Antihypertensive drugs list of drugs. Combined modern antihypertensive drugs. What are the features of diuretics

Previously, the pressure was lowered using the usual foxglove. Over time, the drugs were gradually improved. But mortality from hypertension and the complications it causes was high. Various antihypertensive medicines are developed annually. New generation drugs are constantly appearing, which are not only effective, but also give fewer side reactions.

What should be antihypertensive drugs

The normal level of blood pressure depends on the vascular tone. When they spasm, caused by the 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 dilate blood vessels. The means made on the basis of foxglove did quite well with this. However, the mortality rate from hypertension was high. Mainly due to complications caused by the disease and the 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 effects 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 either. They are being improved, creating effective remedies for hypertension.

Modern hypertensive

For the treatment of hypertension, medications belonging to different groups are used. Complex preparations give the greatest effect. They not only reduce blood 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 medications are classified according to how they alter normal pressure regulation.

List of groups of effective antihypertensive drugs:

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

Thanks to this variety, 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 drugs

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

1. Sedatives (clonidine guanfacine, rilmenidine, methyldopa). Affect the vasomotor center located in the cerebral cortex, thus forcing smooth muscles to relax. As a result, the walls of blood vessels expand and the pressure decreases. But they cause drowsiness.
2. Ganglion blocking agents (pentamine, benzohexonium). They act on the nerve nodes that innervate the muscle tissue. But their use leads to a decrease in the tone of all organs. They can cause constipation, 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). Decreases 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, and lower the level of norepinephrine. Therefore, these drugs are considered the most effective antihypertensive agent.

Drugs with neurotropic action reduce blood pressure well, have a beneficial effect on the work of the heart, and β-blockers and on the kidneys. But they can cause a ton of side effects. Overdose of sedatives can cause cardiac arrest. Adrenergic blockers 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 is important to know! Abrupt cessation of neurotropic medication leads to a rapid and persistent increase in blood pressure.

Myotropic drugs

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

Calcium channel blockers:

• phenigidine;
• diltiazem;
• isradipine;
• verapamil.

Potassium channel activators:

• minoxidil;
• diazoxide.

Stimulants of the formation of nitric oxide:

• sodium nitroprusside;
• molsidomin.

Phosphodiesterase inhibitors:

• papaverine hydrochloride;
• bendazole;
• apressin;
• theobromine.

Phosphodiesterase inhibiting drugs have been used for a long time. But now they are almost never prescribed, since they cause an increase in the work of the heart. New generation drugs, mainly those related to calcium channel blockers, are much more effective. They have few side effects.

It is important to know! Verapamil can not be combined with β-blockers... Together, they can cause serious complications in the heart.

Medicines affecting humoral regulation

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

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

ACE-inhibiting pills have been used for a long time. A well-known and widely used drug in this group is captopril. It slows down the breakdown of bradycardin (a substance that dilates blood vessels), 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.

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

At the moment, drugs are being developed that affect angiotensive receptors. Their effect 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 is important to know! Angiotensin receptor blockers should not be taken by pregnant or lactating women.

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

But recent studies have shown that it is undesirable for men to take this drug. It is a testosterone antagonist and therefore can cause impotence, feminization.

Among the drugs that affect the humoral regulation of pressure, a special place is occupied by the recently developed drug aliskeren.

It belongs to potent drugs, has a long-lasting effect. A small dose of this drug is enough for a day. Nor does it cause any 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 bloodstream, thereby reducing pressure.

Modern diuretics alter the reaction 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. A decrease in their number leads to serious complications. Therefore, with diuretics, asparkam and panangin are necessarily prescribed.

What modern antihypertensive drugs are better

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

1. Neurotrophins inhibit the central nervous system. They cause drowsiness, distraction of attention. In large doses, they can cause cardiac arrest... With prolonged use, patients complain of fatigue, depression. Ganglion blockers 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 essential potassium and magnesium from the body. Promote 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 MEDICINES (Greek, hypo- + lat. tensio tension, tension) - medicines that lower blood pressure.

The mechanism and localization of action are distinguished: neurotropic I. e. myotropic G. of page. 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. The vegetative nervous system), neurotropic G. of page is distinguished. central and peripheral action. To neurotropic G. of page. central actions include clonidine and methyldopa.

Clonidine is an active antihypertensive drug that 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, vasodilatation and a decrease in the Underworld. The duration of its antihypertensive 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, often intravenously, slowly. The most common side effects of clonidine are dry mouth, constipation; in the first days of treatment, drowsiness and lethargy are also observed. With a rapid intravenous administration, the 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, since with a sharp withdrawal of the drug, the development of a hypertensive crisis is likely (withdrawal syndrome). Before canceling clonidine, a gradual (within 7-10 days) decrease in its dose is necessary.

