Index of drugs

Treatment of essential hypertension in children and adolescents aged 6 to 18 years and in adults. Treatment of patients in a stable clinical condition with symptomatic heart failure or asymptomatic left ventricular systolic failure after a recent (12 hours to 10 days) myocardial infarction. Treatment of symptomatic heart failure if angiotensin converting enzyme (ACE) inhibitors can not be used or as a combination therapy with ACE inhibitors if beta blockers can not be used.

1 tabl powl. contains 80 mg or 160 mg of valsartan.

Angiotensin II receptor antagonist (AT type₁). Selectively binds to the AT receptor₁by blocking the effects of angiotensin II. It has no agonist activity towards the AT receptor₁it does not bind or block other hormone receptors or ion channels important for regulation in the circulatory system. It is not an ACE inhibitor (kinase II), so it does not increase the effects of bradykinin-dependent effects. In the majority of patients, after administration of a single oral dose, the onset of antihypertensive activity occurs within 2 hours and the maximum reduction of blood pressure is achieved within 4-6 hours. The antihypertensive effect persists for 24 hours after the dose is taken. The bioavailability of valsartan after oral administration is approximately 23%. Valsartan achieves C_max 2-4 h after administration. In 94-97% it is bound to plasma proteins. It is metabolized to a small extent to pharmacologically inactive hydroxymetabolite. It is excreted mainly in unchanged form with faeces (83%) and urine (13%). 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. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (glomerular filtration rate, GFR <60 ml / min / 1.73 m²).

Do not use the preparation 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 impairment without cholestasis, patients with creatinine clearance <10 ml / min and dialysis patients. The safety of valsartan has not been established in patients who have recently had a kidney transplant and in patients with bilateral renal artery stenosis or stenosis of an active kidney. Use with caution in patients with unilateral renal artery stenosis. Due to the risk of hypotension, carefully use in patients with sodium deficiency or dehydrated - before starting treatment with hyponatremia and / or volume of circulating blood should be compensated, for example by reducing the dose of diuretic. Due to the risk of hyperkalemia, the use of potassium supplements, potassium-sparing diuretics, potassium-containing potassium replacers or drugs that increase blood potassium (eg heparin) is not recommended; if such combination therapy is necessary, blood potassium should be closely monitored. In patients after myocardial infarction and in patients with heart failure, caution should be used at the beginning of treatment. In patients who have recently had a myocardial infarction, the concomitant use of valsartan and an ACE inhibitor is not recommended. In patients with heart failure, combination therapy with 3 drugs: ACE inhibitor, β-blocker and valsartan is not recommended. In patients in whom renal function may depend on the activity of the renin-angiotensin 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 and (or) death; since valsartan is an angiotensin II receptor antagonist, it can not be ruled out that the use of valsartan may be associated with impaired renal function. Renal function should be monitored regularly during treatment, especially in patients with heart failure, after myocardial infarction, with renal artery stenosis and in children. 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 recent myocardial infarction is not recommended. 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 concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren increases the risk of hypotension, hyperkalaemia and renal dysfunction (including acute renal failure) - therefore, dual blocking of the RAA system is not recommended by concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren. If the use of a dual RAA blockade is absolutely necessary, it should only be carried out under the supervision of a specialist, and the vital parameters of the patient, such as kidney function, electrolyte concentration and blood pressure should be closely monitored. In patients with diabetic nephropathy, ACE inhibitors and angiotensin II receptor antagonists should not be used concurrently.

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

Hypertension. Adults. Uncommon: vertigo, coughing, abdominal pain, fatigue. Not known: hemoglobin decrease, hematocrit reduction, neutropenia, thrombocytopenia, hypersensitivity (including serum sickness), hyperkalemia, hyponatremia, vasculitis, increased liver enzymes, increased bilirubin in the blood, angioneurotic edema, rash, pruritus, muscle pain , renal failure and impaired renal function, 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 the population of children from 6 to 18 years and 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 with coexisting chronic kidney disease, hyperkalaemia was more frequently observed.Condition after myocardial infarction and / or heart failure. Adults. Common: dizziness, dizziness related to the position of the body, hypotension, orthostatic hypotension, renal failure and renal dysfunction. Uncommon: hyperkalemia, fainting, headache, labyrinthine dizziness, heart failure, cough, nausea, diarrhea, angioneurotic edema, acute renal failure, increased creatinine in the blood, weakness, fatigue. Not known: thrombocytopenia, hypersensitivity (including serum sickness), hyponatraemia, vasculitis, increased liver enzymes, rash, pruritus, muscle pain, increased blood urea nitrogen.

Orally.Adults. Hypertension. The recommended starting dose is 80 mg once a day. The antihypertensive effect appears within 2 weeks, and the maximum antihypertensive effect occurs after 4 weeks. In some patients whose blood pressure is not adequately controlled, the dose can be increased to 160 mg, and up to a maximum of 320 mg. Further lowering of blood pressure can be obtained after using a diuretic such as hydrochlorothiazide. The preparation can be used simultaneously with other antihypertensive drugs.Condition after a recent myocardial infarction. Treatment can be started as early as 12 hours after the diagnosis of myocardial infarction. The starting dose is 20 mg twice daily, then in a few weeks the dose should be gradually increased to 40 mg, 80 mg and 160 mg, given twice a day. The maximum target dose is 160 mg 2 times a day. It is usually recommended that patients should receive a dose of 80 mg twice daily for the first 2 weeks after starting treatment, and the maximum 160 mg administered dose twice daily should be achieved within 3 months. If symptomatic hypotension or renal dysfunction occurs 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 the patient's condition 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 given at intervals of at least 2 weeks until the patient receives the highest dose. 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 may be used in patients who are taking other medicines for the treatment of heart failure. However, concomitant combination therapy with 3 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 adolescents aged 6 to 18 years. Hypertension. Children about the month of <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 the body weight is: ≥ 18 kg to <35 kg - 80 mg; ≥ 35 kg to <80 kg - 160 mg; ≥ 80 kg to ≤ 160 kg - 320 mg. In children and adolescents with mild to moderate hepatic impairment, the dose should not exceed 80 mg daily. No dose adjustment is required in children and adolescents with a creatinine clearance> 30 ml / min - renal function and potassium levels should be monitored. The use in children and adolescents with a creatinine clearance <30 ml / min and in those in whom dialysis is used is not recommended.
The tablets can be taken with or without water.