Losartan is a time-tested medicine for hypertension (high blood pressure). According to clinical studies, it was concluded that the risk of developing heart disease when taken, reducing the incidence of strokes and heart attacks. Also, the drug slows down the progress of kidney failure, helps in the restoration of kidney function after transplant. Let's take a closer look at the drug "Losartan", instructions for use, indications for admission and possible side effects.

The active ingredient of the drug is potassium losartan. The composition contains the following excipients:

The drug is available in the form of round film-coated tablets. They are convex on both sides, there is a roughness on the surface. This is their only form of release. The dosage is 12.5; 25; 50; 100 mg.

The color of the tablet depends on the dosage:

• 12.5 mg - white-grayish color;
• 25 mg - white-grayish color;
• 50 mg - pink;
• 100 mg - yellow.

Thanks to this difference, the dosage can be differentiated even without packaging. There are three types of packaging:

1. Blisters that fit in a cardboard box. Each blister contains 10 or 15 pieces. The number of blisters is 2-6.
2. Contoured cell packaging in the amount of 10-30 pieces. The box contains 1-6 packs of pills;
3. Banks of 10-100 tablets.

pharmachologic effect

Losartan is a specific angiotensin II receptor antagonist. Designed for indoor use. Angiotensin binds to AT1 receptors, which are localized in smooth muscle tissues, heart, kidneys and adrenal glands, and performs the necessary biological functions. These include the release of aldosterone and vasoconstriction. It also helps the proliferation of smooth muscle cells.

Losartan is a blocker of all physiological effects of angiotensin II, regardless of the source and route of synthesis. Communication with AT1 receptors is selective, there is no communication and blocking of the receptors of other ion channels and hormones, which are important for the functioning of the cardiovascular system. It also does not inhibit ACE, which contributes to the degradation of bradykinin. In this regard, side effects that are associated with bradykinin are rare.

When the drug is taken, the activity of plasma renin increases, because of this, angiotensin II is more concentrated in it. In this case, antihypertensive activity and a decrease in the concentration of plasma aldosterone remain. This indicates an effective blockade of angiotensin II receptors. After the cancellation of "Losartan" occurs, the concentration of angiotensin II and plasma renin activity decreased to the initial value within three days.

Losartan has a high affinity for angiotensin II receptors. Its concentration in blood plasma depends on the dosage of the drug. The greatest effect is achieved after 3-6 weeks from the start of use.

In patients with arterial hypertension and proteinuria (more than 2 g per day) in the absence of diabetes mellitus, proteinuria, immunoglobulin G and albumin excretion decrease.

In female representatives of the postmeionusal period, who used the drug in a dosage of 50 mg per day for a month, no effect of treatment on systemic and renal prostaglandin levels was found. The drug is not associated with autonomic reflexes and does not affect plasma norepinephrine levels for a long time.

Pharmacokinetics

With internal use, losartan is absorbed from the gastrointestinal tract. Systemic bioavailability is approximately 33% regardless of food. On average, the maximum concentration is reached after an hour.

Losartan, together with its active metabolite, binds to plasma proteins more than 99%. The volume of distribution is 34 liters. Losartan hardly crosses the blood-brain barrier.

The effect of "primary passage" of losartan through the liver occurs. About 14% of the dosage of losartan becomes its active metabolite with a carboxyl group.

Plasma clearance of losartan together with the active metabolite is 600 ml and 50 ml per minute, renal clearance is 74 ml and 26 ml per minute. When taken internally, about 4% of the dosage is excreted through the kidneys in unchanged form, about 6% as an active metabolite. Losartan has linear pharmacokinetics if the dosage for internal administration is up to 200 mg. It is excreted through the kidneys and bile.

When comparing males with arterial in old and young age, a significant difference in plasma concentrations of losartan was not found. For female representatives, the indicator was twice as high as for men. No difference was found in the concentrations of the active metabolite.

In patients with creatinine clearance of more than 10 ml / min of losartan in plasma, the concentration was the same as in people with healthy kidneys. Patients who required hemodialysis had about twice the concentration-time area of \u200b\u200bpatients with healthy kidneys.

Indications for use

Let's consider what the Losartan tablets help with. Basically, they are prescribed for hypertension (arterial hypertension), especially in the early stages.
In addition, the drug "Losartan" has the following indications for use:

• ischemia of the heart of a chronic nature;
• reducing the risk of cardiovascular disease and death in patients with arterial hypertension and left ventricular hypertrophy;
• a decrease in the volume of circulating blood;
• recovery after kidney transplant;
• normalization of kidney function and their protection in the diagnosis of type 2 diabetes mellitus.

The question often arises as to what pressure should be taken "Losartan". It is impossible to give a clear answer to it, since each has its own. Under certain indicators, one person may feel good, while the other will significantly decrease his working capacity and worsen his health.

A specialist should determine when to prescribe a medicine, the dosage and duration of the course. The generally accepted borderline state is 135 by 86 mm Hg. Art. Exceeding this indicator indicates the need to take antihypertensive drugs.

Contraindications

Before taking it, you need to go through a full examination, since drugs that lower blood pressure usually have many contraindications.

Contraindications to taking "Losartan":

• excessive sensitivity to ingredients in the composition;
• severe renal failure;
• genetic lactose intolerance;
• pregnancy;
• feeding;
• age up to 18 years.

Important: "Losartan" is a drug that directly affects the renin-angiotensin-aldosterone system. Taking it during pregnancy in the second and third trimester can lead to developmental defects of the child, leading to negative consequences, reaching intrauterine death. If pregnancy is established while taking the drug, you must immediately stop the therapeutic course.

Currently, there is no information on the release of the active substance "Losartan" along with breast milk. Because of this, you should not start taking the product while feeding. If, due to the woman's condition, this is not possible, lactation should be suspended for the entire duration of treatment.

Instructions for use

Usually, for hypertensive disease, "Losartan" is prescribed in a dosage of 50 mg, which must be taken once a day at any time. Some people need to double it, and they need strict medical supervision. The dosage of 100 mg is divided into two doses. A dose reduction is necessary for liver diseases, with caution taken with pathologies of the kidneys.

The specialist issues instructions after examining the patient and diagnosing. Do not self-medicate. When taking it, it is important to constantly monitor the pressure indicators.

The maximum concentration of the active substance is reached within 60 minutes. The duration of action is a day. A noticeable effect of the treatment is achieved after 4-6 weeks with regular use. The activity of the drug is not affected by food consumption, so you can choose a convenient time for taking.

For patients with chronic heart failure, the daily dosage is 12.5 mg, which is increased to 25 mg a week later and to 50 mg a week later.

In case of liver failure or the patient's age over 75 years, it is recommended to start therapy with a dosage of 25 mg per day.

The main condition for therapy is regular use of the drug and strict adherence to the dose recommended by the doctor. The patient should not independently decide to stop taking, even if there is a noticeable improvement. If there was a one-time missed appointment, you should take the medicine as soon as the patient remembered about it. In the case when the time for the next appointment has already come, you need to skip the last one, and again return to the standard treatment regimen.

The medicine is prescribed for elderly and senile patients. Standard doses are observed, which can be adjusted by the doctor according to individual indicators. This group of patients should be constantly monitored for kidney function. This is especially important when taking diuretics and non-steroidal anti-inflammatory drugs at the same time.

Side effects

Patients are usually well tolerated. Side effects are mild enough not to require drug withdrawal.

Side effects (more than 1%)

General violations:

• excessive fatigue;
• pain in the chest;
• asthenia;
• peripheral edema;
• weakness.

In the cardiovascular system:

• tachycardia;
• feeling of palpitations.

Digestive system:

• dyspepsia;
• pain in the abdomen;
• nausea;
• diarrhea.

Musculoskeletal system:

• back pain;
• pain in the legs;
• muscle cramps.

Central nervous system:

• headache;
• sleep problems;

Respiratory system:

• swelling of the nasal mucosa;
• infectious processes in the upper respiratory tract;
• cough;
• sinusitis;
• bronchitis;
• pharyngitis.

Side effects (less than 1%)

The cardiovascular system:

• bradycardia;
• vasculitis;
• arterial hypotension, especially in patients with intravascular dehydration (for example, when diagnosed with severe heart failure or when using a high dosage of diuretics);
• arrhythmia;
• dose-dependent orthostatic hypotension;
• myocardial infarction.

Digestive system:

Skin:

• excessive sweating;
• baldness;
• dry skin;
• photosensitivity;
• erythema;
• ecchymosis.

Allergies:

• angioedema (including swelling of the larynx and vocal fold, which leads to obstruction of the airways, swelling of the tongue, face, pharynx, lips);
• hives;
• rashes on the skin;

Hematopoietic system:

• eosinophilia;
• anemia;
• purple Schoenlein-Genoch;
• thrombocytopenia.

Sensory organs and nervous system:

• insomnia;
• drowsiness;
• fainting;
• depressive conditions;
• migraine;
• peripheral neuropathy;
• shiver;
• violations of taste buds;
• ataxia;
• memory problems;
• state of anxiety;
• tinnitus;
• conjunctivitis;
• pathology of vision.

Musculoskeletal system:

• arthritis;
• fibromyalgia;
• pain in the knees and shoulders.

Urinary system:

• impaired renal function;
• infectious processes in the urinary tract;
• strong urge to urinate.

Reproductive system:

• impotence;
• decreased sex drive.

Other side effects:

• nosebleed;
• exacerbation of gout.

Laboratory indicators:

• often - hyperkalemia (potassium more than 5.5 mmol / l);
• infrequently - an increase in urea, creatinine, residual nitrogen in serum);
• very rarely - an increase in the activity of grapsaminases in a moderate form (alanine aminotransferase, aspartate amipotransferase), hyperbilirubia.

