Antihypertensive drugs list of drugs. Modern antihypertensive drugs combined. What are the features of diuretics

Previously, the pressure was lowered with the help of an ordinary foxglove. Over time, medicines gradually improved. But mortality from hypertension and its complications was high. Various antihypertensive drugs are developed every year. New generation drugs are constantly appearing that are not only effective, but also give fewer adverse reactions.

What should be antihypertensive drugs

Normal level blood pressure depends on vascular tone. With their spasm caused by contraction of smooth muscle tissue, the lumen narrows, which leads to hypertension. This usually occurs during physical exertion or due to nervous strain. But sometimes the pressure rises due to the development of diseases of the cardiovascular system, kidneys, hormonal imbalance. To normalize it, the doctor prescribes antihypertensive drugs.

Medicines used to treat hypertension need to do more than just dilate blood vessels. With this, the tools made on the basis of foxglove coped quite well. However, mortality from hypertension was high. Mainly due to complications caused by the disease and side effects of drugs.

An effective drug for hypertension should:

1. Normalize pressure for a long time.
2. Beneficial effect on target organs (kidneys, heart, eyes).
3. Do not give adverse reactions. The negative impact of the drug should be minimized.

In order for medicines to meet all these requirements, various research and development of new generation drugs are constantly being carried out in the world.

But the old effective medicines are not forgotten. They are improved by creating effective means from hypertension.

Modern hypertensive

For the treatment of hypertension, medicines belonging to various groups are used. Greatest effect give complex preparations. They not only reduce pressure by dilating blood vessels, but also restore the functioning of the kidneys and heart, and prevent the development of severe complications.

All antihypertensive drugs affect the natural mechanism of blood pressure regulation. They can affect the central nervous system or inhibit the production of hormones and enzymes that cause hypertension. All drugs are classified according to how they alter the normal regulation of blood pressure.

List of groups of effective antihypertensive drugs:

• neurotropic;
• myotropic action;
• affecting humoral regulation;
• diuretics.

Thanks to this diversity, it is easier to choose the drug individually. But the choice must be made by the doctor. Only a specialist will prescribe the necessary pills, since all new generation medicines have a multifaceted effect.

Neurotropic agents

Medicines in this group affect the central nervous system. They reduce the activity of the sympathetic nervous system. This relieves the tension of smooth muscle tissue, which leads to a decrease in pressure. These include:

1. Sedatives (clonidine guanfacine, rilmenidine, methyldopa). They affect the vasomotor center located in the cerebral cortex, thus forcing smooth muscles to relax. As a result, the walls of the vessels expand and the pressure decreases. But they make you sleepy.
2. Ganglioblocking agents (pentamine, benzohexonium). They affect the nerve nodes that innervate muscle tissue. But their use leads to a decrease in the tone of all organs. They can cause constipation and blurred vision.
3. α-blockers (phentolamine, tropafen, prazosin). Influencing the receptors located in the vascular wall, they have a depressing effect on the vasomotor center.
4. Sympatholytics (reserpine, guanethidine, pargyline). Reduce the level of norepinephrine, which causes vasoconstriction.
5. β-blockers (anaprilin, atenolol, talinolol, metoprolol, labetalol). This is a new generation of drugs that affect not only the vasomotor center. They weaken the work of the heart, reduce the production of renin, reduce the level of norepinephrine. Therefore, these drugs are considered the most effective antihypertensive agent.

Drugs with neurotropic action well reduce pressure, have a beneficial effect on the work of the heart, and β-blockers and on the kidneys. But they can cause a mass side effects. An overdose of sedatives can cause cardiac arrest. Adrenoblockers are not recommended for bronchial asthma. All of these drugs have many contraindications. Therefore, before you start taking pills, you should consult your doctor.

It's important to know! Abrupt discontinuation of neurotropic drugs leads to a rapid and persistent increase in pressure.

Myotropic drugs

They affect ion exchange in smooth muscle tissue. Myotropic tablets work different ways, but lead to the same result - a decrease in pressure.

Calcium channel blockers:

• fenigidin;
• diltiazem;
• isradipine;
• verapamil.

Potassium channel activators:

• minoxidil;
• diazoxide.

Nitric oxide stimulators:

• sodium nitroprusside;
• molsidomine.

Phosphodiestase inhibitors:

• papaverine hydrochloride;
• bendazol;
• apressin;
• theobromine.

Phosphodiesterase inhibitor drugs have been used for a long time. But now they are almost not prescribed, as they cause an increase in the work of the heart. New generation drugs, mainly calcium channel blockers, are much more effective. They have minor side effects.

It's important to know! Verapamil cannot be combined with β-blockers. Together, they can cause serious complications in the work of the heart.

Medicines affecting humoral regulation

The body produces a hormone that increases blood pressure - angiotensin. Therefore, drugs have been developed that inhibit its production. These include:

• angiotensin-converting enzyme (ACE) inhibitors;
• angiotensin receptor blockers;
• aldosterone receptor blockers.

