Arterial hypertension drugs. Centrally acting drugs for hypertension Drugs used to treat hypertension

In the medulla oblongata (this is the lowest part of the brain) is vasomotor (vasomotor) center... It has two departments - pressor and depressor, which increase and decrease blood pressure, respectively, acting through the nerve centers of the sympathetic nervous system in the spinal cord. The physiology of the vasomotor center and the regulation of vascular tone is described in more detail here: http://www.bibliotekar.ru/447/117.htm (text from a textbook on normal physiology for medical schools).

The vasomotor center is important for us because there is a group of drugs that act on its receptors and thus lower blood pressure.

Departments of the brain.

Classification of centrally acting drugs

To drugs that primarily affect on sympathetic activity in the brain, relate:

  • clonidine (clonidine),
  • moxonidine (physiotens),
  • methyldopa (can be used in pregnant women),
  • guanfacine,
  • guanabenz.

In the search for pharmacies in Moscow and Belarus, no methyldopa, guanfacine and guanabenzabut sold clonidine (strictly according to the recipe) and moxonidine.

There is also a central component of action, about them - in the next section.

Clonidine (clonidine)

Clonidine (clonidine) inhibits the secretion of catecholamines by the adrenal glands and stimulates alpha 2 -adrenergic receptors and I 1 -imidazoline receptors of the vasomotor center. It reduces blood pressure (by relaxing blood vessels) and heart rate (heart rate). Clonidine also has hypnotic and analgesic effect.

The scheme of regulation of cardiac activity and blood pressure.

In cardiology, clonidine is used mainly for treatment of hypertensive crises... This drug is adored by criminals and ... retired grandmothers. Attackers like to mix clonidine into alcohol, and when the victim is “cut out” and falls asleep, they rob fellow travelers ( never drink alcohol on the road with unfamiliar people!). This is one of the reasons why clonidine (clonidine) has long been sold in pharmacies. exclusively by prescription.

The popularity of clonidine as a remedy for arterial hypertension in grandmothers "clonidine" (who cannot live without taking clonidine, like smokers without a cigarette) is due to several reasons:

  1. high efficiency drug. Local doctors prescribe it for the treatment of hypertensive crises, as well as for despair when other drugs are not effective enough or the patient cannot afford it, but something needs to be treated. Clonidine lowers blood pressure even when other drugs are ineffective. Gradually, the elderly develop mental and even physical dependence on this drug.
  2. hypnotic (sedative) Effect. Cannot sleep without their favorite medicine. Sedatives are generally popular with people, I previously wrote in detail about.
  3. anesthetic the effect also matters, especially in old age, when “ everything hurts».
  4. wide therapeutic interval (i.e. a wide range of safe doses). For example, the maximum daily dose is 1.2-2.4 mg, which is as much as 8-16 0.15 mg tablets. Few pills for pressure can be taken with impunity in such quantities.
  5. cheapness drug. Clonidine is one of the cheapest drugs, which is of paramount importance for a poor pensioner.

Clonidine is recommended for use only for the treatment of hypertensive crises, for regular intake 2-3 times a day, it is undesirable, since rapid significant fluctuations in blood pressure during the day are possible, which can be dangerous for blood vessels. The main side effects: dry mouth, dizziness and lethargy (not for drivers), development is possible depression (then clonidine should be canceled).

Orthostatic hypotension (lowering blood pressure in an upright position) clonidine does not cause.

Most dangerous side effect of clonidine - withdrawal syndrome... Grandmothers - "klofelinschitsy" take many pills per day, bringing the average daily intake to high daily doses. But since the drug is purely prescription, it will not be possible to create a six-month supply of clonidine at home. If local pharmacies, for some reason, have interruptions in supply of clonidine, these patients develop severe withdrawal symptoms. As with. Absent in the blood, clonidine no longer inhibits the release of catecholamines into the blood and does not lower blood pressure. Patients are worried agitation, insomnia, headache, palpitations, and very high blood pressure... Treatment consists in the introduction of clonidine, and.

Remember! Regular taking clonidine should not stop abruptly... You need to cancel the drug gradually, replacing? - and? -adrenergic blockers.

Moxonidine (Physiotens)

Moxonidine is a modern promising drug that can be briefly called “ improved clonidine". Moxonidine belongs to the second generation of drugs acting on the central nervous system. The drug acts on the same receptors as clonidine (clonidine), but the effect on I 1 - imidazoline receptors expressed much more strongly than the effect on alpha2-adrenergic receptors. Due to the stimulation of I 1 -receptors, the release of catecholamines (adrenaline, norepinephrine, dopamine) is inhibited, which lowers blood pressure (blood pressure). Moxonidine long-term maintains a reduced level of adrenaline in the blood. In some cases, like clonidine, in the first hour after oral administration before a decrease in blood pressure, it may increase by 10%, which is due to stimulation.

In clinical research Moxonidine reduced the systolic (upper) blood pressure by 25-30 mm Hg. Art. and diastolic (lower) pressure of 15-20 mm without developing drug resistance over 2 years of treatment. The effectiveness of the treatment was comparable to that of a beta-blocker atenolol and ACE inhibitors captopril and enalapril.

Antihypertensive effect Moxonidine lasts 24 hours, the drug is taken Once a day... Moxonidine does not increase blood sugar and lipids, and its effect does not depend on body weight, gender, and age. Moxonidine reduced LVH ( left ventricular hypertrophy), which allows the heart to live longer.

The high antihypertensive activity of moxonidine made it possible to use it for the complex treatment of patients with CHF (chronic heart failure) with II-IV functional class, but the results in the study MOXCON (1999) were depressing. After 4 months of treatment, the clinical study had to be terminated early because of the high mortality in the experimental group compared to the control group (5.3% versus 3.1%). Overall mortality increased due to increased rates of sudden death, heart failure, and acute myocardial infarction.

Moxonidine causes fewer side effects compared to clonidinealthough they are very similar. In comparative cross 6-week study of moxonidine with clonidine ( each patient received both compared drugs in a random sequence) side effects led to discontinuation of treatment in 10% of patients receiving clonidine, and only in 1.6% of patientstaking moxonidine. More often disturbed dry mouth, headache, dizziness, tiredness or drowsiness.

Withdrawal syndrome was observed on the first day after discontinuation of the drug in 14% of those who received clonidine, and only in 6% of patients receiving moxonidine.

Thus, it turns out:

  • clonidine is cheap but has many side effects
  • moxonidine costs much more, but is taken once a day and is better tolerated. It can be prescribed if drugs from other groups are not effective enough or are contraindicated.

Output: if financial situation allows, between clonidine and moxonidine for permanent reception, it is better to choose the latter (1 time per day). Clonidine is taken only in case of hypertensive crises, it is not a drug for every day.

Article update 01/30/2019

Arterial hypertension (AG) in the Russian Federation (RF) remains one of the most significant medical and social problems. This is due to the widespread prevalence of this disease (about 40% of the adult population of the Russian Federation has an increased level of blood pressure), as well as to the fact that hypertension is the most important risk factor for major cardiovascular diseases - myocardial infarction and stroke.

Constant persistent increase in blood pressure (BP) up to 140/90 mm. rt. Art. and higher - a sign of arterial hypertension (essential hypertension).

Risk factors contributing to the manifestation of arterial hypertension include:

  • Age (men over 55, women over 65)
  • Smoking
  • sedentary lifestyle,
  • Obesity (waist over 94 cm for men and over 80 cm for women)
  • Familial cases of early cardiovascular disease (in men under 55, in women under 65)
  • Pulse blood pressure in the elderly (difference between systolic (upper) and diastolic (lower) blood pressure). Normally, it is 30-50 mm Hg.
  • Fasting plasma glucose 5.6-6.9 mmol / L
  • Dyslipidemia: total cholesterol more than 5.0 mmol / L, low-density lipoprotein cholesterol 3.0 mmol / L or more, high-density lipoprotein cholesterol 1.0 mmol / L or less for men, and 1.2 mmol / L or less for women, triglycerides more than 1.7 mmol / l
  • Stressful situations
  • alcohol abuse,
  • Excessive salt intake (more than 5 grams per day).

Also, the development of hypertension is facilitated by such diseases and conditions as:

  • Diabetes mellitus (fasting plasma glucose 7.0 mmol / L or more with repeated measurements, as well as plasma glucose after meals 11.0 mmol / L or more)
  • Other endocrinological diseases (pheochromocytoma, primary aldosteronism)
  • Diseases of the kidneys and renal arteries
  • Taking medications and substances (glucocorticosteroids, non-steroidal anti-inflammatory drugs, hormonal contraceptives, erythropoietin, cocaine, cyclosporine).

Knowing the causes of the disease, you can prevent the development of complications. The elderly are at risk.

According to the modern classification adopted by the World Health Organization (WHO), hypertension is divided into:

  • Grade 1: Increased blood pressure 140-159 / 90-99 mm Hg
  • Grade 2: Increased blood pressure 160-179 / 100-109 mm Hg
  • Grade 3: Increase in blood pressure to 180/110 mm Hg and above.

Home-based BP measurements can be a valuable adjunct in monitoring treatment efficacy and are important in identifying hypertension. The patient's task is to keep a diary of self-monitoring of blood pressure, where blood pressure and heart rate are recorded when measured, at least in the morning, at lunch, in the evening. It is possible to make comments on lifestyle (getting up, eating, physical activity, stressful situations).

Blood pressure measurement technique:

  • Rapidly pump air into the cuff to a pressure level of 20 mm Hg higher than systolic blood pressure (SBP), when the pulse disappears
  • Blood pressure is measured with an accuracy of 2 mm Hg
  • Decrease the pressure in the cuff at a rate of approximately 2 mm Hg per second
  • The pressure level at which the 1st tone appears corresponds to the SBP
  • The pressure level at which the tones disappear corresponds to diastolic blood pressure (DBP)
  • If the tones are very weak, you should raise your hand and perform several squeezing movements with the hand, then repeat the measurement, while not pressing the artery with the membrane of the phonendoscope
  • At the initial measurement, blood pressure is recorded on both arms. Further, the measurement is carried out on the arm on which the blood pressure is higher
  • In patients with diabetes mellitus and in persons receiving antihypertensive drugs, blood pressure should also be measured after 2 minutes in a standing position.

