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Modern means for lowering blood pressure

 
 
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Update article 01/30/2019

Arterial hypertension (AH) remains one of the most significant medical and social problems. This is due to the wide spread of this disease (about 40% of the adult population has an elevated level of blood pressure), as well as the fact that hypertension is the most important risk factor for major cardiovascular diseases - myocardial infarction and stroke.

Permanent Resistant increase in blood pressure (BP) to 140/90 mm. Hg Art. and above - a sign of arterial hypertension (hypertension).

The risk factors that contribute to the manifestation of hypertension include:

    Age (men over 55, women over 65)
    Smoking
    sedentary lifestyle,
    Obesity (waist size over 94 cm for men and over 80 cm for women)
    Family cases of early cardiovascular disease (in men younger than 55 years old, in women younger than 65 years old)
    The magnitude of pulse blood pressure in the elderly (the difference between systolic (upper) and diastolic (lower) blood pressure). Normally, it is 30-50 mm Hg.
    Plasma glucose on an empty stomach 5.6-6.9 mmol / l
    Dyslipidemia: total cholesterol is more than 5.0 mmol / l, cholesterol low-density lipoproteins 3.0 mmol / l and more, high-density lipoprotein cholesterol 1.0 mmol / l and less for men, and 1.2 mmol / l and 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 contribute to 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 eating 11.0 mmol / l and more)
    Other endocrinological diseases (pheochromocytoma, primary aldosteronism)
    Kidney and renal artery disease
    Medications and substances (glucocorticosteroids, nonsteroidal anti-inflammatory drugs, hormonal contraceptives, erythropoietin, cocaine, cyclosporine).

Knowing the causes of the disease, you can prevent the development of complications. Elderly people are at risk.

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

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

Indices of blood pressure obtained at home can be a valuable addition to monitoring the effectiveness of treatment and are important in detecting hypertension. Task Patient - keep a diary of self-monitoring of blood pressure, where blood pressure and pulse rates are recorded at least in the morning, at lunch, in the evening. maybe commenting on lifestyle (lifting, eating, physical activity, stressful situations).

The technique of measuring blood pressure:

    Rapidly pump air into the cuff up to the level of pressure, at 20 mm Hg, exceeding the systolic blood pressure (MAP), at the disappearance of the pulse
    Blood pressure is measured to an accuracy of 2 mm Hg.
    Reduce cuff pressure at a speed of approximately 2 mm Hg in 1 second
    The pressure level at which the 1st tone appears corresponds to the GARDEN
    The level of pressure at which the disappearance of the tones corresponds to the diastolic blood pressure (DBP)
    If the tones are very weak, you should raise your hand and perform several squeezing movements with a brush, then repeat the measurement, and you should not squeeze too much phonendoscope membrane artery
    In the primary measurement fix blood pressure on both hands. 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 be measured after 2 minutes of standing.

Patients with hypertension experience pain in the head (often in the temporal, occipital region), episodes of dizziness, rapid fatigue, poor sleep, pain may occur in heart, blurred vision.
Complicated disease hypertensive crises (when blood pressure rises sharply to high numbers, there is frequent urination, headache, dizziness, heartbeat, heat sensation); renal dysfunction - 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 general practitioner or cardiologist who will prescribe the necessary examinations, and subsequently determine further treatment tactics. Only after carrying out the necessary set of examinations is it possible to talk about the appointmentdrug therapy.

Self-prescribing drugs can threaten the development of undesirable side effects, complications and can be fatal! Is forbidden self-use of drugs on the principle of "helped friends" or resort to the recommendations of pharmacists in pharmacy chains !!! Application antihypertensive drugs possible only on prescription!

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

1. Lifestyle change activities:

    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
    The increase in physical activity - regular aerobic (dynamic) load for 30-40 minutes at least 4 times a week
    Reducing the consumption of salt to 3-5 g / day
    Changes 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 reducing animal fat intake.

These activities are prescribed to all patients with hypertension, including those receiving antihypertensive drugs. They allow: reduce arterial pressure, reduce the need for antihypertensive drugs, a positive effect on existing risk factors.

***

2. Drug therapy

Today we will talk about these drugs - modern drugs for the treatment of hypertension.
Arterial hypertension is a chronic disease that requires not only constant control of blood pressure, but also constant medication.

