Valsacor
Valsacor (valsartan) is a selective angiotensin II receptor antagonist that blocks AT1 receptors. Used in cardiology for the treatment of arterial hypertension, incl. in pediatric practice in patients 6-18 years old. Valsacor does not suppress angiotensin-converting enzyme (ACE), and therefore does not cause a dry cough, unlike ACE inhibitors. In the treatment of hypertension, Valsacor reduces blood pressure without causing tachycardia. A single dose of the drug begins to act within two hours after administration, and the peak antihypertensive effect is observed at 4-6 hours. The therapeutic effect is maintained throughout the day. With regular use of Valsacor, the most pronounced decrease in blood pressure is observed after 2-4 weeks. The use of the drug in combination with hydrochlorothiazide enhances the antihypertensive effect. Sudden cessation of the drug course is not accompanied by the development of withdrawal syndrome (in particular, it does not cause a sharp increase in blood pressure). In post-infarction patients, Valsacor reduces the risk of sudden cessation of cardiac activity, hospitalization, incl. due to recurrent myocardial infarction or stroke. When using Valsacor and lifestyle correction in patients suffering from arterial hypertension due to insulin resistance, there was a decrease in the risk of developing diabetes mellitus.
When using Valsacor in pediatrics, the drug provides a smooth decrease in blood pressure. The magnitude of this decrease is determined by the dose of the drug. When using Valsacor simultaneously with potassium-sparing diuretics or heparin, it is necessary to regularly check the presence of potassium in the blood to prevent the development of hyperkalemia. Patients suffering from kidney disease take Valsacor on a general basis: no dose adjustment is required. In patients with liver pathologies, the drug is used with extreme caution. In post-infarction patients, it is not recommended to use Valsacor together with ACE inhibitors: this will not bring clinical benefits, but will increase the risk of adverse reactions. The use of Valsacor in this category of patients should be started with caution. While using the drug, weakness or vertigo may occur, so during the drug course it is not recommended to engage in activities that require increased attention, concentration and reaction speed (driving a car, working on potentially dangerous mechanisms, etc.). The presence of food contents in the gastrointestinal tract does not significantly affect the rate and completeness of absorption of valsartan and its bioavailability, therefore Valsacor can be taken regardless of meals.
Valsacor® H80
Common drug interactions for valsartan and hydrochlorothiazide
Concomitant use is not recommended
Lithium preparations
With the simultaneous use of ACE inhibitors, AR II or thiazide diuretics with lithium preparations, a reversible increase in the concentration of lithium in the blood plasma and the development of intoxication were observed. The risk of toxic effects associated with the use of lithium preparations may further increase when used simultaneously with Valsacor® N 80, since the renal clearance of lithium preparations is reduced by the influence of thiazide diuretics. If simultaneous use with lithium preparations is necessary, the concentration of lithium in the blood plasma should be carefully monitored.
Concomitant use with caution
Other antihypertensive drugs
The antihypertensive effect may be enhanced when used simultaneously with other drugs that lower blood pressure (for example, ACE inhibitors, beta-blockers, slow calcium channel blockers (SCBCs), guanethidine, methyldopa, vasodilators, direct renin inhibitors, ARA II).
Pressor amines (eg, norepinephrine and epinephrine)
The effect of pressor amines may be weakened, which does not require discontinuation of the simultaneous use of valsartan and HCTZ.
Nonsteroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase-2 (COX-2) inhibitors
With simultaneous use of ARA II and HCTZ with NSAIDs, the diuretic and antihypertensive effects may be weakened. In conditions of hypovolemia, the development of acute renal failure is possible; it is recommended to monitor renal function at the beginning of therapy, as well as to adequately replenish the patient's blood volume.
Drug interactions for valsartan
Concomitant use is contraindicated
Concomitant use of ARB II, including valsartan, with drugs containing aliskiren is contraindicated in patients with diabetes and/or with moderate or severe renal impairment (GFR less than 60 ml/min/1.73 m2 body surface area) and is not recommended in others patients.
Concomitant use of ARB II with ACE inhibitors is contraindicated in patients with diabetic nephropathy and is not recommended in other patients.
