Bloktran ®

General characteristics. Structure:

Active agent: potassium of a lozartan of 50 mg

Excipients:

Kernel: sugar milk (lactose), cellulose microcrystallic, polyvinylpirrolidone low-molecular (povidone), potato starch, magnesium stearate for pharmaceutical industry, aerosil (silicon dioxide colloid).

Cover: a gidroksipropilmetiltsellyuloz (gipromelloz), кополивидон, titanium dioxide, talc, the twin-80 (polysorbate), sikovit yellow-orange 85 E 110.

Description
Round biconvex tablets, coated light pinkish-orange color.

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 resistance (OPSS), 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 develops 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 use drug 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 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:

The drug Bloktran® 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 is titrated with a week interval (i.e. 12,5 mg/days, 25 mg/days, 50 mg/days) to an average maintenance dose of 50 mg. 1 time a day depending on portability of drug the patient.

At purpose of drug to the patients receiving diuretics in high doses, it is necessary to lower an initial dose to 25 mg of 1 times a day.

It is not required to adjust a dose to patients of old age or patients with an impaired renal function, including the patients who are on a hemodialysis.

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

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 Bloktrana® 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 syvorochny 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 of development or even death of the developing fruit.

Therefore at pregnancy emergence reception of Bloktrana® 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 of Bloktranom®.

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 Bloktran® is well transferred, 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, sleep disorders, drowsiness, dysmnesias, peripheral neuropathy, paresthesias, a 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, locks.

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 1% - 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 a hydrochlorothiazide, 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, beta 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 for patients 18 years are younger).

With care liver and/or renal 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:

List B. In the dry place at a temperature not higher than 30 S. Hranit in the place, unavailable to children.

Period of validity - 2 years. Drug cannot be used after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated 50 mg.

On 10 tablets in a blister strip packaging. 1, 2, 3, 5 or 6 planimetric packagings with the application instruction in a pack from a cardboard.