VALZ

Active material: Valsartan
When ATH: C09CA03
CCF: Angiotensin II receptor antagonists
ICD-10 codes (testimony): I10, I21, I50.0
When CSF: 01.04.02
Manufacturer: ACTAVIS GROUP hf. (Iceland)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills, Film-coated Pink colour, round, lenticular, scored on both sides, side risk and marking “V” one side.

Excipients: lactose monohydrate, microcrystalline cellulose, Croscarmellose sodium, povidone K29-32, talc, magnesium stearate, colloidal silicon dioxide.

The composition of the coating film: Opadraj II 85G34643 pink (polyvinyl alcohol, talc, Titanium dioxide, MACROGOL-3350, dye iron oxide yellow, iron oxide red dye, lecithin).

7 PC. – blisters (4) – packs cardboard.

Pills, Film-coated yellow color, Oval, lenticular, scored on one side, side risk and marking “V” on the other hand.

Excipients: lactose monohydrate, microcrystalline cellulose, Croscarmellose sodium, povidone K29-32, talc, magnesium stearate, colloidal silicon dioxide.

The composition of the coating film: Opadraj II 85G32408 yellow (polyvinyl alcohol, talc, Titanium dioxide, MACROGOL-3350, dye iron oxide yellow, iron oxide red dye, lecithin).

7 PC. – blisters (4) – packs cardboard.

* international non-proprietary name, recommended by the WHO – valzartan.

Pharmacological action

Peripheral vasodilators, provides gipotenzivne effect. Specific blocker AT₁-Angiotensin II receptor , It does not inhibit ACE. Does not affect the contents of General Hs, TG, glucose and uric acid in the blood.

Beginning effect through 2 hours after ingestion, max. – through 4-6 no; duration – more 24 no. After the regular admission maximum decline ad comes through 2-4 of the week. Missing the syndrome with a sudden admission.

Pharmacokinetics

Absorption

After taking the drug inside fast absorption, the intake varied. The mean value of the absolute bioavailability – 23%. When taking the drug with food AUC valsartan decreases by 48%, though, starting around 8 hours after ingestion, concentrations of valsartan in plasma as if I receive it on an empty stomach, and in the case of the reception with food, similar. Reduction in AUC is not accompanied by a clinically significant decrease in therapeutic effect of valsartan, the product can be applied regardless of the meal.

In the range studied doses the kinetics of valsartan has a linear nature. Concentration-time curve of valsartan has the character of a downward multieksponentsialny.

Distribution

Plasma protein binding (mostly to albumin) high – 94-97% . When it reaches the equilibrium State (V)_d – 17 l.

When you reapply a valsartan was observed indicators of kinetic changes. Before the drug at a dose of 1 times/day, there was a slight accumulation of valsartan.

Metabolism

Pharmacologically inactive gidroksimetabolit is found in the blood plasma in low concentrations (less 10% by AUC of valsartan).

Deduction

(T_1/2a < 1 no, T_1/2b is about 9 no).

Once inside 83% valsartan appears to jelchew the intestine and 13% kidney, mainly unchanged.

Compared to hepatic blood flow (about 30 l /), plasma clearance valsartan relatively small (about 2 l /). When normal glomeruliarna filtering (120 ml / min) Kidney klirens is about 30% of the total plasma clearance.

Pharmacokinetics in special clinical situations

Concentrations of valsartan in plasma has no differences in men and women.

Testimony

- Arterial hypertension;

- Congestive heart failure (II-IV functional class NYHA classification) – in the complex therapy (excluding combination of valsartan + ACE inhibitor + selective beta);

to improve the survival rate of patients with acute myocardial infarction (period 12 h to 10 days), complicated by left ventricular failure and / or left ventricular systolic dysfunction, in the presence of a stable hemodynamic.

Dosage regimen

Assign inside, independently of the reception shortages, drinking plenty of fluids.

