Universal reference book for medicines
Product name: Lozartan-Richter (LOSARTAN-RICHTER)

Active substance: losartan

Type: Angiotensin II receptor antagonist

Manufacturer: GEDEON RICHTER (Hungary) produced by GEDEON RICHTER-RUS (Russia)
Composition, form of production and packaging
The tablets covered with a film shell of
white or almost white color, round, biconcave, with a risk on one side and engraving "50" - on the other.

1 tab.

Losartan potassium 50 mg

Excipients: silicon dioxide colloid - 0.75 mg, magnesium stearate - 1.5 mg, croscarmellose sodium - 3 mg, pregelatinized starch - 20.2 mg, microcrystalline cellulose - 74.55 mg.

Composition of the film shell: opadray 33G28523 white (triacetin 0.3 mg, macrogol 0.4 mg, lactose monohydrate 1.05 mg, titanium dioxide (CI77891, E171) 1.25 mg, hypromellose 2 mg).

10 pieces.
- blisters (1) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
The tablets covered with a film shell of white or almost white color, oval, biconcave, with engraving "100" on one side and smooth on the other.

1 tab.

Losartan Potassium 100 mg

Excipients: silicon dioxide colloid - 1.5 mg, magnesium stearate - 3 mg, croscarmellose sodium - 6 mg, pregelatinized starch - 40.4 mg, microcrystalline cellulose - 149.1 mg.

The composition of the film shell: opadray 33G28523 white (triacetin - 0.6 mg, macrogol - 0.8 mg, lactose monohydrate - 2.1 mg, titanium dioxide (CI77891, E171) - 2.5 mg, hypromellose - 4 mg).

10 pieces.
- blisters (1) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2016.

PHARMACHOLOGIC EFFECT

Specific antagonist of angiotensin II receptors (type AT 1 ).
Angiotensin II selectively binds to the AT 1 receptors found in many tissues (in the smooth muscle tissues of the vessels, in the adrenal, kidney and heart) and causes important biological effects, including. vasoconstriction and aldosterone release, as well as proliferation of smooth muscle cells.
In vitro and in vivo studies have shown that losartan and its pharmacologically active metabolite block all physiologically important effects of angiotensin II
regardless of the source or the route of its synthesis.
Does not inhibit kinase II - an enzyme that destroys bradykinin.
Reduces the overall peripheral resistance of blood vessels (OPSS), the concentration in the blood of norepinephrine and aldosterone, blood pressure (BP), pressure in a small circle of blood circulation; reduces afterload, has a diuretic effect. Prevents development of myocardial hypertrophy, increases exercise tolerance in patients with chronic heart failure (CHF).
After a single oral intake, the hypotensive effect (decrease of systolic and diastolic blood pressure) reaches a maximum after 6 hours, then gradually decreases within 24 hours.

The maximum hypotensive effect develops in 3-6 weeks after the start of regular intake of the drug.

Losartan does not inhibit angiotensin-converting enzyme (ACE) and, accordingly, does not interfere with the destruction of bradykinin, therefore, Losartan has no side effects, indirectly associated with bradykinin (eg, angioedema).

In patients with arterial hypertension with proteinuria (more than 2 g / day) without concomitant diabetes, the use of the drug significantly reduces proteinuria, albumin and immunoglobulin G excretion.

Lozartan stabilizes the level of urea in the blood plasma.
Does not affect vegetative reflexes. Losartan in a dose up to 150 mg / day does not affect the level of triglycerides, total cholesterol and high-density lipoprotein cholesterol (HDL) in the blood serum in patients with arterial hypertension. At the same dose, losartan does not affect the fasting blood glucose level.
PHARMACOKINETICS

Suction

When ingested, losartan is well absorbed, metabolized at the "first pass" through the liver by carboxylation with the participation of the cytochrome P450 isoenzyme CYP2C9 with formation of a 10-40 times more active metabolite.
Systemic bioavailability of losartan is about 33%. C max losartan in the blood plasma after ingestion is achieved after 1-1.5 h, C max of its active metabolite - after 3-4 hours. Food intake does not affect the bioavailability of losartan.
Distribution

92% of losartan and 99% of its active metabolite binds to blood plasma proteins, mainly with albumins.
V d losartan - 34 liters. Losartan practically does not penetrate the blood-brain barrier.
Metabolism

Approximately 14% of losartan taken by the patient inside becomes an active metabolite.
In a small number of patients (approximately 1%), a minimum amount of active metabolite is formed from losartan.
Excretion

The plasma clearance of losartan is 600 ml / min, and the active metabolite is 50 ml / min.
The renal clearance of losartan and its active metabolite is 74 ml / min and 26 ml / min, respectively. Losartan and its active metabolite is characterized by linear pharmacokinetics when administered in doses up to 200 mg.
After oral administration, the plasma concentrations of losartan and its active metabolite decrease polyexponentially with a finite T 1/2 of losartan for about 2 hours and an active metabolite about 6-9 hours. When taking the drug at a dose of 100 mg / day, neither losartan nor the active metabolite significantly cumulate in the blood plasma.

