Teveten^® (Tablets) Instructions for Use

ATC Code

C09CA02 (Eprosartan)

Active Substance

Eprosartan (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Angiotensin II receptor antagonist

Pharmacotherapeutic Group

Angiotensin II receptor antagonist

Pharmacological Action

Antihypertensive agent, a synthetic angiotensin II receptor antagonist, a non-biphenyl tetrazole derivative.

Eprosartan selectively binds to AT₁ receptors located in the vessels, heart, kidneys, and adrenal cortex, forming a strong bond with them followed by slow dissociation.

Angiotensin II binds to AT₁ receptors in many tissues (including vascular smooth muscle, adrenal glands, kidneys, heart) and causes vasoconstriction, sodium retention, and aldosterone release, target organ damage – myocardial and vascular hypertrophy.

Eprosartan prevents the development or attenuates the effects of angiotensin II. It suppresses the activity of the RAAS. It has vasodilatory, hypotensive, and indirectly – diuretic effects.

It reduces arterial vasoconstriction, total peripheral resistance, pressure in the pulmonary circulation, reabsorption of fluid and sodium ions in the proximal segment of the renal tubules, and aldosterone secretion. With long-term use, it suppresses the proliferative effect of angiotensin II on vascular smooth muscle cells and myocardium.

In patients with arterial hypertension, Eprosartan does not affect the concentrations of TG, total cholesterol (Ch) or LDL-Ch in the blood, determined on an empty stomach. Furthermore, Eprosartan does not affect fasting blood glucose concentration.

It increases renal blood flow and glomerular filtration rate, reduces albumin excretion (nephroprotective action), while maintaining renal autoregulation regardless of the severity of renal failure.

Discontinuation of eprosartan treatment is not accompanied by a withdrawal syndrome.

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

The hypotensive effect after a single dose lasts for 24 hours, a sustained therapeutic effect appears with regular use – after 2-3 weeks without changing heart rate.

Pharmacokinetics

After oral administration of a single 300 mg dose, the bioavailability is approximately 13%. When eprosartan is taken with food, a clinically insignificant decrease in absorption (less than 25%), C_max in plasma and AUC values is observed. C_max is reached in 1-2 hours. Plasma protein binding is 98% and is constant over the range of therapeutic concentrations. It is excreted in breast milk. V_d is 13 L, total clearance is 130 ml/min. It practically does not accumulate. T_1/2 is 5-9 hours. It is excreted mainly unchanged – through the intestine (90%), by the kidneys (7%). A small part (less than 2%) is excreted by the kidneys in the form of glucuronides. 20% of the concentration in urine is eprosartan acyl glucuronide, 80% is unchanged Eprosartan.

In elderly individuals, C_max and AUC values increase on average by 2 times, which does not require adjustment of the dosage regimen. In moderate chronic renal failure (creatinine clearance from 30 to 59 ml/min), AUC and C_max values are 30%, and in severe cases (creatinine clearance from 5 to 29 ml/min) – 50% higher compared to healthy individuals. In hepatic insufficiency after oral administration of a single dose, AUC (but not C_max) increases by almost 40% compared to healthy individuals. It is practically not removed by hemodialysis (clearance – less than 1 L/h).

Indications

Treatment of arterial hypertension.

ICD codes

Dosage Regimen

Tablets

Take orally regardless of meals. The recommended dose is 600 mg once daily in the morning. The maximum antihypertensive effect usually develops after 2-3 weeks of treatment.

Eprosartan is used both as monotherapy and as part of combination therapy (including with thiazide diuretics, calcium channel blockers).

For patients with renal insufficiency with creatinine clearance less than 60 ml/min, the daily dose should not exceed 600 mg.

Adverse Reactions

Nervous system disorders very common – headache; common – dizziness, asthenia.

Cardiovascular system disorders uncommon – pronounced decrease in blood pressure.

Respiratory system disorders rhinitis.

Digestive system disorders: common – nonspecific complaints from the gastrointestinal tract (e.g., nausea, diarrhea, vomiting).

Urinary system disorders impaired renal function, including acute renal failure, especially in at-risk patients (e.g., with renal artery stenosis).

Allergic reactions skin manifestations (including skin rash, itching); uncommon – angioedema (including face, lips, tongue, pharynx).

Immune system disorders: uncommon – hypersensitivity.

Contraindications

Hemodynamically significant bilateral renal artery stenosis and stenosis of the artery of a single kidney; pregnancy; lactation (breastfeeding); children and adolescents under 18 years of age (efficacy and safety not established); hypersensitivity to eprosartan.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Use in Renal Impairment

In patients whose renal function depends on the activity of the renin-angiotensin-aldosterone system (e.g., with severe heart failure, bilateral renal artery stenosis or renal artery stenosis of a single kidney), during treatment with ACE inhibitors, oliguria and/or progressive azotemia develop, and in rare cases, acute renal failure.

Pediatric Use

Contraindicated in children.

Special Precautions

Not recommended for the treatment of patients with primary hyperaldosteronism.

Use with caution in severe chronic heart failure (NYHA functional class IV); reduced circulating blood volume and/or excessive excretion of sodium chloride from the body (including as a result of vomiting, diarrhea, taking diuretics in high doses); in patients on hemodialysis or with creatinine clearance less than 30 ml/min; with stenosis of the aortic and mitral valves, as well as with hypertrophic cardiomyopathy.

Use with particular caution in patients with impaired liver function and coronary artery disease, due to insufficient clinical experience of use in these categories of patients.

There are no data on the use of eprosartan in patients with end-stage renal failure and recent kidney transplantation.

Drug Interactions

Eprosartan can be used in combination with thiazide diuretics (including hydrochlorothiazide) and slow calcium channel blockers (including sustained-release nifedipine), without expecting a clinically significant undesirable interaction, while mutual enhancement of the hypotensive effect occurs.

With the simultaneous use of eprosartan with potassium-sparing diuretics, dietary supplements containing potassium, salt substitutes containing potassium and other drugs that increase the level of potassium in the blood serum (e.g., heparin), an increase in the level of potassium in the blood serum is possible. During treatment with drugs affecting the RAAS, hyperkalemia may develop, especially in patients with renal and/or hepatic insufficiency.

The antihypertensive effect of eprosartan may be potentiated by other antihypertensive agents.

Cases of reversible increase in serum lithium concentration and the development of toxic reactions with the simultaneous administration of lithium preparations with ACE inhibitors are known. The possibility of a similar effect after taking eprosartan cannot be excluded (with this combination, monitoring of plasma lithium concentration is recommended).

With the simultaneous use of eprosartan with NSAIDs, there is a possibility of deterioration of renal function, including the risk of acute renal failure, and an increase in serum potassium levels, especially in patients with pre-existing renal impairment (these combinations should be used with caution, especially in elderly patients; monitoring of renal function is recommended).

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.