If the patient observes an aggravation of the listed side effects or other pathological conditions, he needs to contact a medical institution.

Overdose

• decrease in pressure;
• rapid pulse.

Interaction with other medications

When taking certain drugs together with Losartan, there may be negative consequences. Interaction can manifest itself when using dietary supplements with potassium in the composition, potassium-sparing diuretics and non-steroidal anti-inflammatory drugs. Also, the body can metabolize drugs in different ways, so their joint use with "Losartan" can cause an increase to the upper mark of active substances.

It is dangerous to take Losartan tablets with the following drugs:

• ACE inhibitors. The work of "Losartan" is similar to this group, and he is not included in it. Because of this, hyperkalemia, a dangerous decrease in pressure, renal failure may develop;
• ... Pressure may drop sharply. To prevent this from happening, the specialist must adjust the dosage of the drug "Losartan";
• Potassium salt substitutes or potassium supplements. Potassium levels can rise very high, leading to pathologies associated with the cardiovascular system;
• Potassium-sparing diuretics. An excess of potassium in the blood may occur due to improper absorption of diuretics by the body;
• Rifampicin. The level of the active substance of the drug in the body decreases due to improper absorption of "Losartan";
• Lithium. An increase in the amount of lithium in the blood and a change in metabolism;
• Non-steroidal anti-inflammatory drugs. With kidney failure and kidney disease, there is a risk of worsening the current condition.

Interaction with alcohol

You can use alcohol and Lozartan pressure pills under the following conditions:

• men: one day before and 14 hours after drinking the drink;
• women: 32 hours before and 20 hours after drinking alcohol;
• after 15 days, if there was a therapeutic course, regardless of gender.

To minimize the risk of health threats, it is best to avoid alcohol for the entire course of treatment.

It is forbidden to take alcohol:

• together with the drug;
• during pregnancy at any time;
• during a therapeutic course.

Admission in childhood

According to the instructions, the use of the drug is prohibited to treat patients under the age of eighteen. This is due to the lack of information about the effectiveness and safety of admission in children.

Application during pregnancy

The drug is prohibited for pregnant and lactating women. The drug affects the renin-angiotensin-aldosterone system, which has an extremely negative effect on the health of the developing fetus. There is no information on the excretion of the drug in milk, therefore, you should interrupt the feeding or replace the drug.

special instructions

The drug should be prescribed with caution for the following diagnoses:

• if the patient has a history of angioedema, it is important to exercise caution in connection with cases of anaphylactic reactions and angioedema with involvement of the pharynx and larynx;
• in the case of a reduced BCC, symptomatic arterial hypotension may occur, therefore a lower dose is required;
• with mitral or aortic stenosis and obstructive hypertrophic cardiomyopathy;
• with ischemic heart disease and cerebrovascular diseases;
• with CHF, there is a risk of severe hypotension and acute renal failure;
• with primary hyperaldosteronism;
• with violations of the liver, the concentration of the substance in the plasma increases;
• with violations of the kidneys.

Analogs

The names of similar medicines for high blood pressure:

• "Presartan";
• Losartan Teva;
• Losartan Hydrochlorothiazide;
• Brozaar;
• Losartan Canon;
• Losartan Richter;
• "Angiazar";
• "Pulsar";
• "Closart";
• "Kozaar";
• Blocktran;
• "Cardomin";
• Losakar;
• Xartan;
• "Lothar".

Lozartan is a pharmaceutical drug used to lower blood pressure (BP).

This drug with the active substance of the same name belongs to the group of sartans. Losartan belongs to biphenyl derivatives of tetrazole.

Chemical formula: C 22 H 23 ClN 6 O. Name: 2-Butyl-4-chloro-1 - [- 4-yl] methyl] -1H-imidazole-5-methanol.

In this drug, Losartan is represented by a potassium salt.

In terms of physical properties, it is a white or whitish crystalline powder, readily soluble in water and in ethyl alcohol, and poorly soluble in organic solvents.

Mechanism of action

The action of Losartan, like other sartans, is associated with the ability to influence the RAAS - the renin-angiotensin-aldosterone system. The end product of the reactions occurring in this system is angiotensin II. This protein compound is the end product of complex biochemical reactions.

In a simplified form, these reactions can be represented as follows. The liver synthesizes the protein angiotensinogen. Under the action of another protein, renin, produced by the kidneys, angiotensinogen is converted into angiotensin I, which is physiologically inactive.

Further, angiotensin I, with the participation of an angiotensin-converting enzyme (ACE), is activated into angiotensin II. It is through this compound that the RAAS realizes its effect on the organism of mammals and humans. Under the influence of angiotensin II, small muscle-type arteries (arterioles) spasm, which leads to an increase in the total peripheral resistance (OPS) of blood vessels and to an increase in blood pressure.

Maintaining blood pressure at a stable level is vital. But its excessive growth (arterial hypertension) is a negative moment, leading to the development of hypertension and cardiac pathology.

In addition, the RAAS activates the sympathetic nervous system. This system, through the mediators-catecholamines, adrenaline and norepinephrine, spasms the vessels, and thus aggravates hypertension. Angiotensin II stimulates the synthesis of aldosterone by the adrenal cortex and vasopressin by the neurohypophysis (posterior lobe of the pituitary gland).

These hormones act to retain sodium and water in the body. This phenomenon additionally stimulates the growth of blood pressure, is manifested by the retention of water and sodium in the body, a decrease in urinary excretion (diuresis) and an increase in the volume of circulating blood.

The negative effect of angiotensin II on the vessels is also expressed in the fact that it stimulates the synthesis of low-density cholesterol (low-density lipoproteins), and thereby contributes to the formation of atherosclerotic plaques on the endothelium (inner wall) of the vessels.

Under the action of this substance, foci of growth of fibrous tissue are formed in the heart muscle. Structurally, this process is manifested by thickening (hypertrophy) of the myocardium, cardiosclerosis, and, as a consequence, arrhythmias due to disturbances in the cardiac conduction system.

Sclerosis of the kidneys (nephrosclerosis) with arterial hypertension is caused by spasm of the renal arteries. The name of this pathological condition is the primary shriveled kidney. It is a frequent companion of hypertension. Manifested by renal impairment (nephropathy) and progressive renal failure.

Nephropathy is a typical complication of diabetes mellitus. The problem is that angiotensin II also negatively affects carbohydrate metabolism. It increases the tolerance of fat cells to insulin, which leads to type II diabetes. Also, angiotensin II slows down the excretion of uric acid salts by the kidneys, and this can lead to gout.

Angiotensin II exerts its effect by acting on receptors located in the corresponding tissues: in the vascular endothelium, in the myocardium, in the adrenal glands and in the kidneys, in adipose tissue. These receptors are heterogeneous. Therefore, several types of angiotensin (AT) receptors are distinguished.

The negative effect is realized through AT-1 receptors. Stimulation of AT-2 receptors causes opposite effects: dilation (vasodilation) of blood vessels and inhibition of sclerotic processes in the heart and kidneys. The functions of other, AT-3 and AT-4 receptors are not fully understood.

Losartan selectively blocks AT-1 receptors. At the same time, vasodilation, a decrease in blood pressure, an improvement in blood circulation in the myocardium, in the kidneys, and in the brain are noted. The insulin tolerance of cells increases, and the effectiveness of insulin in lowering blood sugar increases.

Intravascular atherosclerotic processes slow down. Clinically, this is manifested by stabilization of blood pressure, improvement of exercise tolerance. The frequency of angina attacks in ischemic heart disease is reduced. Likewise, the risk of developing myocardial infarction is reduced.

AT-2 receptors Losartan does not block, but on the contrary, indirectly stimulates them. The bottom line is that when the renal arteries expand, the kidneys begin to synthesize renin compensatory.

Ultimately, this leads to an increase in the amount of angiotensin II. Not finding the point of application due to blockade of AT-1 receptors, it begins to actively act on AT-2 receptors, thereby causing the corresponding effects: vasodilation and improvement of metabolic processes in tissues.

Losartan competitively binds to AT-1 receptors. This means that when the level of angiotensin II increases, it binds to receptors, displacing it.

However, in the liver, it is transformed with the formation of the metabolite EXP-3174. In terms of its activity, this metabolite is tens of times higher than the original substance, and noncompetitively, i.e., irreversibly, binds to AT-1 receptors. The value of the drug also lies in the fact that neither it nor its metabolites accumulate in the body. Addiction does not develop to this medicine.

History of creation

Work on the synthesis of Losartan began in 1980. Initially, this drug was codenamed S-8307. A little later, in 1986, the final version of the drug was obtained, which in its activity was 10,000 times higher than the original S-8307. In 1995 g.

Losartan has been formally recommended for use in the treatment of cardiovascular disease by the US Food and Drug Administration. It was the second of the synthesized sartans.

Although in fact it can be considered the first, tk. its predecessor, Saralazin, has never been used in clinical practice due to its side effects. Sartans, selective AT-2 receptor antagonists, can be considered the “youngest” drug group.

Their effectiveness lies in the fact that they block the very last, final link of the RAAS. In this, sartans compare favorably with another group - ACE inhibitors.

The bottom line is that in addition to ACE, other enzyme compounds are involved in the synthesis of angiotensin II, which are not affected by ACE inhibitors. And sartans, by blocking receptors, prevent the action of angiotensin II on tissues, regardless of the pathway of its synthesis.

Currently, these drugs are included in most drug regimens for the treatment of arterial hypertension and heart disease. It is actively used in the USA, Zap. Europe, Russia and many post-Soviet countries.

In the early years of application, Losartan's worldwide sales revenues were $ 200 million. In 2005, a similar amount exceeded the $ 3 billion mark.