Losartan and its metabolites are excreted through the intestine and the kidneys.
The kidneys excreted 35% (of which 4% - unchanged and 6% - in the form of an active metabolite), the rest (60%) through the intestine.
In healthy volunteers after ingestion of 14 With isotope labeled losartan, a radioactive label was found in urine in an amount of about 35%, in feces - about 58%.

Pharmacokinetics in specific patient groups

In patients with alcoholic liver cirrhosis of mild and moderate severity, the concentration of losartan was 5 times, and the active metabolite was 1.7 times higher than in healthy male volunteers.

With CC above 10 ml / min, the concentration of losartan in the blood plasma does not differ from that with normal kidney function.
In patients who need hemodialysis, the AUC value is approximately 2 times higher than in patients with normal renal function.
Neither losartan nor its active metabolite is removed from the body by hemodialysis.

The concentrations of losartan and its active metabolite in blood plasma in elderly men with arterial hypertension do not differ significantly from the values ​​of these parameters in young men with arterial hypertension.

Values ​​of plasma concentrations of losartan in women with arterial hypertension are 2 times higher than the corresponding values ​​in men with hypertension.
This pharmacokinetic difference is not clinically relevant. The concentration of the active metabolite in men and women does not differ.
INDICATIONS

- arterial hypertension;

- Chronic heart failure (with ineffective therapy with ACE inhibitors);

- Type 2 diabetes mellitus with proteinuria (reduced risk of hypercreatininemia and proteinuria);

- reduction in the risk of developing cardiovascular disease and mortality in patients with hypertension and left ventricular hypertrophy.

DOSING MODE

Inside, 1 time / day, regardless of food intake.

Arterial hypertension

In most cases, the initial and maintenance dose is 50 mg 1 time / day.
The maximum antihypertensive effect is achieved in 3-6 weeks after the start of the drug. If necessary, the dose of the drug can be increased to 100 mg / day (in 1 or 2 doses)
Against the background of taking large doses of diuretics, it is recommended to start therapy with a drug with 25 mg / day (1/2 tablespoons of 50 mg) in 1 dose.

It is not necessary to adjust the dose to elderly patients or patients with impaired renal function, incl.
patients on hemodialysis.
Chronic heart failure (with ineffective therapy with ACE inhibitors)

The initial dose of the drug is 50 mg 1 time / day.
In the future, hydrochlorothiazide can be added at low doses and / or the dose of Lozartan-Richter can be increased to 100 mg / day.
Kidney protection in patients with type 2 diabetes mellitus with proteinuria

The initial dose is 50 mg 1 time / day.
In the course of treatment, depending on the indices of arterial pressure, one can increase the daily dose of the drug to 100 mg / day in 1 or 2 doses.
Chronic heart failure

For the treatment of chronic heart failure, the initial dose of the drug is 12.5 mg 1 time / day (Lozartan-Richter may be used in another dosage form - tablets of 12.5 mg).

In order to achieve a normal maintenance dose of 50 mg / day, the dose of the drug should be increased gradually, at intervals of 1 week (for example, 12.5 mg, 25 mg, 50 mg with a single dose per day).
Losartan-Richter is usually prescribed in combination with diuretics and cardiac glycosides.
The dose of the drug should be increased according to the following scheme:

1st week: from the 1st to the 7th day - 1 tablet 12.5 mg 1 time / day.

2nd week: from the 8th to the 14th day - 1/2 tablet 50 mg 1 time / day.

3rd week: from the 15th to the 21st day - 1 tablet 50 mg 1 time / day.

4th week: from the 22nd to the 28th day - 1 tablet 50 mg 1 time / day.

SIDE EFFECT

The side effects of Losartan-Richter are usually transient and do not require withdrawal of the drug.

In the use of the drug for the treatment of essential hypertension in controlled trials, only the incidence of dizziness differed from placebo by more than 1% (4.1% vs. 2.4%) among the side effects.

The dose-dependent orthostatic effect, characteristic of antihypertensive agents, was observed in less than 1% of patients with Lozartan-Richter application.

