Vanatex 160 mg tablets №28

Author Ольга Кияница

2017-05-11

Amount in a package -
Product form Pills
Manufacturer Polpharma (Poland)
Registration certificate UA/12634/01/02
The main medicament Vanatex
morion code 230055

Vanatex instructions for use

Tradename

Vanatex

International Nonproprietary Name

Valsartan

Dosage form

Tablets coated with 80 mg, 160 mg

Composition

One tablet contains

active substance - valsartan 80 mg, 160 mg

auxiliary substances: lactose monohydrate, sodium croscarmellose, silicon dioxide colloidal anhydrous, magnesium stearate

composition of the coating Advantia Prime 171996BA01: hypromellose 6 cP, macrogol 400, titanium dioxide E 171, iron (III) oxide red E172 (for a dosage of 80 mg),

the composition of the coating Advantia Prime 145010BA01: hypromellose 6 cP, macrogol 400, titanium dioxide E 171, iron (III) oxide red E172, iron (III) oxide yellow E172, iron (III) oxide black E172 (for dosage 160 mg).

Description

Round tablets, with a flat surface, covered with a pink coating, with a separation risk (for a dosage of 80 mg).

Tablets of oblong form, with biconvex surface, covered with a coat of light brown color, with a separation risk (for a dosage of 160 mg).

Pharmacotherapeutic group

Drugs affecting the system of renin-angiotensin.

Angiotensin II antagonists.

ATS code C09CA03

Pharmacological properties

Pharmacokinetics

Suction

After oral administration, the maximum valsartan concentration in the plasma is detected after 2-4 hours. The average absolute bioavailability of the drug is 23%. In the case of valsartan with food, the area under the curve (AUC) for valsartan is reduced by approximately 40%, and the maximum plasma concentration (Cmax) is approximately 50%, while for 8 hours after application, the concentration of valsartan in the blood plasma is equivalent concentration of active substance in patients taking the drug on an empty stomach. However, along with a decrease in AUC, clinically significant weakening of the therapeutic effect does not occur, therefore, valsartan can be taken regardless of food intake.

Distribution

The volume of distribution during the equilibrium period is low (about 17 L), which indicates the absence of valsartan deposition in tissues. Valsartan binds to plasma proteins (94 - 97%), mainly with albumins.

Biotransformation

Valsartan is slightly biotransformed, only about 20% of the dose is found in the form of metabolites. Hydroxymetabolite was detected in plasma at low concentrations (less than 10% of the area under the curve (AUC) for valsartan). This metabolite is pharmacologically inactive.

Excretion

Valsartan exhibits a multidisciplinary kinetics of the elimination process (t ½ α <1 h and t ½ β approximately 9 h). First of all, valsartan is excreted with bile in the stool (about 83% of the dose) and kidneys with urine (about 13% of the dose), unchanged. The plasma clearance of valsartan is about 2 l / h, and the renal clearance is about 0, 62 l / h (approximately 30% of the total clearance). The half-life of valsartan is 6 hours.

In patients with heart failure

The mean time to reach the maximum concentration, as well as the half-life in the phase of valsartan removal in patients with heart failure and in healthy volunteers are similar. Values of AUC and Cmax of valsartan are practically proportional to the increased dose in the clinical aspect of dosing (40 mg to 160 mg of valsartan twice daily). The average cumulation coefficient is about 1.7. The clearance of valsartan after oral administration is about 4.5 l / h. Age does not affect the observed clearance in patients with heart failure.

Pharmacodynamics

Vanatex is a strong and specific antagonist of the angiotensin II receptor (AH II). Selectively acts on the subtype of the AT1 receptor, which is responsible for the studied effects of angiotensin II (vasoconstriction, aldosterone secretion, etc.).Valsartan does not even show partial antagonism to the AT1 receptor and has a large (approximately 20,000-fold) affinity for the AT1 receptor than for the AT2 receptor. It has not been established that valsartan binds or blocks other hormone receptors or ion channels that are significant for cardiovascular regulation.

Valsartan does not inhibit the activity of the angiotensin converting enzyme (ACE, kininase II), which converts AG I to AG II and causes the breakdown of bradykinin. Taking into account the absence of influence on ACE and the absence of a potentiated action of bradykinin or substance P, the probability of coughing with the use of angiotensin II receptor antagonists is small.

In patients with arterial hypertension and type 2 diabetes mellitus, as well as with microalbuminuria, it has been established that valsartan reduces the excretion of albumin in the urine.

It was found that a dose of 160-320 mg of valsartan caused a clinically significant decrease in UAE in patients with arterial hypertension and type 2 diabetes.