Patients with hypertension experience pain in the head (often in the temporal and occipital region), episodes of dizziness, rapid fatigue, poor sleep, possibly heart pain, visual impairment.
The disease is complicated by hypertensive crises (when blood pressure rises sharply to high numbers, there is frequent urination, headache, dizziness, palpitations, feeling of heat); impaired renal function - nephrosclerosis; strokes, intracerebral hemorrhage; myocardial infarction.

To prevent complications, patients with hypertension need to constantly monitor their blood pressure and take special antihypertensive drugs.
If a person is worried about the above complaints, as well as pressure 1-2 times a month, this is a reason to contact a therapist or cardiologist, who will prescribe the necessary examinations, and subsequently determine further treatment tactics. Only after carrying out the necessary complex of examination is it possible to talk about the appointment of drug therapy.

Self-administration of medications can threaten the development of unwanted side effects, complications and can be fatal! It is forbidden to use medicines on their own according to the principle “helped friends” or to resort to the recommendations of pharmacists in pharmacy chains !!! The use of antihypertensive drugs is possible only as directed by a doctor!

The main goal of treating patients with hypertension is to minimize the risk of developing cardiovascular complications and death from them!

1. Activities to change lifestyle:

  • To give up smoking
  • Normalization of body weight
  • Consumption of alcoholic beverages less than 30 g / day of alcohol for men and 20 g / day for women
  • Increase in physical activity - regular aerobic (dynamic) load for 30-40 minutes at least 4 times a week
  • Reducing the consumption of table salt to 3-5 g / day
  • A change in diet with an increase in the consumption of plant foods, an increase in the diet of potassium, calcium (found in vegetables, fruits, grains) and magnesium (found in dairy products), as well as a decrease in the consumption of animal fats.

These measures are prescribed to all patients with arterial hypertension, including those receiving antihypertensive drugs. They allow: to lower blood pressure, to reduce the need for antihypertensive drugs, to favorably influence the existing risk factors.

2. Drug therapy

Today we will talk about these drugs - modern means for the treatment of arterial hypertension.
Arterial hypertension is a chronic disease that requires not only constant monitoring of blood pressure, but also constant medication. There is no course of antihypertensive therapy, all drugs are taken indefinitely. If monotherapy is ineffective, a selection of drugs from different groups is carried out, often combining several drugs.
As a rule, the desire of a patient with hypertension is to purchase the strongest, but not expensive, drug. However, you need to understand that this does not exist.
What drugs are offered for this to patients suffering from high blood pressure?

Each antihypertensive drug has its own mechanism of action, i.e. affect certain "Mechanisms" of increasing blood pressure :

a) Renin-angiotensin system - in the kidneys, the substance prorenin is produced (with a decrease in pressure), which passes in the blood into renin. Renin (a proteolytic enzyme) interacts with a blood plasma protein - angiotensinogen, resulting in the formation of an inactive substance angiotensin I. Angiotensin interacts with an angiotesin-converting enzyme (ACE) into the active substance angiotensin II. This substance promotes an increase in blood pressure, vasoconstriction, an increase in the frequency and strength of heart contractions, arousal of the sympathetic nervous system (which also leads to an increase in blood pressure), and an increase in the production of aldosterone. Aldosterone promotes sodium and water retention, which also increases blood pressure. Angiotensin II is one of the most powerful vasoconstrictor substances in the body.

b) Calcium channels of our body cells - calcium in the body is in a bound state. When calcium enters the cell through special channels, a contractile protein, actomyosin, is formed. Under its action, the vessels narrow, the heart begins to contract more strongly, the pressure rises and the heart rate increases.

c) Adrenergic receptors - in our body, in some organs there are receptors, the irritation of which affects blood pressure. These receptors include alpha-adrenergic receptors (α1 and α2) and beta-adrenergic receptors (β1 and β2). Stimulation of α1-adrenergic receptors leads to an increase in blood pressure, α2-adrenergic receptors - to a decrease in blood pressure. Α-adrenergic receptors are located in arterioles. β1-adrenergic receptors are localized in the heart, in the kidneys, their stimulation leads to an increase in heart rate, an increase in myocardial oxygen demand and an increase in blood pressure. Stimulation of β2-adrenergic receptors located in the bronchioles causes the expansion of the bronchioles and the removal of bronchospasm.

d) Urinary system- as a result of an excess amount of water in the body, blood pressure rises.

e) Central nervous system- Excitation of the central nervous system increases blood pressure. The brain contains vasomotor centers that regulate blood pressure levels.

So, we examined the main mechanisms of increasing blood pressure in the human body. It's time to move on to the means for lowering pressure (antihypertensive), which affect these very mechanisms.

Classification of drugs for arterial hypertension

  1. Diuretics (diuretics)
  2. Calcium channel blockers
  3. Beta-blockers
  4. Drugs acting on the renin-angiotensive system
    1. Angiotensive receptor blockers (antagonists) (sartans)
  5. Centrally acting neurotropic agents
  6. Drugs acting on the central nervous system (CNS)
  7. Alpha blockers

1. Diuretics (diuretics)

As a result of the removal of excess fluid from the body, blood pressure decreases. Diuretics prevent the reabsorption of sodium ions, which are then excreted and carried away with them. In addition to sodium ions, diuretics flush out potassium ions from the body, which are necessary for the cardiovascular system to function. There are potassium-sparing diuretics.

Representatives:

  • Hydrochlorothiazide (Hypothiazide) - 25mg, 100mg, is a part of combination drugs; Long-term use at a dosage higher than 12.5 mg is not recommended, due to the possible development of type 2 diabetes!
  • Indapamide (Arifonretard, Ravel SR, Indapamide MV, Indap, Ionic retard, Acripamidretard) - more often the dosage is 1.5 mg.
  • Triampur (a combination diuretic containing potassium-sparing triamterene and hydrochlorothiazide);
  • Spironolactone (Veroshpiron, Aldactone). Has a significant side effect (in men it causes the development of gynecomastia, mastodynia).
  • Eplerenone (Inspra) - often used in patients with chronic heart failure, does not cause the development of gynecomastia and mastodynia.
  • Furosemide 20mg, 40mg. The drug is short but fast acting. It inhibits the reabsorption of sodium ions in the ascending knee of Henle's loop, proximal and distal tubules. Increases the excretion of bicarbonates, phosphates, calcium, magnesium.
  • Torasemide (Diuver) - 5mg, 10mg, is a loop diuretic. The main mechanism of action of the drug is due to the reversible binding of torasemide to the sodium / chlorine / potassium ion counterporter located in the apical membrane of the thick segment of the ascending part of Henle's loop, as a result of which the reabsorption of sodium ions is reduced or completely inhibited and the osmotic pressure of the intracellular fluid and water reabsorption decrease. Blocks myocardial aldosterone receptors, reduces fibrosis and improves diastolic myocardial function. Torasemide, to a lesser extent than furosemide, causes hypokalemia, while it is more active, and its effect is longer.

Diuretics are prescribed in combination with other antihypertensive drugs. Indapamide is the only diuretic used for hypertension alone.
Fast-acting diuretics (furosemide) are undesirable to use systematically in hypertension, they are taken in emergency conditions.
When using diuretics, it is important to take potassium supplements in courses of up to 1 month.

2. Calcium channel blockers

Calcium channel blockers (calcium antagonists) are a heterogeneous group of drugs that have the same mechanism of action, but differ in a number of properties, including pharmacokinetics, tissue selectivity, and the effect on heart rate.
Another name for this group is calcium ion antagonists.
There are three main AA subgroups: dihydropyridine (the main representative is nifedipine), phenylalkylamines (the main representative is verapamil) and benzothiazepines (the main representative is diltiazem).
Recently, they began to be divided into two large groups, depending on the effect on the heart rate. Diltiazem and verapamil are referred to as the so-called “slowing down” calcium antagonists (nondihydropyridine). Another group (dihydropyridine) includes amlodipine, nifedipine and all other dihydropyridine derivatives that increase or do not change the heart rate.
Calcium channel blockers are used for arterial hypertension, coronary heart disease (contraindicated in acute forms!) And arrhythmias. For arrhythmias, not all calcium channel blockers are used, but only pulsating ones.

Representatives:

Pulsing (non-dihydropyridine):

  • Verapamil 40mg, 80mg (prolonged: Isoptin SR, Verogalid EP) - dosage 240mg;
  • Diltiazem 90mg (Altiazem PP) - dosage 180mg;

The following representatives (dihydropyridine derivatives) are not used for arrhythmias: Contraindicated in acute myocardial infarction and unstable angina !!!

  • Nifedipine (Adalat, Kordaflex, Kordafen, Kordipin, Corinfar, Nifecard, Fenigidin) - dosage 10 mg, 20 mg; Nifecard XL 30mg, 60mg.
  • Amlodipine (Norvask, Normodipin, Tenox, Cordi Cor, Es Cordi Cor, Cardilopin, Kalchek,
  • Amlotop, Omelarkardio, Amlovas) - dosage 5mg, 10mg;
  • Felodipine (Plendil, Felodip) - 2.5mg, 5mg, 10mg;
  • Nimodipine (Nimotop) - 30mg;
  • Lacidipine (Lazipil, Sakur) - 2mg, 4mg;
  • Lercanidipine (Lerkamen) - 20mg.

Of the side effects of dihydropyridine derivatives, it is possible to indicate edema, mainly of the lower extremities, headache, redness of the face, increased heart rate, increased urination. If swelling persists, the drug must be replaced.
Lerkamen, a representative of the third generation of calcium antagonists, due to its higher selectivity to slow calcium channels, causes edema to a lesser extent compared to other representatives of this group.

3. Beta-blockers

There are drugs that do not selectively block receptors - non-selective action, they are contraindicated in bronchial asthma, chronic obstructive pulmonary disease (COPD). Other agents selectively block only the beta receptors of the heart - selective action. All beta-blockers interfere with the synthesis of prorenin in the kidneys, thereby blocking the renin-angiotensin system. In this regard, the vessels dilate, blood pressure decreases.

