APF instructions for use. ACE inhibitors: list of latest generation drugs. ACE inhibitors - contraindications

One of the most common pathologies among older people is hypertension. In most cases, it is provoked by oligopeptide angiotensin.

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

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

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

Research was conducted in the USA. , Zofenopril was successfully used at that time. Moreover, the prescription was made at the beginning to those patients who had hypertension of the third or fourth degree.

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

The third generation of effective blood pressure tablets is represented by Fosinopril. The newest drug is prescribed for acute heart attack. It is effective for diabetes mellitus and kidney diseases.

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

ACE inhibitors - 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 new generation of ACE drugs that do not allow calcium compounds to penetrate into the blood vessels and heart. Due to this, the body’s need for excess oxygen is reduced, and blood pressure is normalized.

Latest generation inhibitor Losartan

Latest generation ACE inhibitors, list:

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

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

If you have hypertension, do not choose your medications yourself. Otherwise, you can only worsen your condition.

Latest generation ACE inhibitors: advantages

To reduce deaths, comprehensive treatment must be used. Including angiotensin-converting enzyme inhibitors.

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

minimum side effects, improve the patient’s condition;
The effect of the tablets is quite long-lasting, not the same as that of the blood pressure medications forty years ago. In addition, they have a positive effect on the functioning of the heart, vascular system, and kidneys;
help improve the functioning of the nervous system;
The tablets act purposefully without affecting other organs. Therefore, older people do not experience any complications;
have a beneficial effect on the psyche and prevent depression;
normalize the size of the left ventricle;
do not affect the physical, sexual, emotional state of the patient;
for diseases of the bronchi, these are the drugs that are recommended; they do not cause complications;
have a positive effect on kidney function. Normalize metabolic processes in which uric acid and lipids are involved.

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

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

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

Side effects

New drugs in this series minimize the impact of side effects on the overall condition of the patient’s body. And yet the negative impact is felt, which requires replacing the dosage form with other tablets.

15–20% of patients experience the following side symptoms:

manifestation of cough due to the accumulation of bradykinin. In this case, ACE is replaced with ARA-2 (angiotensin receptor blockers - 2);
disruption of the gastrointestinal tract, liver function - in rare cases;
hyperkalemia – excess potassium levels in the body. Such symptoms occur when taking ACE inhibitors in combination with loop diuretics. With single use of recommended doses, hyperkalemia does not occur;
Treatment of hypertension and heart failure with maximum dosages of ACE inhibitor drugs leads to renal failure. Most often, the phenomenon is observed in patients with pre-existing kidney damage;
When you self-prescribe blood pressure medications, sometimes, very rarely, allergic reactions occur. It is better to start using it in a hospital, under the supervision of specialists;
a persistent decrease in blood pressure (hypotension) of the first dose - manifests itself in patients with initially low blood pressure and in those patients who do not control the readings of the tonometer, but take pills to lower it. Moreover, they themselves prescribe maximum doses.

Drugs for high blood pressure 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 products.

Contraindications for use

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

The drugs are contraindicated for patients who cannot tolerate the active ingredient of a particular drug.

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

It is not recommended to use antihypertensive pills in patients under eighteen years of age. Individuals with anemia and other blood diseases should not use inhibitors. Leukopenia can also be considered one of them. 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 it occurs in children who are born in a marriage from parents who initially have close family ties.

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

Video on the topic

About the treatment of hypertension with new generation drugs:

If high blood pressure does not appear often, then you should start taking ACE tablets under the supervision of a specialist doctor with small dosages. If you experience slight dizziness at the beginning of using inhibitors, 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 so will your blood pressure.

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

The list of ACE inhibitors is extremely wide. They differ in chemical structure and names, but their principle of action is the same - blockade of the enzyme that produces active angiotensin, causing persistent hypertension.

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

For the treatment of arterial hypertension, ACE inhibitors are prescribed as monotherapy, that is, maintaining blood pressure is achieved by taking one drug, or in 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 medications.

Modern ACE inhibitors not only combine well with drugs from other groups, which is especially important for older patients with concomitant pathology of internal organs, but also have a number of positive effects - nephroprotection, improvement of 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 to convert angiotensin I to angiotensin II. The latter promotes vasospasm, due to which total peripheral resistance increases, as well as the production of aldosterone by the adrenal glands, which causes sodium and fluid retention. As a consequence of these changes, it increases.

