Valsartan 40 mg, 30 film-coated tablets
Registration Certificate Holder
PRANAFARM (Russia)
Dosage form
Medicine - Valsartan
Description
Film-coated tablets
light pink, round, biconvex, with a notch on one side; on the fracture, two layers are visible - a white or almost white core and a film shell.
1 tab.
valsartan 40 mg
Excipients
: microcrystalline cellulose 45.1 mg, croscarmellose sodium 2.75 mg, colloidal silicon dioxide 1.35 mg, magnesium stearate 0.8 mg.
Film shell composition:
Opadry Pink 3 mg, including polyvinyl alcohol 1.2 mg, macrogol-3350 - 0.731 mg, red iron oxide dye - 0.012 mg, yellow iron oxide dye - 0.007 mg, talc 0.444 mg, titanium dioxide 0.606 mg.
7 pcs. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 7 pcs. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 7 pcs. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 7 pcs. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 7 pcs. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 7 pcs. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 7 pcs. — contour cellular packaging (aluminum/PVC) (8) — cardboard packs. 7 pcs. — contour cellular packaging (aluminum/PVC) (10) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 10 pieces. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (8) — cardboard packs. 10 pieces. — contour cellular packaging (aluminum/PVC) (10) — cardboard packs. 14 pcs. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 14 pcs. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 14 pcs. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 14 pcs. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 14 pcs. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 14 pcs. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 14 pcs. — contour cellular packaging (aluminum/PVC) (8) — cardboard packs. 14 pcs. — contour cellular packaging (aluminum/PVC) (10) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 20 pcs. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (8) — cardboard packs. 20 pcs. — contour cellular packaging (aluminum/PVC) (10) — cardboard packs. 28 pcs. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 28 pcs. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 28 pcs. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 28 pcs. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 28 pcs. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 28 pcs. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 28 pcs. — contour cellular packaging (aluminum/PVC) (8) — cardboard packs. 28 pcs. — contour cellular packaging (aluminum/PVC) (10) — cardboard packs. 30 pcs. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 30 pcs. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 30 pcs. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 30 pcs. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 30 pcs. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 30 pcs. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 30 pcs. — contour cellular packaging (aluminum/PVC) (8) — cardboard packs. 30 pcs. — contour cellular packaging (aluminum/PVC) (10) — cardboard packs. 56 pcs. — contour cellular packaging (aluminum/PVC) (1) — cardboard packs. 56 pcs. — contour cellular packaging (aluminum/PVC) (2) — cardboard packs. 56 pcs. — contour cellular packaging (aluminum/PVC) (3) — cardboard packs. 56 pcs. — contour cellular packaging (aluminum/PVC) (4) — cardboard packs. 56 pcs. — cellular contour packages (aluminum/PVC) (5) — cardboard packs. 56 pcs. — contour cellular packaging (aluminum/PVC) (6) — cardboard packs. 56 pcs. — contour cellular packaging (aluminum/PVC) (8) — cardboard packs. 56 pcs. — contour cellular packaging (aluminum/PVC) (10) — cardboard packs. 7 pcs. — polymer jars (1) — cardboard packs. 10 pieces. — polymer jars (1) — cardboard packs. 14 pcs. — polymer jars (1) — cardboard packs. 20 pcs. — polymer jars (1) — cardboard packs. 28 pcs. — polymer jars (1) — cardboard packs. 30 pcs. — polymer jars (1) — cardboard packs. 40 pcs. — polymer jars (1) — cardboard packs. 50 pcs. — polymer jars (1) — cardboard packs. 100 pieces. — polymer jars (1) — cardboard packs.
Indications
Treatment of arterial hypertension.
Treatment of chronic heart failure (II-IV functional class according to the NYHA classification) in patients receiving traditional therapy with diuretics, digitalis drugs, as well as ACE inhibitors or beta-blockers.
Contraindications for use
Pregnancy, hypersensitivity to valsartan.
pharmachologic effect
Antihypertensive agent. It is a specific angiotensin II receptor antagonist. It has a selective antagonistic effect on AT1 receptors, which are responsible for the effects of angiotensin II.
Due to the blockade of AT1 receptors, the plasma concentration of angiotensin II increases, which can stimulate unblocked AT2 receptors. Does not have agonist activity against AT1 receptors. The affinity of valsartan for AT1 receptors is approximately 20,000 times higher than for AT2 receptors.
Does not inhibit ACE. Does not interact with or block other hormone receptors or ion channels that are important for regulating the functions of the cardiovascular system. Does not affect the level of total cholesterol, TG, glucose and uric acid in the blood plasma.
