ACE inhibitors (ACE inhibitors): mechanism of action, indications, list and choice of drugs. ACE inhibitors - a list of drugs. The mechanism of action of new generation ACE inhibitors and ACE contraindications instructions for use

Angiotensin II is an important hormone that regulates the activity of the cardiovascular system. The advent of angiotensin-converting enzyme (ACE) inhibitors, drugs that reduce its level in the blood, has become a significant breakthrough in the treatment of arterial hypertension (AH). Now drugs that suppress the activity of the renin-angiotensin system occupy a leading position in the fight against the main cause of death - cardiovascular pathology. The first ACE blocker - captopril - was synthesized in 1977. To date, many representatives of this class have been developed, which, according to their chemical structure, are divided into three large groups.

Classification of ACE inhibitors

1. Compounds containing a sulfhydryl group: captopril, fentiapril, pivalopril, zofenopril, alacepril.
2. Drugs with a carboxy group: enalapril, lisinopril, benazepril, quinapril, moexipril, ramipril, spirapril, perindopril, pentopril, cilazapril, trandolapril.
3. Phosphorus-containing compounds: fosinopril.

Many angiotensin-converting enzyme blockers are esters that are 100-1000 times less potent than their active metabolites, but have greater oral bioavailability.

Representatives of this pharmaceutical group differ according to three criteria:

• activity;
• original form: precursor of the active compound (prodrug) or active substance;
• pharmacokinetics (degree of absorption from the digestive system, the effect of food on the bioavailability of the drug, half-life, distribution in tissues, elimination mechanisms).

None of the ACE inhibitors has significant advantages over other representatives of this class: they all effectively suppress the synthesis of angiotensin II from angiotensinI, have similar indications, contraindications and side effects. However, these drugs differ significantly in the nature of distribution in tissues. However, it is not yet known whether this will provide any new benefits.

With the exception of fosinopril and spirapril, which are equally eliminated by the liver and kidneys, angiotensin-converting enzyme blockers are mainly excreted in the urine. Consequently, renal dysfunction reduces the excretion of most of these drugs, and their dose in such patients should be reduced.

List of trade names for ACE inhibitors

1. Captopril: Angiopril®, Blockordil, Kapoten®, Katopil, etc.
2. Enalapril: Bagopril®, Berlipril®, Vasolapril, Invoril®, Corandil, Miopril, Renipril®, Renitek, Ednit®, Enalakor, Enam®, Enap®, Enarenal®, Enafarm, Envipril, etc.
3. Lisinopril: Dapril®, Diropress®, Diroton®, Zonixem®, Irumed®, Lizacard, Lysigamma®, Lisinoton®, Lisiprex®, Lizonorm, Listril®, Liten®, Prinivil, Rileys-Sanovel, Sinopril, etc.
4. Perindopril: Arentopres, Hypernik, Parnavel, Perineva®, Perinpress, Prestarium®, Stoppress, etc.
5. Ramipril: Amprilan®, Vasolong, Dilaprel®, Korpril®, Pyramil®, Ramepress®, Ramigamma, Ramicardia, Tritace®, Hartil®, etc.
6. Quinapril: Accupro®.
7. Zofenopril: Zocardis®.
8. Moexipril: Moex®.
9. Spirapril: Quadropril®.
10. Trandolapril: Gopten®.
11. Cilazapril: Inhibase®, Prilazid.
12. Fosinopril: Monopril®, Fozicard®, Fosinap, Fozinotek, etc.

There are also drugs that are ready-made combinations of ACE inhibitors with diuretics and / or calcium antagonists.

Scope of application

Arterial hypertension

These drugs are widely used as antihypertensive drugs, since they reduce blood pressure in all forms of hypertension, with the exception of primary hyperaldosteronism. Monotherapy with ACE inhibitors normalizes blood pressure in about 50% of patients with mild to moderate hypertension.

Representatives of this class reduce the risk of cardiovascular complications in hypertension to a greater extent compared to other antihypertensive drugs.

Angiotensin-converting enzyme blockers are the drugs of choice for hypertension associated with diabetes mellitus (they inhibit the progression of diabetic nephropathy) and left ventricular hypertrophy. They are also recommended in the combination of hypertension with coronary heart disease.

Heart failure

ACE inhibitors are prescribed for any degree of heart failure, since these drugs prevent or inhibit its development, reduce the likelihood of sudden death and myocardial infarction, and improve quality of life. Treatment is started with small doses, since these patients may experience a sharp drop in blood pressure, especially against the background of a decrease in the mass of circulating blood. In addition, they reduce the dilatation (expansion) of the left ventricle and, to some extent, restore the normal ellipsoid shape of the heart.

myocardial infarction

ACE inhibitors reduce mortality when administered early in myocardial infarction. They are especially effective when combined with hypertension and diabetes. If there are no contraindications (cardiogenic shock, severe arterial hypotension), they should be prescribed immediately in conjunction with thrombolytics (enzymes that destroy an already formed thrombus), antiplatelet agents (aspirin, cardiomagnyl) and β-blockers. Patients at risk (major myocardial infarction, heart failure) should take these drugs for a long time.

Stroke prevention

ACE inhibitors shift the balance between the coagulation and fibrinolytic systems of the blood towards the latter. Scientific studies have shown that they significantly reduce the incidence of heart attack, stroke, mortality in patients with vascular pathology, diabetes mellitus and other risk factors for cerebrovascular accidents.

Chronic renal failure (CRF)

Angiotensin-converting enzyme blockers prevent or slow down kidney damage in diabetes mellitus. They not only prevent diabetic nephropathy, but also inhibit the development of retinopathy in insulin-dependent diabetes mellitus. ACE inhibitors inhibit the progression of chronic renal failure in other renal pathologies, including severe ones.

Side effect

Serious side effects of representatives of this pharmaceutical group are quite rare, they are usually well tolerated.

• Arterial hypotension. The first dose of the drug can lead to a sharp drop in blood pressure in patients with increased plasma renin activity, i.e.:
• with Na + deficiency;
• receiving combined antihypertensive therapy;
• with heart failure.

In such cases, start with very low doses of ACE inhibitors or advise the patient to increase salt intake and cancel diuretic drugs before starting therapy.

• Cough. About 5-20% of patients taking drugs of this pharmaceutical group complain of persistent dry cough. This side effect is usually dose-independent and occurs more frequently in women, usually within 1 week to 6 months of starting treatment. After the abolition of the ACE blocker, the cough disappears on average in 4 days.
• Hyperkalemia. Significant potassium retention is rare in individuals with normally functioning kidneys. However, ACE inhibitors can cause hyperkalemia in patients with renal insufficiency, as well as in those taking potassium-sparing diuretics (amiloride, triamterene, spironolactone), potassium preparations, β-blockers, or non-steroidal anti-inflammatory drugs (NSAIDs).
• Acute renal failure (ARF). Can lead to acute renal failure with narrowing of the renal arteries on both sides, narrowing of the artery of a single kidney, heart failure, or a decrease in the mass of circulating blood due to diarrhea or diuretics. The likelihood of acute renal failure is especially high in elderly patients with heart failure. However, if treatment is started in a timely and correct manner, kidney function is completely normal in almost all patients.
• Impact on the fetus. They do not affect the fetus in the period of organogenesis (I trimester), but their intake in the II and III trimesters can lead to oligohydramnios, underdevelopment of the skull and lungs, intrauterine growth retardation, death of the fetus and newborn. Thus, drugs of this pharmaceutical group are not contraindicated in women of childbearing age, but as soon as it becomes known that a woman is pregnant, angiotensin-converting enzyme inhibitors should be immediately discontinued. If this is done in the first trimester, the risk of negative effects on the fetus is reduced to zero.
• Rash. Members of this group sometimes cause a maculopapular rash, which may be accompanied by itching. It disappears on its own or after a dose reduction of an ACE blocker or a short course of antihistamines (diphenhydramine, suprastin, tavegil, etc.).
• Proteinuria (excretion of protein in the urine). In patients taking drugs of this pharmaceutical group, proteinuria sometimes develops (more than 1 g / day), but it is rather difficult to prove its connection with taking ACE inhibitors. It is believed that proteinuria is not a contraindication to their appointment - on the contrary, these drugs are recommended for certain kidney diseases accompanied by proteinuria (for example, diabetic nephropathy).
• Quincke's edema. In 0.1-0.2% of patients, representatives of this pharmaceutical group cause angioedema. This side effect does not depend on the dose and, as a rule, occurs within a few hours after the first dose. In severe cases, airway obstruction and respiratory problems develop, which can lead to death. When the drug is discontinued, Quincke's edema disappears in a few hours; during this time, measures are taken to maintain airway patency, if necessary, adrenaline, antihistamines and glucocorticosteroids (dexamethasone, hydrocortisone, prednisolone) are administered. Blacks are 4.5 times more likely to have angioedema when taking ACE inhibitors than whites.
• Taste disorders. Patients taking drugs of this pharmaceutical group sometimes note a decrease or loss of taste. This side effect is reversible and is more common with captopril.
• Neutropenia. This is a rare but severe side effect of ACE blockers. It is observed mainly in the combination of hypertension with collagenosis or parenchymal kidney disease. If the serum creatinine concentration is 2 mg or more, the dose should be reduced.
• A very rare and reversible side effect of ACE inhibitors is glucosuria (the presence of sugar in the urine) in the absence of hyperglycemia (high blood sugar). The mechanism is not known.
• Hepatotoxic action. It is also an extremely rare reversible complication. Usually it is manifested by cholestasis (stagnation of bile). The mechanism is not known.

