Lozarel
Lozarel: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Losarel
ATX code: C09CA01
Active ingredient: losartan (losartan)
Manufacturer: LEK dd (Slovenia)
Description and photo update: 28.11.2018
Prices in pharmacies: from 200 rubles.
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Lozarel is an antihypertensive drug, angiotensin II receptor antagonist.
Release form and composition
The drug is available in the form of film-coated tablets: white with a yellow tint or white, round, biconvex, with a dividing line on one side (30 pcs. In blisters, in a cardboard box 3 blisters and instructions for the use of Lozarel).
1 tablet contains:
- active substance: potassium losartan - 50 mg;
- auxiliary components: lactose monohydrate, microcrystalline cellulose, magnesium stearate, colloidal anhydrous silicon dioxide, pregelatinized starch;
- composition of the film shell: macrogol 400, hypromellose, titanium dioxide (E171), hyprolose, talc.
Pharmacological properties
Pharmacodynamics
Lozarel is an antihypertensive drug, the active ingredient of which is losartan, which is a selective angiotensin II receptor antagonist (type AT 1). In the smooth muscle tissues of blood vessels, in the tissues of the heart, adrenal glands, kidneys, there are AT 1 -receptors, the selective binding of angiotensin II to them causes vasoconstriction, release of aldosterone and proliferation of smooth muscles. The action of losartan and its pharmacologically active metabolite is aimed at blocking all physiologically important effects of angiotensin II, regardless of the nature of its origin. At the same time, losartan does not have an inhibitory effect on kinase II, an enzyme that degrades bradykinin.
The manifestation of the clinical effect after taking Lozarel is a decrease in the total peripheral vascular resistance, a decrease in the concentration of aldosterone in the blood, a decrease in systolic and diastolic blood pressure (BP), and pressure in the pulmonary circulation. In addition, the drug has a diuretic effect, reduces afterload, prevents the onset of myocardial hypertrophy, in patients with chronic heart failure - helps to increase exercise tolerance.
Against the background of a single dose of the pill, the maximum hypotensive effect is achieved after 6 hours, then it gradually decreases within 24 hours. After 21-42 days of regular administration of Lozarel, the maximum hypotensive effect occurs. Does not inhibit angiotensin-converting enzyme (ACE), does not interfere with the destruction of bradykinin, does not cause side effects indirectly associated with bradykinin.
With arterial hypertension without concomitant diabetes mellitus with proteinuria, taking tablets significantly reduces proteinuria, excretion of immunoglobulins G and albumin.
Losartan helps to stabilize the level of urea in the blood plasma, does not affect autonomic reflexes, and does not affect the level of norepinephrine in the blood plasma for a long time.
In patients with arterial hypertension, a daily dose of up to 150 mg has no effect on the level of total cholesterol, high-density lipoprotein cholesterol and triglycerides in the blood serum, or on fasting blood glucose.
Pharmacokinetics
After oral administration, losartan is well absorbed from the gastrointestinal tract. During the first passage through the liver, it is metabolized by carboxylation with the participation of the CYP2C9 isoenzyme and the formation of an active metabolite. The systemic bioavailability of losartan is approximately 33%. The maximum concentration (C max) of the active substance of Lozarel in the blood serum is reached after approximately 1 hour, and its active metabolite - after 3-4 hours. Concomitant food intake does not affect the bioavailability of losartan. At a dose of up to 200 mg, losartan retains linear pharmacokinetics.
Plasma protein binding (mainly albumin) - more than 99%.
V d (volume of distribution) is 34 liters.
Almost does not penetrate the blood-brain barrier.
Up to 14% of the losartan dose taken orally is converted into an active metabolite.
Plasma clearance of losartan is 600 ml / min, renal clearance is 74 ml / min, its active metabolite is 50 ml / min and 26 ml / min, respectively.
Through the kidneys, approximately 4% is excreted unchanged, in the form of an active metabolite - up to 6% of the dose taken. The rest is excreted through the intestines.
The final half-life of the unchanged active substance is about 2 hours, and its active metabolite is up to 9 hours.
Against the background of the use of Lozarel in a daily dose of 100 mg, there is a slight accumulation of losartan and its active metabolite in the blood plasma.