There is no course of antihypertensive therapy, all drugs are taken indefinitely. With the ineffectiveness of monotherapy, the selection of drugs from different groups, often combining several drugs.
As a rule, the desire of a patient with hypertension - to buy the most powerful, but not expensive drug. However, it is necessary to understand that this does not exist.
What drugs for this offer 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 - the prorenin substance is produced in the kidneys (with a decrease in pressure), which is converted into renin in the blood. Renin (proteolytic enzyme) interacts with angiotensinogen plasma protein, resulting in an inactive substance angiotensin I. Angiotensin when interacting with Angiotezin-converting enzyme (ACE) turns into the active substance Angiotensin II. This substance contributes to high blood pressure, narrowing of blood vessels, an increase in the frequency and strength of heart contractions, the excitation of the sympathetic nervous system (which also leads to an increase in blood pressure), increased aldosterone production.

Aldosterone contributes to the retention of sodium and water, which also increases blood pressure. Angiotensin II is one of the most powerful vasoconstrictor substances in the body.

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

c) Adrenoreceptors - in our bodies in some organs there are receptors, irritation of which affects blood pressure. These receptors include alpha-adrenoreceptors (α1 and α2) and beta-adrenergic receptors (β1 and β2). Stimulation of α1 -adrenoreceptors leads to an increase in blood pressure, α2-adrenoreceptors - to a decrease in blood pressure. α-adrenoreceptors are located in arterioles. β1-adrenoreceptors are localized in the heart, in the kidneys, their stimulation leads to an increase in heart rate, increase myocardial oxygen demand and increase blood pressure. Stimulation of β2-adrenoreceptors located in the bronchioles causes expansion of the bronchioles and 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. In the brain are vasomotor centers that regulate the level of arterial
pressure.

So, we have considered the main mechanisms for increasing blood pressure in the human body. It's time to switch to pressure reduction.

(antihypertensives) that affect these very mechanisms.
Classification of agents for arterial hypertension

    Diuretics (diuretics)
    Calcium channel blockers
    Beta blockers
    Agents acting on the renin-angiotensin system
        Angiotensin-converting enzyme (ACE) inhibitors
        Angiotensive receptor blockers (antagonists) (sartans)
    Neurotropic centrally acting agents
    Drugs acting on the central nervous system (CNS)
    Alpha blockers

***

1. Diuretics (diuretics)

As a result of elimination of excess fluid from the body, blood pressure decreases. Diuretics prevent the reabsorption of ions sodium, which as a result are brought out and carry water. In addition to sodium ions, diuretics wash out potassium ions from the body, which are necessary for work of cardio-vascular system. There are diuretics, saving potassium.

Representatives:

    Hydrochlorothiazide (Hypothiazide) - 25mg, 100mg, is included in the combination preparations; Not recommended for prolonged use in dosages above 12.5 mg, in connection with the possible development of type 2 diabetes!
    Indapamide (Arifonrethard, Ravel SR, Indapamid MV, Indap, Ionik retard, Acripamidretard) - usually a dosage of 1.5 mg.
    Triampur (a combination diuretic containing potassium-sparing triamteren and hydrochlorothiazide);
    Spironolactone (Veroshpiron, Aldactone). It 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. Slows down the reabsorption of sodium ions in the ascending knee of the loop of Henle, proximal and distal tubules. Increases the excretion of bicarbonates, phosphates, calcium, magnesium.
    Torasemide (diuver) - 5 mg, 10 mg, is a loopback diuretic. The main mechanism of drug action is due to the reversible binding of torasemide to the counterporter
sodium / chlorine / potassium ions located in the apical membrane of the thick segment of the ascending part of the loop of Henle, resulting in reduced or completely inhibited reabsorption of sodium ions and decreases the osmotic pressure of intracellular fluid and the reabsorption of water. Blocks myocardial aldosterone receptors, reduces fibrosis and improves the diastolic function of the myocardium. Torasemide to a lesser extent than furosemide, causes hypokalemia, while it exhibits greater activity, and action is longer.

Diuretics prescribed in combination with other antihypertensive drugs. The drug indapamide is the only diuretic used in hypertension alone.
Rapid diuretic action (furosemide) is undesirable to be applied systematically in patients with hypertension, they are taken in emergency conditions.
When using diuretics, it is important to take potassium preparations for courses up to 1 month.

2. Calcium channel blockers

Calcium channel blockers (calcium antagonists) - a heterogeneous group of drugs that have the same mechanism of action, but differ in a number of properties,

including pharmacokinetics, tissue selectivity, the effect on heart rate.
Another name for this group is calcium ion antagonists.
There are three main AK subgroups: dihydropyridine (the main representative is nifedipine), phenylalkylamines (the main representative is verapamil) and benzothiazepines.

