The antihypertensive drug valsartan belongs to the group of angiotensin II receptor blockers (ARBs). ARBs are perhaps the most promising drugs for the treatment of hypertension today. In our country, valsartan was approved for medical use in 1997. To date, the effectiveness of this drug in the treatment of arterial hypertension, chronic heart failure, as well as in eliminating the consequences of myocardial infarction has been fully proven. The pharmacokinetic and pharmacodynamic characteristics of valsartan have been repeatedly reviewed in a number of reviews published in domestic and foreign medical periodicals. For arterial hypertension, the drug is effective both as monotherapy and as a combination treatment. The antihypertensive effect of valsartan depends on the dose taken. Thus, according to one randomized study, treatment with high (320 mg/day) doses of the drug provided a greater reduction blood pressure than moderate dose therapy (160 mg/day). As for tolerability, in terms of the development of side effects, both regimens of taking the drug were comparable. In addition to bringing blood pressure within the desired range, valsartan has a beneficial effect on the well-being of patients, improving the quality of life in certain aspects. Thus, the drug has a positive effect on sex life hypertensive patients, and in elderly patients it improves cognitive function. A number of studies have examined the effectiveness of valsartan in comparison with other antihypertensive drugs. Valsartan has been shown to have comparable antihypertensive activity to amlodipine, but has some additional benefits. For example, it causes a more pronounced decrease in left ventricular hypertrophy, a decrease in the excretion of albumin in the urine, and has a more pronounced effect on the sympathetic nervous system. In several randomized clinical trials The combined use of valsartan with the thiazide diuretic hydrochlorothiazide was studied.
Without exception, all publications noted the effectiveness and safety of this antihypertensive “duet”, and combination therapy was much more effective than taking each of these drugs separately. The combination of valsartan with hydrochlorothiazide is comparable in its antihypertensive activity to the combination of valsartan with amlodipine. The mechanism of action of valsartan is due to its ability to selectively block AT1 receptors, due to which angiotensin II has no choice but to silently admit its defeat in the struggle for a place in the sun (read: for a place on its “personal” receptors). Thus, the body is removed from the vasopressor influence of angiotensin II, which determines the antihypertensive effect of the drug. Valsartan, unlike angiotensin-converting enzyme inhibitors (enalapril, captopril, etc.), does not cause a dry cough, which is due to the lack of influence on the enzyme kinase II, which is responsible for the breakdown of bradykinin. The decrease in blood pressure observed while taking the drug is not accompanied by any changes in heart rate. After oral administration of valsartan in a single dose, the onset of hypotensive effect, as a rule, is observed after 1-2 hours, and the peak decrease in blood pressure can be expected at 4-6 hours. The duration of action of a single dose of the drug is 24 hours. With a regular course of taking valsartan, stabilization of blood pressure at the target level is achieved in 2-4 weeks. Abrupt withdrawal of the drug does not cause withdrawal syndrome (in the form of a sharp increase in blood pressure). The effectiveness of valsartan in chronic forms heart failure is due to its ability to level Negative consequences excessive hyperactivity of the renin-angiotensin-aldosterone system and its main “tool” - angiotensin II.
Pharmacology
Antihypertensive agent. It is a specific angiotensin II receptor antagonist. It has a selective antagonistic effect on AT 1 receptors, which are responsible for the implementation of the effects of angiotensin II.
Due to the blockade of AT 1 receptors, the plasma concentration of angiotensin II increases, which can stimulate unblocked AT 2 receptors. Does not have agonistic activity against AT 1 receptors. The affinity of valsartan for AT 1 receptors is approximately 20,000 times higher than for AT 2 receptors.
Does not inhibit ACE. Does not interact with or block other hormone receptors or ion channels having important to regulate functions of cardio-vascular system. Does not affect the level of total cholesterol, TG, glucose and uric acid in 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.
Pharmacokinetics
After oral administration, valsartan is rapidly absorbed from the gastrointestinal tract, the degree of absorption is characterized by individual differences. Absolute bioavailability averages 23%. The pharmacokinetic curve of valsartan has a multi-exponential character (T 1/2 in the α-phase< 1 ч и T 1/2 в β-фазе - около 9 ч), кинетика линейная.
No changes in pharmacokinetic parameters were observed during course use.
When taking valsartan with food, the AUC decreases by 48%, while approximately 8 hours after administration, plasma concentrations of valsartan are the same in patients taking it with food and on an empty stomach. The decrease in AUC is not accompanied by a clinically significant decrease therapeutic effect.
