Universal reference book for medicines
Product name: Tevetene ® (TEVETEN ® )

Active substance: eprosartan

Type: Angiotensin II receptor antagonist

Manufacturer: ABBOTT HEALTHCARE PRODUCTS (Netherlands) manufactured by ABBOTT HEALTHCARE (France)
Composition, form of production and packaging
The tablets covered with a film shell of
white color, oval, biconcave, with engraving "5046" on one side;
on a cross-section of a tablet of white color.
1 tab.

eprosartan mesylate 735.8 mg,

which corresponds to the content of eprosartan 600 mg

[PRING] microcrystalline cellulose - 43.3 mg, lactose monohydrate 43.3 mg, pregelatinized starch 43.3 mg, crospovidone 38.5 mg, magnesium stearate 7.2 mg, purified water 50.9 mg.

The composition of the shell: opedrai ® white (OY-S-9603) - 38.5 mg (hypromellose - 23 mg, macrogol - 3.08 mg, polysorbate 80 - 0.39 mg, titanium dioxide dye (E171) - 12.03 mg).

14 pcs.
- blisters (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

Antihypertensive drug, angiotensin II receptor antagonist.

Eprosartan selectively acts on AT 1 -receptors located in the vessels, heart, kidneys and adrenal cortex, forms a strong bond with them, followed by a slow dissociation.

Angiotensin II binds to AT 1 -receptors in many tissues (including in the smooth muscles of blood vessels, adrenal glands, kidneys, heart) and causes vasoconstriction, sodium retention and aldosterone release, target organ damage-myocardial hypertrophy and vessels.

Eprosartan prevents the development or weakening of the effects of angiotensin II.
Inhibits the activity of the renin-angiotensin-aldosterone system (RAAS). Has vasodilating, hypotensive and mediated - diuretic action.
Reduces arterial vasoconstriction, OPSS, pressure in a small circle of circulation, reabsorption of fluid and sodium ions in the proximal segment of the renal tubules, the secretion of aldosterone.
With prolonged use suppresses the proliferative effect of angiotensin II on smooth muscle cells of blood vessels and myocardium.
Hypotensive action after taking a single dose persists for 24 hours, persistent therapeutic effect is manifested with regular admission - in 2-3 weeks without changing the heart rate.

Does not cause the development of orthostatic hypotension in response to taking the first dose of the drug.

In patients with hypertension, eprosartan does not affect the concentration of TG, total cholesterol (Xs), or LDL-cholesterol in the fasting blood.
In addition, eprosartan does not affect the concentration of glucose in the blood on an empty stomach.
Increases renal blood flow and the rate of glomerular filtration, reduces the excretion of albumins (nephroprotective effect), while maintaining renal self-regulation, regardless of the severity of renal failure.

Does not affect the purine metabolism, does not have a significant effect on the excretion of uric acid by the kidneys.

Less often than ACE inhibitors, it causes the appearance of effects associated with bradykinin (including dry persistent cough).

The incidence of dry, persistent cough in patients receiving eprosartan is 1.5%.
When replacing the ACE inhibitor with eprosartan in patients with a cough, the frequency of dry persistent cough is consistent with placebo.
Termination of eprosartan treatment is not accompanied by withdrawal syndrome.

During clinical trials, application of the drug at a daily dose of up to 1200 mg for 8 weeks was effective without an apparent relationship between dose and the incidence of reported adverse events.

Eprosartan does not inhibit the isoenzymes CYP1A, 2A6, 2C9 / 8, 2C19, 2D6, 2E and 3A of the cytochrome P450 system in vitro.

PHARMACOKINETICS

Suction

After oral administration in a single dose of 300 mg, the bioavailability of the drug is 13%.
C max eprosartan in blood plasma is achieved in 1-2 hours.
When taking Eprosartan concomitantly with food, there is a clinically insignificant decrease in absorption (less than 25%), C max in blood plasma and AUC values.

Distribution

The binding to plasma proteins is 98% and has a constant character in the range of therapeutic concentrations.

V d - 13 liters.
Practically does not cumulate.
Excretion

T 1/2 is 5-9 hours. The total clearance is 130 ml / min.

