Universal reference book for medicines
Product name: TAREG (TAREG)

Active substance: valsartan

Type: Angiotensin II receptor antagonist

Manufacturer: NOVARTIS PHARMA (Switzerland) NOVARTIS PHARMA EGYPT (Egypt)
Composition, form of production and packaging
Tablets, film-coated
1 tab.

valsartan 80 mg

14 pcs.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (4) - packs of cardboard.
14 pcs.
- blisters (7) - packs of cardboard.
Tablets, film-coated 1 tab.

valsartan 40 mg

14 pcs.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (4) - packs of cardboard.
14 pcs.
- blisters (7) - packs of cardboard.
Tablets, film-coated 1 tab.

valsartan 80 mg

14 pcs.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (4) - packs of cardboard.
14 pcs.
- blisters (7) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Valsartan is an active specific antagonist of angiotensin II receptors, intended for oral administration.
Selectively blocks receptors of the subtype AT 1 , which are responsible for the effects of angiotensin II. The consequence of the blockade of AT 1 -receptors is an increase in the plasma concentration of angiotensin II, which can stimulate unblocked AT 1 -receptors. Valsartan does not have any marked agonistic activity with respect to AT 1 -receptors. The affinity of valsartan for the receptors of the AT1 subtype is approximately 20,000 times higher than that of the AT 2 receptor subtype. Valsartan does not interact and does not block the receptors of other hormones or ion channels that are important in regulating the functions of the cardiovascular system.
The likelihood of coughing with valsartan is very low, which is due to the lack of influence on the ACE, which is responsible for the degradation of bradykinin.
A comparison of valsartan with an ACE inhibitor demonstrates that the incidence of dry cough is significantly (p <0.05) lower in patients taking the drug than in patients taking an ACE inhibitor (2.6% versus 7.9%, respectively). In the group of patients who previously developed a dry cough with the ACE inhibitor, in valsartan treatment this undesirable phenomenon (AE) is noted in 19.5% of cases, and in the treatment with thiazide diuretic - in 19.0% of cases, while in the group of patients, treated with an ACE inhibitor, cough was observed in 68.5% of cases (p <0.05).
Application for arterial hypertension

In the treatment of valsartan in patients with arterial hypertension, a decrease in blood pressure is noted, not accompanied by a change in heart rate.

After application of a single dose of the drug in most patients, the onset of antihypertensive action is observed within 2 hours, and the maximum decrease in blood pressure is reached within 4-6 hours, which lasts more than 24 hours. With repeated use of the drug, the maximum decrease in blood pressure, regardless of the dose, is achieved within 2-4 weeks, and is maintained at the achieved level during prolonged therapy.
In the case of simultaneous application of the drug with hydrochlorothiazide, a significant additional decrease in blood pressure is achieved. A sharp discontinuation of valsartan is not accompanied by a significant increase in blood pressure or other AEs. In patients with arterial hypertension, type 2 diabetes and nephropathy, taking valsartan in a dose of 160-320 mg, there is a significant decrease in proteinuria (36-44%).
Application after acute myocardial infarction

When the drug is used for 2 years in patients between 12 hours and 10 days after acute myocardial infarction (complicated by left ventricular failure and / or left ventricular systolic dysfunction), the overall mortality, cardiovascular mortality and the time to the first hospitalization by the exacerbation of chronic heart failure, repeated myocardial infarction, sudden cardiac arrest and stroke (without a lethal outcome).
The safety profile of valsartan in patients with acute myocardial infarction is similar to that in other conditions.
Chronic heart failure (CHF)

When using valsartan (at 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 NYHA classification with left ventricular ejection fraction (LV) (93%), diuretics (86%), digoxin (67%), and beta-blockers (36%) show a significant decrease (less than 40%) and an internal diastolic diameter of more than 2.9 cm / m 2 , receiving standard therapy, including ACE inhibitors on 27.5%) of the risk of hospitalization for worsening of the course of CHF.