The side effects observed with the use of the drug are classified into categories according to the frequency of their occurrence: very often? 1/10, often> 1/100 or?
1/10, sometimes? 1/1000 or? 1/100, rarely? 1/10000 or? 1/1000, very rarely? 1/10000, including individual messages.
Side effects, occurring with a frequency of more than 1%:

Losartan (n = 2085) Placebo (n = 535)

General symptoms

asthenia / fatigue 3.8 3.9

pain in the chest 1.1 2.6

peripheral edema 1.7 1.9

The cardiovascular system

heart beat 1.0 0.4

tachycardia 1.0 0.7

Digestive system

abdominal pain 1.7 1.7

diarrhea 1.9 1.9

dyspeptic phenomena 1.1 1.5

nausea 1.8 2.8

Musculoskeletal system

back pain 1.6 1.1

muscle spasm

Nervous System / CNS

Vertigo 4.1 2.4

headache 14.1 17.2

insomnia 1.1 0.7

Respiratory system

cough 3.1 2.6

nasal congestion 1.3 1.1

pharyngitis 1.5 2.6

Sinusitis 1.0 1.3

upper respiratory infections 6.5 5.6

Side effects, occurring with a frequency of less than 1%

On the part of the cardiovascular system : orthostatic hypotension (dose-dependent), epistaxis, palpitations, tachy- and bradycardia, arrhythmias, angina pectoris, vasculitis.

On the part of the digestive system : a decrease in appetite, dry mouth, toothache, vomiting, flatulence, gastritis, constipation, hepatitis, a violation of liver function, very rarely - a moderate increase in the activity of "liver" transaminases, hyperbilirubinemia.

Dermatological reactions: dry skin, erythema, photosensitization, increased sweating, alopecia.

Allergic reactions : urticaria, rash, itching, angioedema (including swelling of the larynx and tongue, causing airway obstruction and / or swelling of the face, lips, throat).
In some patients, there was an indication in the anamnesis of the transferred angioedema while taking other medications, including. ACE inhibitors.
On the part of the hematopoiesis system : anemia (a slight decrease in the concentration of hemoglobin and hematocrit, an average of 0.11 g% and 0.09 volume%, respectively, rarely having clinical significance), thrombocytopenia, eosinophilia, purpura Shenlaine-Genocha.

From the musculoskeletal system : arthralgia, arthritis, shoulder pain, knee joint, fibromyalgia.

From the side of the central nervous system and sensory organs : anxiety, sleep disturbance, drowsiness, memory disorders, peripheral neuropathy, paresthesia, hypesthesia, tremor, ataxia, depression, syncopal conditions, ringing in the ears, taste disorder, visual impairment, conjunctivitis, migraine.

From the respiratory system : dyspnoea, bronchitis, edema of the nasal mucosa.

From the urinary system : mandatory urination, urinary tract infections, impaired renal function.

From the side of water-electrolyte balance : often - hyperkalemia (the level of potassium in the blood plasma is more than 5.5 mmol / l).

From the side of metabolism : infrequently - increased levels of urea and residual nitrogen or creatinine in the blood serum.

Other : gout, decreased libido, decreased potency.

CONTRAINDICATIONS

- pregnancy and the period of breastfeeding;

- age under 18 years (effectiveness and safety not established);

lactose intolerance;

- galactosemia;

- syndrome of impaired glucose / galactose absorption;

- Hypersensitivity to the components of the drug.

With caution : arterial hypotension, disturbance of water-electrolyte balance, decrease in the volume of circulating blood, hepatic and / or renal failure (including bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney).

PREGNANCY AND LACTATION

There are no data on the use of losartan in pregnancy.
Perfusion of kidneys in the fetus, which depends on the activity of the renin-angiotensin system, begins to function in the third trimester of pregnancy. The risk to the fetus increases with the use of losartan in the II and III trimesters of pregnancy. When pregnancy is established, losartan should be discontinued immediately.
There is no data on the isolation of losartan with breast milk.
Therefore, when prescribing losartan therapy, the question of abolishing breastfeeding should be addressed.
APPLICATION FOR FUNCTIONS OF THE LIVER

With caution appoint patients with renal failure (including with bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney).

With CC above 10 ml / min, the concentration of losartan in the blood plasma does not differ from that with normal kidney function.
In patients who need hemodialysis, the AUC value is approximately 2 times higher than in patients with normal renal function.
Neither losartan nor its active metabolite is removed from the body by hemodialysis.

Due to the suppression of the renin-angiotensin system, the drug may worsen the function of the kidneys, especially patients whose functional renal state is heavily dependent on the renin-angiotensin-aldosterone system, for example, in the presence of severe CHF or previously present renal dysfunction.

Drugs that affect the renin-angiotensin-aldosterone system can increase the level of residual nitrogen or creatinine in the blood plasma in patients with bilateral renal artery stenosis or stenosis of the artery of a single kidney.

These changes in kidney function may disappear after discontinuation of therapy with the drug.

During treatment with Lozartan-Richter, special attention should be paid to patients who have severe renal failure and to patients after kidney transplantation, as these patients had anemia



APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Be wary appoint patients with hepatic insufficiency.

