BLOKTRAN

Active material: Lozartan
When ATH: C09CA01
CCF: Angiotensin II receptor antagonists
ICD-10 codes (testimony): I10, I50.0
When CSF: 01.04.02
Manufacturer: OAO Pharmstandard-Leksredstva (Russia)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills, coated light pink-orange, round, lenticular.

Excipients: lactose, microcrystalline cellulose, povidone (low molecular weight polyvinylpyrrolidone), potato starch, magnesium stearate, colloidal silicon dioxide (aэrosyl).

The composition of the shell: gipromelloza (hydroxypropyl), kopovydon (copolyvidonum), Titanium dioxide, talc, polysorbate-80 (Tween-80), sikovit yellow-orange 85 (E110).

10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (2) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.
10 PC. – packings Valium planimetric (5) – packs cardboard.
10 PC. – packings Valium planimetric (6) – packs cardboard.

Pharmacological action

Antihypertensive drugs. The specific angiotensin II receptor antagonist (subtype AT₁). He inhibits kinase II – enzyme, destroys bradykinin. Reduces PR, the blood concentration of epinephrine and aldosterone, FROM, the pressure in the pulmonary circulation. Umenyshaet postnagruzku, It has a diuretic effect. It prevents the development of myocardial hypertrophy, improves exercise tolerance in patients with heart failure.

After a single dose antihypertensive effect (umenyshenie sistolicheskogo and diastolicheskogo AD) reaches through 6 no, then for 24 h is gradually reduced.

The maximum antihypertensive effect is achieved through 3-6 weeks after the start of dosing.

Pharmacokinetics

Absorption

Losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability – about 33%. T_max losartan achieved through 1 no.

Metabolism

Treated effect “first pass” through the liver, metabolized by carboxylation with the participation of isoenzyme CYP2C9 with the formation of the active metabolite. T_max achieved through the active metabolite 3-4 no. The binding to plasma proteins – 99%.

Deduction

T_1/2 Losartan is 1.5-2 no, and its major metabolite – 6-9 no. About 35% the dose is excreted in the urine, about 60% – through the intestine.

Pharmacokinetics in special clinical situations

Established, losartan concentration in blood plasma in patients with liver cirrhosis is significantly increased, so patients with liver disease history should use the drug at a lower dose.

Testimony

- Arterial hypertension;

- Congestive heart failure (in a combination therapy, in case of intolerance or failure of therapy with ACE inhibitors).

Dosage regimen

The drug is taken orally, regardless of the meal, the multiplicity of reception – 1 time / day.

At hypertension the average daily dose is 50 mg. In some cases, in order to achieve greater effect, increase the dose to 100 mg 2 receiving or 1 time / day.

The starting dose for patients with Heart Failure is 12.5 mg 1 time / day. Usually, the dose is increased at weekly intervals (ie. 12.5 mg / day, 25 mg / day 50 mg / day) to the average maintenance dose 50 mg 1 time / day depending on patient tolerability.

In appointing the drug to patients, receiving diuretics at higher doses, the initial dose should be reduced to 25 mg 1 time / day.

Established, losartan concentration in blood plasma patients with liver cirrhosis is significantly increased, so patients with a history of liver disease should use the drug at a lower dose.

In elderly patients, as well as in patients with impaired renal function, including patients on hemodialysis, there is no need to adjust the initial dose.

The safety and efficacy of the drug in children not set.

Side effect

From the central and peripheral nervous system: ≥1% – dizziness, asthenia, headache, fatiguability, insomnia; <1% – anxiety, sleep disturbance, drowsiness, memory disorders, perifericheskaya neuropathy, paresthesia, gipestezii, migraine, tremor, ataxia, depression, syncope.

From the senses: ≥1% – tinnitus, taste disturbance, vision changes, conjunctivitis.

The respiratory system: ≥1% – nasal congestion, cough *, upper respiratory tract infection (fever, sore throat, sinusopatiя *, sinusitis, pharyngitis); <1% – dyspnoea, bronchitis, rhinitis.

From the digestive system: ≥1% – nausea, diarrhea *, dyspeptic symptoms *, abdominal pain; ≤1% – anorexia, dry mouth, toothache, vomiting, flatulence, gastritis, constipation.

On the part of the musculoskeletal system: ≥1% – convulsions, myalgia *, backache, Chest, legs; ≤1% – arthralgia, shoulder pain, slaughter, arthritis, fibromyalgia.

Cardio-vascular system: orthostatic hypotension (dozozavisimaya), heartbeat, Rituals- or bradycardia, Arrhythmia, angina.

With the genitourinary system: <1% – urgent need to urinate, urinary tract infection, impairment of renal function, the weakening of the libido, impotence.

Dermatological reactions: <1% – xerosis, эritema, hot flushes, photosensitivity, increased perspiration, alopecia.

Allergic reactions: <1% – hives, rash, itch, angioedema (incl. person, lips, throat and / or tongue).

Other: hyperkalemia (serum potassium more 5.5 mmol / l), anemia.

* – side effects, the frequency of which is comparable to placebo.

Communication side effects, occurring with a frequency <1% cases, with the use of losartan is not proven.

In most cases Bloktran^® well tolerated, side effects are transient in nature and do not require discontinuation of the drug.

Contraindications

- Hypotension;

- Hyperkalemia;

- Degidratatsiya;

- Pregnancy;

- Lactation (breast-feeding);

- Up to 18 years (efficacy and safety have not been established);

- Hypersensitivity to the drug.

FROM caution should be prescribed the drug for liver and / or kidney failure.

Pregnancy and lactation

Data on the use of losartan during pregnancy is not. However it is known, that drugs, acting directly on the renin-angiotensin system, when used in II and III trimesters of pregnancy, may cause a defect or even death of the developing fetus. Therefore, when a pregnancy reception Bloktrana^® should cease immediately.

In the appointment during lactation should decide to discontinue breast-feeding or discontinue therapy Bloktranom^®.

Cautions

It is necessary to carry out the correction of dehydration prior to the appointment Bloktrana^® or start treatment with the drug at a lower dose.

Preparations, affecting renin-angiotensin system, can increase the concentration of blood urea and serum creatinine in patients with bilateral renal artery stenosis or stenosis of a solitary kidney.

During treatment should regularly monitor the concentration of potassium in the blood, especially in elderly patients, renal impairment.

Overdose

Symptoms: marked reduction in blood pressure, tachycardia, because of the parasympathetic (vagal) stimulation may occur bradycardia.

Treatment: diurez, simptomaticheskaya therapy; hemodialysis nyeeffyektivyen.

Drug Interactions

The drug may be administered in combination with other antihypertensives. It should be borne, that Bloktran^® increases (mutually) the effect of other antihypertensive agents (incl. diuretics, beta-blockers, simpatolitikov).

There was no clinically significant interaction with hydrochlorothiazide, digoksinom, nepryamыmy anticoagulants, cimetidine, fenoʙarʙitalom.

Patients with dehydration (previous treatment with diuretics in high doses) may occur marked reduction of blood pressure.

When combined with potassium-sparing diuretics and potassium supplements increase the risk of hyperkalemia.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored in a dry, inaccessible to children at temperature not exceeding 30 ° C. Shelf life – 2 year.