Index of drugs

Treatment of primary hypertension in adults and hypertension in children and adolescents from 6 to 18 years of age. Treatment of adult patients clinically stable with symptomatic heart failure or asymptomatic left ventricular systolic dysfunction after the (from 12 h to 10 days) myocardial infarction. Treatment of symptomatic heart failure in adult patients in situations where ACE inhibitors can not be used or in combination therapy with ACE inhibitors when beta-blockers can not be used.

1 tabl powl. contains 80 mg or 160 mg of valsartan. The tablets contain lactose.

Valsartan is an active, potent and specific angiotensin II receptor antagonist. It acts selectively on the AT receptor subtype₁by blocking the effects of angiotensin II. It has no agonist activity towards the AT receptor₁, is also not an inhibitor of angiotensin convertase (kininase II) - an enzyme that converts angiotensin I into angiotensin II and breaks down bradykinin. Valsartan does not bind to and blocks other hormone receptors and ion channels, which play a role in the regulation of cardiovascular function. The onset of antihypertensive activity occurs within 2 h, and the maximum reduction of pressure is achieved within 4-6 h and lasts for 24 h. The bioavailability is 23%. It is strongly bound to plasma proteins (94-97%), mainly with albumin. It is excreted mainly in unchanged form with bile (83%) and urine (13%), to a small extent it is metabolized to pharmacologically inactive hydroxymetabolite. T_0,5 is 6 hours.

Hypersensitivity to valsartan or to any of the excipients. Severe hepatic dysfunction, liver biliary cirrhosis and cholestasis. II and III trimester of pregnancy. Concurrent use of angiotensin receptor antagonists (including valsartan) or ACE inhibitors and aliskiren in patients with diabetes or renal insufficiency (GFR <60 ml / min / 1.73 m²).

Due to lack of safety experience, caution should be exercised in patients with creatinine clearance <10 ml / min and in dialysis patients. In rare cases, symptomatic hypotension may occur at the beginning of treatment in patients with hyponatremia and / or in dehydration, eg due to high doses of diuretics. Sodium deficiency and / or circulating blood volume should be corrected before starting treatment, eg by reducing the dose of diuretic. In patients with bilateral renal artery stenosis or artery stenosis of the sole active kidney, the safety of the preparation has not been established. Short-term administration of valsartan to patients with secondary renal hypertension in relation to unilateral renal artery stenosis did not induce any significant changes in renal hemodynamics, creatinine or blood urea nitrogen. However, as other medicines that affect the renin-angiotensin-aldosterone system may increase blood urea and serum creatinine in patients with unilateral renal artery stenosis, regular monitoring of renal function is recommended. There is no experience regarding the safety of the preparation in patients who have recently had a kidney transplant. The preparation should not be used in patients with primary hyperaldosteronism. Particularly cautiously use in patients with aortic or mitral valve stenosis or hypertrophic cardiomyopathy with narrowing of the left ventricle outflow pathway. Use with caution in patients with mild to moderate hepatic dysfunction without cholestasis. In patients after recent myocardial infarction, concomitant use of valsartan and Captopril is not recommended - combined use increases the risk of side effects compared to monotherapy. Caution should be exercised at the beginning of treatment in patients after myocardial infarction. The assessment of patients after myocardial infarction should always include assessment of renal function.Use of the preparation in patients after myocardial infarction usually results in lowering of blood pressure, but discontinuation of the drug is usually not necessary. In patients with heart failure, the concomitant use of an ACE inhibitor, a β-blocker and valsartan increases the risk of side effects in the absence of clinical benefit and therefore combination therapy is not recommended. Caution should be exercised when initiating therapy in patients with heart failure. Use of the preparation in patients with heart failure usually causes a decrease in blood pressure, but discontinuation due to persistent symptomatic hypotension is not usually necessary. In patients in whom renal function may depend on the activity of the renin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure), treatment with ACE inhibitors has been associated with oliguria and / or progressive azotemia and, in rare cases, with acute renal failure. kidney and / or death; it can not be ruled out that the use of valsartan may be associated with impaired renal function. The treatment should be discontinued immediately in patients who have had angioneurotic edema and should not be re-used in these patients. Due to the risk of hypotension, syncope, hyperkalemia and renal dysfunction (including acute renal failure), dual RAA blocking is not recommended (eg, by the combined use of an angiotensin II receptor antagonist with an ACE inhibitor or aliskiren); if the use of the RAA double block is absolutely necessary, it should only be carried out under the supervision of a specialist. At the same time, angiotensin II receptor antagonists and ACE inhibitors should not be used in patients with diabetic nephropathy. During treatment with valsartan, renal function and serum potassium should be carefully monitored. This is particularly important in conditions that may worsen the kidneys (fever, dehydration). Clinical experience with the administration of valsartan to children and adolescents with mild or moderate hepatic impairment is limited. The use of valsartan in children and adolescents with a creatinine clearance <30 ml / min and in those in whom dialysis is administered is not recommended. The safety and efficacy of valsartan in children <6 years of age have not been established. The use of valsartan in children and adolescents <18 years with heart failure and after a recent myocardial infarction is not recommended. Due to the lactose content, the preparation should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption.

