Vyloset - instructions for use, analogs, reviews and release forms (tablets 5 + 80 mg, 5 + 160 mg, 5 + 320 mg, 10 + 160 mg and 10 + 320 mg) of the drug for the treatment of hypertension and pressure reduction in adults, children and in pregnancy

In this article, you can read the instructions for using the drug Vamloset. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Vamloset in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Vuloset analogues in the presence of existing structural analogs. Use to treat hypertension and reduce pressure in adults, children, as well as during pregnancy and lactation.

Vamloset - A combined antihypertensive drug containing two active substances with a complementary mechanism for controlling blood pressure (BP). Amlodipine, a derivative of dihydropyridine, belongs to the class of blockers of "slow" calcium channels (BCCC), Valsartan - to the class of angiotensin receptor antagonists 2. The combination of these components has a mutually complementary antihypertensive effect, which leads to a more pronounced decrease in blood pressure in comparison with AD in their separate application.

Composition

Amlodipine (in the form of besylate) + Valsartan + auxiliary substances.

Pharmacokinetics

The pharmacokinetics of Amlodipine and valsartan is characterized by linearity.

Amlodipine / Valsartan

After ingestion of amlodipine / valsartan combination, the maximum concentrations of valsartan and amlodipine in the blood plasma (Cmax) are reached after 3 hours and 6-8 hours, respectively. The rate and degree of absorption are equivalent to the bioavailability of valsartan and amlodipine when taken separately.

Amlodipine

After ingestion, amlodipine is slowly absorbed from the digestive tract. Bioavailability does not depend on food intake.

Biotransformation: Amlodipine is intensively (about 90%) metabolized in the liver with the formation of inactive metabolites.

Excretion: Amlodipine is excreted from the blood plasma biphasic, with terminal half-life (T1 / 2) from 30 to 50 hours. Equilibrium concentrations in the blood plasma are achieved after prolonged oral administration for 7-8 days. 10% of unchanged amlodipine and 60% of amlodipine in the form of metabolites is excreted by the kidneys.

Valsartan

After taking valsartan inside Cmax is achieved in 2-3 hours.

Biotransformation: valsartan does not undergo a pronounced metabolism. Only about 20% of the dose is determined in the blood plasma in the form of metabolites.

Valsartan is excreted mainly unchanged with bile through the intestine (about 83%) and kidneys (about 13%).

Children (up to 18 years of age)

There is no pharmacokinetic data on the use of the drug in this group of patients.

Indications

• Arterial hypertension (patients who are shown combined therapy).

Forms of release

The coated tablets are 5 + 80 mg, 5 + 160 mg, 5 + 320 mg, 10 + 160 mg and 10 + 320 mg.

Instructions for use and dosage

Inside, squeezed a small amount of water, regardless of the time of food intake 1 time per day.

The recommended daily dose is 1 tablet of the drug Vamloset, containing a combination of amlodipine / valsartan in a dose of 5/80 mg, 5/160 mg, 10/160 mg, 5/320 mg or 10/320 mg. Begin taking the drug Vamloset recommended with a dose of 5/80 mg once a day. You can increase the dose 1-2 weeks after the start of therapy.

The maximum daily dose is 5/320 mg (in terms of valsartan) or 10/160 mg (in terms of amlodipine) or 10/320 mg.

Special patient groups

Amlodipine

Patients with impaired renal function: dose adjustment is not required.

Patients with impaired liver function: should be used with caution.

Elderly patients: dose adjustment and dosing regimen is not required.

Valsartan

Patients with renal dysfunction: in patients with impaired renal function (QC more than 30 ml / min), correction of the initial dose is not required.

Patients with impaired hepatic function: valsartan is contraindicated in patients with severe hepatic insufficiency, biliary cirrhosis and cholestasis. The maximum daily dose of valsartan for mild to moderate hepatic insufficiency is 80 mg. The drug Vamloset in a dose of 5/160 mg, 5/320 mg, 10/160 mg and 10/320 mg is contraindicated.

Elderly patients: dose adjustment is not required.