drug interaction

Antacids (maalox, almagel, etc.) reduce the bioavailability of ACE blockers. Capsaicin (an alkaloid of hot pepper varieties) increases the cough caused by drugs in this group. NSAIDs, including aspirin, reduce their antihypertensive effect. Potassium-sparing diuretics and potassium preparations in combination with ACE inhibitors can lead to hyperkalemia. Representatives of this pharmaceutical group increase the serum level of digoxin and lithium and increase the allergic reaction to allopurinol (an anti-gout agent).

An integrated approach is practiced in the treatment of hypertension. Monotherapy is justified only at the initial stages of the development of the disease. One of the first-line drugs are ACE inhibitors - drugs that act directly on adrenal hormones, which provoke an increase in blood pressure due to fluid retention in the body.

ACE inhibitors are drugs that act on the angiotensin-converting enzyme. Under the action of angiotensin, there is an increase in the production of aldesterone, which entails an increase in vascular tone and fluid retention in the body, as a result of which blood pressure rises.

Angiotensin-converting enzyme inhibitors inhibit the synthesis of specific hormones that cause hypertension. To date, drugs of this group are prescribed to almost all patients in the absence of contraindications as a means to control blood pressure.

The mechanism of action of this group of drugs occurs in two stages. One side,

This group of drugs is almost always included in the treatment regimen.

ACE inhibitors affect the synthesis of angiotensin, which increases vascular tone. Angiotensin, in turn, provokes increased production of aldesterone. This hormone is produced by the adrenal glands and causes fluid retention in the body in response to salt intake. Slowing down the production of aldesterone reduces swelling and reduces the pressure of blood on the walls of blood vessels, while a decrease in angiotensin leads to a normalization of the frequency of contractions of the heart muscle and a decrease in vascular tone.

In addition, ACE inhibitors significantly increase the effectiveness of diuretics by reducing the synthesis of the hormone that causes swelling. Thus, they are shown as part of complex therapy for hypertension of degrees 2 and 3, but not as an independent remedy.

The mechanism of action of the latest generation of ACE inhibitors affects the normalization of the cardiovascular system, including the heart itself, and the urinary system. In addition, drugs in this group can reduce the risk of target organ damage when blood pressure rises above 180 mm Hg.

Classification of drugs

ACE inhibitors are divided into synthetic and natural. The drugs used in the treatment of hypertension are synthetic drugs. Natural inhibitors are released as a result of a specific reaction between whey and casein.

ACE inhibitors are divided into three groups, depending on the active substance. Distinguish:

• preparations of the sulfhydryl group;
• drugs of the carboxyl group;
• phosphonate ACE inhibitors.

The mechanism of action of drugs, regardless of the group, is absolutely the same. These drugs are complete analogues of each other, as they have the same effect on the cardiovascular system. The only difference between ACE inhibitors of different groups lies in the mechanism of excretion of the active substance after taking the pill. This must be taken into account when prescribing the drug to patients with renal insufficiency.

Some ACE inhibitors are excreted by the kidneys, others are processed in the liver - this must be taken into account in the pathologies of these organs.

List of drugs of the sulfhydryl group

The list of ACE inhibitor drugs of the sulfhydryl group is quite wide, but the most commonly used:

• captopril;
• benazepril;
• zofenopril.

One of the most popular and used drugs for the treatment of hypertension is captopril. The active substance has the following trade names - Captopril, Kapoten, Bokordil.

A feature of this group of drugs is the absence of a prolonged action. The taken tablet is active for no more than six hours, so the drug is taken 2-3 times a day. Drugs of this group are prescribed for arterial hypertension against the background of coronary heart disease, often combined with diuretics.

The advantage of drugs of the sulfhydryl group is good tolerance by the body. They can be taken with diabetes and heart failure.

The recommended dosage of Captopril is up to 100 mg per day. It is taken an hour before meals, 1 or 2 tablets, depending on the amount of active ingredient in one tablet. When prescribing a drug, it is taken into account that it is excreted by the kidneys, therefore, in case of renal failure, the drug is not prescribed.

Benazepril is taken a maximum of twice a day, since the active substance is released slowly. The recommended regimen is one tablet in the morning and evening at regular intervals.

Zofenopril is also taken two tablets per day. Unlike other drugs of the sulfhydryl group, this medicine has a lower burden on the kidneys, however, in case of renal failure, it can only be used under medical supervision.

Captopril is among the most popular drugs

Drugs of the carboxyl group

ACE inhibitors of the carboxyl group are drugs with the following active ingredients in the composition:

• Quinapril;
• Renitek;
• Ramipril;
• Lisinopril.

The list of drugs in this group is very wide and includes more than 15 active ingredients. All of them have a similar mechanism of action, contraindications and indications for use.

Features of drugs of the carboxyl group:

• prolonged action;
• pronounced vasodilating effect;

Metabolism of the active substance occurs mainly in the liver, which can significantly reduce the burden on the kidneys. Medicines have a pronounced vasodilating effect, due to which there is a rapid decrease in blood pressure. These properties of drugs of the carboxyl group should be taken into account when taken by patients with grade 3 hypertension. In this case, the rapid normalization of blood pressure can adversely affect the work of the heart muscle.

Due to the prolonged action, such drugs are taken 1 time per day. The release of the active substance occurs slowly, which allows for a long and stable therapeutic effect.

It is sufficient to take these preparations once a day.

Phosphinyl group preparations

The third group of ACE inhibitors includes two active substances - fosinopril and ceronapril. These drugs are more likely to control the morning jumps in blood pressure with hypertension, and not for complex treatment. As an independent remedy, preparations of the phosphinyl group are not effective enough.

The peculiarity of the drugs is a prolonged action, which allows you to control the level of blood pressure even during a night's rest. The metabolism of these drugs is carried out simultaneously in the kidneys and the liver, which makes it possible to prescribe the drug in case of impaired renal function in older patients.

Another feature is a convenient reception scheme. It is enough to take the drug only once a day in the morning to ensure a stable therapeutic effect.

Combination drugs of a new generation

The drugs of the third group belong to a new generation of drugs for hypertension, along with combined drugs.

Their advantages:

• prolonged action;
• ease of use;
• good tolerance;
• complex action.

Due to the peculiarities of the metabolism of the active substance, new generation drugs can be used to treat patients with renal insufficiency and diabetes mellitus. This is very important, since hypertension is diagnosed mainly at an older age against the background of concomitant chronic diseases.

Combined drugs can be taken by hypertensive patients with diabetes mellitus

Combination drugs include drugs containing calcium channel blockers and ACE inhibitors, or diuretics and ACE inhibitors. Such drugs are very convenient in that you can take just one drug to control blood pressure.

ACE inhibitor and diuretic combination:

• Caposide;
• Ramazid N;
• Fosicard N.

Such drugs have a more pronounced hypotensive effect, while they can be used as monotherapy for hypertension of 1 and 2 degrees. In addition, they are convenient to take - just 1 tablet per day to ensure a stable therapeutic effect throughout the day.

At an older age, there is a violation of the elasticity of large arteries. This is due to physiological changes against the background of constantly elevated pressure. When the vessels lose their flexibility and their permeability is impaired, treatment is carried out with combined drugs that contain an ACE inhibitor and a calcium antagonist. The list of such funds:

• Triapin;
• Tarka;
• Aegipres;
• Koripren.

