Вальсакор®

General characteristics. Structure:

KERNEL:

Active agent: валсартан 80 mg or 160 mg

Excipients: lactoses monohydrate, cellulose microcrystallic, povidone, croscarmellose sodium, silicon dioxide colloid, anhydrous, magnesium stearate.

COVER:

Tablet, film coated, 80 mg: a gipromelloza, titanium dioxide (E171), dye ferrous oxide red (E172), a macrogoal - 4000.

Tablet, film coated, 160 mg: a gipromelloza, titanium dioxide (E171), dye ferrous oxide yellow (E172), dye ferrous oxide red (E172), a macrogoal - 4000.

Pharmacological properties:

Pharmacodynamics. Valsartan is the selection antagonist of receptors of angiotensin II (AT1 type) for intake, the nonprotein nature.

Has selective antagonistic effect on AT1 subtype receptors. Increase in plasma concentration of angiotensin II which can stimulate not blocked AT2 subtype receptors that presumably regulates effects of AT1 receptors is a consequence of blockade of AT1 receptors. Valsartan has no agonistic activity concerning AT1 receptors. Its affinity to AT1 subtype receptors approximately in 20000 times more, than to AT2 subtype receptors.

Valsartan does not inhibit the angiotensin-converting enzyme (ACE) known also under the name of a kininaza II which turns angiotensin I into angiotensin II and bradikinin destroys. Due to the lack of influence on APF, effects of bradikinin and substance P therefore at reception of antagonists of angiotensin II development of dry cough is improbable are not exponentiated. Valsartan does not enter interaction and does not block the receptors of other hormones or ion channels participating in regulation of functions of cardiovascular system.

At treatment of arterial hypertension валсартан reduces arterial pressure, without influencing the heart rate (HR). After intake of a single dose of drug the anti-hypertensive effect develops within 2 hours, and the maximum lowering of arterial pressure (ABP) is reached within 4-6 hours. The anti-hypertensive effect of drug remains within 24 hours after its reception. At repeated purposes of a valsartan the maximum decrease in the ABP, regardless of doses, is reached in 2-4 weeks and supported at the reached level during long therapy. The combination with a hydrochlorothiazide allows to reach significant additional decrease in the ABP.

The sudden termination of reception of a valsartan is not followed by sharp raising of the ABP or other undesirable clinical effects.

Tolerance to an exercise stress

At impact assessment of the valsartan (appointed in addition to standard therapy of heart failure) on portability of an exercise stress at patients with chronic heart failure of the II-IV functional classes on classification of NYHA and with the fraction of emission of a left ventricle (FELV) <40% increase in time of an exercise stress in comparison with initial indicators was noted.

There is no syndrome of "cancellation" at the sudden termination of reception.

Pharmacokinetics. Valsartan is quickly soaked up after intake, however extent of absorption varies over a wide range. The average size of absolute bioavailability of a valsartan makes 23%. Time necessary for achievement of the maximum concentration (TCmax), - 2 hours. After regular reception the maximum decrease in the ABP occurs in 4 weeks. At administration of drug once in days its accumulation is insignificant. Plasma concentration of a valsartan are identical at men and women. Valsartan actively contacts proteins of serum (94-97%), is preferential with a seralbumin. Equilibrium volume of distribution of drug small, about 17 liters. Plasma clearance rather low (about 2 l/hour) when comparing with a hepatic blood-groove (about 30 l/hour). It is metabolized by the fermental CYP2C9 system. The elimination half-life makes 9 hours. The quantity of the valsartan which is removed through intestines makes 70% of the dose which is soaked up after intake.

With urine 30% are removed, it is preferential in not changed look. At reception of a valsartan with food the area under a curve "concentration time" (AUC) decreases by 48%. Nevertheless, in 8 hours after administration of drug plasma concentration of the valsartan accepted on an empty stomach and with food are identical. Reduction of AUC is not followed by clinically significant reduction of therapeutic effect of a valsartan therefore drug can be used both to, and after food.

Indications to use:

• Arterial hypertension.
• Chronic heart failure (the II-IV functional class on NYHA classification) as a part of complex therapy (against the background of standard therapy) and at the patients who are not receiving APF inhibitors.
• Decrease in cardiovascular mortality at stable patients at whom LZh insufficiency/dysfunction owing to the postponed myocardial infarction developed.

Route of administration and doses:

Inside, regardless of meal, frequency rate of reception - 1 - 2 time a day.

Arterial hypertension

The recommended dose makes 80 mg once a day, irrespective of age, sex or race of the patient. The anti-hypertensive effect develops within 2 weeks and reaches the maximum in 4 weeks. The maximum daily dose - 320 mg a day. Patients with an impaired renal function and a liver of not biliary origin and without cholestasia do not need change of doses of drug. The combination with other hypotensive drugs is possible.

Chronic heart failure

The recommended starting dose makes 40 mg two times a day. Perhaps gradual increase up to 80 mg, at good tolerance - to 160 mg two times a day, i.e. to the maximum dose transferred by the patient. The maximum daily dose - 320 mg divided into 2 receptions. At the patients who are at the same time receiving diuretics, and also at patients with heart failure constant control of function of kidneys, the ABP is necessary. At emergence of clinical signs of arterial hypotension, it is necessary to reduce doses.

