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.
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.
Valsacor
When using the drug Valsacor in patients with hypertension, regular monitoring of laboratory parameters is not required.
Hyponatremia and/or dehydration.
In patients with severe hyponatremia and/or dehydration, for example due to taking large doses of diuretics, in rare cases, arterial hypotension with clinical manifestations may develop at the beginning of therapy with Valsacor. Before starting treatment, it is recommended to restore the sodium content and/or replenish the volume of blood volume, in particular by reducing the doses of diuretics.
If arterial hypotension with clinical manifestations develops: the patient must be placed in a horizontal position and, if necessary, injected intravenously with a 09% sodium chloride solution. Therapy with Valsacor can be continued only after stabilization of hemodynamic parameters.
Hyperkalemia.
The simultaneous use of potassium-sparing diuretics (spironolactone eplerenone triamterene amiloride), potassium preparations, potassium-containing nutritional supplements or other drugs that can increase the level of potassium in the blood serum (for example, heparin) is not recommended. It is necessary to monitor the potassium content in the blood plasma.
Renal artery stenosis.
Short-term use of valsartan in patients with renovascular hypertension developed secondary to unilateral stenosis of the artery of a solitary kidney was not accompanied by significant changes in renal hemodynamic parameters, creatinine or urea nitrogen concentrations in the blood serum. Since other drugs acting on the RAAS can increase the concentrations of urea and creatinine in the blood serum in patients with bilateral renal artery stenosis or stenosis of the artery of a solitary kidney, it is recommended as a precaution to constantly monitor these indicators.
Condition after kidney transplantation.
The safety of Valsacor in patients who have recently undergone kidney transplantation has not been established.
Primary hyperaldosteronism.
Patients with primary hyperaldosteronism are resistant to antihypertensive drugs that affect the RAAS; therefore, the use of Valsacor is not recommended for such patients.
Stenosis of the aortic and/or mitral valves HOCM.
Valsacor should be used with caution in patients with hemodynamically significant stenosis of the aortic and/or mitral valves or with HOCM.
Renal dysfunction.
In patients with impaired renal function, no dose changes are required. Since there is no data on the use of the drug in severe renal failure (creatinine clearance less than 10 ml/min or 0167 ml/s) and in patients on hemodialysis in such cases the drug is recommended to be used with caution.
The simultaneous use of ARB II including valsartan or ACE inhibitors with aliskiren is contraindicated in patients with impaired renal function (creatinine clearance less than 60 ml/min).
Liver dysfunction.
For patients with mild or moderate liver dysfunction of non-biliary origin without cholestasis, the drug Valsacor at a dosage of 320 mg is contraindicated since the maximum daily dose should not exceed 80 mg.
History of angioedema.
Among patients with angioedema (swelling of the larynx and vocal cords causing obstruction of the airways and/or swelling of the face, lips, pharynx and/or tongue) during treatment with Valsacor, cases of a history of angioedema development were observed, including in response to ACE inhibitors. If angioedema develops, the drug should be discontinued immediately and the possibility of repeated use should be excluded.
Arterial hypertension.
For hypertension, the drug Valsacor can be used in monotherapy or simultaneously with other antihypertensive drugs, in particular diuretics.
CHF/increasing survival of patients with acute myocardial infarction.
It is possible to use the drug Valsacor in combination with other drugs used for acute myocardial infarction (thrombolytics, acetylsalicylic acid as an antiplatelet agent, beta-blockers and HMG-CoA reductase inhibitors (statins)). The simultaneous use of Valsacor and ACE inhibitors in this category of patients is not recommended because this combination therapy does not lead to an additional clinical effect and is accompanied by an increased risk of adverse events compared to therapy with the two drugs separately.
In patients with CHF, triple combination therapy: Valsacor with an ACE inhibitor and a beta-blocker is not recommended because it does not lead to additional clinical effect and is accompanied by an increased risk of adverse events.
The use of the drug Valsacor in patients with CHF or acute myocardial infarction often leads to a slight decrease in blood pressure, usually without discontinuation of the drug when dosing instructions are followed.
In patients whose renal function may depend on the activity of the RAAS (for example, in patients with CHF II-IV FC according to the NYNA classification), therapy with ACE inhibitors and ARA II is accompanied by oliguria and/or an increase in azotemia and, in rare cases, acute renal failure and/or death . Since valsartan is an ARA II, the possibility of deterioration of renal function with its use cannot be excluded.
