Instruction for use: Valsacor

Dosage form: film coated tablets

Active substance: Valsartanum

ATX

C09CA03 Valsartan

Pharmacological group

Angiotensin II receptor antagonist [Angiotensin II receptor antagonists (AT1-subtype)]

Nosological classification (ICD-10)

I10 Essential (primary) hypertension: hypertension; Arterial hypertension; Arterial hypertension crisis course; Essential Hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Primary hypertension; Arterial hypertension, complications of diabetes; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; arterial Hypertension; malignant Hypertension; Hypertonic disease; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; Isolated systolic hypertension

I15 Secondary hypertension: Arterial hypertension, complications of diabetes; hypertension; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; hypertension; arterial Hypertension; malignant Hypertension; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; hypertension; Arterial hypertension; Arterial hypertension crisis course; renovascular hypertension; Hypertension symptomatic; Renal hypertension; Renovascular hypertension; renovascular hypertension; Symptomatic hypertension

I21.9 Acute myocardial infarction, unspecified: Changes in left ventricle with myocardial infarction; Changes in the left atrium with myocardial infarction; Myocardial infarction; Myocardial infarction without Q wave; Myocardial infarction without signs of chronic heart failure; Myocardial infarction with unstable angina; Pirouette tachycardia with myocardial infarction

I50.0 Congestive heart failure: anasarca heart; Decompensated congestive heart failure; Congestive heart failure; Congestive heart failure with high afterload; Congestive chronic heart failure; Cardiomyopathy with severe chronic heart failure; Compensated chronic heart failure; Swelling with circulatory failure; Edema of cardiac origin; Swelling of the heart; Edematous syndrome in diseases of the heart; Edematous syndrome in congestive heart failure; Edematous syndrome in heart failure; Edematous syndrome in heart failure or liver cirrhosis; right ventricular failure; Congestive Heart Failure; Heart failure stagnant; Heart failure with low cardiac output; Heart failure is a chronic; Cardiac edema; Chronic decompensated heart failure; Chronic Congestive Heart Failure; Chronic heart failure; Change of liver function in heart failure

I50.9 Heart failure, unspecified: Diastolic rigidity; Diastolic heart failure; Cardiovascular failure; Heart failure with diastolic dysfunction; Cardiovascular failure

Composition

Tablets covered with a film coating.

core

active substance:

Valsartan 80 mg

Auxiliary substances: lactose monohydrate - 30 mg; MCC - 41 mg; Povidone K25 - 1.5 mg; Croscarmellose sodium - 2 mg; Silicon dioxide colloidal - 1 mg; Magnesium stearate 4.5 mg

Membrane film: hypromellose 6c - 3 mg; Titanium dioxide (E171) - 0.68 mg; Ferric dye oxide red (E172) - 0.02 mg; Macrogol 4000 - 0.3 mg

Tablets covered with a film coating.

core

active substance:

Valsartan 160 mg

Auxiliary substances: lactose monohydrate - 60 mg; MCC - 82 mg; Povidone K25 - 3 mg; Croscarmellose sodium - 4 mg; Silicon dioxide colloidal - 2 mg; Magnesium stearate 9 mg

Membrane film: hypromellose 6c - 5.52 mg; Titanium dioxide (E171) - 1.36 mg; Ferric iron oxide yellow (E172) - 0.5 mg; Ferric dye oxide red (E172) - 0.02 mg; Macrogol 4000 - 0.6 mg

Tablets covered with a film coating.

core

active substance:

Valsartan 320 mg

Auxiliary substances: lactose monohydrate - 120 mg; MCC - 164 mg; Povidone K25 - 6 mg; Croscarmellose sodium - 8 mg; Silicon dioxide colloidal - 4 mg; Magnesium stearate - 18 mg

Membrane film: hypromellose 6c - 11.2 mg; Titanium dioxide (E171) 2.4 mg; Ferric iron oxide yellow (E172) - 1 mg; Iron dye red oxide (E172) 0.2 mg; Macrogol 4000 - 1.2 mg

Description of dosage form

Tablets of 80 mg: round, biconcave, with a risk on one side, covered with a film shell of pink color.

View of the fracture: a white rough mass with a film shell of pink color.

Tablets 160 mg: oval, biconcave, with a risk on one side, covered with a film coat of brownish-yellow color.

View of the fracture: a white rough mass with a film coating of a brownish-yellow color.