When taking valsartan once a day, the accumulation is insignificant. Plasma concentrations of valsartan were similar in women and men.
Binding to plasma proteins, mainly albumin, is 94-97%. Vd at equilibrium is about 17 liters.
Plasma clearance of valsartan is about 2 l/h. Excreted in feces - 70% and in urine - 30%, mainly unchanged.
In biliary cirrhosis or biliary obstruction, the AUC of valsartan increases approximately 2-fold.
Release form
Light pink, film-coated tablets, round, biconvex, scored on one side; two layers are visible on the fracture - the core is white or almost white and film shell.
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.
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56 pcs. - contour cellular packaging (aluminum/PVC) (8) - cardboard packs.
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Dosage
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.
The maximum daily dose is 320 mg in 2 divided doses.
Interaction
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.
Side effects
From the cardiovascular system: arterial hypotension, postural dizziness, postural hypotension.
From the side of the central nervous system: dizziness, headache.
From the outside 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).
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.
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.
Due to inhibition of the RAAS, changes in renal function are possible in susceptible patients.
Use in children
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; acute renal failure with a risk of death.
The safety and effectiveness of valsartan in children has not been established.
Impact on the ability to drive vehicles and operate machinery
Valsartan: instructions for use and reviews
Latin name: Valsartan
ATX code: C09CA03
Active substance: valsartan
Manufacturer: Mylen Laboratories Limited (India), KRKA (Slovenia), Zhuhai Rundumintong Pharmaceutical Co., Ltd., Livzon Group Changzhou Kony Pharmaceutical Co., Second Pharma Co. (China), Ozon LLC, Atoll LLC, Obolenskoye pharmaceutical company(Russia)
Updating the description and photo: 19.08.2019
Valsartan is an angiotensin II receptor antagonist.
Release form and composition
Dosage forms:
- film-coated tablets: round, biconvex, light pink in color, core - almost white or white, for tablets at a dose of 40 mg and 80 mg - a dividing line on one side (7, 10, 14, 20, 28, 30 or 56 pieces in a blister pack, in a cardboard pack of 1, 2, 3, 4, 5, 6, 8 or 10 packs of 7, 10, 14, 20, 28, 30, 40, 50 or 100 pieces. in a polymer jar, 1 jar in a cardboard pack);
- capsules: hard gelatin, opaque, size No. 2 (capsules 20, 40, 80 mg), size No. 0 (capsules 160 mg); 20 mg capsules - light yellow, body - beige, cap - creamy; 40 mg capsules – the body and cap are light yellow with a creamy tint; 80 mg capsules – body and cap light yellow with a beige tint; 160 mg capsules – light brown body and cap (10, 20 or 30 pcs. in blister packs, in a cardboard pack 1, 2, 3, 4, 5 or 10 packs; 10, 20, 30, 40, 50 or 100 pcs. in a polymer jar, 1 jar in a cardboard pack).
1 tablet contains:
- active substance: valsartan – 40 mg, 80 mg or 160 mg;
- auxiliary components: microcrystalline cellulose, croscarmellose sodium, colloidal silicon dioxide, magnesium stearate;
- shell composition: Opadry pink (macrogol-3350, polyvinyl alcohol, talc, titanium dioxide, yellow iron oxide dye, red iron oxide dye).
1 capsule contains:
- active ingredient: valsartan – 20 mg, 40 mg, 80 mg or 160 mg;
- auxiliary components: microcrystalline cellulose, croscarmellose sodium, povidone K17, colloidal silicon dioxide, magnesium stearate;
- composition of the capsule body and cap: gelatin, yellow iron oxide dye, red iron oxide dye, titanium dioxide; In addition, capsules in a dose of 160 mg contain black iron oxide dye.
Pharmacological properties
The drug is characterized by antihypertensive properties.
Pharmacodynamics
Valsartan is an active, specific angiotensin II receptor antagonist intended for oral administration. It selectively blocks receptors of the AT 1 subtype, which are responsible for the effects of angiotensin II. As a result of this blockade, the concentration of angiotensin II in the blood plasma increases, which can lead to stimulation of unblocked AT 2 receptors. Valsartan is not characterized by agonistic activity against AT 1 receptors of any severity. The affinity of this substance for receptors of the AT 1 subtype is approximately 20,000 times higher than for receptors of the AT 2 subtype.