With mild and moderate severity of alcoholic cirrhosis of the liver, the concentration of losartan increases 5 times, and the active metabolite - 1.7 times, compared with patients without this pathology.
The concentration of losartan in the blood plasma in patients with creatinine clearance (CC) above 10 ml / min is similar to that in patients with normal renal function. When CC is less than 10 ml / min, the value of the total concentration of the drug (AUC) in the blood plasma increases by about 2 times.
During hemodialysis, losartan and its active metabolite are not removed from the body.
In elderly men with arterial hypertension, the level of drug concentration in blood plasma does not differ significantly from similar parameters in young men.
With arterial hypertension in women, the plasma concentration of losartan is 2 times higher than in men. The content of the active metabolite is similar. This pharmacokinetic difference has no clinical significance.
Indications for use
- arterial hypertension;
- chronic heart failure - with the ineffectiveness of the use of ACE inhibitors;
- arterial hypertension in patients with left ventricular hypertrophy - to reduce the risk of cardiovascular complications and mortality;
- nephropathy in type 2 diabetes mellitus - in order to reduce the risk of developing proteinuria and hypercreatininemia.
Contraindications
- syndrome of impaired absorption of glucose or galactose, galactosemia, lactose intolerance;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to the components of the drug.
Lozarel tablets should be used with caution in patients with hepatic impairment, impaired water and electrolyte balance, reduced circulating blood volume (BCC), renal failure, bilateral renal artery stenosis or stenosis of an artery of a single kidney.
Lozarel, instructions for use: method and dosage
Lozarel tablets are taken orally, regardless of the meal.
Recommended dosage:
- arterial hypertension: initial and maintenance dose - 50 mg once a day. In the absence of a sufficient clinical effect in some patients, it is allowed to increase the dose to 100 mg, in this case the tablets are taken 1 or 2 times a day. With concomitant therapy with high doses of diuretics, the use of Lozarel should be started with 25 mg (1/2 tablet) 1 time per day;
- chronic heart failure: the initial dose is 12.5 mg (1/4 tablet) once a day, every 7 days the dose is doubled, gradually increasing it to 50 mg a day, taking into account the tolerability of the drug;
- type 2 diabetes mellitus with proteinuria (to reduce the risk of developing hypercreatininemia and proteinuria): the initial dose is 50 mg once a day. Depending on the blood pressure indicators during treatment, the dose can be increased to 100 mg in 1 or 2 doses;
- arterial hypertension in patients with left ventricular hypertrophy (lowering the risk of cardiovascular complications and mortality): the initial dose is 50 mg once a day, if necessary, it can be increased to 100 mg.
For patients with impaired renal function (CC less than 20 ml / min), a history of liver disease, dehydration, over the age of 75 years or during dialysis, the initial daily dose of Lozarel should be prescribed in the amount of 25 mg (1/2 tablet).
Side effects
- from the respiratory system: often - infections of the upper respiratory tract, nasal congestion, swelling of the nasal mucosa, pharyngitis, dyspnea, cough, bronchitis;
- on the part of the cardiovascular system: sometimes - dose-dependent orthostatic hypotension, palpitations, epistaxis, tachycardia, arrhythmias, angina pectoris, bradycardia, vasculitis, myocardial infarction;
- from the senses and the nervous system: often - headache, fatigue, dizziness, insomnia, asthenia; sometimes - drowsiness, sleep disturbance, anxiety, memory disorders, migraine, peripheral neuropathy, tremor, ataxia, paresthesia, hypesthesia, syncope, depression, visual impairment, conjunctivitis, ringing in the ears;
- from the digestive tract: often - nausea, abdominal pain, diarrhea, dyspeptic symptoms; sometimes - dry mouth, taste disturbance, toothache, flatulence, constipation, vomiting, anorexia, gastritis, liver dysfunction, hepatitis;
- from the musculoskeletal system: often - pain in the back, chest and / or legs, convulsions, myalgia; sometimes - arthralgia, fibromyalgia, arthritis; rarely - rhabdomyolysis;
- on the part of the immune system: sometimes - the development of allergic reactions in the form of urticaria, itching, rash, angioedema;
- on the part of the hematopoietic system: sometimes - eosinophilia, anemia, thrombocytopenic purpura, thrombocytopenia;
- from the urinary system: sometimes - frequent urge to urinate, urinary tract infections, impaired renal function;
- from the reproductive system: sometimes - decreased libido, impotence;
- dermatological reactions: sometimes - increased sweating, dry skin, subcutaneous hemorrhage, erythema, photosensitivity, alopecia;
- laboratory parameters: often - hyperkalemia; sometimes - an increased content of urea, residual nitrogen or creatinine in the blood serum; very rarely - hyperbilirubinemia, a moderate increase in the activity of alanine aminotransferase (ALT) and aspartate aminotransferase (AST);
- others: gout.
