Valsacor

A relatively new drug that has a blood pressure lowering effect based on blocking the receptors of the oligopeptide hormone - angiotensin II. The h and hd variants of this drug are a complex that combines valsartan and hydrochlorothiazide in various doses, which reduces blood pressure in the arteries by acting on the renin-angiotensin-aldosterone system.

Indications Valsacora

Dysfunction of the heart muscle in combination with high blood pressure, post-infarction condition, high blood pressure that cannot be controlled by antihypertensive monodrugs.

Release form

Tablets with dosage of active ingredients:

Valsacor contains 40, 80, 160 and 320 mg of valsartan.

Valsartan, mg Hydrochlorothiazide, mg

Valsacor® h 80 80 12.5
Valsacor® h 160 160 12.5
Valsacor® hd 160 160 25
Valsacor® h 320 320 12.5
Valsacor® hd 320 320 25

Pharmacodynamics

The main active ingredient is valsartan, an angiotensin II receptor blocker (subtype AT1). This is the main peptide of the system regulating blood pressure and its volume in the body, acting as follows - by narrowing the vessels and increasing their peripheral resistance, angiotensin receptors of the second subtype connect with receptors of the first subtype. These physiological effects lead to a jump in blood pressure. The active ingredient, blocking AT-1 angiotensin receptors (A II), promotes a quantitative increase in free AII in the blood serum and an increase in the level of AT2 receptors, which connect with each other in the absence of free AT-1 receptors. This leads to a hypotensive effect, a decrease in systemic peripheral vascular resistance and systolic blood volume.

The action of Valsacor does not affect the contractile activity of the myocardium, effectively eliminates swelling and normalizes breathing in patients with impaired cardiac function.

Valsacor H and HD are complex drugs containing another active ingredient – the diuretic hydrochlorothiazide, which effectively reduces blood pressure and promotes the elimination of Na, Cl, K and water from the body.

The active ingredients of the complex drug synergistically complement each other's effectiveness and reduce the likelihood of unwanted side effects.

After two weeks from the start of the therapeutic course, significant normalization of arterial pressure is observed. The maximum effect of treatment with this drug is recorded after about a month. A single oral dose of the drug provides a 24-hour effect.

Pharmacokinetics

The active ingredients are well absorbed in the gastrointestinal tract. Valsartan binds to serum proteins almost completely (approximately 98%), hydrochlorothiazide – by 40-70%. The greatest diuretic effect develops after four hours and lasts for about 12.

Valsartan is excreted mainly through the intestines, a small part is excreted in the urine. Hydrochlorothiazide is eliminated through the kidneys, the main part - unchanged.

Dosing and administration

This drug is dosed for each patient taking into account his personal sensitization and the desired hypotensive effect.

At the beginning of treatment, a daily dosage of 80 mg of Valsacor is prescribed once or in two doses. After four weeks from the beginning of treatment, when the greatest hypotensive effect is observed, the dosage is adjusted.

The largest standard daily dose of the drug to lower blood pressure is 160 mg taken once or twice a day, 80 mg at 12-hour intervals.

If this treatment regimen is ineffective,
Options h or hd are used. Dosage is individual. For patients with liver dysfunction (without cholestasis) and with a creatinine excretion rate above 30 ml per minute, the dose is not adjusted.

When the contractility of the heart muscle decreases, a daily dosage of 80 mg of Valsacor is usually prescribed in two doses. Gradually, taking into account susceptibility to the active component, the single dosage is increased to 160 mg and taken at intervals of 1/2 day.

The maximum daily dose of valsartan is 320 mg.
With simultaneous administration of a diuretic, the maximum dose is 160 mg per day.

In post-infarction conditions, the intake of these tablets is prescribed with a daily dosage of 40 mg (it is divided into two doses, using Valsacor 40 tablets with a dividing notch),
maintaining a time interval of at least 12 hours. The dosage is gradually adjusted upwards, taking into account susceptibility to the active component, the maximum possible dosage of which is 320 mg per day.

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Use Valsacora during pregnancy

It is not recommended for pregnant women, women planning pregnancy and women breastfeeding. During this period, treatment should be carried out with antihypertensive drugs with an established safety profile for this category of patients.

