Losartan

Chemical name

2-Бутил-4-хлор-1-[[2'-(1Н-те тразол-5-ил)[1,1'-бифенил ]-4-ил]-метил]-1Н- imidazol-5-metanol (as potassium salt)

Gross

C22-H23-Cl-N6-O

Characteristics

White or no white crystalline powder. It is soluble in water and not in the organic solvent (acetonitrile and methyl).

Of drugs

Drugs, the antihypertensive. Does receptors angiotenzina II (subtype AT_1) in a variety of tissues, including korkowoe napochechnikov substance, the brain, the kidneys, the liver, smooth muscles vessels, the heart and hinders the development effects angiotenzina II. Decreases hypertension vazokonstricciu, round, the pressure on a small number of blood circulation, reduces jamming pressure in the lung blood vessels and slows the release of aldosterone, warns delay sodium and water in the body. Increases tolerance to physical activity in patients with heart недостаточностью.Пос��е single admission gipotenzivne Effects (decrease Sad and Dad) reaches its maximum at 6 h and gradually (within 24 h) decreasing. Stable lowering AD, most of the patients have to 3-6-i week course Primenenia.v experiments on rats and mice, in the two years receiving the maximum dose carry (more than 200 mg / kg / day) cancer is not detected. However, the female rats showed a slight increase in the frequency of Adenomas atinusov pancreas. The studies in vitro and in vivo mutagenic properties can be found. Fertility and reproductive function of male rats receiving inside doses up to 150 mg / kg / day did not vary. When a breeding rats doses of 100 mg / kg / day and a reduction in the number of yellow bodies implants and Zarodyshei.bystro drawn from the blood. Low bioavailability (approximately 33%), as "first pass" through the liver lozartan is biotransformation by carbauxilirovania with zitohroma 2S9 P450 3A4 and with the formation of a metabolita in 10-40 times greater than the original substance. C_max achieved through 6.3.13 (lozartan) and 3-4 hour (the active metabolite), the plasma protein binds to 98.7% (lozartan), and 99.8% (metabolite), T_1/2 is 1.5-2 hours and 6-9 hours, respectively. In addition to active carboksiproizvodnyi formed several inactive metabolites. Excreted kidneys approximately 35% (4% in unmodified form, and about 6% of the active metabolita) with faeces-approximately 60%.

Indications

Arterial hypertension, chronic heart failure.

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.

Patient interaction

Do (mutually) effect etc. gipotenziveh funds (mochegonnah, beta-adrenoblokatorov, simpatolitikov). Increases risk giperkaliemii co applied kalisberegatmi dioretikami drugs and potassium.

Overdosing

Symptoms : gipotenzia, climate variation (tachycardia or aetiology caused either wandering nerve). Treatment : Forward diurez, symptomatic therapy. Haemodialysis ineffective.

Precautions

Patients with liver disease (especially with cirrhosis), incl. in history, it is necessary to appoint a smaller dose. Be wary when using stenoze bilateral renal arteries or stenoze renal artery only kidney (elevated risk of kidney function), with moderate to severe violation of kidney function, congestive heart failure in patients with dehydration (probably the symptomatic hypotension), or giponatriemiei.

Dosing and Administration

Inside, adults, regardless of the meal, every day. When hypertension is 50 mg, if necessary, to a gradual increase in dose (in some cases up to the maximum daily-100 mg), with the dehydration initial dose of 25 mg. In chronic heart failure, 12.5 mg, with a gradual increase in two phases (after one week up to 25 mg, and after one hour, 50 mg) to the normal maintenance dose of 50 mg.

Literature

1. Mareyev VY New advances in optimizing treatment for chronic heart недостаточности//Кард иология.- 1997 .- T. 37 N-12 - C. 4-9.2. Metelitsa VI Receptor blockers angiotenzina II / / Ter. archive-1996 .- T. 68 N-8 .- C. 64-67.3. A. Sidorenko, DV Preobrazhensky Lozartan - blokator At_1-angiotenzinovykh receptors : a new direction in the treatment of chronic heart недостаточности//Кард иология.- 1997 .- T. 37 N-10-C 84-87.4. Skvortsov AA, Mareyev VY, Yuri Belenkov Receptor blockers angiotenzina II (the act; First clinical результаты)//Кардиоло��ия.- 1998 .- T. 38 N-4 - C. 36-50.5. Conlin PR, Spence D., Williams B. et al. Angiotensin II antagonists for hypertension : Are there differences in efficacy? / / Am. J. Hypertens 2000 .- .- V. 1913-N4 (stay) .- P. 418-426.6. S. Oparil, E. Barr, M. Elkins et al. Efficacy, tolerability, and effects on quality of life of losartan, alone or with hydrochlorothiazide, versus amlodipine, alone or with hydrochlorothiazide, in patients with essential hypertension / / Clin. Ther-1996 .- V. 18-N 4 .- P. 608-625.

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