Description
Latin name
TEVETEN
Release form
film-coated tablets.
Packing
14 pcs.
Pharmacological action
Pharmacodynamics
Antihypertensive drug, angiotensin II receptor antagonist.
Eprosartan selectively acts on the AT1 receptors located in the vessels, heart, kidneys, and adrenal cortex, forms a strong bond with them, followed by slow dissociation.
Angiotensin II binds to AT1 receptors in many tissues (including in the smooth muscles of blood vessels, adrenal glands, kidneys, heart) and causes vasoconstriction, sodium retention and aldosterone release, damage to target organs – myocardial and vascular hypertrophy.
Eprosartan prevents the development or attenuates the effects of angiotensin II. It has a vasodilating, hypotensive and indirect diuretic effect.
Reduces arterial vasoconstriction, OPSS, pressure in the pulmonary circulation, reabsorption of water and sodium in the proximal segment of the renal tubules, and secretion of aldosterone. With prolonged use, it inhibits the proliferative effect of angiotensin II on vascular and myocardial smooth muscle cells.
Permanent antihypertensive effect persists for 24 hours without the development of orthostatic arterial hypotension in response to the first dose. Stabilization of antihypertensive action with regular use occurs after 2-3 weeks, without changing heart rate.
In patients with arterial hypertension, eprosartan does not affect the concentration of TG, total cholesterol (Ch) or LDL-C in the blood, determined on an empty stomach. In addition, eprosartan does not affect fasting blood glucose concentrations.
Has a nephroprotective effect, reducing the excretion of albumin, while maintaining renal autoregulation, regardless of the degree of renal failure.
Does not affect purine metabolism, has no significant effect on uric acid excretion in urine.
Eprosartan does not enhance the effects associated with bradykinin and mediated by ACE, such as coughing. The incidence of dry, persistent cough in patients receiving eprosartan is 1.5%. When replacing an ACE inhibitor with eprosartan in patients suffering from cough, the frequency of dry persistent cough corresponds to placebo.
Discontinuation of eprosartan does not cause withdrawal.
Pharmacokinetics
Absorption
After oral administration in a single dose of 300 mg, the bioavailability of the drug is 13%. Cmax of eprosartan in plasma is reached after 1-2 hours.
When taking eprosartan at the same time as food, a clinically insignificant decrease in absorption (less than 25%), Cmax in plasma and AUC values are observed.
Distribution of
Plasma protein binding is 98% and is constant in the range of therapeutic concentrations.
Vd – 13 L Almost does not cumulate.
The excretion of
T1 / 2 is 5 9 hours. The total clearance is 130 ml / min.
It is excreted mainly unchanged – with feces 90%, with urine – 7%. A small part (less than 2%) is excreted by the kidneys in the form of glucuronides. 20% of the concentration in urine is acylglucuronide of eprosartan, 80% is unchanged eprosartan.
Pharmacokinetics in special clinical cases
The degree of binding to plasma proteins does not depend on gender, age, the presence of impaired liver function and does not change with mild or moderate renal failure, but may decrease in severe renal failure.
Pharmacokinetics not studied in individuals under 18 years of age.
When using eprosartan in patients with moderate chronic renal failure (KK from 30 to 59 ml / min), the values of AUC and Cmax are 30% higher, and with a severe degree (KK from 5 to 29 ml / min) – 50% higher compared to healthy people.
With liver failure, the AUC value (but not Cmax) increases, on average, by 40%, which does not require correction of the dosing regimen.
In elderly people, the values of Cmax and AUC increase on average by 2 times, which does not require correction of the dosage regimen.
Body weight, gender, and racial differences do not affect the pharmacokinetics of eprosartran.
Indications
Arterial hypertension.
Contraindications
Hypersensitivity to the components of the drug
pregnancy and lactation
children and adolescents under 18 years of age (efficacy and safety have not been established).
Caution: in severe heart failure (NYHA class III and IV functional class) with bilateral renal artery stenosis with single kidney renal artery stenosis with lowering of bcc as a result of vomiting, diarrhea, and high-dose diuretics.
The safety of Teveten in patients with end-stage renal failure (creatinine clearance less than 5 ml / min, grade II uremia), as well as in patients on hemodialysis, has not been established.
Use during pregnancy and lactation
Teveten is contraindicated in pregnancy and lactation.
In case of pregnancy diagnosis, the drug should be discontinued and the patient should be warned of possible undesirable consequences.
If you need to use the drug during lactation, breastfeeding should be discontinued.
Composition
1 film-coated tablet contains:
Active ingredient: eprosartan mesylate – 735.8 mg, which corresponds to 600 mg of eprosartan.
Excipients: microcrystalline cellulose, lactose monohydrate, pregelatinized starch, crospovidone, magnesium stearate, purified water.
Shell: Opadry white (OY-S-9603) (hypromellose, macrogol, polysorbate 80, dye: titanium dioxide (E171)).
Dosage and administration of
The drug is taken orally, regardless of food intake.
The recommended dose is 600 mg 1 time / day in the morning. The selection of the initial dose is not required for elderly patients and for patients suffering from liver failure.
For patients with severe or moderate renal failure (creatinine clearance less than 60 ml / min), the daily dose should not exceed 600 mg.
The duration of use of Teveten is not limited.
Overdose
There is limited data on overdose in humans. The drug is well tolerated when taken orally. The efficacy of the drug in daily doses up to 1.2 g is shown when taken for 8 weeks, with no dependence of the frequency of adverse effects on the dose.
Symptoms: most likely a marked decrease in blood pressure.
Treatment: carrying out symptomatic therapy.
Storage conditions
Store at a temperature not exceeding 25 ° C.
Keep out of the reach of children.
Expiration
2 years.
for srdlfp pharmacy terms for
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Prescription
dosage form
dosage form
tablets
