New generation high blood pressure tablets: list of long-acting drugs. Antihypertensive drugs will help cope with hypertension

Antihypertensive drugs are used to reduce blood pressure (blood pressure) both in hypertension and in symptomatic hypertension. Currently, a significant number of antihypertensive drugs are used in clinical practice. Depending on the mechanism of action, antiadrenergic agents, vasodilators, calcium antagonists, angiotensin II antagonists, and diuretics are distinguished.

In this material we will consider the general principles of action of antihypertensive drugs, focusing only on specific representatives of a particular group. If you are interested in a wider list of medications, with a detailed description of each, we recommend our newer material - Antihypertensives: more specifically.

Antiadrenergic agents act on the sympathetic nervous system. According to the mechanism of action, they can be ganglio- and postganglionic blockers, α-, β-adrenergic blockers, and also acting predominantly on central sympathetic activity.
Drugs that act primarily on central sympathetic activity include clonidine and methyldopa. The hypotensive effect of these drugs is due to a direct effect on the α-receptors of the CNS (central nervous system), at the same time they inhibit sympathetic impulses from the vasomotor center in the CNS, which leads to a decrease in blood pressure (blood pressure), bradycardia (decreased heart rate), a decrease in peripheral vascular resistance, including kidney ones. The drugs reduce plasma renin levels, have a moderate sedative effect, but retain sodium and water. When these drugs are combined with diuretics, the hypotensive effect increases significantly. The combination with reserpine is undesirable, since it potentiates drowsiness and depression. These drugs are used with caution in the elderly, since collapsed states and depression are possible. Clonidine and methylzhofa are discontinued gradually to avoid hypertensive crises (withdrawal syndrome may occur).
Clonidine(clonidine, hemitone, catapressan). The hypotensive effect occurs within 1 hour and lasts up to 8-12 hours. The initial dose is usually 0.1-0.15 mg per day, with most of the drug taken at night. The dose of the drug is increased every 2-3 days to 0.3-0.45 mg in 2-3 doses. 0.5-1.0 ml of 0.01% clonidine solution in 10 ml of isotonic solution is administered intravenously over 3-5 minutes. The same doses are administered intramuscularly. Clonidine is non-toxic, but can cause dry mouth, drowsiness, and constipation. After parenteral administration, orthostatic hypotension may occur. Contraindications: severe atherosclerosis, depression, alcoholism, severe heart failure. It is not recommended to prescribe clonidine to pilots and drivers during work. Release form: tablets of 0.075 mg and 0.15 mg, ampoules of 1.0 ml of 0.01% solution.
Methyldopa(dopegit, aldomet) use 0.25-0.5 g 2-4 times (up to 3 g) per day. You can take the entire daily dose at one time. The maximum effect occurs after 4-6 hours and lasts 24-48 hours. Methyldopa is most often combined with diuretics. The drug is usually well tolerated by patients, but dry mouth, lethargy, depression, sexual dysfunction, fever, and myalgia may occur. With long-term treatment, jaundice may occur due to intrahepatic cholestasis (stagnation of bile in the liver). Contraindications: acute hepatitis, liver cirrhosis, pheochromocytoma, pregnancy. Release form: tablets of 0.25 g.

Ganglioblockers(benzohexonium, pentamine) simultaneously block both sympathetic and parasympathetic nerve nodes. Due to the blockade of the parasympathetic nodes, paresis of the gallbladder, dry mouth, and impotence may occur. Therefore, these drugs are prescribed only perenterally for hypertensive crises. After each injection, the patient should lie or recline with his head elevated for about 2 hours to avoid orthostatic hypotension.

Benzohexonium has a hypotensive effect by reducing arteriolar tone and reducing general peripheral resistance; it significantly reduces venous tone and venous pressure, as well as pressure in the pulmonary artery and right ventricle. The drug has a sedative effect, inhibits thyroid function, and increases insulin sensitivity in patients with diabetes. Used intramuscularly or subcutaneously at 12.5-25 mg (0.5-1 ml of 2.5% solution). 0.5-1.5 ml of a 2.5% solution is administered intravenously over 2-5 minutes under blood pressure monitoring. You can repeat the injections 3-4 times a day. Benzohexonium is combined with diuretics, apressin, reserpine.

Contraindications: acute myocardial infarction, cerebral thrombosis, pheochromocytoma. Release form: ampoules of 1 ml of 2.5% solution. Pentamin administered only in a hospital, intramuscularly at 0.25-0.5 5% solution, intravenously at 0.2-0.5 ml of 5% solution in 20 ml of isotonic solution or 5% glucose solution. Release form: ampoules of 1-2 ml of 5% solution.

Postganglionic blockers: reserpine, raunatin, octadin.
Reserpine(rausedil, serpasil) destroys the sites of connection with adrenaline and other amines, resulting in a sympathetic blockade. The hypotensive effect is gradual - over several weeks. The parasympathetic effect is manifested in bradycardia, swelling of the mucous membrane of the nasopharynx, increased acidity of gastric juice, increased motility of the gastrointestinal tract, and miosis. Reserpine is used orally (preferably once before bedtime) at 0.1-0.25 mg, then the dose is gradually increased to 0.3-0.5 mg per day. The drug can be administered intramuscularly or intravenously, 1 ml of 0.1-0.25% solution. 10-14 days after achieving the hypotensive effect, the dose of the drug is slowly reduced. Abrupt withdrawal may cause cardiac arrest. Reserpine is best prescribed with diuretics, as it causes sodium and water retention; it potentiates (strengthens) the depressant effect (lowering blood pressure) of barbiturates and alcohol on the central nervous system (CNS). For many people, reserpine causes heart pain.

Contraindications: severe circulatory failure, bradycardia, gastric ulcer, nephrosclerosis, epilepsy, depression. Release form: tablets of 0.1-0.25 mg, ampoules of 1 ml of 0.1-0.25% solution.

Raunatin contains reserpine and other alkaloids, its hypotensive effect is more gradual than that of reserpine. Raunatin has antiarrhythmic properties; drowsiness and nasal congestion are observed less frequently. It is better to start treatment with 0.002 g at night, if necessary increasing the dose to 0.004-0.006 g per day. The hypotensive effect of raunatin is enhanced in combination with diuretics and vasodilators. Contraindications the same as for reserpine. Release form: tablets of 0.002 g.
Octadine(isobarine, guanethidine sulfate, ismelin). The hypotensive effect occurs after 4-7 days of treatment. Treatment begins with 12.5 mg 1 time per day in the morning after meals, after 5-7 days the dose is gradually increased by 12.5 mg. Due to the accumulation of the drug, the hypotensive effect may persist for 1-2 weeks after its discontinuation. When using Octadine, there may be pain in the parotid glands, bradycardia, swelling of the veins in the legs, and diarrhea. Contraindications: severe cerebral atherosclerosis, acute myocardial infarction, exacerbation of duodenal ulcer, renal failure, pheochromocytoma, pregnancy. Release form: tablets of 0.25 mg.
Combined drugs: cristepine (brinerdine) - 0.1 mg of reserpine, 0.58 mg of dihydroergotoxin and 5 mg of clopamide (brinaldix) in tablets; adelfan - 0.1 mg of reserpine and 10 mg of hydrolasine in 1 tablet; trirezide-K contains, in addition to these two drugs, 10 mg of hypothiazide and 0.35 g of potassium chloride.

α-blockers- phentolamine, tropafen and pyrroxane act for a short time and therefore they are used only for hypertensive crises. During injections and for 1.5-2 hours after it, the patient should be in a horizontal position to avoid orthostatic hypotension. When using these drugs, side effects are possible: dizziness, tachycardia, itching, swelling of the nasal mucosa, vomiting, diarrhea. Contraindications: coronary heart disease (CHD) with attacks of angina, severe heart failure, cerebrovascular accident. Release form: phentolamine(regitin) - ampoules of 1 ml of 0.5% solution, tropafene- ampoules of 1 ml of 1% or 2% solution, pyrroxane- ampoules of 1 ml of 1% solution. Hypotensive effect prazosin(adversuten) is accompanied by tachycardia, but when taking the first dose, hypotension may develop, including fainting. It also has a vasodilating effect. Begins treatment with a test dose of 0.5 - 1 mg at bedtime, then 1 mg 2-3 times a day. Gradually increase the dose to 20 mg per day in 2-3 doses. The full effect is assessed after 4-6 weeks. There are no contraindications. Release form: tablets of 1.2 and 5 mg, capsules of 1 mg.