Side effect

• nasopharyngitis;
• flu;
• hypersensitivity;
• hypokalemia;
• anorexia;
• hypercalcemia;
• hyperlipidemia;
• anxiety;
• headache;
• lack of coordination;
• dizziness;
• postural dizziness;
• paresthesia;
• drowsiness;
• deterioration of vision;
• impaired vision;
• vertigo;
• noise in ears;
• a feeling of palpitations;
• tachycardia;
• fainting;
• orthostatic hypotension;
• marked decrease in blood pressure;
• cough;
• pain in the pharynx and larynx;
• diarrhea, constipation;
• nausea;
• feeling of discomfort in the abdomen;
• pain in the upper abdomen;
• dryness of the oral mucosa;
• erythema;
• skin rash;
• exanthema;
• hyperhidrosis;
• itching;
• arthralgia;
• backache;
• swelling of the joints;
• muscle spasms;
• a feeling of heaviness in the whole body;
• pollakiuria;
• polyuria;
• erectile disfunction;
• asthenia;
• increased fatigue;
• edema;
• pastosity.

Contraindications

• hypersensitivity to amlodipine, other dihydropyridine derivatives, valsartan, or other components of the drug;
• severe hepatic insufficiency (more than 9 points on the Child-Pugh scale), biliary cirrhosis and cholestasis;
• pregnancy and the period of breastfeeding;
• severe renal failure (QC less than 30 ml / min), use in patients on hemodialysis;
• severe arterial hypotension (systolic blood pressure less than 90 mm Hg), collapse, shock (including cardiogenic shock);
• obstruction of the outflow tract of the left ventricle (including hypertrophic obstructive cardiomyopathy (GOKMP) and severe aortic stenosis);
• hemodynamically unstable heart failure after acute myocardial infarction;
• primary hyperaldosteronism;
• simultaneous use with aliskiren in patients with diabetes mellitus or renal dysfunction (CC less than 60 ml / min).

The safety of using the drug Vamloset in patients after the kidney transplantation, as well as children and adolescents under 18 years old is not established.

Application in pregnancy and lactation

The use of the drug Vamloset is contraindicated in pregnancy. Given the mechanism of action of antagonists of angiotensin 2 receptors, one can not exclude the risk for the fetus when applying the drug in the first trimester of pregnancy. Like any other drug that directly affects the renin-angiotensin-aldosterone system (RAAS),The drug Vamloset should not be used during pregnancy, as well as women planning a pregnancy. When using funds that affect RAAS ,. it is necessary to inform women of childbearing age about the potential risk of adverse effects of these drugs on the fetus during pregnancy. When planning pregnancy, it is recommended that the patient be transferred to alternative antihypertensive therapy, taking into account the safety profile. In case of diagnosing pregnancy, you should stop taking the drug Vamloset and ,. if necessary, translate into alternative antihypertensive therapy.

The drug Vamloset, as well as other drugs having a direct effect on RAAS, is contraindicated in 2-3 trimesters of pregnancy, since it can cause fetotoxic effects (renal dysfunction, fetal bone fetal decay, oligohydramnios) and neonatal toxic effects (renal failure, arterial hypotension , hyperkalemia) and fetal death. If nevertheless used the drug in 2-3 trimesters of pregnancy, then it is necessary to perform ultrasound examination of the kidneys and bones of the fetal skull.Newborns, whose mothers took the drug VAMOLOSET during pregnancy, should be under observation, as. it is possible to develop an arterial hypotension in a newborn.

It is not recommended to use Vamloset during breastfeeding. If you need to use the drug VAMOLOSET during lactation, breastfeeding should be discontinued.

Use in children

Contraindicated in children and adolescents under the age of 18 years. the safety of the drug Vamloset in children and adolescents under 18 years is not established.

Application in elderly patients

Correction of dose and dosage regimen is not required.

special instructions

Patients with hyponatraemia and / or a decrease in BCC

In patients with uncomplicated arterial hypertension taking combination therapy with amlodipine / valsartan, severe arterial hypotension was observed in 0.4% of cases.