At hypertension the recommended initial dose is Valz 80 mg 1 time / day. Gipotenzivny effect develops in the first 2 weeks of therapy. The maximum effect is reached after 4 weeks of taking the drug. Patients, for which daily dose 80 mg does not give the desired therapeutic effect, It is recommended to increase the daily dose to 160 mg. Additionally can be assigned another antihypertensive tool (eg, diuretic).

At chronic heart failure the recommended initial dose-at Valz 40 mg 2 times / day. With insufficient therapeutic effect requires a gradual increase in dose to 80 mg 2 times/day and with good endurance – to 160 mg 2 times / day. From the moment you begin treatment with Valz until receiving the maximum dose interval should be observed at least 2 weeks. The maximum daily dose – 320 mg 2 admission. May reduce doses while admission dioretikov.

Valz can be used in combination with other drugs, designed for the treatment of chronic heart failure. However, you should not assign Valz in combination with ACE inhibitor + selective beta.

Post-myocardial infarction When stable hemodynamic performance treatment can be started during 12 hours after acute myocardial infarction. The initial dose - 20 mg (1/2 tab. 40 mg) 2 times / day, with a consequent increase in doses up to 40 mg, 80 mg, 160 mg 2 times per day within a few weeks, to achieve maximum daily dose 160 mg 2 times / day. Achieving a dose 80 mg 2 times per day is recommended by the end of the 2-nd 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 acceptability of the drug. In the case of symptomatic arterial hypotension or If the kidney function Valz dose should be reduced.

In patients with impaired kidney with QC more 10 ml / min dose adjustment is required.

In patients with mild and moderate liver without the development of cholestasis the maximum daily dose should not exceed Valz 80 mg.

Side effect

Determination of the frequency of adverse reactions: Often (≥1/10); often (≥1/100, but < 1/10); sometimes (≥ 1/1000, but < 1/100); rarely (≥ 1/10 000, but <1/1000), rarely (<1/10 000).

Cardio-vascular system: often – orthostatic hypotension²; sometimes – decrease in blood pressure^1,2, heart failure¹; rarely – vasculitis; rarely – bleeding.

The respiratory system: sometimes – cough.

From the digestive system: sometimes – diarrhea, abdominal pain; rarely – nausea⁴.

CNS: often – postural dizziness²; sometimes – fainting¹, insomnia, depression, decreased libido; rarely – dizziness⁴, neuralgia; rarely – headache⁴.

By the authority hearing and labyrinth apparatus: sometimes – vertigo.

From the hematopoietic system: often – neutropenia, rarely – thrombocytopenia.

Allergic reactions: rarely – serum sickness, hypersensitivity; rarely – angioedema³, skin rash, itch.

On the part of the musculoskeletal system: sometimes – backache, muscle cramps, arthritis, myalgia; rarely – arthralgia.

By mochevyvydelitel'noj systems: rarely – impairment of renal function^3,4, acute renal failure³.

Metabolism: sometimes – hyperkalemia^1,2.

Infection: often – viral infections; sometimes – upper respiratory tract infection, pharyngitis, sinusitis, conjunctivitis; rarely – rhinitis, gastroenteritis.

From the laboratory parameters: reduction of hemoglobin and hematocrit, giperkreatininemiя, giperʙiliruʙinemija, increase in liver transaminases, increasing the concentration of urea nitrogen in serum.

Other: sometimes – feeling tired, asthenia, nose bleed, swelling.

¹ – It was reported during the period of treatment after acute myocardial infarction.

² – It has been reported in the treatment of chronic heart failure.

³ – sometimes reported in the period of treatment after acute myocardial infarction.

⁴ – the most frequently occurring during treatment of chronic heart failure (often – dizziness, impairment of renal function, hypotension; sometimes – headache, nausea).

Contraindications

- Abnormal liver function, associated with obstruction of the biliary tract (incl. biliary cirrhosis, cholestasis);

- Severe renal insufficiency (CC less than 10 ml / min), incl. Patients, on hemodialysis;

- Pregnancy;

- Lactation (breast-feeding);

- Up to 18 years (efficacy and safety have not been established);

- Lactose intolerance, galactosemia or syndrome of impaired glucose/Galactose malabsorption;

- Hypersensitivity to the drug.