Tablets 320 mg: oval, biconcave, with a risk on one side, covered with a film shell of light brown color.

View of the fracture: a white rough mass with a film shell of light brown color.

Pharmachologic effect

Mode of action - antihypertensive.

Pharmacodynamics

Valsartan is a selective antagonist of angiotensin II receptor (type AT1) for oral administration, non-protein nature.

Selectively blocks AT1-receptors. The consequence of the blockade of AT1-receptors is an increase in the plasma concentration of angiotensin II, which can stimulate unblocked AT2 receptors, which counterbalances the vasopressor effects associated with the excitation of AT1 receptors. Valsartan has no agonistic activity against AT1 receptors. Its affinity for AT1 receptors is about 20,000 times higher than for AT2 receptors.

Valsartan does not inhibit ACE, also known as kininase II, which converts angiotensin I into angiotensin II and breaks down bradykinin. Due to the lack of influence on ACE, the effects of bradykinin and substance P are not potentiated. The frequency of development of dry cough is lower in patients receiving angiotensin II receptor antagonists (ARA II), in comparison with patients receiving an ACE inhibitor. Valsartan does not interact and does not block the receptors of other hormones or ion channels involved in the regulation of CCC functions.

Use in hypertension in patients older than 18 years

When treating arterial hypertension (AH), valsartan reduces blood pressure without affecting the heart rate.

After ingestion of a single dose of the drug, the antihypertensive effect develops within 2 hours, and the maximum decrease in blood pressure is achieved within 4-6 hours. The antihypertensive effect of valsartan persists for 24 hours after its administration. With the constant use of valsartan, the maximum decrease in blood pressure, regardless of dose, is achieved after 2-4 weeks and is maintained at the reached level during prolonged therapy. Simultaneous use with hydrochlorothiazide allows achieving a significant additional reduction in blood pressure.

Sudden abolition of valsartan is not accompanied by a sharp increase in blood pressure or other undesirable clinical consequences (ie, withdrawal syndrome does not develop). In patients with AH, diabetes mellitus (DM) type 2 and nephropathy, taking valsartan at a dose of 160-320 mg / day, there is a significant decrease in proteinuria (36-44%).

Application after acute myocardial infarction (MI) in patients older than 18 years

When valsartan is used for 2 years, with the onset of admission from 12 hours to 10 days after the onset of myocardial infarction (complicated by left ventricular failure and / or left ventricular systolic dysfunction), the overall mortality, cardiovascular mortality and the time to the first hospitalization for exacerbation decrease The course of CHF, repeated myocardial infarction, sudden cardiac arrest and stroke (without a lethal outcome).

CHF in patients older than 18 years

Using valsartan (at an average daily dose of 254 mg) for 2 years in patients with NYHA class II-IV CHF with a left ventricular ejection fraction (LVEF) of less than 40% and an internal diastolic diameter of more than 2.9 cm / m2 (ACE inhibitors, diuretics, digoxin, beta-blockers), there was a significant reduction in the risk of hospitalization for worsening of CHF flow, slowing of CHF progression, improvement of the NYHA class of CHF functional class, increased LVEF, and menshenie severity of heart failure symptoms and improved quality of life compared with placebo.

Use in patients over 18 years with AH and impaired glucose tolerance

With the use of valsartan and lifestyle changes, there was a statistically significant reduction in the risk of developing diabetes in patients with AH and impaired glucose tolerance. Valsartan had no effect on the incidence of fatal outcomes as a result of cardiovascular events, myocardial infarction and transient ischemic attacks without a lethal outcome, on the frequency of hospitalizations due to exacerbation of CHF or unstable angina, arterial revascularization in this category of patients differing in age, sex and race accessories. In patients receiving valsartan, the risk of developing microalbuminuria was significantly lower than in patients not receiving this therapy.

The recommended initial dose of valsartan in patients with AH and impaired glucose tolerance is 80 mg once a day. If necessary, the dose may be increased to 160 mg.

Application in children and adolescents from 6 to 18 years with AH

In children and adolescents from 6 to 18 years old, valsartan provides a dose-dependent smooth decrease in blood pressure. When valsartan is used, the maximum decrease in blood pressure, regardless of the dose taken internally, is achieved within 2 weeks and is maintained at the achieved level during prolonged therapy.