Output is mainly unchanged - through the intestine (90%), kidney (7%).
A small part (less than 2%) is excreted by the kidneys in the form of glucuronides. 20% of the concentration in the urine is acylglucuronide eprosartan, 80% - unchanged eprosartan.
Pharmacokinetics in special clinical cases

The degree of binding to plasma proteins does not depend on sex, age, the presence of violations of liver function and does not change with mild or moderate renal insufficiency, but may decrease with severe renal failure.

In persons under 18 years of age, pharmacokinetics have not been studied.

When Eprosartan is used in patients with chronic renal insufficiency of moderate severity (CK from 30 to 59 ml / min), the values ​​of AUC and C max are 30% higher, and with a severe degree (SC from 5 to 29 ml / min) - by 50% higher in comparison with healthy people.

In liver failure, the value of AUC (but not C max ) increases, on average, by 40%, which does not require correction of the dosing regimen.

In elderly people, the values ​​of C max and AUC increase by an average of 2 times, which does not require correction of the dosing regimen.

Body weight, sexual and racial differences do not affect the pharmacokinetics of eprosartrans.

INDICATIONS

- arterial hypertension.

DOSING MODE

The drug is taken orally, regardless of food intake.

The recommended dose is 1 tab.
1 time / day. Eprosartan can be used alone or in combination with other antihypertensive drugs. The maximum reduction in blood pressure in most patients is achieved in 2-3 weeks of treatment.
Dose correction is not required for elderly patients and patients with mild and moderate renal failure (QC-30 mL / min) .

For patients with moderate and severe renal failure (CC less than 60 ml / min), the daily dose should not exceed 600 mg.

SIDE EFFECT

Most often, patients receiving eprosartan reported such adverse reactions to the drug as headache and nonspecific complaints on the condition of the digestive system that occurred in approximately 11% and 8% of patients, respectively.

The incidence of adverse reactions listed below was determined as follows: very often (? 1/10);
often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10 000, <1/1000); very rarely (<1/10 000), including individual messages.
From the side of the central nervous system: very often - headache;
often - dizziness, asthenia.
From the side of the cardiovascular system: infrequent - a pronounced decrease in blood pressure.

From the respiratory system: rhinitis.

From the skin and subcutaneous fat: often - allergic skin reactions (for example, skin rash, itching);
infrequently - angioedema (including face, lips, tongue, pharynx).
From the digestive system: often - nonspecific complaints from the digestive tract (for example, nausea, diarrhea, vomiting).

From the immune system: infrequently - hypersensitivity.

On the part of the genitourinary system: a violation of kidney function, incl.
acute renal failure, especially in patients at risk (for example, with renal artery stenosis).
CONTRAINDICATIONS

- hemodynamically significant bilateral stenosis of the renal arteries and stenosis of the artery of a single kidney;

- lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome (the preparation contains lactose monohydrate);

- Pregnancy;

- lactation period;

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

- Hypersensitivity to the components of the drug.

Caution should be applied to the drug in severe chronic heart failure (IV functional class according to the NYHA classification);
Reduction of BCC and / or excessive elimination of sodium chloride from the body (including as a result of vomiting, diarrhea, the intake of diuretics in high doses); in patients on hemodialysis or with QC less than 30 ml / min; with stenosis of the aortic and mitral valves, as well as in hypertrophic cardiomyopathy.
The company does not have data on the safety of the drug Teveten ® in patients with terminal stage of renal failure and recent kidney transplantation.

Teveten ® is not recommended for the treatment of patients with primary hyperaldosteronism.

Special care should be taken when prescribing Teveten ® for the treatment of patients with impaired hepatic and coronary artery disease, due to insufficient experience in these categories of patients.

PREGNANCY AND LACTATION

Pregnancy

Teveten ® is contraindicated in pregnancy.

Patients planning a pregnancy should switch to taking alternative antihypertensive drugs that have established safety characteristics for use in pregnancy.
Teveten® therapy should be discontinued immediately after pregnancy is established and, if necessary, alternative therapy should be initiated.
It is known that therapy with angiotensin II receptor antagonists in the II and III trimesters of pregnancy is toxic to the fetus (impaired renal function, low blood pressure, ossification of the skull bones) and newborn (renal failure, arterial hypotension, hyperkalemia).
If nevertheless eprosartan was used in the period from the second trimester of pregnancy, it is recommended to perform ultrasound monitoring of kidney function and the condition of the fetal skull.
Newborns whose mothers have taken eprosartan should be carefully monitored for arterial hypotension.