FROM caution use in patients with hypotension, hyperkalemia, on a diet with restriction of sodium intake, when hyponatremia, bilateral renal artery stenosis or stenosis of the artery to a solitary kidney, with primary hyperaldosteronism, aortic and mitral stenosis, hypertrophic obstructive cardiomyopathy, states, accompanied by a decrease in the bcc (incl. diarrhea, vomiting).

Pregnancy and lactation

Data on the use of valsartan in pregnancy is not. Fetal renal perfusion, which depends on the development of the renin-angiotensin system, begins to function in the III trimester of pregnancy. The risk to the fetus increases when taking valsartan in II and III trimestrah. When establishing pregnancy drug therapy should be discontinued immediately Valz.

No data on the allocation of valsartan with breast milk. Therefore, if necessary, the use of the drug during lactation should decide on the termination of breastfeeding or the abolition of valsartanom therapy in view of its importance for the mother.

Cautions

In patients with a marked shortage of sodium in the body and/or reduced BCC, eg, as a consequence of the admission dioretikov at high doses, in rare cases, it can at the beginning of therapy valsartanom develop expressed arterial gipotenzia. Before starting therapy with Valz we recommend that you restore the electrolytes and fluids in the body, in particular, by reducing the doses of diuretics.

The drug can be used in conjunction with Valz other drugs, intended for treatment of myocardial infarction, such as trombolitiki, acetylsalicylic acid, beta-blockers, Statins and diuretics. Joint reception of ACE inhibitors is not recommended.

When it renovskularna hypertension requires regular monitoring of urea and creatinine in the blood.

When coupled with the use of drugs, containing potassium, its salts and drugs, relating to group kalisberegath dioretikov, conduct regular monitoring of the level of potassium in the blood plasma.

In chronic heart failure in the early drug treatment, there may be a slight decrease Valz HELL , Therefore, we recommend that you monitor ad at the beginning of therapy.

As a result of inhibition of Renin-angiotensin-aldosterone system activity in some patients, changes of kidney function. In patients with severe chronic heart failure, whose kidney function depends on the Renin-angiotensin-aldosterone system activity, treatment with ACE inhibitors and angiotensin receptor antagonists may be accompanied by oliguria and/or increasing азотемии and (rarely) acute renal failure and/or death.

It is not recommended to the joint use of the drug in patients Valz, suffering from chronic heart failure, with ACE inhibitors and beta-adrenoblokatorami, in view of the possible increased risk of developing side effects.

In patients with unilateral or bilateral renal artery stenosis requires regular monitoring of creatinine and urea nitrogen in serum.

Effects on ability to drive vehicles and management mechanisms

During treatment, it is necessary to be careful when driving vehicles and other potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: marked reduction in blood pressure, that can lead to loss of consciousness and collapse.

Treatment: gastric lavage, receiving a sufficient number of activated carbon, in / introduction 0.9% sodium chloride solution. Valsartan is not displayed when active dialysis is associated with blood plasma proteins.

Drug Interactions

When treating hypertension valsartanom did not have clinically significant interactions with other drugs used at the same time (eg, cimetidine, warfarin, Digoxin, atenolol, amlodipine, glibenclamide, furosemid, Indomethacin, gidroxlorotiazid).

Potassium-sparing diuretics, potassium supplements, salt, containing potassium, preparations, increase the level of potassium in the blood plasma (such as heparin) increase the risk of hyperkalemia.

Other hypotensives and diuretics increase antigipertenzivny effect of valsartan.

Antihypertensive effect of the drug may be weakened when coupled with the use of NSAIDS, incl. with the selective inhibitors of Cox-2 and acetylsalicylic acid in a dose of 3 g / day.

When coupled with the use of ACE inhibitors reported reversible lithium concentration in the blood plasma and the development of toxic effects.

Very limited experience in the use of valsartan and preparations, containing lithium. In the case of the use of drugs, containing lithium, patients, receiving Valz, It is recommended to control the concentration of lithium in the plasma.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 30 ° C. Shelf life – 3 year.