The onset of the antihypertensive effect of valsartan after oral administration in a single dose is observed within 2 hours after administration, the maximum effect is achieved within 4-6 hours.
Drug interactions
With the simultaneous use of diuretics in high doses, arterial hypotension may develop.
With the simultaneous use of potassium-sparing diuretics, heparin, dietary supplements or salt substitutes containing potassium, hyperkalemia may develop.
When used simultaneously with indomethacin, the antihypertensive effect of valsartan may be reduced.
When used simultaneously with lithium carbonate, a case of lithium intoxication has been described.
Dosage regimen
Take orally at a dose of 80 mg 1 time / day or 40 mg 2 times / day, daily. If there is no adequate effect, the daily dose can be gradually increased.
Maximum daily dose
is 320 mg in 2 doses.
Side effect
From the cardiovascular system:
arterial hypotension, postural dizziness, postural hypotension.
From the side of the central nervous system:
dizziness, headache.
From the digestive system:
diarrhea, nausea, increased bilirubin levels.
From the urinary system:
rarely - impaired renal function, increased levels of creatinine and urea nitrogen (especially in chronic heart failure).
From the side of metabolism:
hyperkalemia.
From the hematopoietic system:
neutropenia, decrease in hemoglobin and hematocrit.
Allergic reactions:
rarely - angioedema, rash, itching, serum sickness, vasculitis.
Other:
fatigue, general weakness, cough, pharyngitis, increased risk of developing viral infections.
special instructions
With hyponatremia and/or a decrease in blood volume, as well as during therapy with high doses of diuretics, in rare cases, valsartan can cause severe arterial hypotension. Before starting treatment, violations of water-salt metabolism should be corrected.
In patients with renovascular hypertension secondary to renal artery stenosis, serum urea and creatinine levels should be regularly monitored during treatment. There are no data on the safety of use in patients with CC less than 10 ml/min.
Use with extreme caution in patients with bile duct obstruction.
Due to inhibition of the RAAS, changes in renal function are possible in susceptible patients. When using ACE inhibitors and angiotensin receptor antagonists in patients with severe chronic heart failure, oliguria and/or an increase in azotemia was observed, and acute renal failure with a risk of death rarely developed.
The safety and effectiveness of valsartan in children has not been established.
Effect on the ability to drive vehicles and operate machinery
When using valsartan, it is recommended to be careful when driving a vehicle and operating machinery.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated.
Valsartan is contraindicated for use during pregnancy.
It is not known whether valsartan is excreted into breast milk in humans. Use during lactation (breastfeeding) is not recommended.
Experimental
studies
have shown that valsartan is excreted in breast milk in rats.
Use for renal impairment
Restrictions for impaired renal function - With caution.
In patients with renovascular hypertension secondary to renal artery stenosis, serum urea and creatinine levels should be regularly monitored during treatment. There are no data on the safety of use in patients with CC less than 10 ml/min.
Due to inhibition of the RAAS, changes in renal function are possible in susceptible patients.
Use in children
Restrictions for children - Contraindicated.
The safety and effectiveness of valsartan in children has not been established.
Valsartan, 30 pcs., 160 mg, film-coated tablets
Active specific angiotensin II receptor antagonist, intended for oral administration. Selectively blocks receptors of the AT1 subtype, which are responsible for the effects of angiotensin II. The consequence of AT1 receptor blockade is an increase in the plasma concentration of angiotensin II, which can stimulate unblocked AT2 receptors. Valsartan does not have any pronounced antagonistic activity against AT1 receptors. The affinity of valsartan for receptors of the AT1 subtype is approximately 20,000 times higher than for receptors of the AT2 subtype.
Valsartan does not interact with or block other hormone receptors or ion channels that are important for regulating the function of the cardiovascular system.
The likelihood of coughing when using valsartan is very low, which is due to the lack of influence on the angiotensin converting enzyme (ACE), which is responsible for the degradation of bradykinin.
A comparison of valsartan with an ACE inhibitor showed that the incidence of dry cough was significantly (p < 0.05) lower in patients receiving valsartan than in patients receiving an ACE inhibitor (2.6% versus 7.9%, respectively). In the group of patients who had previously developed a dry cough during treatment with an ACE inhibitor, during treatment with Valsartan this complication was noted in 19.5% of cases, and during treatment with a thiazide diuretic - in 19% of cases, while in the group of patients receiving treatment ACE inhibitor, cough was observed in 68.5% of cases (p < 0.05).
