Universal reference book for medicines
Product name: VALSARTAN ZENTIVA (VALSARTAN ZENTIVA)

Active substance: valsartan

Type: Angiotensin II receptor antagonist

Manufacturer: ZENTIVA (Czech Republic)
Composition, form of production and packaging
The tablets covered with a film cover of
dark pink color, round, biconcave, with risk from one side;
the core on a transverse cut is white or almost white.
1 tab.

valsartan 80 mg

Auxiliary substances: SMCC 90 (microcrystalline cellulose - 32.83 mg, colloidal silicon dioxide - 670 μg) - 33.5 mg, sorbitol 9.25 mg, magnesium carbonate 90 (magnesium carbonate 8.325 mg, pregelatinized starch 832.5 μg, water 92.5 μg ) - 9.25 mg, corn pregelatinized corn starch - 3 mg, povidone K25 - 7.5 mg, sodium stearyl fumarate - 4 mg, sodium lauryl sulfate - 1 mg, crospovidone Type A - 13 mg, silicon dioxide colloidal anhydrous (Aerosil 200 Pharma) - 2 mg.

The composition of the film shell: lactose monohydrate - 327 μg, hypromellose - 2.027 mg, talc - 385 μg, macrogol / PEG 6000 - 324 μg, iron oxide red oxide - 137 μg.

14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (6) - packs of cardboard.
15 pcs.
- blisters (2) - packs of cardboard.
15 pcs.
- blisters (6) - packs of cardboard.
Tablets covered with a film coat of brownish-yellow color, round, biconvex, with a risk on one side;
the core on a transverse cut is white or almost white.
1 tab.

valsartan 160 mg

Auxiliary substances: SMCC 90 (microcrystalline cellulose - 65.66 mg, colloidal silicon dioxide - 1.34 mg) 67 mg, sorbitol 18.5 mg, magnesium carbonate 90 (magnesium carbonate 16.65 mg, pregelatinized starch 1.665 mg, water 185 μg ) - 18.5 mg, corn pregelatinized corn starch - 6 mg, povidone K25 - 15 mg, sodium stearyl fumarate - 8 mg, sodium lauryl sulfate - 2 mg, crospovidone Type A - 26 mg, silicon dioxide colloidal anhydrous (Aerosil 200 Pharma) - 4 mg.

The composition of the film shell: lactose monohydrate - 948 μg, hypromellose - 4.054 mg, talc - 770 μg, macrogol / PEG 6000 - 649 μg, iron oxide oxide yellow - 18 μg, ferric oxide brown oxide - 52 μg, dye indigo carmine aluminum varnish - 9 mcg.

14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (6) - packs of cardboard.
15 pcs.
- blisters (2) - packs of cardboard.
15 pcs.
- blisters (6) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Specific antagonist of angiotensin II receptors.
Selectively blocks receptors of the subtype AT1, which are responsible for the known effects of angiotensin II. The consequence of the blockade of AT1-receptors is an increase in the plasma concentration of angiotensin II, which can stimulate unblocked AT2 receptors.
Valsartan does not have any marked agonistic activity against AT1 receptors.
The affinity of valsartan for the receptors of the AT1 subtype is about 20,000 times higher than in the AT2 receptor subtype.
The likelihood of coughing with valsartan is very low, which is due to the lack of influence on ACE, kininase II, which is responsible for the degradation of bradykinin.

In the treatment of valsartan in patients with hypertension, there is a decrease in blood pressure, not accompanied by a change in heart rate.

After taking the drug inside in a single dose in most patients, the onset of antihypertensive action is noted within 2 hours, and the maximum decrease in blood pressure is achieved within 4-6 hours. After taking the drug, the antihypertensive effect persists for more than 24 hours. With repeated admission, the maximum decrease in blood pressure, of the accepted dose, is usually achieved within 2-4 weeks and maintained at the achieved level during prolonged therapy.
In the case of a combination of the drug with hydrochlorothiazide, a significant additional reduction in blood pressure is achieved. The sudden discontinuation of valsartan is not accompanied by a sharp increase in blood pressure or other undesirable clinical consequences.
The mechanism of action of valsartan in chronic heart failure (CHF) is based on its ability to eliminate the negative consequences of chronic hyperactivation of RAAS and its main effector, angiotensin II, vizoconstriction;
fluid retention in the body; cell proliferation leading to remodeling of target organs (heart, kidneys, vessels); stimulation of excessive synthesis of hormones acting synergistically with RAAS (catecholamines, aldosterone, vasopressin, endothelin). Against the background of the use of valsartan in CHF, prednagruzka decreases, the wedging pressure in the pulmonary capillaries (DZLK) decreases and the diastolic pressure in the pulmonary artery increases, the cardiac output increases. Along with hemodynamic effects, valsartan, due to the mediated blockade of aldosterone synthesis, reduces the retention of sodium and water in the body.
It was found that the drug had no significant effect on the concentration of total cholesterol, uric acid, as well as in the study of fasting - the concentration of triglycerides and glucose in the blood serum.

