Telmisartan

Chemical name

4'-[[4-Метил-6-(1-метил-2-бе нзимидазолил)-2-пропил -1-бензимидазолил]мети л]-2-бифенил-карбонова�� acid

Gross

C33-H30-N4-O2

Characteristics

White or colourless crystalline powder odourless, virtually nerastvorim in water at pH from 3 to 9, partially soluble in strong acid (except salt), soluble in strong scheloch.

Of drugs

Drugs, the antihypertensive. Does receptors angiotenzina II (AT_1 subtype). Dozozawisimo ingibiruet pressornoe influence angiotenzina II, lowers the level of concentration in plasma increases diurez, excretion of sodium and chloride. Provides nefroproteguoe influence diminishes albuminurii level. At 10% fat lowers blood is not enough clubockovu filtering. In high doses, reduces the severity thyroid diseases. Patients arterial hypertension decreases as Sad, and Dad, without altering Css.horosho drawn from the blood. Absolute bioavailability of 60% (through economies of the first passage "through the liver). After receiving a single dose of 80 mg C_max achieved within 1 h. Intensive contacts with plasma proteins, mainly from albuminom and acid альфа_1-гликопротеино��. The evenly distributed in the body (which is highly lipofilen and easily penetrates the tissues), the distribution of 500 litres. Metabolised in the liver by kongugirovania with glukuronova acid, forming a stable atilglukuronid inactive, which is rapidly excreted from jelchew : in the faeces found about 85% of telmisartan unchanged and 11% glukuronida; Renal excretion is less than 2%. Return slowly T_1/2 is about 21 hours for men and 31 hours for women. Gipotenzia made through three hours after the intake of continuing more than 24 hours and off for a 4-8 week course of application. In a reception AD gradually (in a few days), returning to the original values without development "ricochetna" hypertension.

Indications

Arterial hypertension.

Restrictions on the use of

Children and adolescence (safety and efficacy of the use of children and teenagers to be determined).

Pregnancy and lactation

Contraindicated in pregnancy. The planned pregnancy recommended in the product antigipertenzive other means. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, obstruction of psoriasis, heavy human liver and kidneys, pregnancy, breast-feeding.

Side-Effects

From the nervous system and sensory organs :> 1% headache, Golovokrugenie.so part of the intestine :> 1% nausea, neuralgia, pain in the abdomen, Diarea.so the respiratory system :> 1% cough, pharyngitis, flu symptoms, reduced tolerance to infections upper respiratory Putei.prochie : > 1% pain in the chest and lower back, mialgia, infections urinary tract, lower hemoglobin content, increased uric acid.

Patient interaction

Hydrochlorothiazide increases (mutually) gipotenzivny effect. Together appointment ACE inhibitors, kalisberegath dioretikov and other drugs, can raise potassium levels in the plasma, as well as kalisoderjath food additives, especially in patients with renal insufficiency, and that the risk of giperkaliemii. Increases lithium concentration in the blood and C_max digoxin (20%).

Overdosing

Symptoms : Gipotenzia.lechenie : symptomatic and supportive therapy. Haemodialysis ineffective.

Precautions

Be wary appoint patients with symptomatic renovskularna hypertension caused by stenosis bilateral renal artery stenosis or renal artery only functioning kidney (it increases the risk of severe hypotension and renal failure). In patients with moderately impaired renal need regular monitoring of creatinine and electrolytes (potassium) in the plasma. Caution must be exercised in the appointment of people with low BCC and / or lack of sodium (for the treatment of dioretikami, a limited flow of salt, diarrhea, vomit), stenosis arteries and mitral valve with obstructive gipertroficescoy cardiomiopatiei, moderately impaired liver, severe heart failure (constant monitoring of potassium and creatinine in the serum) in the heart (possibly of acute coronary syndrome and myocardial infarction), ulcers or stomach duodenal ulcer in the process of being increased, or other diseases of the digestive tract (probably a gastrointestinal bleeding). Is not recommended in the primary aldosteronizme, congenital fruktozy intolerances (1 tablet 80 mg contains 338 mg electricity). Caution must be exercised to drivers of vehicles and people skills relate to the high concentration of attention. Together admission digoxin or preparations lithium requires monitoring of their content in the blood serum.

Dosing and Administration

Inside, regardless of mealtimes, 20-40 mg / day at a time, if necessary, up to 80 mg. In patients with moderately impaired liver daily dose should not exceed 40 mg.

Literature

Neutel JM, Smith D.H.G., P. Reilly The efficacy and safety of telmisartan compared to enalapril in patients with severe hypertension / / Int. J. Clin. Pract 1999-V-53-N 3 .- P. 1-4.

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