Description
Release form
Film-coated tablets
Pharmacological action
Combined antihypertensive drug containing active substances with a complementing mechanism of blood pressure control. Amlodipine dihydropyridine derivative, belongs to the class of slow calcium channel blockers (BMCC), valsartan – to the class of angiotensin II receptor antagonists. The combination of these components has a mutually complementary antihypertensive effect, which leads to a more pronounced decrease in blood pressure than when used separately.
Indications
– Arterial hypertension in patients who are shown combination therapy.
Contraindications
– skin tuberculosis
– viral infections of the skin
– vaccination
– perioral dermatitis
– rosacea (rosacea)
– hypersensitivity to any component of the drug. hypertrophic obstructive cardiomyopathy (GOKMP) and severe aortic stenosis)
– hemodynamically unstable heart failure after acute myocardial infarction
– simultaneous use with aliskiren in patients with diabetes mellitus or impaired renal function (CK less than 60 ml / min) srdlrdp – pregnancy
– period of lactation (breastfeeding)
– hypersensitivity to amlodipine, other derivatives of the dihydropyridine series, valsartan or to other components tomers drug.
The safety of the drug Vamloset in patients after kidney transplantation, as well as children and adolescents under the age of 18, has not been established.
With caution, the drug should be prescribed for impaired liver function of mild (5-6 points on the Child-Pugh scale) and moderate (7-9 points on the Child-Pugh scale) severity of obstructive diseases of the biliary tract impaired renal function of mild to moderate severity ( KK 30-50 ml / min) unilateral or bilateral renal artery stenosis or artery stenosis of a single kidney of chronic heart failure III-IV functional class according to NYHA classification of hyperkalemia hyponatremia following a diet with a limited intake I have reduced sodium bcc (including diarrhea, vomiting) in patients with hereditary angioneurotic edema, or edema with previous therapy with angiotensin II receptor antagonists in patients with mild and moderate mitral and aortic stenosis.
Use during pregnancy and lactation
Use of the drug Vamloset is contraindicated in pregnancy. Given the mechanism of action of angiotensin II receptor antagonists, the risk to the fetus when using the drug in the first trimester of pregnancy cannot be ruled out. Like any other drug that directly affects the renin-angiotensin-aldosterone system (RAAS), Vamloset should not be used during pregnancy, as well as for women planning a pregnancy. When using drugs that affect RAAS. it is necessary to inform women of childbearing age about the potential risk of negative 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, transfer to alternative antihypertensive therapy.
Special instructions
Patients with hyponatremia and / or a decrease in bcc
In patients with uncomplicated arterial hypertension receiving amlodipine / valsartan combination therapy, severe arterial hypotension was observed in 0.4% of cases.
In patients with activated RAAS (for example, patients with dehydration and / or hyponatremia who are taking diuretics in high doses), when taking angiotensin II receptor antagonists, symptomatic arterial hypotension may develop. Before starting treatment, you should restore the sodium content and / or replenish the BCC, in particular, by reducing the doses of diuretics or start therapy under close medical supervision.
With the development of a marked decrease in blood pressure, the patient should be moved to a horizontal position with a low headboard and, if necessary, intravenously infuse 0.9% sodium chloride solution. The therapy with Vamloset can be continued after the stabilization of hemodynamic parameters.
Hyperkalemia
Use caution when using potassium-sparing diuretics, potassium preparations, dietary supplements containing potassium or other drugs that can increase potassium in the blood plasma (for example, heparin). It is necessary to regularly monitor the potassium content in blood plasma.
Renal artery stenosis
Vamloset should be used with caution in patients with arterial hypertension on the background of unilateral or bilateral renal artery stenosis or artery stenosis of a single kidney, given the possibility of increasing serum concentrations of urea and creatinine.
Status after kidney transplantation
The safety of the amlodipine / valsartan combination in patients who have recently undergone kidney transplantation has not been established.
Impaired liver function
Valsartan is excreted predominantly unchanged with bile. In patients with impaired liver function, T1 / 2 lengthens, and AUC increases. Caution should be exercised when using the drug Vamloset in patients with impaired liver function of mild (5-6 points on the Child-Pugh scale) or moderate (7-8 points on the Child-Pugh scale) or obstructive biliary tract diseases.
Impaired renal function
Dose adjustment of the drug Vamlocet in patients with impaired renal function of mild or moderate severity is not required. In patients with moderate impaired renal function, it is recommended to control the potassium content and plasma creatinine concentration. The simultaneous use of angiotensin II receptor antagonists, including valsartan, or ACE inhibitors with aliskiren is contraindicated in patients with impaired renal function (CC less than 60 ml / min).
Primary hyperaldosteronism
Given the defeat of RAAS in primary hyperaldosteronism, patients in this group should not be prescribed angiotensin II receptor antagonists, incl. valsartan.