β-blockers reduce the work of the heart and have a moderate disaggregant, vasodilator and sedative effect. They are especially indicated when there is an increase mainly in systolic blood pressure.
Anaprilin(Inderal, Obzidan, Propranolol) in people under 40 years of age promotes a clear decrease in blood pressure, in patients over 60 years of age the effect is less pronounced. The drug is prescribed orally before meals, gradually increasing the dose from 40 mg to 160-480 mg per day in 2-4 doses. A pronounced hypotensive effect is observed after 2-4 weeks of use. It is especially advisable to prescribe this drug to patients with angina pectoris and tachycardia.

Contraindications: bronchial asthma, severe circulatory failure, bradycardia, atrioventricular and sinoauricular blockade, weak sinus node syndrome, Raynaud's syndrome, pregnancy. Release form: tablets of 10 and 40 mg, ampoules of 1 and 5 ml of 0.1% solution.

Vasodilators divided into arteriolar and venous. Arteriolar vasodilators (apressin, diazoxide, minoxidil) reduce total peripheral resistance by direct action on arterioles. Due to the dilation of arterioles, cardiac output, heart rate and the force of myocardial contraction increase. But these drugs increase the myocardial oxygen demand, which can result in coronary insufficiency, and cause sodium and water retention, so they should be combined with diuretics.

Apressin(hydralazine, depressan) is one of the most powerful vasodilators, but its hypotensive effect appears gradually. Treatment begins with 10-25 mg 2-4 times a day, gradually increasing the dose to 100-200 mg per day. Contraindications: severe cerebral atherosclerosis, severe ischemic heart disease (coronary heart disease), systemic lupus erythematosus, gastric ulcer, active autoimmune processes, peripheral neuropathy. Release form: tablets of 0.01 and 0.025 g.
Diazoxide(hyperstat) - the maximum hypotensive effect occurs 2-5 minutes after intravenous administration and lasts 2-24 hours. Blood pressure usually does not fall below normal, and orthostatic hypotension does not develop. For hypertensive crises, 75-300 mg of the drug is administered intravenously quickly, without mixing with other solutions. Diazoxide is a strong uterine relaxant. Many patients develop transient hyperglycemia when using it. Contraindications: diabetes mellitus, severe renal failure, dissecting aortic aneurysm. Release form: tablets of 50 mg, ampoules of 20 ml (300 mg).
Minoxidil The action is similar to apressin, but more effective. The hypotensive effect occurs in the first 2 hours and lasts up to 24 hours. Use starting with a dose of 1-2.5 mg per day, followed by a gradual increase to 40 mg. Contraindications: renal failure. Release form: tablets of 0.001 g.
Arteriolar and venous dilator sodium nitroprusside(niprid), when administered intravenously, gives a hypotensive effect due to dilation of peripheral vessels and a decrease in peripheral resistance, as well as a direct effect on the vascular wall of arterioles and venules. The initial dose for intravenous administration is 0.05 g. The maximum dose should not exceed 0.15 g. Indications for the use of sodium nitroprusside: hypertensive crisis, arterial hypertension refractory (resistant) to conventional therapy. Used in hospital. Contraindications: coarctation of the aorta, arteriovenous shunts. Release form: ampoules of 50 mg of the drug.
Calcium antagonist phenigidine(nifedipine, Corinfar): the hypotensive effect is observed 30-60 minutes after taking the drug, reaches a maximum after 1-2 hours and lasts up to 4-6 hours. Apply 10-20 mg 3-4 times a day. Adverse reactions: feeling of heat, redness of the face, neck, hands; drowsiness, headache, swelling of the legs.

Contraindications: pregnancy. Release form: tablets and dragees, 0.01 g each.
Verapamil(isoptin) has a less pronounced hypotensive effect compared to phenigidine. Treatment begins with 40-80 mg per day, if necessary, the dose is gradually increased to 720 mg. Contraindications: circulatory failure. Release form: tablets of 0.04 and 0.08 g, ampoules of 2 ml of 0.25% solution.
Angiotensin II antagonist captopril lowers the concentration of angiotensin II and aldosterone in the blood, providing a strong and long-lasting hypotensive effect, reduces the frequency of cardiac contractions, and increases diuresis. Treatment begins with 25-50 mg 2-3 times a day, then gradually increases the dose to 600-800 mg per day.

Contraindications: renal artery stenosis, severe renal failure. Release form: tablets of 25, 50 and 100 mg.

Achieving a clear antihypertensive effect through monotherapy diuretics is associated with a high risk of complications due to loss of electrolytes in the urine. In this regard, it is necessary to examine the potassium content at least once every 3 months. Sodium and calcium in the blood, record ECG. It is advisable to use diuretics in combination with other antihypertensive drugs, mainly when diastolic blood pressure increases (the “water-salt form” of hypertension).
The most widely used in clinical practice is hypothiazide. After taking the drug at a dose of 100 mg, a clear hypotensive effect occurs after 3-5 hours, and a dose of the drug 25-30 mg leads to a decrease in blood pressure after a day. The most pronounced effect is observed on the 5-7th day of treatment. Release form: tablets of 0.025 and 0.1 g.
Furosemide- the most powerful diuretic of the loop of Henle. The effect on blood pressure is somewhat inferior to hypothiazide. The hypotensive effect is observed 1-2 hours after taking the drug and lasts 5-8 hours. Release form: tablets of 40 mg, ampoules of 2 ml of 1% solution.
Ethacrynic acid(uregitis) does not provide a sufficient hypotensive effect and can only be used in combination with other drugs. Release form: tablets of 0.05 and 0.1 g, ampoules of 0.05 g of sodium salt of ethacrynic acid.
Klopamide(Brinaldix) has significant antihypertensive activity. Release form: tablets of 0.02 g.
The main advantage of potassium-sparing diuretics (spironolactone, triamterene) over other diuretics is that they remove little potassium salts from the body, so for prevention purposes they are usually used in combination with more powerful diuretics. Blood pressure decreases noticeably only after 2-4 weeks from the start of therapy spironolactone(veroshpiron, aldactone). Daily dose 50-400 mg in 2-4 doses. Release form: tablets of 0.025 g.
Triamterene the nature of its action resembles that of veroshpiron. Take 25 mg 2 capsules per day. Release form: capsules of 0.05 g.
Additional administration of hypothiazide can achieve a more significant reduction in blood pressure. A combination preparation is convenient for practical use triampur, containing 25 mg of triamterene and 12.5 mg of hypothiazide.
Intermittent use of diuretics is used as the main or as an additional method of treatment when prescribing other antihypertensive drugs. “Moderate diuretics” are prescribed, but with a long-lasting effect: hypothiazide, clopamide are taken for 2-4 days in a row, followed by a break of 2-3 days, a single dose 2 times a week is possible. For sodium-dependent ("water-salt" form of hypertension, continuous use of diuretics is recommended: small doses of hypothiazide (25-50 mg per day) in combination with triamterene 50-100 mg per day.

IN prevention And therapy In case of hypertension, a low-salt diet, regular physical activity, adequate sleep, and, if necessary, sedatives are of great importance. You should also not forget about natural remedies that lower blood pressure. Lately, the greatest interest has been, oddly enough,

Antihypertensive drugs are used in cases where it is necessary to lower blood pressure. It increases with hypertension, as well as with symptomatic hypertension. Depending on their mechanism of action, all these drugs are divided into vasodilators, antiadrenergic agents, angiotensin II antagonists, calcium antagonists and diuretics.

Antihypertensive drugs - classification of drugs

Antiadrenergic drugs have an effect on the sympathetic nervous system, these are the drugs "Clonidine" and "Methyldopa". These drugs directly affect the receptors of the central nervous system and thereby cause a decrease in blood pressure and a decrease in pulse. Also, these antihypertensive drugs reduce the amount of renin in plasma, and their disadvantage is the ability to retain sodium and water. If they are taken together with diuretics, the effect will be much better. It is better not to take them with reserpine, so as not to cause drowsiness and depression. Elderly people should be careful when taking these medications, as depression and collapsed states may occur. If methyldopa and clonidine are discontinued, this is done gradually.

