ventricular arrhythmia;
    4. Reduced excretion of protein through the urine;
    5. The blood flow in the kidneys increases, while the glomerular filtration rate does not decrease.
    6. Does not affect the levels of sugar, cholesterol and purines in the blood;
    7. Tissue sensitivity to insulin increases, thereby reducing insulin resistance.

    Due to the fact that sartans are a wide variety of drugs with different composition and dosage of the active substance, there is no single instruction for their use.

    Each individual drug is accompanied by an individual instruction that must be followed when using the medication.

    It is extremely important to start taking the medicine only after examining a doctor and conducting appropriate studies. Be sure to take into account the individual characteristics of the patient's body.

    Despite the fact that the side effects characteristic of other groups, sartans cause much less often, research on these agents is ongoing, and recommendations from experts should be carefully considered.

    General indications

    Medical experts prescribe sartans for people who have:

    1. Hypertension, which is the main indicator for their use.
    2. Heart failure, which can develop against the background of overactive activity of the renin-angiotensin-aldosterone system. At an early stage, it allows to normalize cardiac function.
    3. Nephropathy is a dangerous consequence of diabetes, arterial hypertension. With the disease, there is a decrease in the amount of proteins excreted in the urine. Medicines help slow down the development of kidney failure.

    Such drugs do not affect metabolism, bronchial patency, organs of vision. In rare cases, they can cause a dry cough, an increase in potassium levels. The effect of the use of medicines will be visible in a month.

    Sartans for arterial hypertension most often do not cause an adverse reaction, but sometimes patients may notice such problems:

    • dizziness;
    • the appearance of sharp pains in the head;
    • sleep is disturbed;
    • the temperature increases;
    • nausea accompanied by vomiting;
    • constipation or diarrhea;
    • itching occurs.

    Therapy should take place only under the supervision of the attending physician. It is forbidden to take medications during childbearing and breastfeeding, they should not be given to children. With great care, the use of medicines by patients suffering from renal pathology, as well as by elderly people, is allowed.

    The doctor selects the dosage for the patient individually, which is guaranteed to quickly lead to a good result that lasts for a long time.

    The drugs have a therapeutic effect similar to placebo, therefore they have a minimum of side effects and are well tolerated, compared with ACE inhibitors. Sartans do not cause a dry cough, and the risk of angioedema is minimal.

    But it must be taken into account that angiotensin II receptor blockers in some cases are able to quickly reduce blood pressure due to the activity of renin in the blood plasma. With bilateral narrowing of the renal arteries in a patient, the work of the kidneys may be disrupted.

    Sartans are not approved for use during pregnancy, as this adversely affects the development of the fetus.

    Despite the presence of undesirable effects, Eprosartan and other sartans are classified as drugs that are well tolerated and rarely cause adverse reactions in the treatment of high blood pressure. The drug is well combined with other drugs against hypertension, the best therapeutic effect is observed during the additional use of diuretic drugs.

    Sartans are well tolerated, and side effects are much less common than those of analogues according to indications. In this case, the components of the drugs can cause an allergic reaction.

    Sometimes, after taking drugs from the sartans group, dizziness, insomnia, and headache are noted.