ACE inhibitor pills have been used for a long time. A well-known and widely used drug of this group is captopril. It slows down the breakdown of bradycardin (a substance that dilates blood vessels), and has a beneficial effect on the heart. But it is better to use it in combination with diuretics and β-blockers. It causes tachycardia, dry cough, angioedema.

Omapatrilat belongs to the new generation drugs. It inhibits ACE and endopeptidase, which destroys bradycardin, adrenomedulin (vasodilating peptides).

On the this moment drugs that act on angiotensin receptors are being developed. Their action is stronger and longer lasting.

List of AT-receptor blockers:

• losartan;
• irbesartan;
• valsartan;
• telmisartan.

They can cause dizziness, allergies, but side effects are extremely rare. It's important to know! Angiotensin receptor blockers should not be taken by pregnant or lactating women.

Aldosterone inhibitors affect kidney function by reducing the absorption of water and sodium. As a result, the volume of circulating blood decreases, which helps to reduce pressure. by the most effective drug thought to be spironolactone.

But recent studies have shown that men should not take this drug. It is a testosterone antagonist and therefore can cause impotence, feminization.

Among the drugs that affect the humoral regulation of blood pressure, the recently developed drug aliskeren occupies a special place.

It belongs to potent drugs, has a long-lasting effect. A small dose of this drug is enough for a day. And at the same time, it does not cause special side effects. But only a doctor can determine the need to take it and the dosage.

Drugs that affect water-salt metabolism are used to treat hypertension. They reduce the amount of fluid and sodium ions entering the blood, thereby helping to reduce pressure.

Modern diuretic drugs change the response of blood vessels to the effects of various substances. They increase susceptibility to sympatholytics, ganglion blockers. Reduce the effects of norepinephrine and other vasoconstrictors.

List of the most effective diuretics:

• hypothiazide;
• lasix;
• ethacrynic acid;
• aldactone.

Most diuretics remove potassium and magnesium from the body. And these trace elements are important for the functioning of the heart and nervous system. Reducing their number leads to serious complications. Therefore, with diuretics, asparkam and panangin must be prescribed.

What modern antihypertensive drugs are better

All drugs that affect the natural mechanism of pressure regulation are effective in the treatment of hypotension. But each group has its own side effects:

1. Neurotropins inhibit the work of the central nervous system. Cause drowsiness, absent-mindedness. In large doses, they can cause cardiac arrest.. With prolonged use, patients complain of fatigue, depression. Ganglioblockers cause constipation, urinary retention (therefore, diuretics are recommended in combination with them), glaucoma, blurred vision.
2. Myotropic drugs affect all organs. They can disrupt the work of the heart, kidneys, liver.
3. Drugs that affect hormones and enzymes can cause persistent hypotension. They are not recommended for pregnant women and for kidney disease. They also contribute to the appearance of edema and allergies.
4. Diuretics remove the necessary potassium and magnesium from the body. Contribute to an increase in blood lipids and glucose. And this causes the development of atherosclerosis. They are also dangerous for those who have suffered a myocardial infarction or suffer from chronic arrhythmia.

HYPOTENSIVE DRUGS(Greek, hypo- + lat. tensio tension, tension) - medicines that lower blood pressure.

According to the mechanism and localization of action, there are: neurotropic T. e. myotropic G. s. diuretics, angiotensin antagonists and calcium channel blockers.

Neurotropic antihypertensive drugs lead to a decrease in the Underworld by reducing the influence of the sympathetic nervous system on the heart and blood vessels, which leads to a decrease in cardiac output and expansion of peripheral vessels. Depending on the level, on Krom the sympathetic innervation is blocked (see. Autonomic nervous system), neurotropic G. are distinguished. central and peripheral action. To neurotropic G. of page. central action include clonidine and methyldopa.

Clonidine is an active antihypertensive drug, which also has a certain sedative effect. It lowers the tone of the vasomotor center and thereby reduces the descending sympathetic influences, which leads to a reduction in cardiac output, vasodilation and a decrease in the Underworld. The duration of its hypotensive action at the end of a single dose is 6-8 hours. Clonidine is used for the systematic treatment of arterial hypertension, and for the relief of hypertensive crises. In the latter case, it is administered parenterally, more often intravenously, slowly. The most characteristic side effects of clonidine are dry mouth, constipation; in the first days of treatment, drowsiness and lethargy are also observed. With rapid intravenous administration, a peripheral adrenomimetic effect of clonidine may appear in the form of a short-term increase in the Underworld. Treatment with clonidine is forbidden to end unexpectedly, because with a sharp withdrawal of the drug, the development of a hypertensive crisis (withdrawal syndrome) is likely. Before the abolition of clonidine, a gradual (within 7-10 days) decrease in its dose is necessary.

