WALZ - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 21.11 mg, microcrystalline cellulose 18.00 mg, croscarmellose sodium 5.40 mg, povidone K29-32 3.60 mg, talc 0.9 mg, magnesium stearate 0.63 mg, silicon dioxide colloid 0,3 6 mg;

Film Sheath: Opapray II 85G32407 yellow about 3.60 mg (polyvinyl alcohol 1.584 mg, talc 0.720 mg, titanium dioxide 0.598 mg, macrogol-3350 0.444 mg, iron oxide dye yellow 0.128 mg, lecithin 0.126 mg).

1 tablet of 80 mg contains:

Active substance: valsartan 80 mg;

Excipients: lactose monohydrate 42.22 mg, microcrystalline cellulose 36.00 mg, croscarmellose sodium 10.80 mg, povidone K29-32 7.20 mg, talc 1.8 mg, magnesium stearate 1.26 mg, silicon dioxide colloid 0.72 mg;

Film Sheath: Opapray II 85G34643 Pink about 7.20 mg (polyvinyl alcohol 3.168 mg, talc 1.440 mg, titanium dioxide 1.373 mg, macrogol-3350 0.889 mg, iron oxide oxide yellow 0.029 mg, ferric oxide red oxide 0.049 mg, lecithin 0.252 mg).

1 tablet of 160 mg contains:

Active substance: valsartan 160 mg;

Excipients: lactose monohydrate 84.44 mg, microcrystalline cellulose 72.00 mg, croscarmellose sodium 21.60 mg, povidone K29-32 14.40 mg, talc 3.6 mg, magnesium stearate 2.52 mg, silicon dioxide colloid 1.44 mg;

Film Sheath: Opapray II 85G32408 yellow about 14,40 mg (polyvinyl alcohol 6,336 mg, talc 2,880 mg, titanium dioxide 1,976 mg, macrogol-3350 1,778 mg, iron oxide dye yellow 0,910 mg, iron oxide dye red 0.016 mg, lecithin 0.504 mg).

Description:

For tablets 40 mg: oval, biconvex tablets of yellow color, film-coated, labeled "V" on the one hand, risk on the other hand and lateral risks.

For tablets 80 mg: round biconvex tablets of pink color, covered with a film sheath, with risk from both sides, lateral risks and marking "V" on the one hand.

For tablets 160 mg: oval, biconvex tablets of yellow color, film-coated, with risk on the one hand, lateral risks and labeling "V" on the other hand.

Pharmacotherapeutic group:Angiotensin II receptor blocker

ATX: & nbsp

C.09.C.A.03 Valsartan

C.09.C.A Angiotensin II antagonists

Pharmacodynamics:

Peripheral vasodilator, has an antihypertensive effect. Specific blocker AT₁-receptor angiotensin II, does not inhibit angiotensin-converting enzyme (ACE); does not affect the content of total cholesterol, triglycerides, 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 (BP) occurs in 2-4 weeks.There is no "cancellation" syndrome with sudden discontinuation of admission.

Pharmacokinetics:

After ingestion absorption - fast, the degree of absorption is variable. The average value of absolute bioavailability is 23%. The pharmacokinetic curve of valsartan has a downward multiexponential character (t_1/2α<l h and t_1/2βabout 9 hours).

In the range of doses studied, the kinetics of valsartan is linear. With repeated use of valsartan, no changes in the kinetic parameters were noted. When taking the dose once a day, there was an insignificant cumulation of valsartan. The concentration of valsartan in the blood plasma does not differ between men and women.

Valsartan binds well to blood plasma proteins (94-97%), mainly with serum albumins. When the equilibrium state is reached, the volume of distribution is 17 liters. In comparison with the hepatic blood flow (about 30 l / h), the plasma clearance of valsartan occurs relatively slowly (about 2 l / h). The drug is excreted with bile and kidneys, mostly unchanged. At a normal level of glomerular filtration (120 ml / min), the kidney clearance is about 30% of the total plasma clearance.Hydroxymetabolite is found in blood plasma at low concentrations (less than 10% of the area under the concentration-time curve (AUC) for valsartan). This metabolite is not pharmacologically active. After oral administration, 83% of valsartan is excreted through the intestine and 13% through the kidneys, mostly unchanged.

