Composition, form of production and packaging
The tablets covered with a film cover of yellow color, oval, biconcave, with marking "V" on the one hand, risk from the other side and lateral risks.
1 tab.
valsartan 40 mg
Excipients: lactose monohydrate 21.11 mg, microcrystalline cellulose 18 mg, croscarmellose sodium 5.4 mg, povidone K29-32 3.6 mg, talc 0.9 mg, magnesium stearate 0.63 mg, silicon colloidal dioxide 0.36 mg.
The composition of the film shell: opadray II 85G32407 yellow - 3.6 mg (polyvinyl alcohol - 1.584 mg, talc - 0.72 mg, titanium dioxide - 0.598 mg, macrogol 3350 - 0.444 mg, iron oxide oxide yellow - 0.128 mg, lecithin - 0.126 mg).
7 pcs. - blisters (2) - packs of cardboard.
7 pcs. - blisters (4) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
14 pcs. - blisters (4) - packs of cardboard.
14 pcs. - blisters (7) - packs of cardboard.
The tablets covered with a film covering of pink color, round, biconcave, with risk from two parties, lateral risks and marking "V" on the one hand.
1 tab.
valsartan 80 mg
Excipients: lactose monohydrate 42.22 mg, microcrystalline cellulose 36 mg, croscarmellose sodium 10.8 mg, povidone K29-32 7.2 mg, talc 1.8 mg, magnesium stearate 1.26 mg, silicon dioxide colloid 0.72 mg.
Composition of the film sheath: opedrai II 85G34643 pink 7.2 mg (polyvinyl alcohol 3.168 mg, talc 1.44 mg, titanium dioxide 1.373 mg macrogol 3350 0.889 mg iron oxide yellow oxide 0.029 mg iron oxide red 0.049 mg , lecithin - 0.252 mg).
7 pcs. - blisters (2) - packs of cardboard.
7 pcs. - blisters (4) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
14 pcs. - blisters (4) - packs of cardboard.
14 pcs. - blisters (7) - packs of cardboard.
The tablets covered with a film cover of yellow color, oval, biconcave, with risk on the one hand, lateral risks and labeling "V" on the other hand.
1 tab.
valsartan 160 mg
Excipients: lactose monohydrate - 84.44 mg, microcrystalline cellulose - 72 mg, croscarmellose sodium - 21.6 mg, povidone K29-32 - 14.4 mg, talc - 3.6 mg, magnesium stearate - 2.52 mg, silicon colloidal dioxide - 1.44 mg.
The composition of the film shell: opadray II 85G32408 yellow - 14.4 mg (polyvinyl alcohol - 6.336 mg, talc - 2.88 mg, titanium dioxide 1.976 mg, macrogol 3350-1.778 mg, iron dye oxide yellow 0.91 mg, iron oxide red oxide 0.016 mg , lecithin - 0.504 mg).
7 pcs. - blisters (2) - packs of cardboard.
7 pcs. - blisters (4) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - 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 2016.
PHARMACHOLOGIC EFFECT
Peripheral vasodilator, has an antihypertensive effect. The specific blocker of AT 1 -receptor angiotensin II, does not inhibit ACE. Does not affect the content of total XC, TG, glucose and uric acid in the blood.
The onset of the effect occurs 2 hours after ingestion, the maximum after 4-6 hours; the duration of the action is more than 24 hours. After regular administration, the maximum decrease in blood pressure occurs in 2-4 weeks. There is no withdrawal syndrome with sudden discontinuation of admission.
PHARMACOKINETICS
Suction
After taking the drug inside absorption is fast, the degree of absorption is variable. The average value of absolute bioavailability is 23%. When taking the drug with food AUC valsartan decreased by 48%, although starting from about 8 hours after taking the drug, the concentration of valsartan in the blood plasma, both in the case of its reception on an empty stomach, and in the case of food intake, are the same. AUC reduction is not accompanied by a clinically significant decrease in the therapeutic effect of valsartan, so the drug can be used regardless of food intake.
In the range of doses studied, the kinetics of valsartan is linear. The pharmacokinetic curve of valsartan has a downward multi-exponential character.
Distribution
The binding with plasma proteins (mainly with albumins) is high - 94-97%. When the equilibrium state is reached, V d is 17 liters.
With repeated use of valsartan, no changes in the kinetic parameters were noted. When taking the drug at a dose of 1 time / day, there was an insignificant cumulation of valsartan.
Metabolism
Pharmacologically inactive hydroxymetabolite is found in blood plasma at low concentrations (less than 10% of Valsartan AUC).
Excretion
T 1/2? - <1 h, T 1/2? is about 9 hours.
After ingestion, 83% of valsartan is excreted with bile through the intestine and 13% by the kidneys, mostly unchanged.