Methyldopa, as well as clonidine, reduces the underworld by inhibiting the vasomotor center and, thanks to this, decreasing the 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 for about 1 day. Use methyldopa for the systematic treatment of arterial hypertension. A side effect of the drug is manifested by drowsiness, depression, dyspeptic disorders, retention of salts and water in the body, and from time to time disorders of hematopoiesis.

Among neurotropic G. of page. peripheral action, depending on the effect of drugs on different links of the peripheral part of the sympathetic innervation, are distinguished: ganglion blockers, sympatholytics and adrenergic blockers.

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 crust, time as G. with. they are used by Ch. 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, ganglion blockers in modern honey. in practice, in most cases, they are not used, because they cause a large number of side effects.

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 the 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, it has a sedative effect. It is used for the systematic treatment of hypertension. It is well tolerated and, in small doses, does not cause side effects in most cases. 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, it is contained in the preparation raunatin (syn. Rauvazan). Octadine is more effective than reserpine. But honey. practice is used much less often, because it leads to a number of side effects - dizziness, weakness, diarrhea, edema, and orthostatic hypotension. He is appointed by ch. arr. with serious forms of hypertension.

Adrenergic blocking agents block peripheral adrenergic receptors (see Adrenomimetic agents) and thereby weaken the effect of sympathetic innervation and prevent the effects of adrenaline circulating in the blood on the heart and blood vessels, a-blockers (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 extent to reflex tachycardia. It is used to treat various forms of arterial hypertension. Other a-adrenergic blockers (phentolamine, tropafen) as G. of page. prescribed for the most part with pheochromocytoma. a-, b-blocker labetalol, which blocks both a- and b-adrenergic receptors, has certain advantages over a-blockers. So, the decrease in vascular resistance caused by it is not accompanied by reflex tachycardia, since labetalol at one moment blocks the b-adrenergic receptors of the heart. In addition, the presence of b-adrenergic blocking activity in labetalol enhances its hypotensive effect. Labetalol is used to treat arterial hypertension and to relieve hypertensive crises.

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

Myotropic antihypertensive drugs act specifically on the smooth muscles of the vessels, causing them to expand and decrease thanks to this Hell. Certain drugs of this group, for example, apressin, diazoxide and minoxidil, lower the underworld, acting mainly on arterioles. They affect the tone of the veins insignificantly 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, it is recommended to prescribe apressin in combination with b-blockers. In addition, when using apressin, dizziness, pain in the heart, nausea, vomiting, and erythematous skin rashes may 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 mostly for the relief of hypertensive crises.

Minoxidil is superior in hypotensive activity to diazoxide and, unlike it, is effective when taken internally. 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, while other G. of page. do not give the desired result, for example, in malignant hypertension.

To myotropic G. of page. acting on both arterioles and veins, sodium nitroprusside belongs, to-ry is the most effective drug of this group. It is effective only when administered intravenously and acts for a short time, 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 to relieve hypertensive crises. Magnesium sulfate is also used by Ch. arr. with hypertensive crises, prescribing it along with this intramuscularly.

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

Angiotensin antagonists. For the treatment of certain forms of arterial Hypertension as G. of page. drugs are proposed, the effect of which is associated with the elimination of the effect of angiotensin II - an endogenous pressor polypeptide. Such drugs are called angiotensin antagonists. They have a pronounced 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, angiotensin receptor blockers, for example, saralazin, and angiotensin-converting enzyme inhibitors, which interfere with the formation of angiotensin II from angiotensin I, for example, captopril (syn. Skin), are isolated among angiotensin antagonists. From drugs of this group to honey. practice apply Ch. arr. captopril, to-ry used for the systematic treatment of arterial hypertension caused by the increased content of angiotensin II in the blood.

Calcium channel blockers (syn. Calcium antagonists). The hypotensive effect of drugs in this group is due to the fact that they block calcium channels of cell membranes and interfere with the flow 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. In addition, calcium channel blockers have an antianginal and antiarrhythmic effect, and reduce platelet aggregation. For the treatment of arterial hypertension from the drugs of this group, phenigidine (syn. Nifedipine) and verapamil (syn. Isoptin) are prescribed.