When taking the drug with food AUC Valsartan is reduced by 48%, although starting from about the 8th hour after taking the drug, the concentration of valsartan in the blood plasma, both in the case of taking it on an empty stomach, and in case of reception with food, are the same. Decrease AUC is not accompanied by a clinically significant decrease in the therapeutic effect of valsartan, so the drug can be used regardless of food intake.

Indications:

- Arterial hypertension;

- chronic heart failure (II-IV functional class by classification NYHA) as part of complex therapy (excluding combination valsartan + and ACE + beta-blocker);

- increased survival of patients with acute myocardial infarction (12 hours-10 days) complicated by left ventricular failure and / or left ventricular systolic dysfunction, with stable hemodynamics

Contraindications:

- Hypersensitivity to valsartan or to the excipients of the drug;

- violations of the liver, associated with obstruction of the biliary tract (including biliary cirrhosis, cholestasis);

- severe renal failure (creatinine clearance (CK) less than 10 ml / min), including patients on hemodialysis;

- pregnancy and lactation;

- age under 18 years (effectiveness and safety not established);

- lactose intolerance, galactosemia or the syndrome of impaired glucose / galactose absorption.

Carefully:

Arterial hypotension, hyperkalemia, diet with sodium restriction, hyponatremia, bilateral stenosis of the renal arteries or stenosis of the single kidney artery, primary hyperaldosteronism, aortic and mitral stenosis, hypertrophic obstructive cardiomyopathy; conditions, accompanied by a decrease in the volume of circulating blood (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 the renin-angiotensin system, begins to function in the third trimester of pregnancy.The risk to the fetus increases with the use of valsartan in the second and third trimesters. When a pregnancy is established, valsartan should be stopped immediately.

There is no data on the isolation of valsartan in breast milk. Therefore, the question of stopping breastfeeding or abolishing valsartan therapy should be addressed, given its importance to the mother.

Dosing and Administration:

Inside, regardless of food intake, with enough liquid.

Arterial hypertension: the recommended initial dose of Vals is 80 mg once a 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.

Chronic heart failure (CHF): the recommended initial dose of Vals is 40 mg 2 times a day. With insufficient therapeutic effect, a gradual increase in the dose to 80 mg 2 times a day is required and with good tolerability - up to 160 mg 2 times a day.From the moment of the beginning of treatment by Valz preparation till the moment of achievement of reception of the maximum dosage there should be an interval not less than two weeks. The maximum daily dose is 320 mg in 2 divided doses. It is possible to lower doses while taking diuretics.

Vals can be used in combination with other medicines intended for the treatment of chronic heart failure. However, taking Valz in combination with an ACE + beta-blocker inhibitor is not recommended (see section Special instructions).

After myocardial infarction: with stable parameters of hemodynamics treatment can be started within 12 hours after acute myocardial infarction. Initial dose - 1/2 tablets 40 mg (20 mg) twice a day, followed by an increase in the dose to 40 mg, 80 mg, 160 mg twice a day for several weeks, until the maximum daily dose of 160 mg twice a day.

Reaching a dose of 80 mg twice a day is recommended by the end of the second week of treatment, 160 mg twice a day - by the end of the third month of therapy. Dose should be increased, based on the patient's tolerability of the drug.

In the case of symptomatic arterial hypotension or with impaired renal function, the dose of Valz should be reduced.

Impaired kidney and liver function

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 effects:

Frequency of side effects: very often (≥1 / 10); often (≥1 / 100, but <1/10); sometimes (≥1 / 1000, but <1/100); rarely (≥1 / 10000, but <1/1000), very rarely (<1/10000).

From the cardiovascular system: often - orthostatic hypotension^#; sometimes - a decrease in blood pressure^*#, heart failure^*; rarely - vasculitis; very rarely bleeding.

From the respiratory system: sometimes - a cough.

From the digestive system: sometimes - diarrhea, abdominal pain; very rarely - nausea^##.

From the central nervous system: often - postural dizziness^#; sometimes - a syncope^*, insomnia, depression, decreased libido; rarely - dizzy^##, neuralgia; very rarely - headache^##.