Pharmacokinetics

Suction. After taking valsartan inside Cmax in the blood plasma is achieved within 2-4 hours. The average absolute bioavailability is 23%. When valsartan is used with food, AUC and Cmax in blood plasma are reduced by 40 and 50%, respectively. However, 8 hours after taking the drug, the plasma concentrations of valsartan taken on an empty stomach and with food are the same. AUC reduction is not accompanied by a clinically significant decrease in the therapeutic effect of valsartan, so the preparation of Valsacor® can be taken regardless of the time of meal.

Distribution. Vd of valsartan in the equilibrium period after IV administration was about 17 L, indicating that there was no pronounced valsartan distribution in the tissues. Valsartan actively binds to blood plasma proteins (94-97%), mainly with albumin.

Metabolism. Valsartan is not subjected to significant biotransformation, only about 20% of the dose taken orally is excreted as metabolites. The hydroxyl metabolite is determined in the blood plasma at low concentrations (less than 10% of the valsartan AUC). This metabolite has no pharmacological activity.

Excretion. Valsartan is biphasic: the α-phase with T1 / 2α is less than 1 hour and the β-phase with T1 / 2β is about 9 hours. Valsartan is excreted mainly unchanged through the intestine (about 83%) and kidneys (about 13%) . After IV introduction, the plasma clearance of valsartan is about 2 l / h, the renal clearance is 0.62 l / h (about 30% of the total clearance). T1 / 2 valsartan is 6 hours.

Pharmacokinetics of special groups of patients

Patients with CHF. In patients with CHF, the time to achieve Cmax and T1 / 2 is similar to that of healthy volunteers. The increase in AUC and Cmax is directly proportional to an increase in the dose of valsartan (from 40 to 160 mg twice a day). The cumulative factor is, on average, 1.7. When administered, the clearance of valsartan is about 4.5 l / h. The age of patients with CHF did not affect the clearance of valsartan.

Patients of advanced age (over 65 years). In some patients over the age of 65, the bioavailability of valsartan was higher than that of young patients, which is not clinically relevant.

Patients with impaired renal function. Renal clearance of valsartan is only 30% of the total clearance, so there is no correlation between renal function and systemic bioavailability of valsartan. Dose adjustments in patients with impaired renal function (Cl creatinine more than 10 mL / min) are not required. The safety of valsartan in patients with Cl creatinine less than 10 ml / min and patients on hemodialysis is not established, therefore, in such patients the drug should be used with caution. Since the degree of binding of valsartan to plasma proteins is high, its excretion in hemodialysis is unlikely.

Patients with impaired hepatic function. About 70% of the absorbed dose of valsartan is excreted through the intestine, mostly unchanged. Valsartan is not significantly metabolized. In patients with mild or moderate impairment of liver function, a 2-fold increase in AUC of valsartan was observed compared with that in healthy volunteers. However, there is no correlation between valsartan AUC values and the degree of hepatic function impairment. The use of valsartan in patients with severe impairment of liver function has not been studied.

Patients from 6 to 18 years. The pharmacokinetics of valsartan in children and adolescents 6 to 18 years old does not differ from the pharmacokinetics of valsartan in patients older than 18 years.

Indications of the drug Valsacor

Patients over 18 years of age

arterial hypertension.

Chronic heart failure (NYHA class II-IV functional class) as part of complex therapy (against standard therapy) in patients not receiving ACE inhibitors;

Increased survival of patients after acute myocardial infarction complicated by left ventricular failure and / or left ventricular systolic dysfunction (LV), with stable hemodynamic parameters.

Patients 6 to 18 years of age

Arterial hypertension in children and adolescents from 6 to 18 years.

Contraindications

Increased sensitivity to valsartan or other components of the drug;

Severe violations of the liver (more than 9 points on the scale Child-Pugh), biliary cirrhosis and cholestasis;

Simultaneous use with aliskiren in patients with diabetes mellitus or moderate and severe renal dysfunction (Cl creatinine less than 60 mL / min);

Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption syndrome, as the composition of the drug Valsacor® includes lactose;

pregnancy;

The period of breastfeeding;

Age up to 6 years - according to indications arterial hypertension, up to 18 years - according to other indications.