Initiation of therapy in patients with CHF or acute myocardial infarction should be done with caution. Renal function should always be assessed when assessing patients.
Special information on excipients.
The drug Valsacor contains lactose; therefore, the drug is contraindicated in patients with lactase deficiency, lactose intolerance, and glucose-galactose malabsorption syndrome.
Care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions, as dizziness or weakness may develop due to arterial hypotension.
Valsacor: use according to instructions
The drug is taken as prescribed by a cardiologist for the following pathologies:
- heart failure of non-acute severity: with functional disorders while maintaining a stable physical condition and during periods of remission;
- after a heart attack, with persisting dysfunction of the left ventricle of the myocardium;
- chronic heart failure without correction of the condition with ACE inhibitors;
Valsacor N and ND are prescribed in cases of hypertension as part of complex treatment.
The treatment regimen depends on the existing health problems:
- average daily dosage at the initial stage: 20–40 mg of the drug twice a day;
- if necessary, the dose of the drug is increased to 160 mg per day;
- The maximum dose of medication per day is 320 mg.
The tablets are taken with a sufficient amount of water, regardless of meal time. There is no need to chew or crush the medicine beforehand. Valsacor is used for long-term correction of physical condition. The general course of its use is at least several months. If side effects are detected, the dose of the drug is reduced or it is recommended to buy a similar antihypertensive drug.
Valsacor, 90 pcs., 80 mg, film-coated tablets
Hyperkalemia.
Caution should be exercised when using potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium supplements, potassium-containing salt substitutes or other drugs that can increase plasma potassium levels (for example, heparin). It is necessary to regularly monitor the potassium content in the blood plasma.
Renal dysfunction.
In patients with impaired renal function, no dose changes are required. Because There are no data on the use of the drug in severe renal failure (creatinine Cl less than 10 ml/min or 0.167 ml/s) and in patients on hemodialysis; in such cases, the drug is recommended to be used with caution.
The simultaneous use of valsartan with aliskiren in patients with moderate and severe renal impairment (creatinine clearance less than 60 ml/min) is contraindicated.
Liver dysfunction.
In patients with mild to moderate liver dysfunction without cholestasis, Valsacor® should be used with caution.
Patients with hyponatremia and/or dehydration.
In patients with severe hyponatremia and/or dehydration, for example due to taking large doses of diuretics, in rare cases, arterial hypotension with clinical manifestations may develop at the beginning of therapy with Valsacor®. Before starting treatment, it is recommended to restore sodium and/or bcc levels, in particular by reducing the doses of diuretics.
Renal artery stenosis.
The use of valsartan in a short course in patients with renovascular hypertension, which developed secondary to stenosis of the artery of a single kidney, does not cause significant changes in renal hemodynamics, creatinine concentration or urea nitrogen in the blood serum. However, given that other drugs that affect the RAAS may cause an increase in serum urea and creatinine concentrations in patients with bilateral renal artery stenosis or arterial stenosis of a solitary kidney, it is necessary to regularly monitor the concentrations of creatinine and residual urea nitrogen in the blood serum.
Condition after kidney transplantation.
The safety of using Valsacor® in patients who have recently undergone kidney transplantation has not been established.
Primary hyperaldosteronism.
Patients with primary hyperaldosteronism are resistant to antihypertensive drugs that affect the RAAS, therefore the use of Valsacor® is not recommended for such patients.
Stenosis of the aortic and/or mitral valves, HOCM.
The drug Valsacor® should be used with caution in patients with hemodynamically significant stenosis of the aortic and/or mitral valves or with HOCM.
The period after an MI.
Concomitant use with ACE inhibitors is not recommended, because has no additional clinical benefits over monotherapy and increases the risk of adverse events.
The use of valsartan in patients after a myocardial infarction often leads to a slight decrease in blood pressure, but discontinuation of therapy due to arterial hypotension is usually not required if drug dosage recommendations are followed.
Treatment with Valsacor® should be initiated cautiously. Assessment of the condition of patients after acute myocardial infarction should include monitoring of renal function.
Possible simultaneous use in acute MI with other drugs: thrombolytics, acetylsalicylic acid, beta-blockers and HMG-CoA reductase inhibitors (statins).
CHF.