The use of the drug in patients with hypertension as a result leads to a decrease in blood pressure without affecting the pulse rate.

The sudden discontinuation of the drug is not accompanied by the development of the "withdrawal" syndrome. With the course of the drug in patients with arterial hypertension, the drug has no significant effect on the level of total cholesterol, uric acid, and also on fasting - on the concentration of triglycerides and glucose in the blood serum.

The use of the drug reduces the incidence of hospitalization due to heart failure, slowing the progression of heart failure, improving the functional class according to the NYHA classification (classification of the New York Association of Cardiology), increasing the ejection fraction.

The use of Vanatex, like captopril, helps to reduce the overall mortality after myocardial infarction and is effective in treating patients at high risk of cardiovascular complications after myocardial infarction.

Indications for use

- essential hypertension

- conditions after a recent myocardial infarction (from 12 hours to 10 days), treatment of patients in a clinically stable state with symptomatic heart failure or asymptomatic left ventricular dysfunction

- heart failure (treatment of symptomatic heart failure if ACE inhibitors can not be used, or as a combined treatment with ACE inhibitors, if drugs that block β-adrenergic receptors can not be used)

Dosing and Administration

Vanatex can be taken regardless of food intake, should be washed down with water.

Arterial hypertension

The recommended initial dose of valsartan is 80 mg once daily. The pronounced antihypertensive effect is observed for 2 weeks, and its maximum is reached within 4 weeks. In patients who can not achieve proper control of blood pressure, the dose can be increased to 160 mg, and to a maximum of 320 mg.

Valsartan can be used in combination with other antihypertensive drugs. The additional use of a diuretic, such as hydrochlorothiazide, causes a more pronounced decrease in blood pressure in these patients.

Conditions after a recent myocardial infarction

In patients in a clinically stable state, treatment can be started 12 hours after diagnosis of myocardial infarction. After an initial dose of 20 mg twice a day for the next few weeks, the dose of valsartan should be gradually increased to 40 mg, 80 mg and 160 mg applied twice daily. The initial dose is provided by a divided tablet of 40 mg.

The maximum dose is 160 mg, taken twice a day. Typically, patients are advised to take a dose of 80 mg twice a day at the beginning of treatment for 2 weeks, and a maximum target dose of 160 mg taken twice a day should be released within 3 months, depending on the patient's tolerance of the drug. If there is a development of symptomatic arterial hypotension or impaired renal function, an option should consider reducing the dose.

Valsartan can be used in patients in combination with other drugs used to treat myocardial infarction, such as thrombolytics, acetylsalicylic acid, β-adrenergic receptor blockers, statins and diuretics. It is not recommended simultaneous use with ACE inhibitors.

Evaluation of the patient's condition after a previous myocardial infarction should always include an assessment of kidney function.

Heart failure

The recommended initial dose of valsartan is 40 mg twice daily. The initial dose is provided by a divided tablet of 80 mg.

The next increase in the dose to 80 mg and 160 mg, applied twice a day, should be performed with at least two-week intervals, until the maximum dose tolerated by the patient is reached. In the case of simultaneous use of a diuretic, you should consider the option of reducing its dose. The maximum daily dose used in clinical trials was 320 mg of valsartan in divided doses.

Valsartan can be used in patients taking other medications used to treat heart failure. However, combination therapy with three drugs (valsartan with ATK inhibitors and β-adrenergic receptor blockers) is not recommended.

An assessment of the condition of patients with heart failure should always include an assessment of kidney function.

There is no need to change dosing in elderly people and in patients with creatinine clearance> 10 ml / min.

In patients with mild to moderate liver function disorders that occur without cholestasis, doses exceeding 80 mg of valsartan per day should not be administered.

Side effects

Frequently (≥ 1/100 to <1/10)

- dizziness, dizziness associated with the position of the body

- arterial hypotension, orthostatic hypotension

- Insufficiency and impaired renal function Not very often (≥ 1/1000 to <1/100)

- dizziness of vestibular origin

- cough

- abdominal pain, nausea, diarrhea

- a feeling of fatigue, weakness

- Hyperkalemia

- fainting, headache

- heart failure

- vasomotor edema

- acute renal failure, increased serum creatinine concentration

Frequency unknown

- decrease in hemoglobin concentration, decrease in hematocrit, neutropenia, thrombocytopenia

- Hypersensitivity, including serum sickness

- vasculitis

- increased activity of liver enzymes, increased concentration
bilirubin in serum

- angioedema, rash, itching

- myalgia, arthralgia

- increase in the concentration of urea nitrogen in the blood

Contraindications

- Hypersensitivity to the active substance or any of the components of the drug

- severe violations of the liver, biliary cirrhosis and cholestasis

- pregnancy and lactation period

- children and adolescents under the age of 18 due to lack of safety and efficacy data

Drug Interactions

Non-recommended drug combinations

Lithium

There have been reports of reversible increases in serum lithium concentrations and an increase in its toxicity in the combined use of ATA inhibitors. Due to lack of experience in the field of simultaneous use of valsartan and lithium, such combined treatment is not recommended. If such a combination treatment is necessary, careful monitoring of the concentration of lithium in the blood serum is recommended.

