Pharmacological properties of the drug Valsacor
The active hormone of the renin-angiotensin-aldosterone system is angiotensin II, which is formed from angiotensin I with the participation of ACE. Angiotensin II binds to specific receptors that are located on the cell membranes of various tissues. It has a whole range of physiological effects, exhibiting both direct and indirect effects on the regulation of blood pressure. As a powerful vasoconstrictor, angiotensin II has a direct pressor effect. In addition, it promotes sodium retention and aldosterone secretion. Valsartan is an oral, potent and specific angiotensin II receptor antagonist. Selectively acts on receptors of the AT1 subtype, which are responsible for the action of angiotensin II. When the concentration of angiotensin II in the blood plasma increases after blockade of AT1 receptors by valsartan, stimulation of unblocked AT2 receptors occurs, which regulate the action of AT1 receptors. Valsartan does not exhibit any agonistic activity towards AT1 receptors and has a significantly greater affinity (approximately 20,000 times) for AT1 receptors than for AT2 receptors. Valsartan does not inhibit the activity of ACE, also known as kininase II, an enzyme that converts angiotensin I into angiotensin II and catalyzes the breakdown of bradykinin. Angiotensin II antagonists do not cause cough because they do not affect the activity of ACE and do not increase the production of bradykinin and substance P. In clinical studies in which valsartan was compared with other ACE inhibitors, the incidence of dry cough in patients taking valsartan was significantly lower (P ≤0.05) than in patients using an ACE inhibitor (2.6% compared with 7.9%). In a clinical trial, dry cough was reported in 19.5% of patients taking valsartan, 19.0% of patients taking a thiazide diuretic, compared with 68.5% of patients taking an ACE inhibitor (P≤0.05). Valsartan does not bind to or block other hormonal receptors or ion channels important for the regulation of the cardiovascular system. Treatment of patients with hypertension (arterial hypertension) with valsartan helped reduce blood pressure without affecting heart rate. In most patients, the hypotensive effect develops within 2 hours after a single oral dose, and the maximum effect on blood pressure is observed after 4–6 hours and lasts 24 hours. With repeated administration of the drug at any dose, the maximum reduction in blood pressure is achieved after 2–4 weeks and persists throughout the entire treatment period. With the combined use of hydrochlorothiazide, a significant additional reduction in blood pressure occurs. Discontinuation of valsartan does not cause a sudden increase in blood pressure and other undesirable clinical events in patients. In a long-term study of the use of valsartan in patients with heart failure, it was noted that in patients taking valsartan, there was a decrease in plasma norepinephrine and brain natriuretic peptide levels compared to the initial level. Valsartan produced significant improvements in pulmonary capillary wedge pressure, systemic vascular resistance, cardiac output, and systolic blood pressure. Patients using valsartan experience a significant increase in ejection fraction and a decrease in the internal diameter of the left ventricle compared to the initial state, and a significant decrease in the severity of symptoms of heart failure, including shortness of breath, fatigue, swelling and breath sounds. Valsartan is rapidly absorbed after oral administration, but the amount absorbed varies significantly. The average absolute bioavailability of valsartan is 23%. Valsartan is characterized by multi-exponential elimination kinetics (half-life in the α phase ≤1 hour and half-life in the β phase ≈9 hours). The pharmacokinetics of valsartan in the studied dose range is linear. With repeated administration of the drug, the pharmacokinetic parameters do not change; When the drug is administered once a day, only a slight accumulation of valsartan is observed. Valsartan binds well to serum proteins (94–97%), mostly to albumin. The volume of distribution at steady state is low (≈17 l). Plasma clearance occurs relatively slowly (≈2 L/h) compared to hepatic blood flow (≈30 L/h). The drug is excreted mainly unchanged: 70% of the absorbed amount is in feces, 30% in urine. When valsartan is taken with food, AUC decreases by 48%; however, after 8 hours, the concentration of valsartan in the blood plasma is the same both when taken on an empty stomach and when taken with food. This indicates the possibility of using valsartan regardless of food intake.
Mechanism of action of drugs
Valsacor provides a long-term reduction in the resistance of vascular walls, prevents their spasms, improves myocardial contractility, and increases the volume of blood pumped by the heart. As a result, unfavorable symptoms of deficiency disappear:
- think in your ears and head;
- swelling;
- dyspnea;
- physical weakness;
- dizziness.
