Vamloset coated pills 10mg + 160mg N28
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Active ingredients
Amlodipine
Release form
Pills
Composition
1 tablet contains: Active ingredient: amlodipine besylate 13.88 mg, which corresponds to the content of amlodipine 10 mg; valsartan A substance granules 251.35 mg, which corresponds to the content of valsartan 160 mg. The adjuvants of the substance granules: microcrystalline cellulose 82 mg, croscarmellose sodium - 4.75 mg, povidone - 3 mg, sodium lauryl sulfate - 1.6 mg. mg, magnesium stearate - 9 mg, colloidal silicon dioxide - 2 mg. The composition of the film coating: opadry II white - 7.8 mg (polyvinyl alcohol - 40%, titanium dioxide (E171) - 25%, macrogol - 20.2%, talc - 14.8% ), iron dye yellow oxide (E172) - 0.2 mg.
Pharmacological effect
Hypotensive.
Pharmacokinetics
Linearity The pharmacokinetics of amlodipine and valsartan are characterized by linearity. Amlodipine / valsartan After ingestion of the amlodipine / valsartan combination, Cmax of valsartan and amlodipine in the blood plasma is reached in 3 and 6–8 h, respectively. The rate and extent of absorption are equivalent to the bioavailability of valsartan and amlodipine when taking each of them separately. Amlodipine Absorption. After oral administration, amlodipine is slowly absorbed from the gastrointestinal tract. Cmax is achieved in 6–12 hours. Absolute bioavailability is 64–80%. Bioavailability does not depend on food intake. Distribution. Vd is approximately 21 L / kg. According to in vitro data, the link to plasma proteins is 97.5%. Biotransformation. Amlodipine is intensively (about 90%) metabolized in the liver to form inactive metabolites. Excretion. Amlodipine is derived from blood plasma in two phases, with terminal T1 / 2 from 30 to 50 hours. Css in blood plasma is reached after prolonged oral administration for 7–8 days. 10% unchanged amlodipine and 60% amlodipine in the form of metabolites excreted by the kidneys. Valsartan Absorption. After taking valsartan inside Cmax is achieved in 2–3 hours. The average absolute bioavailability is 23%. When taking valsartan with food, there is a decrease in bioavailability (by value of AUC) by about 40%, and Cmax - by about 50%. Approximately 8 hours after ingestion, plasma concentrations of valsartan in the group of patients taking it with food and in the group taking it on an empty stomach are equalized. Reducing AUC is not clinically significant, so valsartan can be taken regardless of food intake. Distribution.Vss of valsartan after the on / in the introduction is about 17 liters, which indicates the absence of an extensive distribution of valsartan in the tissues. Valsartan is largely associated with serum proteins (94–97%), mainly with serum albumin. Biotransformation. Valsartan is not subject to pronounced metabolism. Only about 20% of the dose taken is determined in plasma in the form of metabolites. Hydroxyl metabolite is determined in plasma in low concentrations (less than 10% of the AUC of valsartan). This metabolite is pharmacologically inactive. Excretion. Valsartan is biphasic: the α phase with T1 / 2α is less than 1 hour and the β phase with T1 / 2β is about 9 hours. Valsartan is mainly excreted unchanged with bile through the intestines (about 83%) and the kidneys (about 13%). After intravenous injection, plasma clearance of valsartan is about 2 l / h and its renal clearance is 0.62 l / h (about 30% of the total clearance). T1 / 2 of valsartan is 6 hours. Special groups of patients are Children (age up to 18 years). There is no pharmacokinetic data on the use of the drug in this group of patients. Patients of advanced age (over 65 years). Tmax of amlodipine in the blood plasma of young patients and elderly patients alike. In elderly patients, the clearance of amlodipine tends to decrease, which leads to an increase in AUC and T1 / 2. In elderly patients, the mean values of systemic exposure (AUC) to valsartan are slightly more pronounced than in younger patients. However, this was not clinically significant. Considering the good tolerability of amlodipine and valsartan in patients of elderly and younger age, it is recommended to use the usual dosing regimens. Violation of the kidney function. In patients with renal failure, the pharmacokinetic parameters do not change. The renal clearance of valsartan is only about 30% of the total plasma clearance, therefore, no correlation has been found between kidney function and systemic exposure (AUC value) to valsartan. Changes in the initial dose are not required in patients with mild to moderate renal dysfunction (Cl creatinine 30–50 ml / min). Violation of the liver. Experience with the use of the drug in patients with impaired liver function is limited. Patients with impaired liver function have reduced clearance of amlodipine, which leads to an increase in AUC of about 40-60%.On average, in patients with impaired mild liver function (5-6 points on the Child-Pugh scale) and moderate (7-9 points on the Child-Pugh scale) degree, the bioavailability (in terms of AUC) of valsartan is doubled compared with healthy volunteers of the corresponding age , sex and body weight.