Lactation period

Due to the lack of data on the use of Teveten ® during breastfeeding, if possible, this drug should be replaced with other antihypertensive drugs that have established safety profiles, especially when feeding a newborn or premature baby.

APPLICATION FOR FUNCTIONS OF THE LIVER

For patients with severe or moderate renal insufficiency (CC less than 60 ml / min), the daily dose should not exceed 600 mg.

The company does not have data on the safety of the drug Teveten ® in patients with terminal stage of renal failure and recent kidney transplantation.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Special care should be taken when prescribing Teveten ® for the treatment of patients with impaired hepatic function, due to insufficient experience in these categories of patients


APPLICATION FOR CHILDREN

Contraindicated in children


APPLICATION IN ELDERLY PATIENTS

Dose adjustment is not required for elderly patients


SPECIAL INSTRUCTIONS

Symptomatic arterial hypotension

In patients with reduced BCC (as a result of diuretic therapy), with limited intake of table salt, with prolonged and repeated vomiting, taking Teveten ® can cause the development of symptomatic arterial hypotension.
Before beginning treatment with Teveten ®, it is necessary to correct the BCC.
Renal failure, severe chronic heart failure

In patients whose renal function depends on the activity of RAAS (eg, in severe chronic heart failure IV functional class according to NYHA classification) during treatment with ACE inhibitors, oliguria and / or progressive azotemia may develop and, in rare cases, severe renal failure.

Due to the inadequate experience with the use of angiotensin II receptor antagonists in patients with severe chronic heart failure or renal artery stenosis of a single kidney, renal function impairment can not be ruled out with the use of Teveten ® , due to the suppression of RAAS.

Before prescribing Teveten ®, patients with renal insufficiency and, periodically, during the course of therapy should monitor the kidney function.
If there is a worsening of renal function during this period, the advisability of continuing treatment with Teveten ® should be reconsidered.
Angiotensin antagonists reduce the pressure less effectively in patients with Negroid races suffering from hypertension, due to the higher prevalence of conditions characterized by low levels of renin.

Impact on the ability to drive vehicles and manage mechanisms

The effect of eprosartan on the ability to drive a vehicle and work with mechanisms has not been studied, but on the basis of pharmacodynamic properties, it can be said that such effects do not.

During the treatment with Teveten ® , caution should be exercised when driving vehicles and occupations

potentially dangerous activities that require increased concentration and speed of psychomotor reactions, due to the possibility of dizziness and weakness.

OVERDOSE

There are only limited data on overdose.
The drug is well tolerated when ingested.
Symptoms: marked decrease in blood pressure.

Treatment: symptomatic therapy.

DRUG INTERACTION

Eprosartan does not affect the pharmacokinetics of digoxin and the pharmacodynamics of warfarin or glibenclamide.

Ranitidine, ketoconazole, fluconazole do not affect the pharmacokinetics of eprosartan.

Eprosartan can be used in combination with thiazide diuretics (including hydrochlorothiazide) and blockers of "slow" calcium channels (including nifedipine prolonged action) without waiting for clinically significant undesirable interactions, with a mutual strengthening of the hypotensive effect.

Combined use of Teveten with potassium-sparing diuretics, nutritional supplements containing potassium, salt substitutes containing potassium and other drugs that raise the level of potassium in the blood serum (for example, heparin) can cause an increase in the serum potassium level.
During treatment with drugs that affect RAAS, hyperkalemia may develop, especially in patients with renal and / or hepatic insufficiency.
The antihypertensive action of Teveten can be potentiated by other antihypertensive drugs.

There are cases of reversible increase in the concentration of lithium in the blood serum and the development of toxic reactions with simultaneous administration of lithium preparations with ACE inhibitors.
We can not exclude the possibility of developing this effect after taking eprosartan, therefore it is recommended to control the concentration of lithium in blood plasma with simultaneous administration with eprosartan.
Co-administration with NSAIDs may lead to an increased risk of impaired renal function, including the possibility of developing acute renal failure, and an increase in potassium levels in the blood serum, especially in patients with an existing renal impairment.
Such combinations should be used with caution, especially in elderly patients. Patients are recommended to perform volume replacement therapy and monitor kidney function.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children, dry place at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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