(the main representative is diltiazem).
Recently, they have been divided into two large groups depending on the effect on heart rate. Diltiazem and verapamil belong to the so-called “Slowing down the rhythm” of calcium antagonists (non-dihydropyridine). The other group (dihydropyridine) includes amlodipine, nifedipine and all other derivatives.

dihydropyridine, increasing or not changing the heart rate.
Calcium channel blockers are used for hypertension, coronary heart disease (contraindicated in acute forms!) And arrhythmias. With arrhythmias not all calcium channel blockers are used, but only pulsating ones.

Representatives:

Pulsation (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, Kordafleks, Kordafen, Cordipin, Corinfar, Nifecard, Fenigidin) - dosage 10 mg, 20 mg; NifecardXL 30mg, 60mg.
    Amlodipine (Norvask, Normodipin, Tenox, Cordi Cor, Es Cordi Cor, Cardilopin, Calchek,
    Amlotop, Omelarcardio, Amlovas) - dosage 5 mg, 10 mg;
    Felodipine (Plendil, Felodip) - 2.5 mg, 5 mg, 10 mg;
    Nimodipine (Nimotop) - 30 mg;
    Lacidipine (Lacipil, Sakur) - 2 mg, 4 mg;
    Lercanidipine (Lerkamen) - 20 mg.

Of the side effects of dihydropyridine derivatives, we can indicate edema, mainly lower extremities, headache, facial flushing, increased heart rate, increased urination. If the swelling persists, you need to replace the drug.
Lerkamen, which is the third generation of calcium antagonists, due to higher selectivity to slow calcium channels, causes swelling in less than other members of this group.

***

3. Beta-blockers

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

Representatives:

    Metoprolol (Betalok ZOK 25mg, 50mg, 100mg, Egilok retard 25mg, 50mg, 100mg, 200mg, Egilok C, Vazokardinardard 200 mg, Metocardardard 100 mg) ;;
    Bisoprolol (Concor, Coronal, Biol, Bisogamma, Kordinorm, Niperten, Biprol, Bidop, Aritel) - most often a dosage of 5 mg, 10 mg;
    Nebivolol (Nebilet, Binelol) - 5 mg, 10 mg;
    Betaxolol (Lokren) - 20 mg;
    Carvedilol (Carvendrend, Coriol, Talliton, Dilatrend, Akridiol) - mainly dosage 6.25 mg, 12.5 mg, 25 mg.

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

The main contraindications to beta-blockers:

    bronchial asthma;
    low pressure;
    sick sinus syndrome;
    peripheral artery disease;
    bradycardia;
    cardiogenic shock;
    atrioventricular block second or third degree.

4. Agents acting on the renin-angiotensin system

The drugs act on different stages of the formation of angiotensin II. Some inhibit (inhibit) the angiotensin-converting enzyme, others block the receptors to which

Angiotensin II is effective. The third group inhibits renin, is represented by only one drug (aliskiren).
Angiotensin-converting enzyme (ACE) inhibitors

These drugs prevent the transition of angiotensin I to active angiotensin II. As a result, the concentration of angiotensin II decreases in the blood, the vessels expand, the pressure going down.
Representatives (in parentheses are the synonyms - substances with the same chemical composition):

    Captopril (Capoten) - dosage 25mg, 50mg;
    Enalapril (Renitec, Berlipril, Renipril, Ednit, Enap, Enarenal, Enam) - the dosage is most often 5 mg, 10 mg, 20 mg;
    Lisinopril (Diroton, Dapril, Lysigamma, Lisinoton) - dosage most often 5 mg, 10 mg, 20 mg;
    Perindopril (Prestarium A, Perinev) - Perindopril - dosage 2.5 mg, 5 mg, 10 mg. Perineva - dosage 4 mg, 8 mg .;
    Ramipril (Tritatse, Amprilan, Hartil, Piramil) - dosage 2,5mg, 5mg, 10mg;
    Hinapril (Akkupro) - 5 mg, 10 mg, 20 mg, 40 mg;
    Fozinopril (Fozikard, Monopril) - at a dosage of 10 mg, 20 mg;
    Trandolapril (Gopten) - 2 mg;
    Zofenopril (Zokardis) - dosage of 7.5 mg, 30 mg.