In patients with CHF, the simultaneous use of three classes of drugs is not recommended: ACE inhibitors, beta-blockers and valsartan, because this therapy did not provide additional clinical effect, and the risk of adverse events increased. Use in patients with CHF is usually accompanied by a decrease in blood pressure, however, if recommendations for dose selection are followed, treatment rarely requires discontinuation due to arterial hypotension. Treatment with Valsacor® in patients with CHF should be initiated with caution. Due to the suppression of RAAS activity in some patients (for example, in patients with CHF III–IV functional class according to the NYNA classification, whose kidney function depends on the state of the RAAS) during therapy with ACE inhibitors, a change in renal function is possible: the development of oliguria and/or progressive azotemia, and in in rare cases - acute renal failure and/or death. The drug Valsacor® blocks angiotensin II receptors, so patients with CHF require regular monitoring of renal function.
History of angioedema.
Among patients with angioedema during therapy with Valsacor®, there were cases of a history of angioedema, incl. and ACE inhibitors. If angioedema develops, the drug should be discontinued immediately and the possibility of repeated use should be excluded.
Special information on excipients
The drug Valsacor® contains lactose, so it should not be used for the following conditions: lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.
Impact on the ability to perform potentially hazardous activities that require special attention and quick reactions (for example, driving, working with moving mechanisms).
Due to the possibility of dizziness or weakness while using the drug Valsacor®, care must be taken when driving vehicles and engaging in potentially hazardous activities.
Side effects
During treatment with Valsacor, the following are likely:
- severe hypotension;
- muscle weakness, drowsiness, fatigue;
- loss of appetite, nausea, impaired intestinal motility;
- back pain;
- cough;
- insomnia.
In case of overdose, vomiting, disturbances in heart rhythm, coordination of movements, water-salt balance develop, a sharp headache occurs, a feeling of stunnedness, fainting, and toxic shock are possible.
Precautions and contraindications
Valsacor requires careful use and constant monitoring of well-being in cases of impaired renal and liver function during treatment after a heart attack. The drug enhances the toxic effect of medications containing acetylsalicylic acid. It is not advisable to take Valsacor simultaneously with cardiac glycosides, anti-gout medications, or potassium-sparing agents.
When combined with barbiturates, adrenergic blockers, vasodilators, the diuretic and hypotensive effect of Valsacor is enhanced. It is important to remember this when choosing dosages.
The medicine affects psychomotor reactions, so during the treatment period caution is required when creating vehicles and operating special equipment.
The drug is incompatible with alcohol and can provoke a sharp drop in blood pressure, hypoxia and vascular collapse.
It is necessary to refuse therapy with Valsacor:
- with renal artery stenosis, not on hemodialysis, with severe renal failure;
- with cirrhosis, severe hepatosis;
- acute dehydration;
- during pregnancy and lactation;
- in case of individual intolerance to the components.
Caution is required in various forms of cardiomyopathy, stenosis of the mitral valve or aorta.
Instructions for use VALSACOR® H80 (VALSACOR® H80)
Changes in serum electrolytes
The simultaneous use of potassium-containing nutritional supplements, potassium-sparing diuretics, potassium-containing salt substitutes or other substances that can increase the level of potassium in the blood (including heparin) with valsartan is not recommended. Appropriate monitoring of serum potassium levels is necessary.
There are reports of the development of hypokalemia during treatment with thiazide diuretics, including hydrochlorothiazide. Frequent monitoring of serum potassium levels is recommended. Treatment with thiazide diuretics, including hydrochlorothiazide, can cause hyponatremia and hypochloremic alkalosis. Thiazides, including hydrochlorothiazide, increase urinary excretion of magnesium, which can lead to hypomagnesemia. Thiazide diuretics reduce calcium excretion. This can lead to hypercalcemia. During treatment with diuretics, regular periodic monitoring of serum electrolytes should be carried out.
Patients with sodium and/or fluid deficiency
Patients receiving thiazide diuretics, including hydrochlorothiazide, should be monitored for signs of electrolyte and fluid imbalances.
In patients with severe sodium and/or fluid deficiency taking diuretics in high doses, in rare cases, symptomatic arterial hypotension may develop at the beginning of therapy with Valsacor® H80. Before starting treatment with Valsacor® H80, it is necessary to restore the content of electrolytes and fluid in the body.
Patients suffering from severe congestive heart failure or other diseases accompanied by stimulation of the RAAS
In cases where renal function is primarily dependent on the activity of the RAAS (for example, patients suffering from severe heart failure), treatment with ACE inhibitors may be accompanied by the development of oliguria and/or progressive azotemia, and, in rare cases, acute renal failure. The safety of Valsacor® H80 in patients with severe congestive heart failure has not been established. Therefore, we cannot exclude the fact that due to inhibition of the RAAS, the use of Valsacor® H80 may cause renal dysfunction. Such patients should not be prescribed Valsacor® H80.