In most cases, Koripren is prescribed. It is advisable to use such drugs for the treatment of hypertension when other drugs, including ACE inhibitors as an independent agent, are ineffective. They are usually prescribed to patients over 65 years of age with an increased risk of thrombosis and myocardial infarction.

Features of use in hypertension

ACE inhibitors are prescribed mainly for hypertension. However, this is not the only scope of this group of drugs.

A feature of drugs of the ACE inhibitor group is a positive effect on target organs. Taking these drugs helps to minimize the risk of developing dangerous consequences, such as stroke or myocardial infarction.

With hypertension of the 1st degree, there is a steady, but slight increase in blood pressure, not higher than 140 mm Hg. If the disease develops against the background of any chronic diseases and the cardiologist has reason to believe that the disease will progress rapidly, ACE inhibitors are prescribed as monotherapy. The combination of drugs in this group with a diet, giving up bad habits and normalizing the daily regimen, allows you to achieve a steady decrease in blood pressure in half of the patients taking the medicine.

Hypertension of the 2nd degree is characterized by a steady increase in blood pressure up to 160 mm Hg. and higher. This increases the risk of damage to any organ. Usually, vision suffers first (angiopathy develops) or kidneys. With such pressure, diet therapy and load reduction are no longer enough, it is necessary to take medication. In this case, ACE inhibitors have two goals - to achieve a stable decrease in pressure and to avoid the development of complications. Usually, complex therapy is used, including a diuretic, calcium antagonists and ACE inhibitors. Timely treatment allows to achieve a stable hypotensive effect in 70% of cases and prevent the development of dangerous complications.

With grade 3 hypertension, blood pressure rises above 160 mm Hg. The use of diuretics and calcium antagonists as monotherapy shows poor results, therefore, new generation combined agents are used for treatment. The danger of hypertension of the 3rd degree is the development of hypertensive crises, disruption of the work of two or more target organs (heart, kidneys, brain, organs of vision). Usually, severe hypertension occurs against the background of diabetes mellitus, vascular atherosclerosis, or other chronic diseases. In this case, it is necessary to take drugs for life.

In the initial stages of hypertension, ACE inhibitors are taken as the main drug, in later stages - as part of complex therapy.

Use in heart failure

Among the indications for the use of ACE inhibitors is any form of heart failure. The drugs in this group help:

• Avoid disease progression
• Reduce the load on blood vessels and the heart;
• Prevent the development of myocardial infarction.

The use of ACE inhibitors in patients with heart failure reduced the risk of sudden death due to cardiac arrest by 2.5 times. In addition, according to the patients themselves, drugs in this group significantly improve the quality of life with this diagnosis.

With heart failure, drugs begin to be taken with caution. At the beginning of treatment, reduced dosages are indicated, no more than ¼ of the recommended amount given in the instructions. Such a precautionary measure is due to the risk of a sudden drop in blood pressure to critical values. As the body gets used to the drug, the dosage gradually increases, eventually reaching the recommended one.

In addition, drugs of this group can be used during the recovery period after myocardial infarction.

ACE inhibitors in renal failure

In kidney failure, ACE inhibitors help slow down the progression of the disease. They are prescribed, including in case of impaired renal function against the background of diabetes mellitus. It is important to select a drug taking into account its metabolism and excretion from the body. For the treatment and control of kidney function, drugs should be selected, the metabolism of which is carried out in the liver. This is an important condition for achieving a sustainable therapeutic effect.

With kidney damage, drugs are selected that are excreted by the liver

Contraindications

Only a doctor should prescribe drugs of the ACE inhibitor group, after collecting an anamnesis and a detailed examination of the patient. Before taking the drug, the patient is advised to read the instructions for the drug again. The following diseases and conditions are contraindications:

• Rheumatoid arthritis;
• Lupus erythematosus;
• Pregnancy;
• lactation period.

ACE inhibitors should not be taken in case of individual intolerance. Special instructions may vary, depending on the specific drug, so it is important to carefully study the instructions.

Taking this group of drugs during pregnancy can cause fetal malformations that are incompatible with life.

Taking ACE inhibitors with hypotension is categorically contraindicated, otherwise there is a risk of developing coma due to a decrease in blood pressure to critical values.

Side effects

If the medicine is chosen correctly, the patient follows the doctor's recommendations and does not exceed dosages, the development of side effects is unlikely, since the drugs of the ACE inhibitor group are well tolerated by the body.

Nevertheless, with hypersensitivity and violation of the regimen, the development of undesirable phenomena is possible:

• hypotension;
• dry cough, difficult to treat;
• potassium retention in the body (hyperkalemia);
• the formation of protein compounds in the urine;
• impaired renal function;
• excretion of glucose into the urine;
• allergic rash and angioedema.

The most common side effect is a persistent cough.

The most common dry cough when taking drugs in this group. This side effect occurs in about 1/5 of patients taking ACE inhibitors to control blood pressure. It is difficult to get rid of a cough with the help of special drugs, but it goes away on its own within a few days after the withdrawal of ACE inhibitors.

With individual intolerance to the drug, a severe allergic reaction and Quincke's edema may develop. Such complications are very rare, but they pose a serious danger not only to health, but also to the life of the patient.

With a decrease in blood pressure to dangerous values ​​​​and the development of hypotension, it is necessary to consult a doctor about changing the regimen of taking the drug or reducing the dosage. Usually this phenomenon is observed when taking too large doses of the drug against the background of heart failure.

As a rule, all complications when taking ACE inhibitors are reversible, or disappear on their own after discontinuation of the drug. However, it is recommended that you tell your doctor about any change in how you feel after starting a new medication.

Drug Interactions

Drugs used to treat gastritis and heartburn, which have an enveloping effect (Maalox, Gaviscon), significantly reduce the absorption of inhibitors by the stomach, which reduces their bioavailability and therapeutic effect. With the simultaneous use of ACE inhibitors with such drugs, it may be necessary to adjust the regimen for taking antihypertensive drugs.

The hypertensive effect of ACE inhibitors decreases when taken simultaneously with non-steroidal anti-inflammatory drugs (Ibuprofen, Nimesulide, Diclofenac). Simultaneous administration of acetylsalicylic acid and ACE inhibitors reduces the effectiveness of the latter.

For a complete list of drug interactions and important warnings, please refer to the prescribing information for the medicinal product, which should be read carefully before starting treatment.

If you need to increase or decrease the dosage of the medication you take, you should contact your cardiologist, but do not try to change the treatment regimen yourself. It is important to remember that any drugs for the treatment of hypertension, if taken incorrectly, can lead to irreversible consequences, so you should trust your doctor, but do not try to treat the disease yourself.

One of the most common pathologies among the elderly is hypertension. In most cases, it provokes oligopeptide angiotensin.

To eliminate its negative effects on the body, new generation inhibitors are used - angiotensin-converting enzymes. These drugs are being improved every year.

The new generation differ from the previously created dosage forms (more than 35–40 years ago) in their effectiveness.

This issue is not often discussed. Nevertheless, three generations of effective drugs for the treatment of hypertension in patients can be distinguished. The first generation of tools of this kind was created in 1984.

Studies were carried out in the USA. , Zofenopril was already successfully used at that time. Moreover, the appointment was made at the beginning of those patients who had hypertension of the third, fourth degree.

Later, second-generation inhibitors appeared - they are also new drugs for hypertension. Unlike the first, they show their effect on the patient within 36 hours. These include: Perindopril, Enalapril, Moexipril, Trandolapril and others.

The third generation of effective pressure tablets is represented by Fosinopril. The newest drug is prescribed, acute heart attack. It is effective in diabetes mellitus, kidney disease.

Choose a drug for the treatment of hypertension according to the clinical picture, and not according to its belonging to a particular generation.

ACE inhibitors - a list of new generation drugs

Remedies for high blood pressure appeared almost in the 2000s. They have a complex effect on the patient's body as a whole. The effect occurs due to the impact on metabolic processes in which calcium is present. It is the ACE drugs of the new generation that do not allow calcium compounds to penetrate into the vessels, the heart. Due to this, the body's need for excess oxygen is reduced, the pressure is normalized.

Last generation inhibitor Losartan

ACE inhibitors of the latest generation, list:

• Losartan, Telmisartan, Rasilez;
• Cardosal, Benazepril;
• Fosinopril, Moexpril, Ramipril;
• Trandolapril, Cardosal, Lisinopril;
• Quinapril, Perindopril, Eprosartan;
• Lisinoproil, Dapril,;
• Zofenopril, Fosinopril.