The risk of cough during treatment with the drug is very low, which is explained by the lack of effect on the angiotensin-converting enzyme (ACE), which is responsible for the degradation of bradykinin. When comparing valsartan with an ACE inhibitor, it was found that the incidence of dry cough attacks was significantly lower in patients taking valsartan compared to patients taking an ACE inhibitor (2.6% and 7.9%, respectively). In the group of patients who previously had a dry cough during therapy with an ACE inhibitor, when using valsartan this complication was observed in 19.5% of cases, and when using a thiazide diuretic - in 19% of cases, while in the group of patients undergoing ACE inhibitor therapy, cough was recorded in 68.5% of cases.
Valsartan does not interact with or block ion channels or receptors of other hormones that play important role in the regulation of the cardiovascular system. Treatment with this drug in patients with arterial hypertension accompanied by a decrease in blood pressure, which does not lead to a change in heart rate.
After oral administration of a single dose of valsartan, in most patients, the antihypertensive effect is recorded within 2 hours, and a peak decrease in blood pressure is observed after approximately 4-6 hours. After reception medicine the antihypertensive effect lasts for approximately 24 hours. When re-prescribing valsartan maximum reduction blood pressure, regardless of the dose taken, is achieved on average within 2–4 weeks and remains at the achieved level during a long course of therapy. When this drug is combined with hydrochlorothiazide, an additional decrease in blood pressure is observed, confirmed by reliable clinical data. Sudden withdrawal of valsartan does not lead to sharp increase blood pressure or other undesirable consequences.
The mechanism of action of the drug in chronic heart failure lies in its ability to eliminate the negative consequences of chronic hyperactivation of the renin-angiotensin-aldosterone system (RAAS) and its main effector, angiotensin II. These include vasoconstriction, stimulation of excessive synthesis of hormones that have a synergistic effect in relation to the RAAS (endothelin, catecholamines, vasopressin, aldosterone, etc.), cell proliferation, causing remodeling of target organs (kidneys, blood vessels, heart), fluid retention in the body . In patients with chronic heart failure while taking valsartan, the cardiac output, diastolic pressure decreases in pulmonary artery and wedge pressure in the pulmonary capillaries, preload decreases. The use of the drug is not only accompanied by hemodynamic effects, but also reduces water and sodium retention in the body due to indirect blockade of aldosterone production.
It has been proven that valsartan does not significantly affect the level of uric acid, total cholesterol, or, when tested on an empty stomach, the level of glucose and triglycerides in the blood serum.
Pharmacokinetics
After oral administration, valsartan is absorbed from high speed, however, the degree of absorption can vary widely. On average, the absolute bioavailability of this substance reaches 23%. Its maximum concentration in blood plasma is recorded after 2 hours. With regular use of valsartan, the maximum reduction in blood pressure is observed after 4 weeks. With a single dose of the drug during the day, valsartan accumulates slightly. Its content in blood plasma is the same in women and men.
Valsartan demonstrates high binding activity to plasma proteins (94–97%), mainly to albumin. Its distribution volume is small and equal to approximately 17 liters. Plasma clearance is relatively low (about 2 L/hour) compared to hepatic blood flow (about 30 L/hour).
The metabolism of valsartan is not very pronounced (approximately 20% of the dose taken is converted into metabolites). A hydroxyl metabolite is detected in small concentrations in blood plasma [its AUC (area under the concentration-time curve) is less than 10% of that for valsartan]. This metabolite has no pharmacological activity. Valsartan has a biphasic elimination from the body: the half-life for the alpha phase is less than 1 hour, and for the beta phase it is approximately 9 hours.
Valsartan is excreted primarily unchanged in feces (approximately 83% of the dose taken) and urine (approximately 13% of the dose taken).
Taking valsartan with food leads to a decrease in AUC by approximately 48%. However, 8 hours after the drug enters the body, the concentration of the active substance in the blood plasma, taken on an empty stomach and with food, turns out to be the same. A decrease in AUC is not accompanied by a clinically significant decrease in the therapeutic effect of valsartan, so the drug can be taken both before and after meals.
In patients with chronic heart failure, the time to reach maximum concentration and half-life are identical to those in healthy volunteers. The increase in maximum concentration and AUC is directly proportional to the increase in the dose of the drug (during the experiment it increased from 40 to 160 mg taken 2 times a day). The average cumulation factor is 1.7. When administered orally in such patients, the clearance of valsartan reached approximately 4.4 l/hour, while the age of the patients did not affect its value.