Contraindications

Sensitization to active and additional ingredients of the drug, variants h and hd + to sulfonamides.

Pregnancy, lactation and age group 0-17 years.

Variants h and hd are not recommended for patients with severe liver pathologies, cholestasis, anuria, renal failure (creatinine excretion rate less than 30 ml per minute), on hemodialysis, after kidney transplantation, with renal artery stenosis and diseases where kidney function is determined by the RAAS (renin-angiotensin-aldosterone) system.

Valsacor h and hd are contraindicated in cases of decreased serum Na and Ca levels, low plasma concentration of K ions and increased blood uric acid levels (symptomatic), diabetes mellitus - patients taking aliskiren.
With caution, dose valsartan in patients after a heart attack and with impaired cardiac muscle function. This category of patients requires regular monitoring of kidney function during treatment with Valsacor.

Caution should be exercised when prescribing and dosing this drug to the following categories of patients:

• with Libman-Sachs disease;
• with narrowing of the lumen of the renal artery;
• water-electrolyte imbalance;
• with narrowing of the lumen of the aorta or bicuspid valve;
• hypertrophy of the walls of the left and right ventricles of the heart;

And also people whose work requires increased concentration.

Side effects Valsacora

Valsacor therapy may result in the following adverse effects:

• infection with viruses and bacteria with the development of respiratory infections (inflammation of the nasal sinuses and mucous membrane of the pharynx, runny nose, cough);
• dyspeptic symptoms, dizziness, weakness, pain in the head, muscles, joints during the treatment period;
• hyperkalemia, allergic rashes, negative impact on renal function.

Therapy with variants h and hd in addition to those already mentioned can lead to:

• arrhythmia, attacks of angina pectoris, significant hypotension;
• anemia, blood thinning and poor clotting;
• hepatitis, bile stagnation;
• mood swings, polarity of emotions, insomnia, drowsiness, numbness of the limbs;
• malignant exudative erythema, Quincke's edema, toxic epidermal necrolysis;
• sodium and/or potassium deficiency, tinnitus, hyperglycemia, hypercreatininemia, impaired renal excretory function and bile flow, minor hearing and visual disturbances, increased sweating.

Overdose

Overdose of Valsacor has not been reported. Potential symptoms of overdose of valsartan may include severe hypotension, possibly including impaired consciousness, shock, or collapse.
Overdose of hydrochlorothiazide may result in lethargy, decreased blood volume, and electrolytic imbalance, possibly with muscle spasms and heart failure.

First aid for clinically insignificant symptoms consists of appropriate treatment and administration of enterosorbents. Clinically significant reduction in blood pressure is corrected by infusion of NaCl solution (0.9%).

Interactions with other drugs

The combination of Valsacor with drugs containing K and diuretics that do not excrete K increases the likelihood of hyperkalemia.

The drug interactions of Valsacor h and hd are determined by the presence of hydrochlorothiazide.

Its combination with drugs containing Li or K increases the likelihood of excess serum levels of these substances. When prescribing such a combination, it is recommended to monitor the concentration of electrolytes in the blood.

Plasma concentration of K should be monitored when combined with antiarrhythmics and antipsychotics that promote activation of contractions of the heart muscle (the so-called "pirouette").

The risk of hypercalcemia increases when this active substance is combined with Ca and vitamin D3 preparations.

Concomitant use of Valsacor H and HD with hypoglycemic, anti-gout drugs, pressor amines and tubocurarine may require adjustments in their dosage.

Hydrochlorothiazide increases the likelihood of an increase in blood glucose levels from the action of ß-blockers and hyperstat.

Anticholinergics help to increase its bioavailability, while cholestyramine and cholestipol help to decrease it.

This substance increases the likelihood of developing the myelosuppressive effect of cytostatic drugs and the adverse effects of amantadine.

Nonsteroidal anti-inflammatory drugs reduce its effectiveness and the risk of developing renal failure increases.

Combination with methyldopa can provoke a reduction in the life cycle of red blood cells, with ethyl alcohol – orthostatic hypotension, with cyclosporine antibiotics – symptoms of gout.

Combination with tetracycline antibiotics increases their content in urine.

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Storage conditions

Store without damaging the packaging and at a temperature of up to 25°C.

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Shelf life

2 years.