Indications
Used in the treatment of anal fissures and hemorrhoids.
Contraindications
- severe liver failure (more than 9 points on the Child-Pugh scale); - biliary cirrhosis and cholestasis; - severe renal failure (CC 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 infarction that myocardium; - simultaneous use with aliskiren in patients with diabetes mellitus or renal dysfunction (CC less than 60 ml / min); - primary hyperaldosteronism; - pregnancy; - lactation (breastfeeding); - hypersensitivity to amlodipine, other dihydropyridine derivatives row, valsartan or other components of the drug. The safety of using Vamloset drug in patients after kidney transplantation, as well as children and adolescents under the age of 18 years has not been established.
Use during pregnancy and lactation
The drug Vamloset is contraindicated during pregnancy. Considering the mechanism of action of APA II, the risk to the fetus cannot be ruled out when using the drug in the first trimester of pregnancy. Like any other drug that has a direct effect on the RAAS, you should not use the drug Vamloset during pregnancy, and also women planning a pregnancy. When prescribing agents that affect the 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 a pregnancy, it is recommended to transfer the patient to alternative antihypertensive therapy taking into account the safety profile. If pregnancy is diagnosed, you should stop taking Wamloset and, if necessary,Vamloset, like other drugs that have a direct effect on the RAAS, is contraindicated in the II – III trimesters of pregnancy, as it can cause fetotoxic effects (impaired renal function, delayed ossification of the bones of the cranium of the fetus, oligohydramnios) and neonatal toxic effects (renal failure, arterial hypotension, hyperkalemia) and fetal death. If, nevertheless, the drug was used in the II – III trimesters of pregnancy, then an ultrasound of the kidneys and bones of the fetal skull must be performed. Newborns whose mothers were taking the drug Vamloset during pregnancy should be monitored because possible development of arterial hypotension in the newborn. It is not recommended to use the drug Vamloset during breastfeeding. If necessary, drug therapy Vamloset during lactation, breastfeeding should be stopped.
Dosage and administration
The drug should be taken orally, 1 time / day, regardless of the meal, with a small amount of water. The recommended daily dose is 1 tab. Vamloset, containing amlodipine / valsartan combination 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. Initial dose of the drug Vamloset - 5 mg / 80 mg 1 time / day You can increase the dose in 1-2 weeks after starting 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 Patients with impaired function renal dose adjustment is not required. Patients with impaired liver function should use the drug with caution. Elderly patients do not need dose adjustment or dosing regimen. Valsartan patients with impaired renal function (CK> 30 ml / min) do not need to adjust the initial dose. Valsartan azan in patients with severe liver failure, biliary cirrhosis and cholestasis. The maximum daily dose of valsartan for mild to moderate hepatic insufficiency is 80 mg. The drug Vamloset at 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
Infectious and parasitic diseases: often - influenza. For the metabolism: often - hypokalemia; infrequently - hypercalcemia, hyperlipidemia, hyperuricemia, hyponatremia. For the nervous system: often - headache; infrequently - lack of coordination, dizziness, postural dizziness,paresthesia, drowsiness; rarely, anxiety. For the organ of vision: infrequently, visual impairment; rarely - visual impairment. On the part of the organ of hearing and labyrinth disturbances: infrequently - vertigo; rarely - tinnitus. From the cardiovascular system: infrequently - a feeling of heartbeat, tachycardia, orthostatic hypotension; seldom - pronounced decrease in blood pressure, fainting. On the part of the respiratory system: often - nasopharyngitis; infrequently - cough, sore throat and larynx. From the digestive system: rarely - diarrhea, nausea, abdominal discomfort, pain in the upper abdomen, constipation, dry mouth. From the skin and subcutaneous tissues: rarely - erythema, skin rash; rarely - exanthema, hyperhidrosis, pruritus. From the musculoskeletal system: rarely - arthralgia, back pain, swelling of the joints; rarely, muscle spasms, a feeling of heaviness throughout the body. From the urinary system: rarely pollakiuria, polyuria. From the genital organs and the breast: rarely erectile dysfunction. Allergic reactions: rarely hypersensitivity. General disorders and disorders at the injection site: often - asthenia, fatigue, swelling of the face, feeling a rush of blood to the skin of the face, edema, peripheral edema, pastoznost; infrequently, anorexia. In patients receiving the amlodipine / valsartan combination, peripheral edema