In some patients over the age of 65 years, the systemic bioavailability of the drug is higher than that in patients young, however, this fact does not have any particular clinical significance.
No correlation was found between renal function and systemic bioavailability of the drug. In patients with renal dysfunction and CC more than 10 ml/min, there is no need to adjust the dose of valsartan. To date, no studies have been conducted on the use of the drug in patients on hemodialysis. Valsartan has a high degree of binding to plasma proteins, so its removal through hemodialysis is almost impossible.
In patients with mild to moderate liver dysfunction, the bioavailability of valsartan increases by 2 times compared to healthy volunteers. However, the AUC values of this substance do not correlate with the degree of impairment liver function. The use of the drug in patients with severe liver dysfunction has not been studied.
Indications for use
- chronic heart failure (as part of standard therapy using cardiac glycosides, diuretics, angiotensin-converting enzyme inhibitors or beta-blockers);
- arterial hypertension.
In addition, to increase survival, Valsartan is prescribed to patients with stable hemodynamic parameters after acute myocardial infarction complicated by systolic dysfunction left ventricle and/or left ventricular failure.
Contraindications
- age under 18 years;
- severe form (above 9 points on the Child-Pugh scale) of liver dysfunction, cholestasis, biliary cirrhosis;
- concomitant therapy with angiotensin II receptor antagonists or ACE inhibitors (angiotensin-converting enzyme) with aliskiren in patients with diabetes mellitus;
- period of pregnancy planning and childbearing;
- breast-feeding;
- individual hypersensitivity to the components of the drug.
According to the instructions, Valsartan should be prescribed with caution to patients who limit their salt intake and have bilateral stenosis. renal arteries, stenosis of the artery of a single kidney, after kidney transplantation, with renal failure [creatinine clearance (CC) less than 10 ml/min], hemodialysis, primary hyperaldosteronism, reduced circulating blood volume (CBV) (including conditions with diarrhea and vomiting), liver failure of non-biliary genesis of mild and moderate degree severity (without cholestasis), hypertrophic obstructive cardiomyopathy, chronic heart failure II–IV functional class according to the NYHA classification, mitral or aortic stenosis.
Instructions for use of Valsartan: method and dosage
Film-coated tablets
The tablets are taken orally, swallowed whole and washed down with water.
- chronic heart failure: initial dose – 40 mg 2 times a day. Within 14 days, taking into account individual tolerability of the drug, single dose should be gradually increased to 80 mg or 160 mg. This may require reducing the dose of concomitantly used diuretics. The maximum daily dose is 320 mg;
- arterial hypertension: initial dose – 80 mg 1 time per day. In the absence of the desired therapeutic effect after 14–28 days of therapy, daily dose you can increase to 320 mg or prescribe additional diuretics.
To improve survival after suffered a heart attack myocardium, the use of Valsartan should be started within the first 12 hours, taking 20 mg 2 times a day. Over the next 14 days, the dose is gradually increased by titration, taking 40 mg, then 80 mg 2 times a day. By the end of the third month of therapy, it is recommended to achieve the target dose of 320 mg per day, taking 160 mg 2 times a day. When increasing the dose, it is necessary to take into account the patient’s tolerance to the drug.
In case of impaired renal function or in elderly patients, no dose adjustment is required.
In mild or moderate forms of liver dysfunction of non-biliary origin without cholestasis, the dose of the drug should not exceed 80 mg per day.
Capsules
Capsules are intended for oral administration.
Side effects
- digestive system: nausea, diarrhea, increased bilirubin levels;
- cardiovascular system: postural hypotension, postural dizziness, arterial hypotension;
- hematopoietic system: decreased hemoglobin and hematocrit levels, neutropenia;
- nervous system: headache, dizziness;
- metabolism: hyperkalemia;
- urinary system: rarely – functional disorder kidneys, increased levels of urea nitrogen and creatinine (especially in patients with chronic heart failure);
- allergic reactions: rarely - itching, rash, serum sickness, angioedema, vasculitis;
- other: general weakness, fatigue, cough, increased risk of viral infections, pharyngitis.