With caution: hyperkalemia; Simultaneous use of potassium-sparing diuretics; Preparations of potassium; Potassium-containing food additives or other drugs that can increase the potassium content in the blood plasma (eg heparin); Light and moderate violations of the liver function of non-biliary genesis without the phenomena of cholestasis; Severe renal dysfunction (Cl creatinine less than 10 ml / min - no clinical data), renal dysfunction in patients 6-18 years of age (Cl creatinine less than 30 ml / min), incl. Hemodialysis, hyponatremia, adherence to a diet with restriction of consumption of table salt, conditions accompanied by a decrease in BCC (including diarrhea, vomiting); Bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney; Condition after kidney transplantation; Primary hyperaldosteronism, in patients with chronic cardiac insufficiency III-IV functional class (according to NYNA); The kidney function of which depends on the state of RAAS; Stenosis of the aortic and / or mitral valve; Hypertrophic obstructive cardiomyopathy (GOKMP), in patients with hereditary angioedema or angioneurotic edema on the background of previous therapy with ARA II or ACE inhibitors.

It is not recommended to use ARA II, including valsartan, simultaneously with ACE inhibitors, since their simultaneous use does not have advantages over monotherapy with valsartan or ACE inhibitor with respect to total mortality.

Application of pregnancy and breastfeeding

The use of ARA II in the first trimester of pregnancy is not recommended. The use of ARA II is contraindicated in the II-III trimesters of pregnancy, since the use of fetotoxic effects in the II-III trimesters of pregnancy can cause fetotoxic effects (decreased kidney function, low blood pressure, slowing ossification of the fetal bones) and neonatal toxic effects (renal failure, arterial hypotension, hyperkalemia).

If nevertheless used the drug in the II-III trimesters of pregnancy, then it is necessary to carry out ultrasound of the kidneys and bones of the fetal skull.

When planning pregnancy, the patient is recommended to be transferred to alternative antihypertensive therapy taking into account the safety profile. When confirming the pregnancy, the preparation Valsacor® should be canceled as soon as possible.

Newborns, whose mothers received ARA II during pregnancy, need medical supervision, since There is a risk of developing arterial hypotension. There is no data on the isolation of valsartan in breast milk. Therefore, the question of stopping breastfeeding or abolishing valsartan therapy and transferring to alternative antihypertensive therapy should be resolved taking into account the safety profile.

Side effects

Classification of the frequency of development of side effects of the World Health Organization (WHO): very often - ≥1 / 10; Often from ≥1 / 100 to <1/10; Infrequently - from ≥1 / 1000 to <1/100; Rarely - from ≥1 / 10000 to <1/1000; Very rarely - <1/10000; Frequency is unknown - cannot be estimated based on available data.

The safety profile of valsartan in patients with AH at the age of 6 to 18 years does not differ from the safety profile of valsartan in patients with AH older than 18 years.

Arterial hypertension

On the part of the blood and lymphatic system: the frequency is unknown - a decrease in hemoglobin, a decrease in hematocrit, neutropenia, thrombocytopenia.

On the part of the immune system: the frequency is unknown - hypersensitivity reactions, including serum sickness.

From the side of metabolism and nutrition: the frequency is unknown - an increase in the content of potassium in the blood serum, hyponatremia.

From the side of the organ of hearing and labyrinthine disturbances: infrequently - vertigo.

From the side of the vessels: the frequency is unknown - vasculitis.

From the respiratory system, chest and mediastinum: infrequently - cough.

From the digestive tract: infrequently - pain in the abdomen.

On the part of the liver and bile ducts: the frequency is unknown - a violation of the liver, including an increase in the concentration of bilirubin in the blood plasma.

From the skin and subcutaneous tissues: the frequency is unknown - angioedema, skin rash, skin itch, bullous dermatitis.

From the side of the musculoskeletal and connective tissue: the frequency is unknown - myalgia.

From the side of the kidneys and urinary tract: the frequency is unknown - renal dysfunction and kidney failure, increased serum creatinine concentration.

General disorders and disorders at the injection site: infrequently - increased fatigue.

In the course of clinical trials, the following adverse events were observed in patients with AH, the causal relationship of which was not established with the use of valsartan: arthralgia, asthenia, back pain, diarrhea, dizziness, insomnia, decreased libido, nausea, peripheral edema, pharyngitis, rhinitis, Sinusitis, upper respiratory tract infections.

After suffering acute myocardial infarction and / or chronic heart failure (NYHA functional class II-IV)

On the part of the blood and lymphatic system: the frequency is unknown - thrombocytopenia.