Representatives:

  • Metoprolol (Betaloc ZOK 25mg, 50mg, 100mg, Egilok retard 25mg, 50mg, 100mg, 200mg, Egilok C, Vasokardinretard 200 mg, Metocardretard 100 mg) ;;
  • Bisoprolol (Concor, Coronal, Biol, Bisogamma, Cordinorm, Niperten, Biprol, Bidop, Aritel) - most often the dosage is 5mg, 10mg;
  • Nebivolol (Nebilet, Binelol) 5 mg, 10 mg
  • Betaxolol (Lokren) - 20 mg;
  • Carvedilol (Carvetrend, Coriol, Talliton, Dilatrend, Acridiol) - mainly a dosage of 6.25mg, 12.5mg, 25mg.

Drugs in this group are used for hypertension, combined with coronary heart disease and arrhythmias.
Short-acting drugs, the use of which is not rational for hypertension: anaprilin (obzidan), atenolol, propranolol.

The main contraindications for beta blockers are:

  • bronchial asthma;
  • low pressure;
  • sick sinus syndrome;
  • peripheral arterial pathology;
  • bradycardia;
  • cardiogenic shock;
  • atrioventricular block of the second or third degree.

4. Drugs acting on the renin-angiotensin system

The drugs act at different stages in the formation of angiotensin II. Some inhibit (suppress) the angiotensin-converting enzyme, others block the receptors on which angiotensin II acts. The third group inhibits renin, represented by only one drug (aliskiren).

Angiotensin-converting enzyme (ACE) inhibitors

These drugs prevent the conversion of angiotensin I to active angiotensin II. As a result, the concentration of angiotensin II in the blood decreases, the vessels dilate, and the pressure decreases.
Representatives (synonyms are indicated in brackets - substances with the same chemical composition):

  • Captopril (Kapoten) - dosage 25mg, 50mg;
  • Enalapril (Renitek, Berlipril, Renipril, Ednit, Enap, Enarenal, Enam) - the dosage is most often 5mg, 10mg, 20mg;
  • Lisinopril (Diroton, Dapril, Lizigamma, Lizinoton) - the dosage is most often 5mg, 10mg, 20mg;
  • Perindopril (Prestarium A, Perineva) - Perindopril - dosage 2.5mg, 5mg, 10mg. Perineva - dosage 4mg, 8mg;
  • Ramipril (Tritace, Amprilan, Hartil, Pyramil) - dosage 2.5mg, 5mg, 10mg;
  • Hinapril (Akcupro) - 5mg, 10mg, 20mg, 40mg;
  • Fosinopril (Fozikard, Monopril) - at a dosage of 10mg, 20mg;
  • Trandolapril (Gopten) - 2mg;
  • Zofenopril (Zokardis) - dosage 7.5mg, 30mg.

The drugs are available in different dosages for therapy with varying degrees of increased blood pressure.

A feature of the drug Captopril (Capoten) is that it is rational due to its short duration of action only with hypertensive crises.

A prominent representative of the Enalapril group and its synonyms are used very often. This drug does not differ in the duration of action, therefore, it is taken 2 times a day. In general, the full effect of ACE inhibitors can be observed after 1-2 weeks of drug use. In pharmacies you can find a variety of generics (analogues) of enalapril, i.e. cheaper drugs containing enalapril, which are produced by small manufacturers. We discussed the quality of generics in another article, but here it is worth noting that generics of enalapril are suitable for someone, for someone they do not work.

ACE inhibitors have a side effect - dry cough. In cases of coughing, ACE inhibitors are replaced with drugs of another group.
This group of drugs is contraindicated in pregnancy, has a teratogenic effect in the fetus!

Angiotensin receptor blockers (antagonists) (sartans)

These drugs block angiotensin receptors. As a result, angiotensin II does not interact with them, blood vessels dilate, blood pressure decreases

Representatives:

  • Losartan (Cozaar 50mg, 100mg; Lozap 12.5mg, 50mg, 100mg; Lorista 12.5mg, 25mg, 50mg, 100mg; Vazotenz 50mg, 100mg);
  • Eprosartan (Teveten) - 400mg, 600mg;
  • Valsartan (Diovan 40mg, 80mg, 160mg, 320mg; Valsacor 80mg, 160mg, 320mg, Valz 40mg, 80mg, 160mg; Nortivan 40mg, 80mg, 160mg; Valsafors 80mg, 160mg);
  • Irbesartan (April) - 150mg, 300mg;
    Candesartan (Atacand) - 8mg, 16mg, 32mg;
    Telmisartan (Mikardis) - 40mg, 80mg;
    Olmesartan (Cardosal) - 10mg, 20mg, 40mg.

Just like the predecessors, they allow you to evaluate the full effect 1-2 weeks after the start of the intake. Does not cause dry cough. Should not be used during pregnancy! If pregnancy is detected during the treatment period, antihypertensive therapy with drugs of this group should be discontinued!

5. Neurotropic agents of central action

Centrally acting neurotropic drugs affect the vasomotor center in the brain, reducing its tone.

  • Moxonidine (Physiotens, Moxonitex, Moxogamma) - 0.2 mg, 0.4 mg;
  • Rilmenidine (Albarel (1mg) - 1mg
  • Methyldopa (Dopegit) 250 mg

The first representative of this group is clonidine, which was previously widely used in hypertension. Now this drug is dispensed strictly by prescription.
Currently, moxonidine is used both for emergency care in hypertensive crisis and for routine therapy. Dosage 0.2mg, 0.4mg. The maximum daily dosage is 0.6 mg / day.

6. Funds acting on the central nervous system

If hypertension is caused by prolonged stress, then drugs acting on the central nervous system are used (sedatives (Novopassit, Persen, Valerian, Motherwort, tranquilizers, sleeping pills).

7. Alpha-blockers

These agents bind to alpha-adrenergic receptors and block them from the irritating effect of norepinephrine. As a result, blood pressure decreases.
The representative used - Doxazosin (Kardura, Tonokardin) - is more often produced in dosages of 1 mg, 2 mg. It is used to relieve seizures and long-term therapy. Many alpha blocker drugs have been discontinued.

Why are several drugs taken at once for arterial hypertension?

At the initial stage of the disease, the doctor prescribes one drug, based on some research and taking into account the existing diseases in the patient. If one drug is ineffective, it is not uncommon to add other drugs to create a blood pressure lowering drug combination that targets different blood pressure lowering mechanisms. Combination therapy for refractory (persistent) arterial hypertension can combine up to 5-6 drugs!

The drugs are selected from different groups. For example:

  • aCE inhibitor / diuretic;
  • angiotensin receptor blocker / diuretic;
  • aCE inhibitor / calcium channel blocker;
  • aCE inhibitor / calcium channel blocker / beta-blocker;
  • angiotensin receptor blocker / calcium channel blocker / beta-blocker;
  • aCE inhibitor / calcium channel blocker / diuretic and other combinations.

There are drug combinations that are irrational, such as pulsating beta-blockers / calcium channel blockers, beta-blockers / centrally acting drugs, and other combinations. It is dangerous to self-medicate !!!

There are combination drugs that combine components of substances from different groups of antihypertensive drugs in 1 tablet.

For example:

  • aCE inhibitor / diuretic
    • Enalapril / Hydrochlorothiazide (Co-renitec, Enap NL, Enap N,
    • Enap NL 20, Renipril GT)
    • Enalapril / Indapamide (Enziks duo, Enziks duo forte)
    • Lisinopril / Hydrochlorothiazide (Iruzid, Lizinoton, Liten N)
    • Perindopril / Indapamide (NoliprelA and NoliprelAforte)
    • Quinapril / Hydrochlorothiazide (Akkuzid)
    • Fosinopril / Hydrochlorothiazide (Fosicard N)
  • angiotensin receptor blocker / diuretic
    • Losartan / Hydrochlorothiazide (Gizaar, Lozap plus, Lorista N,
    • Lorista ND)
    • Eprosartan / Hydrochlorothiazide (Teveten Plus)
    • Valsartan / Hydrochlorothiazide (Co-diovan)
    • Irbesartan / Hydrochlorothiazide (Co-aprovel)
    • Candesartan / Hydrochlorothiazide (Atacand Plus)
    • Telmisartan / HCT (Mikardis Plus)
  • aCE inhibitor / calcium channel blocker
    • Trandolapril / Verapamil (Tarka)
    • Lisinopril / Amlodipine (Equator)
  • angiotensin receptor blocker / calcium channel blocker
    • Valsartan / Amlodipine (Exforge)
  • dihydropyridine calcium channel blocker / beta-blocker
    • Felodipine / metoprolol (Logimax)
  • beta-blocker / diuretic (not for diabetes and obesity)
    • Bisoprolol / Hydrochlorothiazide (Lodoz, Aritel plus)

All drugs are available in different dosages of one and the other component; the doctor should select the doses for the patient.

Achieving and maintaining target blood pressure levels require long-term medical supervision with regular monitoring of the patient's compliance with recommendations for lifestyle changes and adherence to the prescribed antihypertensive drugs, as well as correction of therapy depending on the effectiveness, safety and tolerability of treatment. With dynamic observation, it is crucial to establish personal contact between the doctor and the patient, to educate patients in schools for hypertensive patients, increasing patient adherence to treatment.

april 27, 2012

In the treatment of hypertension, there are two approaches: drug therapy and the use of non-drug methods of lowering blood pressure.

Non-drug therapy of hypertension

If you carefully study the table "Risk stratification in patients with arterial hypertension", you will notice that the risk of serious complications, such as heart attacks, strokes, is influenced not only by the degree of increase in blood pressure, but also by many other factors, for example, smoking, obesity, sedentary lifestyle life.

Therefore, it is very important for patients suffering from essential hypertension to change their lifestyle: to quit smoking. start following a diet, as well as choosing physical activity that is optimal for the patient.

It is necessary to understand that lifestyle changes improve the prognosis for arterial hypertension and other cardiovascular diseases, no less than blood pressure ideally controlled with the help of medications.

To give up smoking

Thus, the life expectancy of a smoker is on average 10-13 years less than that of nonsmokers, with cardiovascular diseases and oncology becoming the main causes of death.

If you quit smoking, the risk of developing or aggravating heart and vascular diseases decreases within two years to the level of nonsmokers.

Diet

Compliance with a low-calorie diet with the use of large amounts of plant foods (vegetables, fruits, herbs) will reduce the weight of patients. It is known that every 10 kilograms of excess weight increases blood pressure by 10 mm Hg.

In addition, excluding cholesterol-containing foods from food will reduce blood cholesterol levels, a high level of which, as can be seen from the table, is also one of the risk factors.