Overdose
The main symptom of an overdose of Valsartan is a pronounced decrease in blood pressure, which in the future can lead to clouding of consciousness, state of shock and/or collapse. In this case, symptomatic therapy is recommended, the specifics of which depend on the severity of the symptoms and the time that has passed since taking the drug. In case of accidental overdose, vomiting should be induced (if Valsartan has been taken recently) or gastric lavage should be performed. If there is a pronounced decrease in blood pressure, according to the protocols, it is necessary to administer a 0.9% sodium chloride solution intravenously and lay the patient down, placing his legs in an elevated position, for a period of time sufficient for therapy. Active measures are also being taken to restore the full functioning of the cardiovascular system, including regular monitoring of the amount of urine excreted, the volume of circulating blood and the activity of the heart and respiratory system.
special instructions
If the content of bcc and/or sodium is reduced, the use of Valsartan should be started after their levels in the body are restored; if necessary, the dose of the diuretic is reduced. This will avoid clinical manifestations arterial hypotension, which rarely occurs at the beginning of treatment.
It is recommended to combine with caution with potassium-containing biologically active additives and salt substitutes, potassium-sparing diuretics, heparin, or other drugs that may contribute to the development of hyperkalemia.
With unilateral or bilateral renal artery stenosis, regular monitoring of the concentration of creatinine and urea in the blood serum is required.
The combination of the drug or ACE inhibitors with aliskiren should be avoided in case of severe renal impairment (creatinine clearance less than 30 ml/min).
When treating patients with biliary obstruction, the clearance of valsartan is reduced.
For patients in whom Valsartan has caused Quincke's edema, drug therapy is discontinued with a ban on resuming its use.
For arterial hypertension in patients with primary hyperaldosteronism, the use of the drug has no therapeutic effect.
Due to the risk of a significant hypotensive effect of the drug, blood pressure (BP) should be regularly monitored at the beginning of therapy in patients with chronic heart failure or myocardial infarction.
There is a risk of developing oliguria and/or worsening azotemia, and in rare cases, acute renal failure and/or fatal outcome in chronic heart failure of functional class II–IV (NYHA classification), therefore these categories of patients should be provided with periodic assessment of renal function.
In the treatment of arterial hypertension, in addition to monotherapy, the drug can be used in combination with acetylsalicylic acid, thrombolytics, beta-blockers and HMG-CoA reductase inhibitors (statins). It is not recommended to use concomitantly with ACE inhibitors, since monotherapy in in this case has advantages.
At combination therapy chronic heart failure, the prescription of diuretics, cardiac glycosides, beta-blockers or ACE inhibitors is indicated. The use of a combination of ACE inhibitors, beta-blockers and Valsartan is not recommended.
Due to the risk of dizziness or fainting during treatment, care should be taken when operating vehicles and machinery.
Use during pregnancy and lactation
Taking Valsartan during pregnancy is strictly contraindicated. The risk to the fetus in this case turns out to be quite significant, which is due to the mechanism of action of angiotensin II receptor antagonists. The effect of ACE inhibitors (drugs that affect the RAAS) on the fetus when prescribed in the second and third trimesters of pregnancy can lead to disturbances in its development and intrauterine death. According to retrospective data, when taking ACE inhibitors in the first trimester of pregnancy, the risk of having children with intrauterine malformations increases. There is information on renal dysfunction, oligohydramnios in newborns and spontaneous abortions in mothers who accidentally received valsartan during pregnancy. This drug should also not be used in women planning pregnancy. In this case, the doctor must inform women of reproductive age about possible risk negative influence valsartan on the fetus during pregnancy.
If pregnancy occurs during treatment with Valsartan, it should be discontinued as soon as possible. Information about the penetration of the drug into breast milk are absent, therefore taking the drug is contraindicated during breastfeeding.
Use in childhood
The effectiveness and safety of the drug in children have not been proven.
For impaired renal function
There is no information on the safety of taking Valsartan in patients with CC less than 10 ml/min. Since RAAS inhibition occurs in susceptible patients, it may be accompanied by changes in renal function.
Drug interactions
With simultaneous use of Valsartan:
- agents acting on the renin-angiotensin-aldosterone system (RAAS) have an effect on increasing the incidence of renal dysfunction, arterial hypotension and hyperkalemia compared with monotherapy;
- atenolol, warfarin, cimetidine, furosemide, digoxin, indomethacin, amlodipine, hydrochlorothiazide, glibenclamide do not cause clinically significant interactions;
- non-steroidal anti-inflammatory drugs, including selective cyclooxygenase-2 inhibitors, can reduce the antihypertensive effect of valsartan, cause an increase in potassium in the blood plasma and a deterioration in renal function;
- Lithium preparations enhance their toxic effect by increasing the lithium content in the blood plasma;
- potassium preparations, potassium-sparing diuretics (including amiloride, spironolactone, triamterene), potassium-containing salts can help increase the level of potassium concentration in the blood serum, and in case of heart failure, the level of creatinine in the blood serum;
- Rifampicin, cyclosporine, ritonavir may increase the concentration of valsartan in the blood serum.