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

If there is a lack of angiotensin-converting enzyme, the pathway for the formation of angiotensin II does not start and there is no increase in blood pressure. In addition, ACE inhibitors stop the breakdown of bradykinin, which is necessary for vasodilation and blood 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;
Reducing blood pressure;
Improving blood flow in the coronary, cerebral arteries, kidney and muscle vessels;
Reducing the likelihood of development.

The mechanism of action of ACE inhibitors includes a protective effect on the myocardium. So, they prevent the appearance, and if it already exists, then the systematic use of these drugs contributes to its reverse development with a decrease in the thickness of the myocardium. They also prevent overstretching of the heart chambers (dilatation), 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 proliferation 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 metabolic parameters. They facilitate binding to receptors in tissues, normalize metabolism, increase the concentration necessary for the proper functioning of muscle cells, and promote the removal of sodium and fluid, the excess of which provokes a rise 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 ultimately die from kidney failure associated with arteriolosclerosis due to hypertension. On the other hand, with symptomatic renal hypertension, patients already have some form of renal pathology.

ACE inhibitors have an undeniable advantage - they protect the kidneys better than all other drugs 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 use 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:

Combination of hypertension with diabetic nephrosclerosis;
Renal pathology with high blood pressure;
Hypertension with congestion;
Heart failure with reduced left ventricular output;
Systolic dysfunction of the left ventricle without taking into account pressure indicators and the presence or absence of clinical cardiac dysfunction;
Acute myocardial infarction after stabilization of pressure or a condition after a heart attack, when the left ventricular ejection fraction is less than 40% or there are signs of systolic dysfunction against the background of a heart attack;
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:

For those for whom beta blockers and diuretics cause severe side effects, are not tolerated or are ineffective;
Persons predisposed to diabetes;
Patients already diagnosed with 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 there is a need to additionally take a beta-blocker, calcium antagonist or diuretic. Combination therapy is indicated at stage III of the pathology, in patients with concomitant diseases and in old age.

Before prescribing a drug 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 medications. In their absence, the drug that should be most effective for a given patient is selected based on the characteristics of its metabolism and the route of elimination (through the liver or kidneys).

The dosage of ACE inhibitors is selected individually, experimentally. First, the minimum amount is prescribed, then the dose is adjusted to the average therapeutic dose. When starting treatment and during the entire dose adjustment phase, blood pressure should be regularly measured - it should not exceed the norm or become too low at the moment of maximum effect of the medicine.

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

Experts do not recommend taking maximum doses 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 a combined therapy regimen, but without increasing the dose of the ACE inhibitor.

As with any medicines, there are contraindications. These drugs are not recommended for use by pregnant women, as it may impair blood flow in the kidneys and disrupt their function, as well as increase the level of potassium in the blood. A negative impact on the developing fetus in the form of defects, miscarriages and intrauterine death is possible. Given the excretion of drugs in breast milk, breastfeeding should be discontinued when used during lactation.

Contraindications also include:

Individual intolerance to ACE inhibitors;
both renal arteries or one of them with a single kidney;
Severe stage of renal failure;
any etiology;
Childhood;
Systolic blood pressure level 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 and blood vessels of the legs. Due to undesirable drug interactions, it is better not to take ACE inhibitors simultaneously with indomethacin, rifampicin, some psychotropic drugs, and allopurinol.

Despite being well tolerated, ACE inhibitors can still cause adverse reactions. Most often, patients who take them for a long time report episodes of dry cough, allergic reactions, and kidney disorders. These effects are called specific, while nonspecific effects include taste distortion, indigestion, and skin rash. A blood test may detect anemia and leukopenia.

Video: dangerous combination - ACEI and spironolactone

Groups of angiotensin-converting enzyme inhibitors

The names of drugs to lower blood pressure are widely known to a large number of patients. Some take the same inhibitor for a long time, others are prescribed combination therapy, and some patients are forced to change one inhibitor to another at the stage of selecting an effective drug and dose to lower blood pressure. ACE inhibitors include enalapril, captopril, fosinopril, lisinopril, etc., which differ in pharmacological activity, duration of action, and method of elimination from the body.