Limiting table salt to 4-5 grams per day has been proven to reduce blood pressure, since with a decrease in salt content, the amount of fluid in the vascular bed will also decrease.

In addition, reducing weight (especially waist circumference) and limiting sweets will reduce the risk of developing diabetes, which significantly worsens the prognosis of patients with arterial hypertension. But even in patients with diabetes, weight loss can lead to normalization of blood glucose.

Physical exercise

Exercise is also very important for hypertensive patients. With physical activity, the tone of the sympathetic nervous system decreases: the concentration of adrenaline, norepinephrine decreases, which have a vasoconstrictor effect and increase heart contractions. And as you know, it is the imbalance in the regulation of cardiac output and vascular resistance to blood flow that causes an increase in blood pressure. In addition, with moderate loads performed 3-4 times a week, the cardiovascular and respiratory systems are trained: blood supply and oxygen delivery to the heart and target organs improve. In addition, exercise, coupled with diet, leads to weight loss.

It should be noted that in patients with low and moderate risk of cardiovascular complications, treatment of hypertension begins with the appointment for several weeks or even months (at low risk) of non-drug therapy, the purpose of which is to reduce the volume of the abdomen (less than 102 in men, less than 88 cm), as well as the elimination of risk factors. If there are no dynamics against the background of such treatment, pills are added.

In patients with high and very high risk according to the risk stratification table, drug therapy should be prescribed already at the moment when hypertension is first diagnosed.

Drug therapy for hypertension.

The scheme for selecting treatment for patients with essential hypertension can be formulated in several theses:

  • In low- to moderate-risk patients, therapy begins with one blood pressure lowering drug.
  • For patients with high and very high risk of cardiovascular complications, it is advisable to prescribe two drugs in a small dosage.
  • If the target blood pressure (at least below 140/90 mm Hg, ideally 120/80 and below) is not achieved in patients with low and moderate risk, either increase the dosage of the drug they receive, or start giving the drug from another groups in a small dose. In case of repeated failure, it is advisable to treat with two drugs of different groups in small dosages.
  • If BP targets are not met in high-risk and very high-risk patients, you can either increase the dosage of the patient's drugs or add a third drug from a different group to treatment.
  • If, with a decrease in blood pressure to 140/90 or below, the patient's well-being has worsened, it is necessary to leave taking drugs at this dosage until the body gets used to the new blood pressure figures, and then continue lowering blood pressure to the target values \u200b\u200b- 110 / 70-120 / 80 mm Hg

Groups of drugs for the treatment of arterial hypertension:

The choice of drugs, their combinations and dosage should be made by a doctor, while it is necessary to take into account the presence of concomitant diseases and risk factors in the patient.

The main six groups of drugs for the treatment of hypertension are listed below, as well as absolute contraindications for drugs in each group.

  • Angiotensin converting enzyme inhibitors - ACE inhibitors: enalapril (Enap, Enam, Renitek, Berlipril), lisinopril (Diroton), ramipril (Tritace®, Amprilan®), fosinopril (Fozicard, Monopril) and others. Drugs in this group are contraindicated in high blood potassium, pregnancy, bilateral stenosis (narrowing) of the renal vessels, angioedema.
  • Angiotensin-1 Receptor Blockers - ARBs: valsartan (Diovan, Valsakor®, Valz), losartan (Kozaar, Lozap, Lorista), irbesartan (Aprovel®), candesartan (Atakand, Kandekor). Contraindications are the same as for ACE inhibitors.
  • β-blockers - β-AB: nebivolol (Nebilet), bisoprolol (Concor), metoprolol (Egilok®, Betalok®) . Drugs of this group cannot be used in patients with atrioventricular block of 2 and 3 degrees, bronchial asthma.
  • Calcium antagonists - AK. Dihydropyridine: nifedipine (Cordaflex®, Corinfar®, Cordipin®, Nifecard®), amlodipine (Norvask®, Tenox®, Normodipin®, Amlotop). Non-dihydropyridine: Verapamil, Diltiazem.

ATTENTION! Nonhydropyridine calcium channel antagonists are contraindicated in chronic heart failure and atrioventricular block of 2-3 degrees.

  • Diuretics (diuretics). Thiazide: hydrochlorothiazide (Hypothiazide), indapamide (Arifon, Indap). Loopback: spironolactone (Veroshpiron).

ATTENTION! Diuretics from the group of aldosterone antagonists (Veroshpiron) are contraindicated in chronic renal failure and high blood potassium.

  • Renin inhibitors. This is a new group of drugs that have shown themselves well in clinical trials. The only renin inhibitor currently registered in Russia is Aliskiren (Rasilez).

Effective combinations of drugs that reduce blood pressure

Since patients often have to prescribe two or sometimes more drugs that have an antihypertensive (pressure lowering) effect, the most effective and safe group combinations are given below.

  • aCE inhibitors + diuretic;
  • aCE inhibitors + AK;
  • ARB + \u200b\u200bdiuretic;
  • ARRA + AK;
  • AK + diuretic;
  • AK dihydropyridine (nifedipine, amlodipine, etc.) + β-AB;
  • β-AB + diuretic :;
  • β-AB + α-AB: Carvedilol (Dilatrend®, Acridilol®)

Irrational combinations of antihypertensive drugs

The use of two drugs of the same group, as well as combinations of drugs indicated below, is unacceptable, since drugs in such combinations increase the side effects, but do not potentiate the positive effects of each other.

  • aCE inhibitors + potassium-sparing diuretic (Veroshpiron);
  • β-AB + nondihydropyridine AA (Verapamil, Diltiazem);
  • β-AB + centrally acting drug.

Combinations of drugs that are not found in any of the lists belong to an intermediate group: their use is possible, but it must be remembered that there are more effective combinations of antihypertensive drugs.

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No. 7. Centrally acting drugs for the treatment of arterial hypertension

You are reading a series of articles on antihypertensive (antihypertensive) drugs. If you want a more holistic view of the topic, please start at the very beginning: an overview of antihypertensive drugs acting on the nervous system.

In the medulla oblongata (this is the lowest part of the brain) is vasomotor (vasomotor) center... It has two departments - pressor and depressor... which increase and decrease blood pressure, respectively, acting through the nerve centers of the sympathetic nervous system in the spinal cord. The physiology of the vasomotor center and the regulation of vascular tone is described in more detail here: http://www.bibliotekar.ru/447/117.htm (text from a textbook on normal physiology for medical schools).

The vasomotor center is important for us because there is a group of drugs that act on its receptors and thus lower blood pressure.

Departments of the brain.

Classification of centrally acting drugs

To drugs that primarily affect on sympathetic activity in the brain... relate:

  • clonidine (clonidine) ,
  • moxonidine (physiotens) ,
  • methyldopa (can be used in pregnant women),
  • guanfacine ,
  • guanabenz .

In the search for pharmacies in Moscow and Belarus, no methyldopa, guanfacine and guanabenza... but sold clonidine (strictly according to the recipe) and moxonidine .

The central component of action is also found in serotonin receptor blockers. about them - in the next part.

Clonidine (clonidine)

Clonidine (clonidine) inhibits the secretion of catecholamines by the adrenal glands and stimulates alpha 2 -adrenergic receptors and I 1 -imidazoline receptors of the vasomotor center. It reduces blood pressure (by relaxing blood vessels) and heart rate (heart rate). Clonidine also has hypnotic and analgesic effect .

The scheme of regulation of cardiac activity and blood pressure.

In cardiology, clonidine is used mainly for treatment of hypertensive crises... This drug is adored by criminals and. retired grandmothers. Attackers like to mix clonidine into alcohol, and when the victim is “cut out” and falls asleep, they rob fellow travelers ( never drink alcohol on the road with unfamiliar people!). This is one of the reasons why clonidine (clonidine) has long been sold in pharmacies. exclusively by prescription .

The popularity of clonidine as a remedy for arterial hypertension in grandmothers "clonidine" (who cannot live without taking clonidine, like smokers without a cigarette) is due to several reasons:

  1. high efficiency drug. Local doctors prescribe it for the treatment of hypertensive crises, as well as for despair when other drugs are not effective enough or the patient cannot afford it, but something needs to be treated. Clonidine lowers blood pressure even when other drugs are ineffective. Gradually, the elderly develop mental and even physical dependence on this drug.
  • hypnotic (sedative) Effect. Cannot sleep without their favorite medicine. Sedatives are generally popular with people, I previously wrote in detail about Corvalol.
  • anesthetic the effect also matters, especially in old age, when “ everything hurts ».
  • wide therapeutic interval (i.e. a wide range of safe doses). For example, the maximum daily dose is 1.2-2.4 mg, which is as much as 8-16 0.15 mg tablets. Few pills for pressure can be taken with impunity in such quantities.
  • cheapness drug. Clonidine is one of the cheapest drugs, which is of paramount importance for a poor pensioner.
  • Clonidine is recommended for use only for the treatment of hypertensive crises... for regular intake 2-3 times a day, it is undesirable, since rapid significant fluctuations in blood pressure during the day are possible, which can be dangerous for blood vessels. The main side effects. dry mouth, dizziness and lethargy (not for drivers), development is possible depression (then clonidine should be canceled).

    Orthostatic hypotension (lowering blood pressure in an upright position) clonidine does not cause .

    Most dangerous side effect of clonidine - withdrawal syndrome... Grandmothers - "klofelinschitsy" take many pills per day, bringing the average daily intake to high daily doses. But since the drug is purely prescription, it will not be possible to create a six-month supply of clonidine at home. If local pharmacies, for some reason, have interruptions in supply of clonidine... these patients develop severe withdrawal symptoms. As with a binge. The absence of clonidine in the blood no longer inhibits the release of catecholamines into the blood and does not lower blood pressure. Patients are worried agitation, insomnia, headache, palpitations, and very high blood pressure... Treatment consists of the administration of clonidine, alpha-blockers and beta-blockers.

    Remember! Regular taking clonidine should not stop abruptly... You need to cancel the drug gradually... replacing α- and β-blockers.

