Valsartan

Chemical name

N-[п-(о-1Н-Тетразол-5-илф��нил)бензил]-N-валерил-L -валин

Gross

C24-H29-N5-O3

Characteristics

White or almost white powder. Rat in ethanol and methanol, little soluble in water.

Of drugs

Drugs, the antihypertensive. Competitive blocking receptors angiotenzina II (subtype AT_1) located in the blood vessels, heart, kidneys, brain, lungs and napochechnikov crust. Suppress all indirectly through AT_1 receptors effects angiotenzina II, including vazokonstricciu and aldosterone secretion. Decreases heart enlargement in patients with arterial hypertension. No impact on the total cholesterol, triglycerides, glucose and uric кислоты.Антигипертен��ивный effect develops within 2 h after administration of a single dose reaches its peak four to six hours and lasts for up to 24 hours The regular use of permanent decline in AD is 2-4 Ned.bystro drawn from the blood. Bioavailability of 35% (average 25%). C_max is 2-4 hours Away reduces AUC by 40% and C_max 50% without altering effectiveness. Linking plasma proteins (mostly albuminom) 94-97%. The distribution-17 litres. A small percentage (20%) biotransformiroetsa education inactive metabolita (valeril hydroxy valsartan) and the bulk-excreted unchanged to mostly with the faeces (70%) and urine (30%). T_1/2 about 9 C.auc and C_max increase in patients older age (over 65 years) to 70% and 35% Sootvetstvenno.v experimental studies in mice and rats was not carcinogenic action in a 24 months in doses up to 160 (mouse), and up to 200 mg / kg / day (rats), which corresponds to 2.6 and 6 MRDC. The male and female rats (up to 200 mg / kg / day inside) adverse actions on the reproductive function is not supported. Mutagenic properties valsartan have been detected.

Indications

Arterial hypertension.

Restrictions on the use of

Children's age (the effectiveness and safety of the children have not been established).

Pregnancy and lactation

Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, pregnancy, breast-feeding.

Side-Effects

From the nervous system and sensory organs : seldom-weakness, headache, Golovokrugenie.so part of the intestine : rarely diarrhoea, nausea, abdominalnaya pain, increase in liver Transaminaz.so the circulatory system and blood (blood, gemostaz) : rarely neutropenia (1.9%), anemia, a decline Gematokrita.prochie : rarely cough, giperkaliemia, viral infection.

Patient interaction

Do (mutually) gipotenzivny dioretikov effect. Kalisberegate dioretiki, as well as preparations containing potassium, increase the risk giperkaliemii.

Overdosing

Symptoms : gipotenzia, tachycardia or Bradikardia.lechenie : symptomatic therapy; Dialysis ineffective.

Precautions

Caution must be exercised in the appointment of people with a deficit of sodium and / or BCC (due to increased risk of excessive arterial hypotension), the stenosis bilateralnam renal artery stenosis or renal artery only kidney (a control of creatinine and urea nitrogen in serum), with the expressed impaired kidney (Cl creatinine less than 10 ml / min) Heavy impaired liver cirrhosis biliarian, obstruction psoriasis ways if it is accompanied by a kalisberegath dioretikov, drugs or potassium kalisoderjath additives. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention.

Dosing and Administration

Inside, 80 mg once a day; With inefficiency can increase dose to 160 mg or more a more antigipertenzivnogo product (eg dioretika).

Literature

1. Markham A., K. Goa Valsartan. A review of its pharmacology and therapeutic use in essential hypertension / / Drugs - 1997 .- V. 54 N-2-P. 299-311.2. Thurmann P. Angiotensin II antagonism and the heart : valsartan in left ventricular hypertrophy / / J. Cardiovasc. Pharmacol 1999 .- .- V. 33-N-1 P. 33-36.

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