Valsacor N maintains normal blood pressure, reduces the likelihood of valsartan side effects, and helps hypertensive patients maintain good health. Hydrochlorothiazide in its composition has a diuretic effect, stimulates the excretion of excess sodium and chlorine.
The medicine quickly dissolves in the stomach after administration and is absorbed into the blood. The effect of one dose of tablets develops over 30–60 minutes, reaches a maximum after 4–5 hours and lasts up to a day. With regular use, Valsacor provides an increasing antihypertensive effect after 3-4 weeks - it prevents the development of high blood pressure.
About 60% of hydrochlorothiazide ingested interacts with blood proteins; in combination with valsartan, it is less bioavailable. The components of the drugs do not accumulate in the body. Metabolism occurs in the liver, then the remaining substances are excreted through the intestinal contents and through the kidneys. Disintegration and release occur approximately 9 hours after the dose of the drug.
Use of the drug Valsacor
AH (arterial hypertension) The recommended dose of Valsacor is 80 mg 1 time per day, regardless of the patient’s age, gender or race. The hypotensive effect is achieved after 2 weeks, and the maximum antihypertensive effect is achieved after 4 weeks of treatment. For patients who do not achieve an adequate reduction in blood pressure, the daily dose can be increased to 160 mg or supplemented with diuretic therapy. There is no need to change the dose in patients with impaired renal or hepatic function of non-biliary origin in the absence of cholestasis. Valsacor can also be taken in combination with other antihypertensive drugs. Heart failure The recommended initial dose is 40 mg 2 times a day. This dose is gradually increased to 80 mg twice daily and then to 160 mg twice daily, the highest dose the patient can tolerate. The maximum daily dose of valsartan is 320 mg. For patients who are simultaneously treated with a diuretic, it is recommended to reduce the dose of Valsacor. Post-myocardial infarction Treatment with the drug can begin 12 hours after myocardial infarction. The initial dose of Valsacor is 20 mg 2 times a day. At the beginning of treatment, it is recommended to use Valsacor 40 mg tablets with a notch on one side. After a few weeks, the dose should be gradually increased to 40, 80 and 160 mg 2 times a day, depending on the patient’s tolerance to treatment. If symptomatic hypotension or renal failure occurs, the dose should be reduced.
Side effects of the drug Valsacor
During treatment with the drug, viral infections, upper respiratory tract infections, rhinitis, sinusitis, and pharyngitis often occurred (≥1%). Nervous system and mental disorders; headache, dizziness; cough; nausea, diarrhea, abdominal pain; back pain and arthralgia; hyperkalemia; fatigue. Rarely (≤1%) rash, itching, insomnia, and swelling were noted; isolated cases of hypersensitivity reactions; very rarely - renal function disorders. The frequency of side effects does not depend on the dose and period of treatment, as well as the gender, race and age of the patient.
Special instructions for the use of the drug Valsacor
Caution should be exercised when starting treatment in patients with heart failure after myocardial infarction. They often initially experience a slight decrease in blood pressure, however, if dosing instructions are properly followed, such symptomatic hypotension for the most part does not cause discontinuation of treatment. During treatment with Valsacor, renal function should be regularly checked in patients with heart failure and special caution should be exercised with the combined use of ACE inhibitors, beta-adrenergic blockers and angiotensin II receptor antagonists (AT1 subtype). In debilitated patients and/or with significantly reduced sodium levels (for example, those taking high doses of diuretics), symptomatic hypotension may rarely occur when starting treatment with Valsacor. Before starting therapy, it is necessary to restore the amount of water and sodium in the body (for example, by reducing the dose of the diuretic). If arterial hypotension occurs, the patient should be placed in a horizontal position and, if necessary, given an intravenous infusion of 0.9% sodium chloride solution. After stabilization of blood pressure, treatment with Valsacor can be continued. During therapy, it is recommended to carefully evaluate patients with unilateral or bilateral renal artery stenosis, since drugs that affect the activity of the renin-angiotensin-aldosterone system can cause an increase in serum urea and creatinine levels. The drug should be used with caution in patients with impaired renal function and obstructive diseases of the biliary tract. In this case, the dose should not be reduced. Since Valsacor contains lactose, the drug is not recommended for use in patients with galactosemia, lactase deficiency or impaired glucose/galactose absorption. In patients with hypersensitivity, changes in the functional activity of the kidneys may occur, which are caused by inhibition of the activity of the renin-angiotensin system. Treatment with ACE inhibitors and angiotensin II receptor antagonists (AT1 subtype) should not be carried out in patients whose renal function depends on the activity of the renin-angiotensin-aldosterone system. This can cause oliguria, progressive azotemia, and sometimes acute renal failure or death. Children. The safety and effectiveness of the drug in treating children has not been established. Period of pregnancy or breastfeeding. Given the mechanism of action of angiotensin II receptor antagonists, a risk to the fetus cannot be excluded. It has been shown that the use of ACE inhibitors in the second and third trimester of pregnancy can cause damage and death of the fetus. Like other drugs that act directly on the renin-angiotensin-aldosterone system, Valsacor is not recommended for use during pregnancy. It is not known whether valsartan passes into breast milk, so Valsacor is not recommended for use during breastfeeding. The ability to influence reaction speed when driving vehicles or working with other mechanisms. As with the use of other antihypertensive drugs, during treatment with Valsacor it is recommended to exercise caution when driving vehicles and operating machinery.