    Moxonidine (Physiotens)

    Moxonidine is a modern promising drug that can be briefly called “ improved clonidine ". Moxonidine belongs to the second generation of drugs acting on the central nervous system. The drug acts on the same receptors as clonidine (clonidine), but the effect on I 1 - imidazoline receptors expressed much more strongly than the effect on alpha2-adrenergic receptors. Due to the stimulation of I 1 -receptors, the release of catecholamines (adrenaline, norepinephrine, dopamine) is inhibited, which lowers blood pressure (blood pressure). Moxonidine long-term maintains a reduced level of adrenaline in the blood. In some cases, like clonidine, in the first hour after oral administration before a decrease in blood pressure, it may increase by 10%, which is due to the stimulation of alpha1 and alpha2-adrenergic receptors.

    In clinical research Moxonidine reduced the systolic (upper) blood pressure by 25-30 mm Hg. Art. and diastolic (lower) pressure of 15-20 mm without developing drug resistance over 2 years of treatment. The effectiveness of the treatment was comparable to that of a beta-blocker atenolol and ACE inhibitors captopril and enalapril .

    Antihypertensive effect Moxonidine lasts 24 hours, the drug is taken Once a day... Moxonidine does not increase blood sugar and lipids, and its effect does not depend on body weight, gender, and age. Moxonidine reduced LVH ( left ventricular hypertrophy), which allows the heart to live longer.

    The high antihypertensive activity of moxonidine made it possible to use it for the complex treatment of patients with CHF (chronic heart failure) with II-IV functional class, but the results in the study MOXCON (1999) were depressing. After 4 months of treatment, the clinical study had to be terminated early because of the high mortality in the experimental group compared to the control group (5.3% versus 3.1%). Overall mortality increased due to increased rates of sudden death, heart failure, and acute myocardial infarction.

    Moxonidine causes fewer side effects compared to clonidine... although they are very similar. In comparative cross 6-week study of moxonidine with clonidine ( each patient received both compared drugs in a random sequence) side effects led to discontinuation of treatment in 10% of patients receiving clonidine, and only in 1.6% of patients... taking moxonidine. More often disturbed dry mouth, headache, dizziness, tiredness or drowsiness .

    Withdrawal syndrome was observed on the first day after discontinuation of the drug in 14% of those who received clonidine, and only in 6% of patients receiving moxonidine.

    Thus, it turns out:

    • clonidine is cheap but has many side effects
    • moxonidine costs much more, but is taken once a day and is better tolerated. It can be prescribed if drugs from other groups are not effective enough or are contraindicated.

    Output... if financial situation allows, between clonidine and moxonidine for permanent reception, it is better to choose the latter (1 time per day). Clonidine is taken only in case of hypertensive crises, it is not a drug for every day.

    Hypertension treatment

    What methods are used to treat hypertension? In what cases is hospitalization necessary for hypertension?

    Non-drug treatments for hypertension

    • Low-calorie diet (especially if you are overweight). With a decrease in excess body weight, a decrease in blood pressure is noted.
    • Limiting the intake of table salt to 4 - 6 g per day. This increases the sensitivity to antihypertensive therapy. There are salt "substitutes" (potassium salt preparations - sanasol).
    • The inclusion in the diet of foods rich in magnesium (legumes, millet, oatmeal).
    • Increased physical activity (gymnastics, dosed walking).
    • Relaxation therapy, autogenous training, acupuncture, electrosleep.
    • Elimination of harm (smoking, drinking alcohol, taking hormonal contraceptives).
    • Employment of patients taking into account his illness (excluding night work, etc.).

    Drug-free treatment carried out with a mild form of arterial hypertension. If after 4 weeks of such treatment, the diastolic pressure remains 100 mm Hg. Art. and above, then they switch to drug therapy. If the diastolic pressure is below 100 mm Hg. Art. then non-drug treatment is continued for up to 2 months.

    In persons with a burdened history, with left ventricular hypertrophy, drug therapy is started earlier or combined with non-drug therapy.

    Medication for the treatment of arterial hypertension

    There are many antihypertensive drugs. When choosing a drug, many factors are taken into account (gender of the patient, possible complications).

    • For example, centrally acting drugs that block sympathetic influences (clonidine, dopegit, alpha-methyl-DOPA).
    • In women in the climacteric period, when there is a low activity of renin, relative hyperaldosteronism, a decrease in the level of progesterone, hypervolumic conditions are often noted, and "edematous" hypertensive crises develop. In such a situation, the drug of choice is a diuretic (saluretic).
    • There are powerful drugs - ganglion blockers, which are used in the relief of hypertensive crisis or together with other antihypertensive drugs in the treatment of malignant hypertension. Ganglion blockers should not be used in the elderly who are prone to orthostatic hypotension. With the introduction of these drugs, the patient must be in a horizontal position for some time.
    • Beta-blockers provide a hypotensive effect by reducing the minute volume of the heart and plasma renin activity. In young people, they are the drugs of choice.
    • Calcium antagonists are prescribed when hypertension is combined with ischemic heart disease.
    • Alpha-adrenergic blockers.
    • Vasodilators (eg, minoxidil). They are used in addition to the main therapy.
    • Angiotensin converting enzyme (ACE) inhibitors. These drugs are used in all forms of hypertension.

    When prescribing drugs, the state of the target organs (heart, kidneys, brain) is taken into account.

    For example, the use of beta-blockers in patients with renal failure is not indicated, since they impair renal blood flow.

    It is not necessary to strive for a rapid decrease in blood pressure, since this can lead to a deterioration in the patient's well-being. Therefore, the drug is prescribed starting with small doses.

    Arterial hypertension therapy regimen

    There is a treatment regimen for arterial hypertension: at the first stage, beta-blockers or diuretics are used; at the second stage "beta-blockers + diuretics", possibly an ACE inhibitor; with severe hypertension, complex therapy is carried out (possibly an operation).

    A hypertensive crisis often develops when medical recommendations are not followed. In crises, drugs are most often prescribed: clonidine, nifedipine, captopril.

    Indications for hospitalization

    • Clarification of the nature of arterial hypertension (if it is impossible to perform studies on an outpatient basis).
    • Complication of the course of arterial hypertension (crisis, stroke, etc.).
    • Refractory arterial hypertension, not amenable to antihypertensive therapy.

    Essential hypertension (HD) is an increase in blood pressure (BP) above 140/80 MHg.

    Distinguish between essential and symptomatic hypertension. Essential hypertension, which is often called essential hypertension (HD), accounts for about 90% of all cases of arterial hypertension. In essential hypertension, the specific cause of the increase in blood pressure, as a rule, cannot be identified. In the development of this form of the disease, an important role belongs to the activation of the sympatho-adrenal, renin-angiotensin, kalekriein-kinin systems. The reasons for such activation may be hereditary predisposition, psychoemotional overstrain, overweight, physical inactivity, etc. Hypertension is called symptomatic or secondary if the cause of the increase in pressure are diseases or damage to organs (kidneys, endocrine disorders, congenital and acquired defects of the heart and blood vessels). Treatment of this form of HD begins with the elimination of the cause that caused the increase in blood pressure. Hypertensive disease is not dangerous in itself - complications of hypertension - hemorrhagic stroke, heart failure, nephrosclerosis, coronary heart disease - pose a threat.

    Therapy for patients with hypertension has two objectives:

    1. Reduce blood pressure below 140/90 mm Hg. Art.

    2. to prevent or slow down the development of complications;

    Currently, a large number of groups of drugs are used to treat hypertension:

    1. β-blockers;

    2. ACE inhibitors;

    5.diuretics,

    4. blockers of slow calcium channels;

    5. α-blockers;

    6. blockers of AT1-anigiotensin receptors;

    7. agonists of I 1 -imidazodine receptors;

    8.agonists of central α 2 -adrenergic receptors

    9.vasodilators

    10. other groups of drugs that reduce blood pressure.

    However, despite the many pharmacological groups, the first four play the main role in the treatment of hypertension.

    β-ADRENO BLOCKERS.

    (for a detailed description of the group, see the lecture on β-blockers)

    β-blockers belong to the first-line drugs of antihypertensive drugs, especially their use in patients with increased activity of the sympathoadrenal system, β-blockers have several mechanisms leading to a persistent decrease in blood pressure:

    Decrease in cardiac output by 15-20% due to weakening of myocardial contractility and a decrease in heart rate,

    Decrease in the activity of the vasomotor center,

    Decreased secretion of renin,

    Decrease in the total peripheral vascular resistance (this effect is expressed in drugs with vasodilating activity)

    In the treatment of hypertension, preference should be given to β-blockers with vasodilating properties (carvedilol and nebivolol) and cardioselective drugs (atenolol, betaxolop, bisoprolol). The former are recommended to be used because of the increased peripheral vascular resistance in most patients. The latter, to a lesser extent than non-selective drugs, negatively affect vascular tone. In addition, cardioselective blockers are safer when administered to patients with bronchial asthma. With hypertension, it is advisable to use long-acting drugs (betaxolol, talinolol-retard, nadolol, atenolol). First, it is more convenient for patients to take the drugs once a day. Secondly, the use of short-acting drugs has disadvantages: fluctuations in the activity of the sympathoadrenal system in accordance with changes in the concentration of the drug in the body during the day, and with a sudden withdrawal of the drug, it is possible to develop the syndrome of "recoil" - a sharp increase in blood pressure. A stable hypotensive effect of β-blockers develops 3-4 weeks after starting the drug. It is stable and does not depend on physical activity and psychoemotional state of the patient. β-blockers reduce left ventricular hypertrophy and improve myocardial contractile activity.

    The antihypertensive effect of β-blockers is enhanced when combined with diuretics, calcium antagonists, α-blockers, ACE inhibitors.

    α - ADRENO BLOCKERS.

    The classification of α-adrenergic receptor blockers is based on their selectivity in relation to various α-adrenergic receptors:

    1. Non-selective α-adrenoblotators: dihydrogenated ergot alkaloids, tropafen, phentolamine;

    2. Selective α-adrenergic blockers: prozosin, doxazosin, terazosin.

    Currently, selective α-adrenergic blockers are used for hypertension. Drugs blocking α-adrenergic receptors reduce systemic vascular resistance, reverse the development of left ventricular hypertrophy, and improve the lipid composition of the blood. The presence of a large number of α-adrenergic receptors in the smooth muscles of the prostate gland and the bladder neck allows the use of drugs in patients with prostate adenoma to improve urination.