Concomitant use is not recommended
Potassium-sparing diuretics (spiropolactone, eplerenone, triamterene, amiloride), potassium supplements, potassium-containing table salt substitutes and other drugs and substances that can cause an increase in potassium levels in the blood serum (for example, heparin)
If simultaneous use with drugs that affect potassium levels is necessary, it is recommended to monitor the potassium content in the blood plasma.
Concomitant use with caution
When used simultaneously with ARA II, including valsartan, with drugs that affect the RAAS, such as ACE inhibitors or aliskiren, the incidence of arterial hypotension, hyperkalemia, and renal dysfunction increases. It is necessary to monitor blood pressure, renal function, and electrolyte levels in the blood plasma in such patients.
Transport proteins
In vitro studies on liver cultures showed that valsartan is a substrate for the OATPIB1/OATPIB3 and MRP2 transporter proteins. Concomitant use of valsartan with inhibitors of the OATP1B1/OATP1B3 transport protein (rifampicin, cyclosporine) or MRP2 (ritonavir) may increase the systemic exposure of valsartan (Cmax and AUC). Caution must be exercised when starting simultaneous use with the above drugs or after their discontinuation.
No drug interactions
No clinically significant interactions have been identified with the following drugs: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, HCTZ, amlodipine and glibenclamide.
Drug interactions for HCTZ
Concomitant use with caution
Medicines that affect potassium levels in blood plasma
When used simultaneously with loop diuretics, glucocorticosteroids (GCS), adrenocorticotropic hormone (ACTH), amphotericin B, benzathine benzylpenicillin, carbenoxolone, laxatives, acetylsalicylic acid or its derivatives, the risk of developing a decrease in potassium in the blood plasma and hypokalemia increases. In this case, it is recommended to monitor the potassium content in the blood plasma.
Drugs that can cause polymorphic ventricular tachycardia of the torsade de pointes type
When using antiarrhythmic drugs of classes IA and III and some antipsychotic drugs (neuroleptics) with HCTZ, caution should be exercised, as there is a risk of developing arrhythmias against the background of possible hypokalemia. Monitoring of potassium levels in blood plasma is recommended.
Non-depolarizing peripheral muscle relaxants (tubocurarine)
HCTZ potentiates the action of muscle relaxants.
Hypoglycemic agents (oral and insulin)
With simultaneous use, dose adjustment of hypoglycemic agents may be required.
Metformin should be taken with caution, since the development of lactic acidosis induced by renal failure while taking HCTZ is possible.
Medicines that affect plasma sodium levels
With long-term simultaneous use with antidepressants, anticonvulsants, antipsychotic (neuroleptic) drugs (for example, carbamazepine), etc., caution should be exercised, as the risk of developing hyponatremia increases. It is recommended to regularly monitor the sodium content in the blood plasma.
Cardiac glycosides
Hypokalemia and hypomagnesemia while taking thiazide diuretics may contribute to the development of cardiac arrhythmias in patients receiving cardiac glycosides.
N- and m-anticholinergics
H- and m-anticholinergic agents (atropine, biperiden) can increase the bioavailability of thiazide diuretics by reducing the peristaltic activity of the gastrointestinal tract (GIT) and slowing gastric emptying. Accordingly, gastrointestinal motility stimulants (cisapride) may reduce the bioavailability of thiazide diuretics.
Anion exchange resins (colestyramine and colestipol)
The absorption of thiazide diuretics, including HCTZ, is reduced with simultaneous use of cholestyramine and colestipol. Therefore, HCTZ should be taken 4 hours before or 4-6 hours after taking anion exchange resins.
Methyldopa
Isolated cases of the development of hemolytic anemia have been described with the simultaneous use of methyldopa and HCTZ.
Vitamin D and calcium salts
The simultaneous use of thiazide diuretics, including HCTZ, with vitamin D or calcium salts can lead to an increase in calcium levels in the blood plasma as a result of increased calcium reabsorption.
Cyclosporine
With simultaneous use of HCTZ and cyclosporine, the risk of developing hyperuricemia and symptoms similar to exacerbation of gout increases.
Radiocontrast agents containing iodine
Hypovolemia that develops while taking diuretics increases the risk of developing acute renal failure. It is necessary to replenish the blood volume before using products with a high iodine content (for example, radiocontrast agents containing iodine).