Valsacor tablets p/o 160 mg No. 15x2 (valsartan)
Name
Valsacor.
Release form
Film-coated tablets.
Dosage
160 mg. Quantity per package: 30 pcs.
Manufacturer
Krka dd.
INN
Valsartan.
FTG
Angiotensin II receptor antagonist.
What is the drug and what is it used for?
Valsacor® belongs to a class of medications known as angiotensin II receptor antagonists, which help control high blood pressure (BP). Angiotensin II is a substance in your body that increases vascular tone, thereby causing an increase in blood pressure. Valsacor® acts by blocking the effect of angiotensin II. As a result, the blood vessels relax and blood pressure decreases. Valsacor® film-coated tablets 80 mg and 160 mg can be used for three different indications: • Treatment of high blood pressure in adults and children aged 6 to 18 years High blood pressure (BP) increases the workload of the heart and arteries. If left untreated, it can cause damage to blood vessels in the brain, heart and kidneys, as well as stroke, heart failure or kidney failure. High blood pressure increases the risk of myocardial infarction. Lowering blood pressure usually reduces the risk of developing these diseases. • Treatment of adult patients after a recent heart attack (myocardial infarction) “Recent” in this case means a period of 12 hours to 10 days. • Treatment of symptomatic heart failure in adult patients Valsacor® can be used for the treatment of symptomatic heart failure in adult patients. Valsacor® is used when a group of drugs called angiotensin-converting enzyme (ACE) inhibitors (medicines to treat heart failure) cannot be used or the drug may be used in addition to ACE inhibitors when other drugs to treat heart failure cannot be used. Symptoms of heart failure include shortness of breath and swelling of the feet and legs due to fluid retention. This occurs when the heart muscle cannot pump blood enough to move blood throughout the body.