PHARMACOKINETICS

Suction

After taking the drug, suction of valsartan takes place quickly, but the degree of absorption varies widely.
The average absolute bioavailability is 23%.
In the range of doses studied, the kinetics of valsartan is linear.
With repeated use of the drug, no changes in the kinetic parameters were noted. Food reduces the effect of valsartan by approximately 40% and C ss by approximately 50%, although approximately 8 hours after dosing, the concentration of valsartan in the blood plasma in the food group and in the fasting group was the same. However, this decrease in concentration is not accompanied by a clinically significant decrease in the therapeutic effect, so valsartan can be administered regardless of the intake of food.
Distribution

V d of valsartan in the equilibrium state after intravenous administration is about 17 liters, which indicates that valsartan is not distributed intensively in the tissues.The binding of valsartan to plasma proteins is significant - 94-97%, mainly with albumin.

Metabolism

Valsartan is not significantly metabolized.
Only about 20% of the dose is found in the form of metabolites. In the blood plasma, a pharmacologically inactive hydroxymetabolite is found.
Excretion

In comparison with the hepatic blood flow (about 30 l / h) the plasma clearance of valsartan is relatively small (about 2 l / h).
T 1/2 is about 9 hours. The amount of valsartan emitted through the intestine is 70%. About 30% of the kidneys are excreted, mostly unchanged.
Pharmacokinetics in special clinical cases

In some elderly patients, the systemic effect of valsartan was slightly more pronounced than in young patients, but it was not shown to have any clinical significance.

There was no correlation between renal function and systemic valsartan.
In patients with impaired renal function (CK> 10 ml / min), dose adjustment is not required.The experience of safe use of the drug in patients with CC <10 ml / min and being on hemodialysis is absent. However, valsartan has a high degree of binding to blood plasma proteins, so its elimination in hemodialysis is unlikely.
About 70% of the absorbed dose of valsartan is excreted through the intestine, mostly unchanged.
Valsartan does not undergo significant biotransformation, the systemic action of valsartan does not correlate with the degree of hepatic function impairment. Therefore, patients with hepatic insufficiency of non-biliary origin and in the absence of cholestasis do not require a dose adjustment of valsartan. The use of valsartan in patients with severe impairment of liver function has not been studied.
The mean time to reach C max and T 1/2 of valsartan in patients with CHF is similar to that of healthy volunteers.
Cmax in blood plasma and AUC increase linearly and practically proportionally with increasing dose in the interval of clinical doses (from 40 to 160 mg 2 times / day).
INDICATIONS

- arterial hypertension;

- chronic heart failure (II-IV functional class according to NYHA classification) in patients receiving standard therapy, incl.
diuretics, cardiac glycosides, as well as ACE inhibitors or beta-blockers (not simultaneously) (the use of each of these drugs is not mandatory);
- to improve the survival of patients with acute myocardial infarction and after suffering acute myocardial infarction complicated by left ventricular failure and / or left ventricular systolic dysfunction, with stable hemodynamic parameters.

DOSING MODE

Is taken orally, without chewing, regardless of food intake.

Arterial hypertension

The recommended initial dose is 80 mg 1 time / day, regardless of the race, sex and age of the patient.
The onset of antihypertensive action is observed within 2 hours, the maximum decrease in blood pressure is achieved within 4-6 hours. The antihypertensive effect persists for more than 24 hours. The maximum daily dose is 320 mg. It is possible to combine with diuretics.
Chronic heart failure

For 40 mg (1/2 tablets of 80 mg) 2 times / day, with a gradual increase to 80 mg 2 times / day, with good tolerability - up to 160 mg 2 times / day.
The maximum daily dose is 320 mg in 2 divided doses.
The period after the transferred myocardial infarction

Treatment is started within 12 hours after myocardial infarction with an initial dose of 20 mg 2 times / day, followed by an increase in the dose (40 mg, 80 mg, 160 mg 2 times / day) for several weeks, until the target dose of 160 mg 2 times / day.

Reaching the dose of 80 mg 2 times / day is recommended by the end of the second week, 160 mg 2 times / day - by the end of 3 months of therapy.
The maximum daily dose is 320 mg in 2 divided doses.
Achieving the target dose depends on the tolerability of the drug during the titration period.

In elderly patients, dose adjustment is not required.