Synthesis technology

The production technology of the drug involves the production of potassium salt nanocapsules enclosed in a xanthan gum shell. For this, potassium Losartan is added to the suspension of the gum in benzene in the presence of the enzyme preparation E472C. The resulting mixture is stirred at a speed of 1000 / sec. Then add hexane, filter and dry.

Release forms

Tablets 50 and 100 mg

Losartan is produced under non-proprietary names by many foreign (Lek, Sandoz, Teva, Richter) and domestic firms. Therefore, on the pharmaceutical market, in addition to the Russian ones, one can find foreign (mainly Polish and Hungarian) analogues.

Among doctors and patients, the drug is better known under the trade name Cozaar, manufactured by Merck Sharp Dome in England. In Russia and the CIS countries, the generic Lorista is widespread, which is produced by the Russian branches of the Krka company.

Other generics include:

• Blocktran - Pharmstandard, Russia;
• Vasotenz - Actavis, Iceland;
• Lozal - Zentiva, Slovakia;
• Lozarel - Lek, Slovenia, Lek;
• Presartan - Ipka, India.

All these drugs are pills. The mass of the tablets is 50 and 100 mg. Blockran can have a mass of 12, 5 mg. The quality of generics, both Russian and foreign, is good.

But Russian drugs are cheaper. Abroad, the drug may have the names Lozanorm, Lozarbon, Lozium, Lostad, Sartkasal, and many others. Along with Losartan, biphenyl derivatives of tetrazole are used, in which the active and substances are: Candesartan, Valsartan, Tazosartan, Ibesartan.

Indications

• Arterial hypertension;
• Chronic heart failure;
• Diabetic nephropathy.

Dosage

The tablets are taken once in a daily dose. This dose is in most cases 50 mg. With a weak hypotensive effect, the daily dose can be increased to 100 mg in a single dose. The use of tablets is independent of food intake.

The drug is taken in a long course, because the maximum hypotensive effect is achieved after 3-6 weeks of continuous use. Losartan can be combined with other antihypertensive drugs. In the case of a combination with diuretics, it is recommended to reduce the initial daily dose to 25 mg.

In chronic heart failure, it is recommended to start taking with a minimum dose of 12.5 mg, increasing it to 25 and 50 mg during each subsequent week. Patients suffering from hepatic insufficiency, as well as persons over 75 years of age, are advised to take the drug in a daily dose of 25 mg.

Pharmacodynamics

The drug is absorbed into the digestive tract. Systemic bioavailability is 33%. In the liver, Losartan undergoes metabolic transformations, during which the active metabolite EXP-3174 and several other inactive metabolites are formed. Moreover, EXP-3174 accounts for about 14% of Lozartan taken internally. The maximum concentration is formed 1 hour after its administration.

For an active metabolite, this figure is 3-4 hours. In patients with cirrhosis of the liver, the concentration of the drug and its metabolites may be several times higher than those in healthy individuals. About 99% of Losartan and EXP-3174 binds to plasma proteins.

The drug is excreted through the kidneys and through the intestines. Moreover, 6% of the drug taken orally is excreted through the kidneys in the form of an active metabolite, and 4% - unchanged. The half-life of Losartan is 2 hours, and EXP-3174 is 6-9 hours.

Side effects

• Cardiovascular system: dose-dependent hypotension, bradycardia, arrhythmias, nosebleeds, increased frequency of angina attacks;
• Gastrointestinal tract: anorexia, dry mouth, nausea, vomiting, constipation, flatulence, exacerbation of gastritis, hepatitis, increased liver enzymes in blood plasma, jaundice;
• CNS: general weakness, sleep disturbances, fainting, migraine, memory disorders, tremors of the extremities, peripheral sensory disturbances of the type of paresthesia;
• Urinary system: impaired renal function, rarely - an urgent urge to urinate;
• Musculoskeletal system: arthralgia and myalgia;
• Skin and mucous membranes: urticaria, itching, angioedema, erythema, excessive sweating, photosensitivity, alopecia;
• Blood: anemia, eosinophilia, thrombocytopenic purpura, hyperkalemia;
• Sense organs: conjunctivitis, vision, taste disturbances, ringing in the ears;
• Reproductive system: decreased libido, impotence.

These side effects are rare, and many patients tolerate Losartan well.

Contraindications

• Individual intolerance to Losartan;
• Severe liver failure;
• Dehydration;
• Hypotension;
• Age under 18.

It is prescribed with caution for renal failure, renal artery stenosis, hyperkalemia, as well as mitral and aortic stenosis.

Interaction with other drugs

• Potassium-sparing diuretics, potassium preparations - exacerbation of hyperkalemia;
• Rifampicin and Fluconazole - reduce the content of the active metabolite in the blood;
• Lithium preparations - increasing their toxicity;
• NSAIDs - weakening of the hypotensive effect of Losartan, reversible deterioration of renal function;
• Other antihypertensive drugs, antipsychotics, tricyclic antidepressants, Amifostin, Baclofen - increased antihypertensive effect;
• Aleskiren (renin inhibitor) - hypotension, hyperkalemia, impaired renal function.

Pregnancy and lactation

There is no data on the negative effect of Losartan on the fetus. Nevertheless, it has been established that all drugs that affect the RAAS are potentially dangerous in terms of fetal death, especially in late pregnancy - in the II-III trimesters. Therefore, during pregnancy, reception is highly undesirable. Lactation is also a contraindication to taking Losartan. Otherwise, breastfeeding should be stopped.

Storage

Store at a temperature not exceeding 30 0 C. Shelf life - 2 years. The drug is dispensed by prescription.

Dear Pharmamir website visitors. This article is not medical advice and cannot serve as a substitute for consulting a doctor.

Catad_pgroup Angiotensin receptor antagonists

Losartan - instructions for use

Registration number:

LP-005949

Trade name:

Losartan

International non-proprietary name: (INN):

losartan

Dosage form:

film-coated tablets

Composition:

Each 12,500 mg film-coated tablet contains:
Active substance: Losartan potassium - 12,500 mg
Excipients: lactose monohydrate - 6,250 mg, microcrystalline cellulose (PH 102) - 13,875 mg, pregelatinized corn starch - 4,500 mg, magnesium stearate - 0,375 mg
Tablet shell: hypromellose - 0.394 mg, hydroxypropyl cellulose - 0.281 mg, gitana dioxide - 0.450 mg.

Each 25,000 mg film-coated tablet contains:
Active substance: Losartan Potassium 25,000 mg
Excipients: lactose monohydrate - 12,500 mg, microcrystalline cellulose (PH 102) - 27,750 mg, pregelatinized corn starch - 9,000 mg, magnesium stearate - 0.750 mg
Tablet shell: hypromellose - 0.920 mg, hydroxypropyl cellulose 0.650 mg, titanium dioxide - 1.050 mg.

Each tablet is 50,000 mg film-coated. contains:
Active substance: Losartan Potassium 50,000 mg
Excipients: lactose monohydrate - 25,000 mg, microcrystalline cellulose (PH 102) - 55,500 mg, pregelatinized corn starch - 18,000 mg, magnesium stearate - 1,500 mg
Tablet shell: hypromellose - 1,840 mg, hydroxypropyl cellulose 1,310 mg, titanium dioxide - 2,100 mg.

Each 100.00 mg film-coated tablet contains:
Active substance: Losartan potassium - 100.00 mg
Excipients: lactose monohydrate - 50,000 mg, microcrystalline cellulose (PH 102) - 111,000 mg, pregelatinized corn starch - 36,000 mg, magnesium stearate - 3,000 mg
Tablet shell: hypromellose - 3,680 mg, hydroxypropyl cellulose - 2,620 mg, titanium dioxide - 4,200 mg.

Description

Tablets 12.5 mg:
White to off-white, round, biconvex film-coated tablets, smooth on both sides.
25 mg tablets:
Oval biconvex tablets, film-coated from white to almost white, with an embossed inscription "25" on one side.
50 mg tablets:
Oval biconvex tablets, film-coated from white to almost white, with an embossed inscription "50" on one side.
100 mg tablets:
Capsule-shaped biconvex tablets, film-coated from white to almost white, with an embossed inscription "100" on one side.

Pharmacotherapeutic group:

angiotensin II receptor antagonist

ATX code:

Pharmacological properties

Mechanism of action
Angiotensin II is a powerful vasoconstrictor, the main active hormone of the renin-angiotensin-aldosterone system (RAAS), as well as a decisive pathophysiological link in the development of arterial hypertension (AH).
Angiotensin II binds to AT 1 receptors found in many tissues (eg, vascular smooth muscle, adrenal gland, kidney and heart) and causes a number of important biological effects, including vasoconstriction) and the release of aldosterone. Angiotensin II also stimulates the proliferation of smooth muscle cells. The role of the second type of angiotensin II receptor in cardiovascular homeostasis of AT 2 subtype is unknown.
Losartan is a selective antagonist of AT 1 -receptors of angiotensin II, effective when taken orally. Losartan and its pharmacologically active carboxylated metabolite (E-3174), as in vitro so and in vivo block all physiological effects of angiotensin II, regardless of the source or route of synthesis. Unlike some peptide angiotensin II antagonists, losartan does not have agonist effects.
Losartan selectively binds to AT 1 -receptors and does not bind or block the receptors of other hormones and ion channels, which play an important role in the regulation of the function of the cardiovascular system. In addition, losartan does not inhibit the angiotensin-converting enzyme (ACE, kininase II), which contributes to the degradation of bradykinin. Consequently, the effects that are not directly related to the blockade of AT 1 receptors, in particular, the enhancement of the effects associated with exposure to bradykinin or the development of edema (losartan 1.7%, placebo 1.9%), are not related to the action of losartan.