Use after an acute myocardial infarction

At clinically stable patients treatment can be begun in 12 hours after development of a myocardial infarction. After purpose of an initial dose in 20 mg two times a day, the dose of a valsartan gradually increases to 40 mg, 80 mg, and 160 mg two times a day within several weeks. The maximum daily dose - 160 mg two times a day. In two weeks after an initiation of treatment drug Valsakor, it is necessary to reach a dose of 80 mg 2 times a day, and the dose of 160 mg 2 times a day can be reached in 3 months of therapy by drug Valsakor. Achievement of a target dose depends on portability of a valsartan during titration of a dose.

At development of symptomatic hypotension or renal failure it is necessary to reduce a drug dose.

Assessment of a condition of patients after a myocardial infarction has to include control of function of kidneys.

With abnormal liver functions of not biliary genesis without the phenomena of a cholestasia of dose adjustment it is not required to patients.

Features of use:

Arterial hypotension, liver failure against the background of impassability of bilious ways, a renal failure (the clearance of creatinine (CC) less than 10 ml/min.), including the patients who are on a hemodialysis, a hyponatremia, a diet with sodium consumption restriction, the bilateral stenosis of renal arteries or a stenosis of an artery of the only kidney, states which are followed by decrease in the volume of the circulating blood (VCB) (including diarrhea, vomiting).

Influence on ability to drive the car and other mechanisms 

patients need to be careful when driving and other mechanisms requiring special attention.

Side effects:

From the central and peripheral nervous system: often - a headache, dizziness, including postural, вертиго; not often - sleeplessness; sometimes - a syncope (at use after the postponed myocardial infarction).

From respiratory system, bodies of a thorax and a mediastinum: often - cough, infections of upper parts of respiratory tracts, pharyngitis, rhinitis, sinusitis.

From cardiovascular system: often - the expressed decrease in the ABP and orthostatic hypotension; sometimes (at use after the postponed myocardial infarction) - heart failure.

From digestive tract: often - nausea, diarrhea, an abdominal pain.

From skin and hypodermic cellulose: seldom - skin rash.

From muscles, a skeleton and connecting fabric: often - a dorsodynia, a mialgiya, an arthralgia.

From urinogenital system: not often - decrease in a libido; very seldom - a renal failure.

Allergic reactions: very seldom - a Quincke's disease, skin rash, a skin itch, hypersensitivity reactions, including a serum disease and a vasculitis.

From laboratory parameters: seldom - decrease in concentration of hemoglobin and a hematocrit, a neutropenia, thrombocytopenia, a giperkreatininemiya, a hyperbilirubinemia, increase in activity of "hepatic" transaminases, increase in a serumal urea nitrogen; often - a hyperpotassemia.

Others: often - the general weakness; not often - hypostases, an adynamy, increased fatigue.

Interaction with other medicines:

Clinically significant pharmacokinetic interactions with other medicines are noted. The drugs tested in clinical trials included Cimetidinum, warfarin, digoxin, атенолол, indometacin, a hydrochlorothiazide, амлодипин and Glibenclamidum.

As валсартан is not exposed to essential metabolism, it is not necessary to expect also the significant medicinal interactions connected with induction or inhibition of system of P450 cytochrome. The concomitant use of kaliysberegayushchy diuretics (Spironolactonum, Triamterenum, amiloride), kaliysoderzhashchy nutritional supplements can lead to a hyperpotassemia, in communication; what it is required to be careful with. At joint reception with diuretics strengthening of hypotensive effect is possible.

Contraindications:

• Hypersensitivity to a valsartan or to other components of drug.
• Pregnancy and period of a lactation.
• Age up to 18 years (efficiency and safety of a valsartan at children is not proved).
• A lactose intolerance, a galactosemia or a syndrome of the broken absorption of a glucose/galactose.

Pregnancy and feeding by a breast

There are no data on use of a valsartan at pregnancy. Renal perfusion of a fruit which depends on development a system renin-angiotenzinovoy begins to function in the third trimester of pregnancy. The risk for a fruit increases at reception of a valsartan in the second and third trimesters. At pregnancy establishment therapy valsartany has to be immediately stopped. There are no data on allocation of a valsartan in maternal milk. Therefore it is necessary to resolve an issue of the feeding termination by a breast or therapy cancellation valsartany taking into account its importance for mother.

Overdose:

Symptoms: the overdoses of a valsartan given about effects are absent. Despite the lack of enough data, the main expected drug overdose manifestation - the expressed decrease in the ABP which can lead to a collapse and/or shock.

Treatment: symptomatic, is recommended to cause vomiting and to wash out a stomach. At development of arterial hypotension intravenously enter 0,9% chloride sodium solution. The hemodialysis is inefficient.

Storage conditions:

Period of validity 3 years. Not to apply after expiry date. To store at a temperature not above 30 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 80 mg and 160 mg.

On 7 or 14 tablets in the blister. On 2 or 4 blisters (the blister on 7 tablets); 1 or 2 blisters (the blister on 14 tablets) in a cardboard pack together with the application instruction.