Methyldopa, as well as clonidine, reduces the Underworld due to the inhibition of the vasomotor center and, due to this, a decrease in descending sympathetic influences. In terms of hypotensive activity, it is inferior to clonidine. The hypotensive effect at the end of taking the drug inside begins after 2-5 hours and lasts about 1 day. Use methyldopa for the systematic treatment of arterial hypertension. Side effects of the drug are manifested by drowsiness, depression, dyspeptic disorders, retention of salts and water in the body, and sometimes hematopoietic disorders.

Among neurotropic G. of page. peripheral action, depending on the effect of drugs on different parts of the peripheral sympathetic innervation, there are: ganglion blockers, sympatholytics and adrenoblockers.

Ganglion blockers (see. Ganglion blocking agents) lead to a rapid decrease in the Underworld, due to the blockade of sympathetic influences on the heart and blood vessels at the level of the sympathetic ganglia. In a crust, time as G. of page. they are used in arr. for the relief of hypertensive crises (eg pentamine, benzohexonium), and small-acting drugs (eg hygronium) for controlled hypotension. For the systematic treatment of arterial hypertension, ganglionic blockers in modern honey. In practice, in most cases they are not used, because they cause a large number of side effects.

The sympatholytic agents reserpine and octadine act on the endings of postganglionic sympathetic fibers, causing them to deplete the stores of the mediator - norepinephrine (see Mediators) and thereby reducing the sympathetic effects on the heart and blood vessels. This leads to bradycardia, decreased cardiac output, decreased non-specialized peripheral resistance, and hypotension. These drugs are characterized by a slow development of the hypotensive result (within several days) and its enormous duration: after the termination of treatment with sympatholytics, the hypotensive effect persists for 1-2 weeks. Reserpine is a rauwolfia alkaloid. Along with the hypotensive has a sedative effect. It is used for the systematic treatment of hypertension. It is well tolerated and in small doses, side effects, in most cases, does not cause. High doses of reserpine can lead to drowsiness, diarrhea, shortness of breath, skin rashes, etc. It is part of the combined antihypertensive drugs brinerdine and adelfan, along with other rauwolfia alkaloids, is contained in the drug raunatin (syn. rauvasan). Octadine is superior in efficacy to reserpine. But in honey In practice, it is used much less frequently, because it leads to a number of side effects - dizziness, weakness, diarrhea, swelling, and orthostatic hypotension. He is appointed by arr. with severe forms of hypertension.

Adrenoblocking agents block peripheral adrenergic receptors (see. Adrenomimetic agents) and due to this, weaken the effect of sympathetic innervation and prevent the effect of adrenaline circulating in the blood on the heart and blood vessels, a-Adrenoblockers (prazosin, phentolamine, tropafen), blocking vascular a-adrenergic receptors, lead to vasodilation and hypotension, which, in most cases, is accompanied by the origin of reflex tachycardia. Prazosin differs from other a-blockers in that it leads to a lesser degree of reflex tachycardia. It is used to treat various forms of arterial hypertension. Other a-blockers (phentolamine, tropafen) as G. s. prescribed for the most part in pheochromocytoma. a-, b-Adrenergic blocker labetalol, which blocks both a- and b-adrenergic receptors, has some advantages over a-blockers. Thus, the decrease in vascular resistance caused by it is not accompanied by reflex tachycardia, since labetalol blocks the b-adrenergic receptors of the heart at one moment. In addition, the presence of labetalol b-adrenergic blocking activity enhances its hypotensive effect. Labetalol is used to treat arterial hypertension, and to relieve hypertensive crises.

Very effective G. with. are b-blockers (anaprilin, etc.), the mechanism of hypotensive action to-rykh consists of several components. First of all, drugs in this group slow down and weaken heart contractions and, as a result, reduce cardiac output. The tone of the blood vessels at the beginning of treatment with b-blockers may increase a couple. But with their systematic use, a gradual expansion of blood vessels occurs, which is regarded as a compensatory reaction in response to a decrease in cardiac output. In addition, b-blockers reduce the secretion of renin by the kidneys, and some of them have a depressing effect on the vasomotor center. β-blockers are used for the systematic treatment of arterial hypertension, mostly in young people with a hyperdynamic type of blood circulation, i.e., with increased heart function.

Myotropic antihypertensive drugs act specifically on the smooth muscles of the vessels, causing them to expand and decrease due to this Hell. Some drugs in this group, for example, apressin, diazoxide and minoxidil, lower the Underworld, acting mainly on arterioles. They have little effect on the tone of the veins and, therefore, do not cause orthostatic hypotension.

Apressin acts for 6-12 hours. Treatment with apressin may be accompanied by tachycardia and increased cardiac output, since the sympathetic nervous system is reflexively activated. As a result, apressin is recommended to be prescribed in combination with b-blockers. In addition, when using apressin, dizziness, pain in the heart area, nausea, vomiting, erythematous skin rashes can appear.

Diazoxide is characterized by high hypotensive activity, but its effect is fully manifested only with intravenous administration of the drug. Based on this, it is used for the most part for the relief of hypertensive crises.

