Valsacor

616 8 minutes read

Active material: Valsartan
When ATH: C09CA03
CCF: Angiotensin II receptor antagonists
ICD-10 codes (testimony): I10, I50.0
When CSF: 01.04.02
Manufacturer: KRKA d.d. (Slovenia)

DOSAGE FORM, COMPOSITION AND PACKAGING

Pills, Film-coated brown-yellow, round, slightly biconcave, with Valium on one side.

	1 tab.
valsartan *	40 mg

Excipients: lactose monohydrate, microcrystalline cellulose, povidone, Croscarmellose sodium, Colloidal anhydrous silica, magnesium stearate.

The composition of the shell: gipromelloza, Titanium dioxide (E171), dye iron oxide yellow (E172), macrogol 4000.

7 PC. – blisters (2) – packs cardboard.
7 PC. – blisters (4) – packs cardboard.
7 PC. – blisters (20) – packs cardboard.
7 PC. – blisters (80) – packs cardboard.
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (20) – packs cardboard.
10 PC. – blisters (50) – packs cardboard.
14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
14 PC. – blisters (10) – packs cardboard.
14 PC. – blisters (40) – packs cardboard.

Pills, Film-coated Pink colour, round, lenticular, with Valium on one side.

	1 tab.
valsartan *	80 mg

Excipients: lactose monohydrate, microcrystalline cellulose, povidone, Croscarmellose sodium, Colloidal anhydrous silica, magnesium stearate.

The composition of the shell: gipromelloza, Titanium dioxide (E171), iron oxide red dye (E172), macrogol 4000.

Pills, Film-coated brown-yellow, Oval, lenticular, with Valium on one side.

	1 tab.
valsartan *	160 mg

Excipients: lactose monohydrate, microcrystalline cellulose, povidone, Croscarmellose sodium, Colloidal anhydrous silica, magnesium stearate.

The composition of the shell: gipromelloza, Titanium dioxide (E171), dye iron oxide yellow (E172), iron oxide red dye (E172), macrogol 4000.

* international non-proprietary name, recommended by the WHO – valzartan.

Pharmacological action

Angiotensin II receptor antagonists.

Valsartan is an Angiotensin II receptor antagonist selective (AT type₁) orally, non-protein nature.

Provides selective antagonistic effect on the receptor subtype AL₁. A consequence of the blockade AT₁-receptors is increased plasma concentration of angiotensin II, that can stimulate the receptor subtype unlocked AL₂, that allegedly regulates the effects AT₁-receptors. Valsartan does not have aktavnosti against agonisticheskoj AT₁-receptors. His affinity for the receptor subtype AT₁ about 20 000 times higher, receptor subtypes than AT₂.

Valsartan does not inhibit ACE, also known as the kininazy II, which converts angiotensin I to Angiotensin II and bradykinin. Due to the lack of effect on ENZYME, not potencirujutsja effects of bradykinin and substance p, Therefore, when taking Angiotensin II antagonists are unlikely to develop dry cough. Valsartan does not interact and does not block other hormone receptors or ion channels, involved in the regulation of cardiovascular functions.

When treating hypertension valsartan reduces ad, without affecting HEART RATE.

After ingestion of a single dose of the drug antigipertenzivny effect develops over 2 no, and the maximum reduction of HELL is achieved within 4-6 no. Antigipertenzivny effect drug lasts for 24 hours after his admission. The reappointments valsartan maximum reduction of HELL, regardless of the dose, achieved through 2-4 week and is supported on the achieved level in the course of long-term therapy. Combination with hydrochlorthiazide achieves significant additional decline AD.

Sudden cessation of receiving valsartan has not been accompanied by a sharp rise of hell or other undesirable clinical effects.

Tolerance to physical activity

When evaluating the effect of valsartan (naznachavshegosja in addition to the standard therapy for heart failure) the portability physical activity in patients with chronic heart failure functional class II-IV NYHA classification and with left ventricular ejection fraction (LVEF) <40% There has been an increase in the time physical activity compared to benchmarks.

Missing syndrome “cancel” with a sudden admission.

Pharmacokinetics

Absorption

Valsartan is rapidly absorbed after administration inwards, However, the extent of absorption varies widely. When receiving valsartan with food decreases the AUC on 48%. Nonetheless, through 8 h after administration of the drug plasma concentrations of valsartan, taken on an empty stomach and with food, the same. Reduction in AUC is not accompanied by a clinically significant decrease in therapeutic effect of valsartan, the product can be used to, and after eating.