Pharmacodynamics
During the period of losartan administration, the elimination of the negative feedback, which consists in the suppression of renin secretion by angiotensin II, leads to an increase in the activity of blood plasma renin (ARP). The growth of ARP is accompanied by an increase in the level of angiotensin II in the blood plasma. It was reported that with long-term (6-week) treatment of patients with hypertension with losartan at a dose of 100 mg / day, at the time of reaching the maximum concentration in the blood plasma, a 2-3-fold increase in the level of angiotensin II in the blood plasma was observed. In some patients, an even greater increase was observed, especially with a short duration of treatment (2 weeks). However, antihypertensive activity and a decrease in plasma aldosterone concentration were manifested after 2 and 6 weeks of therapy, which indicates an effective blockade of angiotensin II receptors. ARP and the level of angiotensin II decreased to the initial values \u200b\u200bobserved before the start of taking the drug, 3 days after the discontinuation of losartan. The effect of the drug on ARP and angiotensin II levels was comparable to that of 50 mg losartan.
Since losartan is a specific antagonist of the AT 1 receptors of angiotensin II, it does not inhibit ACE (kininase II), an enzyme that inactivates bradykinin. A study comparing the effects of losartan at doses of 20 mg and 100 mg with the effects of an ACE inhibitor in response to angiotensin I, angiotensin II, and bradykinin showed that losartan blocks the effects of angiotensin I and angiotensin II without affecting the effects of bradykinin. These results are consistent with the data on the specificity of the mechanism of action of losartan. In contrast, the ACE inhibitor blocked the response to angiotensin I and increased the severity of the response to bradykinin, without affecting the severity of the response to angiotensin II, which demonstrates the pharmacodynamic difference between losartan and ACE inhibitors.
Plasma concentrations of losartan and its active metabolite, as well as the antihypertensive effect of losartan, increase with increasing dose of the drug. Since losartan and its active metabolite are angiotensin II receptor antagonists, they both contribute to the antihypertensive effect.
It was reported that in a clinical study with a single dose of 100 mg of losartan potassium, which included healthy volunteers (men), administration of the drug under conditions of a high- and low-salt diet did not affect the glomerular filtration rate (GFR), effective renal plasma flow and filtration fraction. Losartan has a natriuretic effect, which was more pronounced with a low-salt diet and, apparently, was not associated with the suppression of early sodium reabsorption in the proximal renal tubules. Losartan also caused a transient increase in renal excretion of uric acid.
In patients with hypertension, proteinuria (at least 2 g / 24 hours), without diabetes mellitus and taking losartan at a dose of 50 mg with a gradual increase to 100 mg for 8 weeks, there was a significant decrease in proteinuria by 42%. The fractional excretion of albumin and immunoglobulins (IgG) also decreased significantly. In these patients, losartan stabilized the GFR and reduced the filtration fraction.
In postmenopausal women with hypertension, taking losartan at a dose of 50 mg / day for 4 weeks, there was no effect of therapy on the renal and systemic levels of prostaglandins.
Losartan does not affect autonomic reflexes and does not have a long-term effect on plasma norepinephrine levels.
In patients with hypertension, losartan at doses up to 150 mg / day did not cause clinically significant changes in the concentration of fasting triglycerides, total cholesterol and high density lipoprotein cholesterol (HDL). In the same doses, losartan had no effect on fasting blood glucose concentration.
In general, losartan caused a decrease in serum uric acid concentration (usually less than 0.4 mg / dL), which persisted during long-term therapy.
In controlled clinical trials, which included patients with hypertension, there were no cases of drug withdrawal due to an increase in serum creatinine or potassium concentration.
In a 12-week parallel study, which enrolled patients with NYHA functional class II-IV left ventricular failure and most of them received diuretics and / or cardiac glycosides, the effects of losartan at doses of 2.5, 10, 25 and 50 mg / days with a placebo. In doses of 25 and 50 mg per day, the drug had positive hemodynamic and neurohormonal effects that were observed throughout the study.
Hemodynamic effects included an increase in cardiac index and a decrease in pulmonary capillary wedge pressure, as well as a decrease in systemic vascular resistance, mean systemic blood pressure, and heart rate (HR). The incidence of arterial hypotension in these patients depended on the dose of the drug. Neurohormonal effects included decreased blood levels of aldosterone and norepinephrine.

Pharmacokinetics
Suction
When taken orally, losartan is well absorbed and metabolized during "primary passage" through the liver, resulting in the formation of an active carboxylated metabolite and inactive metabolites. The systemic bioavailability of losartan is approximately 33%. Average maximum concentrations (C max) of losartan and its active metabolite are reached after 1 hour and after 3-4 hours, respectively. When taking losartan with food, there was no clinically significant effect on the plasma concentration profile of losartan.
Distribution
Losartan and its active metabolite bind to blood plasma proteins (mainly albumin) by more than 99%. The volume of distribution of losartan is 34 liters. Studies in rats have shown that losartan practically does not cross the blood-brain barrier.
Metabolism
Approximately 14% of a dose of losartan administered intravenously or orally is metabolized to form an active metabolite. After oral administration and / or intravenous administration of losartan labeled with 14 C, the circulating radioactivity of blood plasma was mainly determined by losartan and its active metabolite. In addition to the active metabolite, biologically inactive metabolites are formed, including two main metabolites formed as a result of hydroxylation of the butyl group of the chain, and one minor metabolite, N-2-tetrazole glucuronide.
Taking the drug simultaneously with food intake does not have a clinically significant effect on its serum concentrations.
Withdrawal
Plasma clearance of losartan and its active metabolite is about 600 ml / min and 50 ml / min, respectively. The renal clearance of losartan and its active metabolite is approximately 74 ml / min and 26 ml / min, respectively. After oral administration, about 4% of the dose taken is excreted unchanged by the kidneys and about 6% - in the form of an active metabolite. The pharmacokinetic parameters of losartan and its active metabolite when administered orally (in doses up to 200 mg) are linear.
The half-life (T 1/2) of losartan and the active metabolite in the terminal phase of losartan and the active metabolite is 2 hours and 6-9 hours, respectively. There is no cumulation of losartan and its active metabolite when used in a dose of 100 mg once a day. It is excreted mainly through the intestines with bile - 58%, by the kidneys - 35%.

Pharmacokinetics in special patient groups
Elderly patients
Plasma concentrations of losartan and its active metabolite in elderly patients with hypertension do not differ significantly from these indicators in young patients with hypertension.
Floor
Plasma concentrations of losartan were 2 times higher in women with hypertension compared with men with hypertension. The concentrations of the active metabolite did not differ in men and women. This clear pharmacokinetic difference has no clinical significance.
Patients with impaired liver function
When losartan was taken orally by patients with mild and moderate alcoholic cirrhosis, the plasma concentrations of losartan and its active metabolite were 5 and 1.7 times higher, respectively, than in young healthy male volunteers.
Patients with impaired renal function
Plasma concentrations of losartan in patients with creatinine clearance (CC) above 10 ml / min did not differ from those in patients with normal renal function. When comparing the area under the concentration curve (PCC) in patients with normal renal function, the PCC of losartan in patients on hemodialysis was approximately 2 times higher. Plasma concentrations of the active metabolite do not change in patients with impaired renal function or in patients on hemodialysis. Losartan and its active metabolite cannot be removed by hemodialysis.

Indications for use

• Arterial hypertension.
• Reduction in the risk of associated cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy, manifested by a cumulative reduction in the incidence of cardiovascular mortality, stroke and myocardial infarction.
• Chronic kidney disease in patients with arterial hypertension and type 2 diabetes mellitus with concomitant proteinuria ≥0.5 g / day as an antihypertensive agent as part of complex therapy.
• Chronic heart failure with treatment failure with ACE inhibitors or intolerance to ACE inhibitors. It is not recommended to transfer patients with chronic heart failure and stable indicators while taking ACE inhibitors to drug therapy.

Contraindications

• Hypersensitivity to any of the ingredients in this drug.
• Simultaneous use with aliskiren or aliskiren-containing drugs in patients with diabetes mellitus and / or moderate or severe renal impairment (GFR less than 60 ml / min / 1.73 m² of body surface area) (see the section "Interaction with other drugs").
• Severe violations of liver function (no experience with use).
• Concomitant use with ACE inhibitors in patients with diabetic nephropathy.
• Lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (the drug contains lactose).
• Pregnancy and the period of breastfeeding.
• Age up to 18 years (efficacy and safety have not been established).

Carefully

Bilateral stenosis of the renal arteries or stenosis of an artery of a solitary kidney; hyperkalemia; condition after kidney transplantation (no experience with use); aortic stenosis, mitral stenosis; hypertrophic obstructive cardiomyopathy; heart failure with concomitant severe renal failure; chronic heart failure IV functional class according to NYHA classification; heart failure with life-threatening arrhythmias; coronary artery disease; cerebrovascular diseases; primary hyperaldosteronism; a history of angioedema; use in patients of the black race.
Patients with a reduced volume of circulating blood (for example, receiving treatment with large doses of diuretics) may experience symptomatic arterial hypotension.