Minoxidil is superior in antihypertensive activity to diazoxide and, unlike it, is effective when taken orally. It acts for a long time (24 hours or more), since it selectively accumulates in the vascular wall. The drug often turns out to be effective in those cases, at a time when other G. s. do not give the desired result, for example, in malignant hypertension.

To myotropic G. of page. acting both on arterioles, and on veins, sodium nitroprusside belongs, to-ry is the most effective preparation of this group. It is effective only when administered intravenously and does not last long, and therefore it is used mainly for the relief of hypertensive crises.

To myotropic G. of page. also include dibazol and magnesium sulfate (see Magnesium). Dibazol, when administered orally, is ineffective, therefore, it is prescribed much more often intravenously for the relief of hypertensive crises. Magnesium sulfate besides apply hl. arr. with hypertensive crises, prescribing it along with this intramuscularly.

Diuretics. Diuretics play an important role in the treatment of arterial hypertension. Their hypotensive effect is due to the ability to remove sodium ions and water from the body. Most extensively as G. with. use dichlothiazide, furosemide, clopamide, etc. These drugs have a moderate hypotensive effect. In addition, they enhance the effects of other G. s. for example, clonidine, methyldopa, sympatholytics, apressin, and therefore diuretics in most cases are combined with these antihypertensive drugs.

Angiotensin antagonists. For the treatment of certain forms of arterial hypertension as G. s. medicines are offered, influence to-rykh is connected with elimination of influence of angiotensin II — endogenous pressor polypeptide. Such drugs are called angiotensin antagonists. They render the expressed hypotensive effect of hl. arr. with an increased content of angiotensin II in the blood, in particular with renovascular hypertension. According to the mechanism of action among angiotensin antagonists, angiotensin receptor blockers, for example, saralazine, and angiotensin-converting enzyme inhibitors that interfere with the formation of angiotensin II from angiotensin I, for example, captopril (syn. skin) are distinguished. From the preparations of this group to honey. practice apply ch. arr. captopril, to-ry is used for the systematic treatment of arterial hypertension caused by an increased content of angiotensin II in the blood.

Calcium channel blockers (syn. calcium antagonists). The hypotensive effect of this group of drugs is due to the fact that they block the calcium channels of cell membranes and interfere with the entry of calcium ions into myocardial cells and smooth muscle cells of the vascular wall. This leads to a decrease in cardiac output, vasodilation and a decrease in the Underworld. Calcium channel blockers also have an antianginal and antiarrhythmic effect, reduce platelet aggregation. For the treatment of arterial hypertension from the drugs of this group, fenigidin (syn. nifedipine) and verapamil (syn. isoptin) are prescribed.

So, G. s. represented by a large number medicines, belonging to different pharmacol, groups and owning different mechanisms and localization of action. In modern pharmacotherapy of arterial hypertension, the fundamental principle is the combined use of drugs from groups that differ in mechanism and localization of action, which allows one moment to influence a couple of links in the regulation of the Underworld and increases the effectiveness of antihypertensive therapy.

The main antihypertensive drugs are given in the table.

Brief Medical Encyclopedia. publishing house "Soviet Encyclopedia", second edition, 1989, Moscow

Content

The group of drugs that have an antihypertensive effect is very diverse and includes drugs from many chemical classes. The use of drugs in this category is advisable for the treatment of arterial hypertension and other pathological conditions characterized by spasm of peripheral vessels.

General information about hypertension

In medical practice, the term "hypertension" is used to refer to a condition in which there is an increase in hydrostatic pressure in the hollow organs and cavity formations of the body. This concept is often used in relation to essential hypertension (hypertension), which is one of the most common types of hypertension, accounting for 90-95% of all cases. The main symptom of the disease is a steady increase in blood pressure, which is a consequence of various reasons and can lead to the development of serious complications.

Depending on the causative factors, hypertension is divided into several varieties. The main types of hypertension are essential (represented directly by hypertension) and symptomatic (in which an increase in pressure occurs along with the appearance of other symptoms of a disease). Other types of hypertension that are much less common include:

• renovascular (occurs due to narrowing of the renal arteries with impaired blood supply to the kidneys);
• venous (the cause is an increase in hydrostatic pressure in the veins);
• intracranial (due to swelling of the brain, which can occur in the presence of malignant neoplasms in the cranial cavity, hypersecretion of cerebrovascular fluid or a violation of its outflow);
• hemodynamic (occurs due to a sharp increase in cardiac output and an increase in peripheral vascular resistance);
• hyperkinetic (due to an increase in the minute volume of blood circulation with unchanged vascular resistance);
• other types (about 40).

The symptomatology of the pathology depends on its type and stage, but the signs of the disease are very pronounced, and they cannot be ignored. Treatment of hypertension in the absence of direct indications for surgical intervention is carried out by conservative methods with the use of antihypertensive agents. The action of drugs in this group is based on the effect on the mechanism of formation high blood pressure, which is due to the following main points:

• minute volume of blood circulation (or cardiac output) - a change in value occurs with an increase in the frequency of contractions of the heart muscle;
• peripheral vascular resistance - the total contractile force of the arteriole system (small arteries preceding the capillaries);
• total volume of circulating blood - the total volume of liquid blood in functioning vessels (including deposited blood - currently located in the liver, kidneys and other organs, temporarily not taking part in blood circulation).

