Vazotenz

General characteristics. Structure:

Active agents:
Active agent of a lozartan of potassium: 12,5 mg, 25 mg, 50 mg and 100 mg.
Excipients: Mannitolum, cellulose microcrystallic, croscarmellose sodium, K-30 povidone, magnesium stearate, gipromelloza 6, titanium dioxide (Е 171), magnesium hydrosilicate (talc), propylene glycol.

Description. Round (for tablets with a dosage of 100 mg - oval) biconvex tablets, white color, coated, with designation on the one hand "1L" (for tablets with a dosage of 12,5 mg), "2L" (for tablets with a dosage of 25 mg), "3L" (for tablets with a dosage of 50 mg) and "4L" (for tablets with a dosage of 100 mg). Tablets of 50 mg with risks on both sides and side risks.

Pharmacological properties:

Pharmacodynamics. Hypotensive drug, is a specific antagonist of receptors of angiotensin II (AT1 subtype). Does not suppress a kinase of II - the enzyme destroying bradykinin. Reduces the general peripheric vascular resistance (GPVR), concentration in blood of adrenaline and Aldosteronum, the arterial pressure (AP), pressure in a small circle of blood circulation; reduces an afterload, renders diuretic effect. Interferes with development of a hypertrophy of a myocardium, increases tolerance to an exercise stress at patients with heart failure.

After a single dose hypotensive action (the ABP decreases systolic and diastolic) reaches a maximum in 6 hours, then during 24 h gradually decreases.

The maximum hypotensive effect is reached in 3-6 weeks after the beginning of administration of drug.

Pharmacological data indicate that concentration of a lozartan in a blood plasma at patients with cirrhosis considerably increases therefore patients with liver diseases in the anamnesis should apply in lower dose.

Pharmacokinetics. Lozartan is quickly absorbed from digestive tract. Bioavailability - about 33%. Has effect of "the first passing" through a liver; it is metabolized by a carboxylation with the participation of an isoenzyme 2C9 of P450 cytochrome with formation of an active metabolite. Communication with proteins of a blood plasma - 99%.

Time of achievement of the maximum concentration of a lozartan makes 1 hour, an active metabolite 3-4 hours, after intake. Elimination half-life of 1,5 - 2 h, and its main metabolite of 6-9 h, respectively. About 35% of a dose are removed with urine, about 60% - through intestines.

Indications to use:

- Arterial hypertension;
- Chronic heart failure (as a part of a combination therapy, at intolerance or inefficiency of therapy by APF inhibitors).

Route of administration and doses:

Vazotenz accept inside, regardless of meal, frequency rate of reception - 1 time a day.

At arterial hypertension the average daily dose makes 50 mg. In some cases for achievement of bigger effect the dose is increased to 100 mg in two steps or once a day.

The initial dose for patients with heart failure makes 12,5 mg of 1 times a day. As a rule, the dose increases with a week interval (i.e. 12,5 mg/days, 25mg/days and 50 mg/days) to an average maintenance dose of 50 mg of 1 times a day depending on portability of drug the patient.

At purpose of drug the patients receiving diuretics in high doses Vazotenz should lower an initial dose of drug to 25 mg of 1 times a day.

Patients with abnormal liver functions should appoint lower doses of Vazotenz.

Patients of advanced age, and also at patients with renal failures, including patients on dialysis, have no need for correction of an initial dose.

Use in pediatrics
Safety and efficiency of drug at children are not established.

Features of use:

It is necessary to carry out correction of dehydration to purpose of drug Vazotenz or to begin treatment with use of drug in lower dose.

The drugs making impact on a renin-angiotenzinovuyu system can increase concentration of urea in blood and serumal creatinine at patients with a bilateral renal stenosis or a stenosis of an artery of the only kidney.

During treatment it is regularly necessary to control potassium concentration in blood, especially at patients of advanced age, at renal failures.