On the part of the immune system: the frequency is unknown - hypersensitivity reactions, including serum sickness.

From the side of metabolism and nutrition: infrequently - hyperkalemia, the frequency is unknown - an increase in potassium in the blood serum, hyponatremia.

From the nervous system: often - dizziness, postural dizziness; Infrequently - a syncope, a headache.

From the side of the organ of hearing and labyrinthine disturbances: infrequently - vertigo.

From the heart: infrequently - increased symptoms of CHF.

From the side of the vessels: often - marked decrease in blood pressure, orthostatic hypotension; Frequency is unknown - vasculitis.

From the respiratory system, chest and mediastinum: infrequently - cough.

From the digestive tract: infrequently - nausea, diarrhea.

From the side of the liver and biliary tract: the frequency is unknown - a violation of the liver.

From the skin and subcutaneous tissues: infrequently - angioedema, frequency unknown - skin rash, skin itch, bullous dermatitis.

From the musculoskeletal and connective tissue: rarely - rhabdomyolysis; Frequency is unknown - myalgia.

From the side of the kidneys and urinary tract: often - a violation of kidney function and kidney failure; Infrequently - acute renal failure, increased serum creatinine concentration; Frequency unknown - increase in urea nitrogen in blood plasma.

General disorders and disorders at the injection site: infrequently - asthenia, fatigue.

Interaction

Simultaneous use is contraindicated

The simultaneous use of ARA II, including valsartan, or ACE inhibitors with aliskiren is contraindicated in patients with diabetes or moderate and severe renal impairment (Cl creatinine less than 60 mL / min).

Simultaneous use is not recommended

Lithium. Simultaneous use with lithium preparations is not recommended. Possibly a reversible increase in the concentration of lithium in blood plasma and an increase in its toxic effect. The risk of toxic manifestations associated with the use of lithium drugs may be further increased with simultaneous use with the drug Valsacor® and diuretics. If it is necessary to simultaneously apply with lithium preparations, the concentration of lithium in the blood plasma should be carefully monitored.

Potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium preparations, potassium-containing food supplements and other drugs and substances that can cause hyperkalemia (eg, heparin). If it is necessary to simultaneously apply with drugs that affect the potassium content, it is recommended to monitor the potassium content in the blood plasma

Use with caution at the same time

Double blockade of RAAS. In some patients, double blockade of RAAS was accompanied by the development of arterial hypotension, fainting, hyperkalemia and impaired renal function (including acute renal failure (ARF).) Caution should be exercised while using ARA II, including valsartan with drugs that affect RAAS, such as inhibitors ACE or aliskiren.

NSAIDs, incl. Selective inhibitors of COX-2, acetylsalicylic acid at a dose of more than 3 g / day and nonselective NSAIDs. With simultaneous use with valsartan, it is possible to reduce the antihypertensive effect, increase the risk of kidney dysfunction and increase the potassium content in blood plasma. Prior to the initiation of combination therapy, it is recommended to evaluate the function of the kidneys, as well as to correct the disturbances of the water-electrolyte balance.

Protein-carriers. In vitro studies on liver cultures have shown that valsartan is a substrate for OATP1B1 / OATP1B3 and MRP2 carrier proteins. The simultaneous use of valsartan with inhibitors of the OATP1B1 / OATP1B3 carrier protein (rifampicin, cyclosporin) or MRP2 (ritonavir) may increase the systemic exposure of valsartan (Cmax and AUC). Caution should be exercised at the beginning of simultaneous use with the above drugs or after their withdrawal.

Lack of drug interaction

There were no clinically significant interactions with the following drugs: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine and glibenclamide, hydrochlorothiazide, amlodipine and glibenclamide.

Patients from 6 to 18 years. In children and adolescents, AH is often associated with impaired renal function. The simultaneous use of valsartan with other drugs that affect RAAS can cause an increase in potassium levels in plasma in these patients. Care should be taken when applying the above combination at the same time and regularly monitor kidney function and potassium levels in the blood plasma in this group of patients.

Dosing and Administration

Inside, regardless of meal time.

Patients over 18 years of age

Arterial hypertension. The recommended initial dose of Valsacor® is 80 mg once a day, regardless of race, age or sex of the patient. Antihypertensive effect develops within 2 weeks and reaches its maximum after 4 weeks. Patients who cannot achieve adequate control of blood pressure, a daily dose of valsartan can be gradually increased to a maximum daily dose of 320 mg.