Classification of antihypertensive drugs

Many factors can act as a trigger for primary hypertension - from stressful conditions to pathological changes in the vascular walls, which increase the permeability of their membranes for sodium, potassium and calcium ions. An important role in the development of high blood pressure is played by the activation of the renin-angiotensin-aldosterone system (the secretion of hormones that regulate the total volume of blood in the body).

Regardless of the underlying causes of hypertension, the main pathogenic factors remain an increase in cardiac output and peripheral vascular resistance, so antihypertensive therapy is aimed at weakening their influence. The goal of treating hypertension is to lower blood pressure to normal levels (below 140/90 mmHg), which is achieved through lifestyle modification (primary measure) and the use of antihypertensive medications.

To influence the cause of high blood pressure and minimize the risk of complications from the cardiovascular system, scientists in the pharmaceutical industry have developed several groups of antihypertensive drugs, each of which has specific characteristics. When drawing up a scheme for drug therapy of hypertension, the doctor, based on the protocol principles for the treatment of this disease, selects one or more drugs from the following classification groups of antihypertensive drugs:

• neurotropic:

1. Sedatives (tranquilizers, sedatives, herbal remedies).
2. Antiadrenergic (central action, peripheral (ganglioblockers, sympatholytics, alpha-blockers, beta-blockers, alpha-beta-blockers).

• myotropic:

1. calcium antagonists.
2. Potassium channel activators.
3. Donators of nitric oxide.
4. Other.

• drugs that affect the renin-angiotensin system:

1. Angiotensin-converting enzyme (ACE) inhibitors.
2. Angiotensin receptor antagonists.
3. Other.

• means that affect the water-salt metabolism:

1. Diuretics (saluretics, benzothiazine derivatives, osmotic).
2. Aldosterone receptor blockers.

• combined antihypertensive drugs (Adelfan, Trirezide, Brinerdin, Sinipress).

Antiadrenergics

The hormone of the adrenal medulla, norepinephrine, is involved in the mechanism of increasing blood pressure. At nervous tension, stress, other emotional upheavals, there is an increase in the level of norepinephrine in the blood, which leads to a sharp increase in cardiac output and, as a result, an increase in pressure. Such effects are provided by the reaction of specific receptors that are sensitive to adrenergic substances (adrenaline and noradrenaline) - adrenoreceptors.

In the course of scientific research, the ability of certain substances to block adrenoreceptors was discovered, depriving adrenergic elements of the ability to act on them. Blockade of alpha receptors leads to obstruction of the effect of norepinephrine on the vessels, and beta receptors on the heart and bronchi. This discovery has found wide application in medical practice. Drugs containing substances that can act on adrenoreceptors are called antiadrenergic drugs and are widely used in antihypertensive therapy.

The main effects that determine the range of indications for antiadrenergic drugs for use are the normalization of blood and intraocular pressure, antiarrhythmic action and a decrease in myocardial (middle muscle layer of the heart) oxygen demand. Antihypertensive therapy with the use of this group of drugs in most cases is supplemented with diuretics and cholinomimetics. According to the type of action, antiadrenergics are divided into central and peripheral.

central action

The main antihypertensive effects of centrally acting antiadrenergics are due to inhibition of the activity of pressor neurons of the vasomotor center (a set of nerve cells that regulate vascular tone and heart rate). The result of these processes is a decrease in the overall tone of sympathetic innervation, manifested in:

• decrease in cardiac output (due to a decrease in the frequency of contractions of the heart muscle);
• vasodilation;
• decrease in total peripheral vascular resistance.

Antihypertensive drugs belonging to the group of central antiadrenergics are represented by Clonidine (Clonidine, Gemiton), Guanfacine (Estulik), Methyldofoy (Dopegid), Moxonidine (Cint). These drugs differ in the duration of the antihypertensive effect, the mechanism of action and the severity of side effects, so the doctor should make a decision on the use of drugs of this pharmacological group for the treatment of hypertension. The main characteristics of popular central antiadrenergics are:

Peripheral action

According to the international anatomical-therapeutic-chemical classification medicines(ATC), antihypertensive drugs that have an antiadrenergic effect of the peripheral type, belong to the code CO2C. This section of the ATC includes 3 subsections:

• alpha-adrenergic blockers (CO2CA);
• alpha-beta-blockers (CO2CB);
• guanethidine derivatives (CO2CC).