Using inhibitors for a long period, patients will not experience side effects if the dose of the drug is not exceeded. Patients will experience an improvement in their quality of life. In addition to lowering pressure, there is a normalization of the work of the heart muscle, blood circulation in the vessels, cerebral arteries. The likelihood of developing arrhythmias is blocked.

If you have hypertension, then do not choose your own drugs. Otherwise, you can only worsen your condition.

Latest Generation ACE Inhibitors: Benefits

Comprehensive treatment should be used to reduce deaths. Including inhibitors of angiotensin-converting enzymes.

Thanks to the new inhibitors, you will experience a number of advantages over the outdated hypertension pills:

1. minimum side effects, improve the patient's condition;
2. the effect of the pills is quite long, not the same as that of drugs for pressure forty years ago. In addition, they have a positive effect on the work of the heart, vascular system, kidneys;
3. contribute to the improvement of the nervous system;
4. tablets act purposefully, without affecting other organs. Therefore, older people do not experience any complications;
5. have a beneficial effect on the psyche, prevent depressive states;
6. normalize the size of the left ventricle;
7. do not affect the physical, sexual, emotional state of the patient;
8. for diseases of the bronchi, just such drugs are recommended, they do not cause complications;
9. have a positive effect on kidney function. Normalize metabolic processes in which uric acid and lipids are involved.

New inhibitors are indicated for diabetes, pregnancy. (Nifedipine, Isradipine, Felodipine) is not recommended for patients after a stroke and with heart failure.

Beta-blockers can also be used in the above patients with a stroke, etc. These include: Acebutalol, Sotalol, Propanolol.

New inhibitors come in different groups - it all depends on the components that make up the composition. Accordingly, it is necessary for the patient to select them depending on the general condition and the active substance in the tablets.

Side effects

New drugs of this series minimize the impact of side effects on the state of the patient's body as a whole. And yet, the negative impact is felt, which requires the replacement of the dosage form with other tablets.

15-20% of patients have the following side effects:

• manifestation of cough due to the accumulation of bradykinin. In this case, ACE is replaced by ARA-2 (angiotensin receptor blockers - 2);
• violation of the gastrointestinal tract, liver function - in rare cases;
• hyperkalemia is an excess of potassium in the body. Such symptoms occur with the combined use of ACE with loop diuretics. With a single use of the recommended doses, hyperkalemia does not appear;
• treatment of hypertension and heart failure with maximum doses of ACE inhibitors leads to renal failure. Most often, the phenomenon is observed in patients with previously existing kidney lesions;
• when self-prescribing remedies for pressure, sometimes, very rarely, allergic reactions occur. It is better to start using in a hospital, under the supervision of specialists;
• a persistent decrease in pressure (hypotension) of the first dose - manifests itself in patients with initially low pressure and in those patients who do not control the readings of the tonometer, but drink pills to reduce it. And they themselves prescribe the maximum dose.

High blood pressure drugs are used not only for the treatment of cardiac pathologies, they are also used in endocrinology, neurology, and nephrology. Young people are especially susceptible to ACE inhibitors. Their body quickly responds to the effects of the active components of these funds.

Contraindications for use

With caution, pressure pills are prescribed to pregnant women after undergoing a medical examination. And they are taken under the supervision of the attending physician if other treatment is ineffective.

Drugs are contraindicated in patients who do not tolerate the active component of a particular drug.

Because of this, allergies can develop. Or worse, angioedema.

It is not recommended to use tablets for hypertension in patients who are not yet eighteen years old. Do not use inhibitors for people with anemia and other blood diseases. They can also include leukopenia. This is a dangerous disease characterized by a decrease in the number of leukocytes in the blood.

With porphyria, there is an increased content of porphyrins in the blood. Most often occurs in children who are born in a marriage union from parents who initially have close family ties.

Carefully study the instructions for the ACE inhibitor before use, especially contraindications and dosage.

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About the treatment of hypertension with new generation drugs:

If high blood pressure does not appear often, then you should start drinking ACE tablets under the supervision of a specialist doctor with small dosages. If there is slight dizziness at the beginning of the use of inhibitors, then take the first dosage before going to bed. Don't get out of bed abruptly in the morning. In the future, your condition will normalize and the pressure too.

ACE inhibitors (from Latin APF, ACE inhibitors, or angiotensin-converting enzyme inhibitors) are an extensive group of medicines that block a chemical that affects the narrowing of the walls of blood vessels and an increase in blood pressure.

The use of inhibitors occurs in pathologies of the vascular and cardiac systems, most often in hypertension.

Today, drugs in this group are the most common and affordable, in terms of pricing, drugs that resist high blood pressure.

IAPF, what is it?

Human kidneys produce a certain enzyme called renin. It is from him that a series of chemical reactions starts, which lead to the formation of another element in the blood plasma and tissues, called angiotensin-converting enzyme.

The identical name of the latter is angiotensin - it is he who stores the property of narrowing the walls of blood vessels, thereby increasing the speed of blood flow and blood pressure.

Along with this, the growth of its indicators in the blood leads to the production of various hormones by the adrenal glands that retain sodium in the tissues, which increases the narrowing of the vascular walls, which increases the number of heart contractions and increases the volume of fluid inside the human body.

During the course of the above processes, a vicious circle of chemical reactions is formed, which leads to sustained high pressure and damage to the walls of blood vessels. Such processes ultimately lead to the progression of chronic kidney and heart failure.

It is drugs from the group of ACE inhibitors that help break the vicious chain by blocking processes at the stage of the angiotensin-converting enzyme.

The inhibitor contributes to the accumulation of a substance such as bradykinin, which prevents the progression of pathological reactions in cells in case of kidney and heart failure (rapid division, development and necrosis of cells of the heart muscle, kidneys and vessel walls).

Due to their properties, ACE inhibitors are treated not only for hypertension, but also used for preventive purposes, to prevent the death of heart muscle tissue, stroke, and heart and kidney failure.

Also, the drugs help to improve the metabolism of lipids and carbohydrates, which allows them to be used quite successfully in diabetes mellitus, elderly people with lesions of other organs.

Modern ACE inhibitors are among the most effective drugs in the fight against hypertension. Unlike other vasodilating drugs, they prevent vasoconstriction and have a milder effect.

New generation inhibitors are perfectly combined with drugs from other groups, improve blood circulation in the coronary arteries and normalize metabolic processes.

Self-medication can lead to complications.

Classification of ACE inhibitors by generation

Classification of drugs in this group is based on several factors.

The primary division into subspecies occurs according to the initial substance that is part of the drug (the main role is played by the active part of the molecule, which ensures the duration of the effect on the body).

This is what helps during the appointment to correctly calculate the dose and accurately identify the period of time after which you need to re-take the medicine.

Comparative characteristics by generation of ACE inhibitors are shown in the table below.

Active group of molecules	Name	Characteristic
First generation (sulfhydryl group)	captopril, pivalopril, zofenopril	The mechanism of action of this group is manifested in an increase in the action of ACE inhibitors, but it is quite simply oxidized, which allows it to act for a short period of time.
Second generation (carboxyl group)	Perindopril, Enalapril, Lisinopril	They are characterized by an average time of action, but they are characterized by high permeability in the tissue
Latest generation (phosphinyl group)	Fosinopril, Ceronapril	The drugs are long-acting and have a high rate of permeability in tissues and further accumulation in them.

The mechanism for converting a chemical into an active agent also helps classify ACE inhibitors into subgroups.

ACE inhibitor	Drug activity
First class drugs (Captopril)	Dissolved by fats, getting into the human body in an active form, converted into the liver cavities and excreted in an altered form, and perfectly pass through cell barriers
Second class drugs (Fosinopril)	They dissolve with fats, are activated during chemical processes in the cavities of the liver or kidneys and are excreted in an altered form. Perfectly absorbed through cell barriers
Third class drugs (Lisinopril, Ceronapril)	They are dissolved in water, when ingested, they occur in an active form, they are not converted in the liver, they are excreted intact. Pass through cell barriers more poorly

The final classification occurs according to the methods of excretion of their body.

There are several different methods:

• Excretion occurs, for the most part, by the liver (about sixty percent). An example of such a drug is Trandolapril;
• Excretion occurs by the kidneys. Examples of such ACE inhibitors are Lisinopril and Captopril;
• Excretion occurs, for the most part, by the kidneys (about sixty percent). Examples of such drugs are Enalapril and Perindopril;
• Excretion occurs with the help of the kidneys and liver. Examples are Fosinopril and Ramipril.

This classification helps to select the most appropriate ACE inhibitor for people suffering from severe pathologies of the liver or kidney system.