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

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

The list of drugs is constantly expanding as experience in the use of individual drugs accumulates, and the newest drugs undergo 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, and dissolved in fats or water. Most of them are converted into active forms only after passing through the digestive tract, but four drugs immediately represent an 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 (althiopril);
II - lipophilic precursors of ACE inhibitors, the prototype of which is enalapril (perindopril, cilazapril, moexipril, fosinopril, trandolapril);
III - hydrophilic drugs (lisinopril, ceronapril).

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

ACE inhibitors are not usually divided into generations, but still this division occurs conventionally. The newest drugs are practically no different in structure from their “older” analogues, but the frequency of administration and accessibility to tissues may differ for the better. In addition, the efforts of pharmacologists are aimed at reducing the likelihood of side effects, and new drugs are generally better tolerated by patients.

One of the longest used ACE inhibitors is enalapril. It does not have a prolonged effect, so the patient is forced to take it several times a day. In this regard, many experts consider it outdated. 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 ACEIs from other groups may be contraindicated.

Zofenopril Its chemical composition is similar to captopril, but has a prolonged effect - 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 case of congestive heart failure, reduces the likelihood of complications and prolongs life.

The advantage of quadropril is its uniform hypotensive effect, which persists throughout the entire period between tablets taken due to its long half-life (up to 40 hours). This feature virtually eliminates the likelihood of vascular accidents in the morning, when the effect of ACE inhibitors 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 the next pill, the hypotensive effect will be maintained until the next day when he remembers about it.

Due to the pronounced protective effect on the heart and blood vessels, as well as long-term action, Zofenopril is considered by many experts to be the best for treating 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 impact on both diseases is very relevant.

New generation ACE inhibitors, 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 much easier for the patient, because to maintain normal blood 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 the 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 newest ones, and their effectiveness is almost the same, so a specialist must rely on a specific clinical situation.

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

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

Thus, there is little difference which ACE inhibitor the doctor chooses for long-term treatment of hypertension - the “older” one or the latest one synthesized. By the way, in the USA, lisinopril remains the most frequently prescribed drug - one of the first drugs used for about 30 years.

It is more important for the patient to understand that taking ACE inhibitors should be systematic and constant, even lifelong, 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 another tablet and not to change either the dosage or the name of the drug on your own. If necessary, the doctor will prescribe additional or, but ACE inhibitors are not canceled.

Video: lesson on ACE inhibitors

Video: ACE inhibitors in the “Live Healthy” program

The list of ACE inhibitor drugs includes widely used drugs for decompensated myocardial dysfunction and kidney pathologies. The benefits of such medicines have been proven. Their use shows a positive clinical effect and has significantly reduced mortality.

When prescribing medications, an individual approach to each patient is of great importance. In order for the treatment to be safe and beneficial, it is important to correctly determine the dosage regimen and frequency, as there is a risk of a sharp drop in pressure.

List of new generation ACE inhibitor drugs

Medicines from the phosphoryl group based on fosinopril are highly effective in the treatment of cardiovascular diseases.

It is believed that therapy with such medications reduces the frequency of dry cough attacks, which is the most common side effect. A distinctive feature of such drugs is the adaptive mechanism of elimination - through the kidneys and liver.

1. Fosinopril (Russia). It is recommended by treatment standards as a safe ACE inhibitor for hypertension. Has a relaxing effect on the walls of blood vessels.

Eliminates the possibility of developing hypokalemia.

With systematic use, signs of disease regression are noted.

Rarely causes a dry cough.

Tablets 10 mg 30 pcs. - 215 rubles.

2. Fosicard (Serbia). Effective in combination therapy. The pharmacological effects of the ACE inhibitor Fosicard include a pronounced antihypertensive effect.

A persistent decrease in blood pressure occurs an hour after taking the medicine.

A small number of side effects are observed in elderly patients and patients with diabetes.

An adequately selected dosage increases the effectiveness of the medicine.

Packaging of tablets 20 mg, 28 pcs. - 300 rub.

