Lozartan

General characteristics. Structure:

Active ingredient: 50 mg or 100 mg of a lozartan in 1 tablet.

Anti-hypertensive drug.

Pharmacological properties:

Pharmacodynamics. Blocks angiotensin II receptors (AT1 subtype) in various fabrics, including cortical substance of adrenal glands, a brain, kidneys, a liver, smooth muscles of vessels, heart and interferes with development of effects of angiotensin II. Reduces arterial vasoconstriction, OPSS, pressure in a small circle of blood circulation, lowers jamming pressure in pulmonary vessels, slows down release of Aldosteronum, warns a delay of sodium and water in an organism. Increases tolerance to an exercise stress at patients with heart failure.

After a single dose hypotensive action (decrease the GARDEN and DAD) reaches a maximum in 6 h and gradually (during 24 h) decreases. Stable decrease in the ABP at most of patients is observed by 3-6th week of course use.

In experiences on the rats and mice, within 2 years receiving the most tolerable doses (more than 200 mg/kg/days) of cancerogenic action it is not revealed. However at females of rats some increase in frequency of development of adenomas of an acinus of a pancreas was revealed. In the researches in vitro and in vivo mutagen properties are not found. Fertility and reproductive function of males of the rats receiving up to 150 mg/kg/days in a dose did not change. At introduction to females of rats of doses of 100 mg/kg/days reduction of number of yellow bodies, implants and germs was also more observed.

Pharmacokinetics. It is quickly soaked up from a GIT. Bioavailability is small (about 33%) as at "the first passing" through a liver лозартан initial substance is exposed to biotransformation by a carboxylation with the participation of P450 2C9 and 3A4 cytochrome with formation of the main metabolite, in 10-40raz more active, than. Cmax is reached in 1 h (лозартан) and 3–4 h (an active metabolite), contact proteins of plasma for 98,7% (лозартан) and for 99,8% (metabolite), T1/2 makes 1,5–2 h and 6–9 h respectively. In addition to active carboxyderivative several inactive metabolites are formed. Kidneys excrete about 35% (from them 4% in not changed look and about 6% in the form of an active metabolite), with excrements — about 60%.

Indications to use:

Arterial hypertension; chronic heart failure (as a part of a combination therapy, at intolerance or inefficiency of therapy by APF inhibitors); decrease in risk of development of a stroke in patients with arterial hypertension and a hypertrophy of a left ventricle; protection of function of kidneys at patients with a diabetes mellitus of type 2 with a proteinuria for the purpose of decrease in a proteinuria, reduction of progressing of damage of kidneys, decrease in risk of development of an end-stage (prevention of need of carrying out dialysis, probability of increase in level of creatinine in blood serum).

Route of administration and doses:

Inside, the adult, irrespective of meal, 1 times a day.

At arterial hypertension — 50 mg, if necessary perhaps gradual increase in a dose (in some cases to maximum daily — 100 mg), against the background of dehydration an initial dose of 25 mg.

At chronic heart failure — 12,5 mg with a gradual uvelicheniyemv 2 stages (in 1 week — to 25 mg and in 1 week — 50 mg) to a usual maintenance dose of 50 mg.

Features of use:

Patients with liver pathology (especially at cirrhosis), including in the anamnesis, need to appoint smaller doses. With care apply at a bilateral stenosis of renal arteries or a renal artery stenosis of the only kidney (the risk of a renal failure is increased), at a moderate or heavy renal failure, congestive heart failure, at patients with dehydration (development of symptomatic hypotension is probable) or a hyponatremia.

Use at pregnancy and feeding by a breast. Contraindicated at pregnancy. Category of action on a fruit on FDA — C (the I trimester). Category of action on a fruit on FDA — D (II and III trimesters). For the period of treatment it is necessary to stop breastfeeding.

Side effects:

From a nervous system and sense bodys: ≥1% — dizziness, adynamy/exhaustion, a headache, sleeplessness;

From respiratory system: ≥1% — a nose congestion, cough, upper respiratory tract infections (the increased body temperature, a pharyngalgia, etc.), a sinusopatiya, sinusitis, pharyngitis;

From bodies of a GIT: ≥1% — nausea, diarrhea, the dispeptic phenomena, an abdominal pain;

From a musculoskeletal system: ≥1% — spasms, a mialgiya, a dorsodynia, a thorax, legs;

Others: ≥1% — a hyperpotassemia.

Interaction with other medicines:

Strengthens (mutually) effect of other antihypertensives (diuretics, beta adrenoblockers, sympatholytics). Increases risk of a hyperpotassemia at combined use with kaliysberegayushchy diuretics and drugs of potassium.

Any clinically significant medicinal interactions with a hydrochlorothiazide, digoxin, indirect anticoagulants, Cimetidinum, phenobarbital, ketokonazoly and erythromycin are noted. During a concomitant use with rifampicin and flukonazoly decrease in level of an active metabolite of a lozartan of potassium was noted. Clinical effects of this phenomenon are not known.

Contraindications:

Hypersensitivity, pregnancy, feeding by a breast.

Restrictions to use. Children's age (safety and efficiency of use for children are not defined).

Overdose:

Symptoms: hypotension, change of ChSS (the tachycardia or bradycardia caused by excitement of a vagus nerve).

Treatment: Artificial diuresis, symptomatic therapy. The hemodialysis is inefficient.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 50 mg and 100 mg. 10 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.