Lozap pills 50mg №90

Coated Tablets white or almost white, round; on a break - a white or almost white core with a white or almost white shell.

Excipients: microcrystalline cellulose, mannitol, croscarmellose sodium, povidone 30, Magnesium stearate, hypromellose, titanium dioxide, talc, propylene glycol.

10 pieces. - blisters (3) - packs cardboard.

Angiotensin II Receptor Antagonist

• tab., pokr. shell, 12.5 mg: 30 pcs. - P No. 095897/01, August 17, 2004
• tab., pokr. shell, 50 mg: 30 pcs. - P No. 095897/01, August 17, 2004

Mechanism of action

Antihypertensive drug. Specific antagonist of angiotensin II receptors (subtype AT₁). He inhibits kinase II - an enzyme that destroys bradykinin.

Reduces the OPSS, the concentration in the blood of adrenaline and aldosterone, blood pressure, pressure in the pulmonary circulation; reduces afterload, has a diuretic effect. Interferes with the development of myocardial hypertrophy, increases exercise tolerance in patients with heart failure.

After a single dose, the antihypertensive effect (decrease in systolic and diastolic blood pressure) reaches a maximum after 6 hours, then gradually decreases within 24 hours. The maximum antihypertensive effect is achieved 3-6 weeks after starting the drug.

Suction

After oral administration, losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 33%. Time to reach C_max losartan is 1 hour, the active metabolite is 3-4 hours.

Distribution

Plasma protein binding - 99%.

Metabolism

Exposed to the effect of "first pass" through the liver, metabolized by carboxylation with the participation of isoenzyme 2C9 cytochrome P₄₅₀ with the formation of an active metabolite.

Removal

T_1/2 losartan - 1.5-2 hours, and its main metabolite is 6-9 hours. About 35% of the dose is excreted in the urine, about 60% - in the feces.

Pharmacokinetics in special clinical situations

The concentration of losartan in the blood plasma of patients with cirrhosis of the liver increases significantly.

Indications and usage

- arterial hypertension;

- heart failure (as part of combination therapy, with intolerance or failure of therapy with ACE inhibitors).

At hypertension the average initial daily dose is 50 mg. The frequency of admission - 1 time / day. In some cases, to achieve a greater effect, the dose is increased to 100 mg in 2 or 1 dose.

When prescribing the drug patients receiving diuretics in high doses, The initial dose of Lozapa should be 25 mg 1 time / day.

Initial dose for patients with heart failure is 12.5 mg 1 time / day. As a rule, the dose increases with a weekly interval (ie, 12.5 mg / day, 25 mg / day, 50 mg / day) to an average maintenance dose of 50 mg 1 time / day, depending on the tolerance of the patient.

Lozap should be prescribed in lower doses.

Have elderly patientsas well as patients with impaired renal function, including patients on dialysis, no need to adjust the initial dose.

Tablets are taken orally, regardless of the meal.

Adverse reactions

Nervous system: 1% or more - dizziness, asthenia, fatigue, headache, insomnia.

Respiratory: ≥1% - nasal congestion, infection of the upper respiratory tract.

Gastrointestinal: ≥1% - nausea, abdominal pain.

Musculoskeletal system: ≥1% - convulsions, pain in the back, chest, legs.

Cardiovascular: ≥1% - orthostatic hypotension (dose-dependent), palpitations, tachy- or bradycardia, arrhythmias, angina pectoris.

Other: anemia.

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

Contraindications

- arterial hypotension;

- hyperkalemia;

- dehydration;

- pregnancy;

- lactation period;

- children's and teenage age up to 18 years;

- hypersensitivity to the drug.

Pregnancy and Breastfeeding

There are no data on the use of Lozap during pregnancy. However, it is known that drugs acting directly on the renin-angiotensin system, when applied in the second and third trimesters of pregnancy, can cause a defect of development or even death of a developing fetus. Therefore, when a pregnancy occurs, Lozapa should be stopped immediately.

If necessary, the use of Lozapa during lactation should make a decision either to stop breastfeeding or to discontinue treatment with the drug, taking into account its importance to the mother.

Lozap should be prescribed in lower doses.

In patients with impaired renal function, including patients on dialysis, no need to adjust the initial dose.

Special notes

It is necessary to carry out the correction of dehydration before the appointment of Lozap or begin treatment with the use of the drug at a lower dose.

Lozap may be administered as part of combination therapy with other antihypertensive drugs.

Some drugs that affect the renin-angiotensin system can increase blood urea and serum creatinine in patients with bilateral renal stenosis or arterial stenosis of a single kidney.

During the period of treatment should regularly monitor the concentration of potassium in the blood, especially in elderly patients, with impaired renal function.

Use in pediatrics

Safety and efficacy of the drug Lozap at children and adolescents under the age of 18 not installed.

Overdosage

Symptoms: pronounced decrease in blood pressure, tachycardia; Bradycardia may appear due to parasympathetic (vagal) stimulation.

Treatment: forced diuresis, symptomatic therapy; hemodialysis is not effective.

Drug Interactions

There was no clinically significant interaction between Lozap and hydrochlorothiazide, Digoxin, indirect anticoagulants, cimetidine, and phenobarbital.

In patients with dehydration caused by the previous use of diuretics in high doses, with the use of Lozapa, there may be a pronounced decrease in blood pressure.

With simultaneous use of Lozapa with other antihypertensive drugs (diuretics, beta-blockers, sympatholytics), the hypotensive action is mutually reinforced.

The combined use of Lozap with potassium-sparing diuretics and potassium preparations increases the risk of hyperkalemia.

Storage conditions

List B. The drug should be stored in a dry place inaccessible to children at a temperature not exceeding 30 ° C.