    Prazosin is a selective short-acting α 1 -adrenoceptor blocker. When taken orally, it is rapidly absorbed in the gastrointestinal tract. Bioavailability of prazosin is 60%. More than 90% of prazosin binds to plasma proteins. The maximum concentration in the blood is determined after 2-3 hours. The half-life of prazosin is 3-4 hours. The latent period of the drug is 30-60 minutes, the duration of action is 4-6 hours. It is metabolized in the liver. 90% of prazosin and its metabolites are excreted through the intestines, the rest through the kidneys. The drug is taken 2-3 times a day, the daily dose is 3-20 mg. Prazosin is characterized by the "first dose" effect - a sharp decrease in blood pressure after taking the first dose of the drug, so treatment is started with small doses of the drug (0.5-1 mg). The drug causes postural hypotension, weakness, drowsiness, dizziness, headache.

    Doxazosin is a long-acting α-adrenergic blocker. The drug has a beneficial effect on the lipid profile of the blood, does not cause the "first dose" effect. Doxazosin is almost completely absorbed in the gastrointestinal tract. Food slows down the absorption of the drug by about 1 hour. The bioavailability of doxazosia is 65-70%. The maximum concentration in the blood is determined 2-3.5 hours after taking the drug. The half-life is 16-22 hours. Duration of action - 18-36 hours. Doxazosin is prescribed once a day.

    Phentolamine is a non-selective α-blocker. It is mainly used in the treatment of hypertensive crises associated with hypercatecholemia, for example, in patients with pheochromocytoma. In addition, phentolamine is used for diagnostic purposes if pheochromocytoma is suspected.

    BLOCKERSα- and β-ADRENORECEPTORS.

    Labetalol (Trandat) is a β-adrenergic blocker that simultaneously exerts an α 1 -adrenoceptor blocking effect. Labetalol, as an α-adrenoblockato, is 2-7 times less active than phentolamine, and as a β-adrenergic agent, it is 5-18 times less active than anaprilin. the drug has a hypotensive effect, mainly by reducing peripheral vascular resistance. Labetalol has little effect on the value of cardiac output and heart rate. The main indication for the use of the drug is hypertensive crisis.

    Diuretics

    Diuretics have been used for hypertension for a long time, but in the beginning they were used as auxiliary drugs. Now many drugs can be used for long-term monotherapy of hypertension.

    Considering the negative significance of increasing the concentration of sodium ions in the plasma and vascular wall in the pathogenesis of hypertension, the main role in treatment belongs to saluretic drugs - drugs whose mechanism is associated with inhibition of sodium and chlorine reabsorption. These include benzothiadiazine derivatives and heterocyclic compounds. The last few hours have been called thiazide-like diuretics.

    In emergency situations, for example in a hypertensive crisis, stronger drugs are used - "loop" diuretics: furosemide and ethacrynic acid. Potassium-sparing diuretics play a supportive role and are usually prescribed with thiazide and loop diuretics to reduce potassium loss.

    The initial reduction in blood pressure with the use of saluretic diuretics is associated with increased sodium excretion, decreased plasma volume, and decreased cardiac output. After two months, the diuretic effect decreases, cardiac output normalizes. This is due to a compensatory increase in the concentration of renin and aldosterone, which inhibit fluid loss. The hypotensive effect of diuretics at this stage is explained by a decrease in peripheral vascular resistance, most likely due to a decrease in the concentration of sodium ions in the cells of vascular smooth muscles. Diuretics reduce both systolic and diastolic pressure, slightly affecting cardiac output.

    Hydrochlorothiazide (hypothiazide, esidrex) - a medium in strength and duration urinary agent, a typical representative of thiazide diuretics. The drug primarily increases the excretion of sodium, chlorine and, secondarily, water, mainly in the initial part of the distal tubules of the nephron. Hydrochlorothiazide is well absorbed in the gastrointestinal tract. The latent period of the drug is 1-2 hours, the maximum effect develops after 4 hours, the duration of action is 6-12 hours. 95% of hydrochlorothiazide is excreted unchanged in the urine.

    The drug is prescribed during or after meals at 25-100 mg / day in 1-2 doses in the first half of the day. With prolonged use of the drug, hypokalemia, hyponatremia, hypomagnesemia, hypochloremic alkalosis, hyperuricemia may develop. Hydrochlorothiazide can cause weakness, leukocytopenia, and skin rashes.

    Indapamide (arifon) has not only a diuretic effect, but also a direct vasodilator on the systemic and renal arteries. The decrease in blood pressure with the use of the drug is explained not only by a decrease in sodium concentration, but also by a decrease in the total peripheral resistance due to a decrease in the sensitivity of the vascular wall to norepinephrine and angiotensin II, an increase in the synthesis of prostaglandins (E 2), a weak anticalcium effect of the drug. With prolonged use in patients with moderate hypertension and impaired renal function, indapamide increases the glomerular filtration rate. The drug is well absorbed in the gastrointestinal tract, the maximum concentration in the blood is determined after 2 hours. In the blood, the drug binds to proteins by 75%, and can reversibly bind to erythrocytes. The half-life of indapamide is about 14 hours. 70% of it is excreted through the kidneys, the rest through the intestines. Indapamide at a dose of 2.5 mg once a day has a prolonged hypotensive effect. Side effects when using indapamide are observed in 5-10% of patients. Possible nausea, diarrhea, skin rash, weakness.

    Furosemide (lasix) - strong, short-acting diuretic. Furosemide interferes with the reabsorption of sodium and chlorine ions in the ascending part of the Henle loop. The latent period of furosemide with enteral administration is 30 minutes, with intravenous administration - 5 minutes. The action of the drug with the opening inside lasts 4 hours, with intravenous administration for 1-2 hours. Intravenous administration of the drug at a dose of up to 240 mg / day is used to relieve a hypertonic crisis. Side effects: hypokalemia, hyponatremia, hypochloremic alkalosis, dizziness, muscle weakness, convulsions.

    Ethacrynic acid in pharmacodynamic and pharmacokinetic parameters is close to furosemide.

    Spironolactone is a potassium-sparing steroid diuretic. The drug is an aldosterone antagonist, acts at the level of the distal convoluted tubules and collecting ducts. It has a weak and inconsistent hypotensive effect, which manifests itself 2-3 weeks after the appointment of the drug. The indication for the use of the drug is hypertonia in adrenal aldosteroma. Side effects: nausea, vomiting, dizziness, gynecomastia, in women - menstrual irregularities.

    ANGIOTENSIN-CONVERSING FACTOR INHIBITORS (ACE inhibitors).

    The renin-angiotensin system is of particular importance in the development and progression of arterial hypertension and heart failure. The function of the renin-angiotensin-aldosterone system (RAAS) is to regulate the balance of fluid and electrolytes, arterial pressure and blood volume. The main components of the RAAS are angiotensinogen, angiotensin I, angiotensin II. Renin, an angiotensin-converting enzyme, and angiotensinase, an enzyme that destroys angiotensin II, are involved in the activation and inactivation of these components.

    In the secretion of renin, the main role is played by the cells of the juxtaglomerular (JH) apparatus in the wall of the afferent arterioles of the renal glomeruli. Renin secretion occurs in response to a fall in blood pressure in the renal vessels below 85 mm or to an increase in β 1 -sympathetic activity. Renin secretion is inhibited by angiotensin II, vasopressin. Renin converts α-globulin - angiotesinogen (synthesized in the liver) into angiotensin I. Another enzyme - angiotensin-converting enzyme (ACE) converts angiotensin I into angiotensin II. The effects of angiotensin II on target cells are mediated through angioeisin receptors (AT). The information is intracellularly transmitted by regulatory G-proteins. They realize the inhibition of adenylate cyclase or the activation of phospholipase C or open the calcium channels of the cell membrane. These processes are responsible for the various cellular effects of target organs. First of all, this concerns changes in the tone of smooth muscle cells of the vascular walls. The activation of the RAAS leads to vasoconstriction as a result of the direct action of AP on vascular smooth muscle cells and, secondarily, as a result of aldosterone-dependent sodium retention. The resulting increase in blood volume increases preload and cardiac output.

    The study of the RAAS led to the creation of ACE inhibitors, which have a therapeutic effect in a variety of pathologies, primarily in hypertension and heart failure.

    The mechanism of the antihypertensive action of ACE inhibitors:

    1. Drugs, by inhibiting ACE activity, reduce the formation or release of such vasoconstrictor and sodium retention substances as angiotensin II, aldosterone, norepinephrine, vasopressin.

    2. The drugs increase the content in tissues and blood of such vasorelaxants as bradykinin, prostaglandins E 2 and I 1, endothelial relaxation factor, atrial natriuretic hormone.

    3. Decreased sodium retention as a result of decreased aldosterone secretion and increased renal blood flow.

    ACE inhibitors are relatively uncommon for side effects. In addition to allergic reactions, the most famous is the appearance of a dry cough. There is an assumption that the reason for this may be the excessive release of bradykinin in the bronchial mucosa. Cough is noted in 8% of patients taking long-term ACE inhibitors.

    From the group of angiotensin-converting enzyme inhibitors, captopril, enalapril maleate, lisinopril, which is a metabolite of enaprilin, and ramipril are used in clinical practice.

    There are short-acting (captopril) and long-acting (more than 24 hours) drugs (enalapril, lnzinopril, ramipril).

    Captopril (kapoten) lowers blood pressure at any initial renin level, but to a greater extent at elevated levels. Captopril increases serum potassium levels. Captopril is rapidly absorbed from the gastrointestinal tract. Food intake reduces its bioavailability by 35-40%. Only 25-30% of the drug binds to plasma proteins. Its maximum concentration in the blood is reached within 1 hour. The half-life of free captopril is 1 hour, and in combination with the metabolite it is 4 hours. The drug is administered orally, starting at a dose of 25 mg 2-3 times a day. The most common side effects are cough, skin rashes, and impaired taste. After stopping treatment, these symptoms disappear.

    Enaladryl maleate (renitec), when taken orally, is hydrolyzed and converted into the active form - enalaprilat. Its bioavailability is about 40%. After oral administration in healthy and patients with arterial hypertension, the drug is found in the blood after 1 hour and its concentration reaches a maximum after 6 hours. T1 / 2 is 4 hours. In the blood, enalapril maleate binds to proteins by 50%, is excreted in the urine. The drug is prescribed for arterial hypertension and heart failure at a dose of 5-10 mg 2 times a day. Side effects are very rare.