In comparison with the hepatic blood flow (about 30 l / h), the plasma clearance of valsartan is relatively small (about 2 l / h). At a normal level of glomerular filtration (120 ml / min), the kidney clearance is about 30% of the total plasma clearance.
Pharmacokinetics in special clinical cases
The concentration of valsartan in the blood plasma does not differ between men and women.
INDICATIONS
- arterial hypertension;
- chronic heart failure (IIHA functional class according to NYHA classification) - as part of complex therapy (excluding the combination of valsartan + ACE inhibitor + beta adrenoblocker);
- to improve the survival of patients with acute myocardial infarction (from 12 hours to 10 days) complicated by left ventricular failure and / or left ventricular systolic dysfunction, with stable hemodynamic parameters.
DOSING MODE
Assign inside, regardless of food intake, drinking with a sufficient amount of liquid.
With arterial hypertension, the recommended initial dose of Vals is 80 mg 1 time / day. The hypotensive effect develops in the first 2 weeks of therapy. The maximum effect is achieved after 4 weeks of taking the drug. In patients for whom a daily dose of 80 mg does not give the desired therapeutic effect, it is recommended to increase the daily dose to 160 mg. Additionally, another antihypertensive agent (e.g., a diuretic) may be administered.
In chronic heart failure, the recommended initial dose of Vals is 40 mg twice daily. With insufficient therapeutic effect, a gradual increase in the dose to 80 mg 2 times / day is required and with good tolerability - up to 160 mg 2 times / day. From the moment of the beginning of treatment with Valz until the maximum dose is reached, an interval of at least 2 weeks should be observed. The maximum daily dose is 320 mg in 2 divided doses. It is possible to lower doses while taking diuretics.
Valz can be used in combination with other medicines intended for the treatment of chronic heart failure. However, Valz should not be administered in combination with an ACE + beta-blocker inhibitor.
After myocardial infarction with stable hemodynamics, treatment can be started within 12 hours after acute myocardial infarction. The initial dose of 20 mg (1/2 tablets 40 mg) 2 times / day, followed by an increase in the dose to 40 mg, 80 mg, 160 mg 2 times / day for several weeks, until the maximum daily dose of 160 mg 2 times / day. Reaching a dose of 80 mg 2 times / day is recommended by the end of the second week of treatment, 160 mg 2 times / day - by the end of 3 months of therapy. The dose should be increased taking into account the tolerability of the drug. In case of symptomatic arterial hypotension or in case of impaired renal function The dose of Vals should be reduced.
In patients with impaired renal function with QC greater than 10 ml / min, dose adjustment is not required.
In patients with mild and moderate impairment of liver function without development of cholestasis, the maximum daily dose of Valz should not exceed 80 mg.
SIDE EFFECT
Determination of the frequency of adverse reactions: very often (? 1/10); often (? 1/100, but <1/10); sometimes (? 1/1000, but <1/100); rarely (? 1/10 000, but <1/1000); very rarely (<1/10 000).
From the cardiovascular system: often - orthostatic hypotension 2 ; sometimes - a decrease in blood pressure 1,2 , heart failure 1 ; rarely - vasculitis; very rarely bleeding.
From the respiratory system: sometimes - cough.
On the part of the digestive system: sometimes - diarrhea, abdominal pain; very rarely - nausea 4 .
From the side of the central nervous system: often - postural dizziness 2 ; sometimes - fainting 1 , insomnia, depression, decreased libido; rarely - dizziness 4 , neuralgia; very rarely - headache 4 .
From the side of the hearing organ and labyrinthine apparatus: sometimes - vertigo.
From the hemopoietic system: often - neutropenia, very rarely - thrombocytopenia.
Allergic reactions: rarely - serum sickness, hypersensitivity; very rarely - angioedema, edema, skin rash, itching.
From the musculoskeletal system: sometimes - back pain, muscle cramps, arthritis, myalgia; very rarely - arthralgia.
From the side of the urinary system: very rarely - renal dysfunction 3.4 , acute renal failure 3 .
From the side of metabolism: sometimes - hyperkalemia 1,2 .
Infections: often - viral infections; sometimes - infections of the upper respiratory tract, pharyngitis, sinusitis, conjunctivitis; very rarely - rhinitis, gastroenteritis.
On the part of laboratory indicators: a decrease in hemoglobin and hematocrit, hypercreatininaemia, hyperbilirubinemia, increased activity of hepatic transaminases, an increase in the concentration of urea nitrogen in the serum.
Other: sometimes - a feeling of fatigue, asthenia, nosebleeds, swelling.
1 - reported during treatment after acute myocardial infarction;
2 - reported in the treatment of chronic heart failure;
3 - sometimes reported during treatment after acute myocardial infarction;
4 - the most common during the treatment of chronic heart failure (often - dizziness, dysfunction of the kidneys, arterial hypotension, sometimes - headache, nausea).