Analogs
Analogs of Valsartan are: Valz, Diovan, Valsacor, Valsartan Zentiva.
Terms and conditions of storage
Keep away from children.
Store at temperatures up to 25 °C, protected from light.
Shelf life – 3 years.
Valsartan tablets have an effect that is aimed at providing competitive blocking of AT1 receptors of angiotensin II, which are located in the vascular endothelium and renal tissue, as well as the heart muscle and brain, adrenal cortex and pulmonary tissues.
As a result, angiotensin effects are suppressed.
The medication helps reduce myocardial hypertrophy, which develops against the background of arterial hypertension.
There is no effect on the concentration of glucose and cholesterol, uric acid with triglycerides.
After a single dose, the effect is observed two hours after taking the tablets and lasts about a day. A lasting therapeutic result occurs after several weeks of treatment.
Indications for use of the drug are:
- Development of arterial hypertension.
- Chronic heart failure, which is treated with various diuretics, products containing digitalis extract, as well as beta-blockers and ACE inhibitors.
The drug "Valsartan" is used only orally. The tablets do not need to be chewed.
Patients who suffer from arterial hypertension are prescribed a standard dosage of 80 mg per day. An increase in the dose is allowed only if the desired therapeutic result is not observed.
The maximum daily dose should not exceed 640 mg. To achieve the required dose, the daily dosage is gradually increased.
After a heart attack, it is necessary to prescribe 40 mg per day in the morning. Then a gradual increase is carried out over three months, so that the dose is 320 mg per day.
If hypotension occurs in the patient, the dosage should be reduced immediately.
Release form and composition
The drug "Valsartan" is produced in the form of tablets, which differ in dosage (there are three different dosages).
The composition includes the following chemically active substances:
- Valsartan is the active ingredient.
- Aerosil.
- Magnesium stearate.
- Croscaramellose sodium.
- Special dye “Opadriy Pink”.
This medicine interacts with various drugs:
Contraindications
Valsartan cannot be used by every person who has certain indications for therapy using this drug.
There is a whole scroll various contraindications prohibiting the use of these tablets:
- The period of bearing a child.
- Breastfeeding (lactation period).
- Individual hypersensitivity to any of the components included in the drug.
- Enough severe violations normal functions liver.
- Certain pediatrician indications.
Patients should take the tablets with extreme caution who have the following diagnosis:
- Severe dehydration.
- Severe kidney failure.
- Development of renal artery stenosis.
- Severe obstruction of the biliary tract.
- Patients who adhere to a sodium-free diet.
During pregnancy and lactation
Due to the danger to the fetus, medications that contain valsartan are prohibited from being prescribed to pregnant women.
Side effects
Valsartan during treatment can cause the occurrence and intensive development of various side effects:
Before starting therapy with this medication, it is necessary to correct the concentration of Na+ in the blood or bcc.
Patients who suffer from renovascular hypertension should constantly monitor the amount of urea, as well as creatinine contained in the blood. If pregnancy occurs during therapy, the medicine should be discontinued immediately.
They are used with special caution by people who are engaged in work that requires increased attention and speed of not only motor, but also mental reactions.
Storage conditions and periods
In addition, it must be inaccessible to small children.
Best before date tablets is 3 years.
Price
In pharmacies operating in the territory Russian Federation , drug If necessary, Valsartan can be purchased for approximately 174 rubles.
In all Ukrainian pharmacies the cost of this medicine is in the range of 60-80 hryvnia.
Analogs
The most common analogues of Valsartan today are the following medications:
These drugs are used in cases where it is necessary to replace Valsartan with another medicine, which may be caused by individual intolerance to the components that make up these tablets, as well as various other reasons.
The replacement should not be made by the patient independently - the use of any analogue can only be prescribed by the attending physician, taking into account the results of the preliminary examination of the patient.
In this medical article you can read: medicine Valsartan. The instructions for use will explain at what pressure the tablets can be taken, what the medicine helps with, what are the indications for use, contraindications and side effects. The annotation presents the forms of release of the drug and its composition.