In patients with alcoholic liver cirrhosis of mild and moderate severity, the concentration of losartan was 5 times, and the active metabolite was 1.7 times higher than in healthy male volunteers.
Therefore, patients with a history of liver disease should be prescribed a drug in a lower dose.
APPLICATION FOR CHILDREN

Contraindicated in children under the age of 18 years (there is insufficient data on efficacy and safety).

APPLICATION IN ELDERLY PATIENTS

The concentrations of losartan and its active metabolite in blood plasma in elderly men with arterial hypertension do not differ significantly from the values ​​of these parameters in young men with arterial hypertension.
It is not necessary to adjust the dose to elderly patients.
During treatment with the drug Lozartan-Richter should monitor the potassium level in the blood serum, especially in elderly patients.

SPECIAL INSTRUCTIONS

Hypersensitivity reactions

There may be an angioedema.

Arterial hypotension and disturbance of water-electrolyte balance

In the presence of hypovolemia (for example, when therapy with large doses of diuretics), symptomatic arterial hypotension may develop.
This condition must be corrected before starting a course of therapy with Lozartan-Richter or starting therapy with a lower dose.
With kidney disease with or without diabetes mellitus, violations of the water-electrolyte balance are often encountered, which must be corrected.
In clinical studies conducted with patients with type 2 diabetes mellitus with proteinuria, the frequency of occurrence of hyperkalemia increased with Lozartan-Richter therapy compared with placebo. However, the level of hyperkalemia only in a small number of cases required the discontinuation of the drug.
Impaired liver function

According to pharmacokinetic studies, the concentration of losartan in the blood plasma increases significantly with cirrhosis of the liver, so patients with a history of liver disease should be prescribed a drug in a lower dose.

Impaired renal function

Due to the inhibition of the renin-angiotensin system, the drug may worsen renal function, especially in patients whose functional renal state is heavily dependent on RAAS, for example, in the presence of severe CHF or previously present renal dysfunction.

Drugs that affect RAAS can increase the level of residual nitrogen or creatinine in the blood plasma in patients with bilateral renal artery stenosis or stenosis of the artery of a single kidney.

These changes in kidney function may disappear after discontinuation of therapy with the drug.

During treatment with Lozartan-Richter, special attention should be given to patients with severe renal failure and to patients after kidney transplantation, as these patients had anemia.

Hyperkalemia and violation of water-salt balance

During treatment with the drug Lozartan-Richter should monitor the potassium level in the blood serum, especially in elderly patients.

Lactose intolerance

When lactose intolerance should be taken into account that the Losartan-Richter 50 mg tablet contains 1.050 mg of lactose, a tablet of 100 mg to 2.10 mg of lactose.

Influence on ability to drive and other mechanisms

Data on the impact of Losartan-Richter on the ability to drive vehicles and other mechanisms are not provided.

OVERDOSE

Symptoms: marked decrease in blood pressure, tachycardia;
As a result of parasympathetic (vagal) stimulation, a bradycardia can develop.
Treatment: conduct symptomatic therapy, forced diuresis.
Hemodialysis is ineffective.
DRUG INTERACTION

There were no pharmacokinetic interactions of Losartan-Richter with hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole and erythromycin.

According to reports, rifampicin and fluconazole reduce the level of the active metabolite in the blood plasma.
The clinical significance of these interactions is still unknown.
As with the use of other agents that inhibit angiotensin II or its effect, the combined use of Lozartan-Richter with potassium-sparing diuretics (eg, spironolactone, triamterene, amiloride), potassium and potassium-containing preparations increases the risk of hyperkalemia.

Nonsteroidal anti-inflammatory drugs (NSAIDs), incl.
selective inhibitors of cyclooxygenase-2 (COX-2), acetylsalicylic acid at a dose of more than 3 g / day, may reduce the effectiveness of angiotensin II receptor antagonists. The combined use of angiotensin II receptor antagonists with NSAIDs, including selective inhibitors of COX-2 may lead to a decrease of renal function, including acute renal failure and increase in potassium level in blood plasma (especially with decreased kidney function). This effect is usually reversible.
When the joint application of angiotensin II receptor antagonists and drugs lithium may increase the concentration of lithium in the blood plasma. The combined use of Losartan Richter and lithium salts is possible only when the intended use of the potential risk. In the case of their joint application should regularly monitor the level of lithium in blood plasma.
The combined use of Losartan Richter diuretics exerts an additive effect. (Mutually) the effect of other antihypertensive agents (diuretics,? Adrenoblokatorov, simpatolitikov).
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be kept out of the reach of children, dry place at a temperature not higher than 25 ° C. Shelf life 50 mg tablets - 5 years, tablets 100 mg - 3 years.
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