Universal reference book for medicines
Product name: VALSAFORCE (VALSAFORCE )

Active substance: valsartan

Type: Angiotensin II receptor antagonist

Manufacturer: Farmaplant Fabrication chemischer Produkte (Germany) produced SYNTHESIS (Russia) marketing in the territory of the Russian Federation Promo-Med (Russia)
Composition, form of production and packaging
The tablets covered with a cover of
yellow color, round, biconcave form.

1 tab.

valsartan 80 mg

- "- 160 mg

Auxiliary substances: microcrystalline cellulose, low molecular weight polyvinylpyrrolidone (povidone), sugar milk (lactose), potato starch, aerosil (silicon dioxide colloid), talc, magnesium stearate, hydroxypropylmethylcellulose (hypromellose), titanium dioxide, polyethylene glycol 4000 (macrogol), tropeolin O.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (3) - packs cardboard.
14 pcs.
- packings of cellular contour (1) - packs cardboard.
14 pcs.
- packings cellular planimetric (2) - packs cardboard.
28 pcs.
- polymer cans (1) - packs of cardboard.
28 pcs.
- cans of glass (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2012.

PHARMACHOLOGIC EFFECT

Angiotensin II receptor antagonist.
The active hormone of the renin-angiotensin-aldosterone system (RAAS) is angiotensin II, which is formed from angiotensin I with the participation of ACE. Angiotensin II binds to specific receptors located on cell membranes in various tissues. It has a wide range of physiological effects, including primarily both direct and indirect participation in the regulation of blood pressure. Being a potent vasoconstrictor, angiotensin II causes a direct pressor response. In addition, it promotes sodium retention and stimulates the secretion of aldosterone.
Valsartan - a specific antagonist of angiotensin II receptors, intended for oral administration.
Has an antagonistic effect selectively on the receptors of the AT1 subtype, which are responsible for the known effects of angiotensin II. The consequence of the blockade of AT 1 -receptors is an increase in the plasma concentration of angiotensin II, which can stimulate unblocked AT 2 receptors. Does not have any expressed agonistic activity against AT 1 -receptors. The affinity of valsartan for the receptors of the AT1 subtype is approximately 20,000 times higher than that of the AT 2 receptor subtype.
In the treatment of valsartan in patients with hypertension, there is a decrease in blood pressure, not accompanied by a change in the pulse rate.
After administration of a single dose of the drug in most patients, the onset of antihypertensive action is observed within 2 hours, and the maximum decrease in blood pressure is achieved within 4-6 hours. After taking the drug, the antihypertensive effect persists for more than 24 hours. For repeated prescriptions of the drug, the maximum decrease in blood pressure, of the accepted dose, is usually achieved within 2-4 weeks and maintained at the achieved level during prolonged therapy.
The sudden discontinuation of valsartan is not accompanied by a sharp increase in blood pressure or other undesirable clinical consequences.

PHARMACOKINETICS

After taking the drug, suction of valsartan takes place quickly, but the degree of absorption varies widely.
The average absolute bioavailability of valsartan is 23%.
The pharmacokinetic curve has a downward multiexponential character (T 1/2? - <1 h and T 1/2? - about 9 h).

In the range of doses studied, the kinetics of valsartan is linear.
With repeated use of the drug, no changes in the kinetic parameters were noted. When taking the drug 1 time / day, the cumulation is insignificant. Plasma concentrations in women and men were similar.
Valsartan is bound to a significant extent (by 94-97%) with serum proteins, mainly albumin.
V d in the equilibrium state is low (about 17 liters). In comparison with the hepatic blood flow (about 30 l / h), the plasma clearance of valsartan occurs relatively slowly (about 2 l / h).
The amount of valsartan that is excreted with feces is 70% (of the amount taken internally in the dose).
With urine output is about 30%, mostly in unchanged form.
Pharmacokinetics in selected groups of patients

Elderly patients

In some elderly patients, the systemic effect of valsartan was somewhat more pronounced than in young patients, however, no clinical significance of this was shown.

Patients with impaired renal function

There was no correlation between renal function and systemic exposure to valsartan, which was to be expected, given that for this substance, the kidney clearance is only 30% of the total clearance value.
Therefore, in patients with impaired renal function, dose adjustment is not required. However, valsartan has a high degree of binding to blood plasma proteins, so its elimination in hemodialysis is unlikely.
Patients with impaired hepatic function

About 70% of the amount absorbed dose of the drug is excreted with bile, mostly unchanged.
Valsartan does not undergo significant biotransformation, and, as can be expected, systemic exposure to valsartan does not correlate with the degree of hepatic impairment. Therefore, in patients with hepatic insufficiency of non-biliary origin and in the absence of cholestasis, no adjustment of the dose of the drug is required.
INDICATIONS

- arterial hypertension;

- chronic heart failure (II-IV functional class according to NYHA classification) in patients receiving standard therapy, incl.
diuretics, digitalis preparations, as well as ACE inhibitors or beta-blockers (not simultaneously). The use of each of these drugs is not mandatory.
DOSING MODE

Take the tablets inside without chewing, regardless of food intake.

With arterial hypertension

The recommended dose is 80 mg 1 time / day.
Antihypertensive effect develops within 2 weeks of treatment; The maximum effect is observed after 4 weeks. Those patients who can not achieve an adequate reduction in blood pressure, a daily dose can be increased to 160 mg or additionally prescribed diuretic drugs. The maximum daily dose is 320 mg.
Patients with impaired renal function or patients with hepatic impairment not accompanied by cholestasis do not need to change the dose of the drug.

Valsafors can also be administered in conjunction with other antihypertensive agents.