was less common (5.8%) than in patients receiving only amlodipine (9%). Amlodipine From the hematopoietic system: very rarely - leukopenia, thrombocytopenia sometimes with purpura. From the side of metabolism: very rarely - hyperglycemia. Mental disorders: infrequently - depression, insomnia / sleep disorders, mood lability; rarely - confusion of consciousness. For the nervous system: often - dizziness, headache, drowsiness; infrequently - a violation of taste, paresthesia, syncope, tremor, hypesthesia; very rarely - muscle hypertonus, peripheral neuropathy; frequency unknown - extrapyramidal disorders. From the organ of vision: infrequently - visual impairment, visual disturbance. From the organ of hearing and labyrinth disorders: rarely - tinnitus. From the cardiovascular system: often - a feeling of palpitations, a feeling of blood rush to the skin individuals, marked reduction in blood pressure; very rarely - arrhythmias (including bradycardia,ventricular tachycardia and atrial fibrillation), myocardial infarction, vasculitis. On the respiratory system: infrequently - shortness of breath, rhinitis; very rarely - cough. From the digestive system: often - nausea, abdominal discomfort, pain in the upper abdomen; infrequently - change of stool, diarrhea, dryness of the oral mucosa, dyspepsia, vomiting; rarely - gastritis, gingival hyperplasia, pancreatitis. From the liver and biliary tract: very rarely - increased activity of liver enzymes (more often with cholestasis), increased plasma bilirubin concentration, hepatitis, intrahepatic cholestasis, jaundice. On the side of the skin and subcutaneous tissues : infrequently - alopecia, rash, erythema, photosensitivity reactions, pruritus, hyperhidrosis, purpura, skin rash, change in skin color; very rarely - erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome. For the musculoskeletal system: often - ankle swelling; infrequently - arthralgia, back pain, muscle spasms, myalgia. From the urinary system: infrequently - urination disorder, nocturia, pollakiuria. From the genital organs and breast: rarely - erectile dysfunction, gynecomastia. General disorders and disorders at the injection site: often - increased fatigue, peripheral edema; infrequently - asthenia, discomfort, malaise, non-cardiogenic pain in the heart, pain. Laboratory and instrumental data: infrequently - increase / increase in body weight. Allergic reactions: very rarely - hypersensitivity reactions, urticaria, angioedema. decrease in hemoglobin and hematocrit, leukopenia, neutropenia, thrombocytopenia, sometimes with purpura. On the part of the organ of hearing and labyrinth disorders: not often - vertigo. On the side of the cardiovascular system: frequency known - vasculitis. From the respiratory system: infrequently - cough. From the digestive system: rarely - 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, increasing bilirubin concentration blood plasma. From the side of the skin and subcutaneous tissues: the frequency is unknown - itchy skin,skin rash. From the musculoskeletal system: the frequency is unknown - myalgia. From the urinary system: the frequency is unknown - increased creatinine concentration in the blood plasma, impaired kidney function, including acute renal failure. General disorders and disorders at the injection site: infrequently - increased fatigability. Laboratory and instrumental data: frequency unknown - increase in serum potassium. Allergic reactions: very rarely - hypersensitivity reactions; frequency is unknown - angioedema. Undesirable effects, which were previously reported with each of the components, may occur with the use of Vamloset, even if they were not observed in clinical studies. Amlodipine Frequently: drowsiness, dizziness, feeling of palpitations, abdominal pain, nausea , ankle swelling. Often: insomnia, mood lability (including anxiety), depression, tremor, taste disturbance, fainting, hypoesthesia, visual disturbances (including diplopia), tinnitus, marked decrease in blood pressure, odes ka, rhinitis, vomiting, dyspepsia, alopecia, purpura, discoloration of the skin, hyperhidrosis, pruritus, 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 hypertonus, peripheral neuropathy, myocardial infarction, arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), you smoker, pancreatitis, gastritis, gingival hyperplasia, hepatitis, jaundice, increased activity of liver enzymes (most often due to cholestasis), angioedema, erythema multiforme, urticaria, exfoliative dermatitis, Stevens-Johnson syndrome, photosensitivity. : decrease in hemoglobin and hematocrit, neutropenia, thrombocytopenia, an increase in the content of potassium in the blood serum, an increase in the activity of liver enzymes, an increase in the concentration of b lirubina in plasma creatinine concentration in blood plasma, renal function, including renal failure, angioedema, myalgia, vasculitis, hypersensitivity including serum sickness.