The average absolute bioavailability of valsartan is 23%. T_maxsostavljaet2 h. Plasma concentrations of valsartan are the same for men and women.

After the regular admission maximum decline ad comes through 4 of the week.

Distribution

Serum protein binding, mainly with serum albumin, is 94-97%. V_d about 17 l. Before the drug 1 times/day accumulation it slightly.

Metabolism

Plasma clearance of relatively low – about 2 l/h when compared to hepatic blood flow – about 30 l /. Metabolized by CYP2C9 izofermentom valsartan.

Deduction

T_1/2 is 9 no. Excreted in the feces 70%, urine – 30% (mainly unchanged) valsartan on inside dosage.

Pharmacokinetics in special clinical situations

Considering, that kidney klirens is only 30% the size of the total ground clearance, in patients with impaired renal function is not required correction doses of the drug. Since the degree of binding of valsartan with plasma protein high, its excretion in gemodialise unlikely.

About 70% vsosavshejsja doses of valsartan appears to jelchew, predominantly, in unchanged form. Valsartan is not exposed to significant biotransformation, so his system action does not correlate with the degree of liver.

Therefore, in patients with hepatic insufficiency nebiliarnogo origin and, in the absence of cholestasis is not required to change the dose of valsartan.

In patients with biliarnym cirrhosis of the liver or biliary obstruction AUC valsartan increases approximately 2 times.

Testimony

- Arterial hypertension;

- Congestive heart failure (II-IV functional class NYHA classification) in the complex therapy (against a background of standard therapy) and patients, not receiving ACE inhibitors.

Dosage regimen

The drug should be taken inside, regardless of meals, the reception frequency is 1-2 times / day.

When hypertension

The recommended dose is 80 mg 1 time / day, irrespective of age, patient's gender or race. The maximum daily dose – 320 mg / day.

Antigipertenzivny effect develops over 2 weeks and reaches its peak in 4 of the week. Possible to combine with other hypotensive drugs.

For patients with compromised renal function and liver nebiliarnogo of origin and without cholestasis no changes are required doses.

In chronic heart failure

The recommended starting dose is 40 mg 2 times / day. A gradual increase in dose to 80 mg, with good endurance – to 160 mg 2 times / day, ie. up to a maximum dose of, portable patient. The maximum daily dose – 320 mg 2 times / day.

Patients, at the same time receiving dioretiki, as well as in patients with heart failure requires permanent monitoring of the kidneys, FROM. With the appearance of clinical signs of arterial hypotension, It is necessary to reduce the dose.

Side effect

From the central and peripheral nervous system: often – headache, dizziness (incl. postural), vertigo; sometimes – insomnia, fainting (in applying the drug post-myocardial infarction).

The respiratory system: often – cough, infections of the upper respiratory tract, pharyngitis, rhinitis, sinusitis.

Cardio-vascular system; often – marked reduction in blood pressure, orthostatic hypotension; sometimes – heart failure (in applying the drug post-myocardial infarction).

From the digestive system: often – nausea, diarrhea, abdominal pain.

On the part of the musculoskeletal system: often – backache, myalgia. arthralgia.

From the urinary system: rarely – impairment of renal function.

Reproductive system: sometimes – decreased libido.

By the laboratory parameters: often – hyperkalemia; rarely – reduction of the concentration of hemoglobin and hematocrit, neutropenia, thrombocytopenia, giperkreatininemiя, giperʙiliruʙinemija, increase in liver transaminases, increased serum urea nitrogen.

Allergic reactions: rarely – angioedema, skin rash, itching, hypersensitivity reactions (incl. serum sickness, vasculitis).

Other: often – generalized weakness; sometimes – swelling, asthenia, fatigue.

Contraindications

- Lactose intolerance, galactosemia or syndrome of impaired glucose/Galactose malabsorption;

- Pregnancy;

- Lactation;

- Childhood and adolescence up 18 years (the efficacy and safety of valsartan in children has not been proved);

-hypersensitivity to valsartanu or to other components of the drug.