In patients who did not receive ACE inhibitors, there was a significant reduction in the overall mortality rate (by 33%), cardiovascular mortality and incidence associated with CHF (time to the onset of the first cardiovascular event), which are estimated by the following indicators: death, sudden death with resuscitation, hospitalization for exacerbation of CHF flow, intravenous injection of inotropic or vasodilating drugs for 4 or more hours without hospitalization (by 44%).
In the group of patients receiving ACE inhibitors (without beta-blockers), there is no reduction in the overall mortality rate with valsartan, but the cardiovascular mortality and morbidity associated with CHF decrease by 18.3%.
In general, the use of valsartan reduces the number of hospitalizations for CHF, slows the progression of CHF, improves the functional class of CHF in the NYHA classification, increases the ejection fraction, and decreases the signs and symptoms of heart failure and improves quality of life compared with placebo.

PHARMACOKINETICS

Suction

After taking the drug, suction of valsartan occurs rapidly, C max of the drug in the blood plasma is reached within 2-4 hours. The average absolute bioavailability is 23%.
When using valsartan with food, AUC and C max decrease by 40% and 50%, respectively, although starting from about the 8th hour after taking the drug, the concentration of valsartan in the blood plasma, both in the case of fasting, and in the case of admission food, the same. The decrease in AUC, however, is not accompanied by a clinically significant decrease in the therapeutic effect, so valsartan can be taken regardless of the time of ingestion.
Distribution

V d of valsartan in the equilibrium period after IV injection was about 17 L, which indicates the lack of extensive distribution of valsartan in the tissues.
Valsartan largely binds to serum proteins (94-97%), mainly with albumins.
Metabolism

Valsartan is not subjected to a pronounced metabolism (about 20% of the dose is determined in the form of metabolites).
The hydroxyl metabolite is determined in blood plasma at low concentrations (less than 10% of the valsartan AUC). This metabolite is pharmacologically inactive. Excretion
Valsartan is biphasic: the? -phase with T 1/2 is less than 1 h and the? -phase with T 1/2 is about 9 hours.
Valsartan is excreted mainly unchanged through the intestine (about 83%) and kidneys (about 13%). After iv introduction, the plasma clearance of valsartan is about 2 l / h and its renal clearance is 0.62 l / h (about 30% of the total clearance). T 1/2 of valsartan is 6 hours.
Pharmacokinetics in selected groups of patients

In this category of patients, the time to reach C max and T 1/2 is similar to that of healthy volunteers.
The increase in AUC and C max is directly proportional to the increase in the dose of the drug (from 40 mg to 160 mg 2 times). The cumulation factor averages 1.7. When administered, the clearance of valsartan was approximately 4.5 l / h. The age of patients with CHF did not affect the clearance of valsartan.
In some patients over the age of 65, systemic bioavailability of valsartan is higher than that of young patients, however, there is no clinical significance.

Correlation between renal function and systemic bioavailability of valsartan is absent.
In patients with impaired renal function and creatinine clearance (CK) of more than 10 ml / min, dose adjustment is not required. Currently, there is no data on the use in patients on hemodialysis. Valsartan has a high degree of binding to blood plasma proteins, so its elimination in hemodialysis is unlikely.
In patients with mild and moderate impairment of liver function, the bioavailability (AUC) of valsartan is increased by a factor of 2 compared to healthy volunteers.However, there is no correlation between the values ​​of AUC of valsartan and the degree of impaired hepatic function.
The use of the drug in patients with severe impairment of liver function has not been studied.
INDICATIONS

- arterial hypertension;

- chronic heart failure (II-IV functional class according to NYHA classification) in patients receiving standard therapy, incl.
diuretics, cardiac glycosides, as well as ACE inhibitors or beta-blockers (not simultaneously). The use of each of these drugs is not mandatory;
- to improve the survival of patients after acute myocardial infarction complicated by left ventricular failure and / or left ventricular systolic dysfunction, with stable hemodynamic parameters.

DOSING MODE

Tablets are taken orally, without chewing.