From the organs of hearing and labyrinth apparatus: sometimes - vertigo.

From the hematopoiesis: often - neutropenia, very rarely - thrombocytopenia. Allergic reactions: rarely - serum sickness; hypersensitivity; very rarely - angioedema^**, skin rash, itching.

From the musculoskeletal system: sometimes - back pain, muscle cramps, arthritis, myalgia; very rarely - arthralgia;

From the side of the urinary tract: very rarely - impaired renal function^**##, acute renal failure^**.

From the side of metabolism: sometimes - hyperkalemia^*#.

Infections: often - viral infections; sometimes - infections of the upper respiratory tract, pharyngitis, sinusitis, conjunctivitis; very rarely - rhinitis, gastroenteritis.

Other: sometimes - a feeling of fatigue, asthenia, epistaxis, swelling.

Laboratory indicators: reduction of hemoglobin and hematocrit, hypercreatininemia, hyperbilirubinemia, increased activity of "liver" transaminases, increased concentration of urea nitrogen in blood serum.

* It was reported during treatment after acute myocardial infarction.

^# It was reported in the treatment of CHF

** Sometimes reported during treatment after acute myocardial infarction

^##The most common during the treatment of CHF (often: dizziness, dysfunction of the kidneys, hypotension, sometimes: headache, nausea)

Overdose:

Symptoms: a marked decrease in blood pressure, which can lead to loss of consciousness and collapse.

Treatment: gastric lavage, intake of a sufficient amount of activated charcoal, intravenous injection of 0.9% sodium chloride solution.

Valsartan is not excreted during dialysis due to active binding to plasma proteins.

Interaction:

When treating arterial hypertension with valsartan, there were no clinically significant interactions with other concomitant medications (for example, cimetidine, warfarin, digoxin, atenolol, amlodipine, glibenclamide, furosemide, indomethacin, hydrochlorothiazide).

Potassium-sparing diuretics, potassium preparations, salts containing potassium, drugs that raise the level of potassium in the blood plasma (such as heparin) increase the development of hyperkalemia.

Other antihypertensives and diuretics increase the antihypertensive effect. The antihypertensive effect of the drug may be weakened when combined with non-steroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of cyclooxygenase-2 (COX-2) and acetylsalicylic acid 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 using drugs containing lithium, it is recommended to control the level of lithium in blood plasma.

Special instructions:

In patients with severe sodium deficiency in the body and / or decreased bcc, for example, due to taking large doses of diuretics, 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-blockers, 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 patients with CHF who start treatment with Valzom, there may be a slight decrease in blood pressure, and therefore it is recommended to monitor BP at the beginning of therapy. Due to inhibition of the renin-angiotensin-aldosterone system, some patients may have renal function changes. In patients with severe CHF, whose kidney function depends on the activity of the renin-angiotensin-aldosterone system, 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 suffering from CHF, with ACE inhibitors and beta-adrenoblockers in view of a possible increase in the risk of side effects.

In patients with bilateral or unilateral stenosis of the renal arteries, regular monitoring of creatinine and urea nitrogen in the blood serum is necessary.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and taking other potentially hazardous activities,requiring increased concentration of attention and speed of motor and mental reactions.

Form release / dosage:Tablets, film-coated, 40 mg, 80 mg, 160 mg.

Packaging:For 7, 10 or 14 tablets in a blister of PVC / PE / PVDC / Aluminum foil. For 2 or 4 blisters for 7 tablets; 1, 2, or 3 blisters for 10 tablets, 4 or 7 blisters for 14 tablets together with instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001773/09

Date of registration:10.03.2009 / 30.10.2014

Expiration Date:Unlimited

The owner of the registration certificate:AKTAVIS GROUP, AO AKTAVIS GROUP, AO Iceland

Manufacturer: & nbsp

ACTAVIS, Ltd. Iceland

BALKANPHARMA-DUPNITSA, AD Bulgaria

Representation: & nbspAktavis, Open Company Aktavis, Open Company

Information update date: & nbsp18.01.2017

Illustrated instructions

Instructions

Wales (Valz)