In patients with impaired renal function with CK> 10 ml / min, dose adjustment is not required.

In patients with mild and moderate impairment of liver function without development of cholestasis, the maximum daily dose of the drug should not exceed 80 mg.

SIDE EFFECT

Frequency of side effects: very often (> 10%);
often (> 1% and <10%); infrequently (> 0.1% and <1%); rarely (> 0.01% and <0.1%); very rarely (<0.01%), including individual messages; frequency - can not be set.
Patients with hypertension

From the cardiovascular system: unspecified frequency - vasculitis.

From the respiratory system: infrequently - cough.

From the digestive system: infrequently - pain in the abdomen;
unspecified frequency - a violation of liver function, hyperbilirubinemia, increased activity of "liver" transaminases.
From the skin: very rarely - angioedema, skin rash, itching.

From the musculoskeletal system: unspecified frequency - myalgia.

From the side of the urinary system: unspecified frequency - a violation of kidney function, an increase in the concentration of creatinine in the blood serum.

On the part of the hematopoiesis system: unspecified frequency - reduction of hemoglobin and hematocrit, neutropenia, thrombocytopenia.

Allergic reactions: unspecified frequency - reaction of hypersensitivity, serum sickness.

From the senses: infrequently - vertigo.

Other: infrequently - increased fatigue.

Laboratory indices: of unspecified frequency - increase of potassium concentration in blood serum.

Patients after a previous myocardial infarction and / or CHF

From the side of the cardiovascular system: often - orthostatic hypotension and a pronounced decrease in blood pressure;
infrequently - increased symptoms of CHF;unspecified frequency - vasculitis.
From the respiratory system: infrequently - cough.

From the digestive system: infrequently - diarrhea, nausea;
unspecified frequency - impaired liver function.
From the nervous system: often - dizziness, incl.
postural; infrequently - a syncope, a headache.
From the senses: infrequently - vertigo.

From the hematopoiesis: unspecified frequency - thrombocytopenia.

Allergic reactions: very rarely - angioedema;
unspecified frequency - the reaction of hypersensitivity, serum sickness.
From the musculoskeletal system: rarely - rhabdomyolysis;
Unspecified frequency - myalgia.
From the skin: unspecified frequency - skin rash, itching.

From the urinary system: often - a violation of kidney function;
infrequent acute renal failure; unspecified frequency - hypercreatininaemia, increased concentration of urea nitrogen in the blood serum.
From the side of metabolism: infrequently - hyperkalemia.

Other: infrequently - increased fatigue, asthenia.

CONTRAINDICATIONS

- severe violations of the liver, biliary cirrhosis and cholestasis;

- age up to 18 years;

- Pregnancy;

- the period of lactation (breastfeeding);

- lactose intolerance, lactase deficiency or syndrome, glucose-galactose malabsorption;

- Hypersensitivity to the components of the drug.

With caution should take the drug with bilateral stenosis of the renal arteries;
stenosis of the artery of a single kidney; while observing a diet with restriction of consumption of table salt; at conditions accompanied by a decrease in BCC (including diarrhea and vomiting); in patients with severe renal insufficiency (CC <10 ml / min), incl. when carrying out hemodialysis, when used in patients after kidney transplantation; with primary hyperaldosteronism; light and moderate violations of liver function of non-biliary genesis without the phenomena of cholestasis; with mitral and aortic stenoses; with hypertrophic obstructive cardiomyopathy.
PREGNANCY AND LACTATION

Given the mechanism of action of angiotensin II receptor antagonists, the risk to the fetus can not be ruled out.
The effect of ACE inhibitors (drugs that affect RAAS) on the fetus, if prescribed in the II and III trimesters of pregnancy, leads to its damage and death. According to the retrospective data, the risk of the birth of children with congenital defects increases with the use of ACE inhibitors in the first trimester of pregnancy. There are reports of spontaneous abortions, oligohydramnios and renal dysfunction in newborns whose mothers, during pregnancy, were unintentionally receiving valsartan. Valsartan Zentiva, like any other drug that directly affects RAAS, should not be used during pregnancy. If pregnancy is detected during treatment with Valsartan Zentiva, the drug should be discontinued as soon as possible.
Data on the isolation of valsartan with breast milk are absent.
Therefore, do not prescribe the drug during breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER

In patients with impaired renal function with CK> 10 ml / min, dose adjustment is not required.

Use with caution in patients with severe renal insufficiency (CC <10 mL / min), incl.
when carrying out hemodialysis, when used in patients after kidney transplantation.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

In patients with mild and moderate impairment of liver function without development of cholestasis, the maximum daily dose of the drug should not exceed 80 mg.