Renal artery stenosis
Patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney should not be prescribed Valsacor® H80 for the treatment of hypertension to avoid increases in blood urea and serum creatinine levels.
Primary hyperaldosteronism
Patients with primary hyperaldosteronism should not be prescribed Valsacor® H80, since in such cases the RAAS is not activated.
Aortic stenosis, mitral stenosis, obstructive hypertrophic cardiomyopathy
As with other vasodilators, special caution should be exercised in patients with aortic stenosis, mitral stenosis, or obstructive hypertrophic cardiomyopathy.
Renal dysfunction
Patients with impaired renal function (creatinine clearance ≥30 ml/min) do not require changes in dosage of the drug. When prescribing Valsacor® H80 to patients suffering from impaired renal function, it is recommended to periodically monitor serum levels of potassium, creatinine and uric acid.
Kidney transplant
Currently, there is no experience with the safe use of Valsacor® H80 in patients who have recently undergone kidney transplantation.
Liver dysfunction
Valsacor® H80 should be prescribed with caution to patients with mild or moderate liver dysfunction without cholestasis. Thiazide diuretics should also be taken with caution in patients with impaired liver function or progressive liver disease, because minor changes in fluid and electrolyte balance may increase the risk of hepatic coma.
Angioedema
Cases of angioedema (including swelling of the larynx and glottis, leading to airway obstruction and/or swelling of the face, lips, pharynx and/or tongue) have been reported in patients receiving valsartan. Some of these patients have a history of angioedema while using other drugs, incl. and when using other angiotensin II receptor antagonists. If angioedema develops, treatment with angiotensin II receptor antagonists should be discontinued immediately. Repeated use of the drug is contraindicated.
Systemic lupus erythematosus
Exacerbation or activation of systemic lupus erythematosus has been reported with the use of thiazide diuretics, including hydrochlorothiazide.
Other metabolic disorders
Thiazide diuretics, including hydrochlorothiazide, may alter glucose tolerance and increase serum cholesterol, triglycerides, and uric acid. Patients with diabetes mellitus may require dose adjustments of insulin or oral hypoglycemic agents.
Thiazides may reduce urinary calcium excretion and cause intermittent and mild increases in serum calcium levels in the absence of known disorders of calcium metabolism. Severe hypercalcemia may be a sign of underlying hyperparathyroidism. Thiazides should be discontinued before parathyroid function tests are performed.
Photosensitivity
Cases of photosensitivity reactions have been reported when taking thiazide diuretics. If these reactions occur during treatment, it is recommended to discontinue treatment. If resumption of a diuretic is necessary, it is recommended to protect the exposed areas from the sun or artificial UV rays.
Hypersensitivity reactions
The drug should be prescribed with caution to patients with hypersensitivity to other angiotensin II receptor antagonists. Hypersensitivity reactions to hydrochlorothiazide are most likely in patients suffering from allergies and bronchial asthma.
Acute angle-closure glaucoma
Hydrochlorothiazide has been associated with an idiosyncratic reaction that can lead to acute transient myopia and acute angle-closure glaucoma. There is a sharp decrease in visual acuity or pain in the eyes. These symptoms usually last for several hours a week while using the drug. Untreated glaucoma can lead to permanent vision loss. If intraocular pressure remains uncontrolled, surgical treatment may be required. In such cases, you should immediately stop taking the drug. A risk factor for the development of acute angle-closure glaucoma is an allergic reaction to the use of sulfonamide or penicillin.
Double blockade of the RAAS
When using drugs that affect the RAAS, especially when taken simultaneously, arterial hypotension, syncope, stroke, hyperkalemia, and renal dysfunction (including acute renal failure) have been reported. In patients receiving valsartan and other drugs that affect the RAAS, blood pressure, renal function, and electrolyte levels in the blood should be regularly monitored. In patients with diabetes mellitus and patients with renal failure (GFR <60 ml/min), the simultaneous use of aliskiren and valsartan is contraindicated.
Excipients
Valsacor® H80 contains lactose, therefore the drug is not recommended for patients with lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome.
Impact on the ability to drive vehicles and operate machinery
There is no data on the effect of the drug Valsacor® H80 on the ability to drive vehicles and potentially dangerous mechanisms. When driving or operating machinery, be aware that when taking a combination of valsartan and hydrochlorothiazide, there may be a risk of dizziness or fatigue.
