Expiration date: 08/2025
Composition
Active substance: valsartan - 40,0 mg, 80,0 160,0 mg or mg
Pharmacotherapeutic group
Angiotensin II receptor antagonist
Pharmacological action
Valsartan - active specific antagonist of angiotensin II receptor intended for ingestion. Selectively blocks the AT1 receptor subtype, which is responsible for the effects of angiotensin II. The result of the blockade of AT1 receptors is increased plasma concentration of angiotensin II, which can stimulate unlocked AT2-receptors. Valsartan does not have any pronounced agonistic activity against AT1-receptors. The affinity of valsartan for the AT1 subtype receptors in about 20 000 times higher than for the AT2 receptor subtype. The probability of occurrence of cough with the use of valsartan is very low, due to the lack of effect on angiotensin converting enzyme (ACE), which is responsible for degradation of bradykinin. Comparison of valsartan with the ACE inhibitor showed that the incidence of dry cough was significantly (p <, 0.05) lower in patients treated with valsartan than in patients treated with ACE inhibitor (2.6% versus 7.9%, respectively). In the group of patients who have previously, when treatment with ACE inhibitor developed a dry cough, the treatment with valsartan, this complication was noted in 19.5% of cases, and in the treatment of thiazide diuretic - in 19.0% of cases, while in the group of patients treated with ACE inhibitor, cough was observed in 68.5% of cases (p <, 0.05). Valsartan does not enter into interaction and does not block other hormone receptors or ion channels of importance for the regulation of the functions of the cardiovascular system. The treatment with valsartan in patients with arterial hypertension there is a decrease in blood pressure (BP), is not accompanied by change in heart rate (HR). After ingestion of a single dose of the drug in most patients beginning antihypertensive effect is noted within 2 hours, and maximum reduction of blood pressure is achieved within 4-6 hours. After taking the drug antihypertensive effect persists over 24 hours. With repeated prescriptions maximum decrease in blood pressure, regardless of the dose, is usually achieved within 2-4 weeks and maintained at that level during long-term therapy. In the case of a combination drug with hydrochlorothiazide achieved reliable additional decrease in blood pressure. Abrupt discontinuation of the valsartan is not accompanied by a sharp increase in blood pressure or other undesirable consequences. The mechanism of action of valsartan in chronic heart failure based on its ability to eliminate the negative effects of chronic hyperactivation of the renin-angiotensin-aldosterone system (RAAS) and its main effector angiotensin II, namely, vasoconstriction, fluid retention in the body, the proliferation of cells, leading to remodeling of target organs (heart, kidney, vessels) and stimulation of excess synthesis of hormones, acting synergistically with RA (catecholamines, aldosterone, vasopressin, endothelin, etc.). On the background of the use of valsartan in chronic heart failure (CHF) reduced preload, reduced jamming pressure in the pulmonary capillaries (ZLC) and diastolic pulmonary artery pressure, increased cardiac output. Along with hemodynamic effects, valsartan is mediated through the blockade of the synthesis of aldosterone reduces sodium retention and water in the body. Established that the drug had no significant effect on the concentration of total cholesterol, uric acid, and also in the study on an empty stomach - the concentration of triglycerides and glucose in serum.
Indications for use
Hypertension, congestive heart failure patients receiving standard therapy one or more drugs: diuretics, cardiac glycosides, ACE inhibitors or beta-blockers. The application of each of these drugs is not required to improve the survival of patients after acute myocardial infarction complicated by left ventricular failure and/or systolic dysfunction of the left ventricle, with the presence of stable hemodynamic parameters.
Contraindications
Hypersensitivity to any component of the drug, pregnancy, pregnancy planning, lactation, age to 18 years, severe violations of the liver (more 9 points on a scale child-Pugh), biliary cirrhosis and cholestasis, concomitant use of receptor antagonists of angiotensin II, including valsartan, or of ACE inhibitors with aliskiren in patients with diabetes.
Method of application and doses
Tablets are taken orally without chewing.
Hypertension: the recommended starting dose of Valsartan is 80 mg 1 time a day every day, regardless of race, age and sex of the patient. The antihypertensive effect develops within the first 2 weeks of treatment, the maximum effect observed after 4 weeks. Those patients who fail to achieve adequate therapeutic response, the daily dose of Valsartan may be increased to maximum daily doses of 320 mg or it is necessary to use a diuretic.
Congestive heart failure: the recommended starting dose of Valsartan is 40 mg 2 times a day, every day. The dose of Valsartan should gradually increase for at least 2 weeks to 80 mg 2 times a day, and with good endurance - up to 160 mg 2 times per day. This may require lower doses have also taken diuretics.
The maximum daily dose Valsartan is 320 mg in 2 admission.
To improve survival after myocardial infarction: treatment should start within 12 hours after myocardial infarction. The initial dose is 20 mg (1/2 tablet 40 mg) 2 Aza per day. The increase in dose is titration (40 mg, 80 mg, 160 mg 2 times per day) in the next few weeks until the target dose of 160 mg 2 times per day. The maximum daily dose is 320 mg in 2 admission. Typically, the recommended dose to achieve 80 mg 2 times per day by the end of the second week of treatment. Achievement of the maximum target dose 160 mg 2 times a day is recommended for the end of the third month of therapy with the drug Valsartan. The increase in dose depends on the tolerability of the drug in the titration period. In the case of hypotension accompanied by clinical manifestations or renal dysfunction should consider lowering the dose. Assessment of patients in the period after myocardial infarction should include an assessment of renal function.
Use in patients older than 65 years of age: in the elderly patients dose adjustment is not required.
Patients with impaired renal function: patients with impaired renal function dose adjustment is not required. Currently, there are no clinical data on the use of the drug in patients with KK less 10 ml/min.
Patients with impaired liver function: patients with mild or moderate impaired hepatic function debelyanovo origin without signs of cholestasis, the drug should be used with caution, daily dose should not exceed 80 mg.
Release form
Tablets, film-coated 40 mg, 80 mg and 160 mg 30 pills in the package.
