Index of drugs

Treatment of essential hypertension. Treatment of patients in a clinically stable condition with symptomatic heart failure or asymptomatic left ventricular systolic failure after a recent (12 hours - 10 days) myocardial infarction. Treatment of symptomatic heart failure if ACE inhibitors can not be used or added to ACE inhibitors if beta blockers can not be used.

One tablet contains 80 mg or 160 mg of valsartan.

Valsartan is an orally active, potent and specific angiotensin II receptor antagonist. It acts selectively on the AT1 receptor subtype. Increased plasma levels of angiotensin II after blocking the AT1 receptor by valsartan may stimulate the AT2 receptor, which acts antagonistically to the action of the AT1 receptor. Valsartan does not even show partial agonist activity towards the AT1 receptor and has a much greater (about 20,000 fold) affinity for the AT1 receptor than for the AT2 receptor. It does not inhibit ACE activity, therefore the incidence of dry cough is significantly lower. Valsartan does not bind to other hormone receptors or ion channels that play a role in regulating cardiovascular function or blocking them. In patients with hypertension, it causes a reduction in blood pressure without affecting the pulse rate. The onset of action occurs within 2 h, the maximum pressure drop is achieved within 4-6 h and persists for 24 h. During repeated administration, the maximum reduction in blood pressure is usually achieved within 2-4 weeks and persists during long-term treatment . Valsartan is rapidly absorbed after oral administration, the average absolute bioavailability is 23%. It is highly bound to plasma proteins (94-97%), primarily albumin. It is excreted mainly in unchanged form with faeces (83%) and urine (13%). T_0,5 is 6 hours.

Hypersensitivity to valsartan or other ingredients. Severe liver dysfunction, cirrhosis, cholestasis. Severe renal impairment (creatinine clearance <10 ml / min) and patients undergoing dialysis. 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).

In the case of concomitant use of potassium preparations, potassium-sparing diuretics, potassium chloride substitutes, or other drugs that may cause an increase in potassium ( Heparin, etc.), the preparation should be used with caution and often be monitored for potassium. 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. There is no experience regarding the safety of the preparation in patients who have recently had a kidney transplant. It should not be used in patients with primary aldosteronism due to the fact that the drugs acting on the renin-angitensin-aldosterone system are ineffective in these patients. 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.Use of the preparation in patients after myocardial infarction usually causes a decrease in blood pressure, but discontinuation of the product due to persistent symptomatic hypotension is not usually 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. Careful observation of patients with heart failure at the beginning of treatment. 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 with 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 ; it can not be ruled out that the use of valsartan may be associated with impaired renal function. 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 efficacy and safety of valsartan in children and adolescents (<18 years) has not been established and therefore its use is not recommended.

It is not recommended during the first trimester of pregnancy. In the second and third trimester, the use of the preparation is contraindicated. Administration of the preparation during the second and third trimester of pregnancy results in toxic effects on the fetus (deterioration of fetal renal function, oligohydramnios, delayed ossification of the skull) and the newborn (renal failure, hypotension, hyperkalemia). If the exposure to valsartan occurred from the second trimester of pregnancy, ultrasound examination of the kidneys and skull is recommended. Newborns whose mothers used valsartan should be observed for hypotension. It is not recommended to use the product during breastfeeding. During breastfeeding, in particular newborns and children born prematurely, it is recommended to use other preparations with a better safety profile.

Common: viral infections; dizziness related to the position of the body, orthostatic hypotension. Uncommon: upper respiratory tract infections, pharyngitis, sinusitis; hyperkalemia; depression, insomnia; swoon; conjunctivitis; dizziness, heart failure; hypotension; cough, bleeding from the nose; diarrhea, abdominal pain; back pain, painful muscle cramps, muscle pain, arthritis; tiredness, weakness. Rarely: hypersensitivity, in these serum sickness; dizziness, neuralgia; vasculitis; angioneurotic edema, rash, pruritus. Very rare: gastroenteritis, rhinitis; thrombocytopenia; Headache; haemorrhage; nausea; arthralgia; impaired renal function, acute renal failure, renal failure. In addition, there may be: reduced hemoglobin, decreased hematocrit, neutropenia, increased creatinine, potassium and bilirubin, increased urea nitrogen, liver enzymes.

Orally.Hypertension. The recommended dose is 80 mg once a day. The maximum antihypertensive effect occurs after 4 weeks. For patients who do not have adequate blood pressure control, the dose may be increased to 160 mg or a further diuretic of the thiazide group may be used; The drug can be used simultaneously with other antihypertensive drugs.Condition after a recent myocardial infarction. In stable clinical patients, treatment can be started 12 hours after the diagnosis of a recent myocardial infarction.After an initial dose of 20 mg twice daily, the dose of valsartan should be gradually increased to 40 mg, 80 mg and 160 mg twice daily for the Next few weeks. The maximum target dose is 160 mg twice daily. It is usually recommended that patients should receive a dose of 80 mg twice daily after the start of treatment, and the maximum target dose of 160 mg administered twice a day should be administered within 3 months, depending on the patient's tolerance. If 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, beta blockers, statins and diuretics. Co-administration with ACE inhibitors is not recommended. Evaluation of the condition after a heart attack 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 may be used in patients who are taking other medicines for the treatment of heart failure. However, concomitant use with ACE inhibitors and β-blockers is not recommended. The assessment of the patient's condition with heart failure should always assess renal function.
No dose adjustment is required in patients with creatinine clearance> 10 ml / min and in elderly patients. In patients with mild to moderate hepatic impairment without cholestasis, doses above 80 mg daily should not be used.
The tablets can be taken regardless of meals; should be served with drinks.