Do not take the drug
- if you are allergic to valsartan or any other components of the drug (listed in the “Composition” section); - if you have severe liver disease; - if your pregnancy is more than 3 months old (it is recommended to avoid taking Valsacor® in the early stages of pregnancy, see section “Pregnancy”); - simultaneous use of Valsacor® and drugs that lower blood pressure and contain aliskiren is contraindicated if you have diabetes mellitus or renal failure. If any of the above applies to you, do not take Valsacor®. Special instructions and precautions Before taking Valsacor®, consult your doctor: - if you have liver disease; - if you have serious kidney disease or are on dialysis; - if you have narrowing of the renal artery; - if you have recently undergone a kidney transplant (received a new kidney); - if you are being treated after a myocardial infarction or for heart failure. Your doctor may test your kidney function; - if you have any other serious heart disease other than heart failure or myocardial infarction; - If you have ever had swelling of your tongue or face caused by an allergic reaction called angioedema while taking another drug (including ACE inhibitors), tell your doctor. If these symptoms occur while taking Valsacor®, stop taking it immediately and never start again. See also the section “Possible adverse reactions); - if you are taking medications that increase potassium levels in the blood. These include potassium supplements or salt substitutes containing potassium, potassium-sparing drugs, and heparin. It may be necessary to check the amount of potassium in your blood at regular intervals; - if you are under 18 years of age and are taking Valsacor® in combination with other drugs that inhibit the renin-angiotensin-aldosterone system (drugs that lower blood pressure). Your doctor may test your kidney function and blood potassium levels at regular intervals; - if you suffer from aldosteronism. (This is a disease in which the adrenal glands produce too much of the hormone aldosterone.) If this applies to you, the use of Valsacor® is not recommended; - if you have lost a lot of fluid (dehydration) due to diarrhea, vomiting or high doses of a diuretic (water tablets); - if you are taking any of the following medicines used to treat hypertension: - an ACE inhibitor (eg enalapril, lisinopril, ramipril), in particular if you have kidney disease associated with diabetes; - aliskiren. - if you are taking ACE inhibitors together with certain other medicines used for heart failure that are mineralocorticoid receptor (MCR) antagonists (eg spironolactone, eplerenone) or beta blockers (eg metoprolol). During treatment, your doctor may check your kidney function and measure blood pressure and electrolyte levels (including potassium) in the blood at regular intervals. See also the information under the heading “Do not take this medicine”. You should tell your doctor if you think you are pregnant (or are planning to become pregnant). Valsacor® is not recommended in early pregnancy, and is contraindicated in pregnancy more than 3 months, because the drug may cause serious harm to the baby if taken at this stage of pregnancy (see section "Pregnancy and breastfeeding"). If any of the above applies to you, tell your doctor before you start taking Valsacor®. Valsacor® contains lactose. If you are intolerant to certain sugars, tell your doctor before taking this medicine.
Other drugs
Tell your doctor if you are taking, have recently taken, or may start taking any other medications. The effect of treatment may be altered when taking Valsacor® together with certain other medications. It may be necessary to change the dose, take special precautions, or, in some cases, stop taking one of the medications. This applies to both prescription and over-the-counter drugs, especially: - other drugs that lower blood pressure, especially diuretics (water pills); - drugs that increase potassium levels in the blood. These include potassium supplements or salt substitutes containing potassium, potassium-sparing drugs, and heparin; - a certain group of painkillers called non-steroidal anti-inflammatory drugs (NSAIDs); - certain antibiotics (rifamycin group), drugs used to protect against transplant rejection (cyclosporine) or an antiretroviral drug used to treat HIV/AIDS infection (ritonavir). These drugs may enhance the effect of Valsacor®; - lithium, a drug used to treat some types of mental illness; - ACE inhibitors or aliskiren (see also the information under the headings “Do not take this drug” and “Special instructions and precautions”. Additionally: - if you are taking treatment after a myocardial infarction, combination with ACE inhibitors (medicines for the treatment of heart attack) is not recommended ; - if you are taking treatment after a myocardial infarction, a triple combination with ACE inhibitors and other drugs for the treatment of myocardial infarction, which are known as mineralcorticoid receptor antagonists (MRA) (for example, spironolactone, eplerenone), or beta blockers (for example, metoprolol).
Valsacor® with food, drinks and alcohol
Valsacor® can be taken regardless of meals.
Pregnancy and breastfeeding
If you are pregnant or breastfeeding, think you may be pregnant, or are planning to become pregnant, consult your doctor before using this medicine. - You should tell your doctor if you think you are pregnant (or are planning to become pregnant). Your doctor will advise you to stop taking Valsacor® immediately if you are planning a pregnancy, or as soon as you find out you are pregnant, and will suggest other treatment. Valsacor® is not recommended during the first trimester and is contraindicated in the second and third trimester of pregnancy, because Taking Valsacor® during this period may cause serious harm to your baby. — Tell your doctor if you are breastfeeding or plan to breastfeed. Valsacor® is not recommended for mothers who are breastfeeding, and your healthcare provider may choose a different type of treatment if you want to continue breastfeeding, especially if your baby has just been born or was born prematurely.
Driving vehicles and working with machinery
Before you start driving vehicles or operating machinery that requires concentration, you should know exactly how Valskor® affects you. When taking Valsacor®, as well as other drugs that lower blood pressure, in rare cases dizziness or an effect on concentration may occur.