CONTRAINDICATIONS
- violations of the liver, associated with obstruction of the biliary tract (including biliary cirrhosis, cholestasis);
- renal failure of severe degree (CC less than 10 ml / min), incl. patients on hemodialysis;
- Pregnancy;
- lactation period (breastfeeding);
- age under 18 years (effectiveness and safety not established);
- lactose intolerance, galactosemia or syndrome of impaired glucose / galactose absorption;
- Hypersensitivity to the components of the drug.
With caution should be used in patients with arterial hypotension, hyperkalemia, against a background of a diet with limited sodium intake, hyponatremia, bilateral stenosis of the renal arteries or stenosis of the single kidney artery, with primary hyperaldosteronism, aortic and mitral stenosis, hypertrophic obstructive cardiomyopathy, conditions accompanied by a decrease in BCC (including diarrhea, vomiting).
PREGNANCY AND LACTATION
There are no data on the use of valsartan in pregnancy. Renal perfusion of the fetus, which depends on the development of RAAS, begins to function in the third trimester of pregnancy. The risk to the fetus increases with the use of valsartan in the II and III trimesters. When establishing a pregnancy, therapy with Vals should be stopped immediately.
There is no data on the isolation of valsartan with breast milk. Therefore, if you need to use the drug during lactation, you should decide whether to stop breastfeeding or to cancel therapy with valsartan, given its importance to the mother.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in patients with severe renal insufficiency (CC less than 10 ml / min), incl. in patients on hemodialysis.
In patients with impaired renal function with QC greater than 10 ml / min, dose adjustment is not required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated use in violations of liver function associated with obstruction of the biliary tract (including biliary cirrhosis, cholestasis).
In patients with mild and moderate impairment of liver function without development of cholestasis, the maximum daily dose of Valz is 80 mg.
APPLICATION FOR CHILDREN
Contraindicated: age under 18 years (efficacy and safety not established).
SPECIAL INSTRUCTIONS
In patients with severe sodium deficiency in the body and / or reduced bcc, for example, due to the use of diuretics in high doses, in rare cases, severe arterial hypotension may develop at the onset of valsartan therapy. Before starting therapy with Vals, it is recommended to restore the electrolyte and fluid content in the body, in particular, by reducing the dose of diuretics.
The drug Valz can be used in conjunction with other drugs intended for the treatment of myocardial infarction, such as thrombolytics, acetylsalicylic acid, beta-adrenoblockers, statins and diuretics. Joint administration of ACE inhibitors is not recommended.
With renovascular hypertension, regular monitoring of urea and creatinine in the blood is necessary.
When combined with preparations containing potassium, its salts and preparations belonging to the group of potassium-sparing diuretics, regular monitoring of the level of potassium in the blood plasma is carried out.
In chronic heart failure at the beginning of treatment with the drug Valz, there may be a slight decrease in blood pressure, so it is recommended to monitor BP at the beginning of therapy.
Due to inhibition of RAAS, some patients may have renal function changes. In patients with severe chronic heart failure, whose renal function depends on RAAS activity, treatment with ACE inhibitors and angiotensin receptor antagonists may be accompanied by oliguria and / or increased azotemia and (rarely) acute renal failure and / or fatal.
It is not recommended joint use of Valz in patients with chronic heart failure, with ACE inhibitors and beta-blockers due to a possible increase in the risk of side effects.
Patients with bilateral or unilateral stenosis of the renal arteries need regular monitoring of creatinine and urea nitrogen in the blood serum.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: a marked decrease in blood pressure, which can lead to loss of consciousness and collapse.
Treatment: gastric lavage, intake of sufficient amount of activated carbon, intravenous administration of 0.9% sodium chloride solution. Valsartan is not excreted during dialysis due to active binding to plasma proteins.
DRUG INTERACTION
When treating arterial hypertension with valsartan, there was no clinically significant interaction with other concomitant medications (for example, cimetidine, warfarin, digoxin, atenolol, amlodipine, glibenclamide, furosemide, indomethacin, hydrochlorothiazide).
Potassium-sparing diuretics, potassium preparations, potassium-containing salts, drugs that raise the level of potassium in the blood plasma (such as heparin) increase the risk of hyperkalemia.
Other antihypertensives and diuretics increase the antihypertensive effect of valsartan.
The antihypertensive effect of the drug may be weakened when combined with NSAIDs, including. with selective inhibitors of COX-2 and acetylsalicylic acid at a dose of more than 3 g / day.
In a joint application with ACE inhibitors, a reversible increase in the concentration of lithium in plasma and the development of toxic effects were reported.
Very limited experience in the use of valsartan and preparations containing lithium. In the case of lithium-containing drugs, control of lithium concentration in blood plasma is recommended in patients receiving Valz.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Shelf life - 3 years.
