Valsartan tablets p / o 160mg, No. 30

Treatment of arterial hypertension.

Treatment of chronic heart failure (II-IV functional class according to NYHA classification) in patients receiving traditional therapy with diuretics, digitalis drugs, as well as ACE inhibitors or beta-blockers.

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken orally at a dose of 80 mg 1 time / day or 40 mg 2 times / day, daily. In the absence of an adequate effect, the daily dose can be gradually increased.

The maximum daily dose is 320 mg in 2 divided doses.

Valsartan

• age under 18;

• severe form (above 9 points on the Child - Pugh scale) liver dysfunction, cholestasis, biliary cirrhosis;

• concomitant therapy with angiotensin II receptor antagonists or ACE (angiotensin converting enzyme) inhibitors with aliskiren in patients with diabetes mellitus;

• the period of planning pregnancy and bearing a child;

• breast-feeding;

• individual hypersensitivity to drug components

Caution should be given to patients who limit the consumption of sodium chloride, with bilateral stenosis of the 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 volume blood volume (BCC) (including conditions with diarrhea and vomiting), hepatic failure of non-biliary genesis of mild to moderate severity (without cholestasis), hypertrophic obstructive cardiomyopathy, chronic heart failure II Ц IV functional class according to the NYHA classification, mitral or aortic stenosis.

Clinical and pharmacological group: Angiotensin II receptor antagonist

Pharmaco-therapeutic group: Angiotensin II receptor antagonist

pharmachologic effect

Antihypertensive agent. It is a specific antagonist of angiotensin II receptors. It has a selective antagonistic effect on AT1 receptors, which are responsible for the realization of 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. Has no 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 or block other hormone receptors or ion channels, which are important for the regulation of the functions of the cardiovascular 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 its 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. The absolute bioavailability averages 23%. The pharmacokinetic curve of valsartan has a multi-exponential character (T1 / 2 in the ?-phase <1 h and T1 / 2 in the ?-phase - about 9 hours), the kinetics is linear.

No changes in pharmacokinetic parameters were observed with course use.

When taking valsartan with food, the AUC decreases by 48%, while approximately 8 hours after taking valsartan plasma concentrations 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 in the therapeutic effect.

When taking valsartan 1 time / day, the cumulation is not significantly expressed. Plasma concentrations of valsartan in women and men were the same.

Plasma protein binding, mainly albumin, is 94-97%. Vd in equilibrium is about 17 liters.

Plasma clearance of valsartan is about 2 l / h. It is excreted in the feces - 70% and in the urine - 30%, mainly unchanged.

With biliary cirrhosis or obstruction of the biliary tract, the AUC of valsartan increases approximately 2 times.

Indications

Treatment of arterial hypertension.

Treatment of chronic heart failure (II-IV functional class according to NYHA classification) in patients receiving traditional therapy with diuretics, digitalis drugs, as well as ACE inhibitors or beta-blockers.

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken orally at a dose of 80 mg 1 time / day or 40 mg 2 times / day, daily. In the absence of an adequate effect, the daily dose can be gradually increased.

The maximum daily dose is 320 mg in 2 divided doses.

Side effect

From the side of 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, a decrease in hemoglobin and hematocrit.

Allergic reactions: rarely - angioedema, rash, itching, serum sickness, vasculitis.

Others: fatigue, general weakness, cough, pharyngitis, increased risk of viral infections.

Contraindications for use

• age under 18;

• severe form (above 9 points on the Child - Pugh scale) liver dysfunction, cholestasis, biliary cirrhosis;

• concomitant therapy with angiotensin II receptor antagonists or ACE (angiotensin converting enzyme) inhibitors with aliskiren in patients with diabetes mellitus;

• the period of planning pregnancy and bearing a child;

• breast-feeding;

• individual hypersensitivity to drug components

Caution should be given to patients who limit the consumption of sodium chloride, with bilateral stenosis of the 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 volume blood volume (BCC) (including conditions with diarrhea and vomiting), hepatic failure of non-biliary genesis of mild to moderate severity (without cholestasis), hypertrophic obstructive cardiomyopathy, chronic heart failure II Ц IV functional class according to the NYHA classification, mitral or aortic stenosis.

Application during pregnancy and lactation

Valsartan is contraindicated in pregnancy.

It is not known whether valsartan is excreted in human breast milk. Application during lactation (breastfeeding) is not recommended.

In experimental studies have shown that valsartan is excreted in breast milk in rats.

Application for impaired renal function

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 in predisposed patients, changes in renal function are possible.

Application in children

The safety and efficacy of valsartan in children has not been established.

special instructions

With hyponatremia and / or a decrease in BCC, as well as during therapy with high doses of diuretics, in rare cases, valsartan can cause severe arterial hypotension. Before starting treatment, correction of violations of water-salt metabolism should be carried out.

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 impaired biliary patency.

Due to inhibition of the RAAS in predisposed patients, changes in renal function are possible. With the use of ACE inhibitors and angiotensin receptor antagonists in patients with severe chronic heart failure, oliguria and / or an increase in azotemia were observed, acute renal failure with a risk of death rarely developed.

The safety and efficacy of valsartan in children has not been established.

Influence on the ability to drive vehicles and use mechanisms

When using valsartan, it is recommended to be careful when driving and operating machinery.

Drug interactions

With the simultaneous use of diuretics in high doses, the development of arterial hypotension is possible.

With the simultaneous use of potassium-sparing diuretics, heparin, dietary supplements or salt substitutes containing potassium, hyperkalemia may develop.

With simultaneous use with indomethacin, it is possible to reduce the antihypertensive effect of valsartan.

With simultaneous use with lithium carbonate, a case of the development of lithium intoxication has been described.