With chronic heart failure

The recommended initial dose is 40 mg 2 times / day.
It is possible to gradually increase the dose to 80 mg 2 times / day, with good tolerability - up to 160 mg 2 times / day. The maximum daily dose is 320 mg divided into 2 doses.
In patients who are simultaneously receiving diuretics, as well as in patients with chronic heart failure, regular monitoring of kidney function is necessary.
At the appearance of clinical signs of arterial hypotension, it is necessary to reduce the dose.
SIDE EFFECT

From the side of the central nervous system: often - headache, dizziness, incl.
postural, vertigo; infrequently - insomnia; sometimes - a syncope (at application after the transferred myocardial infarction).
On the part of the respiratory system: often - cough, upper respiratory tract infections, pharyngitis, rhinitis, sinusitis.

From the side of the cardiovascular system: often - a pronounced decrease in blood pressure and orthostatic hypotension;
sometimes (when used after a heart attack) - heart failure.
From the gastrointestinal tract: often - nausea, diarrhea, abdominal pain.

From the skin and subcutaneous fat: rarely - skin rash.

From the osteomuscular system: often - back pain, myalgia, arthralgia.

From the genitourinary system: infrequently - decreased libido;
very rarely - renal dysfunction.
Allergic reactions: very rarely - angioedema, skin rash, itching, hypersensitivity reactions, including serum sickness and vasculitis.

On the part of laboratory parameters: rarely - decrease in hemoglobin and hematocrit concentration, neutropenia, thrombocytopenia, hypercreatininemia, hyperbilirubinemia, increased activity of hepatic transaminases, increased serum urea nitrogen;
often - hyperkalemia.
Other: often - general weakness;
infrequently - edema, asthenia, increased fatigue.
CONTRAINDICATIONS

- hypersensitivity to any of the components of the drug;

- Pregnancy;

- lactation period;

- age under 18 years (efficiency and safety not established).

With caution: bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney, while observing a diet with sodium restriction, in conditions accompanied by a decrease in bcc (including diarrhea, vomiting), hepatic insufficiency against bile duct obstruction, renal failure 10 ml / min), hemodialysis, chronic heart failure.

PREGNANCY AND LACTATION

The drug is contraindicated for use in pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

Patients with impaired renal function do not need a dose adjustment.
However, with severe disorders (CC less than 10 ml / min), caution is recommended.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Patients with hepatic insufficiency do not need a dose adjustment.
Valsartan is excreted mainly unchanged with bile, but in patients with bile duct obstruction, valsartan clearance is reduced. When prescribing the drug, these patients should be very careful.
APPLICATION FOR CHILDREN

Contraindicated in children and adolescents under 18 years.

SPECIAL INSTRUCTIONS

Deficiency in the body of sodium and / or reduced BCC

In patients with severe sodium deficiency and / or reduced bcc, for example, receiving high doses of diuretics, in rare cases, clinically pronounced arterial hypotension may occur at the onset of Valsafors treatment.

Before the start of treatment should be corrected content in the body of sodium and / or BCC, for example, by reducing the dose of the diuretic.
In case of development of arterial hypotension, the patient should be laid on his back, and, if necessary, an intravenous infusion of physiological solution. After the BP stabilizes, the treatment can be continued.
Stenosis of the renal artery

Given that other drugs that affect RAAS can cause an increase in serum urea and creatinine levels in patients with bilateral or unilateral renal artery stenosis, a systematic monitoring of these indicators is recommended as a precautionary measure.

Renal impairment

Patients with impaired renal function do not need to adjust the dose of the drug.
However, with severe disorders (CC less than 10 ml / min), caution is recommended.
Dysfunction of the liver

Patients with hepatic insufficiency do not need to adjust the dose of the drug.
Valsartan is excreted mainly unchanged with bile, but in patients with bile duct obstruction, valsartan clearance is reduced. When prescribing the drug, these patients should be very careful.
Chronic heart failure

Due to oppression of RAAS in sensitive patients, changes in renal function are possible.
In patients with severe chronic heart failure, treatment with ACE inhibitors and angiotensin receptor antagonists may be accompanied by oliguria and / or augmentation of azotemia and (rarely) acute renal failure and / or fatal. Therefore, it is necessary to assess the degree of impaired renal function in patients with heart failure.
Influence on ability to drive a car and work with mechanisms

When appointing Valsafors, as well as other antihypertensive drugs, it is recommended to use caution when driving a car and controlling mechanisms that require increased attention and speed of psychomotor reactions.

OVERDOSE

Symptoms: marked decrease in blood pressure.

Treatment: if the drug has been taken recently, you should induce vomiting.
With a pronounced decrease in blood pressure, the intravenous administration of physiological saline is initiated. It is unlikely that valsartan can be removed from the body by hemodialysis.
DRUG INTERACTION

Clinically significant interactions with such drugs as cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine and glibenclamide have not been identified.

Since valsartan is not subjected to any significant metabolism, it is unlikely that clinically significant interactions with other drugs at the metabolic level that result from induction or inhibition of the cytochrome P450 system.

Despite the fact that valsartan is largely bound to blood plasma proteins, no significant interaction with diclofenac, furosemide and warfarin has been revealed.

Simultaneous use with potassium-sparing diuretics (eg, spironolactone, triamterene, amiloride), potassium or potassium-containing salts, can lead to an increase in potassium concentration in the blood serum.
If such combination treatment is considered necessary, care should be taken.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. Store in a dry place, protected from light and out of the reach of children, at a temperature of no higher than 25 ° C.
Shelf life - 2 years. Do not use after the expiration date printed on the package.
Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Rambler's Top100
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!