3. Monopril (USA). An original remedy with proven effectiveness in the treatment of cardiovascular diseases. One of the best drugs in the list of ACE inhibitor drugs. Increases stability during physical activity. The action lasts up to 24 hours.

Reduces the risk of complications.

Has an antiatherosclerotic effect.

Lowers the level of “bad” cholesterol.

There is a low percentage of side effects. After a long course of treatment, the therapeutic effect persists. It has a convenient dosage regimen - once a day.

Table 20 mg, 28 pcs. 415 rub.

4.Fozinap (Russia). An effective remedy in the treatment of diseases associated with impaired myocardial function. Facilitates the course of persistent arterial hypotension. With a long course of treatment, metabolic disorders are not observed.

Tablets 20 mg, 28 pcs. - 240 rub.

List of second generation drugs

They belong to the carboxyl group. They are produced on the basis of ramipril and lisinopril. To date, these are the most prescribed drugs.

Practice shows that for some groups of patients, second-generation drugs are more suitable than the latest modern ACE inhibitors. When prescribing, the doctor takes into account all the features of the clinical picture, the presence of concomitant diseases, laboratory test results, etc.

Preparations with lisinopril

1. Lisinopril (Russia). Used in the treatment of cardiovascular pathologies. Most effective in a combined treatment regimen. Quickly stabilizes blood pressure. Has a prolonged effect up to a day.

Often prescribed in rehabilitation therapy after strokes.

According to indications, it can be taken by patients with functional liver disorders.

10 mg tablets 30 pieces - 35 rubles.

2. Diroton (Hungary). A high-quality antihypertensive drug with pronounced peripheral vasodilatory properties. Prevents sudden changes in pressure. It works quickly.

This drug of the ACE inhibitor group does not affect the liver. For this reason, it is often prescribed to patients with concomitant diseases: cirrhosis, hepatitis.

Side effects are minimized.

Cost of tablets 5 mg, 28 pcs. - 206 rub.

Medicines with ramipril

1. Ramipril - SZ (Russia). The medication has pronounced antihypertensive activity. In patients with cardiovascular profile, rapid normalization of blood pressure is observed, regardless of body position.

Taking the medication on a regular basis increases the antihypertensive effect over time.

Does not cause withdrawal syndrome.

Table 2.5 mg 30 pieces - 115 rub.

2. Pyramil (Switzerland). Reduces left ventricular hypertrophy, which is the root cause of the development of cardiac lesions.

In patients with cardiovascular pathology, it reduces the likelihood of developing strokes.

An effective ACE inhibitor for diabetes mellitus.

Develops resistance to physical activity.

The medication can be used regardless of food intake.

Tablets 2.5 mg 28 pieces - 220 rub.

3. Amprilan (Slovenia). Long-acting medication. Normalizes metabolic processes in the myocardium.

Prevents intense constriction of peripheral vessels.

Has a cumulative effect. Most effective with long-term therapy.

Steady stabilization of blood pressure is observed in the third or fourth week of use.

Tab. 30 pcs. 2.5 mg - 330 rub.

ACE inhibitors (ACE inhibitors) are new generation medications whose action is aimed at lowering blood pressure. Currently, there are over 100 types of such drugs in pharmacology.

They all have a common mechanism of action, but differ from each other in structure, method of elimination from the body and duration of exposure. There is no generally accepted classification of ACE inhibitors, and all divisions of this group of drugs are conditional.

Conditional classification

According to the method of pharmacological action, there is a classification that divides ACE inhibitors into three groups:

ACEI with a sulfhydryl group;
ACEI with a carboxyl group;
ACEI with a phosphinyl group.

The classification is based on indicators such as the method of elimination from the body, half-life, etc.

Group 1 drugs include:

Captopril (Capoten);
Benazepril;
Zofenopril.

These drugs have indications for use in patients who have hypertension combined with coronary heart disease. They are quickly absorbed into the blood. For more effective action, they are taken 1 hour before meals to speed up the absorption process. In some cases, ACE inhibitors may be prescribed along with diuretics. Medicines in this group can also be taken by diabetics, patients with pulmonary pathology and heart failure.

Patients with urinary system diseases should be treated with caution, since the medicine is excreted by the kidneys.