Use for arterial hypertension in patients over 18 years of age
When treating patients with arterial hypertension with valsartan, a decrease in blood pressure (BP) is observed, not accompanied by a change in heart rate (HR).
After taking a single dose of the drug, in most patients, the onset of the antihypertensive effect is noted within 2 hours, and the maximum reduction in blood pressure is achieved within 4-6 hours. After taking the drug, the antihypertensive effect lasts more than 24 hours.
With repeated prescriptions of the drug, the maximum reduction in blood pressure, regardless of the dose taken, is usually achieved within 2-4 weeks and is maintained at the achieved level during long-term therapy.
When the drug is combined with hydrochlorothiazide, a significant additional reduction in blood pressure is achieved. Abrupt cessation of valsartan is not accompanied by a sharp increase in blood pressure or other undesirable consequences.
Use after acute myocardial infarction in patients over 18 years of age
When using the drug for 2 years in patients who began taking it from 12 hours to 10 days after acute myocardial infarction (complicated by left ventricular failure and/or left ventricular systolic dysfunction), the rates of overall mortality and cardiovascular mortality are reduced and the time until the first hospitalization for exacerbation of CHF, repeated myocardial infarction, sudden cardiac arrest and stroke (without death) increases. The safety profile of valsartan in patients with acute infarction is similar to that in other conditions.
CHF in patients over 18 years of age
The mechanism of action of valsartan in chronic heart failure (CHF) is based on its ability to eliminate the negative consequences of hyperactivation of the renin-angiotensin-aldosterone system (RAAS) and its main effector, angiotensin II, namely vasoconstriction; fluid retention in the body; cell proliferation leading to remodeling of target organs (heart, kidneys, blood vessels); stimulation of excess synthesis of hormones that act synergistically with the RAAS (catecholamines, aldosterone, vasopressin, endothelin, etc.).
With the use of valsartan for CHF, preload decreases, pulmonary capillary wedge pressure (PCWP) and diastolic pressure in the pulmonary artery decrease, and cardiac output increases. Along with hemodynamic effects, valsartan, due to indirect blockade of aldosterone synthesis, reduces sodium and water retention in the body.
It was found that the drug did not have a significant effect on the concentration of total cholesterol, uric acid, and also, when studied on an empty stomach, on the concentration of triglycerides and glucose in the blood plasma.
When using valsartan (in an average daily dose of 254 mg) for 2 years in patients with CHF II (62%), III (36%) and IV (2%) functional class according to the NYHA classification with left ventricular ejection fraction (LV) less than 40% and LV internal diastolic diameter more than 2.9 cm/m2, receiving standard therapy, including ACE inhibitors (93%), diuretics (86%), digoxin (67%) and beta-blockers (36%) there is a significant decrease (by 27.5%) risk of hospitalization due to exacerbation of CHF.
In patients not receiving ACE inhibitors, there was a significant reduction in overall mortality (by 33%), cardiovascular mortality and CHF-related morbidity (time to first cardiovascular event), assessed by the following indicators: death, sudden death with resuscitation, hospitalization for exacerbation of CHF, intravenous administration of inotropic and vasodilator drugs for 4 or more hours without hospitalization (44%). In the group of patients receiving ACE inhibitors (without beta-blockers), during treatment with valsartan there is no reduction in overall mortality, but cardiovascular mortality and morbidity associated with CHF decrease by 18.3%.
In general, the use of valsartan leads to a decrease in the number of hospitalizations for CHF, a slowdown in the progression of CHF, an improvement in the functional class of CHF according to the NYHA classification, an increase in LV ejection fraction, as well as a decrease in the severity of signs and symptoms of heart failure and an improvement in quality of life compared to placebo.
Use in patients over 18 years of age with arterial hypertension and impaired glucose tolerance
When using valsartan and changing lifestyle, there was a statistical reduction in the risk of developing diabetes mellitus in this category of patients. Valsartan had no effect on the incidence of deaths due to cardiovascular events, myocardial infarction and non-fatal ischemic attacks, hospitalizations due to heart failure or unstable angina, arterial revascularization, in patients with impaired glucose tolerance and arterial hypertension, differing in age, gender and race.
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 arterial hypertension and impaired glucose tolerance is 80 mg once a day. If necessary, the dose can be increased to 160 mg.
Use in children and adolescents from 6 to 18 years of age with arterial hypertension
In children and adolescents from 6 to 18 years of age, valsartan provides a dose-dependent, smooth reduction in blood pressure. When using valsartan, the maximum reduction in blood pressure, regardless of the dose taken, is usually achieved within 2 weeks, and is maintained at this level during long-term therapy.