Arterial hypertension

The recommended initial dose of Tape is 80 mg 1 time / day, regardless of race, age and sex of the patient.
Hypotensive effect is noted in the first 2 weeks of treatment; the maximum effect develops after 4 weeks. For those patients who do not achieve an adequate therapeutic response, the daily dose of Taper can be gradually increased to a maximum daily dose of 320 mg in 2 divided doses or diuretics should be used additionally.
Chronic heart failure

The recommended initial dose of Taper is 40 mg 2 times / day.
The dose of the drug should be gradually increased for at least 2 weeks to 80 mg 2 times / day, and with good tolerability - up to 160 mg 2 times / day. The maximum daily dose is 320 mg in 2 divided doses. It may be necessary to reduce the dose of concurrently taken diuretics.
To improve the survival of patients after acute myocardial infarction

Treatment should be started within 12 hours after myocardial infarction.
The initial dose is 20 mg (1/2 tablets 40 mg) 2 times / day. The dose is increased by titration (40 mg, 80 mg, 160 mg 2 times / day) for the next several weeks, until the target dose of 160 mg 2 times / day is reached.
The maximum daily dose is 320 mg in 2 divided doses.
It is usually recommended to increase the dose to 80 mg 2 times / day by the end of 2 weeks of treatment.Achievement of the maximum target dose of 160 mg 2 times / day is recommended by the end of 3 months of therapy with Tapeg. The increase in dose depends on the tolerability of Tape during the titration period.
In the case of development of arterial hypotension accompanied by clinical manifestations, or renal dysfunction should consider reducing the dose.

Evaluation of the condition of patients, in the period after the transferred myocardial infarction, should include an evaluation of the kidney function.

In elderly patients older than 65 years, dose adjustment is not required.

In patients with impaired renal function , dose adjustment is not required.

Patients with mild or moderate impairment of non- biliary liver function without cholestasis should be administered with caution, the daily dose should not exceed 80 mg.

SIDE EFFECT

In patients with hypertension in controlled clinical trials, the incidence of adverse events was comparable to placebo.
There is no data on the dependence of the frequency of any of the undesirable events on the dose or duration of treatment, as well as sex, age or race.
Below are the undesirable phenomena that have been observed during clinical trials, as well as with the use of the drug in clinical practice.

To assess the frequency of adverse events, the following criteria were used: "very often" (> 1/10), "often" (> 1/100, <1/10) "infrequently" (> 1/1000, <1/100), " rarely "(> 1/10 000, <1/1000)," very rarely "(<1/10 000), including individual messages.
Within each group allocated according to frequency of occurrence, undesirable phenomena are distributed in order of decreasing importance.
For all the undesirable phenomena revealed in clinical practice and in the analysis of laboratory indicators (the frequency of development of which can not be established), the gradation "frequency is unknown" was used.
Patients with arterial hypertension.
On the part of the hematopoiesis system : the frequency is unknown - a decrease in hemoglobin, hematocrit, neutropenia, thrombocytopenia.

From the side of the immune system: the frequency is unknown - reactions of hypersensitivity, including serum sickness.

Metabolic disorders: the frequency is unknown - an increase in the potassium content in the blood serum.

From the side of the organ of hearing and labyrinthine disorders: infrequently - vertigo.


From the cardiovascular system: the frequency is unknown - vasculitis.


From the respiratory system: infrequently - cough.

From the digestive system: infrequently - pain in the abdomen.

From the hepatobiliary system: the frequency is unknown - a violation of the liver, including an increase in the concentration of bilirubin in the blood plasma.

From the skin and subcutaneous tissue: very rarely-angioneurotic edema, skin rash, itching.

From the musculoskeletal system: the frequency is unknown - myalgia.

From the side of the kidneys: the frequency is unknown - renal dysfunction, increased serum creatinine concentration.

Other: infrequently - increased fatigue.

Also in the course of clinical studies, the following adverse events were observed in patients with arterial hypertension: the cause-and-effect relationship with the drug was not established: arthralgia, asthenia, back pain, diarrhea, dizziness, insomnia, decreased libido, nausea, peripheral edema, pharyngitis, rhinitis, sinusitis, upper respiratory tract infections, viral infections.

Patients receiving Tareg after acute myocardial infarction and / or CHF.