So, G. with. are represented by a large number of drugs belonging to different pharmacol, groups and possessing different mechanisms and localization of action. In modern pharmacotherapy of arterial hypertension, the fundamental principle is the combined use of drugs from groups of different mechanisms and localization of action, which allows at one moment to influence a pair of Hell's regulation links and increases the effectiveness of antihypertensive therapy.

The main antihypertensive drugs are listed 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 of many chemical classes. The use of medicines of this category is advisable for the treatment of arterial hypertension and other pathological conditions characterized by spasm of peripheral vessels.

Overview of Hypertension

In medical practice, the term "hypertension" is used to denote a condition in which there is an increase in hydrostatic pressure in the hollow organs and cavities of the body. This concept is often used in relation to hypertension (hypertension), which refers to the most common type 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 types. 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:

• vasorenal (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 cerebral edema, 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 symptoms 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 using antihypertensive drugs. The action of drugs in this group is based on the effect on the mechanism of the formation of 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);
• the total volume of circulating blood - the total volume of liquid blood in the functioning vessels (including and deposited - located at the current time in the liver, kidneys and other organs, temporarily not taking part in the blood circulation).

Classification of antihypertensive drugs

The trigger mechanism of primary hypertension can be many factors - 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 blood volume in the body).

Regardless of the underlying causes of hypertension, the main pathogenic factors are increased cardiac output and peripheral vascular resistance, therefore antihypertensive therapy is aimed at weakening their influence. The goal of hypertension treatment is to lower blood pressure to normal values \u200b\u200b(below 140/90 mm Hg), which is achieved through lifestyle modification (first priority) and taking antihypertensive medications.

To influence the cause of an increase in blood pressure and minimize the risks 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 drug therapy regimen for hypertension, the doctor, based on the protocol principles for treating this disease, chooses one or more drugs from the following classification groups of antihypertensive drugs:

• neurotropic:

1. Sedatives (tranquilizers, sedatives, herbal remedies).
2. Antiadrenergic (centrally acting, peripheral (ganglionic blockers, sympatholytics, alpha-blockers, beta-blockers, alpha-beta-blockers).

• myotropic:

1. Calcium antagonists.
2. Potassium channel activators.
3. Nitric oxide donors.
4. Others.

• drugs affecting the renin-angiotensive system:

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

• agents affecting water-salt metabolism:

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

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

Antiadrenergic drugs

The hormone of the adrenal medulla - norepinephrine - is involved in the mechanism of increasing blood pressure. With nervous tension, stress, and other emotional upheavals, the level of norepinephrine in the blood increases, 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 sensitive to adrenergic substances (adrenaline and norepinephrine) - adrenergic receptors.

In the course of scientific research, the ability of some substances to block adrenergic receptors was discovered, depriving adrenergic elements of the ability to act on them. Blockade of alpha receptors leads to the inhibition 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. Medicines that contain substances that can act on adrenergic receptors are called antiadrenergic drugs, and are widely used in antihypertensive therapy.

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

Central action

The main antihypertensive effects of centrally acting antiadrenergic drugs 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 general tone of sympathetic innervation, manifested in:

• a 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 antiadrenergic drugs are represented by Clonidine (Clonidine, Gemiton), Guanfacin (Estulik), Methyldofy (Dopehyde), Moxonidine (Cynt). These drugs differ in the duration of the antihypertensive effect, the mechanism of action and the severity of side effects, therefore, the doctor should make the decision on the use of medicines of this pharmacological group for the treatment of hypertension. The main characteristics of popular central antiadrenergic drugs are:

Peripheral action

According to the international anatomical, therapeutic and chemical classification of drugs (ATC), antihypertensive drugs that have an antiadrenergic effect of the peripheral type are classified as CO2C. This ATX section includes 3 subsections:

• alpha-adrenergic receptor blockers (CO2CA);
• alpha-beta-blockers (C02CB);
• derivatives of guanethidine (C02CC).

The antihypertensive treatment regimen may include drugs, the mechanism of action of which also affects peripheral receptors, but, according to ATC, they belong to other pharmacological groups (such as beta-adrenergic blocking agents (C07A), ganglion blockers (C02B), sympatholytics ( С02LА)). The drugs are divided into subgroups based on similar pharmacodynamics and therapeutic effect. The main characteristics of the funds in this group include:

Drugs affecting the renin-angiotensin system

The hormonal system actively involved in the regulation of blood pressure and blood volume is called the renin-angiotensin system. 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 by renin or ACE and causing vasoconstriction).