In order to further reduce blood pressure, it is possible to use diuretics (hydrochlorothiazide), as well as simultaneous use of other antihypertensive agents.

CHF. The recommended initial dose of Valsacor® is 40 mg 2 times a day. The dose of the drug should be gradually increased for at least 2 weeks to 80 mg twice a day, and with good tolerability - up to 160 mg 2 times a day. The maximum daily dose is 320 mg in two divided doses. It may be necessary to reduce the dose of concurrently taken diuretics.

Possible simultaneous use with other drugs intended for the treatment of CHF. However, simultaneous therapy with drugs of three classes: valsartan, ACE inhibitors and beta-blockers is not recommended.

Assessment of patients with CHF should include monitoring of kidney function.

Application after acute MI. Treatment should be started within 12 hours after the development of acute MI in the presence of stable indicators of hemodynamics. After applying the initial dose of 20 mg twice a day (1/2 of 40 mg), the dose of Valsacor® can be gradually increased by titration up to: 40, 80 and 160 mg twice a day for several weeks. The maximum daily dose is 320 mg in 2 divided doses. It is recommended to increase the dose to 80 mg twice a day by the end of the 2nd week, and the maximum target dose of 160 mg 2 times a day can be achieved by the end of the third month of therapy with the drug Valsacor®. The achievement of the target dose depends on the tolerability of valsartan during the titration period of the doses.

With the development of excessive blood pressure lowering, accompanied by clinical manifestations, or impaired renal function, the dose of the drug should be reduced.

Possible simultaneous use with other drugs, including. Thrombolytic agents, acetylsalicylic acid as an antiplatelet agent, beta-adrenoblockers and inhibitors of HMG-CoA reductase (statins). Simultaneous use with ACE inhibitors is not recommended.

Assessment of patients after acute MI should include monitoring of kidney function.

Patients 6 to 18 years of age

AG. The recommended initial dose of the drug Valsacor® in children and adolescents from 6 to 18 years is 40 mg with a body weight of the child less than 35 kg and 80 mg with a body weight of the child exceeding 35 kg. It is recommended to correct the dose taking into account the decrease in blood pressure. The maximum recommended daily doses are shown below.

With a body weight of ≥8 and <35 kg, the maximum recommended daily dose is 80 mg; From 35 to <80 kg - 160 mg; From ≥80 to ≤160 kg - 320 mg.

The use of higher doses is not recommended.

CHF and transferred MI. The drug Valsacor® is not recommended for the treatment of CHF and advanced acute myocardial infarction in patients younger than 18 years of age.

Patients of advanced age. Correction of the dose of the drug in patients older than 65 years is not required.

Impaired renal function. Correction of the dose in patients with Cl creatinine more than 10 ml / min is not required. The simultaneous use of the drug Valsacor® with aliskiren in patients with moderate and severe renal dysfunction (Cl creatinine less than 60 ml / min) is contraindicated.

Violation of the function of the liver. In patients with mild or moderate impairment of non-biliary liver function without cholestasis, the drug should be used with caution, the daily dose should not exceed 80 mg.

Patients with diabetes mellitus. The simultaneous use of the drug Valsacor® with aliskiren in patients with diabetes is contraindicated.

Overdose

Symptoms: The main expected manifestation of valsartan overdose is a marked decrease in blood pressure, which can lead to impaired consciousness, collapse and / or shock.

Treatment: symptomatic, it is recommended to induce vomiting and rinse the stomach. With the development of a marked decrease in blood pressure, it is necessary to transfer the patient to the supine position with the legs raised upwards, and / or to introduce a 0.9% solution of sodium chloride. It is recommended that the heart and respiratory system, bcc and the amount of urine be regularly monitored. Hemodialysis is ineffective.

Special instructions

Hyperkalemia. With simultaneous use of potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium preparations, potassium-containing salt substitutes or other drugs capable of increasing the potassium content in the blood plasma (eg heparin), care should be taken. It is necessary to regularly monitor the potassium content in the blood plasma.

Impaired renal function. Patients with impaired renal function do not need to change the dose of the drug. Because There are no data on the use of the drug in severe renal failure (Cl creatinine less than 10 ml / min or 0.167 ml / s) and in patients on hemodialysis, in such cases, the drug is recommended to use with caution.