Due to the fact that the generation and class of ACE inhibitor may vary, drugs from the same series may have slightly different mechanisms of action.

Most often, in the instructions for use, which contains all the necessary information about the drug, its mechanism of action is indicated.

What is the mechanism of action in different diseases?

The mechanism of action of ACE inhibitors in hypertension

Medications prevent the transformation of angiotensin, which has a clear vasoconstriction effect. The action diverges on the enzymes of plasma and tissues, which has a mild and lasting result of lowering the pressure. This is the main mechanism of action of ACE inhibitors.

Mechanism of action in kidney failure

The drugs block the production of adrenal enzymes that retain sodium and fluid in the body.

ACE inhibitors help to reduce swelling, restore the walls of the vessels of the renal glomeruli, reduce pressure in them and clear the protein in the kidneys.

Mechanism of action in case of insufficiency of the heart and blood vessels, ischemia, stroke, tissue death of the heart muscle

Since, thanks to ACE inhibitors, angiotensin decreases, the amount of bradykinin increases, which prevents the pathological progression of myocardial cells and vascular walls due to a lack of oxygen in the heart.

Regular use of ACE inhibitors significantly slows down the process of increasing the thickness of the heart muscle and blood vessels, increasing the size of the heart chambers, which are manifested due to hypertension.

Mechanism of action of ACE inhibitors in chronic heart failure

Mechanism of action in atherosclerotic deposits and high blood clotting

Since ACE inhibitors release nitric oxide into the blood plasma, platelet adhesion is provoked and the fibrin index (protein that is involved in the formation of blood clots) is restored.

Medicines have the ability to suppress the production of adrenal hormones that increase the level of "negative" cholesterol in the blood, which gives them anti-sclerotic properties.

Indications for the use of ACE inhibitors

Inhibition has been used in medicine for over thirty years. Their active distribution in the post-Soviet territory began in the 2000s. Characteristically, since that time, ACE inhibitors have taken a leading position among all pressure-lowering drugs.

The main indication for the use of the latest generation of inhibitors is hypertension, and the main advantage is an effective reduction in the risk of progression of burdens of the heart and blood vessels.

Medicines of this group are used to treat the following diseases:

• Prolonged and persistent high blood pressure;
• With symptoms of high blood pressure;
• With high blood pressure, which is accompanied by diabetes;
• Violation of metabolic processes;
• Ischemic lesions;
• Obliterating atherosclerosis of the extremities;
• High blood pressure with heart failure provoked by blood stasis;
• Pathologists of the kidneys, which are accompanied by an increase in pressure;
• Post-stroke state with high blood pressure;
• Atherosclerotic deposits in the carotid artery;
• The death of cardiac muscle tissues of an acute nature after normalization of pressure, or a post-infarction condition, when the ejection of blood from the left ventricle is less than forty percent, or there are signs of systole dysfunction, manifested against the background of the death of cardiac muscle tissues;
• obstructive bronchial disease;
• Left ventricular dysfunction of a systolic nature, without taking into account blood pressure levels and fixation, or the absence of clinical signs of heart failure;
• Atrial fibrillation.

Long-term use of ACE inhibitors entails a significant reduction in the risk of complications in cerebrovascular pathologies, death of heart muscle tissue, heart failure and diabetes.

This is what sets them apart more favorably from drugs such as calcium antagonists and diuretics.

With prolonged use as the only treatment, replacing beta-blockers and diuretics, ACE inhibitors are recommended for the following groups of patients:

• Patients with diagnosed type 2 diabetes;
• People with predisposition to diabetes;
• Patients in whom a beta-blocker or diuretic caused side effects or did not have the desired effect.

When using ACE inhibitors as the only therapeutic drug, efficacy is noted in the first two stages of hypertension and in most young patients.

The effectiveness of such therapy is about fifty percent, which necessitates the parallel use of beta-blockers, diuretics, or calcium antagonists.

Complex therapy is used in the third stage of hypertension and in elderly people with concomitant pathologies.

In order to prevent pressure surges from very low to extremely high, the use of the drug is distributed during the day.

Doctors do not advise using extremely large doses of ACE inhibitors, as the risk of progression of side effects increases and the tolerability of treatment decreases.

If moderate doses of ACE inhibitors are not effective, the best course of action is to add a diuretic or calcium antagonist to the treatment.

Contraindications for ACE inhibitors

Complications can progress directly to the development of the embryo: miscarriage, death inside the womb, congenital malformations. Also, it is not recommended to use ACE inhibitors while breastfeeding.

ACE inhibitors are contraindicated in patients with the following factors, which are listed in the table below.

Contraindications for the use of ACE inhibitors in the presence of pathologies	Factors under which ACE inhibitors are not prescribed
Severe narrowing of the aorta	The period of pregnancy and breastfeeding
Narrowing of both renal arteries	Individual intolerance to the hotel components of the drug
Elevated levels of potassium in the blood	Children's age group
Leukopenia	Atherosclerotic lesions of the coronary arteries of the lower extremities
The indicator of systolic pressure is less than one hundred mm Hg.	Use of Allopurinol, Indomethacin and Rifampicin
Death of liver tissue
Hepatitis in active form

Side effects of ACE inhibitors

ACE inhibitors provoke side effects in especially rare cases.

The most common side effects are shown in the table below.

Side effect	Characteristic
Kidney dysfunction	There is an increase in creatinine in the blood, sugar in the urine, there may be acute kidney failure (in old age, with heart failure, the kidneys may fail altogether)
allergic reactions	There is a rash, urticaria, redness, scabies, swelling
Dry cough	Regardless of dosage, dry cough is noted in twenty percent of patients.
Low pressure	Inherent weakening, lethargy, lowering of blood pressure levels, regulated by lowering the dosage of ACE inhibitors and discontinuation of diuretics
Impact on the liver	Stagnation of bile in the cavity of the gallbladder progresses
Change in taste indicators	There is a violation of sensitivity, or a complete loss of taste
Violations of blood parameters	There is an increase in the number of neutrophils
Dyspepsia	Nausea, gag reflex, diarrhea
Deviations in the balance of electrolytes	An increase in potassium levels, with the use of diuretics and potassium-sparing

What drugs are inhibitors?

The list of ACE inhibitor drugs is widely known to a large number of patients. Some patients are indicated to take one drug, while others require combination therapy.

Before the appointment of ACE inhibitors, a detailed diagnosis and assessment of the risk of progression of complications is carried out. In the absence of risks and the need to use drugs, a course of therapy is prescribed.

The dose is determined individually by trial. It all starts with a small dose, after which it is displayed to the average. At the start of use, and at the entire stage of adjusting the course of treatment, it is necessary to monitor blood pressure indicators until its indicators normalize.

ACE inhibitors Zocardis

ACE inhibitors list of drugs and analogues

The list is shown in the table below, and includes the most common drugs and their analogues.

generation of ACE inhibitors	Name	Similar drugs
First generation	Zofenopril
	Captopril	Kapoten, Angiopril, Katopil
	Benazepril	benzapril
Second generation		Irumed, Diroton, Dapril, Prinivil
	Ramipril	Hartil, Capril, Dilaprel, Vasolong
	Enalapril	Enap, Renitek, Renipril, Vasolapril, Invoril
	Perindopril	Stoppress, Parnavel, Hypernik, Prestarium
	Cilazapril	Inhibeis, Prylazid
	Quinapril	Accupro
	Trandolapril	Gopten
	Spirapril	Quadropril
	Moexipril	Moex
third generation	Ceronapril
	Fosinopril	Fosicard, Monopril, Fosinap

Natural ACE Inhibitors

Drugs from the ACE inhibitor group, of natural origin, have been identified in the study of peptides that are concentrated in the venom of zhararaki. These drugs act as coordinators that limit the processes of strong cell elongation.

Arterial pressure is reduced by reducing peripheral resistance to the walls of blood vessels.

Natural ACE inhibitors enter the human body along with dairy products.

In small amounts, they can be concentrated in whey, garlic and hibiscus.

How to use an ACE inhibitor?

Before using any drugs from the group of ACE inhibitors, you should consult with your doctor. In most cases, ACE inhibitors are taken sixty minutes before a meal.

Doses and frequency of use, as well as the interval between taking tablets, should be determined by a qualified specialist.

When treating with inhibitors, it is necessary to eliminate non-steroidal anti-inflammatory drugs (Nurofen), salt substitutes and products that are saturated with potassium.

