Universal reference book for medicines
Product name: LOZAP ® (LOZAP ® )

Active substance: losartan

Type: Angiotensin II receptor antagonist

Manufacturer: ZENTIVA (Slovak Republic) manufactured by SANECA PHARMACEUTICALS (Slovak Republic)
Composition, form of production and packaging
The tablets covered with a film membrane of
white or almost white color, oblong, biconcave.

1 tab.

Losartan potassium 12.5 mg

Excipients: microcrystalline cellulose, mannitol, crospovidone, silicon dioxide colloidal anhydrous, talc, magnesium stearate.

The composition of the film shell: sepiphilm 752 white (hypromellose, microcrystalline cellulose, macrogol 2000 stearate, titanium dioxide), macrogol 6000.

10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (6) - packs of cardboard.
10 pieces.
- blisters (9) - packs of cardboard.
The tablets covered with a film membrane of white or almost white color, oblong, biconcave, with risk from both sides.

1 tab.

Losartan potassium 50 mg

Excipients: microcrystalline cellulose, mannitol, crospovidone, silicon dioxide colloidal anhydrous, talc, magnesium stearate.

The composition of the film shell: sepiphilm 752 white (hypromellose, microcrystalline cellulose, macrogol 2000 stearate, titanium dioxide), macrogol 6000.

10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (6) - packs of cardboard.
10 pieces.
- blisters (9) - packs of cardboard.
The tablets covered with a film membrane of white or almost white color, oblong, biconcave, with risk from both sides.

1 tab.

Losartan Potassium 100 mg

Excipients: microcrystalline cellulose, mannitol, crospovidone, silicon dioxide colloidal anhydrous, talc, magnesium stearate.

The composition of the film shell: sepiphilm 752 white (hypromellose, microcrystalline cellulose, macrogol 2000 stearate, titanium dioxide) macrogol 6000.

10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (6) - packs of cardboard.
10 pieces.
- blisters (9) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

Antihypertensive drug.
Specific antagonist of angiotensin II receptors (subtype AT 1 ). Does not inhibit kinase II - an enzyme that catalyzes the reaction of the conversion of angiotensin I into angiotensin II. Reduces OPSS, concentration in the blood of adrenaline and aldosterone, blood pressure, pressure in a small circle of blood circulation; reduces afterload, has a diuretic effect. It prevents the development of myocardial hypertrophy, increases tolerance to physical activity in patients with chronic heart failure. Losartan does not inhibit ACE-kininase II and therefore does not interfere with the destruction of bradykinin, therefore side effects mediated by bradykinin (eg, angioedema) are rare.
In patients with arterial hypertension without concomitant diabetes mellitus with proteinuria (more than 2 g / day), the use of the drug significantly reduces proteinuria, albumin excretion and immunoglobulin G.

Stabilizes the level of urea in the blood plasma.
Does not affect vegetative reflexes and does not have a long-term effect on the concentration of norepinephrine in the blood plasma. Losartan in a dose of up to 150 mg / day does not affect the level of triglycerides, total cholesterol and HDL cholesterol in the blood serum in patients with hypertension. At the same dose, losartan does not affect the fasting blood glucose level.
After a single oral intake, the hypotensive effect (systolic and diastolic blood pressure decreases) reaches a maximum after 6 hours, then gradually decreases within 24 hours.

The maximum hypotensive effect develops 3-6 weeks after the start of the drug.

PHARMACOKINETICS

Suction

When administered orally, losartan is well absorbed, and at the same time is metabolized at the "first pass" through the liver by carboxylation with the participation of cytochrome CYP2C9 isoenzyme with the formation of an active metabolite.
Systemic bioavailability of losartan is about 33%. C max losartan and its active metabolite are reached in the blood serum approximately after 1 hour and 3-4 hours after ingestion, respectively. Eating does not affect the bioavailability of losartan.
Distribution

More than 99% of losartan and its active metabolite binds to blood plasma proteins, mainly with albumins.
V d losartan - 34 liters. Losartan practically does not penetrate the BBB.
Metabolism

Approximately 14% of losartan administered to the patient IV, or taken internally, becomes an active metabolite.

Excretion

The plasma clearance of losartan is 600 ml / min, and the active metabolite is 50 ml / min.
The renal clearance of losartan and its active metabolite is 74 ml / min and 26 ml / min, respectively. When ingested, approximately 4% of the dose taken is excreted by the kidneys unchanged and about 6% is excreted by the kidneys in the form of an active metabolite. Losartan and its active metabolite is characterized by linear pharmacokinetics when administered orally at doses up to 200 mg.
After oral administration, the plasma concentrations of losartan and its active metabolite decrease polyexponentially with a finite T 1/2 of losartan for about 2 hours and an active metabolite about 6-9 hours. When taking the drug at a dose of 100 mg / day, neither losartan nor the active metabolite significantly cumulate in the blood plasma.
Losartan and its metabolites are excreted through the intestine and the kidneys. In healthy volunteers, after ingestion of losartan labeled with 14 C isotope, about 35% of the radioactive label is found in urine and 58% in feces.
Pharmacokinetics in special clinical cases

In patients with alcoholic liver cirrhosis of mild and moderate severity, the concentration of losartan was 5 times, and the active metabolite was 1.7 times higher than in healthy male volunteers.

