Valsakor

Valsakor – drug with anti-hypertensive action.

Form of release and structure

Valsakor produce in the form of tablets, film coated, in blisters 7 pieces (on 40 mg, 80 mg and 160 mg) and 14 pieces (on 80 mg, 160 mg and 320 mg).

Active agent – валсартан in quantity is a part of 1 tablet:

• 40 mg – tablets of brownish-yellow color, slightly biconvex, round, with risky on one party;
• 80 mg – tablets of pink color, biconvex, round, with risky on one party;
• 160 mg – tablets of brownish-yellow color, biconvex, oval, with risky on one party;
• 320 mg – tablets of light brown color, biconvex, oval, with risky on one party.

The auxiliary components which are a part of drug: magnesium stearate, lactoses monohydrate, microcrystallic cellulose, croscarmellose sodium, povidone, silicon dioxide colloid anhydrous.

Structure of a cover of tablets:

• 40 mg – a macrogoal 4000, E171 (titanium dioxide), a gipromelloza, E172 (dye ferrous oxide yellow);
• 80 mg – a macrogoal 4000, E171 (titanium dioxide), a gipromelloza, E172 (dye ferrous oxide red);
• 160 mg and 320 mg – a macrogoal 4000, E171 (titanium dioxide), a gipromelloza, E172 (dye ferrous oxide red), E172 (dye ferrous oxide yellow).

Indications to use

• Chronic heart failure (on NYHA classification – the II-IV functional class) as a part of complex therapy (at the same time with standard therapy) and at the patients who are not receiving APF inhibitors;
• Arterial hypertension;
• Decrease in cardiovascular mortality at stable patients at whom insufficiency/dysfunction of a left ventricle because of the postponed myocardial infarction developed.

Contraindications

Contraindications to Valsakor's use are:

• Lactose intolerance, syndrome of the broken absorption of a glucose/galactose or galactosemia;
• Age up to 18 years (safety and efficiency of its use for children is not proved);
• Hypersensitivity to active agent (valsartan) or to other components of drug.

There are no data on use of drug at pregnancy. At pregnancy establishment Valsakor's reception needs to be stopped immediately. For a fruit the risk increases in II and III trimesters.

Data on allocation of a valsartan in maternal milk are absent. Therefore, taking into account importance of therapy for mother, it is necessary to resolve an issue of feeding interruption by a breast or cancellation of administration of drug.

Valsakor it is necessary to take with caution at the following states / diseases:

• Liver failure at impassability of bilious ways;
• Arterial hypotension;
• Stenosis of an artery of the only kidney or bilateral stenosis of renal arteries;
• Renal failure (clearance of creatinine < 10 мл в минуту), в т.ч. находящиеся на гемодиализе больные;
• Diet with sodium consumption restriction;
• Hyponatremia;
• The states which are followed by decrease in volume of the circulating blood including diarrhea, vomiting.

Route of administration and dosage

Valsakor accept inside, regardless of meal. Frequency rate of use – 1-2 times a day.

The recommended dose at arterial hypertension (irrespective of a sex, age or race of the patient) makes 80 mg once a day. The anti-hypertensive effect develops within 2 weeks, reaching the maximum in 4 weeks. The maximum daily dose – 320 mg. And the liver of not biliary origin and without cholestasia of change of doses of drug is not required to patients with renal failures. Perhaps combined use with other hypotensive medicines.

At treatment of chronic heart failure the recommended initial dose makes 40 mg, frequency rate of reception – 2 times a day. It is gradually possible to increase a dose to 80 mg, at good tolerance – to 160 mg (as much as possible) 2 times a day. At the patients who are at the same time receiving diuretics, and also at patients with heart failure it is necessary to control constantly functions of kidneys, arterial pressure. At development of clinical signs of arterial hypotension the dosage needs to be reduced.

At Valsakor's use after an acute myocardial infarction for clinically stable patients therapy needs to be begun within 12 hours after development of a disease. An initial dose – 20 mg 2 times a day (1/2 tablets of 40 mg with risky). Gradually single dose is increased to 40 mg, to 80 mg – in 14 days from an initiation of treatment, and brought to 160 mg 3 months later, without changing frequency rate of reception. Achievement of a target dosage depends on portability of drug during titration of doses.

When developing a renal failure, or symptomatic or arterial hypotension the dose of drug needs to be reduced.

After a myocardial infarction it is necessary to include control of function of kidneys in assessment of a condition of patients.

Dose adjustment is not required to patients with disturbance of work of a liver of not biliary genesis without the cholestasia phenomena.

Side effects

At Valsakor's use the development of side effects which is shown with various frequency is possible:

• Respiratory system, bodies of a thorax and mediastinum: often – rhinitis, cough, pharyngitis, infections of upper parts of respiratory tracts, sinusitis;
• Central and peripheral nervous system: often – a headache, вертиго, dizziness, including postural; infrequently – sleeplessness; sometimes – a syncope (at therapy after the postponed myocardial infarction);
• Skin and hypodermic cellulose: seldom – skin rash;
• Urinogenital system: infrequently – decrease in a libido; very seldom – renal failures;
• Cardiovascular system: often – orthostatic hypotension, the expressed lowering of arterial pressure; sometimes – heart failure (at therapy after the postponed myocardial infarction);
• Muscles, skeleton and connecting fabric: often – a mialgiya, a dorsodynia, an arthralgia;
• Digestive tract: often – diarrhea, nausea, an abdominal pain;
• Laboratory parameters: often – a hyperpotassemia; seldom – decrease in concentration of a hematocrit and hemoglobin, thrombocytopenia, a neutropenia, a hyperbilirubinemia, a giperkreatininemiya, increase in a serumal urea nitrogen and activity of hepatic transaminases;
• Allergic manifestations: very seldom – a skin itch, rash on skin, a Quincke's disease, hypersensitivity reactions, including a vasculitis and a serum disease;
• Others: often – a condition of the general weakness; infrequently – an adynamy, hypostases, increased fatigue.