Conclusion

Drugs from the group of ACE inhibitors are the most common means for resisting hypertension, but can also be used to treat other diseases. A wide range of drugs allows you to choose the remedy individually for each patient.

In addition to the fact that the drugs effectively resist hypertension, they have a number of side effects. That is why it is not recommended to use ACE inhibitors only after consulting with your doctor.

Do not self-medicate and be healthy!

To prevent its influence, the therapy regimen should include drugs that inhibit the action of the hormone. Such agents are angiotensin-converting enzyme inhibitors.

What is APF

Angiotensin-converting enzyme (ACE) inhibitors are a group of natural and synthetic chemical compounds, the use of which has helped to achieve great success in the treatment of patients with cardiovascular pathologies. APF has been used for over 40 years. The very first drug was captopril. Next, lisinopril and enalapril were synthesized, which were replaced by new generation inhibitors. In cardiology, ACE drugs are used as the main agents that have a vasoconstrictive effect.

The benefit of inhibitors is the long-term blocking of the hormone angiotensin II - the main factor that affects the increase in blood pressure. In addition, angiotensin-converting enzyme agents prevent the breakdown of bradykinin, help reduce the resistance of efferent arterioles, release nitric oxide, and increase vasodilating prostaglandin I2 (prostacyclin).

New generation ACE drugs

In the pharmacological group of ACE drugs, repeated-dose drugs (enalapril) are considered obsolete, because. they do not provide the necessary compliance. But at the same time, Enalapril remains the most popular remedy that demonstrates excellent efficacy in the treatment of hypertension. In addition, there is no confirmed evidence that the latest generation of ACE blockers (Perindopril, Fosinopril, Ramipril, Zofenopril, Lisinopril) have more advantages over inhibitors released 40 years ago.

What drugs are ACE inhibitors

Vasodilating powerful angiotensin-converting enzyme agents in cardiology are often used to treat arterial hypertension. Comparative characteristics and list of ACE inhibitors, which are the most popular among patients:

1. Enalapril

• An indirect cardioprotector quickly lowers blood pressure (diastolic, systolic) and reduces the load on the heart.
• Acts up to 6 hours, excreted by the kidneys.
• Rarely may cause visual impairment.
• Price - 200 rubles.

1. Captopril

• Short term remedy.
• Well stabilizes the pressure, but the drug requires multiple doses. The dosage can only be set by a doctor.
• Has antioxidant activity.
• Rarely can provoke tachycardia.
• Price - 250 rubles.

1. Lisinopril

• The drug has a long duration of action.
• It works independently, it does not need to be metabolized in the liver. Excreted through the kidneys.
• The medicine is suitable for all patients, even those who are obese.
• May be used in patients with chronic kidney disease.
• May cause headache, ataxia, drowsiness, tremor.
• The cost of the drug is 200 rubles.

1. Lotensin

• Helps reduce pressure.
• It has vasodilating activity. Leads to a decrease in bradykinin.
• Contraindicated for lactating and pregnant women.
• Rarely, it can cause vomiting, nausea, diarrhea.
• The cost of the medicine is within 100 rubles.

1. Monopril.

• Slows down the metabolism of bradykinin. The volume of circulating blood does not change.
• The effect is achieved after three hours. The drug is usually not addictive.
• With caution, the remedy should be taken by patients with chronic kidney disease.
• Price - 500 rubles.

1. Ramipril.

• The cardioprotector produces ramiprilat.
• Reduces total vascular peripheral resistance.
• Use is contraindicated in the presence of significant hemodynamically arterial stenosis.
• The cost of funds - 350 rubles.

1. Accupril.

• Helps reduce pressure.
• Eliminates resistance in the pulmonary vessels.
• Rarely, the drug can cause vestibular disorders and loss of taste.
• The price is an average of 200 rubles.

1. Perindopril.

• Helps to form an active metabolite in the body.
• Maximum efficiency is achieved within 3 hours after use.
• Rarely, it can cause diarrhea, nausea, dry mouth.
• The average cost of a medicine in Russia is about 430 rubles.

1. Trandolapril.

• With prolonged use reduces the severity of myocardial hypertrophy.
• Overdose can cause severe hypotension and angioedema.
• Price - 500 rubles.

Quinapril.

• Influences the renin-angiotensin system.
• Significantly reduces the load on the heart.
• Rarely can cause allergic reactions.
• Price - 360 rubles.

Classification of ACE inhibitors

There are several ACE inhibitor classifications based on a chemical group in the molecule that interacts with the ACE center; route of excretion from the body; action activity. Based on the nature of the group that binds to the zinc atom, inhibitors are divided into 3 categories. In modern medicine, the chemical ACE inhibitor classification of drugs containing:

• a sulfhydryl group;
• carboxyl group (dicarboxylate-containing preparations);
• phosphinyl group (phosphonate-containing drugs);
• group of natural compounds.

Sulfhydryl group

With the help of specific reagents, sulfhydryl groups of enzymes cause complete or partial inhibition of the activity of various enzymes. Means of this group are calcium antagonists. List of the most famous means of the sulfhydryl group of enzymes:

• Benazepril (Potensin);
• Captopril (Epsitron, Kapoten, Alkadil);
• Zofenopril (Zocardis).

ACE inhibitors with a carboxyl group

The functional monovalent carboxyl group has a positive effect on the life of patients with hypertension. As a rule, dicarboxylate-containing preparations are used only once a day. You can not use such funds for coronary heart disease, diabetes, renal failure. The list of the most famous dicarboxylate-containing drugs:

• Perindopril (Prestarium);
• Enalapril (Enap, Edith, Enam, Renipril, Berlipril, Renitek);
• Lisinopril (Diroton, Lisinoton);
• Ramipril (Tritace, Hartil, Amprilan);
• Spirapril (Quadropril);
• Quinapril;
• Trandolapril;
• Cilazapril.

Phosphonate-containing preparations

The phosphinyl group binds to the zinc ion in the active site of ACE, while inhibiting its activity. Such agents are used to treat kidney failure and hypertension. Phosphonate-containing ACE preparations are generally considered to be a new generation of drugs. They have a high ability to penetrate tissues, so the pressure stabilizes for a long period. The most popular ACE drugs in this group:

Natural ACE Inhibitors

ACE preparations of natural origin were discovered by studying the peptides that are contained in the venom of zhararaki. Such agents act as a kind of coordinators that limit the processes of strong cell elongation. Pressure decreases due to a decrease in peripheral vascular resistance. Natural ACE inhibitors that are ingested with dairy products are called lactokinins and casokinins. In small quantities, they can be found in garlic, hibiscus, whey.

ACE inhibitors - indications for use

Means with angiotensin-converting enzymes are used even in plastic surgery. But, as a rule, they are more often prescribed to patients to lower blood pressure and to those patients who have disorders in the activity of the cardiovascular system (for the treatment of arterial hypertension). It is not recommended to use drugs on your own, since these drugs have many side effects and contraindications. The main indications for the use of ACE inhibitors:

• diabetic nephropathy;
• LV dysfunction (left ventricle) of the heart;
• atherosclerosis of the carotid arteries;
• transferred myocardial infarction;
• diabetes;
• microalbuminuria;
• obstructive bronchial disease;
• atrial fibrillation;
• high activity of the renin-angiotensive system;
• metabolic syndrome.

ACE inhibitors for hypertension

ACE drugs block the angiotensin-converting enzyme. These modern medicines have positive effects on human health by protecting the kidneys and heart. In addition, ACE inhibitors have been widely used in diabetes mellitus. These drugs increase the sensitivity of cells to insulin, improve the absorption of glucose. As a rule, all drugs for hypertension should be taken only once a day. List of drugs used in hypertension:

• Moexzhril;
• lozzhopril (diroton, lysoril);
• Ramipril (tritace);
• Talinolol (beta-blocker);
• Physinopril;
• Cilazapril.

ACE inhibitors in heart failure

Often the treatment of chronic heart failure involves the use of inhibitors. This group of cardioprotectors in tissues and blood plasma prevents the conversion of inactive angiotensin I into active angiotensin II, thereby preventing its adverse effects on the heart, kidneys, peripheral vascular bed, and neurohumoral status. List of cardioprotective drugs that are allowed to take in heart failure:

• Enalapril;
• Captopril;
• antianginal agent Verapamil;
• Lisinopril;
• Trandolapril.

