Teveten

General characteristics. Structure:

Active agent: an eprosartana мезилат 490,55 mg (there correspond 400 mg of an eprosartan)  

Excipients: MKTs — 179,05 mg; lactoses monohydrate — 28,75 mg; starch corn gelated — 28,75 mg; кросповидон — 32 mg; magnesium stearate — 6 mg, the water purified — 34,9 mg  

Cover: Opadry® pink (YS-1-14643-A) — 32 mg (a gipromelloza, a macrogoal, polysorbate 80; dye: ferrous oxide yellow E172; ferrous oxide red E172; titanium E171 dioxide).

Active agent: an eprosartana мезилат 735,8 mg (there correspond 600 mg of an eprosartan)  

Excipients: MKTs — 43,3 mg; lactoses monohydrate — 43,3 mg; starch corn gelated — 43,3 mg; кросповидон — 38,5 mg; magnesium stearate — 7,2 mg; the water purified — 50,9 mg  

Cover: Opadry® white (OY-S-9603) — 38,5 mg (a gipromelloza, a macrogoal, polysorbate 80; dye: titanium E171 dioxide).

Pharmacological properties:

Pharmacodynamics. Selectively affects the angiotenzinovy receptors located in vessels, heart, kidneys and bark of adrenal glands forms with them strong communication with the subsequent slow dissociation. Angiotensin II contacts AT1-receptors in many fabrics (for example in smooth muscles of vessels, adrenal glands, kidneys, heart) and causes vasoconstriction, a delay of sodium and release of Aldosteronum, damage of target organs — a hypertrophy of a myocardium and vessels.

Eprosartan prevents development or weakens effects of angiotensin II. Reduces arterial vasoconstriction, OPSS, pressure in a small circle of blood circulation, a reabsorption of water and ions of sodium in a proximal segment of renal tubules, secretion of Aldosteronum. At prolonged use suppresses proliferative influence of angiotensin II on cells of unstriated muscles of vessels and a myocardium. The permanent anti-hypertensive effect remains during 24 h without development of orthostatic arterial hypotension in response to the first dose. Stabilization of anti-hypertensive action at regular reception occurs in 2–3 weeks without change of ChSS. At patients with arterial hypertension эпросартан does not influence concentration of triglycerides, the general cholesterol or cholesterol as a part of LPNP in blood defined on an empty stomach. Besides, does not influence concentration of glucose in blood on an empty stomach. Has the mediated diuretic and nefroprotektivny effect, reducing removal of albumine, at preservation of renal self-control regardless of degree of a renal failure. Does not influence purine exchange, does not exert significant impact on removal of uric acid with urine. Eprosartan does not strengthen the effects connected with bradikinin (APF-oposredovannykh), for example cough. Frequency of cases of dry, persistent cough at the patients receiving эпросартан — 1,5%. When replacing APF inhibitor eprosartany at the patients who had cough, the frequency of dry persistent cough corresponds to placebo. The treatment termination eprosartany is not followed by a syndrome of "cancellation".

Pharmacokinetics. After intake of a single dose of 300 mg bioavailability makes about 13%. Linkng with proteins of a blood plasma — high (98%) also remains to constants in all therapeutic range of concentration. Extent of linkng with proteins of a blood plasma does not depend on a sex, age, function of a liver and does not change at slightly expressed or moderate renal failure, but can decrease at a heavy renal failure. Cmax of drug is defined by 1–2 h after intake. At reception of an eprosartan along with food clinically insignificant decrease in absorption (<25%), Cmax and AUC is observed. T1/2 — 5–9 h. Distribution volume — 13 l, the general Cl — 130 ml/min. It is removed generally in not changed look — with a stake of 90%, with urine — 7% at intake. Insignificant part (less than 2%) is removed by kidneys in the form of glucuronides. 20% of concentration in urine are made by an acylglucuronide of an eprosartan, 80% — not changed drug. Practically does not kumulirut. The body weight, sexual and racial distinctions do not exert impact on pharmacokinetics of an eprosartan. At persons under 18 the pharmacokinetics was not studied. Increase in advanced age of Cmax and AUC value on average twice that, however, does not demand correction of the mode of dosing. At a liver failure of AUC value (but not Cmax) increase on average for 40% that does not demand correction of the mode of dosing. At treatment eprosartany patients with moderate degree of a chronic renal failure (Cl of creatinine from 30 to 59 ml/min.), AUC and Cmax — for 30%, and with heavy degree (Cl of creatinine from 5 to 29 ml/min.) — is 50% higher in comparison with healthy people.

Indications to use:

Arterial hypertension.