Application during pregnancy and during breastfeeding

The use in the second and third trimesters of pregnancy of drugs acting directly on the RAAS can cause serious damage and even death of the developing fetus, therefore, when pregnancy is diagnosed, the drug Losartan should be immediately canceled and, if necessary, alternative antihypertensive therapy should be prescribed.
Losartan therapy should not be started during pregnancy. If patients planning a pregnancy, continued therapy with losartan is deemed necessary, losartan should be replaced with alternative antihypertensive drugs that have an established safety profile when used during pregnancy.
Although there is no experience with the use of Losartan in pregnant women, preclinical animal studies have shown that taking the drug leads to the development of serious embryonic and neonatal injuries and death of the fetus or offspring. It is believed that the mechanism of these phenomena is due to the impact on the RAAS.
Renal perfusion in the fetus, depending on the development of RAAS, appears in the second trimester, so the risk to the fetus increases if the drug Losartan is used in the second or third trimester of pregnancy. The use of ARA II in the second and third trimesters of pregnancy has a toxic effect on the fetus (decreased renal function, development of oligohydramnios, slowing down of cranial ossification) and the newborn (renal failure, arterial hypotension, hyperkalemia). If the drug Losartan is used in the second trimester of pregnancy and later, an ultrasound examination of the skull and kidney function is recommended.
Newborns whose mothers took Losartan during pregnancy should be carefully examined for arterial hypotension. It is not known whether losartan is excreted in breast milk. Since many drugs are excreted in breast milk, and there is a risk of potential adverse effects in a breastfed baby, a decision should be made whether to stop breastfeeding or discontinue the drug, taking into account the need for the mother to take the drug.

Method of administration and doses

The drug Losartan is taken orally, regardless of food intake.
The tablets are swallowed whole, without chewing, with water.
The drug Losartan can be taken in combination with other antihypertensive drugs.
To ensure the required dosage regimen, it is possible to take the drug Losartan at a dose of 50 mg.
Arterial hypertension
The standard initial and maintenance dose for most patients is 50 mg of Losartan once a day. The maximum antihypertensive effect is achieved within 3-6 weeks from the start of therapy. In some patients, in order to achieve a greater therapeutic effect, the dose may be increased to a maximum daily dose of 100 mg of Losartan once a day.
In patients with reduced circulating blood volume (BCC) (for example, when taking large doses of diuretics), the initial dose of Losartan should be reduced to 25 mg 1 time per day (see section "Special instructions").
There is no need to select an initial dose for elderly patients and patients with impaired renal function, including patients on dialysis.
Patients with a history of liver disease are advised to prescribe lower doses of the drug Losartan (see section "Special instructions").
Reducing the risk of associated cardiovascular morbidity and mortality in patients with hypertension and left ventricular hypertrophy
The standard starting dose of the drug Losartan is 50 mg once a day. In the future, it is recommended to add hydrochlorothiazide in low doses or to increase the dose of Losartan to a maximum daily dose of 100 mg once a day, taking into account the degree of blood pressure reduction.
Kidney protection in patients with type 2 diabetes mellitus with proteinuria
The standard starting dose of the drug Losartan is 50 mg once a day. In the future, the dose of the drug Losartan can be increased to a maximum daily dose of 100 mg once a day, taking into account the degree of decrease in blood pressure.
In chronic kidney disease in patients with arterial hypertension and type 2 diabetes mellitus with concomitant proteinuria, the recommended dose is ≥0.5 g / day (see section "Indications for use").
The drug Losartan can be prescribed in combination with other antihypertensive drugs (for example, diuretics, blockers of "slow" calcium channels, alpha and beta-blockers, central antihypertensive drugs), insulin and other hypoglycemic agents (for example, sulfonylurea derivatives, glitazones and inhibitors glucosidase).
Chronic heart failure
The standard initial dose of the drug Losartan for patients with CHF is 12.5 mg once a day. Typically, the dose is titrated at weekly intervals (i.e. 12.5 mg / day, 25 mg / day, 50 mg / day, 100 mg / day, up to a maximum (only for this indication) dose of 150 mg 1 time per day ) depending on individual tolerance.

Side effect

The following side effects are given in accordance with the following gradations of the frequency of their occurrence in accordance with the classification of the World Health Organization: very often (≥1 / 10); often (≥1 / 100,<1/10); нечасто (≥1/1000, <1/100); редко (≥1/10 000, <1/1000) и очень редко (<1/10 000), частота неизвестна (недостаточно данных для оценки частоты развития).
The side effects of losartan are usually transient and do not require discontinuation of the drug.
When losartan was used to treat hypertension in controlled trials, among the side effects, only the incidence of dizziness differed from placebo by more than 1%.
In addition, dose-dependent orthostatic reactions were reported in less than 1% of patients. Rarely (≥0.01% and ≤0.1% of cases), the development of skin rash was reported, but the frequency of its occurrence was less than with placebo.

Arterial hypertension:
often - dizziness, infrequently - drowsiness, headache, sleep disturbances.
often vertigo.
Heart disorders: infrequently - palpitations, angina pectoris.
not
infrequently - abdominal pain, intestinal obstruction.
infrequently - a rash.
infrequently - asthenia, weakness, edema.
often hyperkalemia; rarely - an increase in the activity of alanine aminotransferase (usually disappears after discontinuation of treatment).
Patients with arterial hypertension and left ventricular hypertrophy:
General disorders and disorders at the injection site: often - asthenia, weakness.
Chronic heart failure:
often anemia.
Nervous system disorders: often - dizziness; infrequently - headache; rarely - paresthesia.
Heart disorders: rarely - fainting, atrial fibrillation, acute cerebrovascular accident.
Vascular disorders: often - (orthostatic) hypotension (including dose-mediated orthostatic effects).
Respiratory, chest and mediastinal disorders: infrequently - shortness of breath, cough.
Gastrointestinal disorders: infrequently - diarrhea, nausea, vomiting.
Skin and subcutaneous tissue disorders: infrequently - urticaria, skin itching, rash.
Kidney and urinary tract disorders: often - impaired renal function, renal failure.
General disorders and disorders at the injection site: infrequently - asthenia, weakness.
Influence on the results of laboratory and instrumental studies: often an increase in the concentration of urea, creatinine and potassium in the blood plasma; infrequently - hyperkalemia.
Arterial hypertension and type 2 diabetes mellitus with impaired renal function:
Nervous system disorders: often - dizziness.
Vascular disorders: often - (orthostatic) hypotension (including dose-mediated orthostatic effects).
General disorders and disorders at the injection site: often - asthenia, weakness.
Influence on the results of laboratory and instrumental studies: infrequently, hyperkalemia (in a clinical study in patients with type 2 diabetes mellitus and nephropathy, hyperkalemia\u003e 5.5 mmol / L developed in 9.9% of patients taking losartan tablets and 3.4% of patients taking placebo ); often hypoglycemia.
Post-registration observation:
Disturbances from the blood and lymphatic system: frequency unknown: anemia, thrombocytopenia.
Immune system disorders: rarely - allergic reactions, anaphylactic reactions, angioedema (including edema of the larynx, vocal folds, face, lips, pharynx and / or tongue (which leads to airway obstruction); in some of these patients, angioedema was previously noted in connection with the appointment other drugs, including ACE inhibitors), vasculitis (including hemorrhagic vasculitis (Schönlein-Henoch disease)).
Mental disorders: frequency unknown: depression
Nervous system disorders: frequency unknown - migraine, taste disturbance.
Hearing disorders and labyrinth disorders: frequency unknown - tinnitus.
Liver and biliary tract disorders: rarely - hepatitis, frequency is unknown - liver dysfunction, pancreatitis.
Skin and subcutaneous tissue disorders: frequency unknown - urticaria, pruritus, rash, photosensitivity.
Musculoskeletal and connective tissue disorders: frequency unknown - myalgia, arthralgia, rhabdomyolysis.
Violations of the genitals and mammary glands: frequency unknown - erectile dysfunction / impotence.
General disorders and disorders at the injection site: frequency unknown - malaise.
Influence on the results of laboratory and instrumental studies: hyponatremia.

Overdose

Symptoms: marked decrease in blood pressure, tachycardia, bradycardia (as a result of vagal stimulation).
Treatment: symptomatic therapy.
Losartan and its active metabolite cannot be removed by hemodialysis.

Interaction with other medicinal products

There were no clinically significant interactions of losartan with hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole and erythromycin. Rifampicin reduces the concentration of the active metabolite in the blood plasma. The clinical significance of this interaction has not been established.
Simultaneous application with aliskiren and preparations containing aliskiren, in patients with diabetes mellitus and / or moderate or severe renal impairment (glomerular filtration rate less than 60 ml / min / 1.73 m² body surface area) is contraindicated.
Fluconazole and rifampicin reduced plasma concentrations of the active metabolite of losartan. The clinical significance of this interaction has not been studied.
The simultaneous use of losartan, as well as other drugs affecting the RAAS with potassium-sparing diuretics (spironolactone, triamterene, amiloride, eplerenone), potassium supplements or potassium salts may increase serum potassium. Simultaneous use is not recommended.
As with the use of other drugs that affect the excretion of lithium, treatment with losartan may be accompanied by a decrease in excretion and an increase in the serum concentration of lithium, therefore, while treating with lithium preparations, its serum concentration should be monitored.
Non-steroidal anti-inflammatory drugs (NSAIDs), including selective COX-2 inhibitors and acetylsalicylic acid in doses of more than 3 g per day, when used simultaneously with angiotensin II receptor antagonists (ARA II), can reduce the effect of antihypertensive drugs.
Therefore, the antihypertensive effect of ARA II can be weakened by NSAIDs, including COX-2 inhibitors and acetylsalicylic acid in doses of more than 3 g per day.
In some patients with impaired renal function treated with NSAIDs, including COX-2 inhibitors, ARA II treatment may cause further deterioration of renal function, including the development of acute renal failure, and an increase in potassium (especially in patients with a history of renal dysfunction ). It should be used concomitantly with NSAIDs with caution, especially in elderly patients. In this case, it is necessary to adequately replenish the BCC and periodically monitor renal function from the start of therapy and thereafter. In some patients with impaired renal function who have used NSAIDs, including selective COX-2 inhibitors, the simultaneous use of ARA II may cause further deterioration in renal function.
Double blockade of RAAS: double blockade of RAAS, i.e. the addition of an ACE inhibitor to ARA II therapy is possible only in individual cases under close monitoring of renal function. In patients with atherosclerosis, heart failure or diabetes mellitus with damage to target organs, double blockade of the RAAS (with the simultaneous use of ARA II, ACE inhibitors or aliskiren) is accompanied by an increased incidence of arterial hypotension, syncope, hyperkalemia and renal dysfunction (including acute renal failure) in comparison with the use of a drug from one of the listed groups.
The simultaneous use of losartan with ACE inhibitors in patients with diabetic nephropathy is contraindicated.
Other drugs that cause arterial hypotension, including tricyclic antidepressants, antipsychotics, baclofen, amifostine: the simultaneous use of drugs that lower blood pressure (main or side effect) may increase the risk of developing arterial hypotension.