In the article, doctors and consumers can only leave real reviews about Valsartan, from which you can find out whether the medicine helped in the treatment of arterial hypertension and blood pressure reduction, heart failure in adults and children, for which it is also prescribed. The instructions list analogues of Valsartan, prices of the drug in pharmacies, as well as its use during pregnancy.
Valsartan is an angiotensin II receptor antagonist. Instructions for use indicate that tablets or capsules of 20 mg, 40 mg, 80 mg, 160 mg effectively reduce blood pressure.
Release form and composition
The drug Valsartan is available in the form:
- Film-coated tablets 40 mg, 80 mg, 160 mg.
- Capsules 20 mg, 40 mg, 80 mg, 160 mg.
Each tablet or capsule contains the main active ingredient valsartan in an amount of 20, 40, 80 or 160 mg.
pharmachologic effect
The drug Valsartan is intended for oral administration. After the tablet enters the digestive canal, rapid absorption of the main active components occurs through the mucous membranes into the general bloodstream. The drug affects the AT1 receptors of angiotensin 2, which are located in the vascular endothelium, kidney tissue, cardiac muscle, lung tissue, adrenal cortex and brain.
The therapeutic effect after a single oral dose develops and becomes maximum after 2 hours. Active components medications reduce cardiac muscle hypertrophy, which often develops against the background of a persistent increase in blood pressure.
Within 3 weeks after regular use of the tablets, patients notice significant improvement general condition, normalization of blood pressure, not only in a state of complete rest, but also during physical activity. In patients with chronic heart failure, swelling of the face decreases and lower limbs, the risk of developing post-infarction complications is significantly reduced.
Indications for use
What does Valsartan help with? Tablets are used for arterial hypertension, as well as to increase the survival rate of people with acute heart attack myocardium, which is complicated by left ventricular systolic dysfunction and/or left ventricular failure. In case of chronic heart failure, it is used as a component of complex treatment.
Instructions for use
Valsartan film-coated tablets
The tablets are taken orally, swallowed whole and washed down with water. Recommended dosage: chronic heart failure: initial dose – 40 mg 2 times a day. Within 14 days, taking into account individual tolerability of the drug, the single dose should be gradually increased to 80 mg or 160 mg. This may require reducing the dose of concomitantly used diuretics.
The maximum daily dose is 320 mg; arterial hypertension: initial dose – 80 mg 1 time per day. If there is no desired therapeutic effect after 14–28 days of therapy, the daily dose can be increased to 320 mg or additional diuretics may be prescribed.
To increase survival after a myocardial infarction, the use of Valsartan should be started within the first 12 hours, taking 20 mg 2 times a day. Over the next 14 days, the dose is gradually increased by titration, taking 40 mg, then 80 mg 2 times a day. By the end of the third month of therapy, it is recommended to achieve the target dose of 320 mg per day, taking 160 mg 2 times a day.
When increasing the dose, it is necessary to take into account the patient’s tolerance to the drug. In case of impaired renal function or in elderly patients, no dose adjustment is required. In mild or moderate forms of liver dysfunction of non-biliary origin without cholestasis, the dose of the drug should not exceed 80 mg per day.
Capsules
Capsules are intended for oral administration. Recommended dosage: daily – 80 mg 1 time per day or 40 mg 2 times per day. In the absence of clinical effect, the daily dose can be gradually increased to 320 mg.
Read also: how to take an analogue for blood pressure - .
Contraindications
The drug according to the instructions is not recommended for patients with the following conditions:
- Pediatric practice.
- Severe liver damage.
- Pregnancy and breastfeeding period.
- Individual intolerance to the components included in the drug.
Valsartan should be prescribed with particular caution to patients with the following pathologies:
- Hyponodium diet.
- Kidney failure.
- Dehydration of the body.
- Obstruction of the bile ducts caused by a tumor or stones;
- Renal artery stenosis.
Side effects
- diarrhea;
- dizziness;
- headache;
- rash;
- angioedema;
- cough;
- arterial hypotension;
- vasculitis;
- neutropenia, decrease in hemoglobin and hematocrit;
- increased risk of developing viral infections;
- postural hypotension;
- serum sickness;
- nausea;
- pharyngitis;
- increased bilirubin levels;
- renal dysfunction;
- increased levels of creatinine and urea nitrogen (especially in chronic heart failure);
- general weakness;
- hyperkalemia;
- fatigue;
- postural dizziness.