Use of the drug
Always take the drug in full accordance with the recommendations of your doctor. This will help you get better treatment results and reduce the risk of side effects. You should consult your doctor if you are unsure. People with high blood pressure often do not notice any signs of this problem. Many people may feel quite normal. This highlights the importance of visiting your doctor even if you feel well. Adult patients with high blood pressure The recommended dose of valsartan is 80 mg per day. In some cases, the doctor may increase the dose (for example, to 160 mg or 320 mg) and prescribe a combination of Valsacor® with other drugs (for example, diuretics). Children and adolescents (ages 6–18 years) with high blood pressure The usual dose for patients weighing up to 35 kg is 40 mg valsartan once daily. The usual starting dose for patients weighing 35 kg or more is 80 mg valsartan once daily. In some cases, the doctor may increase the dose (for example, to 160 mg or a maximum of 320 mg). Adult patients after a recent heart attack Treatment is usually started no later than 12 hours after the heart attack, usually with the lowest dose of 20 mg twice daily. The 20 mg dose is provided by dividing the tablet into a 40 mg dose. Your doctor will increase this dose gradually over several weeks to a maximum dose of 160 mg twice daily. The final dose depends on individual tolerance. Valsacor® can be used together with other drugs to treat a heart attack. Your doctor will prescribe the appropriate treatment for you. Adult patients with heart failure Treatment usually begins with 40 mg twice daily. Your doctor will increase this dose gradually over several weeks to a maximum dose of 160 mg twice daily. The final dose depends on individual tolerance. Valsacor® can be used in combination with other drugs to treat heart failure. Your doctor will prescribe the appropriate treatment for you. Valsacor® can be taken regardless of meals. Swallow Valsacor® tablets with a glass of water. Take Valsacor® at approximately the same time every day. If you take more Valsacor® than you should If you experience severe dizziness and/or fainting, lie down and consult a doctor immediately. If you accidentally take too many tablets, contact your doctor or hospital immediately. If you forget to take Valsacor® Do not take a double dose to make up for the missed dose. If you forget to take a dose, take it as soon as you remember. However, if it is close to your next dose, skip the forgotten dose. If you stop taking Valsacor® Stopping treatment with Valsacor® may cause your condition to worsen. Do not stop taking the drug without consulting your doctor. If you have any further questions about the use of this drug, ask your doctor.
Possible adverse reactions
Like all medicines, this medicine can cause side effects, although not everyone gets them. Some symptoms require immediate medical attention: - symptoms of angioedema (a specific allergic reaction), such as swelling of the face, lips, tongue or throat, difficulty swallowing or breathing, hives, itching. If you experience any of these symptoms, stop taking Valsacor® and contact your doctor immediately (see also section "Special instructions and precautions"). Other side effects include: Common (may affect up to 1 in 10 people): - Dizziness, - Low blood pressure with or without symptoms such as dizziness and fainting when standing up, - Decreased kidney function (a sign of kidney failure). Uncommon (may affect up to 1 in 100 people): - Angioedema (see section "Some symptoms require immediate medical attention"), - Sudden loss of consciousness (fainting), - A spinning sensation (vertigo), - Severely decreased kidney function (a sign of acute renal failure), - Muscle spasms, irregular heart rhythm (signs of hyperkalemia), - Shortness of breath, difficulty breathing when lying down, swelling of the feet and legs (signs of heart failure), - Headache, - Cough, - Abdominal pain, - Nausea, - Diarrhea, - Fatigue, - Weakness. Frequency unknown (frequency cannot be estimated from available data): - Allergic reactions with rash, itching and urticaria; symptoms of fever, joint swelling and pain, muscle pain, swollen lymph nodes and/or flu-like symptoms (serum sickness symptoms), - purplish-red spots, fever, itching (signs of inflammation of the blood vessels, called vasculitis), - unusual bleeding or bruises (signs of thrombocytopenia), - Muscle pain (myalgia), - Fever, sore throat, or mouth ulcers due to infection (symptoms of low white blood cell counts, called neutropenia), - Decreased hemoglobin levels and a decrease in the proportion of red blood cells in the blood (which leads to anemia in severe cases), - Increased levels of potassium in the blood (which can, in rare cases, cause muscle cramps and irregular heart rhythms), - Increased levels of liver enzymes (which may indicate liver damage), including increased bilirubin in the blood (which can cause yellowing of the skin and eyes in severe cases), - increased blood urea levels and increased serum creatinine levels (which may indicate impaired kidney function), - decreased sodium levels in the blood (which can cause fatigue and confusion, and in severe cases, muscle twitching and/or seizures). The frequency of some side effects may vary depending on your condition. For example, side effects such as dizziness and decreased kidney function were observed less frequently in patients being treated for hypertension than in patients being treated for heart failure or after a recent myocardial infarction. Side effects in children and adolescents are similar to those observed in adults.