special instructions

The manifestation of such a symptom of hypersensitivity as angioedema is possible, therefore, patients with a history of angioedema (edema of the face, lips, pharynx / larynx and / or tongue) require careful monitoring of the drug.
In patients with reduced BCC (for example, receiving treatment with high doses of diuretics), symptomatic arterial hypotension may occur at the beginning of treatment with Losartan. Correction of such conditions must be carried out before the appointment of the drug Losartan or start treatment with a lower dose of the drug Losartan (see section "Dosage and Administration").
Impaired fluid and electrolyte balance is characteristic of patients with renal failure with or without diabetes mellitus, therefore careful monitoring of these patients is necessary.
Simultaneous use with potassium preparations, potassium-sparing diuretics is not recommended (see the section "Interaction with other medicinal products"). Caution should be exercised when using Losartan in patients with aortic stenosis, mitral stenosis, and hypertrophic obstructive cardiomyopathy.
Like all drugs with a vasodilating effect, the drug Losartan should be prescribed with caution to patients with coronary heart disease or cerebrovascular diseases, since an excessive decrease in blood pressure in this group of patients can lead to the development of myocardial infarction or stroke.
As with the use of other drugs that have an effect on the RAAS, in patients with CHF and with or without impaired renal function, there is a risk of severe arterial hypotension or acute renal failure.
There is insufficient experience with the use of Losartan in patients with heart failure and concomitant severe renal failure, in patients with severe heart failure (NYHA functional class IV), as well as in patients with heart failure and symptomatic life-threatening arrhythmias. Therefore, the drug Losartan should be prescribed with caution to patients of these groups.
In patients with primary hyperaldosteronism, as a rule, there is no positive response to therapy with antihypertensive drugs that act by inhibiting the RAAS, therefore, the use of Losartan is not recommended in this group of patients.
In patients with cirrhosis of the liver, the concentration of losartan in the blood plasma significantly increases, therefore, patients with a history of liver disease should be prescribed the drug Losartan in lower doses.
There is no experience with the use of the drug Losartan in patients with severely impaired liver function, therefore, the drug should not be used in this group of patients (see the sections "Pharmacological properties", Pharmacokinetics; "Contraindications"; "Dosage and administration").
Drugs that affect the RAAS can increase the concentration of urea in the blood and serum creatinine in patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney.
The experience of using the drug Losartan in patients who underwent kidney transplantation is absent.
It should be borne in mind that ARA II, including losartan, are less effective for the treatment of hypertension when used in patients of the Negroid race than in other patients.

Influence on the ability to drive vehicles, mechanisms

There were no special studies to assess the effect of the drug on the ability to drive vehicles and mechanisms. It should be borne in mind the possibility of drowsiness and dizziness, therefore, care must be taken when performing work that requires increased attention, especially at the beginning of treatment, when increasing the dose of the drug and when driving.

Release form

Film-coated tablets, 12, 5 mg, 25 mg, 50 mg and 100 mg.
10 tablets per PVC-PE-PVDC / aluminum foil blister.
1, 3, 6, 9 blisters of 10 tablets, together with instructions for use, are placed in a cardboard box.
Blisters "in bulk": 100 or 200 blisters of 10 tablets in a cardboard box. Cardboard boxes are placed in a shipping box.

Storage conditions

At a temperature not higher than 25 ° C.
Keep out of the reach of children.

Shelf life

2 years.
Do not use after the expiration date.

Vacation conditions

They let go but the prescription.

A legal entity in whose name the registration certificate was issued:

LLC "Pharmacist", Russia
Address:

Manufacturer, production site address

Produced by:
"Life Pharma FZE", UAE

Packed:
LLC "Pharmacist", Russia
344092, Rostov-on-Don, Kosmonavtov prospect, 2/2

Issuing quality control:
"Life Pharma FZE", UAE
Jebel Ali Free Trade Zone, PO Box 17404, Dubai, United Arab Emirates
Jebel Ali Free Zone, R.O. Box 17404, Dubai, United Arab Emirates

LLC "Pharmacist", Russia
344092, Rostov-on-Don, Kosmonavtov prospect, 2/2

Consumer claims should be sent to:

LLC "Pharmacist", Russia
344092, Rostov-on-Don, Kosmonavtov prospect, 2/2

A synthetic antihypertensive drug is Losartan. Instructions for use indicate at what pressure tablets 12.5 mg, 25 mg, 50 mg and 100 mg Teva, Richter, N with a diuretic effect should be taken. Feedback from patients and recommendations of doctors report that this drug helps in the treatment of arterial hypertension and lowering pressure.

Release form and composition

Losartan is produced in the form of film-coated tablets: round, biconvex. Dosage 12.5 and 25 mg - white with a grayish tinge or white, 50 mg - pink, 100 mg - yellow (in blisters). Active ingredient: potassium losartan - 12.5 mg, 25 mg, 50 mg or 100 mg.

pharmachologic effect

The drug Losartan selectively blocks only the first type of angiotensin receptors. Thus, it has a hypotensive effect on the cardiovascular system and reduces blood pressure. One of the characteristic features of Losartan is the long duration of its exposure.

When taken orally, this drug works throughout the day. The active ingredient of the drug is potassium losartan, a white crystalline powder that dissolves well in ethanol.

Indications for use

What does Losartan help from? Tablets are prescribed if the patient has:

• the risk of developing diseases of the cardiovascular system, in particular stroke;
• chronic heart failure (a pathological condition in which the activity of the cardiovascular system does not provide the body with oxygen, first during physical activity, and then at rest);
• diabetic nephropathy (a term that combines a complex of lesions of the arteries, arterioles, tubules and glomeruli of the kidneys, which develop as a result of metabolic disorders in the kidney tissues);
• arterial hypertension (the state of the body with an increase in blood pressure over 140 mm Hg).

Instructions for use (at what pressure)

Losartan is taken orally, regardless of food intake, at a pressure of over 140 mm Hg. Art. The tablets are swallowed without chewing with water. The frequency of admission is 1 time per day.

Arterial hypertension

With arterial hypertension, the average daily dose is 50 mg once a day. To achieve a greater therapeutic effect, the dose is increased to 100 mg per day. Chronic heart failure The starting dose for patients with chronic heart failure is 12.5 mg once a day.

As a rule, the dose is increased at weekly intervals (i.e. 12.5 mg per day, 25 mg per day and 50 mg per day) to an average maintenance dose of 50 mg once a day, depending on the patient's tolerance to the drug. No dose adjustment is required in elderly patients.

Reducing the risk of development, cardiovascular diseases (including stroke) and mortality in patients with arterial hypertension and left ventricular hypertrophy The initial dose of the drug is 50 mg once a day. In the future, hydrochlorothiazide can be added in low doses or the dose of Losartan can be increased to 100 mg in 1 or 2 doses, taking into account the decrease in blood pressure.

For patients with concomitant type 2 diabetes mellitus with proteinuria, the drug is prescribed in an initial dose of 50 mg 1 time per day with a further increase in the dose to 100 mg per day (taking into account the degree of blood pressure reduction) in one or two doses.

In patients with reduced BCC (for example, when taking diuretics in high doses), the recommended initial dose of Losartan is 25 mg once a day.

Patients with hepatic impairment (less than 9 points on the Child-Pugh scale), during the hemodialysis procedure, as well as patients over 75 years old, are recommended a lower initial dose of the drug - 25 mg 1 time per day. There is not enough experience in the use of the drug in patients with severe hepatic insufficiency, therefore the drug is not recommended in this category of patients.

The drug has no peculiarities of action at the first admission or at its cancellation, but blood pressure control is necessary as when taking any antihypertensive drug. Taking antihypertensive drugs should be carried out at the same set time on the recommendation of a doctor to increase the therapeutic effect.

If you skip taking one dose, you must take the next dose of the drug at the time closest to the time of the usual intake of the drug or at the time when you remembered that you missed the dose by moving the time of taking the next dose. Do not take a double dose of the drug.

Contraindications

Absolute:

Hypersensitivity to drug components.

• Refractory hyperkalemia.
• Lactase deficiency, lactose intolerance and glucose-galactose malabsorption syndrome.
• Dehydration.
• Pregnancy and lactation.
• Age under 18.
• Simultaneous use with aliskiren in patients with diabetes mellitus and / or with functional impairment of the kidneys (at a glomerular filtration rate of less than 60 ml per minute).
• Severe hepatic impairment (due to lack of experience in use).

Relative (diseases / conditions in which Losartan must be used with caution):

• Arterial hypotension.
• Primary aldosteronism.
• Heart failure accompanied by life-threatening arrhythmias.
• Obstructive hypertrophic cardiomyopathy.
• Heart failure accompanied by severe renal failure.
• Decreased volume of circulating blood.
• Liver failure (less than 9 points according to Child-Pugh).
• Severe heart failure (NYHA functional class IV), history of angioedema.
• Stenosis of an artery of a single kidney or bilateral stenosis of the renal arteries.
• Hyperkalemia.
• Cerebrovascular diseases.
• Renal failure
• Coronary artery disease.
• Mitral and aortic stenosis.
• Conditions after kidney transplantation.
• Water and electrolyte imbalance.