Ganglioblockers include the drugs "Benzohexonium", "Pentamine". They block the sympathetic and parasympathetic. Since these antihypertensive drugs block the parasympathetic nodes, gallbladder paresis, dry mouth, and impotence may occur. After the injection, the patient should lie down for at least 2 hours with his head elevated, this is necessary to prevent orthostatic hypotension.

Postganglionic blockers include drugs such as Octadine, Raunatin, and Reserpine. If the drug "Reserpine" is used, its effect lasts for several weeks. It is better to take it together with diuretics, as it also retains water and sodium in the body. The medicine "Raunatit" has an antiarrhythmic effect, and after taking the drug, nasal congestion and drowsiness may occur.

Antihypertensive drugs such as alpha-blockers act quickly and short-term, so they are usually used when a hypertensive crisis occurs. These are drugs such as Tropaphen, Phentolamine and Pirroxan. After administering these medications, the patient also needs to lie down for 1.5-2 hours. These drugs can cause dizziness, tachycardia, itching, swelling of the nasal mucosa, vomiting and diarrhea. They should not be taken if you have coronary artery disease, cerebral circulatory disorders or heart failure.

Beta-blockers reduce the number of heart contractions and have a sedative, disaggregant and vasodilator effect. These are effective for high systolic blood pressure.

Vasodilators are divided into venous and arteriolar. Representatives of arteriolar drugs are Minoxidil, Diazoxide, Apressin. Venous and arteriolar sodium dilator after intravenous administration has a noticeable effect, as peripheral vessels dilate and peripheral resistance decreases.

Antihypertensive drugs, such as (drugs "Phenigidin", "Nifedipine", "Corinfar") cause a decrease in blood pressure within half an hour after taking them, and the maximum effect is observed within an hour and lasts up to 6 hours. After their use, there is redness of the hands, neck, face; Drowsiness, headache, and swelling of the legs may occur. These medications should not be taken during pregnancy.

In the treatment and prevention of hypertension, one must adhere to a low-salt diet, regularly give the body moderate physical activity, get enough sleep and, if necessary, take

Antihypertensive drugs are used to treat hypertension. They are the only means that lower blood pressure and prevent the occurrence of consequences. The latest generation of drugs have minimal side effects and, with the correct dose, do not pose a health risk during long-term use.

Classification of antihypertensive drugs

• First line medications:
  • ACE inhibitors;
  • diuretics;
  • angiotensin receptor blockers;
  • beta blockers;
  • calcium antagonists.
• Second line drugs:
  • alpha-blockers;
  • rauwolfia alkaloids;
  • centrally acting antagonists;
  • direct acting vasodilators.

Types of drugs

ACE inhibitors

The most effective antihypertensive drugs. The property of the group is its effect on the adrenal hormone, which retains fluid in the body, resulting in increased blood pressure. They have vasodilatory activity, but do not affect the heart rate and the amount of blood ejected by the heart. They are recommended for patients with chronic heart failure. With long-term use of new generation ACE inhibitors, blood pressure can be stabilized. Contraindications for use are pregnancy, lactation, high levels of potassium in the blood.

ACE inhibitors with long-term use cause a dry cough.

Diuretics

The hypotensive effect of this group of drugs is due to their diuretic effect. They are able to remove excess fluid from the human body, as a result of which the load on the heart is reduced. People suffering from gout should not use it. Very often, diuretics are prescribed in combination with other antihypertensive drugs. Classification of diuretic drugs:

• Thiazide. The combination of these diuretics with angiotensin receptor antagonists is often used to treat high blood pressure in the elderly and diabetics. Contraindicated for use in renal failure.
• Potassium-sparing antihypertensive drugs. The hypotensive effect is achieved due to the removal of sodium ions, while potassium is retained. The list of these drugs (medicines) is recommended for use by people with chronic heart failure and cardiac edema. It is prohibited to take them in case of chronic renal failure (CKD).
• Loopbacks. The main difference from other diuretics is the ability of the drugs to achieve a faster hypotensive effect. If the dose of the medicine is incorrectly selected, the blood pressure may drop sharply, then hypertensive drugs are used. They are considered the optimal means for relieving a hypertensive crisis, but they are not suitable for long-term use, as they wash out electrolytes with the liquid. This means that loop diuretic tablets can disrupt all metabolic processes in the body. List of main loop diuretics:
  • "Torasemide";
  • "Ethacrynic acid".

Beta blockers

Modern antihypertensive drugs. They reduce cardiac output and the production of renin in the kidneys, which causes vasospasm, resulting in lower blood pressure. Beta-blockers treat a combination of hypertension with angina, arrhythmia and chronic heart failure. Contraindicated in breastfeeding, pregnancy, diabetes, bronchial asthma. After stopping use, withdrawal syndrome may develop.

Calcium antagonists

Medicines that have the ability to block the flow of calcium ions into the smooth muscle cells of blood vessels, which reduces their spasm and lowers pressure. Antihypertensive treatment with this type of medication reduces the risk of heart attack and stroke. Cannot be used for children, patients with cardiovascular insufficiency, pregnant women or during lactation. Depending on the chemical structure, calcium antagonists are divided into the following types:

• dihydropyridines: “Felodipine”, “Amlodipine”;
• benzothiazepines: Diltiazem;
• phenylalkylamines: "Verapamil".

Neurotropic

• Centrally acting drugs:
  • Sedatives. The composition includes motherwort herb, valerian and magnesium sulfate.
  • Sleeping pills. For hypertension, the optimal drugs are: “Phenobarbital”, “Etaminal-sodium”.
  • Neuroleptics. In complex therapy, a list of drugs is used: “Aminazine”, “Reserpine”, “Raunatin”. Many long-acting antipsychotics.
  • Tranquilizers. Used at the initial stage of arterial hypertension: “Sibazon”, “Chlozepin”, “Oxilidine”.
• Neurotropic drugs of peripheral action:
  • Ganglion blockers: “Benzohexonium”, “Pentamine”. This type is used very rarely, due to the large list of side effects.
  • Alpha adrenergic blockers: Phentolamine, Tropaphen, Pirroxan. Used for hypertensive crisis.
  • Beta blockers: Anaprilin, Trazicor. They relieve vasospasm and have a sedative effect.
  • Sympatholytics: “Reserpine”, “Guanetedine”. Most often, combination drugs are used, which include sympatholytics.

Angiotensin receptor blockers

These are new generation drugs that are effective in treating hypertension. They are recommended for long-term use, as they are well tolerated and do not have many side effects or contraindications. Can be prescribed to patients with pathologies of the heart and kidneys. Angiotensin receptor blockers should not be used during pregnancy, hyperkalemia or allergic reactions.

Chapter 17.

Antihypertensive drugs (pharmacology)

Antihypertensives are drugs that lower blood pressure. Most often they are used for arterial hypertension, i.e. with high blood pressure. Therefore, this group of substances is also called antihypertensive drugs.

Arterial hypertension is a symptom of many diseases. There are primary arterial hypertension, or hypertension (essential hypertension), as well as secondary (symptomatic) hypertension, for example, arterial hypertension with glomerulonephritis and nephrotic syndrome (renal hypertension), with narrowing of the renal arteries (renovascular hypertension), pheochromocytoma, hyperaldosteronism, etc.

In all cases, they strive to cure the underlying disease. But even if this fails, arterial hypertension should be eliminated, since arterial hypertension contributes to the development of atherosclerosis, angina pectoris, myocardial infarction, heart failure, visual impairment, and renal dysfunction. A sharp increase in blood pressure - a hypertensive crisis can lead to bleeding in the brain (hemorrhagic stroke).

The causes of arterial hypertension are different for different diseases. In the initial stage of hypertension, arterial hypertension is associated with an increase in the tone of the sympathetic nervous system, which leads to an increase in cardiac output and constriction of blood vessels. In this case, blood pressure is effectively reduced by substances that reduce the influence of the sympathetic nervous system (central-acting antihypertensives, adrenergic blockers).