The antihypertensive treatment regimen may include drugs whose mechanism of action also includes an effect on peripheral receptors, but, according to ATC, they belong to other pharmacological groups (such as beta-blockers (C07A), ganglioblockers (C02B), sympatholytics ( С02LA)). Drugs are divided into subgroups based on similar pharmacodynamics and therapeutic effect. The main features of this group are:

Drugs affecting the renin-angiotensin renal system

The hormonal system that is actively involved in the regulation of blood pressure and circulating blood volume is called renin-angiotensin. This name is due to the components that make up this system - renin (an enzyme produced by the kidneys in response to a decrease in renal pressure) and angiotensin (an oligopeptide hormone formed under the action of renin or ACE and causing vasoconstriction).

ACE, which indirectly participates in the renin-angiotensin cascade of reactions, is the target of many inhibitory drugs, and some antihypertensive drugs target angiotensin specifically. Medicines of both directions belong to the same ATX code - C09 (drugs acting on the renin-angiotensin system), which includes:

• monocomponent and combined ACE inhibitors (C09A, C09B);
• simple preparations of antagonists and combined agents of angiotensin II inhibitors (С09С, С09D);
• other drugs that affect the renin-angiotensin system (C09X).

Means of this group increase natriuresis (sodium excretion in the urine) and total diuresis (the volume of urine excreted), but do not affect the total volume of circulating blood. Drugs are allowed to be taken long time(up to 4 years). To enhance the antihypertensive effects provided, it can be combined with diuretics and other vasodilators. The inclusion of drugs that affect the renin-angiotensin system into the antihypertensive treatment regimen is advisable for:

• symptomatic arterial hypertension caused by impaired blood flow in the kidneys (renal, renovascular);
• the patient's resistance to traditional drugs that reduce blood pressure (or if they are intolerant);
• complex violation of hemodynamics;
• combination of hypertension and sclerosis.

Of the side effects that may accompany the use of drugs in this group, the most common are headaches, dizziness, redness. skin upper body, change in taste sensations. The pharmacological action that determines the therapeutic effects of drugs acting on the renin-angiotensin system is as follows:

A new development in the field of antihypertensive drugs is Omapatrilat, a drug related to vasopeptidase inhibitors (ACE and neutral endopeptidase). The drug is prescribed for mild to moderate hypertension to reduce systolic and diastolic blood pressure without changing the heart rate. Along with properties similar to ACE inhibitors, the drug is able to eliminate the imbalance between pressor (vasoconstrictor) and depressor (inhibitory) reactions, which provides a cardioprotective effect.

Means of myotropic action

Antihypertensive drugs, which include substances that cause relaxation of smooth muscle fibers of blood vessels, belong to the group of myotropic drugs. Due to a decrease in vascular tone, the lumen of the vessels expands, which leads to a decrease in blood pressure. The vasodilatory effect is provided by various mechanisms that serve as a classification feature for dividing myotropic drugs into subgroups:

• blockade of calcium channels of cell membranes of smooth muscle fibers - calcium channel blockers;
• opening of potassium channels for cell membrane hyperpolarization - potassium channel activators;
• a decrease in the concentration of free potassium ions by stimulating cytosolic guanylate cyclase - nitric oxide donators;
• in other ways.

The vasodilatory (vasodilating) effect of myotropic antihypertensive drugs differs in duration and severity therapeutic effect. Popular tools in this group include the following:

Diuretics

Diuretics are used in the treatment of hypertension to remove excess fluid from the body, which may be the cause or effect of high blood pressure. The group of diuretic antihypertensive drugs includes heterogeneous chemical composition and how the drug works. A common factor for classifying drugs as diuretics is their ability to temporarily increase the excretion of water and minerals through the urine.

Depending on the nature of the impact on the body, diuretics are divided into renal (realizing the effect through the kidneys) and extrarenal (acting indirectly through other organs). The mechanism of pharmacological action determines the division of diuretics into types:

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Lecture No. 18

antihypertensive (antihypertensive) drugs

Used to treat hypertension.

Principles of treatment of hypertension

decrease in OPPS - vasodilators (vasodilators).

decrease in cardiac work and decrease in cardiac output. Beta blockers.

decrease in BCC - diuretics (diuretics).

decrease in renin production, activation of the RAAS and the formation of angiotensin II.

decrease in blood clotting.

6) normalization of the lipid spectrum.

7) reduction of neuropsychic stress.

classification of antihypertensive

funds according to the mechanism of action

Neurotropic drugs: means of suppressing SDC , ganglioblockers, sympatholytics, α-, β-AB, α- and β-AB, sedatives.

Myotropic drugs: PDE inhibitors, NO donators, calcium blockers and potassium channel activators, various agents.

Means affecting the RAAS.

Diuretics.

Combined drugs.

antihypertensive agents

central action

Clonidine (clonidine)

Stimulates postsynaptic α 2 -AR and imidazoline I 1 -receptors of neurons of the nuclei of the solitary tract in the medulla oblongata. This leads to suppression of the SDC, a decrease in the tone of the sympathetic innervation and vasodilation.

Increases the tone of the vagus nerves, causes bradycardia and a decrease in cardiac output.

Stimulates peripheral presynaptic α 2 -AR and reduces the release of norepinephrine from nerve endings.