Side effects

Side effects are common:

• dizziness;
• difficulty breathing;
• confusion of thoughts;
• numbness or tingling in the hands, feet, lips;
• state of anxiety;
• pain in the abdomen or stomach;
• unstable breathing during exertion;
• nausea or vomiting;
• bloody blotches in the urine;
• coma;
• blurred vision;
• headache;
• cold sweat;
• irregular heartbeat;
• frequent urge to urinate;
• depression;
• chills;
• painful urination;
• pallor of the skin;
• heart palpitations;
• pain in the bladder;
• increased hunger;
• pain in various parts of the body;
• convulsions;
• feeling tired or weak;
• suddenly and for no reason hematomas;
• heaviness in the legs;
• slurred speech.

Less commonly, when taking Losartan, the following negative reactions occur:

• swelling of the face;
• unsteadiness or awkwardness;
• chest pain or discomfort;
• temporary blindness;
• sweating;
• malaise;
• pain or discomfort in the neck area;
• increased heart rate;
• inability to speak;
• chest tightness or heaviness.

Children, during pregnancy and breastfeeding

The drug is contraindicated during pregnancy and lactation. Since adequate studies of the effect of Losartan on children's health have not been conducted, it is prohibited to use it for the treatment of underage patients.

special instructions

In rare cases, with the use of Losartan, disorders develop in the form of anaphylactic reactions, angioedema with involvement of the pharynx and larynx, causing airway obstruction, and / or edema of the face, lips, tongue and / or pharynx. Therefore, if there is an indication of a history of angioedema, the drug should be taken with extreme caution.

In patients with a reduced volume of circulating blood (for example, receiving high doses of diuretics), symptomatic arterial hypotension may develop. Correction of these conditions should be carried out before the appointment of Losartan or therapy should be started with taking lower doses.

Violations of water and electrolyte balance are characteristic of patients with renal failure with or without type 2 diabetes mellitus. When prescribing Losartan in this category of patients, special care must be taken because of the risk of developing hyperkalemia.

During therapy, it is necessary to regularly monitor the content of potassium in the blood, especially in elderly patients and with functional disorders of the kidneys. Potassium supplements or salt substitutes containing potassium should not be taken without first consulting your doctor.

If there is an indication of a history of liver disease, Losartan should be taken in lower doses, which is associated with an increase in the concentration of the drug in the blood plasma.

Drug interactions

With simultaneous use with diuretics in high doses, arterial hypotension is possible. When used together with potassium-sparing diuretics and potassium preparations, the risk of hyperkalemia increases. When combined with indomethacin, there is a risk of reducing the effectiveness of losartan.

When used simultaneously with orlistat, the antihypertensive effect of losartan decreases. This can lead to the development of a hypertensive crisis, a significant increase in blood pressure. There is a report on the development of lithium intoxication with simultaneous use with lithium carbonate. With simultaneous use with rifampicin, the clearance of losartan increases and its effectiveness decreases.

Analogues of the drug Losartan

Analogs are determined by structure:

1. Blockchain.
2. Lotor.
3. Lakea.
4. Vero Losartan.
5. Vasotens.
6. Zisakar.
7. Lozarel.
8. Losacor.
9. Brozaar.
10. Cardomin Sanovel.
11. Lozap.
12. Karzartan.
13. Presartan.
14. Losartan MacLeods.
15. Losartan Richter.
16. Kozaar.
17. Losartan Teva.
18. Renicard.

Vacation conditions and price

The average cost of Losartan (50 mg tablets No. 30) in Moscow is 112 rubles. Dispensed by prescription.

Store in a dark place, out of reach of children, at temperatures up to 25 C. Shelf life - 3 years.

Also find out at what pressure a close analog can be taken.

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Losartan is one of the best-selling blood pressure medications in the world. The reason for this popularity is the long duration of action and the high safety profile of this drug. The action of Losartan lasts 24 hours, so 1 dose per day is enough.

Compared with other antihypertensive pills, this drug causes side effects at times less often. That is why it is characterized by high adherence to treatment: once having tried Losartan, 92% of patients opt for it.

Who is the drug assigned to?

Deaths from strokes and heart disease ranks first in the structure of deaths among adults worldwide. These diseases are expected to become the main cause of disability in the near future. In Europe, it was possible to reverse this trend, the number of deaths due to cardiovascular diseases (CVD) is slowly but surely declining. Scientists have calculated that the main role in this success belongs not to high-tech methods of treatment, but to simple measures to prevent risk factors for CVD.

The most significant factors are:

• high blood pressure;
• excess cholesterol and triglycerides in blood vessels;
• diabetes;
• obesity.

If the pressure is higher than normal, the risk of death from CVD is about 1%, if high blood pressure is accompanied by another factor - 1.6%, another 2 factors - 3.8%. The task of the doctor in identifying risk factors is to minimize their effect on the body: to reduce blood pressure to target values, to correct the lipid profile and blood glucose, and to normalize weight.

Losartan has a pronounced hypotensive effect, the dose of the drug is selected depending on the initial and target pressure.

The medicine is prescribed in the following cases:

Indications for the use of the drug Lazortan	Purpose of application
Hypertension, including those complicated by left ventricular hypertrophy.	The appointment of the drug should ensure a constant decrease in pressure in adults to 130/85, in the elderly - to 140/90.
Hypertension combined with diabetes.	Patients have a high risk of renal failure, so they try to lower the pressure more, to 130/80 for all ages.
Renal failure	Normalization of pressure slows down the destruction of the kidneys, reduces protein in the urine. The target level is 125/75.
Heart failure.	Pressure pills are prescribed as part of a comprehensive treatment, usually the choice is stopped on ACE inhibitors. Losartan is used if they are contraindicated or do not give the desired effect.

If you choose the right dose and take Losartan without gaps, you can reach the target pressure level in 50% of patients. The rest are recommended combination therapy: another antihypertensive agent is added to the treatment regimen. Modern drugs provide pressure normalization in more than 90% of patients.

The statistics of taking antihypertensive drugs in Russia is depressing: among people with hypertension, about 70% of city dwellers and 45% of village residents know about the disease. Only 23% are treated in a disciplined manner and the pressure is maintained at a normal level.

How does Losartan medicine work?

The first discoveries, which ultimately led to the creation of Losartan, were made at the end of the 19th century. The enzyme renin has been isolated from kidney cells, which is an important part of blood pressure regulation. Several decades later, a substance was discovered in the renal artery that has a powerful effect on the vessels, leading to their narrowing. It was named angiotensin. The last link in the system was discovered in the middle of the 20th century. It was the hormone aldosterone, which is synthesized by the adrenal glands. This turned out to be enough to understand how the vascular tone is maintained in the body and hypertension is prevented.

To put it simply, the following mechanism works in our body: when the pressure drops in the kidneys, renin is formed, which affects angiotensin. Angiotensin is decomposed to angiotensin I, which is an inactive peptide, and then, with the participation of an ACE enzyme, it is converted to angiotensin II. The resulting substance is a strong vasoconstrictor, causes a rapid rise in pressure and stimulates the production of aldosterone, which is responsible for water-salt metabolism.

Losartan was created in the 90s of the last century. It turned out to be the first drug in a fundamentally new group of drugs for pressure, which was called angiotensin II receptor blockers, or ARBs for short. Now there are 6 drugs in this group. All of them, except for Losartan, end in -sartan, therefore they are also called sartans.

The action of Losartan is based on blocking the action of angiotensin II, while the substance does not in any way affect other types of regulation of the work of blood vessels and the heart.

What this medicine helps with:

1. The main action is hypotensive. The medicine begins to reduce the pressure after about an hour, reaching its maximum effect after 6 hours. The total working time is 1 day. Losartan is always prescribed for a long time, since it begins to provide a stable decrease in pressure only after 1-1.5 months.
2. Suppression of the pressure regulation system prevents the progression of heart failure. ACE inhibitors work a little more effectively in this case, but Losartan is better tolerated.
3. Protects the kidney nephrons from destruction, slows down the development of renal failure, postpones the need for hemodialysis patients. Losartan reduces the excretion of protein in the urine by 35%, the probability of complete kidney failure - by 28%.
4. Protects the brain in case of hypertension: reduces the risk of stroke, improves memory. Scientists believe that this action is associated not only with a decrease in pressure, but also with other, not yet studied effects of the drug.
5. It leads to an improvement in the condition of connective tissues: it strengthens the walls of blood vessels, promotes muscle recovery. It is believed that the additional effect of Losartan is “to blame” for this - stimulation of collagen production.
6. Promotes the elimination of excess uric acid, therefore it is especially recommended for lowering blood pressure in patients with gout.

Dosage of Losartan tablets

The active ingredient in Losartan is potassium losartan. The original drug is the American Cozaar of the Merck company. Medicines called Losartan are generics. They contain the same active ingredient and have the same dosages as the original Cozaar.

The following analogues are registered in Russia:

Analogs	A country	Manufacturer	Dosage options, mg				How much does Losartan cost, (rubles for 30 tablets, 50 mg each)
			12,5	25	50	100
Lozaratan	Russia	Tathimpreparat	+	—	+	—	70-140
		Nanolek	—	—	+	+
		Pranapharm	+	+	+	+
		Biocom	+	+	+	—
		Atoll	+	—	+	+
Losartan-Canon		Canonpharm	—	—	+	+	110
Losartan-Vertex		Vertex	+	+	+	+	150
Losartan-TAD	Germany	TAD-Pharma	+	+	+	+	—
Losartan-Teva	Israel	Teva	—	+	+	+	175
Losartan-Richter	Hungary	Gedeon Richter	—	—	+	+	171

Dosages of Losartan tablets:

• 12.5 mg can be used if Losartan is prescribed with other antihypertensive drugs.
• 25 mg is the standard dose for diuretics.
• 50 mg - according to the instructions, this dose allows you to normalize blood pressure in most patients, it is prescribed most often.
• 100 mg is taken if a high pressure reduction is required.