Medicines to treat gout (probenecid, sulfinpyrazone and allopurinol)
When using HCTZ, it is possible to increase the concentration of uric acid in the blood plasma, which may require dose adjustment of drugs for the treatment of gout (for example, increasing the dose of sulfinpyrazone and probenecid). Concomitant use with thiazide diuretics, including HCTZ, may lead to an increased incidence of hypersensitivity reactions to allopurinol.
Amantadine
Concomitant use with thiazide diuretics, including HCTZ, increases the risk of side effects from amantadine.
Beta blockers and diazoxide
Concomitant use with thiazide diuretics, including HCTZ, increases the risk of developing hyperglycemia.
Cytotoxic drugs (cyclophosphamide, methotrexate)
Concomitant use with thiazide diuretics, including HCTZ, reduces the excretion of cytotoxic drugs by the kidneys, which leads to potentiation of their myelosuppressive effect.
Ethanol, barbiturates and narcotic drugs
Concomitant use with thiazide diuretics, including HCTZ, may potentiate the development of orthostatic hypotension.
Valsacor®
When using Valsacor® in patients with hypertension, regular monitoring of laboratory parameters is not required.
Double blockade of the RAAS
In some patients, double blockade of the RAAS was accompanied by the development of severe arterial hypotension, syncope, stroke, hyperkalemia and renal dysfunction (including acute renal failure).
The simultaneous use of ARB II, including valsartan, with drugs that affect the RAAS, such as ACE inhibitors or aliskiren, is not recommended; if such therapy is necessary, blood pressure, renal function, and blood plasma electrolyte levels should be carefully monitored. Concomitant use of ARB II, including valsartan, with drugs containing aliskiren is contraindicated in patients with diabetes mellitus and/or with moderate or severe renal impairment (GFR less than 60 ml/min/1.73 m2 body surface area) and is not recommended in other patients.
The simultaneous use of ARB II with ACE inhibitors is contraindicated in patients with diabetic nephropathy and is not recommended in other patients.
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 levels and/or replenish 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, a 0.9% sodium chloride solution should be administered intravenously. Therapy with Valsacor® can be continued only after stabilization of hemodynamic parameters.
Hyperkalemia
Concomitant use of potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium supplements, potassium-containing nutritional supplements or other drugs that can increase serum potassium levels (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, which developed secondary to unilateral stenosis of the artery of a single kidney, was not accompanied by significant changes in renal hemodynamics, creatinine concentrations or serum urea nitrogen. Because other drugs that affect the RAAS can increase serum urea and creatinine concentrations in patients with bilateral renal artery stenosis or solitary renal artery stenosis, continuous monitoring of these values is recommended as a precaution.
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
The drug 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 change in drug doses is required, since there is no data on the use of the drug Valsacor® in severe renal failure (creatinine clearance less than 10 ml/min or 0.167 ml/s) and in patients on hemodialysis, in such cases In cases, the drug is recommended to be used with caution. Concomitant use of ARB II, including valsartan, or ACE inhibitors with aliskiren is contraindicated in patients with impaired renal function (GFR less than 60 ml/min/1.73 m2 body surface area).
Liver dysfunction
For patients with impaired liver function, biliary cirrhosis and cholestasis, 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 development of angioedema in the anamnesis were observed, including when taking ACE inhibitors. If angioedema develops, the drug should be immediately discontinued and the possibility of its re-use should be excluded.
Arterial hypertension
For hypertension, the drug Valsacor® can be used in monotherapy or simultaneously with other antihypertensive drugs, in particular with 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, since this combination therapy does not lead to additional clinical effect and is accompanied by an increased risk of developing AEs compared to therapy with the two drugs separately.
In patients with CSP, triple combination therapy (with Valsacor®, an ACE inhibitor and a beta-blocker) is not recommended, since it does not lead to additional clinical effect and is accompanied by an increased risk of developing AEs.
The use of Valsacor® in patients with CHF or acute myocardial infarction often leads to a slight decrease in blood pressure. As a rule, discontinuation of the drug is not required if 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 NYHA classification), therapy with ACE inhibitors and ARB II is accompanied by oliguria and/or an increase in azotemia, and in rare cases, AKI and/or death outcome. Since valsartan is a II ARA, the possibility of deterioration of renal function with its use cannot be excluded.
Initiation of therapy in patients with XCII 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.