    1-ANGIOTENSIN RECEPTOR BLOCKERS (AT1)

    For the treatment of hypertension, 1-angiotensin receptor blockers (AT1) are used. The main cardiovascular and neuroendocrine effects of AT1 receptor blockers:

    Systemic arterial vasodilation (decrease in blood pressure, decrease in total peripheral vascular resistance and post-load on the left ventricle);

    Coronary vasodilation (increase in coronary blood flow), improvement of regional blood circulation in the kidneys, brain, skeletal muscles and other organs;

    Reverse development of left ventricular hypertrophy (cardioprotection);

    Increase in natriuresis and diuresis, potassium retention in the body (potassium-sparing effect);

    Decreased secretion of aldosterone,

    Decreased functional activity of the symlatic-adrenal system.

    By the mechanism of action, blockers of AT1 receptors are in many ways similar to ACE inhibitors. Therefore, the pharmacological effects of AT1-blockers and ACE inhibitors are generally similar, but the former, being more selective RAAS inhibitors, are less likely to produce side effects.

    Losartan is the first non-peptide AT1 receptor blocker. After oral administration, losartan is absorbed in the gastrointestinal tract, the concentration of the drug in the blood plasma reaches a maximum within 30-60 minutes. The antihypertensive effect of the drug persists for 24 hours, which is explained by the presence of an active metabolite in it, which blocks AT1 receptors 10-40 times more strongly than losartan. In addition, the metabolite has a longer half-life in blood plasma - from 4 to 9 hours. The recommended dose of losartan for the treatment of arterial hypertension is 50-100 mg / day in one dose. Contraindications to the appointment of AT1-receptor blockers are: individual drug intolerance, pregnancy, breastfeeding.

    Slow calcium channel blockers

    The hypotensive effect of calcium antagonists is associated with a decrease in the content of free calcium in the cytoplasm of cells due to impaired entry of calcium into the cell through voltage-gated slow calcium channels. This leads to relaxation of vascular smooth muscle cells (decrease in total peripheral resistance) and a decrease in the contractile activity of cardiomyocytes. Long-acting drugs are used in the treatment of hypertension. they do not cause reflex stimulation of the sympathetic nervous system. These drugs include amlodipine, mibefradil and retard forms of verapamil, diltiazem, nifedipine.

    Calcium channel blockers are relatively well tolerated by patients. The minimum number of side effects in amlodipine, diltiazem and mibefradil. The side effect of drugs is determined by the chemical structure. So, when using verapamil, constipation is often noted, it is possible to develop a sharp bradycardia, conduction disorders, heart failure. Taking dihydropyridines is often accompanied by redness of the skin, a feeling of heat, and edema, usually localized on the feet and legs.

    Medicines of the central mechanism of action.

    Centrally acting drugs reduce the activity of the vasomotor center of the medulla oblongata.

    Clonidine, an imidazoline derivative, is a central mimetic of α 2 -adreno- and I 1 -imidazoline receptors. The drug stimulates the receptors of the nuclei of the solitary tract of the pro-long brain, which leads to inhibition of the neurons of the vasomotor center and a decrease in sympathetic innervation. The hypotensive effect of the drug is a consequence of a decrease in cardiac activity and total peripheral vascular resistance. Clonidine is well absorbed from the gastrointestinal tract. When administered orally, the latent period of the drug is 30-60 minutes, with intravenous administration - 3-6 minutes. The duration of action varies from 2 to 24 hours. Clonidine is excreted from the body by the kidneys mainly in the form of metabolites. With a sudden withdrawal of the drug, a "recoil" syndrome occurs - a sharp increase in blood pressure. Clonidine has a sedative and hypnogenic effect, potentiates the central effects of alcohol, sedatives, depressants. Clofeliv reduces appetite, the secretion of the salivary glands, retains sodium and water.

    Moxonidine (Zinc) - a selective agonist of I 1 -imidazoline receptors. Activation of imidazoline receptors in the central nervous system leads to a decrease in the activity of the vasomotor center and a decrease in peripheral vascular resistance. In addition, the drug inhibits the renin-angiotensin-aldosterone system. The drug is well absorbed from the gastrointestinal tract and has a high bioavailability (88%). The maximum concentration in the blood is recorded after 0.5 -3 hours. 90% of the drug is excreted by the kidneys, mainly (70%) unchanged. Despite the short half-life (about 3 hours), moxodonin controls blood pressure throughout the day. The drug is prescribed at 0.2-0.4 mg once a day in the morning. Moxonidine can cause fatigue, headaches, dizziness, and sleep disturbances.

    Vasodilators.

    Vasodilators for the treatment of arterial hypertension are represented by drugs of two groups; arteriolar (hydrolazine, dysacoid and minokoid) and mixed (sodium nitroprusside and isosorbide dinitrate). Arteriolar vasodilators dilate resistive vessels (arterioles in small arteries) and decrease total peripheral resistance. In this case, there is a reflex increase in cardiac activity and an increase in cardiac output. The activity of the sympathoadrenadic system increases, and behind it the secretion of renin. The drugs cause sodium and water retention. Mixed-action drugs also cause expansion of capacitive vessels (venules, small veins) with a decrease in venous return of blood to the heart.

    Hydralazine (apressin) - due to the large number of side effects (tachycardia, pain in the heart area, facial redness, headache, lupus erythematosus syndrome), it is rarely used and only in the form of ready-made combinations (adelfan). Hydralazine is contraindicated in case of stomach ulcers, autoimmune processes.

    Diazoxide (hyperstat) - arteriolar vasodilator - activator of potassium channels. The effect on potassium channels leads to hyperpolarization of the membrane of muscle cells, which reduces the intake of calcium ions into the cells, which are necessary to maintain vascular tone. The drug is used intravenously for hypertensive crisis. Duration of action is about 3 hours.

    Minoxidil - arteriolar vasodilator - activator of potassium channels. The drug is well absorbed in the gastrointestinal tract. The half-life is 4 hours. Mnnoxidil is administered orally 2 times a day.

    Sodium nitroprusside (niprid) - mixed vasodilator. The hypotensive effect of the drug is associated with the release of nitric oxide from the drug molecule, which acts similarly to the endogenous endothelium-relaxing factor. Thus, its mechanism of action is similar to nitroglycerin. Sodium nitroprusside is prescribed intravenously for hypertensive crises, acute left ventricular failure. Side effects: headache, anxiety, tachycardia.

    Sympatholytics

    (see the lecture "Adrenolytics") Sympatholytics include reserpine, octadine.

    Reserpine is a rauwolfia alkaloid. The drug disrupts the deposition of norepinephrine in vesicles, which leads to its destruction by cytoplasmic monoamine oxidase and a decrease in its concentration in varicose thickenings. Reserpine reduces the content of noradrenaline in the heart, blood vessels, central nervous system and other organs. The hypotensive effect of reserpine when administered orally develops gradually over several days, after intravenous administration of the drug - within 2-4 hours. Side effects of reserpine: drowsiness, depression, stomach pain, diarrhea, bradycardia, bronchosyasm. The drug causes sodium and water retention in the body.

    Ectadine interferes with the release of norepinephrine and prevents the reuptake of the transmitter by sympathetic endings. The decrease in blood pressure is due to a decrease in cardiac output and a decrease in the total peripheral vascular resistance. The bioavailability of the drug is 50%. The half-life is about 5 days. The drug causes postural hypotension, sodium and water retention in the body, dizziness, weakness, swelling of the nasal mucosa, diarrhea. It is rarely used.


    Hypertension is one of those chronic conditions that you have to fight all your life. Therefore, drugs for hypertension are constantly being improved, new drugs appear - more effective and having less pronounced side effects. It should be noted that in order to achieve the maximum effect, such funds are always included in the complex treatment for high blood pressure.

    Drugs for hypertension - indications for use

    The purpose of prescribing all antihypertensive drugs is to reduce and stabilize blood pressure. The mechanism of action may be different, but it always has the effect of expansion of peripheral vessels. It is due to it that the redistribution of blood occurs - more goes into small vessels, accordingly, tissues receive more nutrition, the load on the heart decreases and blood pressure decreases.

    Depending on the mechanism of action, this effect can be achieved quickly as a result of the use of ACE inhibitors (Captopril, Kapoten), or develop gradually with the appointment of beta-blockers (Concor, Coronal). Medicines, the effect of which is achieved within half an hour, are used to treat hypertensive crisis, myocardial infarction, and cerebral circulation disorders. Gradual remedies are prescribed for daily use.

    A large number of antihypertensive drugs are due to various mechanisms of the onset of the disease, as well as the fact that the selection of drugs for the treatment of hypertension is always carried out individually, based on the characteristics of the course of the disease and concomitant diseases in the patient. The main indications for the appointment of antihypertensive therapy are:

    • Essential arterial hypertension;
    • Heart disease - heart failure, arrhythmia, post-infarction condition;
    • Kidney disease, accompanied by increased blood pressure;
    • Diseases of the nervous system that cause high blood pressure.

    In case of endocrine diseases, the symptom of which may be arterial hypertension, drugs to reduce pressure are prescribed only after consultation with an endocrinologist, since without hormone therapy, their effectiveness is extremely low.

    Diseases such as stenosis of the aorta or renal arteries are also most often contraindications for the appointment of antihypertensive drugs, since their effectiveness in this case is low, and the likelihood of side effects is much higher. Drugs that reduce blood pressure are almost never prescribed to pregnant women, nursing mothers, children and adolescents. The use of antihypertensive drugs from different groups has its own characteristics, indications and contraindications. Therefore, they can only be prescribed by specialists, taking into account the individual characteristics of the patient.

    The main groups of drugs for hypertension

    Drugs for hypertension group of adrenergic blockers

    Adrenoblockers are one of the most commonly used groups of drugs for hypertension, arrhythmias and heart failure. The action of medications is aimed at preventing the synthesis of excitatory neurotransmitters (adrenaline and norepinephrine). These substances cause vasoconstriction, increased blood pressure, increased heart rate and increased heart rate. Adrenergic blockers "turn off" some of the receptors for adrenaline, which is why its effect on the cardiovascular system decreases.