Overdose
Symptoms: data on cases of overdose are currently missing.With an overdose of valsartan, a pronounced decrease in blood pressure and dizziness can be expected. An overdose of amlodipine can lead to a pronounced decrease in blood pressure with possible development of reflex tachycardia and excessive peripheral vasodilation (the risk of severe and persistent arterial hypotension, including the development of shock and death). Treatment: symptomatic, the nature of which depends on the time past from the moment of taking the drug, and the severity of symptoms. In case of accidental overdose, it is necessary to induce vomiting (if the drug has been taken recently) or to perform a gastric lavage. The use of activated carbon in healthy volunteers immediately or within 2 hours after taking amlodipine resulted in a significant decrease in its absorption. With a pronounced decrease in blood pressure on the background of Vamloset taking the drug, it is necessary to transfer the patient to a supine position with raised legs, to take active measures to support the activity of the cardiovascular system, including regular monitoring of the function of the heart and respiratory system, BCC and urine volume. In the absence of contraindications to restore vascular tone and blood pressure, it is possible to use (with caution) vasoconstrictor agents. To eliminate the blockade of calcium channels, it is possible to / in the administration of calcium gluconate solution. Removal of valsartan and amlodipine during hemodialysis is unlikely.
Interaction with other drugs
Vamloset (amlodipine / valsartan) Simultaneous use requiring attention Other antihypertensive drugs (for example, alpha-blockers, diuretics) and drugs that have hypotensive effects (for example, tricyclic antidepressants, alpha-blockers for the treatment of benign prostatic hyperplasia) can be applied, can be treated by a combination of anti-depressants, alpha-blockers for treatment of benign prostatic hyperplasia). Amlodipine Unwanted simultaneous use of Grapefruit or grapefruit juice: the simultaneous use is not recommended, given the possibility of increasing bioavailability in non which patients and enhance the hypotensive deystviya.Odnovremennoe application requiring ostorozhnostiIngibitory isoenzyme CYP3A4: simultaneous application of strong or moderate inhibitors isoenzyme CYP3A4 (protease inhibitors, verapamil or diltiazem, azole antifungal drug, macrolides such as erythromycin, or clarithromycin) may lead to a significant increase in system amlodipine exposure.In elderly patients, these changes are of clinical importance, therefore, medical supervision and dose adjustment are necessary. CYP3A4 isoenzyme inducers (anticonvulsant drugs (for example, carbamazepine, phenobarbital, phenytoin, phosphenytoin, primidon), rifamycin, herbal preparations containing St. John's wort) should be used with care because with simultaneous use may reduce the concentration of amlodipine in the blood plasma. Simvastatin: simultaneous repeated use of amlodipine at a dose of 10 mg and simvastatin at a dose of 80 mg increases the exposure of simvastatin by 77% compared with that with simvastatin monotherapy. Patients receiving amlodipine are recommended to use simvastatin in a dose of not more than 20 mg / day. Dantrolene (w / w): in experiments on animals after ingestion of verapamil and d / dantrolen, there have been cases of ventricular fibrillation and cardiovascular deficiency associated with hyperkalemia. Given the risk of developing hyperkalemia, the simultaneous use of CCL should be avoided, including amlodipine in patients prone to the development of malignant hyperthermia. Simultaneous use requiring attention Others: in clinical studies of amlodipine, there is no significant interaction with thiazide diuretics, alpha-adrenergic blockers, beta-adrenergic blockers, ACE inhibitors, long-acting nitrates, alpha-adrenergic blockers, beta-adrenoblokatorami, ACF inhibitors, long-acting nitrate, alpha-adrenergic blockers, beta-adrenoblokatorami warfarin, atorvastatin, sildenafil, aluminum and / or magnesium-containing antacid preparations, including maalox, simethicone, cimetidine, NSAIDs, antibiotics and hypoglycemic agents for oral administration. Valsartan. Simultaneous use is contraindicated. Simultaneous use of ARA II, including valsartan, or ACE inhibitors with aliskiren is contraindicated in patients with diabetes and impaired kidney function (for example); . Undesirable simultaneous use of Lithium: simultaneous use with lithium preparations is not recommended, since perhaps a reversible increase in the concentration of lithium in the blood plasma and the development of intoxication. If necessary, the simultaneous use of drugs with lithium should be carefully monitored for the concentration of lithium in the blood plasma. CaliSavingdiuretics, potassium preparations, potassium-containing dietary supplements and other drugs and substances that can increase the content of potassium in the blood serum (eg, heparin): if necessary, simultaneous use with drugs that affect the content of potassium, it is recommended to control the content of potassium in the blood plasma. Simultaneous use requiring cautionNPVS, including selective inhibitors of COX-2, acetylsalicylic acid in a dose of more than 3 g / day and other non-selective NSAIDs: with simultaneous use, a decrease in the hypotensive effect, an increase in the risk of developing renal dysfunction and an increase in plasma potassium are possible. At the beginning of therapy, it is recommended to evaluate kidney function, as well as correct the impaired water-electrolyte balance. Inhibitors of carrier proteins: according to the results of an in vitro study, valsartan is a substrate for the carrier proteins OATP1B1 and MRP2. The simultaneous use of valsartan with inhibitors of the OATP1B1 carrier protein (for example, rifampicin, cyclosporine) and an inhibitor of the carrier protein MRP2 (for example, 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 simultaneous therapy. Others: valsartan monotherapy did not reveal clinically significant interactions with the following drugs: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine and glibenclamide.