Angioedema edema
Among patients with angioedema (including laryngeal and vocal cord edema causing obstruction of the airways and / or swelling of the face, lips, pharynx and / or tongue), a history of development was noted during therapy with Vamlocet angioneurotic edema, including on ACE inhibitors. With the development of angioedema, the drug should be immediately discontinued and the possibility of repeated use excluded.
Heart failure / myocardial infarction
In patients whose kidney function may depend on RAAS activity (for example, with severe chronic heart failure), treatment with ACE inhibitors and angiotensin II receptor antagonists is accompanied by oliguria and / or an increase in azotemia, and in rare cases – acute renal failure and / or death. Similar outcomes have been described with valsartan. In patients with chronic heart failure or myocardial infarction, renal function should always be evaluated.
In patients with chronic heart failure of a non-ischemic etiology of functional class III-IV according to 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 frequency of worsening of chronic heart failure between the two groups. Slow calcium channel blockers, including amlodipine should be used with caution in patients with chronic heart failure, because there may be an increased risk of developing cardiovascular complications and death.
Mild to moderate stenosis of the aortic valve and mitral valve
As with any vasodilator, caution should be exercised in patients with mild to moderate mitral stenosis and aortic stenosis.
The combination of amlodipine / valsartan was studied only in patients with arterial hypertension.
Influence on the ability to drive vehicles and control mechanisms
When using the drug Vamloset it is necessary to be careful when driving vehicles and other technical devices that require an increased concentration of attention and speed of psychomotor reactions, because dizziness, fatigue and nausea are possible.
Composition
1 tab.
amlodipine besilate 13.88 mg,
which corresponds to the content of amlodipine 10 mg
valsartan A granule substance 251.35 mg,
which corresponds to the content of valsartan 160 mg
Excipients of the granule substance: microcrystalline cellulose – 75 mg, 82 mg, 82 mg, 3 mg, sodium lauryl sulfate – 1.6 mg.
Excipients: mannitol – 43.77 mg, magnesium stearate – 9 mg, colloidal silicon dioxide – 2 mg.
Composition of the film coat: Opadry II white – 7.8 mg (polyvinyl alcohol – 40%, titanium dioxide (E171) – 25%, macrogol – 20.2%, talc – 14.8%), yellow iron oxide dye (E172) – 0.2 mg.
Dosage and administration
The drug should be taken orally, 1 time / day, regardless of food intake, washed down with a small amount of water.
Recommended daily dose – 1 tab. Vamloset drug containing a combination of amlodipine / valsartan in a dose of 5 mg / 80 mg, 5 mg / 160 mg, 10 mg / 160 mg, 5 mg / 320 mg or 10 mg / 320 mg.
The initial dose of the drug Vamloset – 5 mg / 80 mg 1 time / day. You can increase the dose 1-2 weeks after the start of therapy.
The maximum daily dose is 5 mg / 320 mg (in terms of valsartan) or 10 mg / 160 mg (in terms of amlodipine) or 10 mg / 320 mg.
Amlodipine
Dose adjustment is not required in patients with impaired renal function.
Patients with impaired liver function should use the drug with caution.
Elderly patients do not need a dose adjustment or dosing regimen.
Valsartan
In patients with impaired renal function (CC> 30 ml / min), an initial dose adjustment is not required.
Valsartan is contraindicated in patients with severe hepatic failure, biliary cirrhosis, and cholestasis. The maximum daily dose of valsartan for liver failure of mild to moderate severity is 80 mg. The drug Vamloset in a dose of 5 mg / 160 mg, 5 mg / 320 mg, 10 mg / 160 and 10 mg / 320 mg is contraindicated.
In elderly patients, dose adjustment is not required.