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

A special feature of the drug Captopril (Kapoten) is that, because of its short duration of action, it is rational only in hypertensive crises.

A bright representative of the group Enalapril and its synonyms are used very often. This drug does not differ in the duration of action, so they take 2 times a day.

In general, the full effect of ACE inhibitors can be observed after 1-2 weeks of using the drugs. In pharmacies, you can find a variety of generics (analogues) of enalapril, those. cheaper, containing enalapril drugs that produce small manufacturers. We talked about the quality of generics in another article, here it’s worth It should be noted that enalapril generics are suitable for someone, they do not affect someone.

ACE inhibitors cause a side effect - dry cough. In cases of cough development, ACE inhibitors are replaced by 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, the 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; Valsakor 80mg, 160mg, 320mg, Walz 40mg, 80mg, 160mg; Norstavan 40mg, 80mg, 160mg; Valsfors 80mg, 160mg);
    Irbesartan (Aprovel) - 150 mg, 300 mg;
    Candesartan (Atakand) - 8mg, 16mg, 32mg;
    Telmisartan (Mikardis) - 40 mg, 80 mg;
    Olmesartan (Cardosal) - 10mg, 20mg, 40mg.

As well as the predecessors, allow us to evaluate the full effect in 1-2 weeks after the start of the reception. Do not cause dry cough. Do not use during pregnancy! If pregnancy is detected during treatment, antihypertensive therapy with drugs of this group should be stopped!

5. Neurotropic agents of central action

Neurotropic drugs of central action affect the vasomotor center in the brain, reducing its tone.

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

The first representative of this group is clonidine, widely used previously in hypertension. Now this drug is available strictly on prescription.
Currently, moxonidine is used for emergency treatment of hypertensive crisis, as well as for planned therapy. Dosage 0,2mg, 0,4mg. Maximum daily dosage of 0.6 mg / day.

6. Funds acting on the central nervous system

If hypertension is caused by prolonged stress, then use drugs that act on the central nervous system (sedatives (Novopassit, Persen, Valerian, Pustyrnik, tranquilizers, hypnotics).

7. Alpha blockers

These drugs are attached to alpha-adrenergic receptors and block them for the irritating action of norepinephrine. As a result, blood pressure decreases.
The representative used - Doxazosin (Kardura, Tonokardin) - is more commonly available in dosages of 1 mg, 2 mg. It is used for the relief of attacks and long-term therapy.

Many drugs alpha blockers are discontinued.
Why do you take several medications for hypertension?

In the initial stage of the disease, the doctor prescribes one drug, based on some studies and taking into account the existing diseases in the patient. If one drug
ineffective, other drugs are often added, creating a combination of drugs to lower blood pressure, affecting various mechanisms to reduce blood pressure. Combined therapy for refractory (sustained) arterial hypertension can combine up to 5-6 drugs!

Preparations 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 combinations of drugs that are irrational, for example: beta-blockers / calcium channel blockers, pulsating, beta-blockers / drugs central action and other combinations. It is dangerous to self-medicate !!!

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

**

For example:

    ACE inhibitor / diuretic
        Enalapril / Hydrochlorothiazide (Co-Renitec, Enap NL, Enap N,
        Enap NL 20, Renipril GT)
        Enalapril / Indapamide (Enzix duo, Enzix duo forte)
        Lisinopril / Hydrochlorothiazide (Iruzid, Lisinoton, Liten N)
        Perindopril / Indapamide (NoliprelAi NoliprelAforte)
        Hinapril / Hydrochlorothiazide (Accuzid)
        Fozinopril / hydrochlorothiazide (Fozikard N)
    angiotensin receptor blocker / diuretic
        Losartan / Hydrochlorothiazide (Gizaar, Lozap plus, Lorista N,
        Lorista ND)
        Eprosartan / Hydrochlorothiazide (Teveten plus)
        Valsartan / Hydrochlorothiazide (C-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)
    calcium channel blocker dihydropyridine / beta blocker
        Felodipine / Metoprolol (Logimaks)
    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 follow-up with regular monitoring of patient's lifestyle change recommendations.

and adherence to prescribed antihypertensive drugs, as well as the correction of therapy depending on the effectiveness, safety and tolerability of treatment. With
dynamic observation is crucial to establish personal contact between the doctor and the patient, patient education in schools for patients with hypertension, increasing adherence of the patient to treatment.

Be healthy!

Update article 01/30/2019

Cardiologist Zvezdochetova Natalia Anatolyevna

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