With CC> 10 ml / min, the concentration of losartan in the blood plasma does not differ from that with normal kidney function.
In patients who need hemodialysis, the AUC is approximately 2 times higher than in patients with normal renal function.
Neither losartan nor its active metabolite is removed from the body by hemodialysis.

The concentrations of losartan and its active metabolite in blood plasma in elderly men with arterial hypertension do not differ significantly from the values ​​of these parameters in young men with arterial hypertension.

Values ​​of plasma concentrations of losartan in women with arterial hypertension are 2 times higher than the corresponding values ​​in men with arterial hypertension.The concentrations of the active metabolite in men and women do not differ.
This pharmacokinetic difference is not clinically relevant.
INDICATIONS

- arterial hypertension;

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

- reduction in the risk of developing cardiovascular diseases (including stroke) and mortality in patients with hypertension and left ventricular hypertrophy;

- Diabetic nephropathy in hypercreatininemia and proteinuria (urine albumin and creatinine ratio more than 300 mg / g) in patients with type 2 diabetes and concomitant arterial hypertension (reduction in the progression of diabetic nephropathy to terminal chronic renal failure).

DOSING MODE

The drug is taken orally, regardless of food intake.
Multiplicity of application - 1 time / day.
With arterial hypertension, the average daily dose is 50 mg.
In some cases, to achieve a greater therapeutic effect, the daily dose can be increased to 100 mg in 2 or 1 reception.
The initial dose for patients with chronic heart failure is 12.5 mg 1 time / day.
Typically, the dose is increased 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 drug.
When appointing the drug to patients receiving diuretics in high doses, the initial dose of the drug Lozap ® should be reduced to 25 mg 1 time / day.

For elderly patients, there is no need for dose adjustment.

When the drug is prescribed to reduce the risk of developing cardiovascular diseases (including stroke) and mortality in patients with hypertension and left ventricular hypertrophy, the initial dose is 50 mg / day.
In the future, hydrochlorothiazide can be added at a low dose and / or the dose of Lozap ® can be increased to 100 mg / day in 1-2 doses.
In patients with concomitant type 2 diabetes mellitus with proteinuria, the initial dose of the drug is 50 mg 1 time / day, then the dose is raised to 100 mg / day (taking into account the degree of depression of blood pressure) in 1-2 doses.

Patients with a history of liver disease, dehydration, hemodialysis, and patients older than 75 years are recommended a lower initial dose of the drug - 25 mg (1/2 tablets 50 mg) 1 time / day.

SIDE EFFECT

When using losartan for the treatment of essential hypertension in controlled studies, among all the side effects, only the incidence of dizziness differed from placebo by more than 1% (4.1% vs. 2.4%).

The dose-dependent orthostatic effect, characteristic of antihypertensive agents, was observed in less than 1% of patients with losartan.

Determination of the frequency of side effects: very often (? 1/10);
often (? 1/100,? 1/10); sometimes (? 1/1000,? 1/100); rarely (? 1/10 000,? 1/1000); very rarely (? 1 / 10,000, including individual reports).
Side effects, occurring with a frequency of more than 1%

Side effects Losartan (n = 2085) Placebo (n = 535)

General reactions

Asthenia, fatigue 3.8 3.9

Chest pain 1.1 2.6

Peripheral edema 1.7 1.9

From the side of the cardiovascular system

Palpitation 1.0 0.4

Tachycardia 1.0 1.7

From the digestive system

Pain in the abdomen 1.7 1.7

Diarrhea 1.9 1.9

Dyspeptic phenomena 1.1 1.5

Nausea 1.8 2.8

From the musculoskeletal system

Pain in the back, legs 1.6 1.1

Cramps of the calf muscles 1.0 1.1

From the side of the central nervous system

Vertigo 4.1 2.4

Headache 14.1 17.2

Insomnia 1.1 0.7

From the respiratory system

Cough, bronchitis 3.1 2.6

Nasal congestion 1.3 1.1

Pharyngitis 1.5 2.6

Sinusit 1.0 1.3

Upper respiratory tract infection 6.5 5.6

The side effects of losartan are usually transient and do not require withdrawal of the drug.

Side effects, occurring with a frequency of less than 1%

From the cardiovascular system: orthostatic hypotension (dose-dependent) , epistaxis, bradycardia, arrhythmias, angina pectoris, vasculitis, myocardial infarction.

On the part of the digestive system: anorexia, dryness of the oral mucosa, toothache, vomiting, flatulence, gastritis, constipation, hepatitis, a violation of liver function;
very rarely - a moderate increase in the activity of AST and ALT, hyperbilirubinemia.
Dermatological reactions: dry skin, erythema, ecchymosis, photosensitivity, increased sweating, alopecia.