Potassium-sparing diuretics, substitution therapy with potassium, substitutes for potassium salt, and other substances that can increase the potassium concentration

If the need to use a drug that affects potassium concentration, in combination with valsartan, is confirmed, monitoring of potassium concentration in the plasma is recommended.

Care must be taken when applying simultaneously
Non-steroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of COX-2, acetylsalicylic acid at a dose> 3 g / day and nonselective NSAIDs

In the case of combined use of antagonists of angiotensin II receptors with NSAIDs, an attenuation of hypotensive effect may occur. In addition, simultaneous use of angiotensin II receptor antagonists and NSAIDs may lead to an increased risk of impaired renal function and an increase in serum potassium concentration. Given this, it is recommended to monitor the function of the kidneys at the beginning of treatment, and to ensure proper hydration of the patient.

Other

In the studies of drug interactions of valsartan, there were no clinically significant interactions between valsartan and any of the following substances: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine and glibenclamide.

special instructions

Patients with a deficiency in the body of sodium and / or volume of circulating blood (BCC). In patients with severe deficiency in the body of sodium and / or BCC, for example, receiving high doses of diuretics, in rare cases, symptomatic hypotension may occur at the beginning of Vanatex treatment. Before beginning treatment Vanatex should make a correction in the body sodium and / or volume of circulating blood, for example, by reducing the dose of the diuretic.

In the case of hypotension, the patient should be laid and, if necessary, an intravenous infusion of physiological saline.After the blood pressure stabilizes, the treatment of Vanathex can be continued.

Stenosis of the renal artery. Given that drugs that affect the renin-angiotensin-aldosterone system (RAAS) can cause an increase in serum urea and creatinine levels in patients with bilateral or unilateral stenosis of the renal artery, systematic monitoring of these indicators is recommended as a precautionary measure.

Stenosis of aortic and mitral valves, hypertrophic obstructive cardiomyopathy (GOK). As with all other vasodilators, special care must be taken in the application.

Impaired renal function. For severe disorders (creatinine clearance <10 ml / min), caution should be exercised.

Violation of the function of the liver. Valsartan is excreted mainly unchanged with bile, and in patients with obstructed bile ducts, the clearance of valsartan is reduced. When valsartan is prescribed, patients with bile duct obstruction should be especially careful.

Heart failure / Postmyocardial condition. In patients with heart failure or post-infarction, who take Vanatex in regular doses, there is a slight decrease in blood pressure, but as a rule, it is not necessary to stop therapy due to prolonged symptomatic therapy. Such patients should be careful. Due to inhibition of the renin-angiotensin-aldosterone system, sensitive patients may have renal function changes. In patients with severe heart failure, 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.An assessment of the condition of patients with heart failure or a post-infarction condition should always include an assessment of the state of the kidney function.

Caution is needed in patients with heart failure when using a triple combination of ACE inhibitors, beta-blockers and valsartan. Vanatex can be used in patients treated with other drugs used after myocardial infarction, for example, thrombolytics, acetylsalicylic acid, beta-blockers and statins.

Assessment of the condition of patients after myocardial infarction should always include an assessment of renal function.

Vanatex contains a lactose excipient monohydrate. Patients with rare hereditary pathologies, such as galactose intolerance, lactase deficiency such as Lappa, or glucose-galactose malabsorption syndrome, should not take this product.

Features of the impact on the ability to drive vehicles and potentially dangerous mechanisms

In the course of transport management or maintenance of moving mechanisms, one should take into account the possibility of developing side effects - dizziness and fatigue.

Overdose

Symptoms: severe arterial hypotension, which can lead to a decrease in the level of consciousness, collapse and (or) shock.

Treatment: symptomatic, in case of onset of arterial hypotension - to correct the volume of circulating blood. The removal of valsartan from circulating blood by hemodialysis is unlikely.

Form of production and packaging

For 14 tablets in a contour pack of cells from Al / PVC / PCTFE.

By 2 contour packs together with instructions for use in the state and Russian languages are put in a pack of cardboard.

Storage conditions

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life

4 years

Do not use the drug after the expiration date.


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