On the part of the hematopoiesis system: the frequency is unknown - thrombocytopenia.

From the side of the immune system: the frequency is unknown - reactions of hypersensitivity, including serum sickness.

Metabolic disorders: infrequently - hyperkalemia;
frequency is unknown; -increase of potassium content in serum.
From the nervous system: often - dizziness, postural dizziness;
infrequently - a syncope, a headache.
From the side of the organ of hearing and labyrinthine disorders: infrequently - vertigo.

From the side of the cardiovascular system: often - a marked decrease in blood pressure, orthostatic hypotension;
infrequently - increased symptoms of chronic heart failure; frequency is unknown - vasculitis.
From the respiratory system: infrequently - cough.

From the digestive system: infrequently - nausea, diarrhea.

From the hepatobiliary system: the frequency is unknown - a violation of the liver.

From the skin and subcutaneous tissue: very rarely - angioedema;
frequency unknown - skin rash, itching.
From the musculoskeletal system: the frequency is unknown - myalgia.

From the kidneys: often - a violation of kidney function;
infrequently - acute renal failure, increased serum creatinine concentration; frequency is unknown - an increase in the content of nitrogen in the urine.
Common violations: infrequent - asthenia, increased fatigue.

CONTRAINDICATIONS

- Pregnancy;

- lactation period;

- severe violations of the liver, biliary cirrhosis and cholestasis;

- age up to 18 years;

- Hypersensitivity to any of the components of the drug.

Take care with bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney, while observing a diet with restriction of consumption of table salt;
at conditions accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting); in patients with SC less than 10 ml / min, incl. hemodialysis patients with mild or moderate impairment of liver function of non-biliary origin without cholestasis, mitral or aortic stenosis, hypertrophic obstructive cardiomyopathy, and in patients after kidney transplantation.
PREGNANCY AND LACTATION

Given the mechanism of action of angiotensin II receptor antagonists, the risk to the fetus can not be ruled out.
The effect of ACE inhibitors on the fetus, if used in the II and II trimesters of pregnancy, can lead to its damage and death. According to the retrospective data, when using ACE inhibitors in the first trimester of pregnancy, the risk of having children with congenital defects increases. There are reports of spontaneous abortions, oligohydramnios and renal dysfunction in newborns whose mothers accidentally received valsartan during pregnancy. Tapeg, like any other drug that directly affects RAAS, should not be used during pregnancy, as well as in women planning a pregnancy. When using agents that affect RAAS, the doctor should inform women of childbearing age of the potential risk of adverse effects of these drugs on the fetus during pregnancy. If pregnancy is diagnosed during treatment with Taper, treatment should be discontinued as soon as possible.
It is not known whether valsartan is excreted in breast milk.
Therefore, do not use the drug during lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER

In patients with impaired renal function, dose adjustment is not required


APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in severe violations of liver function, biliary cirrhosis and cholestasis.

Patients with mild to moderate hepatic impairment nebiliarnogo genesis without signs of cholestasis drug should be used with caution, the daily dose should not exceed 80 mg.
APPLICATION FOR CHILDREN

Is contraindicated in children under 18 years old.
APPLICATION IN ELDERLY PATIENTS

Elderly patients over 65 years of correction dose is not required.
SPECIAL INSTRUCTIONS