The simultaneous use of valsartan with aliskiren in patients with moderate and severe impairment of renal function (Cl creatinine less than 60 ml / min) is contraindicated.

Violation of the function of the liver. In patients with mild and moderate impairment of liver function without cholestasis, the preparation Valsacor® should be used with caution.

Patients with hyponatraemia and / or dehydration. In patients with severe hyponatraemia and / or dehydration, for example due to the administration of large doses of diuretics, in rare cases, an initial arterial hypotension with clinical manifestations may develop at the beginning of therapy with Valsacor®. Before treatment, it is recommended to restore the sodium and / or BCC content, in particular, by reducing the dose of diuretics.

Stenosis of the renal artery. The use of short-course valsartan in patients with reninvascular hypertension, which developed secondary to stenosis of the artery of a single kidney, does not cause significant changes in renal hemodynamics, creatinine or urea nitrogen in serum. However, considering that other drugs that affect RAAS can cause an increase in serum urea and creatinine in patients with bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney, it is necessary to regularly monitor the concentrations of creatinine and residual urea nitrogen in the serum.

Condition after kidney transplantation. The safety of Valsacor® in patients who have recently undergone kidney transplantation has not been established.

Primary hyperaldosteronism. Patients with primary hyperaldosteronism are resistant to antihypertensive drugs that affect RAAS; therefore, such patients are not recommended for using Valsacor®.

Stenosis of the aortic and / or mitral valves, GOKMP. The drug Valsacor ® should be used with caution in patients with hemodynamically significant stenosis of the aortic and / or mitral valves or with GOKMP.

The period after the transferred MI. Simultaneous use with ACE inhibitors is not recommended, because Has no additional clinical advantages over monotherapy and increases the risk of developing adverse events.

The use of valsartan in patients after myocardial infarction often leads to a slight decrease in blood pressure, but the cessation of therapy due to arterial hypotension is usually not required if you follow the recommendations for dosing the drug.

Therapy with Valsacor® should be started cautiously. Assessment of patients after acute myocardial infarction should include monitoring of kidney function.

Possible simultaneous use in acute MI with other drugs: thrombolytics, acetylsalicylic acid, beta-adrenoblockers and inhibitors of HMG-CoA reductase (statins).

CHF. In patients with CHF, simultaneous use of three classes of drugs is not recommended: ACE inhibitors, beta-blockers and valsartan, This therapy did not give an additional clinical effect, while the risk of developing unwanted phenomena increased. Usage in patients with CHF is usually accompanied by a decrease in blood pressure, but with the recommendations for the selection of doses, treatment rarely requires withdrawal due to hypotension. Therapy with Valsacor® in patients with CHF should be started with caution. Due to inhibition of RAAS activity in some patients (for example, in patients with CHF III-IV functional class according to the classification of NYNA, the function of the kidneys depends on the state of RAAS) against the background of therapy with ACE inhibitors, a change in renal function is possible: development of oliguria and / or progressive azotemia; Rare cases - ARF and / or death. The drug Valsacor ® blocks the receptors of angiotensin II, so patients with CHF need regular monitoring of kidney function.

Angioedema in history. Among patients with angioneurotic edema on the background of therapy with Valsacor®, there have been cases of angioedema development in the anamnesis, incl. And on ACE inhibitors. With the development of angioedema, immediately discontinue the drug and exclude the possibility of repeated use.

Special information on excipients

The preparation Valsacor® contains lactose, therefore it should not be used in the following conditions: lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

Influence on the ability to perform potentially hazardous activities requiring special attention and quick reactions (for example, vehicle management, work with moving mechanisms). Due to the possibility of dizziness or weakness on the background of the use of the drug Valsakor®, care must be taken when driving vehicles and engaging in potentially hazardous activities.

Release form

Tablets, film-coated, 80 mg, 160 mg. By 7, 10, 14 or 15 of the table. In a blister (contour acrylic packaging) from the combined material of PVC / PE / PVDC-aluminum foil. By 2, 4, 8, 12, 14 or 20 bl. (Contour cell packings) (according to Table 7), or 2, 3, 6 or 9 bl. (Contour cell packs) (10 tabl.), Or 1, 2, 4, 6, 7 or 10 bl. (Contour cell packings) (14 tables each), or 2, 4 or 6 bl. (Contour cell packings) (15 tables each) are placed in a cardboard package.

