Irbesartan

Chemical name

2-Бутил-3-[[2'-(1H-тетразол -5-ил)[1,1'-бифенил]-4-ил]м��тил]-1,3-диазаспиро[4.4]н он-1-ен-4-он (as potassium salt)

Gross

C25-H28-N6-O

Characteristics

White or almost white crystalline powder. It is soluble in ethanol and metilenhloride, nerastvorim in water.

Of drugs

Drugs, the antihypertensive. Vsokospecificno and irreversibly blocks receptors angiotenzina II (AT_1 subtype). Alleviate sossoudossouerveshchee the angiotenzina II, lowers the concentration of aldosterone plasma, reduces round, postnagruzku on the heart, AD system and the pressure on a small range of diseases. No impact on kinazu II (ACE), destroyed bradikinin and participating in education angiotenzina II. There is, after receiving a single maximum impact made through 3-6 hours Gipotenzivne effect lasted for 24 hours If the product is used regularly for 1-2 weeks is the effect of sustainability and four to six weeks is Maximuma.bystro and completely absorbed from the digestive tract, speed technique does not depend on the meals. Bioavailability - 60-80%, C_max defined in 1.5-2 hours Between dose of the drug and its concentration in the blood, there is a linear relationship (in the range of doses of 10-600 mg). Equilibrium concentration in the plasma is achieved within 3 days after the start of treatment. Linking plasma protein-96% of the K-l, the total Cl-spouses ml / min, kidney Cl - 3-3.5 ml / min. Treated biotransformation in the liver by oxidation with zitohroma P450 2S9 and subsequent conjugation with the formation of active metabolites, the main of which is irbesartan glukuronid (6%). T_1/2 - 11-15 h. Excreted kidneys (20%, of which less than 2% in an unmodified form) and Pechenew.wvedenie animals (rats, macaques) in the high dose (500 mg / kg / day) accompanied by the development of degenerative changes in the kidneys (intersticialny jade, tubulyarnoe expansion and / or infiltration bazofilnaya kidney channel, increasing the concentration of uric acid and creatinine plasma), and decreased renal white. The amounts in excess of 90 mg / kg / day (rats) and 110 mg / kg / day (houses), produces гипертрофию/гиперпла��ию ukstaglomeruliarnah Kletok.v a long (2 years) of the experimental animals in doses exceeding MRDC, and only three times (male rats), 3-5 times (male and female mice) and 21 times (male rats) cancer is not detected. In examining other specific toxicity mutagennaya and tertogennaya activity is not identified.

Indications

Arterial hypertension.

Restrictions on the use of

Children's age (safety and efficacy of the children are not identified).

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 :> 1% headache, dizziness, fatigue, the тревоги/возбудимости. Со the circulatory system and blood (blood, gemostaz) :> 1% Tahikardia.so the respiratory system :> 1% infection upper respiratory tract (high body temperature, etc.), sinusopatia, sinusit, pharyngitis, rhinitis, Kashel.so part of the intestine :> 1% diarrhoea, nausea, vomiting, diarrhoea phenomenon Izjoga.so the musculoskeletal system : > 1% musculoskeletal pain (including mialgia, pain in the bones, in the chest). Allergic reactions : :> 1% Sapi.prochie :> 1% pain in the abdominal cavity infection urinary tract.

Patient interaction

Tiazidnye dioretiki added effect. Compatible with other hypotensive Programme (beta-adrenoblokatora, calcium blockers channels), digoxinom, zimetidine. It increases the risk of giperkaliemii co applied kalisberegatmi dioretikami drugs and potassium.

Overdosing

Symptoms : arterial gipotenzia, tachycardia, or (more rarely) Bradikardia.lechenie : induction vomiting and / or stomach wash, the appointment of activated carbon symptomatic therapy; Hepatology ineffective.

Precautions

To use caution in patients with giponatriemiei (dioretikami treatment, restriction of salt diet, diarrhoea, vomiting), in patients in gemodialise (perhaps symptomatic of hypotension), as well as with the dehydrated patients. There is a need to proceed with caution in patients with hypertension renovskularna caused by stenosis bilateral renal artery stenosis or renal artery only kidney (increased risk of severe hypotension and renal failure), or aortalnam mitralnam stenosis, obstructive gipertroficescoy cardiomiopatiei, severe heart failure, and ischemic heart disease (increased risk of myocardial infarction, stroke). Against the backdrop of the kidneys to monitor levels of potassium and creatinine serum. Is not recommended for patients with primary гиперальдостеронизмо м.

Dosing and Administration

Inside, regardless of the meal, once a day, starting and supporting dose is 150 mg (if necessary - 300 mg / day). For patients with gemodialise and patients over 75 initial dose of 75 mg.

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