Route of administration and doses:

Inside, irrespective of meal. The recommended daily dose — 600 mg once a day in the morning. Selection of an initial dose is not required for patients of advanced age and for the patients having a liver failure. For patients with a moderate or heavy renal failure (creatinine Cl <60 ml/min.) the daily dose should not exceed 600 mg. Duration of treatment of Tevetenom® is not limited.

Features of use:

During treatment of hypertensia it is necessary to be careful during the driving of motor transport and occupation potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions because there can be dizziness and weakness.

Symptomatic hypotension. At decrease in OTsK or the expressed decrease in volume of liquid and/or content of salts in an organism (including during treatment by high doses of diuretics, repeated vomiting, long diarrhea, at a diet with considerably reduced consumption of sodium), administration of drug can cause sharp decrease in the ABP (symptomatic hypotension). Before purpose of Tevetena® such disturbances should be eliminated. Tranzitorny decrease in the ABP is not the reason of drug withdrawal since in this case the ABP is stabilized at further reception.

Renal failure (heavy heart failure). At patients whose renal function depends on activity system renin-angiotensin-aldosteronovoy (for example at heavy heart failure of the III-IV FC on NYHA, a bilateral stenosis of renal arteries or a renal artery stenosis of the only kidney) during treatment by APF inhibitors the oliguria and/or the progressing azotemia, and, in rare instances, a heavy renal failure can develop. Due to the insufficient experience of use of antagonists of receptors of angiotensin II for patients with heavy heart failure or a renal artery stenosis, it is impossible to exclude disturbances of renal function against the background of use of Tevetena®, owing to suppression system renin-angiotensin-aldosteronovoy. At patients with a renal failure before purpose of Tevetena® and, periodically, during a course of treatment it is necessary to estimate function of kidneys. If during this period deterioration in renal function is observed, treatment of Tevetenom® should be reconsidered.

Side effects:

The general frequency of the side effects registered at the patients accepting эпросартан is comparable with that at placebo reception. These actions, as a rule, were poorly expressed and short so the termination of a course of treatment was required only from 4,1% of the patients accepting эпросартан during placebo - controlled clinical trials (6,5% — the group has placebo).
From TsNS: seldom — a headache, dizziness, an adynamy.
From cardiovascular system: very seldom — decrease in the ABP, including postural hypotension.
From skin and hypodermic fatty tissue: seldom — skin reactions (rash, an itch and urticaria); very seldom — a face edema, a Quincke's disease.
Others: seldom — cough.

Interaction with other medicines:

Clinically significant interactions of drug were not observed. Eprosartan does not influence pharmacokinetics of digoxin and a pharmacodynamics of warfarin or Glibenclamidum. Pharmacokinetic properties of an eprosartan do not change at its simultaneous use with ranitidine, ketokonazoly or flukonazoly. Eprosartan it is possible to apply in combination with thiazide diuretics (including with a hydrochlorothiazide) and blockers of "slow" calcium channels, including nifedipine of the prolonged action, without expecting clinically significant undesirable phenomena, at the same time Teveten® strengthens their hypotensive effect. Теветен® it is possible to appoint in combination with hypolipidemic means (including with lovastatiny, simvastatiny, pravastatiny, fenofibraty, gemfibrozily and niacin). At purpose of drugs of lithium along with APF inhibitors reversible increase in concentration of ions of lithium in blood serum was observed. It is impossible to exclude similar effect after use of an eprosartan in this connection, in case of the accompanying treatment, it is recommended to control carefully the content of lithium in blood serum.

Contraindications:

- hypersensitivity to drug components;
- pregnancy;
- breastfeeding period;
- age up to 18 years (efficiency and safety are not established).

With care:
- heavy heart failure of the III-IV FC (on NYHA);
- bilateral stenosis of renal arteries, renal artery stenosis of the only kidney;
- decrease in OTsK as a result of vomiting, diarrhea, reception of high doses of diuretics.
The company has no data on safety of Tevetena® at patients with a terminal renal failure (creatinine Cl less than 5 ml/min., uraemia of II), and also at the patients who are on a hemodialysis.

Use at pregnancy and feeding by a breast
Теветен® it is not necessary to apply during pregnancy. In case of pregnancy diagnosing drug it is necessary to cancel and warn the patient about possible undesirable effects immediately. It is not necessary to appoint эпросартан to women during breastfeeding. In need of use of Tevetena®, breastfeeding should be stopped.

Overdose:

There are only limited data on overdose. Drug is well transferred at intake. Efficiency of daily doses to 1200 mg is shown, at reception during 8 weeks and lack of messages on explicit dependence of frequency of adverse effects on a dose.

Symptoms: perhaps expressed decrease in the ABP.
Treatment: symptomatic therapy.

Storage conditions:

In the dry place, at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

In the blister of 14 pieces; in a box 1, 2 or 4 blisters.