The use of angiotensin II receptor antagonists during the first trimester of pregnancy is not recommended (there is a risk of teratogenicity). Use in the second and third trimester of pregnancy is contraindicated. Angiotensin II receptor antagonists administered in the second and third trimester of pregnancy have toxic effects on fetal development (deterioration of renal function, oligohydramnios, delayed ossification of the skull) and newborn (renal failure, hypotension, hyperkalemia) - when exposure to the drug occurred from the second trimester pregnancy, ultrasound examination of the fetus skull and kidneys is recommended; children whose mothers took the drug during pregnancy should be closely monitored for hypotension. The use of valsartan during breast-feeding is not recommended.

Hypertension. Uncommon: vertigo, coughing, abdominal pain, fatigue. Not known: hemoglobin decreased, hematocrit decreased, neutropenia, thrombocytopenia, hypersensitivity (including serum sickness), hyperkalemia, hyponatraemia, vasculitis, increased liver enzymes, increased bilirubin in the blood, angioneurotic edema, rash, pruritus, muscle pain , renal failure and renal impairment, increase in blood creatinine. Children. With the exception of single gastrointestinal disorders (abdominal pain, nausea, vomiting) and dizziness, there were no significant differences in the type, frequency and severity of side effects between the safety profile in children from 6 to 18 years and in the adult population. During the one-year treatment, no effects on the neurocognitive function and development of children from 6 to 16 years were observed.One study reported 2 deaths and isolated cases of significant increases in hepatic transaminase levels. These events occurred in the population of patients with significant coexisting diseases. The causal relationship with treatment with valsartan has not been established. In children and adolescents from 6 to 18 years of age, hyperkalaemia has been observed more frequently with coexisting chronic kidney disease.Condition after myocardial infarction and / or heart failure. Common: dizziness, dizziness related to the position of the body, hypotension, orthostatic hypotension, renal failure and renal dysfunction. Uncommon: hyperkalemia, syncope, headache, diarrheal headache, heart failure, cough, nausea, diarrhea, angioneurotic edema, acute renal failure, increased creatinine in the blood, asthenia, fatigue. Not known: thrombocytopenia, hypersensitivity (including serum sickness), hyponatraemia, vasculitis, increased liver enzymes, rash, pruritus, myalgia, increase in blood urea nitrogen.

Orally.Adults. Hypertension. The recommended dose is 80 mg once a day. The antihypertensive effect is noticeable within 2 weeks and full effect is achieved within 4 weeks. In some patients whose blood pressure is not adequately controlled, the dose can be increased to 160 mg, up to a maximum of 320 mg. The preparation can be used simultaneously with other antihypertensive drugs. Adding a diuretic such as hydrochlorothiazide will allow a greater reduction in blood pressure in these patients.Fresh myocardial infarction. In clinically stable patients, treatment can be started 12 h after myocardial infarction, the initial dose is 20 mg twice daily, then the dose should be gradually increased over a few weeks to 40 mg, 80 mg and 160 mg twice daily. The maximum target dose is 160 mg 2 times a day. It is usually recommended that a dose of 80 mg twice daily is introduced within 2 weeks after the start of treatment, and the maximum target dose of 160 mg administered twice daily should be administered within 3 months, depending on the patient's tolerance. If symptomatic hypotension or renal impairment occurs, a dose reduction should be considered. Valsartan can be used in patients who are taking other medicines for the treatment of myocardial infarction, such as thrombolytics, Acetylsalicylic acid, β-blockers, statins and diuretics. Concomitant use with ACE inhibitors is not recommended. The assessment of patients after myocardial infarction should always include assessment of renal function.Heart failure. The recommended starting dose is 40 mg 2 times a day. Increasing the dose to 80 mg and 160 mg twice daily should be carried out at intervals of at least two weeks to achieve the highest dose tolerated by the patient. If you are taking a diuretic at the same time, you should consider reducing the dose. The maximum daily dose used in clinical trials was 320 mg valsartan in divided doses. Valsartan can be used to treat heart failure. However, combination therapy with three drugs (valsartan, ACE inhibitor and β-blocker) is not recommended. Evaluation of patients with heart failure should always include assessment of renal function.Special groups of patients. In patients with mild to moderate hepatic impairment without cholestasis, the maximum dose is 80 mg per day. No dose adjustment is required in adult patients with creatinine clearance> 10 ml / min and in elderly patients.Children and youth. Hypertension. Children 6-18 years old: oh. <35 kg the starting dose is 40 mg once a day; about mc. ≥35 kg 80 mg once a day. The dose of the preparation should be adjusted depending on the obtained antihypertensive effect. The maximum dose depending on body weight is: ≥18 kg to <35 kg 80 mg; ≥35 kg to <80 kg 160 mg; ≥80 kg to ≤160 kg 320 mg. The use of the preparation in children and adolescents with a creatinine clearance <30 ml / min and those in whom dialysis is used is not recommended. No dose adjustment is required in children and adolescents with a creatinine clearance> 30 ml / min. The kidney function and blood potassium should be closely monitored.In children and adolescents with mild to moderate hepatic impairment the dose should not exceed 80 mg.
The tablets should be taken with or without water.