Eprosartan

Chemical name

(Е)-альфа-[[2-Бутил-1-[(4-к��рбоксифенил)метил]-1H-��мидазол-5-ил]метилен]-2 -тиофенпропановая acid

Gross

C23-H24-N2-O4-S

Characteristics

White or almost white bulk crystalline powder. Nerastvorim in water, it is readily soluble in ethanol.

Of drugs

Drugs, the antihypertensive. Does receptors angiotenzina II (subtype AT_1) in the blood vessels, heart, kidney and napochechnikov crust. Warn development or weakening effect angiotenzina II, stupid action ренин-ангиотензиново�� system. Decreases hypertension vazokonstricciu, round, the pressure on a small range of circulatory, reabsorbqiyu sodium and water in the proximal segment of kidney Channel, aldosterone secretion, gli, arginin-vazopressina. Does presinapticalkie AT_1 receptors sympathetic neurons in the CNS, oppressing release norarenalina and sympathetic stimulation. With long-term use ingibiruet proliferativee effects angiotenzina II in the heart cells and smooth muscle receptacles. Warn or to the opposite of thyroid diseases. Increases kidney bloodstream and reduces the excretion albuminates with urine (nefroproteguoe effect). Increases tolerance to physical activity in patients with heart failure. Do not alter the lipid, and carbohydrate purinovy exchange. Dozozawisimo reduces AD in 50-70% of patients with arterial hypertension I and II degrees. Antigipertenzivny effect after a single dose until 24 h, stabilizing with regular admission 2-3 Ned.ne fully absorbed from the digestive tract, bioavailability is 13%. In appointing prandial C_max achieved in 1-2 hours Getting food down and lost 25% less C_max plasma. Associated with the plasma protein by 99%. T_1/2 - 5-9 pm The distribution-13 litres, the total Cl-130 ml / min. Return with faeces (90%) and urine (7%, of which 20% of atilglukuronida). With long-term use koumouliruet. AUC and C_max increase in patients older twice with kidney failure at 30 (Cl creatinine 30-59 ml / min), 50% (Cl creatinine 5-29 ml / min); In the face of liver failure AUC increased by 40%.

Indications

Arterial hypertension.

Restrictions on the use of

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

Pregnancy and lactation

Contraindicated. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, pregnancy, breast-feeding.

Side-Effects

Headache, dizziness, weakness, diarrhoea, myalgia, rarely zagrudinnaya pain, shortness of breath, cough, angioneuroticeski swelling.

Patient interaction

Compatible with blokatorami calcium channel tiazidnami dioretikami (summation effects), lipid means.

Overdosing

Symptoms : arterial Gipotenzia.lechenie : symptomatic therapy.

Precautions

Be wary when using stenoze aortalni or mitral valve gipertroficescoy cardiomyopathy, ischemic heart disease, severe heart failure, bilateralnom stenoze renal arteries or stenoze renal artery single kidney, renal insufficiency (Cl creatinine less than 30 ml / min), giperkaliemii. There are encouraged to nominate patients with primary гиперальдостеронизмо м.

Dosing and Administration

Inside, regardless of the meals, 800 mg once a day (morning) for a period of two to three weeks. The maximum daily dose of 1200 mg.

Literature

1. Ohlstein E., P. Brooks, Feuerstein G.Z. et al. Inhibition of sympathetic outflow by the angiotensin II receptor antagonist, eprosartan, byt not losartan, valsartan or irbesartan : relationship to differences in prejunctional angiotensin II receptor blockade / / Pharmacology-1997 .- V. 55 .- P. 244-251.2. Willenheimer R., Dahluf B., Rydberg E. et al. AT_1-receptor blockers in hypertension and heart failure : clinical experience and future directions / / Eur. Heart J., 1999 .- V. 20 .- P. 997-1008.

Directory → Organotropona funds → Cardiovascular funds → Receptor antagonists angiotenzina II (At_1-podtip) → Eprosartan