ACE inhibitors in renal failure

For a long time it was believed that inhibitors have a bad effect on the functioning of the kidneys and therefore they were contraindicated even at the initial stage of renal failure. Today, these funds, on the contrary, are prescribed to patients for the treatment of impaired renal function along with diuretics. Angiotensin-converting enzyme preparations reduce proteinuria and improve overall kidney health. You can take the following ACE inhibitors for CKD:

ACE inhibitors - mechanism of action

The mechanism of action of ACE inhibitors is to reduce the activity of angiotensin-converting enzyme, which accelerates the transition of biologically inactive angiotensin I to active II, which has a pronounced vasopressor effect. ACE drugs inhibit the breakdown of bradykinin, which is considered a powerful vasodilator. In addition, these drugs reduce blood flow to the heart muscle, while reducing the load, protect the kidneys from the effects of diabetes and hypertension. Using inhibitors, it is possible to limit the activity of the kallikrein-kinin system.

Taking ACE inhibitors

Many patients with hypertension are often interested in the question, how to take ACE blockers? The use of any drugs must be agreed with the doctor. In general, inhibitors should be taken one hour before meals on an empty stomach. The dosage, frequency of use, the interval between doses should be determined by a specialist. During treatment with inhibitors, it is worth abandoning non-steroidal anti-inflammatory drugs (Nurofen), salt substitutes and foods rich in potassium.

ACE inhibitors - contraindications

List of relative contraindications for taking inhibitors:

• arterial moderate hypotension;
• chronic severe renal failure;
• childhood;
• severe anemia.

Absolute contraindications for ACE inhibitors:

• hypersensitivity;
• lactation;
• bilateral stenosis of the renal arteries;
• severe hypotension;
• aortic severe stenosis;
• pregnancy;
• severe hyperkalemia;
• porphyria;
• leukopenia.

Side effects of ACE inhibitors

While taking inhibitors, it is necessary to be aware of the development of metabolic side effects. Often there may be dizziness, angioedema, dry cough, an increase in potassium in the blood. These complications can be completely eliminated if you stop taking the drug. There are other side effects of ACE:

• itching, rash;
• weakness;
• hepatotoxicity;
• decreased libido;
• fetopathic potential;
• stomatitis, fever, palpitations;
• swelling of the legs, neck, tongue, face;
• there is a risk of falling and fractures;
• diarrhea or severe vomiting.

Price of ACE inhibitors

You can buy inhibitors in a specialized department of the store or in any pharmacy in Moscow. Their price may differ, based on the form of release and the manufacturer's company. Here is a short list of the latest generation of inhibitor drugs and their approximate cost:

Note!

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Video: ACE drugs

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.

ACE inhibitors (ACE inhibitors): mechanism of action, indications, list and choice of drugs

ACE inhibitors (ACE inhibitors, angiotensin-converting enzyme inhibitors, English - ACE) constitute a large group of pharmacological agents used in cardiovascular pathology, in particular arterial hypertension. Today they are both the most popular and the most affordable means of treating hypertension.

The list of ACE inhibitors is extremely wide. They differ in chemical structure and names, but they have the same principle of action - the blockade of the enzyme, with the help of which active angiotensin is formed, which causes persistent hypertension.

The spectrum of action of ACE inhibitors is not limited to the heart and blood vessels. They have a positive effect on the functioning of the kidneys, improve lipid and carbohydrate metabolism, due to which they are successfully used by diabetics, elderly people with concomitant lesions of other internal organs.

For the treatment of arterial hypertension, ACE inhibitors are prescribed as monotherapy, that is, pressure maintenance is achieved by taking a single drug, or as a combination with drugs from other pharmacological groups. Some ACE inhibitors are immediately combined drugs (with diuretics, calcium antagonists). This approach makes it easier for the patient to take the medication.

Modern ACE inhibitors are not only perfectly combined with drugs from other groups, which is especially important for age-related patients with combined pathology of internal organs, but also have a number of positive effects - nephroprotection, improved blood circulation in the coronary arteries, normalization of metabolic processes, so they can be considered leaders in the process. treatment of hypertension.

Pharmacological action of ACE inhibitors

ACE inhibitors block the action of angiotensin-converting enzyme, which is necessary for the conversion of angiotensin I to angiotensin II. The latter contributes to vasospasm, due to which the total peripheral resistance increases, as well as the production of aldosterone by the adrenal glands, which causes sodium and fluid retention. As a result of these changes, blood pressure rises.

Angiotensin-converting enzyme is normally found in blood plasma and tissues. The plasma enzyme causes rapid vascular reactions, for example, during stress, and the tissue enzyme is responsible for long-term effects. ACE-blocking drugs must inactivate both fractions of the enzyme, that is, their ability to penetrate into tissues, dissolving in fats, will be an important characteristic. The effectiveness of the drug ultimately depends on the solubility.

With a lack of angiotensin-converting enzyme, the pathway for the formation of angiotensin II does not start and there is no increase in pressure. In addition, ACE inhibitors stop the breakdown of bradykinin, which is necessary for vasodilation and pressure reduction.

Long-term use of drugs from the ACE inhibitor group contributes to:

• Reducing the total peripheral resistance of the vascular walls;
• Reducing the load on the heart muscle;
• Decreased blood pressure;
• Improving blood flow in the coronary, cerebral arteries, vessels of the kidneys and muscles;
• Reducing the likelihood of developing arrhythmias.

The mechanism of action of ACE inhibitors includes a protective effect on the myocardium. So, they prevent the appearance of hypertrophy of the heart muscle, and if it already exists, then the systematic use of these drugs contributes to its regression with a decrease in the thickness of the myocardium. They also prevent the overstretching of the heart chambers (dilation), which underlies heart failure, and the progression of fibrosis that accompanies hypertrophy and ischemia of the heart muscle.

mechanism of action of ACE inhibitors in chronic heart failure

Having a beneficial effect on the vascular walls, ACE inhibitors inhibit the reproduction and increase in the size of muscle cells of arteries and arterioles, preventing spasm and organic narrowing of their lumens during prolonged hypertension. An important property of these drugs can be considered an increase in the formation of nitric oxide, which resists atherosclerotic deposits.

ACE inhibitors improve many indicators of metabolism. They facilitate the binding of insulin to receptors in tissues, normalize sugar metabolism, increase the concentration of potassium necessary for the proper functioning of muscle cells, and promote the excretion of sodium and fluid, the excess of which provokes an increase in blood pressure.

The most important characteristic of any antihypertensive drug is its effect on the kidneys, because about a fifth of patients with hypertension die in the end from their insufficiency associated with arteriolosclerosis on the background of hypertension. On the other hand, patients with symptomatic renal hypertension already have some form of renal pathology.

ACE inhibitors have an undeniable advantage - they protect the kidneys better than any other means from the harmful effects of high blood pressure. This circumstance was the reason for their widespread use for the treatment of primary and symptomatic hypertension.

Video: basic pharmacology of ACE inhibitors

Indications and contraindications for ACE inhibitors

ACE inhibitors have been used in clinical practice for thirty years; they rapidly spread in the post-Soviet space in the early 2000s, taking a strong leading position among other antihypertensive drugs. The main reason for their appointment is arterial hypertension, and one of the significant advantages is an effective reduction in the likelihood of complications from the cardiovascular system.

The main indications for the use of ACE inhibitors are:

1. Essential hypertension;
2. symptomatic hypertension;
3. The combination of hypertension with diabetes mellitus and diabetic nephrosclerosis;
4. Renal pathology with high blood pressure;
5. Hypertension in congestive heart failure;
6. Heart failure with reduced output from the left ventricle;
7. Systolic dysfunction of the left ventricle without taking into account pressure indicators and the presence or absence of a clinic for cardiac dysfunction;
8. Acute myocardial infarction after stabilization of pressure or a condition after a heart attack, when the ejection fraction of the left ventricle is less than 40% or there are signs of systolic dysfunction against the background of a heart attack;
9. Condition after a stroke with high blood pressure.

Long-term use of ACE inhibitors leads to a significant reduction in the risk of cerebrovascular complications (stroke), heart attack, heart failure, and diabetes mellitus, which distinguishes them from calcium antagonists or diuretics.

For long-term use as monotherapy instead of beta-blockers and diuretics, ACE inhibitors are recommended for the following groups of patients:

• Those in whom beta-blockers and diuretics cause severe adverse reactions are not tolerated or are ineffective;
• Persons predisposed to diabetes;
• Patients with an established diagnosis of type II diabetes.

As the only prescribed drug, an ACE inhibitor is effective in stages I-II of hypertension and in most young patients. However, the effectiveness of monotherapy is about 50%, so in some cases it becomes necessary to additionally take a beta-blocker, calcium antagonist or diuretic. Combination therapy is indicated at stage III pathology, in patients with concomitant diseases and in the elderly.