In kidney disease and in the late stages of hypertension, an increase in blood pressure is associated with activation of the renin-angiotensin system. Angiotensin produced II constricts blood vessels, stimulates the sympathetic system, increases the release of aldosterone, which increases the reabsorption of ions Na+ in the renal tubules and thus retains sodium in the body. Drugs that reduce the activity of the renin-angiotensin system should be prescribed.

With pheochromocytoma (tumor of the adrenal medulla), adrenaline and norepinephrine secreted by the tumor stimulate the heart and constrict blood vessels. Pheochromocytoma is removed surgically, but before surgery, during surgery, or if surgery is not possible, blood pressure is reduced with the help of wasp-blockers.

A common cause of arterial hypertension may be sodium retention in the body due to excessive consumption of table salt and insufficiency of natriuretic factors. Increased content Na+ in the smooth muscles of blood vessels leads to vasoconstriction (impaired function Na+/Ca2+ exchanger: input decreases Na+ and Ca 2+ output; the level of Ca 2+ in the cytoplasm of smooth muscles increases). As a result, blood pressure increases. Therefore, for arterial hypertension, diuretics are often used that can remove excess sodium from the body.

For arterial hypertension of any origin, myotropic vasodilators have an antihypertensive effect.

It is believed that patients with arterial hypertension should use antihypertensive drugs systematically to prevent an increase in blood pressure. For this purpose, it is advisable to prescribe long-acting antihypertensive drugs. The most commonly used drugs are those that act for 24 hours and can be prescribed once a day (atenolol, amlodipine, enalapril, losartan, moxonidine).

In practical medicine, the most commonly used antihypertensive drugs are diuretics, β-blockers, calcium channel blockers, α-blockers, ACE inhibitors, and AT 1 receptor blockers.

To relieve hypertensive crises, diazoxide, clonidine, azamethonium, labetalol, sodium nitroprusside, and nitroglycerin are administered intravenously. For mild hypertensive crises, captopril and clonidine are prescribed sublingually.

Classification of antihypertensive drugs

I .Medicines that reduce the influence of the sympathetic nervous system (neurotropic antihypertensive drugs):

1) means of central action,

2) drugs that block sympathetic innervation.

P. Vasodilators of myotropic action:

1) NO donors,

2) activators of potassium channels,

3) drugs with an unclear mechanism of action.

III . Calcium channel blockers.

IV . Agents that reduce the effects of the reninangiotensin system:

1) drugs that interfere with the formation of angiotensin II (drugs that reduce renin secretion, ACE inhibitors, vasopeptidase inhibitors),

2) AT 1 receptor blockers.

V. Diuretics.

17.1. Drugs that reduce the influence of the sympathetic nervous system (neurotropic antihypertensive drugs)

The higher centers of the sympathetic nervous system are located in the hypothalamus. From here, excitation is transmitted to the center of the sympathetic nervous system, located in the rostroventrolateral region of the medulla oblongata ( RVLM-rostro-ventrolateralmedulla ), traditionally called the vasomotor center. From this center, impulses are transmitted to the sympathetic centers of the spinal cord and further along the sympathetic innervation to the heart and blood vessels. Activation of this center leads to an increase in the frequency and strength of heart contractions (increased cardiac output) and to an increase in the tone of blood vessels - blood pressure increases.

Blood pressure can be reduced by inhibiting the centers of the sympathetic nervous system or by blocking sympathetic innervation. In accordance with this, neurotropic antihypertensive drugs are divided into central and peripheral agents.

TO centrally acting antihypertensive drugs include clonidine, moxonidine, guanfacine, methyldopa.

Clonidine (clonidine, hemitone) is an α2-adrenergic agonist, stimulates α2A-adrenergic receptors in the center of the baroreceptor reflex in the medulla oblongata (nucleus of the solitary tract). In this case, the vagal centers are excited ( nucleusambiguus ) and inhibitory neurons, which have an inhibitory effect on RVLM (vasomotor center). In addition, the inhibitory effect of clonidine on RVLM due to the fact that clonidine stimulates I 1 -receptors (imidazoline receptors).

As a result, the inhibitory effect of the vagus on the heart increases and the stimulating effect of sympathetic innervation on the heart and blood vessels decreases. As a result, cardiac output and the tone of blood vessels (arterial and venous) decrease - blood pressure decreases.

Partly, the hypotensive effect of clonidine is associated with the activation of presynaptic α2-adrenergic receptors at the endings of sympathetic adrenergic fibers - the release of norepinephrine decreases.

In higher doses, clonidine stimulates extrasynaptic a 2 β -adrenergic receptors of smooth muscle of blood vessels (Fig. 45) and, with rapid intravenous administration, can cause short-term vasoconstriction and an increase in blood pressure (therefore, intravenous clonidine is administered slowly, over 5-7 minutes).

Due to the activation of α2-adrenergic receptors in the central nervous system, clonidine has a pronounced sedative effect, potentiates the effect of ethanol, and exhibits analgesic properties.

Clonidine is a highly active antihypertensive drug (therapeutic dose when administered orally 0.000075 g); lasts about 12 hours. However, when used systematically, it can cause a subjectively unpleasant sedative effect (distracted thoughts, inability to concentrate), depression, decreased tolerance to alcohol, bradycardia, dry eyes, xerostomia (dry mouth), constipation, impotence. If you abruptly stop taking the drug, a pronounced withdrawal syndrome develops: after 18-25 hours, blood pressure rises, and a hypertensive crisis is possible. β-Adrenergic blockers increase clonidine withdrawal syndrome, so these drugs are not prescribed together.

Clonidine is used mainly to quickly lower blood pressure during hypertensive crises. In this case, clonidine is administered intravenously over 5-7 minutes; with rapid administration, an increase in blood pressure is possible due to stimulation of vascular α2-adrenergic receptors.

Clonidine solutions in the form of eye drops are used in the treatment of glaucoma (reduces the production of intraocular fluid).

Moxonidine(cint) stimulates imidazoline 1 1 receptors and, to a lesser extent, a 2 adrenergic receptors in the medulla oblongata. As a result, the activity of the vasomotor center decreases, cardiac output decreases and the tone of blood vessels decreases—blood pressure decreases.

The drug is prescribed orally for the systematic treatment of arterial hypertension 1 time per day. In contrast to clonidine, moxonidine causes less pronounced sedation, dry mouth, constipation, and withdrawal symptoms.

Guanfatsin(estulik) similarly to clonidine stimulates central α2-adrenergic receptors. Unlike clonidine, it does not affect receptors. The duration of the hypotensive effect is about 24 hours. It is prescribed orally for the systematic treatment of arterial hypertension. Withdrawal syndrome is less pronounced than with clonidine.

Methyldopa(dopegite, aldomet) chemical structure - a-methyl-DOPA. The drug is prescribed orally. In the body, methyldopa is converted into methylnorepinephrine, and then into methyladrenaline, which stimulate the α2-adrenergic receptors of the baroreceptor reflex center.

Metabolism of methyldopa

The hypotensive effect of the drug develops after 3-4 hours and lasts about 24 hours.

Side effects of methyldopa: dizziness, sedation, depression, nasal congestion, bradycardia, dry mouth, nausea, constipation, liver dysfunction, leukopenia, thrombocytopenia. Due to the blocking effect of a-methyl-dopamine on dopaminergic transmission, the following are possible: parkinsonism, increased production of prolactin, galactorrhea, amenorrhea, impotence (prolactin inhibits the production of gonadotropic hormones). If you abruptly stop taking the drug, withdrawal symptoms appear after 48 hours.

Drugs that block peripheral sympathetic innervation.

To reduce blood pressure, sympathetic innervation can be blocked at the level of:

1) sympathetic ganglia

2) endings of postganglionic sympathetic (adrenergic) fibers

3) adrenergic receptors of the heart and blood vessels. Accordingly, ganglion blockers, sympatholytics, and adrenergic blockers are used.

Ganglioblockers -hexamethonium benzosulfonate(benzohexonium), azamethonium(pentamine), trimethaphan(arfonad) block the transmission of excitation in the sympathetic ganglia (block N N - xo -linoreceptors of ganglion neurons), block N N -cholinergic receptors of chromaffin cells of the adrenal medulla and reduce the release of adrenaline and norepinephrine. Thus, ganglion blockers reduce the stimulatory effect of sympathetic innervation and catecholamines on the heart and blood vessels. There is a weakening of heart contractions and expansion of arterial and venous vessels - arterial and venous pressure decreases. At the same time, ganglion blockers block the parasympathetic ganglia; thus eliminating the inhibitory effect of the vagus nerves on the heart and usually causing tachycardia.

