Valz

General characteristics. Structure:

Active agent: валсартан 40 mg, 80 mg or 160 mg;
Excipients: lactoses monohydrate, cellulose microcrystallic, croscarmellose sodium, K29-32 povidone, talc, magnesium stearate, silicon dioxide colloid;
Film cover:
For tablets of 40 mg: Опадрай II 85G32407 yellow (polyvinyl alcohol, talc, titanium dioxide, a macrogoal - 3350, dye ferrous oxide yellow, lecithin).
For tablets of 80 mg: Опадрай II 85G34643 pink (polyvinyl alcohol, talc, titanium dioxide, a macrogoal - 3350, dye ferrous oxide yellow, dye ferrous oxide red, lecithin).
For tablets of 160 mg: Опадрай II 85G32408 yellow (polyvinyl alcohol, talc, titanium dioxide, a macrogoal - 3350, dye ferrous oxide yellow, dye ferrous oxide red, lecithin).

Description

For tablets of 40 mg: oval biconvex tablets of yellow color, film coated, with marking of "V" on the one hand, risky on the other hand and side risks.
For tablets of 80 mg: round biconvex tablets of pink color, film coated, with risky from two parties, side risks and marking of "V" on the one hand.
For tablets of 160 mg: oval biconvex tablets of yellow color, a pokrytyeplenochny cover, with risky on the one hand, side risks and marking of "V" on the other hand.

Pharmacological properties:

Pharmacodynamics. The peripheral vazodilatator, has hypotensive effect. The specific blocker of AT1 of receptors of angiotensin II, does not inhibit the angiotensin-converting enzyme (ACE); does not influence the content of the general cholesterol, triglycerides, glucose and uric acid in blood. The beginning of effect is noted in 2 h after intake, at most - in 4-6 h; action duration - more than 24 h. After regular reception the maximum lowering of arterial pressure (ABP) comes in 2-4 weeks. There is no syndrome of "cancellation" at the sudden termination of reception.

Pharmacokinetics. After intake absorption - bystry, extent of absorption is variable. Average value of absolute bioavailability - 23%. The pharmacokinetic curve valsartana has the descending multiexponential character (t 1/2a <l of the h and t 1/2b about 9 h).
In the range of the studied doses the kinetics of a valsartan has linear character. At repeated use of a valsartan of changes of kinetic indicators it was not noted. At reception of a dose insignificant cumulation of a valsartan was observed once a day. Concentration of a valsartan in a blood plasma has no distinctions at men and women.
Valsartan well contacts proteins of a blood plasma (94-97%), is preferential with seralbumins. At achievement of an equilibrium state distribution volume - 17 l. In comparison with a hepatic blood-groove (about 30 l/h), the plasma clearance of a valsartan occurs rather slowly (about 2 l/h). Drug is removed with bile and kidneys, is preferential in not changed look. At the normal level of glomerular filtering (120 ml/min.) the renal clearance makes about 30% of the general plasma clearance. Gidroksimetabolit it is found in a blood plasma in low concentration (less than 10% of the area under a curve "concentration time" (AUC) for a valsartan). This metabolite is pharmacological not active. After intake of 83% of a valsartan it is removed through intestines and 13% through kidneys, it is preferential in not changed look.
At administration of drug with AUC food of a valsartan decreases by 48% though, since about the 8th hour after administration of drug, concentration of a valsartan in a blood plasma both in case of its reception on an empty stomach, and in case of reception with food, identical. Reduction of AUC is not followed by clinically significant reduction of therapeutic effect of a valsartan therefore drug can be used irrespective of meal.

Indications to use:

• Arterial hypertension.
• Chronic heart failure (the II-IV functional class on NYHA classification) as a part of complex therapy (excepting a combination валсартан + IAPF + beta adrenoblocker).
• Increase in survival of patients with the acute myocardial infarction (12 h - 10 days) complicated by a left ventricular failure and/or systolic dysfunction of a left ventricle in the presence of stable indicators of a hemodynamics.