Allergic reactions: urticaria, skin rash, itching, angioedema (including swelling of the larynx and tongue, causing airway obstruction and / or swelling of the face, lips, pharynx).

On the part of the hematopoiesis system: sometimes anemia (a slight decrease in the concentration of hemoglobin and hematocrit, an average of 0.11 g% and 0.09 volume%, respectively, rarely of clinical significance), thrombocytopenia, eosinophilia, purpura Shenlen-Henoch.

From the musculoskeletal system: arthralgia, arthritis, pain in the shoulder, knee, fibromyalgia.

From the central nervous system and peripheral nervous system: anxiety, sleep disturbance, drowsiness, memory disorders, peripheral neuropathy, paresthesia, hypoesthesia, tremor, ataxia, depression, fainting, migraine.

From the sense organs: ringing in the ears, violation of taste, visual impairment, conjunctivitis.

From the urinary system: mandatory urination, urinary tract infections, impaired renal function;
sometimes - increased levels of urea and residual nitrogen or creatinine in the blood serum.
On the part of the reproductive system: decreased libido, impotence.

From the side of metabolism: often - hyperkalemia (the level of potassium in the blood plasma is more than 5.5 mmol / l);
gout.
CONTRAINDICATIONS

- Pregnancy;

- lactation period;

- age under 18 years (effectiveness and safety not established);

- Hypersensitivity to the components of the drug.

With caution should be applied to the drug with arterial hypotension, lower bcc, violations of water-electrolyte balance, bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney, with renal / hepatic insufficiency.

PREGNANCY AND LACTATION

There are no data on the use of Lozap ® during pregnancy.
However, it is known that drugs acting directly on RAAS, when used in the II and III trimesters of pregnancy, can cause a developmental defect or even the death of a developing fetus. Therefore, when pregnancy occurs, the use of Lozap ® should be stopped immediately.
If Lozap needs to be used during lactation, a decision should be made either to stop breastfeeding or to stop treatment with the drug.

APPLICATION FOR FUNCTIONS OF THE LIVER

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

During the treatment period, the concentration of potassium in the blood should be regularly monitored in cases of impaired renal function.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Patients with impaired liver function should be prescribed Lozap in lower doses.

APPLICATION FOR CHILDREN

The drug is contraindicated in children and adolescents under 18 years (efficacy and safety not established).

APPLICATION IN ELDERLY PATIENTS

In elderly patients, there is no need to adjust the initial dose.

During the treatment period, the concentration of potassium in the blood should be monitored regularly, especially in elderly patients.

SPECIAL INSTRUCTIONS

It is necessary to correct the dehydration before the administration of the drug Lozap ® or begin treatment with the use of the drug in a lower dose.

Drugs that affect RAAS can increase urea levels in the blood and serum creatinine in patients with bilateral renal artery stenosis or stenosis of the artery of a single kidney.

In patients with cirrhosis of the liver, the concentration of losartan in the blood plasma is significantly increased, and therefore, in the presence of liver diseases in the history, it should be prescribed in lower doses.

During the treatment period, the concentration of potassium in the blood should be monitored regularly, especially in elderly patients, with renal dysfunction.

Use in Pediatrics

The safety and efficacy of Lozap ® in children and adolescents under the age of 18 years have not been established.

Impact on the ability to drive vehicles and manage mechanisms

Lozap ® does not affect the ability to drive vehicles or work with machinery.

OVERDOSE

Symptoms: marked decrease in blood pressure, tachycardia;
Because of parasympathetic (vagal) stimulation, a bradycardia can appear.
Treatment: forced diuresis, symptomatic therapy;
hemodialysis is not effective.
DRUG INTERACTION

The drug can be administered with other antihypertensive agents.
There is a mutual enhancement of the effects of beta-blockers and sympatholytics. With the combined use of losartan with diuretics, an additive effect is observed.
There was no pharmacokinetic interaction of losartan with hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole and erythromycin.

Reportedly, rifampicin and fluconazole reduce the concentration of the active metabolite of losartan in the blood plasma.
The clinical significance of this interaction is still unknown.
As with other agents that inhibit angiotensin II or its effect, the combined use of losartan with potassium-sparing diuretics (for example, spironolactone, triamterene, amiloride), potassium preparations and potassium-containing salts increases the risk of hyperkalemia.

NSAIDs, including selective inhibitors of COX-2, may reduce the effect of diuretics and other antihypertensive agents.

With the combined use of antagonists of angiotensin II and lithium receptors, an increase in the concentration of lithium in the blood plasma is possible.
Given this, it is necessary to weigh the benefit and risk of joint use of losartan with preparations of lithium salts. If a joint application is necessary, the concentration of lithium in the blood plasma should be monitored regularly.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored out of reach of children at a temperature of no higher than 30 ° C.
Shelf life - 2 years.
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