Depresses the central nervous system, has a sedative and hypnotic effect, potentiates the action of hypnotics, psychotropic drugs, alcohol; It is a non-opioid centrally acting analgesic.

Reduces the production of intraocular fluid and reduces intraocular pressure.

The duration of action is 5-12 hours, it is used orally, parenterally, as part of eye drops.

Applies with hypertension stage 1-2, for the relief of hypertensive crisis, with glaucoma.

Side effects: with rapid intravenous administration, hypertension, drowsiness, lethargy, dry mouth, constipation, respiratory depression in children, retains sodium and water in the body, causes withdrawal syndrome (for its prevention, the drug is canceled gradually, within 10-40 days).

Guanfacine - similar to clonidine, acts longer, is prescribed once a day.

Methyldopa (dopegyt) - turns into alpha-methylnorepinephrine, which stimulates the central α 2 -AR and inhibits the SDC. In high doses, it reduces the content of norepinephrine, dopamine and serotonin in brain tissues and most peripheral tissues. Depresses the central nervous system.

Moxonidine (Physiotens, Cint) - selective agonist I 1-imidazoline receptors. It inhibits SDC and dilates blood vessels, reduces the production of renin, AT II, ​​aldosterone, reduces heart function, reduces left ventricular hypertrophy, and has a sedative effect. It has a pronounced hypotensive effect, is prescribed once a day.

Beta blockers

They reduce the work of the heart, reduce cardiac output, depress the central nervous system, reduce renin secretion and RAAS activity, restore the baroreceptor depressor reflex, dilate blood vessels with prolonged use (reduce central sympathetic effects on the heart and blood vessels, reduce the release of norepinephrine from presynaptic endings).

SUBSTANCES AFFECTING THE RAAS

Decreasing renin secretion

- adrenoblockers

Violating the formation of antibodiesII.

A) ACE inhibitors (angiotensin-converting enzyme) - ACE inhibitors captopril (Capoten), enalapril (Enap), etc.

B) vasopeptidase inhibitors - omapatrilat

II(AT 1 )

losartan (cozaar), valsartan (diovan)

Aldosterone antagonists

spironolactone (veroshpiron)

The cardiovascular effects of AT II, ​​mediated by AT 2 - receptors, are opposite to the effects of excitation of AT 1 - receptors. Stimulation of AT 2 - receptors is accompanied by vasodilation, inhibition of cell growth, suppression of proliferation of endothelial and smooth muscle cells and fibroblasts, inhibition of cardiomyocyte hypertrophy.

ACE inhibitors (angiotensin converting enzyme)

1st generation - captopril, 2nd generation - enalapril, lisinopril, perindopril, etc.

Mechanism of action:

They disrupt the transition of AT I to AT II and, in this regard, reduce the tone of arterial and venous vessels, reduce systolic and diastolic blood pressure, the load on the heart, increase blood flow in the organs.

Inhibition of ACE leads to the accumulation of bradykinin, prostacyclin, PG E 2 and other vasodilators.

The hypertrophy of the myocardium and blood vessels decreases, the contractility of the heart increases, and the signs of heart failure decrease.

Increased diuresis.

Application: essential and symptomatic renal hypertension, chronic heart failure, diabetic nephropathy.

Side effects: hypotension, allergic reactions, dry, persistent cough associated with the accumulation of bradykinin (not stopped by codeine), dyspeptic disorders, hyperkalemia.

It is important to consider that ACE inhibitors do not completely block the synthesis of AT II. RAAS is found in many tissues. In particular, in the heart, where the formation of AT II from AT I is catalyzed by the chymase enzyme. Therefore, the RAAS blockers of AT 1 receptors are most completely turned off.

Omapatrilat blocks ACE and neutral endopeptidase, which inactivates endogenous peptides that dilate blood vessels. Therefore, it eliminates the imbalance between pressor and depressor influences.

Applies with GB, chronic heart failure.

Side effects: headache, cough, diarrhea.

Angiotensin receptor blockersII(AT 1 )

Losartan, valsartan, telmisartan, etc. The mechanism of the hypotensive action of these drugs is associated with the development of the following effects:

1. Blockade of AT 1 - receptors prevents the adverse effect of AT II on vascular tone and is accompanied by a decrease in blood pressure.

2. Long-term use of these drugs leads to a weakening of the proliferation of vascular smooth muscle cells, a decrease and even reverse development of left ventricular hypertrophy.

3. Against the background of blockade of AT 1 - receptors, AT II stimulates AT 2 - receptors and dilates blood vessels, reduces the load on the heart.

4. In addition, angiotensins 1-7 are formed from AT I and II, which stimulate AT x receptors, increase the release of NO, PG E and PC and have a vasodilatory, natriuretic and antiplatelet effect.

All AT 1 receptor blockers act gradually, the antihypertensive effect develops smoothly and lasts up to 24 hours. To increase the effectiveness of therapy, it is recommended to combine these drugs with diuretics: Gizaar (losartan + hydrochlorothiazide), Co-diovan (valsartan + hydrochlorothiazide) and others.