During treatment in patients with hypertension do not require regular monitoring of laboratory parameters.
The deficit in the body of sodium and / or reduction bcc
Patients with severe deficiency in the body of sodium and / or reduced BCC, for example, receiving high doses of diuretics, in rare cases, at the beginning of treatment can develop hypotension accompanied by clinical manifestations. Before beginning treatment with Tapeg correction should be carried out in the sodium content of the body and / or to fill the bcc, including by reducing the dose of a diuretic.
Renal artery stenosis
The use of a short course of the drug in patients with renovascular hypertension, which developed secondary to unilateral renal artery stenosis only, does not lead to any significant change in parameters of renal hemodynamics, concentrations of serum creatinine or blood urea nitrogen. However, given that other drugs that affect the RAAS can cause increase in the concentration of urea and serum creatinine in patients with bilateral renal artery stenosis or stenosis of the artery to a solitary kidney, as a precaution we recommend monitoring these indicators.
primary aldosteronism
The drug is not effective for the treatment of hypertension in patients with primary hyperaldosteronism since this category of patients is not marked activation of the RAAS.
CHF / post-myocardial infarction
patients with heart failure or post-myocardial infarction, treatment with Tapeg beginners, often marked by a decrease in blood pressure, and therefore it is recommended to monitor blood pressure at the beginning of therapy. Subject to
recommendations on dosing regimen is usually not necessary to cancel Tapeg drug due to hypotension. Assessment of CHF patients condition should include assessment of renal function. As a consequence of inhibiting the RAAS, some patients may be impaired renal function. In patients with CHF II-IV functional class NYHA classification treatment with ACE inhibitors and angiotensin II receptor antagonists may be associated with oliguria and / or increase of azotemia and in rare cases of acute renal failure and / or death. Therefore, the data categories of patients using the drug Tapeg before and periodically during treatment with the drug, it is necessary to assess renal function.
Combination therapy for hypertension
When hypertension Tapeg preparation may be used in monotherapy as well as in conjunction with other antihypertensives, in particular diuretics.
Combination therapy during the post-myocardial infarction
possible to use Tapeg drug in combination with other drugs used after myocardial infarction, namely: thrombolytics, aspirin as antiplatelet drugs, beta-blockers and inhibitors of HMG-CoA reductase. In this category of patients is not recommended Tapeg drug concurrently with ACE inhibitors, since this combination therapy has advantages over monotherapy with valsartan or ACE inhibitor in relation to total mortality for any reason.
Combination therapy for CHF
In CHF Tapeg formulation can be applied as a monotherapy, and together with other agents - diuretics, cardiac glycosides, ACE inhibitors and beta-blockers or. In this category of patients is not recommended the use of a triple combination therapy with an ACE inhibitor, a beta-blocker and drug Tapeg.
Effects on ability to drive vehicles and management mechanisms.
As the drug therapy may develop adverse effects such as dizziness or syncope, patients receiving the drug Tapeg, caution should be exercised when driving and other lesson potentially dangerous activities.
OVERDOSE

Symptoms at overdose Tapeg main manifestation is a marked decrease in blood pressure, which can lead to inhibition of consciousness, collapse and / or shock.
Treatment:symptomatic, the nature of which depends on the time elapsed since administration of the drug, and the degree of severity of symptoms. In case of accidental overdose, induce vomiting (if the drug was recently adopted) or to gastric lavage. In case of severe hypotension, the patient should be laid, raising legs to the desired therapy period of time, to take proactive measures to support the cardiovascular system, including regular monitoring of the heart and respiratory system, blood volume (CBV), and the number of allocated urine. In marked decrease in blood pressure as a therapy is necessary in / in a 0.9% sodium chloride solution.
DRUG INTERACTION

It is found that when monotherapy valsartan no clinically significant interactions with the following drugs: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine, glibenclamide.
At the same time the use of valsartan with NSAIDs may reduce its antihypertensive action. In the application of angiotensin II receptor antagonists in conjunction with NSAID may worsening renal function and improvement of potassium in the blood plasma. If necessary, concomitant use of valsartan and NSAIDs prior treatment is necessary to evaluate kidney function and correcting violations of water-electrolyte balance.
When applied in conjunction with ACE inhibitors, drugs lithium marked increase lithium content in the blood plasma and increased its toxic action. Taper is not recommended to use simultaneously with lithium drugs (application experience is limited). If necessary, the joint use of the drug and lithium Tapeg drugs should provide control lithium contents in blood plasma.
While the use of biologically active additives containing potassium, potassium-sparing diuretics, potassium-containing salt substitutes or other drugs that may cause increased potassium content of the blood (e.g., heparin), care should be taken to carry out regular monitoring the potassium content in the blood.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

Storing the drug in a dry place at a temperature not higher than 30 ° C.
Keep out of the reach of children.
Shelf life - 3 years.

The drug should not be used after the expiration date.
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