In patients with activated RAAS (eg, in patients with dehydration and / or hyponatremia, taking diuretics in high doses), when angiotensin 2 receptor antagonists are taken, symptomatic arterial hypotension may develop.Before the start of treatment, it is recommended to restore the sodium content and / or replenish the BCC, in particular, by reducing the dose of diuretics or starting therapy under close medical supervision.

With the development of a pronounced decrease in blood pressure: it is necessary to put the patient in a horizontal position with raised legs and. if necessary, intravenously infuse 0.9% solution of sodium chloride. Therapy with Vamloset can be continued after stabilization of hemodynamic parameters.

Hyperkalemia

With the simultaneous use of potassium-sparing diuretics, potassium preparations, dietary supplements containing potassium or other drugs that can increase the potassium content in the blood plasma (eg, heparin), care should be taken. It is necessary to regularly monitor the content of potassium ions in the blood plasma.

Stenosis of the renal artery

The drug Vamloset should be used with caution in patients with arterial hypertension on the background of unilateral or bilateral stenosis of the renal artery or stenosis of the artery of a single kidney, given the possibility of increasing serum concentrations of urea and creatinine.

Condition after kidney transplantation

The safety of the use of amlodipine / valsartan combination in patients who have recently undergone kidney transplantation has not been established.

Impaired liver function

Valsartan is mostly excreted unchanged with bile. In patients, T1 / 2 is prolonged, and AUC - is increased. Caution should be exercised when using the drug VAMOLOSET in patients with mild (5-6 points on the Child-Pugh scale) or moderate (7-8 on the Child-Pugh scale), a violation of liver function or obstructive diseases of the biliary tract.

Impaired renal function

Correction of the dose of the drug Vamloset in patients with mild and moderate renal dysfunction is not required. In patients with moderate renal impairment, control of potassium and creatinine concentrations in blood plasma is recommended. The simultaneous use of ARA 2, including valsartan, or ACE inhibitors with aliskiren is contraindicated in patients with impaired renal function (QC less than 60 ml / min).

Primary hyperaldosteronism

Given the defeat of RAAS in primary hyperaldosteronism, these patients should not be prescribed angiotensin 2 receptor antagonists, including valsartan.

Angioedema

Among patients with angioneurotic edema (including swelling of the larynx and vocal cords causing airway obstruction and / or swelling of the face, lips, pharynx and / or tongue) against the background of therapy with the Vamloset drug, there have been cases of angioedema development in the anamnesis, including and on ACE inhibitors. When developing angioedema, immediately discontinue the drug and exclude the possibility of repeated use.

Heart failure / previous myocardial infarction

In patients whose renal function may depend on the activity of RAAS (eg, in severe CHF), therapy with ACE inhibitors and angiotensin 2 receptor antagonists is accompanied by oliguria and / or increased azotemia, and in rare cases with acute renal failure and / or death. Similar outcomes were described with the use of valsartan. In patients with CHF or a history of myocardial infarction, renal function should always be evaluated.

In patients with CHF of non-ischemic etiology of the 3-4 functional class according to the NYHA classification, the use of amlodipine was accompanied by an increase in the incidence of pulmonary edema compared with placebo in the absence of a significant difference in the incidence of worsening CHF between the two groups.Blocks of "slow" calcium channels, incl. amlodipine, should be used with caution in patients with CHF, since an increased risk of developing cardiovascular complications and death is possible.

Stenosis of aortic valve of mild to moderate degree and mitral valve

As with any vasodilator, care should be taken in patients with mitral stenosis and aortic stenosis of mild to moderate severity.

The combination of amlodipine / valsartan was studied only in patients with arterial hypertension.

Influence on ability to drive vehicles and other mechanisms

When using the drug Vamloset, care must be taken when driving vehicles and other technical devices that require a high concentration of attention and speed of psychomotor reactions. possibly the appearance of dizziness, fatigue and nausea.

Drug Interactions

The drug Vamloset

General drug interactions for the drug VAMOLOSET (amlodipine / valsartan)

Simultaneous application requiring attention

Other antihypertensive drugs (eg, alpha-blockers, diuretics) and drugs that have hypotensive effects (eg, tricyclic antidepressants, alpha-adrenoblockers for the treatment of benign prostatic hyperplasia) can increase the hypotensive effect.