For systematic use, ganglion blockers are of little use due to side effects (severe orthostatic hypotension, impaired accommodation, dry mouth, tachycardia; possible intestinal and bladder atony, sexual dysfunction).

Hexamethonium and azamethonium act for 2.5-3 hours; administered intramuscularly or subcutaneously during hypertensive crises. Azamethonium is also administered intravenously slowly in 20 ml of isotonic sodium chloride solution for hypertensive crisis, edema of the brain, lungs against the background of high blood pressure, for spasms of peripheral vessels, for intestinal, hepatic or renal colic.

Trimetaphan acts for 10-5 minutes; administered in solutions intravenously by drip for controlled hypotension during surgical operations.

Sympatholytics -reserpine, guanethidine(octadine) reduce the release of norepinephrine from the endings of sympathetic fibers and thus reduce the stimulating effect of sympathetic innervation on the heart and blood vessels - arterial and venous pressure decreases. Reserpine reduces the content of norepinephrine, dopamine and serotonin in the central nervous system, as well as the content of adrenaline and norepinephrine in the adrenal glands. Guanethidine does not penetrate the blood-brain barrier and does not change the content of catecholamines in the adrenal glands.

Both drugs differ in their duration of action: after stopping systematic use, the hypotensive effect can last up to 2 weeks. Guanethidine is much more effective than reserpine, but is rarely used due to severe side effects.

Due to the selective blockade of sympathetic innervation, the influences of the parasympathetic nervous system predominate. Therefore, when using sympatholytics, the following are possible: bradycardia, increased secretion of HC1 (contraindicated in peptic ulcers), diarrhea. Guanethidine causes significant orthostatic hypotension (associated with a decrease in venous pressure); When using reserpine, orthostatic hypotension is mild. Reserpine reduces the level of monoamines in the central nervous system and can cause sedation and depression.

A -Adrenergic blockers reduce the stimulating effect of sympathetic innervation on blood vessels (arteries and veins). Due to the dilation of blood vessels, arterial and venous pressure decreases; heart contractions reflexively become more frequent.

a 1 -Adrenergic blockers - prazosin(minipress), doxazosin, terazosin prescribed orally for the systematic treatment of arterial hypertension. Prazosin acts for 10-12 hours, doxazosin and terazosin - 18-24 hours.

Side effects a 1 -adrenergic blockers: dizziness, nasal congestion, moderate orthostatic hypotension, tachycardia, frequent urination.

a 1 a 2 -Adrenergic blocker phentolamine used for pheochromocytoma before surgery and during surgery to remove pheochromocytoma, as well as in cases where surgery is impossible.

β -Adrenergic blockers- one of the most commonly used groups of antihypertensive drugs. When used systematically, they cause a persistent hypotensive effect, prevent sudden increases in blood pressure, practically do not cause orthostatic hypotension, and, in addition to hypotensive properties, have antianginal and antiarrhythmic properties.

β-Adrenergic blockers weaken and slow down heart contractions - systolic blood pressure decreases. At the same time, β-blockers constrict blood vessels (block β 2 -adrenergic receptors). Therefore, with a single use of β-blockers, the mean arterial pressure usually decreases slightly (with isolated systolic hypertension, blood pressure can decrease even after a single use of β-blockers).

However, if p-blockers are used systematically, then after 1-2 weeks the narrowing of blood vessels is replaced by their dilation - blood pressure decreases. Vasodilation is explained by the fact that with the systematic use of beta-blockers, due to a decrease in cardiac output, the baroreceptor depressor reflex is restored, which is weakened in arterial hypertension. In addition, vasodilation is facilitated by a decrease in the secretion of renin by juxtaglomerular cells of the kidneys (block of β 1 -adrenergic receptors), as well as blockade of presynaptic β 2 -adrenergic receptors in the endings of adrenergic fibers and a decrease in the release of norepinephrine.

For the systematic treatment of arterial hypertension, long-acting β 1-blockers are often used - atenolol(tenormin; lasts about 24 hours), betaxolol(valid up to 36 hours).

Side effects of β-blockers: bradycardia, heart failure, difficulty in atrioventricular conduction, decreased HDL levels in the blood plasma, increased bronchial and peripheral vascular tone (less pronounced with β 1 -blockers), increased effect of hypoglycemic agents, decreased physical activity.

a 2 β-Adrenergic blockers -labetalol(trandate), carvedilol(Dilatrend) reduce cardiac output (block of β-adrenoreceptors) and reduce the tone of peripheral vessels (block of α-adrenoreceptors). The drugs are used orally for the systematic treatment of arterial hypertension. Labetalol is also administered intravenously during hypertensive crises.

Carvedilol is also used for chronic heart failure.

17.2. Myotropic antihypertensive drugs

Myotropic antihypertensives are substances that have a direct relaxing effect on the smooth muscles of blood vessels; At the same time, the vessels dilate, blood pressure decreases.

Among myotropic antihypertensive drugs there are:

Donors NO;

Potassium channel activators;

Drugs with an unknown mechanism of action.

Donors NO- drugs whose metabolism releases nitric oxide (NO), identical to endothelial relaxing factor. Drugs in this group include nitroglycerin and sodium nitroprusside. During the metabolism of nitroglycerin, the release of NO is due to the action of thiol enzymes, the depletion of which is associated with rapid addiction to nitroglycerin. Sodium nitroprusside releases NO spontaneously; addiction to the drug does not develop.

NO stimulates guanylate cyclase of vascular smooth muscle; cGMP levels increase, which activates protein kinase G . Under the influence of protein kinase G Phospholamban of the sarcoplasmic reticulum membrane is phosphorylated. At the same time, the activity of phospholamban decreases. The inhibitory effect of phospholamban on the Ca 2+ -ATPase of the sarcoplasmic reticulum is reduced. Under the action of Ca 2+ -ATPase, Ca 2+ ions are transferred from the cytoplasm to the sarcoplasmic reticulum, and the Ca 2+ content in the cytoplasm decreases.

A decrease in the Ca 2+ content in the cytoplasm leads to relaxation of the smooth muscles of blood vessels (the stimulating effect of the Ca 2+ calmodulin complex on myosin light chain kinase decreases).

Nitroglycerineused mainly for ischemic heart disease. Nitroglycerin dilates predominantly venous and, to a lesser extent, arterial vessels (it is believed that the level of thiol enzymes, under the influence of which NO is released from nitroglycerin, is higher in the veins than in the arteries).

As an antihypertensive agent, nitroglycerin solution is administered intravenously. The drug is used to relieve hypertensive crises, as well as to reduce the load on the heart in acute heart failure.

Sodium nitroprusside - one of the most effective vasodilators and antihypertensive drugs. Unlike nitroglycerin, sodium nitroprusside dilates arterial and venous vessels equally. Solutions of sodium nitroprusside are administered intravenously (with simultaneous administration, the duration of action is about 3 minutes).

The drug is used for hypertensive crises, acute left ventricular failure, as well as for controlled hypotension during surgical operations.

Sodium nitroprusside is a cyanide compound.

During its metabolism, in addition to NO, cyanide is released, which, under the influence of liver rhodanase, quickly turns into low-toxic thiocyanate (in case of liver diseases, toxic effects of cyanide may occur - metabolic acidosis, vomiting, respiratory failure, loss of consciousness). Excretion of thiocyanate is slow ( t 1/2 3 days) and with prolonged intravenous administration of sodium nitroprusside, cumulation of thiocyanate occurs and its toxic effect begins to manifest itself - ringing in the ears, blurred vision, disorientation, delirium, convulsions. Therefore, intravenous drip administration of sodium nitroprusside is not recommended for more than 18-34 hours.

Potassium channel activators - diazoxide, minoxidil selectively dilate arterial vessels and reduce blood pressure; the heart rate reflexively increases.