Overdose
Symptoms: marked lowering of blood pressure, tachycardia, bradycardia.
Treatment: forced diuresis, the appointment of symptomatic therapy. Hemodialysis is ineffective.
special instructions
It should be borne in mind that drugs that have an effect on the RAAS system (renin-aldosterone-angiotensin system) can increase the serum concentration of creatinine and urea in bilateral renal artery stenosis or stenosis of an artery of a single kidney.
In patients with dehydration, before the appointment of Losartan, it is necessary to correct dehydration, this will reduce the risk of symptomatic arterial hypotension.
Long-term use of losartan must be accompanied by regular monitoring of the potassium content in the blood plasma.
Influence on the ability to drive vehicles and complex mechanisms
Lozarel does not affect the patient's ability to drive vehicles, including a car, and work with complex mechanisms.
Application during pregnancy and lactation
The use of Lozarel is contraindicated during the period of gestation and breastfeeding.
Pediatric use
The efficacy and safety of the use of losartan in patients under 18 years of age have not been established, therefore, Lozarel should not be prescribed in childhood and adolescence.
With impaired renal function
Care should be taken when treating patients with renal insufficiency, bilateral renal artery stenosis, stenosis of an artery of a single kidney.
Recommended dosage for impaired renal function (CC less than 20 ml / min): initial dose - 25 mg (1/2 tablet) once a day.
For violations of liver function
Care should be taken when treating patients with hepatic impairment.
The initial daily dose of Lozarel for patients with a history of liver disease should be 25 mg (1/2 tablet).
Use in the elderly
The recommended dosage for patients over the age of 75 years: the initial dose of Lozarel is 25 mg (1/2 tablet) once a day.
Drug interactions
Possible drug interaction with the simultaneous use of Lozarel:
- hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole, erythromycin: these drugs do not cause pharmacokinetic interaction with losartan;
- rifampicin, fluconazole: the level of the active metabolite of losartan in the blood plasma may decrease when taking rifampicin or fluconazole;
- potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, potassium-containing salts: the risk of hyperkalemia increases;
- NSAIDs (non-steroidal anti-inflammatory drugs), including acetylsalicylic acid (in a daily dose of 3 g and above), selective cyclooxygenase-2 inhibitors: NSAIDs can reduce the effectiveness of the drug, cause reversible renal dysfunction, including increased plasma potassium levels and acute renal failure, especially in patients with reduced renal function;
- lithium preparations: the risk of a clinically significant increase in the concentration of lithium in the blood plasma increases, therefore the combination of losartan and lithium is allowed only after a thorough assessment of the benefits and risks and should be accompanied by regular monitoring of the lithium content in the blood plasma;
- diuretics, beta-blockers, sympatholytics: an additive effect occurs.
Analogs
Lozarel's analogs are: Losartan, Bloktran, Lozap, Kozaar, Prezartan, Lotor, Agilosartan, Lorista, Losakor, Renikard, Vasotenz, Zisakar.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Lozarelle
Feedback from patients and specialists about Lozarel is positive. Doctors note that the drug, in addition to its antihypertensive action, has an additional diuretic effect. Reception Lozarel reduces the load and prevents the onset and development of myocardial hypertrophy. With chronic heart failure, the ability to withstand physical activity increases.
In patients with diabetes mellitus and nephropathy, taking Lozarel provides relief from edema.
The price of Lozarel in pharmacies
The price of Lozarel for a pack containing 30 tablets can range from 236 rubles.
Lozarel: prices in online pharmacies
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Drug name Price Pharmacy |
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Lozarel 50 mg film-coated tablets 30 pcs. RUB 200 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
