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Valsartan

Valsartan is an active specific angiotensin II receptor antagonist (ARA II), 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 agonistic 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 in regulating the functions of the cardiovascular system.

The likelihood of coughing when using valsartan is very low, which is due to the lack of effect on angiotensin-converting enzyme (ACE), which is responsible for the degradation of bradykinin. Accordingly, when using angiotensin II receptor antagonists, ACE inhibition and accumulation of bradykinin or substance P do not occur. In comparative clinical studies of valsartan with an ACE inhibitor, the incidence of dry cough was significantly (p<0.05) lower in patients taking valsartan than in patients taking an ACE inhibitor (2.6% vs. 7.9%, respectively).

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 oral administration of a single dose of valsartan, in most patients, the onset of the antihypertensive effect is observed within 2 hours, and the maximum reduction in blood pressure is achieved within 4-6 hours, lasting more than 24 hours. With repeated use of valsartan, the maximum reduction in blood pressure, regardless of the dose taken, is usually achieved within 2-4 weeks, and is maintained at this level during long-term therapy. Abrupt cessation of valsartan is not accompanied by a significant increase in blood pressure or other adverse events.

In patients with arterial hypertension, type 2 diabetes mellitus and nephropathy, taking valsartan at a dose of 160-320 mg per day, there is a significant decrease in proteinuria (36-44%).

Use after acute myocardial infarction in patients over 18 years of age

When using valsartan for 2 years in patients who began taking valsartan from 12 hours to 10 days after myocardial infarction (complicated by left ventricular failure and/or left ventricular systolic dysfunction), overall mortality and cardiovascular mortality are reduced and the time until the first hospitalization for exacerbation of chronic heart failure, repeated myocardial infarction, sudden cardiac arrest and stroke (without death) increases. The safety profile of valsartan in patients with acute myocardial infarction is similar to that in other conditions.

Chronic heart failure (CHF) in patients over 18 years of age

The mechanism of action of valsartan in CHF is based on its ability to eliminate the negative consequences of chronic 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). With the use of valsartan for CHF, preload decreases, wedge pressure in the pulmonary capillaries and diastolic pressure in the pulmonary artery decreases, and cardiac output increases. Along with hemodynamic effects, valsartan, due to indirect blockade of aldosterone synthesis, reduces sodium and water retention in the body.

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 intravenous diastolic diameter more than 2.9 cm/m2, receiving standard therapy, including ACE inhibitors (93%), diuretics (86%), digoxin (67%) and beta-blockers (36%), noted significant reduction (by 27.5%) in the 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 morbidity associated with CHF (time to the onset of the first cardiovascular event), which are assessed by the following indicators: death, sudden death with resuscitation, hospitalization for exacerbation of CHF, intravenous administration of inotropic or 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 was no reduction in overall mortality, but cardiovascular mortality and morbidity associated with CHF decreased 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 left ventricular 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 with 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 statistically significant 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 starting dose of valsartan in patients with arterial hypertension and impaired glucose tolerance is 80 mg once daily. If necessary, the dose can be increased to 160 mg.

Use in children and adolescents aged 6 to 18 years 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.

Pharmacodynamics and pharmacokinetics

The active substance of the drug provokes a competitive blocking of AT1 angiotensin II receptors , which are located in the vascular endothelium, cardiac muscle, adrenal cortex, renal tissue, brain and lung tissue. This leads to inhibition of angiotensin effects. The medicine reduces myocardial hypertrophy in arterial hypertension .

After a single use, the effect is noticeable after 120 minutes, it lasts throughout the day. A persistent therapeutic effect is achieved 3 weeks after the first day of the course.

In people with CHF, the medicine eliminates hyperstimulation of the RAAS , prevents pathological cell proliferation swelling . Its administration reduces preload and increases cardiac output .

When combined with K aptopril, it reduces the likelihood of post-infarction complications.

In addition, a common combination is valsartan and amlodipine . These active ingredients are found in medications such as Exforge and Vamloset .

The original drug is quickly absorbed from the gastrointestinal tract. Bioavailability on average is 23%.

Communication with plasma (mainly with albumin ) is about 95%.

Excreted mainly in feces (70%), also excreted in urine (30%), mostly unchanged.

Valsartan price, where to buy

The price of Valsartan in capsules 40 mg, 40 pieces in a pack – 130 rubles. 80 mg tablets (30 pieces in a pack) cost about 220 rubles. And the price of Valsartan in tablets of 160 mg (30 pieces in a pack) is approximately 350 rubles.

Online pharmacies in RussiaRussia

ZdravCity

Valsartan tablets p.p.o.
80 mg 30 pcs. Ozone LLC 265 rub. order
Valsartan tablets p.p.o. 160 mg 30 pcs. Ozone LLC
RUB 363 order
Valsartan tablets p.p.o. 40 mg 30 pcs. Pranapharm LLC
RUB 178 order
Valsartan tablets p.p.o. 160 mg 30 pcs. Pranapharm LLC
RUB 269 order
Read also: Beclazon Eco, 1 piece, 250 mcg/dose, dosed aerosol for inhalation
Valsartan-SZ tab. p/o captivity. 160mg No. 30Northern Star ZAO
RUB 334 order

Analogues of Valsartan

Level 4 ATC code matches:
Telmisartan

Irbesartan

Presartan

Nortivan

Candesartan

Kozaar

Aprovel

Teveten

Blocktran

Cardosal

Losartan

Atakand

Diovan

Valsacor

Mikardis

Vazar

Valz

Lorista

Lozap

The following synonyms and analogues of Valsartan are known:

Valz;
Valaar;
Valsartan A;
Valsasin;
Valsartan N;
Valsartan Zentiva;
Valsacor;
Diovan;
Valsafors;
Nortivan;
Tantordio;
Tareg.

All of the medications listed have their own application characteristics. Valsartan analogs cannot be replaced at your own discretion, without consulting a doctor.

Side effects

Taking this medicine may cause some unwanted effects:

CVS and hematopoietic system: neutropenia , decreased hematocrit , hyperkalemia ;
CNS: dizziness , weakness, headache ;
gastrointestinal tract: diarrhea , abdominal pain , nausea, increased activity of liver transaminases ;
other: cough, viral infections, hyperkalemia .

Adverse reactions when using the drug occur rarely.