Before prescribing a remedy from the ACE inhibitor group, the doctor will conduct a detailed study to exclude diseases or conditions that may become an obstacle to taking these drugs. In their absence, the drug is selected that should be the most effective for this patient based on the characteristics of his metabolism and the route of excretion (through the liver or kidneys).

The dosage of ACE inhibitors is selected individually, empirically. First, the minimum amount is prescribed, then the dose is brought to the average therapeutic dose. At the beginning of the reception and the entire stage of dose adjustment, pressure should be measured regularly - it should not exceed the norm or become too low at the time of the maximum effect of the drug.

In order to avoid large fluctuations in pressure from hypotension to hypertension, the drug is distributed throughout the day in such a way that the pressure, if possible, does not “jump”. The decrease in pressure during the period of maximum action of the drug may exceed its level at the end of the period of action of the tablet taken, but not more than twice.

Experts do not recommend taking the maximum dose of ACE inhibitors, since in this case the risk of adverse reactions increases significantly and the tolerability of therapy decreases. If medium doses are ineffective, it is better to add a calcium antagonist or diuretic to the treatment, making the treatment regimen combined, but without increasing the dose of ACE inhibitors.

As with any drug, there are contraindications to ACE inhibitors. These funds are not recommended for use by pregnant women, as there may be a violation of blood flow in the kidneys and a disorder in their function, as well as an increase in the level of potassium in the blood. A negative impact on the developing fetus in the form of defects, miscarriages and intrauterine death is not excluded. Given the excretion of drugs with breast milk, when they are used during lactation, breastfeeding should be discontinued.

Among the contraindications are also:

1. Individual intolerance to ACE inhibitors;
2. Stenosis of both renal arteries or one of them with a single kidney;
3. Severe stage of renal failure;
4. Increased potassium of any etiology;
5. Childhood;
6. The level of systolic blood pressure is below 100 mm.

Particular care should be taken in patients with cirrhosis of the liver, hepatitis in the active phase, atherosclerosis of the coronary arteries, vessels of the legs. Due to undesirable drug interactions, it is better not to take ACE inhibitors simultaneously with indomethacin, rifampicin, some psychotropic drugs, allopurinol.

Although well tolerated, ACE inhibitors can still cause adverse reactions. Most often, patients who take them for a long time note episodes of hypotension, dry cough, allergic reactions, and disorders in the work of the kidneys. These effects are called specific, and non-specific include taste perversion, indigestion, skin rash. A blood test may reveal anemia and leukopenia.

Video: a dangerous combination - ACE inhibitors and spironolactone

Groups of angiotensin-converting enzyme inhibitors

The names of drugs to reduce pressure are widely known to a large number of patients. Someone takes the same one for a long time, someone is indicated for combination therapy, and some patients are forced to change one inhibitor to another at the stage of selecting an effective agent and dose to reduce pressure. ACE inhibitors include enalapril, captopril, fosinopril, lisinopril, etc., which differ in pharmacological activity, duration of action, and method of excretion from the body.

Depending on the chemical structure, various groups of ACE inhibitors are distinguished:

• Preparations with sulfhydryl groups (captopril, methiopril);
• Dicarboxylate-containing ACE inhibitors (lisinopril, enam, ramipril, perindopril, trandolapril);
• ACE inhibitors with a phosphonyl group (fosinopril, ceronapril);
• Preparations with a hybroxam group (idrapril).

The list of drugs is constantly expanding as experience with the use of individual drugs accumulates, and the latest drugs are undergoing clinical trials. Modern ACE inhibitors have a small number of adverse reactions and are well tolerated by the vast majority of patients.

ACE inhibitors can be excreted by the kidneys, liver, dissolve in fats or water. Most of them turn into active forms only after passing through the digestive tract, but four drugs immediately represent the active drug substance - captopril, lisinopril, ceronapril, libenzapril.

According to the characteristics of metabolism in the body, ACE inhibitors are divided into several classes:

• I - fat-soluble captopril and its analogues (altiopril);
• II - lipophilic precursors of ACE inhibitors, the prototype of which is enalapril (perindopril, cilazapril, moexipril, fosinopril, trandolapril);
• III - hydrophilic preparations (lisinopril, ceronapril).

Second-class drugs may have a predominantly hepatic (trandolapril), renal (enalapril, cilazapril, perindopril) route of elimination, or a mixed route (fosinopril, ramipril). This feature is taken into account when prescribing them to patients with disorders of the liver and kidneys to eliminate the risk of damage to these organs and serious adverse reactions.

One of the most widely used ACE inhibitors is enalapril. It does not have a prolonged action, so the patient is forced to take it several times a day. In this regard, many experts consider it obsolete. At the same time, enalapril to this day shows an excellent therapeutic effect with a minimum of adverse reactions, so it still remains one of the most prescribed drugs in this group.

The latest generation of ACE inhibitors include fosinopril, quadropril and zofenopril.

Fosinopril contains a phosphonyl group and is excreted in two ways - through the kidneys and the liver, which allows it to be prescribed to patients with impaired renal function, for whom ACE inhibitors from other groups may be contraindicated.

Zofenopril is similar in chemical composition to captopril, but has a prolonged action - it must be taken once a day. The long-term effect gives zofenopril an advantage over other ACE inhibitors. In addition, this drug has an antioxidant and stabilizing effect on cell membranes, therefore it perfectly protects the heart and blood vessels from adverse effects.

Another long-acting drug is quadropril (spirapril), which is well tolerated by patients, improves heart function in congestive insufficiency, reduces the likelihood of complications and prolongs life.

The advantage of quadropril is considered to be a uniform hypotensive effect that persists throughout the entire period between taking the tablets due to the long half-life (up to 40 hours). This feature virtually eliminates the likelihood of vascular accidents in the morning, when the action of an ACE inhibitor with a shorter half-life ends, and the patient has not yet taken the next dose of the drug. In addition, if the patient forgets to take another pill, the hypotensive effect will be preserved until the next day, when he still remembers about it.

Due to the pronounced protective effect on the heart and blood vessels, as well as the long-term effect, zofenopril is considered by many experts to be the best treatment for patients with a combination of hypertension and cardiac ischemia. Often these diseases accompany each other, and isolated hypertension itself contributes to coronary heart disease and a number of its complications, so the issue of simultaneous exposure to both diseases at once is very relevant.

ACE inhibitors of the new generation, in addition to fosinopril and zofenopril, also include perindopril, ramipril and quinapril. Their main advantage is considered to be a prolonged action, which makes life very easy for the patient, because to maintain normal pressure, only a single dose of the drug daily is enough. It is also worth noting that large-scale clinical studies have proven their positive role in increasing the life expectancy of patients with hypertension and coronary heart disease.

If it is necessary to prescribe an ACE inhibitor, the doctor faces a difficult task of choosing, because there are more than a dozen drugs. Numerous studies show that older drugs do not have significant advantages over the latest ones, and their effectiveness is almost the same, so the specialist must rely on a specific clinical situation.

For long-term therapy of hypertension, any of the known drugs is suitable, except for captopril, which to this day is used only for the relief of hypertensive crises. All other funds are prescribed for continuous use, depending on concomitant diseases:

• In diabetic nephropathy - lisinopril, perindopril, fosinopril, trandolapril, ramipril (in reduced doses due to slower excretion in patients with reduced renal function);
• With liver pathology - enalapril, lisinopril, quinapril;
• With retinopathy, migraine, systolic dysfunction, as well as for smokers, the drug of choice is lisinopril;
• With heart failure and left ventricular dysfunction - ramipril, lisinopril, trandolapril, enalapril;
• In diabetes mellitus - perindopril, lisinopril in combination with a diuretic (indapamide);
• In ischemic heart disease, including in the acute period of myocardial infarction, trandolapril, zofenopril, perindopril are prescribed.

Thus, it does not make much difference which ACE inhibitor the doctor chooses for the long-term treatment of hypertension - the older one or the last one synthesized. By the way, in the United States, lisinopril remains the most frequently prescribed drug - one of the first drugs that has been used for about 30 years.

It is more important for the patient to understand that taking ACE inhibitors should be systematic and constant, even for life, and not depending on the numbers on the tonometer. In order for the pressure to be maintained at a normal level, it is important not to skip the next pill and not to change either the dosage or the name of the drug on your own. If necessary, the doctor will prescribe additional diuretics or calcium antagonists, but ACE inhibitors are not canceled.