Drug Interactions for Amlodipine

Unwanted simultaneous application

Grapefruit or grapefruit juice: simultaneous use is not recommended, given the possibility of increasing bioavailability in some patients and enhancing the antihypertensive effect.

Concurrent use requiring caution

Inhibitors of the isoenzyme CYP3A4

Simultaneous use with strong or moderate inhibitors of the CYP3A4 isoenzyme (protease inhibitors, Verapamil or diltiazem, azole antifungal drugs, macrolides such as Erythromycin or clarithromycin) can significantly increase the systemic exposure of amlodipine. In elderly patients, these changes are of clinical importance, so medical supervision and dose adjustment are necessary.CYP3A4 isoenzyme inductors (anticonvulsant drugs (eg, carbamazepine, phenobarbital, phenytoin, phosphenytoin, primidone), rifampicin, herbal preparations containing St. John's Wort.) Should be used with caution. with simultaneous application possible decrease in the concentration of amlodipine in the blood plasma.

Simvastatin

Simultaneous re-use of amlodipine in a dose of 10 mg and Simvastatin at a dose of 80 mg increases the exposure of simvastatin by 77% compared with that of monotherapy with simvastatin. Patients receiving amlodipine. It is recommended to use simvastatin in a dose of no more than 20 mg per day.

Dantrolen (intravenous administration): in experiments with animals after oral administration of verapamil and intravenous dantrolene, cases of ventricular fibrillation with a lethal outcome and cardiovascular insufficiency associated with hyperkalemia were observed. Given the risk of hyperkalemia, simultaneous use of blockers of "slow" calcium channels should be avoided, including. amlodipine. in patients prone to the development of malignant hyperthermia.

Simultaneous application requiring attention

Other

In clinical studies of amlodipine, there is no significant interaction with thiazide diuretics, alpha-adrenoblockers, beta-blockers, ACE inhibitors, long-acting nitrates, Nitroglycerin for sublingual use, digoxin, warfarin, atorvastatin, sildenafil, Maalox (aluminum- or magnesium-containing antacids, simethicone) , cimetidine, NSAIDs, antibiotics and hypoglycemic agents for prima.

Drug Interactions for valsartan

Simultaneous use is contraindicated

The simultaneous use of ARA 2, including valsartan, or ACE inhibitors with aliskiren is contraindicated in patients with diabetes mellitus and renal dysfunction (CC less than 60 ml / min).

Unwanted simultaneous application

Lithium

Simultaneous use with lithium preparations is not recommended, because possibly a reversible increase in the concentration of lithium in blood plasma and the development of intoxication. If it is necessary to simultaneously apply with lithium preparations, the concentration of lithium in the blood plasma should be carefully monitored.

Potassium-sparing diuretics, potassium preparations, potassium-containing food additives and other medicines and substances that can increase serum potassium (for example, heparin)

If it is necessary to simultaneously apply with drugs that affect the potassium content, it is recommended to monitor the potassium content in the blood plasma.

Concurrent use requiring caution

Non-steroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of cyclooxygenase-2 (COX-2), Acetylsalicylic acid at a dose of more than 3 g per day and non-selective NSAIDs.

With simultaneous use, it is possible to reduce the hypotensive effect, increase the risk of kidney dysfunction and increase the potassium content in the blood plasma. At the beginning of therapy it is recommended to evaluate the function of the kidneys, and also to correct the disturbances of the water-electrolyte balance.

Protein Transfer Inhibitors

Based on the results of the study, valsartan is the substrate for the carrier proteins OATP1B1 and MRP2. The simultaneous use of valsartan with inhibitors of the carrier protein OATP1B1 (eg, rifampicin, cyclosporin) and an inhibitor of the MRP2 carrier protein (eg ritonavir) can increase the systemic exposure of valsartan (Cmax and AUC).This should be taken into account at the beginning and at the end of the simultaneous therapy.

Others: monotherapy with valsartan showed no clinically significant interactions with the following drugs: cimetidine, warfarin. furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine and glibenclamide.

Analogues of the drug Vamloset

Structural analogs for the active substance:

• Exforge.

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