Route of administration and doses:

Inside, irrespective of meal, washing down with enough liquid. Arterial hypertension
The recommended initial dose of drug Valz makes 80 mg once a day. The hypotensive effect develops in the first 2 weeks of therapy. The maximum effect is reached after 4 weeks of administration of drug. At patients for whom the daily dose of 80 mg does not give desirable therapeutic effect it is recommended to increase a daily dose to 160 mg. Other anti-hypertensive means can be in addition appointed (for example, diuretic).
Chronic Heart Failure (CHF): the recommended initial dose of drug Valz makes 40 mg 2 times a day. At insufficient therapeutic effect gradual increase in a dose to 80 mg 2 times a day is required and at good tolerance - to 160 mg 2 times a day. From the moment of an initiation of treatment drug Valz until achievement of reception of the maximum dosage has to be an interval not less than two weeks. The maximum daily dose - 320 mg in 2 receptions. Decrease in doses at a concomitant use of diuretics is possible.
Valz can be applied in a combination with other medicines intended for treatment of chronic heart failure. However administration of drug Valz in a combination with APF inhibitor + beta adrenoblocker is not recommended (see the section Special instructions).
After the postponed myocardial infarction: at stable indicators of a hemodynamics treatment can be begun during 12 h after an acute myocardial infarction. An initial dose - 1/2 tablets of 40 mg (20 mg) 2 times a day, with the subsequent increase in a dose up to 40 mg, 80 mg, 160 mg 2 times a day within several weeks, before achievement of the maximum daily dose of 160 mg 2 times a day.
Achievement of a dose of 80 mg 2 times a day is recommended by the end of the 2nd week of treatment, 160 mg 2 times a day - by the end of the 3rd month of therapy. The dose should be raised, based on portability of drug the patient.
In case of symptomatic arterial hypotension or at a renal failure the drug dose Valz should be lowered.
Renal failure and liver
With a renal failure at KK more than 10 ml/min. of dose adjustment are not required from patients. At patients with easy and moderate abnormal liver functions without development of a cholestasia the maximum daily dose of drug Valz should not exceed 80 mg.

Features of use:

At patients with the expressed deficit of sodium in an organism and/or reduced OTsK, for example, owing to reception of high doses of diuretics, at the beginning of therapy the expressed arterial hypotension in rare instances can valsartany develop. Before therapy by drug Valz is recommended to recover the content of electrolytes and liquid in an organism, in particular, by reduction of doses of diuretics.
Drug Valz can be used together with other drugs intended for treatment of a myocardial infarction such as trombolitik, acetylsalicylic acid, beta adrenoblockers, statines and diuretics. Joint reception of APF inhibitors is not recommended.
At a renovascular hypertension regular control of content of urea and creatinine in blood is necessary.
At combined use with the drugs containing potassium, its salts and the drugs relating to group of kaliysberegayushchy diuretics carry out regular control of level of potassium in a blood plasma.
The sick HSN beginning have a treatment by Valz, some lowering of arterial pressure in this connection it is recommended to control the ABP at the beginning of therapy can be noted.
Owing to inhibition system renin-angiotensin-aldosteronovoy at some patients changes of function of kidneys are possible. At patients from heavy HSN at whom function of kidneys depends on activity system renin-angiotensin-aldosteronovoy treatment with APF inhibitors and antagonists of angiotenzinovy receptors can be followed by an oliguria and/or increase of an azotemia and (seldom) acute renal failure and/or death.
Combined use of drug Valz at the patients suffering from HSN with APF inhibitors and beta adrenoblockers in a type of possible increase in risk of manifestation of side effects is not recommended.
At patients with a bilateral or unilateral stenosis of renal arteries regular control of content of creatinine and an urea nitrogen in blood serum is necessary.

Influence on ability to drive the car and to perform the works requiring special attention

During treatment it is necessary to be careful when driving motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of motor and mental reactions.