Clinical data are not enough, but, despite it the main expected manifestation of overdose of Valsakor is the expressed lowering of arterial pressure which can become the reason of shock and/or a collapse.

For simplification of a state it is recommended to cause vomiting then to wash out a stomach. The hemodialysis is inefficient. When developing arterial hypotension intravenous administration of 0,9% of solution of sodium of chloride is shown.

Special instructions

Valsakor's use for patients with heart failure usually is followed by lowering of arterial pressure, however at observance of recommendations about selection of doses arterial hypotension seldom happens the therapy cancellation reason. Treatment of patients with heart failure needs to be begun carefully. At some patients because of activity suppression renin-angiotensin-aldosteronovoy of system change of function of kidneys is possible. At heavy heart failure the progressing azotemia and/or an oliguria up to an acute renal failure and/or death can develop (seldom). At patients with heart failure it is necessary to control constantly function of kidneys at simultaneous use of a combination of 3 classes of drugs – beta adrenoblockers, APF inhibitors and antagonists of receptors of AT1 angiotensin II.

Valsakor's use along with other medicines appointed after the postponed myocardial infarction is possible: acetylsalicylic acid, trombolitika, statines and beta adrenoblockers.

Patients with the expressed deficit in an organism of sodium and/or the reduced volume of the circulating blood (for example, because of reception of high doses of diuretics) in an initiation of treatment can sometimes have an expressed arterial hypotension. Before therapy it is recommended to recover the content of electrolytes and liquid in an organism, in particular, having reduced a dose of diuretics.

When developing arterial hypotension with clinical manifestations of the patient it is necessary to lay on a back. If necessary intravenously enter 0,9% chloride sodium solution. Valsakor's reception can be continued only after stabilization of indicators of arterial pressure.

At patients with a unilateral or bilateral stenosis of renal arteries it is necessary to control constantly the maintenance of an urea nitrogen and creatinine in serum.

With an impaired renal function and the liver of change of doses of drug is not required from patients.

Due to the lack of sufficient data about Valsakor's use at a heavy renal failure (clearance of creatinine < 10 мл в минуту или 0,167 мл в секунду) препарат следует применять с осторожностью.

At patients with obstructive diseases of biliary tract decrease in clearance of Valsakor in this connection it is necessary to appoint drug with care is observed.

During therapy patients are recommended to be careful at control of motor transport and other mechanisms requiring from them special attention.

Medicinal interaction

Contraindicated simultaneous use of Valsakor with antagonists of receptors of angiotensin II, including валсартан, or APF inhibitors with aliskireny at patients with a diabetes mellitus and a renal failure (KK < 60 мл в минуту).

Simultaneous use of Valsakor with drugs of lithium is not recommended as perhaps reversible increase in a blood plasma of concentration of lithium and development of intoxication. Combined use with diuretics and drugs of lithium can promote additional increase in concentration of lithium and growth of risk of development of intoxication. In case of need such combined use it is necessary to control carefully concentration of lithium in a blood plasma.

At simultaneous use with kaliysoderzhashchy nutritional supplements, potassium drugs, kaliysberegayushchy diuretics, other substances and medicines which can increase the content of potassium in blood serum (for example, heparin) it is recommended to carry out control of content of potassium in a blood plasma.

At some patients double blockade of RAAS was followed by a loss of consciousness, arterial hypotension, a renal failure (including an acute renal failure) and a hyperpotassemia. It is necessary to be careful at simultaneous use of Valsakor with antagonists of receptors of angiotensin II, including валсартан, with the drugs exerting impact on RAAS (алискирен, APF inhibitors).

At simultaneous use of Valsakor with non-steroidal anti-inflammatory drugs, including the selection TsOG-2 inhibitors, acetylsalicylic acid in a dose more than 3 g a day and non-selective non-steroidal anti-inflammatory drugs, are possible weakening of hypotensive action, increase in risk of emergence of renal failures and content of potassium in a blood plasma. In an initiation of treatment it is recommended to estimate function of kidneys, and also to carry out correction of disturbances of water and electrolytic balance.

Simultaneous use of Valsakor with inhibitors of proteins conveyors OATP1B1/OATR1VZ (for example, cyclosporine, rifampicin) and the efflyuksny MRP2 conveyor (for example, ритонавир) can lead to increase in system exposure of a valsartan (Cmax and AUC) that needs to be considered at the beginning and at the end of simultaneous therapy.

Clinically significant interaction of Valsakor with the following drugs is not revealed: digoxin, warfarin, Cimetidinum, furosemide, indometacin, атенолол, hydrochlorothiazide, Glibenclamidum and амлодипин.

Terms and storage conditions

To store in protected from light, the place, dry, unavailable to children, at a temperature up to 30 °C.

Period of validity – 3 years.