    According to the level of exposure, drugs of this pharmacological group are divided into selective and non-selective. Non-selective (Propranolol, Anaprilin) \u200b\u200baffect all types of adrenergic receptors, causing a strong hypertensive effect and many side reactions in the form of bronchospasm, circulatory disorders in the lower extremities, impotence.

    Selective adrenergic blockers act only on a certain type of receptor. Β-blockers (BAB) are used most often in heart disease associated with hypertension. They block receptors located in the peripheral vessels, which are responsible for their constriction. Due to this, a hypotensive effect is achieved. These include drugs for hypertension such as Carvedilol, Bisoprolol, Metoprolol and others. Indications for the appointment of BAB:

    • hypertonic disease;
    • heart failure;
    • postinfarction condition;
    • arrhythmias with a tendency to tachycardia.

    These drugs can be used in patients with diabetes mellitus after consultation with an endocrinologist. New generation drugs for hypertension in this group, such as Bisoprolol, can be administered to patients with bronchial asthma and COPD with little risk due to their high selectivity. In case of kidney disease, hyperaldosteronism and other diseases not directly related to the heart and blood vessels, they are used as an additional prophylactic agent.

    Alpha-blockers are used much less frequently. They have a strong antihypertensive effect, improve glucose and fat metabolism, and reduce the severity of prostate adenoma symptoms. They are used as a means to control blood pressure in patients with type 2 diabetes mellitus, especially in older men, in the absence of contraindications.

    Funds affecting the RAAS

    The renin-angiotensin-aldosterone system is the second system in the body responsible for maintaining renal blood flow and increasing blood pressure. This is a complex chain of biologically active substances released in sequence. By interrupting this chain, you can weaken its effect on blood pressure. Among the drugs that affect the RAAS, two classes of drugs are used - ACE inhibitors and angiotensin-II receptor blockers.

    ACE inhibitors are quick and slow acting. Rapid-acting hypertension drugs, such as Captopril, are needed to help with hypertensive crisis or myocardial infarction, as well as for the rehabilitation of patients after a heart attack. If necessary, they can be prescribed as a means of daily intake to control blood pressure.

    Enalapril, Lisinopril and other drugs for hypertension for daily use act rather slowly, gradually normalizing blood pressure. Their dosage is selected individually, based on the patient's well-being and the effectiveness of the drug.

    Indications for the use of ACE inhibitors are the following conditions:

    • essential arterial hypertension;
    • heart failure;
    • rehabilitation after myocardial infarction;
    • kidney disease, including diabetic nephropathy.

    Unlike BAB, ACE inhibitors can be prescribed for kidney disease, in which case they do not lose their effectiveness. Contraindications for their use are stenosis of the aorta or renal arteries, endocrine diseases. With heart defects, they are prescribed with caution.

    Angiotensin receptor blockers belong to vasodilator drugs for hypertension. They also affect the RAAS, but at a different stage. Their use allows for long-term exposure, and as a result, more stable pressure control.

    These include funds such as Losartan, Valsartan and others. They have a wider range of applications for kidney diseases and endocrine pathologies. Due to their high specificity, they have few side effects. Drugs of both groups are ineffective for arrhythmias, diseases of the nervous system, causing an increase in blood pressure.

    Calcium channel blockers

    These drugs for hypertension, also called calcium antagonists, block the flow of calcium into muscle tissue. First of all, they affect the tissue of the vessel wall, reducing its ability to contract. Thus, an antihypertensive effect is achieved.

    Side effects include muscle weakness, decreased mental performance, changes in laboratory urine parameters and heart rhythm disturbances. In this group, new-generation drugs for hypertension, such as Amlodipine, have clear indications for use. They should be used under the supervision of a physician, as there is a possibility of developing dangerous complications. Calcium channel blockers are used for the following pathologies:

    • ischemic heart disease;
    • myocardial infarction and post-infarction condition;
    • hypertensive crisis;
    • some heart rhythm disorders.

    Most of the drugs in this group are intended for emergency use. For constant daily use, other drugs are used, with a milder effect and with fewer side effects.

    Diuretics

    Diuretics are also included in the list of drugs for hypertension. They stimulate the excretion of urine, due to which the volume of circulating blood decreases, as a result, blood pressure decreases. The mechanism of action of different groups of diuretics has its own characteristics, as a result of which their side effects also differ.

    Most of the adverse reactions are associated with the loss of electrolytes and dehydration of the body, since it is the concentration of sodium in the urine that regulates its amount. These side effects can be dealt with by taking medications that maintain electrolyte levels in the blood. In case of hypertension, thiazide diuretics and sulfonamides are used (Hypothiazide, Indapamide, Cyclomethiazide). The indications for the use of diuretics in high blood pressure are as follows:

    1. essential hypertension;
    2. heart failure;
    3. kidney disease, including diabetic nephropathy;

    Diuretic drugs should be prescribed with caution for cardiac arrhythmias. Side effects - thirst, muscle weakness, pain, cramps, headaches, heart rhythm disturbances. In severe cases, fainting is possible. Contraindications to use are arrhythmias, endocrine diseases, pregnancy and the period of breastfeeding.

    Centrally acting hypertension drugs

    For arterial hypertension caused by dysregulation of blood pressure by the centers of the brain, drugs for hypertension of central action are used. These are the most radical means for lowering blood pressure, which are used strictly according to indications.

    The most modern drug today is, which is prescribed for diseases of the central nervous system, with a combination of arterial hypertension and diabetes mellitus. The advantage of this drug is that it does not affect the insulin receptors.

    Central antihypertensive drugs can be used in combination with other drugs to lower blood pressure. They have pronounced side reactions - orthostatic hypotension, emotional disturbances, headaches. Contraindicated in mental illness, as well as pregnant and lactating women, as they can cause serious violations of blood pressure regulation in the baby.

    Review of the best drugs for pressure - a list

    Captopril (analogues Kapoten, Alkadil)

    A drug from the group of ACE inhibitors, it blocks the production of an enzyme responsible for vasoconstriction, prevents hypertrophy and thickening of the heart muscle, reduces blood flow to the heart and helps relieve stress. Captopril tablets are intended for the relief of acute conditions (hypertensive crises).

    For long-term use (especially in the elderly with atherosclerosis) are not suitable. During the course of treatment, take 1 tablet twice a day, 1 hour before meals, starting with the minimum doses. The drug has quite a few contraindications (a history of Quincke's edema, pregnancy, lactation, kidney pathology, coronary artery disease, autoimmune diseases) and side effects, therefore, the medicine should be taken strictly according to indications. The average cost of the drug is 20-40 rubles.

    Enalapril (analogues of Enap, Enam, Renipril)

    ACE inhibitor of the carboxyl group, acts more mildly than Captopril and its analogues. Prescribed for daily use in order to control blood pressure. When used correctly, Enalapril significantly increases the life expectancy of patients with hypertension, but can cause such an unpleasant side effect as a dry cough.

    The drug is usually prescribed in a minimum dose (5 mg), taken once (in the morning), then the dose is gradually increased every 2 weeks. Like most medicines in this group, Enalapril has many contraindications, with extreme caution the drug is prescribed for renal and hepatic failure, diabetes mellitus, in old age. If side effects occur, the dose is reduced or the drug is canceled. The price of Enalapril in pharmacies is from 40 to 80 rubles.

    Bisoprolol

    The drug is from the group of selective beta-blockers, effectively reducing the risk of cardiovascular complications at high blood pressure. Suitable for the treatment of resistant forms of hypertension, it is prescribed for angina pectoris, chronic heart failure, patients who have had a heart attack.

    The principle of action of the drug is based on the prevention of the production of hormones (renin and angiotensin 2), which affect vasoconstriction, as well as the blockade of beta receptors of blood vessels. can be used for long-term treatment, it is prescribed once, in a dose of 5-10 mg, taken in the morning. The medication should be canceled gradually, otherwise a sharp jump in pressure is possible. The price of the medicine varies from 50 to 200 rubles.

    Popular sartan (angiotensin receptor blocker). It is a relatively new drug with fewer side effects and a milder and more prolonged action. Effectively reduces blood pressure, the pill must be taken once (in the morning or before bedtime).

    Treatment begins with a therapeutic dose of 50 mg, a persistent hypotensive effect develops on average after a month of regular medication. Lozaratan has few contraindications (pregnancy, lactation, hyperkalemia), but it can cause a number of unwanted side effects. Therefore, you should strictly follow medical recommendations and do not exceed the indicated dosages. The price of the drug is 300-500 rubles.

    Representative of the group of calcium channel blockers. The use of the drug improves exercise tolerance, which is especially important in the treatment of elderly patients with cardiac arrhythmias, angina pectoris or atherosclerosis. When combining the drug with ACE inhibitors, you can refuse to prescribe diuretics.

    The drug is taken once in a dose of 5 mg, then, taking into account the tolerance, the dosage is increased to 10 mg per day. Side effects when taken are rare, contraindications for use are hypersensitivity, liver failure, pregnancy, lactation. The price of the medication is 80-160 rubles.

    Indapamide

    A diuretic from the sulfonamide group, prescribed for severe forms of arterial hypertension, as part of complex therapy. Indapamide can be used for concomitant diabetes mellitus, since it does not affect blood sugar levels. A diuretic reduces the risk of complications in the heart and blood vessels; it is taken daily, at a dose of 2.5 mg, regardless of food.

    After a single dose, the therapeutic effect lasts throughout the day. Indopamine should not be prescribed for severe renal or hepatic impairment, during pregnancy and breastfeeding. The drug can cause allergic reactions and side effects from various body systems (nervous, digestive). The cost of a diuretic is from 120 rubles.

    General principles of treatment

    The modern pharmaceutical industry has not been able to invent drugs for hypertension without side effects, so it is necessary to take into account possible adverse reactions when taking drugs for pressure. The reaction of each patient to a certain drug is individual, therefore it is necessary not only to select the drug itself, but also to accurately calculate the dose.

    Treatment with antihypertensive drugs is always started with the lowest dose, then increased if necessary. If, even at the minimum dose, an undesirable reaction occurs, the drug is canceled and replaced with another.

    In the treatment of arterial hypertension, the financial factor also plays an important role - the cost of these drugs is different, and they have to be taken for life. That is why in the question of which drugs to take for hypertension, the doctor is forced to focus more on the cost of the medication and the patient's financial capabilities.

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