Side effects:

Frequency of side effects: very often (> 1/10); often (> 1/100, but <1/10); sometimes (> 1/1000, but <1/100); seldom (> 1/10000, but <1/1000), it is very rare (<1/10000).
From cardiovascular system: often - orthostatic hypotension *; sometimes – decrease in the ABP, heart failure; seldom - a vasculitis; very seldom - bleedings.
From respiratory system: sometimes - cough.
From the alimentary system: sometimes - diarrhea, abdominal pain; very seldom - nausea #.
From the central nervous system: often - postural dizziness *; sometimes - a faint, sleeplessness, a depression, decrease in a libido; seldom - dizziness *, neuralgia; very seldom - a headache.
From acoustic organs and labyrinth device: sometimes - вертиго.
From bodies of a hemopoiesis: often - a neutropenia, it is very rare - thrombocytopenia.
Allergic reactions: seldom - a serum disease; hypersensitivity; very seldom - a Quincke's disease **, skin rash, an itch.
From a musculoskeletal system: sometimes - a dorsodynia, myotonia, arthritis, a mialgiya; very seldom - an arthralgia;
From urinary tract: very seldom - dysfunction почек**##, an acute renal failure.
From a metabolism: sometimes - a hyperpotassemia
Infections: often - viral infections; sometimes - upper respiratory tract infections, pharyngitis, sinusitis, conjunctivitis; very seldom - rhinitis, a gastroenteritis.
Others: sometimes - feeling of fatigue, an adynamy, nasal bleeding, hypostases.
Laboratory indicators: decrease in level of hemoglobin and hematocrit, giperkreatininemiya, hyperbilirubinemia, increase in activity of "hepatic" transaminases, increase in concentration of an urea nitrogen of blood serum.
* It was reported during treatment after an acute myocardial infarction.
# It was reported at treatment of HSN
** It was sometimes reported during treatment after an acute myocardial infarction
## HSN which is Most often found during treatment (it is frequent: dizziness, renal failure, ipotenziya; sometimes: headache, nausea).

Interaction with other medicines:

At treatment of arterial hypertension valsartany there were no clinically significant interactions with other at the same time used drugs (for example, Cimetidinum, warfarin, digoxin, атенолол, амлодипин, glibenclamide, furosemide, indometacin, a hydrochlorothiazide).
The Kaliysberegayushchy diuretics, drugs of potassium, salts containing the potassium, drugs increasing potassium level in a blood plasma (such as heparin) strengthen development of a hyperpotassemia.
Other antihypertensives and diuretics strengthen anti-hypertensive effect.
The anti-hypertensive effect of drug can be weakened at combined use with non-steroidal anti-inflammatory drugs (NPVP), including the selection inhibitors of cyclooxygenase-2 (TsOG-2) and acetylsalicylic acid more than 3 g/day.
At combined use with APF inhibitors it was reported about reversible increase in concentration of lithium in a blood plasma and development of toxic effects.
Experience of use of a valsartan and the drugs containing lithium is very limited. In case of use of the drugs containing lithium control of level of lithium in a blood plasma is recommended.

Contraindications:

• Hypersensitivity to a valsartan or to drug excipients;
• The abnormal liver functions connected with impassability of bilious ways (including biliary cirrhosis, a cholestasia);
• The expressed renal failure (the clearance of creatinine (CC) less than 10 ml/min.), including the patients who are on a hemodialysis;
• Pregnancy and period of a lactation;
• Age up to 18 years (efficiency and safety are not established);
• A lactose intolerance, a galactosemia or a syndrome of the broken absorption of a glucose/galactose;

With care: arterial hypotension, a hyperpotassemia, a diet with sodium consumption restriction, a hyponatremia, a bilateral stenosis of renal arteries or a stenosis of an artery of the only kidney, primary hyper aldosteronism, an aortal and mitral stenosis, hypertrophic obstructive. cardiomyopathy; the states which are followed by decrease in the volume of the circulating blood (VCB) (including diarrhea, vomiting).

Use at pregnancy and in the period of a lactation

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 expressed decrease in the ABP that can lead to a loss of consciousness and to a collapse.
Treatment: gastric lavage, reception of enough absorbent carbon, intravenous administration of 0,9% of solution of sodium of chloride.
Valsartan is not brought at dialysis in connection with active linkng with proteins of a blood plasma.

Storage conditions:

At a temperature not above 30 °C. To store in the place, unavailable to children! Period of validity 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 40 mg, 80 mg, 160 mg.
On 7, 10 or 14 tablets in the blister from PVC/PE/PVDH / Aluminum foil.
On 2 or 4 blisters on 7 tablets; on 1, 2 or 3 blisters on 10 tablets, on 4 or 7 blisters on 14 tablets together with the application instruction in a pack cardboard.
On 50 or 100 blisters together with application instructions in a cardboard box (for hospitals).