Pregnancy and period of a lactation
There are no data on use of a lozartan at pregnancy. However, it is known that the drugs influencing directly system a renin angiotensin at their use in II and III trimesters of pregnancy, can cause defect unless Tia or even death of the developing fruit. Therefore at pregnancy emergence Vazotenz's reception should be stopped immediately.
At appointment in the period of a lactation it is necessary to make the decision on the termination of breastfeeding or on the termination of treatment by Vazotenz.

Side effects:

* Side effects which frequency of development is comparable to placebo are marked. Communication of the side effects meeting with frequency less than 1% of cases using a lozartan is not proved.

In most cases Vazotenz is well had, side effects have passing character and do not demand drug withdrawal.

From a nervous system and sense bodys: 1% and more - dizziness, an adynamy, a headache, fatigue, sleeplessness; less than 1% - concern, a sleep disorder, drowsiness, dysmnesias, peripheral neuropathy, paresthesias, giposteziya, migraine, a tremor, an ataxy, a depression, a syncope, a ring in ears, taste disturbance, sight change, conjunctivitis.

From respiratory system: 1% and more - a nose congestion, cough *, upper respiratory tract infections (the increased body temperature, a pharyngalgia, a sinusopatiya *, sinusitis, pharyngitis), less than 1% - диспноэ, bronchitis, rhinitis.

From bodies of digestive tract: 1% and more - nausea, diarrhea *, the dispeptic phenomena *, an abdominal pain; less than 1% - anorexia, dryness in a mouth, a dentagra, vomiting, a meteorism, gastritis, a lock.

From a musculoskeletal system: 1% and more - spasms, a mialgiya *, a dorsodynia, a thorax, legs; less than 1% - an arthralgia, shoulder, knee pain, arthritis, fibromyalgia.

From cardiovascular system: orthostatic hypotension (dozozavisimy). heartbeat, takhi-or bradycardia, arrhythmias, stenocardia, anemia.

From urinogenital system: less than 1% - imperative desires on an urination, infections of urinary tract, a renal failure, weakening of a libido, impotence.

From integuments: less than I % - a xeroderma, an erythema, rush of blood, a photosensitization, the increased sweating, an alopecia.

Allergic reactions: less than 1% - urticaria, rash, an itch, a Quincke's disease, including persons, lips, a throat and/or language.

Others: hyperpotassemia (serum potassium more than 5,5 mmol/l).

Interaction with other medicines:

It can be appointed with other antihypertensives.

Clinically significant interaction with Hydrochlorthiazidum, digoxin, indirect anticoagulants, Cimetidinum, phenobarbital is noted.

Patients with dehydration (the previous treatment by high doses of diuretics) can have an expressed decrease in the ABP.

Strengthens (mutually) effect of other antihypertensives (diuretic, β-adrenoblockers, sympatholytics).

Increases risk of a hyperpotassemia at combined use with kaliysberegayushchy diuretics and drugs of potassium.

Contraindications:

- Hypersensitivity to drug components;
- Arterial hypotension;
- Hyperpotassemia;
- Dehydration;
- Pregnancy and period of a lactation;
- Age up to 18 years (efficiency and safety are not established).
With care: liver failure.

Overdose:

Symptoms: the expressed lowering of arterial pressure, tachycardia, because of parasympathetic (vagal) stimulation can develop bradycardia.
Treatment: artificial diuresis, symptomatic therapy; the hemodialysis is inefficient.

Storage conditions:

At a temperature not above 30 °C. To store in the place, unavailable to children! Period of validity 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated on 12,5 mg, 25 mg, 50 mg and 100 mg.

On 7, 10 or 14 tablets in the blister. On 2, 4 blisters on 7 tablets, on 1, 3 blisters on 10 tablets or on 1, 2 blisters on 14 tablets together with the application instruction in a cardboard pack.

On 10, 30 or 60 blisters together with application instructions in a cardboard box (for hospitals).