List of drugs of group 2:

Enalapril;
Quinapril;
Renitek;
Ramipril;
Trandolapril;
Perindopril;
Lisinopril;
Spirapril.

ACE inhibitors containing a carboxyl group have a longer-lasting mechanism of action. They undergo metabolic transformation in the liver, providing a vasodilator effect.

Third group: Fosinopril (Monopril).

The mechanism of action of Fozinopril is aimed primarily at controlling morning increases in blood pressure. It is considered one of the latest generation drugs. It has a long-lasting effect (about a day). It is excreted from the body by the liver and kidneys.

There is a conditional classification of new generation ACE inhibitors, which are a combination with diuretics and calcium antagonists.

ACE inhibitors in combination with diuretics:

Capozide;
Elanapril N;
Iruzid;
Scopril Plus;
Ramazid N;
Accusid;
Phosicard N.

The combination with a diuretic has a faster effect.

ACE inhibitors in combination with calcium antagonists:

Coryprene;
Equacard;
Triapin;
Egipres;
Tarka.

The mechanism of action of these medications is aimed at increasing the distensibility of large arteries, which is especially important for elderly hypertensive patients.

Thus, the combination of drugs provides for enhancing the effect of the drug when the ACEI alone is insufficiently effective.

Advantages

The advantage of ACEI drugs is not only their ability to lower blood pressure: the main mechanism of their action is aimed at protecting the patient’s internal organs. They have a good effect on the myocardium, kidneys, cerebral vessels, etc.

With myocardial hypertrophy, ACE inhibitors contract the heart muscle of the left ventricle more intensely, unlike other drugs for hypertension.

ACEIs improve renal function in chronic renal failure. It is also noted that these drugs improve the general condition of the patient.

Indications

Main indications for use:

hypertension;
myocardial infarction;
atherosclerosis;
left ventricular dysfunction;
chronic heart failure;
cardiac ischemia;
diabetic nephropathy.

How to take ACE inhibitors

It is prohibited to use salt substitutes while taking ACE inhibitors. The substitutes contain potassium, which is retained in the body by drugs against hypertension. You should not eat foods enriched with potassium. These include potatoes, walnuts, dried apricots, seaweed, peas, prunes and beans.

During treatment with inhibitors, you should not take anti-inflammatory non-steroidal drugs such as Nurofen, Brufen, etc. These medications retain fluid and sodium in the body, thereby reducing the effectiveness of ACEIs.

It is very important to monitor blood pressure and kidney function when taking ACE drugs on a regular basis. It is not recommended to discontinue medications on your own without consulting a doctor. A short course of treatment with inhibitors may not be effective. Only with long-term treatment is the medicine able to regulate blood pressure levels and be very effective for concomitant diseases such as heart failure, coronary heart disease, etc.

Contraindications

ACE inhibitors have both absolute and relative contraindications.

Absolute contraindications:

pregnancy;
lactation;
hypersensitivity;
hypotension (below 90/60 mm);
renal artery stenosis;
leukopenia;
severe aortic stenosis.

Relative contraindications:

moderate arterial hypotension (from 90 to 100 mm);
severe chronic renal failure;
severe anemia;
chronic pulmonary heart disease in the stage of decompensation.

Indications for use with the above diagnoses are determined by the treating specialist.

Side effects

ACE inhibitors are often well tolerated. But sometimes side effects of the medicine may occur. These include headache, nausea, dizziness and fatigue. The appearance of arterial hypotension, worsening renal failure, and the occurrence of allergic reactions cannot be ruled out. Less common side effects are dry cough, hyperkalemia, neutropenia, and proteinuria.

You should not self-prescribe ACE inhibitors. Indications for use are determined strictly by the doctor.

Hello, dear friends!

When I saw that the article turned out to be impressive (don’t be alarmed, I divided it into two parts), I poured myself some tea with lemon balm, took out two Korovka candies so that the material could be absorbed better, and started reading.

And you know, it captivated me so much! Many thanks to Anton: he explained everything so interestingly and clearly!

Plunging into the mysterious world of the human body, I never cease to admire how magically Man is created.

It was necessary for the Creator to come up with everything like that! One substance combines with another, a third helps it in this, while something expands, something contracts, something is released, something improves. Moreover, this entire factory works non-stop, day and night!