Reporting Adverse Reactions
If you experience any unwanted reactions, consult your doctor. This recommendation applies to any possible adverse reactions, including those not listed in this leaflet. By reporting side effects, you can help provide more information about the safety of the drug.
Storage of the drug
Store at a temperature not exceeding 30°C. Store in original packaging to protect from moisture. Keep out of the reach of children. Shelf life: 5 years. Do not use the drug after the expiration date indicated on the package. The expiration date is the last day of the month. Do not throw the drug into the water supply or sewer system. Ask your pharmacist how to dispose of medications that are no longer needed. These measures will protect the environment.
Compound
Active ingredient: 1 film-coated tablet contains 80 mg or 160 mg of valsartan. Excipients: lactose monohydrate, microcrystalline cellulose, povidone K 25, croscarmellose sodium, anhydrous colloidal silicon dioxide, magnesium stearate, hypromellose 6sr, titanium dioxide (E 171), red iron oxide (E 172), macrogol 4000. Film-coated tablets , 160 mg additionally contain iron oxide yellow (E 172).
Appearance of the drug and contents of the package
Film-coated tablets 80 mg tablets: round, biconvex tablets with beveled edges, scored on one side, pink film-coated. The score is intended to divide the tablet into two equal parts. Tablets 160 mg: oval, biconvex tablets with a score on one side, film-coated, brownish-yellow in color. The score is intended to divide the tablet into two equal parts. 7 film-coated tablets in a blister ((PVC/PE/PVDC)/aluminum foil). 2 or 4 blisters with an insert in a cardboard box. 10 film-coated tablets in a blister ((PVC/PE/PVDC)/aluminum foil). 3 blisters with an insert in a cardboard box. 14 film-coated tablets in a blister ((PVC/PE/PVDC)/aluminum foil). 1 or 2 blisters with an insert in a cardboard box. 15 film-coated tablets in a blister ((PVC/PE/PVDC)/aluminum foil). 2 or 4 blisters with an insert in a cardboard box.
Vacation conditions
By doctor's prescription.
Buy Valsacor tablet. p/captivity about. 160 mg per blister. in pack No. 15x2 in the pharmacy
Price for Valsacor tablet. p/captivity about. 160 mg per blister. in pack No. 15x2
Instructions for use for Valsacor tablet. p/captivity about. 160 mg per blister. in pack No. 15x2
Interactions of the drug Valsacor
For patients after myocardial infarction, Valsacor can be taken in combination with other drugs, such as thrombolytics, acetylsalicylic acid, beta-adrenergic blockers or statins. When Valsacor is used in combination with potassium-sparing diuretics (such as spironolactone, triamterene, amiloride), potassium preparations or salt substitutes that contain potassium, an increase in the concentration of potassium in the blood serum may occur. There were no signs of clinically significant interaction between Valsacor and other drugs. In clinical studies, drugs such as cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine, and glibenclamide were studied. Since Valsacor does not undergo significant metabolism, it is unlikely that clinically significant interactions in the form of metabolic induction or inhibition of the cytochrome P450 system will occur. Valsartan binds well to plasma proteins, but in vitro did not indicate any interactions at this level with molecules that are also highly protein bound (diclofenac, furosemide or warfarin).
Dosage form and composition
The medication is intended for oral administration and is available in the form of yellow film-coated tablets:
- Valsacor: contains the active substance valsartan - an antagonist of hormone receptors that provokes an increase in pressure in blood vessels, prevents the development of hypertensive attacks;
- Valsacor N80, ND160: a combination drug containing two active ingredients: valsartan and hydrochlorothiazide, has a more pronounced and long-lasting therapeutic effect, reduces blood pressure.
In addition to active compounds, pills contain auxiliary components: MCC, lactose, silicon dioxide, stabilizing and form-building additives.