Inhibitors of AT 1 - receptors are contraindicated in individual hypersensitivity, pregnancy and lactation, since experimental data on animals indicate that drugs that affect the RAAS can cause damage to the fetus, death of the fetus and newborn.

myotropic vasodilators

Blockers of slow calcium channels.

They inhibit the entry of calcium into the cell, dilate arterioles and veins, and reduce systemic arterial pressure. Improve blood supply to vital organs (heart, brain, kidneys). Dihydropyridines (nifedipine, nitrendipine and felodipine) are most effective in arterial hypertension.

Anticalcium drugs apply with moderately severe hypertension, hypertensive crises (nifedipine under the tongue), supraventricular tachyarrhythmias and angina pectoris. For systemic use, it is better to use long-acting drugs.

Potassium channel activators.

Minoxidil, diazoxide.

Minoxidil. Expands arterioles, reduces systolic and diastolic blood pressure, reduces the load on the myocardium, causes reflex tachycardia and an increase in cardiac output. Increases renin activity and retains sodium and water in the body.

Stimulates hair growth in androgen-dependent alopecia, as it dilates blood vessels and improves microcirculation in the skin and trophism of hair follicles.

Application. Particularly severe forms of arterial hypertension, resistant to combination therapy with other antihypertensive drugs; in the form of a solution for external use regine for the treatment of alopecia.

DonorsNO.

Sodium nitroprusside. Mechanism of action. Expands arterioles and veins, which leads to a decrease in blood pressure. With a single-stage intravenous administration, it lasts 1-2 minutes. Therefore, it is administered intravenously in case of hypertensive crises, heart failure, for controlled hypotension.

Side effects: tachycardia, headache, dyspeptic disorders.

Phosphodiesterase inhibitors.

Papaverine is an opium alkaloid of the isoquinoline series. Mechanism of action. It has not only a hypotensive, but also an antispasmodic effect: it reduces the tone of the smooth muscles of the bronchi, gastrointestinal tract, and the genitourinary system. It is used as part of combined preparations for the treatment of hypertension, with spasms of cerebral vessels, with colic, with a hypertensive crisis.

Various myotropic agents.

Bendazole - It has antispasmodic, antihypertensive and immunostimulating effects. Blood pressure decreases as peripheral vessels dilate and cardiac output decreases. The hypotensive activity of dibazol is very moderate, and its effect is short-lived. In hypertension, it is usually prescribed in combination with other antihypertensive drugs. It is used in / in for the relief of a hypertensive crisis.

The immunostimulatory effect is associated with an increase in the synthesis of nucleic acids, proteins and interferon, the formation of antibodies, and an increase in phagocytosis.

Magnesium sulfate- inhibits SDC, inhibits the transmission of excitation in the autonomic ganglia, has a direct myotropic effect, inhibiting the entry of calcium into the cell. It is used to stop a hypertensive crisis.

The latest generation of antihypertensive drugs play an increasing role in the treatment of hypertension in individuals different ages. It is no secret that not only the elderly suffer from high blood pressure, but also younger patients, therefore this problem poses a real danger from a young age.

Pharmaceutics is constantly being improved, new drugs are being invented that lower blood pressure, which can significantly alleviate the condition of sick people. As for the latest generation of antihypertensive drugs, they differ not only in their effectiveness, but also in fewer side effects. In this article, we will consider the drugs of this group in more detail, as well as their main features.

Features of antihypertensive drugs

Arterial hypertension occurs when there is a narrowing of the lumen of blood vessels caused by spasm of smooth muscle tissue.

One of the most popular drugs related to AA-2 is the drug. It has a very strong effect, completely absorbed into the body. In most cases, Losartan is quite well tolerated, so the likelihood of side effects is practically excluded. However, doctors do not recommend using this remedy during gestation and lactation. FREE OF CHARGE.

What tool to choose?

I would like to note right away that the decision to use this or that drug is made only by the attending physician. Naturally, he must refer the patient to various laboratory tests so that the picture of the disease is clearer.
However, each group of drugs that reduce blood pressure has a number of negative effects on the body:

• Drugs that block beta-adrenergic receptors differ in that they have a depressant effect on the central nervous system. Moreover, if the dosage is repeatedly exceeded, then there is a real danger of cardiac arrest.
• Calcium channel blocking drugs can help lower blood pressure readings below normal. There is also a possibility of violation of the functions of internal organs.
• Diuretics are potent diuretics, resulting in flushing useful substances from the body. In particular, we are talking about magnesium and potassium.

As we can see, even the latest generation drugs can cause many unpleasant side effects. In fairness, it should be noted that this often happens through the fault of the patient himself, who independently starts taking this or that remedy, without really understanding the principle of its action.

That is why, only the attending physician should select the drug, based on the results of tests and concomitant human diseases. Among the new names of drugs that have shown themselves well in the fight against arterial hypertension, one can name Rasilez, and Olmesartan.