In general, friends, pour yourself some tea or coffee to complete the buzz (if your blood pressure is OK) and read with feeling, sense, and alignment.

And I give the floor to Anton.

- Thank you, Marina!

Last time we talked to you about how the nervous system regulates blood pressure, and we talked about drugs that affect this process.

Today we will discuss the factors that regulate vascular tone, that is, we will talk about humoral regulation of blood vessels, which is nothing more than regulation by signaling molecules.

Humoral regulation of blood vessels

Humoral regulation is much more ancient and therefore more complex both in description and in understanding.

Let's take a closer look at substances that increase vascular tone.

The first and most famous - adrenalin. This is a hormone of the adrenal cortex, which is released when exposed to the sympathetic nervous system.

The mechanism of its action is associated with the effect on adrenergic receptors, which we already discussed last time. Therefore, you already know what to do with the effect of adrenaline on blood vessels.

The following connection is angiotensin II. This is a powerful vasoconstrictor compound that is formed as a result of a chain of transformations: angiotensinogen - angiotensin I - angiotensin II.

Angiotensinogen is an inactive compound produced in the liver. These transformations are catalyzed by the so-called angiotensin converting enzyme , or simply APF. ACE activity is regulated, in turn, by renin. Remember? We also talked about this.

This substance is secreted by the kidney in response to the influence of sympathetic innervation on it. In addition, the kidney begins to produce renin if the amount of blood supplied to it decreases.

Angiotensin II also affects the adrenal glands, stimulating the release of aldosterone and cortisol – hormones that reduce sodium excretion.

This happens normally.

What happens during stress?

Now imagine a person who experiences chronic stress.

For example, our colleague is a senior manager who deals with difficult clients every day.

During every stressful situation, the sympathetic nervous system is activated. The blood vessels narrow, the heart begins to beat faster, a portion of adrenaline is released from the adrenal glands, and the kidneys begin to secrete renin, which activates ACE.

As a result, the amount of angiotensin II increases, the vessels narrow even more, and the pressure jumps.

If the stress has passed, the activity of the sympathetic nervous system decreases, and gradually everything returns to normal.

However, if the stress is repeated day after day, the blood flow of the kidneys under the influence of adrenaline and angiotensin II becomes worse and worse, the kidneys release even more renin, which promotes even more release of angiotensin II.

This causes the heart to exert more and more force to pump blood into the narrowed arteries.

The myocardium begins to grow. But no one will increase his nutrition, since only muscles grow, not blood vessels.

In addition, large amounts of angiotensin II release aldosterone from the adrenal glands, which reduces sodium excretion, and sodium attracts water, which increases blood volume.

There comes a moment when the heart refuses to work in such conditions and begins to “scandalize” - arrhythmias appear, its contractility decreases, as the heart muscle loses its last strength in trying to pump blood into the narrowed vessels.

The kidneys are also not happy: the blood flow in them is disrupted, the nephrons gradually begin to die.

That is why hypertension entails several complications at once.

And stress is to blame for everything. It is no coincidence that hypertension is called “the disease of unspoken emotions.”

In the same way, any factor that narrows the lumen of the renal artery will work, for example, a tumor compressing the vessel, or an atherosclerotic plaque, or a blood clot. The kidney will “panic” because it lacks oxygen and nutrients, and will begin to release renin in huge portions.

Have I not loaded you too much with physiology?

But without understanding this it is impossible to understand the effect of the drugs to which I now turn.

So, How can all this disgrace be affected by medications?

Since the central link in this story is angiotensin II, it is necessary to somehow reduce its amount in the body. And here drugs that reduce the activity of ACE, or (ACEI), come to the rescue.

ACE inhibitors

Drugs in this group have a vasodilating effect, inhibit the excretion of protein in the urine, and have a diuretic effect (due to the fact that they dilate blood vessels, including those of the kidneys, and reduce the amount of aldosterone). In addition, they reduce the excretion of potassium by the kidneys. The effectiveness of drugs in this group has been proven for heart failure and left ventricular hypertrophy, since they reduce the activity of cardiac muscle growth.