The dilation of arterial vessels is associated with the activation of K + channels in the membranes of smooth muscle fibers of the arteries. At the same time, the release of K+ from cells increases and hyperpolarization of the cell membrane develops. Against the background of hyperpolarization, the opening of voltage-dependent Ca 2+ channels is difficult, calcium-dependent contraction of arterial smooth muscles is disrupted - blood pressure decreases.

The most commonly used potassium channel activators are diazoxide(hyperstat). The drug is administered intravenously during hypertensive crises over 30 seconds. With slower administration, the effectiveness of diazoxide decreases, since the drug is almost completely (94%) bound to blood plasma proteins (for the same reason, diazoxide is not very effective when taken orally). The duration of action of diazoxide is 4-20 hours.

Side effects of diazoxide: arterial hypotension, dizziness, skin flushing, hyperglycemia (decreased insulin secretion due to activation of potassium channels).

Minoxidil(lonitene) is one of the most effective antihypertensive drugs for oral administration. Duration of action is about 24 hours.

As a reaction to a decrease in blood pressure, sympathetic innervation is reflexively activated - pronounced reflex tachycardia occurs, the activity of the renin-angiotensin-aldosterone system increases, resulting in a delay in the body Na+ and water. Therefore, minoxidil is prescribed together with β-blockers and diuretics.

When using minoxidil, increased pressure in the pulmonary artery, effusion in the pericardial cavity, and hypertrichosis are possible. Therefore, minoxidil is prescribed only in cases of severe arterial hypertension when other antihypertensive drugs are ineffective.

Myotropic drugs with an unknown mechanism of action. Hydralazine(apressin) selectively dilates arterial vessels, lowers blood pressure. The mechanism of myotropic action is not clear. Due to a decrease in blood pressure, reflex tachycardia occurs and the renin-angiotensin-aldosterone system is activated. Increased secretion of aldosterone leads to sodium and water retention in the body. It is advisable to combine the drug with substances that reduce the effect of sympathetic innervation (β-blockers, reserpine) and diuretics.

Hydralazine is used for the systematic treatment of severe forms of arterial hypertension (prescribed orally), for hypertensive crises, eclampsia (administered intravenously).

Side effects of hydralazine: dizziness, headache, facial flushing, nasal congestion, tachycardia, postural hypotension, exacerbation of coronary artery disease, nausea, vomiting, diarrhea, skin rashes, paresthesia, proteinuria, leukopenia, anemia, thrombocytopenia. With long-term use of hydralazine in large doses, the development of systemic lupus erythematosus syndrome is possible (more often in women and “slow acetylators”).

Dihydralazinesimilar in properties to hydralazine. In combination with reserpine and hydrochlorothiazide, it is part of the Adelfan-Ezidrex tablets.

Magnesium sulfatewhen administered intramuscularly or intravenously, it causes a pronounced hypotensive effect, which is associated with a myotropic vasodilator effect, as well as a inhibitory effect on the vasomotor center and the transmission of excitation in the sympathetic ganglia.

Magnesium sulfate is administered intramuscularly for hypertensive crises. Intravenous administration of the drug is possible, but this increases the risk of depression of the respiratory center (narcotic effect).

Due to its anticonvulsant and hypotensive properties, magnesium sulfate is used for eclampsia (late toxicosis of pregnancy, which is accompanied by convulsions and increased blood pressure).

17.3. Calcium channel blockers

Substances in this group block voltage-gated calcium channels L -types that have the greatest functional significance for the heart and arterial vessels. In this regard, calcium channel blockers act mainly on the heart and arterial vessels (the effect on venous vessels is negligible, so calcium channel blockers practically do not cause orthostatic hypotension). In addition, these drugs have a weak bronchodilator, tocolytic, antiplatelet and antiatherosclerotic effect. Calcium channel blockers include dihydropyridines, phenylalkylamines and benzothiazepines.

Dihydropyridines - nifedipine, amlodipine, felodipine, lacidipine, nitrendipine, nisoldipine, isradipine act predominantly on arterial vessels and to a lesser extent on the heart.

Nifedipine(phenigidine, corinfar, adalat) dilates arterial vessels and lowers blood pressure.

The effect of nifedipine on the heart consists of 2 components - direct and reflex. In experiments on isolated hearts, nifedipine weakens and slows down heart contractions. In the whole body, under the influence of nifedipine, blood pressure decreases and, in connection with this, reflex tachycardia occurs. The stroke volume of the heart does not change, but in patients with heart failure, nifedipine may reduce myocardial contractility.

The drug is prescribed orally; duration of action is 6-8 hours. For short-term treatment of arterial hypertension, vasospastic angina, Raynaud's syndrome, nifedipine is prescribed 3 times a day.

For the systematic treatment of arterial hypertension, only long-acting nifedipine drugs (retard tablets) are recommended, which act for 24 hours and are prescribed once a day (short-acting drugs, when used systematically, increase the mortality of patients, apparently due to fluctuations in blood pressure).

Side effects of nifedipine: tachycardia, headache, dizziness, facial flushing, nausea, constipation, peripheral edema, in particular, swelling of the ankles (in the area of ​​arteriovenous shunts, arteries, but not veins, dilate; venous outflow is insufficient), paresthesia, myalgia , frequent urination.

For systematic long-term treatment of arterial hypertension, long-acting dihydropyridines are recommended - amlodipine(norvask), felodipine(lendil), lacidipine, which last 24 hours and are prescribed once a day. To reduce tachycardia, dihydropyridine calcium channel blockers are recommended to be combined with β-blockers.

Nimodipine -highly lipophilic calcium channel blocker; easily penetrates the blood-brain barrier. Used to reduce neurological disorders associated with cerebral vascular spasms after subarachnoid hemorrhage.

Phenyl al kylamines - verapamil, gallons of silt act primarily on the heart and to a lesser extent on the arterial vessels. Unlike dihydropyridines, these drugs, when used systemically, weaken and slow down heart contractions and impede atrioventricular conduction. Phenylalkylamines should not be combined with β-blockers.

Verapamil(isoptin) reduces and weakens heart contractions, impedes atrioventricular conduction, dilates small coronary vessels (increases the volumetric velocity of coronary blood flow), moderately dilates peripheral arteries. In high doses, verapamil effectively lowers blood pressure; the hypotensive effect is due to a decrease in cardiac output and total peripheral vascular resistance. The drug is effective for 6-8 hours.

For the systematic treatment of arterial hypertension, verapamil tablets with prolonged release of the drug (retard tablets) are used; prescribed 1 time per day at night.

Verapamil is effective for vasospastic angina and supraventricular tachyarrhythmias.

Verapamil is indicated as an antihypertensive agent for patients with concomitant coronary insufficiency and cardiac arrhythmias.

Side effects of verapamil: bradycardia, heart failure, atrioventricular conduction disturbances, dizziness, nausea, constipation, peripheral edema (mainly swelling of the ankles), which is associated with dilation of arterioles, but not venules. Verapamil is not recommended for use together with β-blockers, since in this case heart failure, bradycardia, and atrioventricular conduction disorders are aggravated.

Benzothiazepines.Diltiazem compared to dihydropyridines, it has a greater effect on the heart and less on arterial vessels, and compared to verapamil, it has a greater effect on arterial vessels and less on the heart.

The drug is prescribed 2-3 times a day (retard tablets - 1 time a day) for arterial hypertension, vasospastic angina and supraventricular tachyarrhythmias.

17.4. Drugs that reduce the activity of the renin-angiotensin system

In many cases, hypertension is associated with increased activity of the renin-angiotensin system. Juxtaglomerular cells (located near the afferent arterioles of the renal glomeruli) in response to a decrease in blood supply to the kidneys and stimulation of sympathetic innervation release renin, which promotes the formation of angiotensin I , from which angiotensin is formed under the influence of angiotensin-converting enzyme (ACE) II.

Angiotensin II stimulates:

1) angiotensin AT 1 -receptors of blood vessels (causes vasoconstriction);

2) sympathetic innervation of the heart and blood vessels (the centers of sympathetic innervation, sympathetic ganglia, presynaptic angiotensin receptors of the endings of adrenergic fibers are stimulated and the release of norepinephrine increases);

3) secretion of aldosterone by cells of the adrenal cortex.