Side effects
Classification of the incidence of side effects. WHO: very often (? 1/10), often (? 1/100 to <1/10), infrequently (? 1/1000 to <1/100), rarely (from? 1/10 000 to <1/1000), very rarely (from <1/10 000), the frequency is unknown (cannot be estimated based on available data). Drug Vamloset Infectious and parasitic diseases: often – flu. From the side of metabolism: often – hypokalemia infrequently – hypercalcemia, hyperlipidemia, hyperuricemia, hyponatremia. From the nervous system: often – headache infrequently – impaired coordination, dizziness, postural dizziness, paresthesia, drowsiness rarely – anxiety. From the side of the organ of vision: infrequently – visual impairment rarely – visual impairment. On the part of the organ of hearing and labyrinth disorders: infrequently – vertigo rarely – tinnitus. From the cardiovascular system: infrequently – palpitations, tachycardia, orthostatic hypotension is rare – a marked decrease in blood pressure, fainting. From the respiratory system: often – nasopharyngitis infrequently – cough, pain in the throat and larynx. From the digestive system: infrequently – diarrhea, nausea, discomfort in the abdomen, pain in the upper abdomen, constipation, dry mouth. From the skin and subcutaneous tissues: infrequently – erythema, skin rash rarely – exanthema, hyperhidrosis, skin itching. From the musculoskeletal system: infrequently – arthralgia, back pain, swelling of the joints rarely – muscle cramps, a feeling of heaviness throughout the body. From the urinary system: rarely – pollakiuria, polyuria. From the genitals and mammary gland: rarely – erectile dysfunction. Allergic reactions: rarely – hypersensitivity. General disorders and disorders at the injection site: often – asthenia, increased fatigue, swelling of the face, sensation of a rush of blood to the skin of the face, edema, peripheral edema, pasty infrequently – anorexia. In patients treated with amlodipine / valsartan, peripheral edema was less common (5.8%) than in patients treated with amlodipine alone (9%). Amlodipine From the hemopoietic system: very rarely – leukopenia, thrombocytopenia, sometimes with purpura. From the side of metabolism: very rarely – hyperglycemia. Mental disorders: infrequently – depression, insomnia / sleep disturbances, mood lability rarely – confusion. From the nervous system: often – dizziness, headache, drowsiness infrequently – taste disturbance, paresthesia, fainting, tremor, hypesthesia is very rare – muscle hypertonicity, peripheral neuropathy frequency is unknown – extrapyramidal disorders. From the side of the organ of vision: infrequently – visual impairment, visual impairment. On the part of the organ of hearing and labyrinth disorders: infrequently – tinnitus. From the cardiovascular system: often – a feeling of palpitations, a sensation of a rush of blood to the skin of the face, a marked decrease in blood pressure is very rare – arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, vasculitis. From the respiratory system: infrequently – shortness of breath, rhinitis is very rare – cough. From the digestive system: often – nausea, abdominal discomfort, pain in the upper abdomen infrequently – stool changes, diarrhea, dry oral mucosa, dyspepsia, vomiting rarely – gastritis, gingival hyperplasia, pancreatitis. From the side of the liver and biliary tract: very rarely – increased activity of liver enzymes (most often with cholestasis), increased plasma bilirubin concentration, hepatitis, intrahepatic cholestasis, jaundice. From the side of the skin and subcutaneous tissues: infrequently – alopecia, exanthema, erythema, photosensitivity reactions, itching, hyperhidrosis, purpura, skin rash, skin discoloration very rarely – erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome. From the musculoskeletal system: often – ankle swelling infrequently – arthralgia, back pain, muscle cramps, myalgia. From the urinary system: infrequently – violation of urination, nocturia, pollakiuria. From the genitals and mammary gland: infrequently – erectile dysfunction, gynecomastia. General disorders and disorders at the injection site: often – fatigue, peripheral edema infrequently – asthenia, discomfort, malaise, non-cardiogenic heart pain, pain. Laboratory and instrumental data: infrequently – decrease / increase in body weight. Allergic reactions: very rarely – hypersensitivity reactions, urticaria, angioedema. Valsartan From the hematopoietic system: frequency is unknown – decreased hemoglobin and hematocrit, leukopenia, neutropenia, thrombocytopenia sometimes with purpura. On the part of the organ of hearing and labyrinth disorders: infrequently – vertigo. From the cardiovascular system: frequency unknown – vasculitis. From the respiratory system: infrequently – cough. From the digestive system: infrequently – a feeling of discomfort in the abdomen, pain in the upper abdomen. From the side of the liver and biliary tract: frequency is unknown – increased activity of liver enzymes, increased concentration of bilirubin in blood plasma. On the part of the skin and subcutaneous tissues: frequency is unknown – itchy skin, skin rash. From the musculoskeletal system: frequency unknown – myalgia. From the urinary system: frequency is unknown – increased plasma creatinine concentration, impaired renal function, including acute renal failure. General disorders and disorders at the injection site: infrequently – increased fatigue. Laboratory and instrumental data: frequency unknown – increased serum potassium. Allergic reactions: very rarely – hypersensitivity reactions frequency unknown – angioedema. Adverse events that were previously reported with the use of each of the components may occur with the use of the drug Vamloset, even if they were not observed in clinical trials. Amlodipine Often: drowsiness, dizziness, palpitations, abdominal pain, nausea, ankle swelling. Infrequently: insomnia, mood lability (including anxiety), depression, tremor, taste disturbance, fainting, hypesthesia, visual impairment (including diplopia), tinnitus, marked decrease in blood pressure, shortness of breath, rhinitis, vomiting, dyspepsia, alopecia, purpura, discoloration of the skin, hyperhidrosis, itching, exanthema, myalgia, muscle cramps, pain, impaired urination, increased urination, impotence, gynecomastia, chest pain, malaise, weight gain, weight loss. Rarely: confusion. Very rare: leukopenia, thrombocytopenia, allergic reactions, hyperglycemia, muscle hypertonicity, peripheral neuropathy, myocardial infarction, arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), vasculitis, pancreatitis, hepatitis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastritis, gastrititis enzymes (most often due to cholestasis), angioedema, erythema multiforme, urticaria, exfoliative dermatitis, Stevens-Johnson syndrome, photosensitivity. Separate cases of extrapyramidal syndrome are described. Valsartan Frequency unknown: decrease in hemoglobin and hematocrit, neutropenia, thrombocytopenia, increased serum potassium, increased activity of liver enzymes, increased plasma bilirubin concentration, increased plasma creatinine concentration, impaired renal function, including renal failure, angioedema, myalgia, vasculitis, hypersensitivity, including serum sickness. Drug Interactions Wamlocet (amlodipine / valsartan) Combinations requiring attention Other antihypertensive drugs (e.g. alpha-blockers, diuretics) and antihypertensive drugs (e.g. tricyclic antidepressants, alpha-blockers for the treatment of benign prostatic hyperplasia), can enhance the antihypertensive effect. Amlodipine Undesirable combinations of Concomitant use with grapefruit or grapefruit juice is not recommended, given the possibility of increased bioavailability in some patients and increased antihypertensive effect. Combinations requiring caution Concomitant use with strong or moderate inhibitors of the CYP3A4 isoenzyme (protease inhibitors, verapamil or diltiazem, antifungal drugs from the azole group, antibiotics from the macrolide group, such as erythromycin or clarithromycin amyloid can significantly increase). In elderly patients, these changes are of clinical importance, therefore, medical supervision and dose adjustment are necessary. When used simultaneously with inducers of the CYP3A4 isoenzyme (anticonvulsants (e.g. carbamazepine, phenobarbital, phenytoin, phosphenytoin, primidone), rifampicin, herbal preparations containing St. John’s wort perforated), be careful, because a decrease in the concentration of amlodipine in blood plasma is possible. The simultaneous repeated use of amlodipine at a dose of 10 mg and simvastatin at a dose of 80 mg increases the exposure to simvastatin by 77% compared to that with simvastatin monotherapy. Patients receiving amlodipine are recommended to use simvastatin in a dose of not more than 20 mg / day. In experimental studies in animals after ingestion of verapamil and iv administration of dantrolene, cases of fatal ventricular fibrillation and cardiovascular failure associated with hyperkalemia were observed. Given the risk of developing hyperkalemia, the simultaneous use of slow calcium channel blockers should be avoided, including amlodipine, in patients prone to developing malignant hyperthermia. Combinations requiring attention In clinical studies, no significant interaction was found with thiazide diuretics, alpha-blockers, beta-blockers, ACE inhibitors, long-acting nitrates, nitroglycerin for sublingual use, digoxin, warfarinomin, aluminator, magnesium-containing antacids, simethicone), cimetidine, NSAIDs, antibiotics and hypoglycemic drugs for oral administration. Valsartan Contraindicated combinations Concomitant use of angiontensin II receptor antagonists, including valsartan, or ACE inhibitors with aliskiren is contraindicated in patients with diabetes mellitus and impaired renal function (CC less than 60 ml / min). Undesirable combinations Concomitant use with lithium preparations is not recommended, because a reversible increase in the concentration of lithium in blood plasma and the development of intoxication is possible. If necessary, simultaneous use with lithium preparations should carefully monitor the concentration of lithium in blood plasma. If necessary, simultaneous use with drugs that affect the potassium content (potassium-sparing diuretics, potassium preparations, potassium-containing food additives and other drugs and substances that can increase serum potassium (for example, heparin)), it is recommended to control the potassium content in blood plasma. Combinations requiring caution When used concomitantly with NSAIDs, including selective COX-2 inhibitors, acetylsalicylic acid at a dose of more than 3 g / day and non-selective NSAIDs may weaken the antihypertensive effect, increase the risk of impaired renal function and increase potassium in the blood plasma. At the beginning of therapy, it is recommended to evaluate renal function, as well as to correct the disturbances in the water-electrolyte balance. According to an in vitro study, valsartan is a substrate for OATP1B1 and MRP2 transporter proteins. The concomitant use of valsartan with OATP1B1 transporter protein inhibitors (e.g. rifampicin, cyclosporin) and MRP2 transporter protein inhibitors (e.g. ritonavir) can increase the systemic exposure of valsartan (Cmax and AUC). This should be considered at the beginning and at the end of concurrent therapy. Monotherapy with valsartan did not reveal a clinically significant interaction with the following drugs: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine and glibenclamide. Storage conditions The drug should be stored out of the reach of children at a temperature not exceeding 30 ° C. Term hodnosty 3 years Active ingredient Amlodipine, Valsartan Terms pharmacy leave with prescription Form of Treatment tablets