Film-coated tablets, 320 mg. By 10, 14 or 15 tables. Blister of combined PVC / PE / PVDH-aluminum foil. By 2, 3 or 14 bl. (On 10 tab.), Or on 1, 2, 4, 7 or 10 bl. (According to 14 tables), or 2 bl. (15 tables each) are placed in a cardboard box.

A comment

The results of the conducted studies demonstrated the following data:

- Valsacor® is an effective and safe antihypertensive drug for treating patients with mild to moderate AH1.

- treatment with Valsacor® leads to an improvement in the symptoms of androgen deficiency, achievement of the target blood pressure level, improvement of the daily BP profile, which also confirms the high efficacy and safety of the drug2.

- use of Valsacor® in patients with heart failure.

The study showed that a 4-month treatment with Valsacor improves the objective and subjective clinical state of patients with heart failure and leads to positive changes in the NYHA functional class. There was an increase in LVEF by 15% 3.

- use of Valsacor® in patients with myocardial infarction.

The study demonstrated a strong persistent antihypertensive effect of Valsacor in patients with myocardial infarction and hypertension. Valsacor® can serve as an alternative to ACE inhibitors, as it has a protective effect, protecting against cardiovascular complications after MI and AH 4.

- Valsartan and violation of diastolic function of the left ventricle.

The experience of using Valsacor® in the form of monotherapy or in combination with hydrochlorothiazide suggests that the drug has good antihypertensive efficacy, has a positive effect on the state of LV diastolic function in patients with initial impairment of it, reduces the activity of nonspecific inflammation and the degree of microalbuminuria. Treatment with preparations of Valsacor®, Valsacor® H 80 and Valsacor® H 160 was not accompanied by the development of adverse reactions3.

- According to the international multicentre study VICTORY in patients with AH 1-2 degree valsartan monotherapy (Valsacor®) and combination with hydrochlorothiazide (Valsacor® H160) significantly reduces the levels of SAD and DAD to normal values. As a result of valsartan therapy and its combination with hydrochlorothiazide, the target values of blood pressure were achieved in 91% of all patients participating in the study. High efficacy and good tolerability of the drug were noted6.

Thus, the results of the conducted studies confirmed the high efficacy and good tolerability of the preparation Valsacor® and its fixed combinations with hydrochlorothiazide in the treatment of patients with arterial hypertension. Patients who underwent MI have the same efficacy in reducing cardiovascular complications, as with ACE inhibitors.

Literature

1. Ostroumova OD, Guseva TF, Shorikova EG The use of the preparation Valsacor® in arterial hypertension: the results of the own Slovenian multicenter study / / RMZ.- Volume 18.- ¹2 .- 2010.

2. Vertkin AL And others. Blockers of receptors 1 of the type of angiotensin II and erectile function // Journal of "Arterial hypertension" .- Volume 17.- ¹2 / 2011.

3. Maksimov L., Derbentseva EA, Dralova OV, Ostroumova O.D. Use of the blocker of AT1-receptors of angiotensin II valsartan in patients with chronic heart failure. Journal of Heart Failure, 2010; 11, No. 5 (61): 307-311.

4. Korytko IN, Akmanova NM, Lagkuti O.T. The experience of using valsartan (Valsacor®) in the treatment of hypertension in patients with myocardial infarction. - "Faces of Ukraine." - 2010 - No. 8.- (144) .- p. 64-66.

5 Svishchenko EP, Matova OO, Mishchenko LA Diastolic LV dysfunction in patients with essential hypertension: the possibility of correction with valsartan .- Arterial hypertension .- 2012- 2 (22) .- 36-43.

6. Chazova IE, Martynyuk TV The first results of the international clinical study VICTORY: efficacy and safety of antihypertensive monotherapy valsartan and its fixed combination with hydrochlorothiazide in different dose regimens in patients with arterial hypertension of the 1 st degree. // Systemic hypertension .- 2015. - 12 (2) .- 71-82.

Conditions of supply of pharmacies

On prescription.

Storage conditions of the drug Valsacor

At a temperature of no higher than 25 ° C, in the original packaging.

Keep out of the reach of children.

The shelf life of the drug Valsacor

5 years.

Do not use beyond the expiration date printed on the package.