All this contributes to increased blood pressure. The renin-angiotensin system is also activated in heart failure, which creates additional stress on the heart. In medical practice, there are mainly 3 options for reducing the activity of the renin-angiotensin system:

1) decrease in renin secretion - β-blockers;

2) disruption of angiotensin formation II - ACE inhibitors, vasopeptidase inhibitors;

3) disruption of the action of angiotensin II - AT 1 receptor blockers.

17.4.1. Agents that reduce renin secretion

Renin secretion is reduced by substances that reduce the stagnating effect of sympathetic innervation on juxtaglomerular cells that produce renin. These cells contain β 1 adrenergic receptors, so one of the components of the mechanism of the hypotensive action of β-blockers is a decrease in renin secretion.

17.4.2. ACE inhibitors

Angiotensin converting enzyme (ACE) promotes the conversion of angiotensin I to angiotensin II , and also inactivates bradykinin, which dilates blood vessels and irritates sensitive receptors.

ACE inhibitors interfere with the formation of angiotensin II. Due to this:

1) the vasoconstrictor effect of angiotensin decreases II;

2) the stimulating effect of angiotensin decreases II on the sympathetic nervous system;

3) the stimulating effect of angiotensin decreases II on the synthesis and secretion of aldosterone (with a decrease in the secretion of aldosterone, excretion from the body increases Na+ and the excretion of K+ is delayed).

In addition, when ACE is inhibited, the inactivating effect of ACE on bradykinin is eliminated - the level of bradykinin increases. Bradykinin has a vasodilating effect, increases vascular permeability, and stimulates sensitive nerve endings.

Decreased angiotensin levels II, Na+ excretion and increased bradykinin levels lead to dilation of blood vessels and a decrease in blood pressure. The heart rate changes little.

Compared to other antihypertensive drugs, ACE inhibitors have a number of advantages:

1) have a persistent hypotensive effect;

2) do not cause sodium and water retention;

3) do not cause orthostatic hypotension and reflex tachycardia;

4) these drugs are not characterized by the development of tolerance upon repeated use;

5) withdrawal syndrome is not expressed.

ACE inhibitors captopril, lisinopril, enalapril, perindopril, etc. are used:

1) with arterial hypertension,

2) for chronic congestive heart failure.

In arterial hypertension, ACE inhibitors are especially effective if the increase in blood pressure is associated with activation of the reninangiotensin system (renal hypertension, late stages of hypertension). ACE inhibitors can be used for arterial hypertension associated with stenosis of the artery of one of the kidneys, but they are contraindicated for bilateral renal artery stenosis (they reduce glomerular filtration due to a decrease in the vasoconstrictor effect of angiotensin II on the efferent arterioles of the renal glomeruli).

In chronic congestive heart failure, ACE inhibitors, by dilating arterial and venous vessels, reduce afterload and preload on the heart, respectively. At the same time, the insufficient heart begins to contract more productively - cardiac output increases.

ACE inhibitors are useful in the post-infarction period: they improve cardiac contractility and reduce mortality.

Captopril (capoten, tensiomin) is prescribed orally. Duration of action is 6-8 hours. To more quickly reduce blood pressure (in mild hypertensive crisis), the drug is used sublingually. In addition to arterial hypertension, captopril is used for chronic heart failure.

Side effects of captopril:

Arterial hypotension upon first use, especially against the background of dehydration (effect of diuretics, excessive sweating);

Dry cough; I

Hives, itchy skin; I action of bradykinin

Angioedema; I

Headache, dizziness;

Taste disturbances, nausea, vomiting, diarrhea or constipation;

Hyperkalemia (decreased aldosterone production);

Proteinuria (especially in patients with impaired renal function);

Paresthesia;

Neutropenia;

Decreased libido.

Lisinoprilvalid 24 hours; prescribed 1 time per day.

Enalapril(Renitec) - prodrug; well absorbed from the gastrointestinal tract; turns into active enalaprilat. Duration of action is 24 hours.

Enalaprilatfor arterial hypertension, it is administered intravenously.

They have properties similar to enalapril. perindopril(prestarium), ramipril(tritatse), trandolapril(hopten), fosinopril moexipril

The side effects of these ACE inhibitors are similar to the side effects of captopril.

17.4.3. Vasopeptidase inhibitors

Vasopeptidases include ACE and neutral endopeptidase, which inactivates atrial natriuretic peptide. Since sodium retention and increased blood pressure are associated with atrial natriuretic peptide deficiency, neutral endopeptidase inhibitors have been proposed to lower blood pressure.

Of particular interest is omapatrilat, which inhibits both neutral endopeptidase and ACE. The drug is prescribed orally for arterial hypertension and heart failure.

17.4.4. AT 1 receptor blockers

Action of angiotensin II associated with its effect on angiotensin receptors, which are designated as AT 1 -receptors and AT 2 receptors.

Losartan(kozaar), valsartan interfere with the action of angiotensin II on AT 1 -receptors of blood vessels, sympathetic innervation and adrenal cortex. This increases the effect of angiotensin II on AT 2 receptors; This is associated with the ability of drugs to reduce myocardial hypertrophy and proliferation of vascular smooth muscles (Table 9).

Losartan and valsartan are used for the systematic treatment of arterial hypertension, especially in cases of intolerance to ACE inhibitors.

The drugs are prescribed orally once a day.

Other drugs in this group - candesartan, irbesartan, tel-misartan have properties similar to losartan.

Unlike ACE inhibitors, AT blockers 1 -receptors do not affect bradykinin levels and cause fewer side effects. In particular, these drugs do not cause a dry cough, and angioedema is rare with their use. Same as ACE inhibitors, AT blockers 1 -receptors can cause hyperkalemia. Possible liver dysfunction.

17.5. Diuretics

Saluretics (diuretics that remove excess blood) are used as antihypertensive drugs. Na + and C I - ) - hydrochlorothiazide, chlorthalidone, furosemide, etc., as well as the aldosterone antagonist - spironolactone.

When patients with arterial hypertension are systematically prescribed diuretics from the groups of thiazides, thiazide-like diuretics, and loop diuretics, the volume of blood plasma decreases in the first days, which leads to a decrease in blood pressure. Subsequently, the volume of blood plasma is restored, and blood pressure remains reduced due to the dilation of blood vessels. The vasodilating effect of diuretics is explained by the removal of ions from the body Na+ . With reduced content Na+ in the smooth muscles of blood vessels, the exchange of extracellular Na+ on intracellular Ca 2+ ions. A decrease in the level of Ca 2+ in the cytoplasm of smooth muscle fibers leads to muscle relaxation and vasodilation.

As antihypertensive drugs, diuretics are prescribed systematically in small doses, usually once a day, for elimination from the body excess Na+ . At higher doses, the diuretic, but not the hypotensive effect of diuretics increases.

Used to quickly lower blood pressure furosemide(Lasix), for long-term systematic treatment - hydrochlorothiazide(dichlorothiazide, hypothiazide), chlorthalidone(oxodoline, hygroton), etc.

For arterial hypertension, diuretics can be used as monotherapy. However, more often they are combined with other drugs that lower blood pressure. With the systematic use of many antihypertensive drugs (central antihypertensive drugs, adrenoblockers, sympatholytics, myotropic vasodilators), the excretion is delayed Na+ from the body. This leads to a delay in water excretion, edema, and also reduces the effectiveness of antihypertensive drugs. Diuretics are combined with many antihypertensive drugs to potentiate their action and reduce side effects.

17.6. Combined use of antihypertensive drugs

In the treatment of arterial hypertension, drugs with different pharmacological properties are often combined to increase the antihypertensive effect and/or to reduce side effects.

Most antihypertensive drugs, when used systematically, cause a delay in the body Na+ and water; this limits their antihypertensive effectiveness. Therefore, such drugs are combined with thiazides, thiazide-like or loop diuretics. For example, for the systematic treatment of arterial hypertension, a combination drug is used tenorist, containing the long-acting β-adrenergic blocker atenolol and the long-acting diuretic chlorthalidone.

Dihydropyridines are combined with β-blockers to reduce tachycardia, and ACE inhibitors are combined with thiazide diuretics to reduce hyperkalemia.

At the same time, some antihypertensive drugs should not be combined, for example, verapamil and β-blockers (increased bradycardia, atrioventricular conduction disturbances), ACE inhibitors and potassium-sparing diuretics (increased hyperkalemia), hydralazine and dihydropyridines (increased tachycardia).