Children, pregnancy and breastfeeding
Taking Valsartan during pregnancy is strictly contraindicated.
This drug should also not be used in women planning pregnancy. In this case, the doctor should inform women of reproductive age about the possible risk of negative effects of valsartan on the fetus during pregnancy.
If pregnancy occurs during treatment with Valsartan, it should be discontinued as soon as possible. There is no information on the penetration of the drug into breast milk, therefore taking the drug is contraindicated during breastfeeding.
The effectiveness and safety of the drug in children have not been proven.
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.
Drug interactions
The drug enhances the effect of diuretics. Medicines containing potassium, as well as potassium-sparing diuretics, increase the likelihood of hyperkalemia.
Analogues of the drug Valsartan
Analogues are determined by structure:
- Vanatex Combi.
- Tantordio.
- Valsartan Zentiva.
- Valaar.
- Artinova.
- Tareg.
- Valsacor N.
- Diovan.
- Valsacor.
- Valz N (with hydrochlorothiazide).
- Nortivan.
- Ko Diovan.
- Duopress.
- Valsafors.
Vacation conditions and price
The average cost of Valsartan (80 mg tablets No. 30) in Moscow is 108 rubles. The medicine is dispensed in pharmacies with a doctor's prescription.
The shelf life of the tablets is 3 years from the date of production, which is indicated on the packaging. The drug should be stored out of the reach of children at a temperature of no more than 30 degrees.
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Valsartan Zentiva
Buy Valsartan Zentiva in pharmacies
DOSAGE FORMS
film-coated tablets 80 mg
MANUFACTURERS
Zentiva a.s. (Czech Republic)
GROUP
Antihypertensives - angiotensin (AII) receptor blockers
INTERNATIONAL NON-PROPENTED NAME
Valsartan
SYNONYMS
Valz, Valsartan, Valsafors, Valsacor, Diovan, Nortivan, Tantordio
DESCRIPTION
PHARMACHOLOGIC EFFECT
Antihypertensive. Competitively blocks angiotensin II receptors (AT1 subtype), located in blood vessels, heart, kidneys, brain, lungs and adrenal cortex. Suppresses all AT1 receptor-mediated effects of angiotensin II, incl. vasoconstriction and aldosterone secretion. Reduces myocardial hypertrophy in patients with arterial hypertension. Does not affect the content of total cholesterol, triglycerides, glucose and uric acid. With regular use, a persistent decrease in blood pressure occurs within 2-4 weeks. Rapidly absorbed from the gastrointestinal tract. A small part is biotransformed to form an inactive metabolite, and the main part is excreted unchanged mainly in feces and urine. No mutagenic properties have been identified in valsartan.
INDICATIONS FOR USE
Arterial hypertension, chronic heart failure as part of complex therapy.
CONTRAINDICATIONS
Pregnancy and breastfeeding. Hypersensitivity. Restrictions on use: Children's age.
SIDE EFFECT
From the outside nervous system and sensory organs: weakness, headache, dizziness. From the gastrointestinal tract: diarrhea, nausea, abdominal pain, increased activity of liver transaminases. From the cardiovascular system and blood (hematopoiesis, hemostasis): neutropenia, anemia, decreased hematocrit. Other: cough, hyperkalemia, viral infections.
INTERACTION
Strengthens (mutually) the hypotensive effect of diuretics. Potassium-sparing diuretics, as well as drugs containing potassium, increase the risk of hyperkalemia.
OVERDOSE
Symptoms: hypotension, tachycardia or bradycardia. Treatment: symptomatic therapy; dialysis is ineffective.
SPECIAL INSTRUCTIONS
Caution should be exercised when prescribing to patients with sodium deficiency and/or a marked decrease in circulating blood volume (due to an increased risk of developing excessive arterial hypotension), with bilateral renal artery stenosis or renal artery stenosis of a single kidney (monitoring of serum creatinine and urea nitrogen concentrations is necessary). ), with severe renal impairment, severe liver dysfunction, biliary cirrhosis, biliary obstruction, with concomitant use of potassium-sparing diuretics, potassium preparations or potassium-containing supplements. Use with caution when working for drivers Vehicle and people whose profession is associated with increased concentration.
STORAGE CONDITIONS
List B. The drug should be stored out of the reach of children at a temperature not exceeding 30°C.