FROM caution use in patients with hypotension, hepatic insufficiency on the background of biliary tract obstruction, renal failure (CC<10 ml / min), incl. patients, hemodialysis, when hyponatremia, diet with restriction of sodium intake, bilateral renal artery stenosis or stenosis of the artery to a solitary kidney, states, accompanied by a decrease in the bcc (incl. diarrhea, vomiting).

Pregnancy and lactation

Data on the use of valsartan in pregnancy is not.

Fetal renal perfusion, which depends on the development of the renin-angiotensin system, begins to function in the III trimester of pregnancy. The risk to the fetus increases when taking valsartan in II and III trimestrah. When establishing pregnancy valsartanom therapy should be immediately discontinued.

Unknown, is allocated whether valsartan with breast milk. Therefore, you should decide on the termination of breastfeeding or the abolition of valsartanom therapy in view of its importance for the mother.

If necessary, the use of the drug during lactation should decide on the termination of breastfeeding or the abolition of valsartanom therapy in view of its importance for the mother.

Cautions

Heart failure

Use in patients with heart failure is usually accompanied by a decline in AD, However, compliance with the recommendations for the selection of doses of treatment rarely requires cancellation due to arterial hypotension. Val'sakorom therapy in patients with heart failure should begin carefully. As a consequence of the Suppression of Renin-angiotensin-aldosterone system activity in some patients it is possible to change the functions of the kidneys.

In severe heart failure may develop oliguria and/or progressive азотемии until (rarely) acute renal failure and/or death. In patients with heart failure requires permanent monitoring of the kidneys while appointing a combination of three classes of drugs – ACE inhibitors, Beta blockers and Angiotensin II receptor antagonists AB₁.

The appointment in combination with other drugs, appointed post-myocardial infarction: thrombolytics, acetylsalicylic acid, Beta-adrenoblokatora and Statins.

A deficiency of sodium and/or fluid

In patients with a marked deficiency in the body of sodium and/or reduced BCC, eg, as a result of receiving large doses of diuretics, in rare cases at the beginning of therapy, valsartanom can develop expressed arterial gipotenzia. Before starting treatment Val'sakorom recommended restore electrolytes and fluids in the body, in particular, by reducing the doses of diuretics.

With the development of arterial hypotension with clinical manifestations: the patient must lay on your back and if necessary/in enter 0.9% sodium chloride solution. Val'sakorom therapy can continue only after stabilization AD indicators.

Renal artery stenosis

In patients with unilateral or bilateral renal artery stenosis must continuously monitor the contents of creatinine and urea nitrogen in serum.

Impaired renal function

In patients with the human kidney dose change is not required. Due to the lack of data on the use of drugs in severe renal failure (CC<10 mL/min or 0.167 ml / s) in such cases, the drug should appoint with caution.

Abnormal liver function

In patients with impaired liver does not require dose changes.

Write mainly jelchew Val'sakor. In patients with obstructive biliary disease decreased clearance of valsartan, in such cases, therefore, the drug should be administered with caution.

Special information for excipients

Val'sakor contains lactose, Therefore, the drug is contraindicated in patients with a deficiency of lactase, galaktozemiej syndrome or broken intake of glucose-Galactose.

Effects on ability to drive vehicles and management mechanisms

Patients should use caution when driving and other mechanisms, require attention.

Overdose

Symptoms: data on effects of valsartan overdose missing. The main expected manifestation of drug overdose is expressed lower ad, that could lead to the collapse and/or shock.

Treatment: symptomatic, It is recommended to cause vomiting and stomach wash. With the development of arterial hypotension in/in introducing 0.9% sodium chloride solution. Hemodialysis nyeeffyektivyen.

Drug Interactions

Clinically significant pharmacokinetic interaction Val'sakora with other drugs not noted.

Preparations, tested in clinical studies, included cimetidine, warfarin, Digoxin, atenolol, Indomethacin, gidroxlorotiazid, Amlodipine and glibenclamide.

Valsartan is not subjected to substantial because metabolism, don't expect and important drug interactions, associated with induction or inhibition of the cytochrome P450 system Isoenzymes.

Simultaneous application of kalisberegath dioretikov (incl. spironolactone, triamteren, amilorida), potassium-based nutritional supplements can lead to giperkaliemii, in linksto than required careful. The combined application with dioretikami may increase gipotenzivnogo effect.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 30 ° C. Shelf life – 2 year.

Vladimir Andreevich Didenko

616 8 minutes read