ACE, which is indirectly involved in the renin-angiotensin cascade of reactions, is a target for many inhibitory drugs, and some antihypertensive drugs specifically target angiotensin. Medicines of both directions belong to the same ATC 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 (C09C, C09D);
• other drugs that affect the renin-angiotensin (C09X) system.

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

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

Of the side effects that may accompany the intake of drugs in this group, the most common are headaches, dizziness, redness of the skin of the upper body, changes in taste. The pharmacological action, which determines the produced therapeutic effects of the 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.

Myotropic agents

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

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

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

Diuretics

Diuretics are used in the treatment of hypertension to remove excess fluid from the body that may cause or result in increased blood pressure. The group of diuretic antihypertensive drugs includes drugs that are heterogeneous in chemical composition and principle of action. A common factor for classifying medicines as diuretics is their ability to temporarily increase the excretion of water and minerals through urine.

Depending on the nature of the effect 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 number 18

antihypertensive (antihypertensive) drugs

They are used to treat hypertension.

Principles of hypertension treatment

decrease in OSPS - vasodilators (vasodilators).

decreased heart function and decreased cardiac output. Beta-blockers.

decrease in BCC - diuretics (diuretics).

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

decreased blood clotting.

6) normalization of the lipid spectrum.

7) reduction of neuropsychic stress.

classification of hypotensive

means by the mechanism of action

Neurotropic drugs:drugs depressing SDC , ganglion blockers, sympatholytics, α-, β-AB, α- and β-AB, sedatives.

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

Funds affecting the RAAS.

Diuretics.

Combined drugs.

antihypertensive drugs

central action

Clonidine (clonidine)

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

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

Reduces the production of intraocular fluid and reduces intraocular pressure.

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

Applicablewith hypertension stage 1-2, for 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 a withdrawal syndrome (for its prevention, the drug is canceled gradually, over 10 - 40 days).

Guanfacine -is similar to clonidine, acts more long-term, is prescribed once a day.

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

Moxonidine (Physiotens, Zinc) -selective agonist I 1 -imidazoline receptors. It inhibits SDC and dilates blood vessels, reduces the production of renin, AT II, \u200b\u200baldosterone, reduces heart function, reduces left ventricular hypertrophy, and has a sedative effect. It has a pronounced hypotensive effect, it is prescribed once a day.

Beta-blockers

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

SUBSTANCES AFFECTING RAAS

Reducing the release of renin

-adrenergic blockers

AT formation disruptingII.

A) ACE inhibitors (angiotensin converting enzyme) - ACE inhibitors captopril (kapoten), enalapril (enap), etc.

B) vasopeptidase inhibitors - omapatrilate

II (AT 1 )

losartan (kosaar), 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 (angiotensin converting enzyme) inhibitors

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

Mechanism of action:

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, load on the heart, and increase blood flow in organs.

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

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

Diuresis increases.

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 take into account 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 enzyme chymase. Therefore, blockers of AT 1 receptors turn off the RAAS most completely.

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

Applicable with hypertension, 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 the 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 vasodilating, 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 case of 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

Slow calcium channel blockers.

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

Anticalcium drugs apply with hypertension of moderate severity, 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 the 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 regaine 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 intravenous injection, it lasts 1-2 minutes. Therefore, it is administered by intravenous drip for hypertensive crises, heart failure, for controlled hypotension.

Side effects:tachycardia, headache, dyspeptic disorders.

Phosphodiesterase inhibitors.

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

Various myotropic drugs.

Bendazol -has an antispasmodic, antihypertensive and immunostimulating effect. BP decreases as peripheral vessels dilate and cardiac output decreases. The antihypertensive activity of dibazol is very moderate, and its effect is short-lived. With hypertension, it is usually prescribed in combination with other antihypertensive drugs. Used in / in to relieve hypertensive crisis.

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

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

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

Pharmaceuticals are 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 vascular lumen caused by a spasm of smooth muscle tissue.

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

Which remedy to choose?

I would like to note right away that the decision to use a particular drug is made only by the attending physician. Naturally, he must direct the patient to various laboratory tests so that the picture of the disease is clearer.
Nevertheless, 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 depressing effect on the central nervous system. Moreover, if the dosage is exceeded many times, then there is a real danger of cardiac arrest.
• Calcium channel blockers can help lower blood pressure readings below normal. There is also a possibility of dysfunction of internal organs.
• Diuretics have a strong diuretic effect, which leads to the leaching of nutrients 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. For the sake of fairness, it should be noted that this is often the fault of the patient himself, who independently begins to take this or that remedy, without really understanding the principle of its action.

That is why, only the attending physician should select the drug, relying on the test results 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.