For a long time, this group of drugs was considered the “gold standard” for the treatment of hypertension. Why? Look: the blood vessels are dilated, the work of the heart is made easier, the kidneys are also happy.

And these drugs also helped reduce mortality from myocardial infarction. It would seem, what more could you want?

The main side effect noted by patients is a dry cough.

In addition, ACE inhibitors cause hypotension (in the case of a single dose of large doses), can provoke the appearance of a rash, loss of taste sensitivity, impotence and decreased libido, a decrease in the content of leukocytes in the blood, and, in addition, they are hepatotoxic.

In general, the list is impressive, and ACE inhibitors have lost their title. However, in Russia they are still considered the first line of treatment for hypertension.

Let's look at them in more detail.

The first drug, the oldest of the entire group, captopril, known as CAPOTEIN.

It is recommended to take it before meals, as food inhibits its absorption. This is one of the fast-acting ACE inhibitors. Its effect develops when taken orally after 30 minutes - 1 hour, when taken sublingually - after 15-30 minutes. Therefore, the drug can be used as an emergency treatment for hypertensive crisis. It is important to remember that you can take no more than two tablets at a time, and no more than six per day.

The drug is contraindicated in pregnant, lactating, persons under 18 years of age, people with renal failure, narrowing of the lumen of both renal arteries.

Side effects include dry mucous membranes, dry cough, increased activity of liver transaminases, headache, dizziness, and there may be allergic reactions.

The second drug is the best-selling ACEIEnalapril, known under the names ENAP, ENAM, BERLIPRIL, RENITEK, etc.

The drug is a prodrug, that is, when taken orally, Enalapril maleate is converted in the liver into the active substance Enalaprilat. In addition to inhibiting ACE, it has a vasodilatory effect, improves renal blood flow, normalizes plasma cholesterol levels, and reduces the loss of potassium ions caused by diuretics.

Eating does not affect the absorption of the drug. It begins to act an hour after ingestion, the duration of action is from 12 to 24 hours, it depends on the dosage.

Contraindicated for persons under 18, pregnant and lactating women, and those with hypersensitivity to ACE inhibitors.

The next drug is lisinopril, or DIROTON.

Its main feature is that it is practically not metabolized in the liver, therefore, much less often than other ACE inhibitors, it causes dry mucous membranes and provokes a dry cough.

Another important advantage of the drug is that the part of it that is bound to ACE is excreted extremely slowly, which allows it to be used once a day. The drug reduces protein loss in urine.

Contraindicated for persons under 18, pregnant and lactating women.

Let's talk now about Perindopril, known as PRESTARIUM, PRESTARIUM A and PERINEVA.

Prestarium and Perineva are available in 4 and 8 mg doses, but Prestarium A is available in 5 and 10 mg doses. As it turned out, Prestarium A contains perindopril arginine, and Perinev and Prestarium contain perindopril erbumine. Comparing the features of pharmacokinetics, I realized this thing. In compounds containing perindopril erbumine, approximately 20% of the substance consumed becomes active, and in the perindopril compound, arginine becomes active - about 30%.

The second important feature is that perindopril has a long half-life, its effectiveness remains for 36 hours. And a lasting effect develops within 4-5 days. For comparison, lisinopril takes 2-3 weeks, enalapril takes a month.

The third feature of the drug is that it has an antiplatelet effect; its mechanism is complex and is associated with the formation of prostacyclin, a compound that reduces the ability of platelets to stick together and adhere to the vascular wall.

In light of this, the indications for use of the drug are wider. In addition to hypertension, it is indicated for chronic heart failure, stable coronary heart disease, to reduce the risk of cardiovascular disaster, and to prevent recurrent stroke in patients who have had cerebrovascular diseases.

The rest of the drugs in this group are similar to each other, only the onset of action and half-life differ. Therefore, I will not consider them separately.

And at the end of today's conversation, one very important warning:

All drugs in this group reduce potassium excretion, and additional intake of potassium-containing drugs such as Asparkam or Panangin without monitoring potassium levels in the blood can lead to hyperkalemia, which, in turn, can cause cardiac arrhythmias and, God forbid, cardiac arrest .

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See you again on the blog for hard workers!

With love to you, Marina Kuznetsova