LOZAP

Active material: Lozartan
When ATH: C09CA01
CCF: Angiotensin II receptor antagonists
ICD-10 codes (testimony): I10, I50.0, N08.3
When CSF: 01.04.02
Manufacturer: ZENTIVA a.s. (Czech Republic)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills, coated white or nearly white, round; of presentations – kernel white or almost white with a cover white or nearly white.

Excipients: microcrystalline cellulose, mannitol, sodium croscarmellose, povidone 30, magnesium stearate, gipromelloza, Titanium dioxide, talc, propylene glycol.

10 PC. – blisters (3) – 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; reduces afterload, 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 (reduction in systolic and diastolic blood pressure) 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

After oral administration, losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability – about 33%. The time to reach C_max Losartan is 1 no, aktivnogo metabolite – 3-4 no.

Distribution

The binding to plasma proteins – 99%.

Metabolism

Treated effect “first pass” through the liver, metabolized by carboxylation with the participation of isoenzyme of cytochrome P450 2C9 to the active metabolite.

Deduction

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

Pharmacokinetics in special clinical situations

Losartan concentration in blood plasma in patients with liver cirrhosis is significantly increased.

Testimony

- Arterial hypertension;

- To reduce the risk of cardiovascular diseases (incl. stroke) and mortality in patients with hypertension and left ventricular hypertrophy;

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

- To protect the kidneys in patients with diabetes mellitus type 2 proteinuria – slow the progression of renal failure, manifested reduced frequency hypercreatininemia, the incidence of end-stage chronic renal failure (requiring dialysis or a kidney transplant), death, as well as the reduction of proteinuria.

Dosage regimen

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

At hypertension the average daily dose is 50 mg. If necessary, the daily dose may be increased to 100 mg 2 or 1 reception.

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 tolerability.

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

Patients with impaired hepatic function should appoint Losap at lower doses.

In elderly patients, and y patients with impaired renal function, including patients on dialysis, there is no need to adjust the initial dose.

The drug can be administered with other antihypertensive agents.

In appointing the drug to reduce the risk of cardiovascular diseases (incl. stroke) and mortality in patients with hypertension and left ventricular hypertrophy the standard starting dose is 50 mg / day. Patients, who have failed to reach target blood pressure in patients receiving this dose Lozap, hydrochlorothiazide may be added in a low dose and / or, if necessary, increased dose to Lozap 100 mg / day.

At Diabetes mellitus type 2 proteinuria the initial dose is 50 mg 1 time / day, if necessary, may increase the dose to 100 mg / day (taking into account the degree of reduction in blood pressure).

Side effect

From the central and peripheral nervous system: ≥1% – dizziness, asthenia, fatiguability, headache, insomnia.

The respiratory system: ≥1% – nasal congestion, infections of the upper respiratory tract.

From the digestive system: ≥1% – nausea, abdominal pain.

On the part of the musculoskeletal system: ≥1% – convulsions, backache, Chest, legs.

Cardio-vascular system: ≥1% – orthostatic hypotension (dozozavisimaya), heartbeat, Rituals- or bradycardia, Arrhythmia, angina.

Other: anemia.

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

Contraindications

- Hyperkalemia;

- Pregnancy;

- Lactation;

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

- Hypersensitivity to the drug.

FROM caution use in patients with hypotension, renal / hepatic insufficiency, degidratacii.

Pregnancy and lactation

Data on the use during pregnancy is not Lozap. However it is known, that drugs, vozdeystvuyushtie sistemu immediately on the renin-angiotensin, when used in II and III trimester of pregnancy may cause a defect in development, or even death of the developing fetus. Therefore, in the event of pregnancy Lozap reception should be stopped immediately.

If necessary, use Lozap lactation should decide, or the termination of breastfeeding, or cessation of treatment.

Cautions

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

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

In patients with liver cirrhosis the concentration of losartan in blood plasma increases considerably, in connection with which the presence of liver diseases in history should be administered in lower doses.

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

Use in Pediatrics

The safety and efficacy of the drug in Losap children and adolescents under the age of 18 years not set.

Overdose

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

Treatment: diurez, simptomaticheskaya therapy; Hemodialysis is not effective.

Drug Interactions

Clinically significant interactions with hydrochlorothiazide Lozap, digoksinom, nepryamыmy anticoagulants, cimetidine, phenobarbital were observed.

Patients with dehydration, caused by the preceding use of diuretics in high doses, against application Lozap may occur marked reduction of blood pressure.

In an application Lozap with other antihypertensive drugs (Diuretics, beta-blockers, simpatolitikami) mutual strengthening hypotensive action.

In a joint application Lozap 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.