special instructions
Patients with hyponatremia and / or a decrease in CVD of patients with uncomplicated arterial hypertension taking the amlodipine / valsartan combination, in 0.4% of cases severe arterial hypotension was observed. In patients with activated RAAS (for example, patients with dehydration and / or hyponatremia treated with diuretics in high doses), while taking ARA II, the development of symptomatic arterial hypotension is possible. Before starting treatment, it is recommended to restore the sodium content and / or replenish the BCC, in particular by reducing the dose of diuretics or initiate therapy under close medical supervision. When a pronounced decrease in blood pressure develops, the patient should be placed in a horizontal position with raised legs and, if necessary, infusion of 0.9% sodium chloride solution.Therapy with Vamloset can be continued after stabilization of hemodynamic parameters. Hyperkalemia When using potassium-saving diuretics, potassium supplements, dietary supplements containing potassium or other drugs that can increase the content of potassium in the blood plasma (eg, heparin), care should be taken. The content of potassium ions in the blood plasma should be regularly monitored. Renal artery stenosisVamloset's drug should be used with caution in patients with arterial hypertension against a background of unilateral or bilateral renal artery stenosis or arterial stenosis of the only kidney, taking into account the possibility of increasing serum concentrations of urea and creatinine. Condition after kidney transplantation use of the combination amlodipine + valsartan in patients who recently underwent kidney transplantation has not been established lena.Narushenie pecheniValsartan functions mainly excreted unchanged in bile. In patients, T1 / 2 is extended, and AUC is increased. Caution should be exercised when using the drug Vamloset in patients with a lung (5–6 points on the Child-Puh scale) or moderate (7–8 points on the Child-Puh scale) impaired liver function or obstructive biliary tract diseases. Violation of the kidney function Correction of the dose of Wamloset drug in patients with mild and moderate renal impairment is not required. In patients with moderate renal impairment, it is recommended that potassium and creatinine plasma levels be monitored. Simultaneous use of ARA II, including valsartan, or ACE inhibitors with aliskiren is contraindicated in patients with impaired renal function (Cl creatinine less than 60 ml / min). Primary hyperaldosteronism Considering RAAS lesion in primary hyper aldosteronism, these patients should not be given ARA II, these patients should not be given ARA II. . valsartan. Angioedema of patients with angioedema (including swelling of the larynx and vocal cords, causing obstruction of the respiratory tract and / or swelling of the face, lips, pharynx and / or tongue) during treatment with the drug Valsacor, there were cases of angioneurotic edema in history, including and ACE inhibitors. With the development of angioedema, the drug should be immediately discontinued and the possibility of repeated use should be discontinued. Heart failure / myocardial infarction in patients whose renal function may depend on the activity of the RAAS (for example, in severe CHF),therapy with ACE and APA II inhibitors is accompanied by oliguria and / or an increase in azotemia, and in rare cases, acute renal failure and / or fatal outcome. Similar outcomes have been described with valsartan. Patients with CHF or myocardial infarction should always evaluate kidney function. In patients with CHF of non-ischemic etiology of functional class III – IV, NYHA 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 rate of CHF between the two groups. . BKK, incl. Amlodipine should be used with caution in patients with CHF, because possible increase in the risk of cardiovascular complications and death. Mild and moderate aortic valve and mitral valve stenosis As with any vasodilator, care should be taken in patients with mitral stenosis and mild and aortic stenosis. The combination of amlodipine + valsartan was studied only in patients with arterial hypertension. The effect on the ability to drive and work with mechanisms. When using the drug Vamloset, care must be taken when driving vehicles and other technical devices that require high concentration of attention and speed of psychomotor reactions, since dizziness, fatigue, and nausea may occur.