17.7. Drugs used for hypertensive crises

During hypertensive crises, due to the risk of stroke, antihypertensive drugs are used, which have a rapid hypotensive effect. For mild crises, they are sometimes limited to sublingual administration of clonidine and captopril. With a significant increase in blood pressure, solutions of antihypertensive drugs are administered parenterally, often intravenously (diazoxide, clonidine, labetalol, sodium nitroprusside, enalaprilat, furosemide).

One of the most pressing problems for many people today is hypertension. Fortunately, surges in blood pressure (BP) can be eliminated using traditional recipes and a number of medications. In addition, some people have completely adapted to living normally with symptoms of high blood pressure, without even noticing a sharp change in blood pressure.

But, as it turned out, stopping the episode is not enough. The whole problem of hypertensive disease lies in the consequences. After all, a sharp increase in blood pressure affects the performance of the heart and kidneys, which act as targets.

Consequently, ignoring attacks of high blood pressure or eliminating an attack without a subsequent course of therapy can even lead to pathological damage to the retina. Based on the danger posed by arterial hypertension, it is necessary to pay attention to therapy that prevents increases in blood pressure and hypertensive crises. Thus, it is possible to protect target organs from pathological damage due to complications of arterial hypertension.

But, before purchasing all the medications that prevent the consequences of high blood pressure, you should conduct a detailed diagnosis in a specialized medical institution, and then decide on medications that do not have side effects.

First of all, attention is paid to the blood pressure indicator. Pathological indicators include indicators exceeding 140 to 90. Until recently, it was believed that different blood pressure indicators were normal for representatives of different age categories. But now doctors have come to the same conclusion that a patient with a blood pressure of 140 over 90 requires therapy. But you don’t always need to resort to medication.

For example, in the absence of manifestations of coronary artery disease, but at the same time persistently high blood pressure, it will be enough to reconsider the usual lifestyle. In this case, normalization of nutrition will be required, including a special diet, psychotherapy and lowering blood pressure through massage and meditation. This technique will be effective if the upper blood pressure threshold does not exceed 160 to 90 and the patient has no concomitant ailments.

Note! A patient with hypertension should monitor their weight. After all, extra pounds will only worsen the clinical picture.

The second exciting question is the desired blood pressure level after therapy and the level that needs to be maintained for a long period. For example, the category of people under 55-60 years of age with complications of hypertension, kidney disease or diabetes mellitus should maintain indicators of no more than 130 to 85.

What aggravates the clinical picture with high blood pressure?

There are several categories of patients with hypertension. The first ones ignore the danger of blood pressure risks and try to live to the best of their health. Thus, considering that if the disease does not cause significant discomfort, then you can get by with pills that block blood pressure surges. The second patients, on the contrary, overestimate the risk and try to cure the disease with all the drugs that come to hand, not paying attention to the side effects, but ignore going to the doctor.

Video - Hypertension: how to protect yourself

How to treat hypertension?

If a patient observes regular jumps in blood pressure to high levels, then he should first visit a doctor. Since all medications are aimed at normalizing the patient’s condition and lowering blood pressure, at the same time they can have side effects.

It is advisable to consider the main drugs:

1. Beta blockers. These are special medications to lower blood pressure by lowering the heart rate. But their downside in the form of side effects is weakness, skin rashes, and excessive slowing of the pulse.
2. ACE inhibitors. The body can produce large amounts of a hormone that negatively affects blood vessels, narrowing them. This group of drugs is aimed at reducing the amount of hormone produced. As a result, blood pressure drops as blood vessels dilate. The negative consequences of inhibitors can manifest themselves in the form of allergic reactions or a sudden cough.
3. Diuretics. This is a group of drugs with a diuretic effect. They are taken to quickly lower blood pressure by removing fluid from the body. But, taking these medications can negatively affect the functioning of the heart, leading to dizziness, seizures and nausea.
4. Calcium antagonists. The main purpose of such drugs is to have a relaxing effect on blood vessels, as a result of which blood pressure decreases. Side effects after taking such drugs manifest themselves in the form of hot flashes, rapid heartbeat, and sometimes even dizziness.
5. Angiotensin antagonists. High blood pressure may be due to the effect of angiotensin 2 on blood vessels, and drugs in this group block this effect. But as a result, dizziness may occur, accompanied by nausea.

That is why it is necessary to consult a doctor and prescribe effective therapy for the treatment of hypertension.

Are there safe drugs?

When high blood pressure interferes with normal life activities, the question arises of how to find the safest medications without side effects. Unfortunately, science has not provided such drugs. After all, it is extremely difficult to develop a universal drug that would suit every patient, but would not have any side effects. But still, new generation drugs have significant advantages over outdated drugs for the treatment of hypertension, they are as follows:

1. Minimizing side effects. There are no absolutely safe drugs for every patient, but new developments select components in such a way that they do not cause negative reactions in the body.
2. Long-acting drugs. Consequently, the dosage of the drug is reduced and thereby minimizes the risk of side effects.
3. New technologies have provided more effective drugs for the treatment of hypertension.
4. Complex preparations have been developed. The risk of side effects is so low that the drug can be considered absolutely safe.

Is it dangerous! Ignoring treatment for hypertension is strictly prohibited, since almost 50% of deaths from stroke are a consequence of hypertension. Therefore, you should not take therapy and examination by a specialist lightly.

Drugs with minimal side effects

The risk of side effects when eliminating high blood pressure will be minimal if you take complex medications. The main representative is Lisinopril is a drug from the ACE inhibitor group, but of the third generation. It contains a diuretic, as a result, the effectiveness of treatment increases significantly.

1. Shows the best results in the treatment of elderly people.
2. Approved for the treatment of patients with diabetes.
3. Minimizes the likelihood of complications.
4. Quickly lowers blood pressure.

Physiotens is the second effective and at the same time safe drug for the treatment of hypertension. If we talk about side effects after taking this drug, they are insignificant and are expressed in the form of dry mouth, mild weakness and drowsiness. Patients do not report any other discomfort.

Physiotens is a safe drug for the treatment of hypertension

Note! These drugs have such minimal side effects that they are truly safe drugs. And most importantly, they do not have a detrimental effect on the respiratory system and do not cause a chronic cough. Therefore, the drugs are approved for patients suffering from bronchial asthma.

Do not forget that Physiotens can be taken by patients with diabetes, since the drug significantly increases insulin sensitivity.

No less effective hypertensive drugs can be considered Moxonidine And Rilmenidine are representatives of selective agonists of imidazoline receptors. They cope well with high blood pressure, without causing side effects at all and have virtually no contraindications.

Among the new generation blockers, it is necessary to highlight the leaders - Nebivolol, Labetalol, Carvedilol. These are excellent drugs for the treatment of hypertension, which rarely cause side effects, but at the same time prevent the terrible consequences of high blood pressure.

Fast-acting drugs

Rapid-acting medications are used to block an attack of hypertension. They are also used as a preventive measure for hypertensive crisis. After taking such tablets, blood pressure decreases instantly, and the pulse returns to normal.

List of the most effective fast-acting drugs with minimal risk of side effects

Attention! If the patient takes Andipal, then taking Papaverine and Dibazol is prohibited in parallel. Since such a drug combination only aggravates the patient’s condition.

Medicines for the elderly

In the first place are drugs to eliminate high blood pressure:

When the patient feels a significant increase in pressure, it is necessary to urgently call a medical team, and first provide the following assistance:

Additionally, it should be noted that pharmacies have outdated drugs that may be recommended to lower blood pressure. One of these is Validol, a drug used for pain in the heart muscle. Also Moxonidine And Clonidine– they were widely used several years ago to quickly reduce the manifestations of hypertension. But today doctors do not advise resorting to such outdated drugs.

Note! Very often diuretics are used to treat high blood pressure, the most popular among them are Furosemide, Lasix, Ravel, Arifon.

It is necessary to understand that when it comes to new generation drugs, they have significantly fewer side effects than previous generations of drugs. At the same time, during treatment with drugs with antihypertensive effects, a correctly selected course of therapy by the doctor, taking into account the individual characteristics of the hypertensive patient and contraindications of the drug, is of great importance.