Contraindicated in severe violations of liver function, biliary cirrhosis and cholestasis.

APPLICATION FOR CHILDREN

Contraindicated in children and adolescents under 18 years.

APPLICATION IN ELDERLY PATIENTS

In elderly patients, dose adjustment is not required.

SPECIAL INSTRUCTIONS

Deficiency in the body of sodium and / or BCC

In patients with severe sodium deficiency and / or reduced bcc, for example, receiving high doses of diuretics, in rare cases after the initiation of therapy with Valsartan Zentiva, severe arterial hypotension may occur.
Before the start of treatment, it is necessary to adjust the sodium and / or BCC deficiency, for example, by lowering the dose of the diuretic.
Stenosis of the renal artery

The use of short-course valsartan in 12 patients with reninvascular hypertension, which developed secondary due to unilateral stenosis of the renal artery, did not lead to significant changes in renal hemodynamics, serum creatinine concentration, or blood urea nitrogen.
However, given that other drugs that affect RAAS can cause an increase in serum urea and creatinine levels in patients with bilateral or unilateral stenosis of the renal artery, it is recommended to monitor these indicators as a precautionary measure.
Chronic heart failure / period after myocardial infarction

In patients with CHF or after myocardial infarction, starting treatment with valsartan, there is often a slight decrease in blood pressure, and therefore it is recommended to monitor BP at the beginning of therapy.
If the recommendations on the dosing regimen are abolished, there is usually no need to cancel the drug due to hypotension.
Due to inhibition of RAAS in sensitive patients, changes in kidney function are possible.
In patients with severe CHF, treatment with ACE inhibitors and angiotensin receptor antagonists may be accompanied by oliguria and / or augmentation of azotemia and in some cases acute renal failure and / or fatal outcome. Therefore, it is necessary to assess the extent of renal dysfunction in patients with heart failure and patients who underwent acute myocardial infarction.
Impaired renal function

The experience of safe use in patients with CC <10 ml / min and in patients on hemodialysis is not available, so use Valsartan Zentiva in such patients is necessary with caution.
In patients with CK> 10 ml / min, dose adjustment is not required.
During treatment with valsartan, the kidney function and the potassium content in the blood plasma must be carefully monitored.

Liver failure

In patients with mild or moderate hepatic insufficiency without the phenomena of cholestasis, Valsartan Zentiva should be used with caution.

Combination Therapy

In CHF valsartan can be prescribed for both monotherapy and together with other agents - diuretics, cardiac glycosides, as well as ACE inhibitors or beta-blockers.
In patients with CHF, caution should be exercised when using a combination of an ACE inhibitor, a beta adrenoblocker and a valsartan. With arterial hypertension, Valsartan Zentiva can be prescribed for both monotherapy and in conjunction with other antihypertensive agents, in particular diuretics. Perhaps the use of valsartan in combination with other drugs administered after myocardial infarction: thrombolytics, acetylsalicylic acid as antiagregatnogo drugs, beta-blockers and inhibitors of HMG-CoA reductase inhibitors (statins).
Impact on the ability to drive vehicles and manage mechanisms

Patients taking Valsartan Zentiva, caution should be exercised when driving and occupations that require high concentration and psychomotor speed reactions (in dizziness and fainting may occur during therapy).
OVERDOSE

Symptoms: marked reduction of blood pressure, which can lead to loss of consciousness and collapse and / or shock.
Treatment: gastric lavage, intake of sufficient amount of activated carbon, intravenous administration of 0.9% sodium chloride solution.
Valsartan is not displayed during dialysis due to severe binding to plasma proteins.
DRUG INTERACTION

With simultaneous use of drugs lithium with ACE inhibitors reported reversible increase lithium content in the blood plasma and the development of toxic effects. Due to the lack of experience in simultaneous use of valsartan and lithium, this combination is not recommended. If necessary, such a combination is recommended to control the content of lithium in the blood plasma.
Potassium-sparing diuretics, potassium supplements, salts containing potassium, drugs that increase the content of potassium in the blood plasma (such as heparin) enhance the development of hyperkalemia. If necessary, concomitant use with valsartan is recommended to control the content of potassium in the blood plasma.
The antihypertensive effect of the drug can be attenuated while the use of NSAIDs, including selective inhibitors of COX-2.
When treating arterial hypertension valsartan had no clinically significant interactions with other drugs applied simultaneously (e.g., cimetidine, warfarin, digoxin, atenolol, amlodipine, glibenclamide, furosemide, indomethacin, hydrochlorothiazide).
Other antihypertensive drugs and diuretics increase the antihypertensive effect.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of no higher than 30 ° C.
Shelf life - 2 years.
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