There are also combination tablets that contain 2 substances with an antihypertensive effect at once: losartan potassium and the diuretic hydrochlorothiazide. Under the name Losartan N they are produced by Kanonfarma, Atoll and Gedeon Richter. The price of Losartan N is 160-430 rubles.

How to take it right

Rules for taking Losartan from the instructions for use:

1. The drug is drunk 1 time a day, but for convenience, the pill can be divided into 2 doses.
2. The instruction states that it does not matter when to take this drug, in the morning or in the evening. Losartan works for at least 24 hours. The main thing is not to change the once set reception time. Patient reviews suggest that the morning reception is still preferable. In this case, the peak of the effectiveness of Losartan falls on the most active daytime.
3. Eating food does not significantly affect the absorption and work of Losartan, so it can be taken before or after meals.
4. The starting daily dosage for most patients is 50 mg. It can be increased not earlier than after a week of taking the medicine.
5. In case of heart failure, the intake begins with 12.5 mg, gradually increasing the dose to 50 mg.
6. In liver failure, severe renal failure, in patients over 75 years of age, the initial dose is 25 mg.
7. The maximum daily dose is 100 mg; in the presence of heart failure, it can be increased by a doctor to 150 mg.

If 1 tablet of Losartan 100 mg is not enough to normalize blood pressure, it can be combined with antihypertensive drugs from other groups.

At what pressure do doctors recommend starting treatment with Losartan? As a rule, from level 140/90. This level is already considered to be elevated and negatively affects the state of blood vessels and the work of the heart, kidneys, and brain. With constantly increased pressure or its repeated jumps, a constant intake of Losartan is prescribed. Hypertension is a chronic disease, so the medicine is drunk even if it seems that the pressure has returned to normal. In addition to pills, effective ways to combat hypertension are weight loss, high activity, quitting smoking, limiting alcohol, increasing vegetable consumption and reducing salt, avoiding stressful situations.

Possible side effects

The side effects of Losartan are mild, usually go away on their own, treatment cancellation is not required. The drug has successfully passed several placebo-controlled studies, during which it was found that the overall frequency of unwanted symptoms occurring when taking Losartan is even slightly lower than in the placebo group (2.3 versus 3.7%).

According to reviews of hypertensive patients, undesirable effects occur extremely rarely; it is possible to track the relationship between taking pills and deterioration of well-being in isolated cases. As a rule, side effects are transient. Patients noted fog in the head, dizziness, dry mouth at the beginning of the intake. By the end of 1 month, these phenomena disappear.

Data from the instructions on side effects that occur in more than 1% (according to the WHO classification are considered frequent) of patients taking Losartan:

Adverse events	Appearance rate,%
	when taking a placebo	when treated with Losartan
Headache	17,2	14,1
ARVI	5,6	6,5
Weakness	3,9	3,8
Nausea	2,8	1,8
Chest pain	2,6	1,1
Cough	2,6	3,1
Pharyngitis	2,6	1,5
Dizziness	2,4	4,1
Swelling of the legs, face	1,9	1,7
Loose stools	1,9	1,9
Increased heart rate	1,7	1
Abdominal pain	1,7	1,7
Flatulence	1,5	1,1
Sinusitis	1,3	1
Muscle pain	1,1	1,6
Muscle spasms	1,1	1
Runny nose	1,1	1,3
Sleep disturbances	0,7	1,1

In 10% of patients with diabetes and impaired renal function, an increase in blood potassium was observed to 5.5 and higher, while the norm was 3.4-5.3. When taking a placebo, such an increase was found in 3.4% of patients. Otherwise, Losartan is well tolerated in this group of patients.

According to the instructions, in heart failure, hyperkalemia was observed in less than 1%, the frequency of undesirable effects increased with an increase in the dose from 50 to 150 mg.

Contraindications for use

Instructions for the use of Losartan contain an exhaustive list of contraindications for taking it:

1. The drug can cause allergic reactions. They occur in less than 1% of hypertensive patients. Anaphylactic reactions are possible, therefore, patients who have previously suffered from angioedema should be especially careful at the beginning of treatment. The risk is highest in people who are allergic to ACE inhibitors.
2. It is forbidden for severe liver failure, since impaired liver function leads to a significant increase in the concentration of losartan potassium in the blood, that is, an overdose. The patient may experience severe hypotension and tachycardia.
3. Losartan and all sartans should not be drunk during pregnancy. According to the FDA classification, this drug belongs to category D. This means that in the course of research it was found and proved its negative effect on the fetus. Perhaps a violation of the kidneys of a child, a slowdown in the growth of the bones of the skull, low water. In the 1st trimester, the use of the drug is less dangerous. The instructions for use contain an indication: if the pregnancy began during the period of taking Losartan, the medicine is urgently canceled. A woman is required to undergo an additional examination in the 2nd trimester - an ultrasound of the fetus to identify possible abnormalities in the development of the kidneys and skull.
4. Losartan is prohibited for HS, as it is not known whether it passes into milk.
5. Losartan tablets cannot be used in children due to the lack of data on its safety for a developing organism.
6. Losartan contains lactose (or cellactose), so the medicine should not be taken if its absorption is disturbed.
7. Due to drug interactions, it is forbidden to drink Losartan with aliskiren (Rixil, Rasilez, Rasilam pressure medications) in patients with a high risk of renal failure: diabetes mellitus and kidney disease.

The following conditions are not strict contraindications for treatment with Losartan, but require special attention to their health: kidney disease, hyperkalemia, heart failure, any disturbances in the blood supply to the brain, excessive production of aldosterone.

Since Losartan does not interact with ethanol, the instructions do not describe the compatibility of alcohol with the drug. However, doctors strictly prohibit taking alcoholic beverages during treatment with any pressure pills. Ethanol worsens the state of blood vessels, promotes the development of hypertension and thereby completely neutralizes the therapeutic effect of Losartan.

Analogues and substitutes

At the moment, more than a dozen Kozaar analogues have been registered in Russia alone, and there are many more of them in the world. In most pharmacies, you can buy 2 versions of Cozaar:

• a pack of 14 tablets of 50 mg each costs about 110 rubles,
• package for 28 tablets, 100 mg each - 185 rubles.

Generic drugs from the largest pharmaceutical companies cost no less, and sometimes a little more than the original. But they can be bought at the nearest pharmacy, and it is possible to choose the desired dosage.

You can replace Losartan with the following drugs:

Lozartan substitutes	Manufacturer	Dosages, mg					Price (rubles for 50 mg, 30 tab.)
		12,5	25	50	100	150
Kozaar	Merck	—	—	+	+	—	220 (price 28 tab.)
Lorista	Krka	+	+	+	+	+	195
Blocktran	Pharmstandard	+	—	+	—	—	175
Lozap	Zentiva	+	—	+	+	—	265
Lozarel	Lek	—	—	+	—	—	210
Vasotenz	Actavis	+	+	+	+	—	270
Presartan	Ipka	—	+	+	+	—	135

Analogues may slightly differ from the original in terms of absorption rate and strength of action, so doctors recommend choosing those generics that have passed their own clinical trials. For example, Lozap and Lorista have a proven hypotensive effect for 24 hours, a uniform effect throughout the entire duration of the action, and a low level of side effects. Reviews of patients confirm the opinion of doctors. Lozartan tablets from Vertex and Ozon (Atoll), Lorista and Lozap have the highest rating.

Studies involving various groups of antihypertensive drugs have not revealed any significant benefits for any of the drugs. This means that all modern drugs are equally effective in reducing blood pressure and CVD risk. Naturally, provided that the dose is correctly selected, and the pills are taken constantly, without gaps. The main differences between pressure drugs are in their tolerance and the strength of side effects, it is according to these criteria that the necessary medicine is selected.

Lozaratan and its analogs are very well tolerated:

1. They less often than others lead to an excessive decrease in pressure, less often they cause collaptoid states in patients.
2. Unlike beta-blockers (propranolol, atenolol, etc.), Losartan analogs do not affect the heart rate, erection, and do not cause bronchospasm with cough.
3. If we compare sartans with their main competitors, ACE inhibitors (captopril, enalapril, ramipril, etc.), it turns out that Losartan causes a cough less often (the instructions for use indicate a frequency of 9.9% for ACE inhibitors, 3.1% for Losartan ), hyperkalemia, Quincke's edema.
4. The action of Losartan does not depend on age, race, sex and hemodynamic parameters.
5. In the reviews of patients who took the drug, there is often a statement that Losartan is weaker than other pressure pills. Research refutes this fact. The fact is that the effect of this drug increases gradually, it gains full strength within 2-5 weeks. After this time, the effectiveness of Losartan is the same as that of other antihypertensive drugs.
6. A review of the data from numerous studies involving Losartan showed that its potency does not differ from ACE inhibitors. They are also close in reducing the incidence of strokes and heart attacks, quality of life, and the effect on the body of patients with nephropathy and diabetes.
7. The long time it takes to achieve the maximum effect is compensated by the persistence of the action of Losartan. With long-term use, the effectiveness of ACE inhibitors and beta-blockers may decrease, and this is much less common with Losartan tablets.
8. In heart failure, the advantage of Losartan and its analogs has not yet been proven; clinical research data do not yet allow a final conclusion. So far, the most effective is the combination of aldosterone antagonists (spironolactone) with beta-blockers. The combination of sartans with ACE inhibitors is in second place.