Buy Losartan-N Richter film-coated tablets 50mg+12.5mg No. 30 in pharmacies

Compound

Losartan-Richter 50 mg 30 pcs. film-coated tablets

pharmachologic effect

Diuretic, hypotensive.

Composition and release form Losartan-Richter 50 mg 30 pcs. film-coated tablets

Tablet - 1 tablet:

• Active substance: losartan potassium 50 mg;
• Excipients: colloidal silicon dioxide - 0.75 mg, magnesium stearate - 1.5 mg, croscarmellose sodium - 3 mg, pregelatinized starch - 20.2 mg, microcrystalline cellulose - 74.55 mg;
• Film shell composition: opadry 33G28523 white (triacetin - 0.3 mg, macrogol - 0.4 mg, lactose monohydrate - 1.05 mg, titanium dioxide (CI77891, E171) - 1.25 mg, hypromellose - 2 mg).

Tablets 50 mg, in blisters, 30 pieces per pack.

Description of the dosage form

Tablets, film-coated, white or almost white, round, biconvex, two layers visible at the break - a white or almost white core and a film shell.

Directions for use and doses

At the beginning of therapy, Losartan-Richter is taken in one dose of 50 mg/day. In the future, it is possible to add hydrochlorothiazide in low doses or increase the dose of losartan to 100 mg/day.

Pharmacodynamics

Antihypertensive agent. It is a non-peptide angiotensin II receptor blocker. It has high selectivity and affinity for AT1 type receptors (with the participation of which the main effects of angiotensin II are realized). By blocking these receptors, losartan prevents and eliminates the vasoconstrictor effect of angiotensin II, its stimulating effect on the secretion of aldosterone by the adrenal glands and some other effects of angiotensin II. It is characterized by a long-term effect (24 hours or more), which is due to the formation of its active metabolite.

Pharmacokinetics

Suction.

Rapidly absorbed from the gastrointestinal tract (GIT). Bioavailability - 25-35%. Average maximum plasma concentrations (Cmax) of losartan and its active metabolite are achieved after 1 hour and after 3-4 hours, respectively. There was no effect of food intake on the absorption of losartan.

Distribution.

Communication with blood plasma proteins (mainly albumin) - 92% (losartan), 99% (metabolite). Practically does not penetrate the blood-brain barrier.

Metabolism.

It has the effect of “primary passage” through the liver, is metabolized by carboxylation with the participation of the CYP2C9 isoenzyme of cytochrome P450 with the formation of an active (10-40 times) metabolite.

Excretion.

The half-life (T1/2) is 1.5-2 hours, and that of its main metabolite is 6-9 hours.

35% is excreted by the kidneys (of which 4% - in the form of unchanged drug and 6% - in the form of the main metabolite); the remaining amount (60%) is through the intestines.

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

When creatinine clearance (CC) is above 10 ml/min, the concentration of losartan in the blood plasma does not differ from that with normal renal function.

In patients requiring hemodialysis, the area concentration-time curve (AUC) is approximately twice as high as in patients with normal renal function.

Neither losartan nor its active metabolite is removed from the body by hemodialysis.

Plasma concentrations of losartan and its active metabolite in elderly male patients with arterial hypertension do not differ significantly from the values ​​of these parameters in young male patients with arterial hypertension.

Plasma concentrations of losartan in women with arterial hypertension are 2 times higher than the corresponding values ​​in men with arterial hypertension.

Concentrations of the active metabolite do not differ between men and women. This pharmacokinetic difference is not clinically significant.

Indications for use Losartan-Richter 50 mg 30 pcs. film-coated tablets

Arterial hypertension.

Chronic heart failure with ineffective treatment with ACE inhibitors.

Kidney failure.

Left ventricular hypertrophy.

Contraindications

• Pregnant and breastfeeding;
• lactose intolerance;
• children, adolescents under eighteen years of age;
• galactose/glucose malabsorption syndrome;
• hypersensitivity to the ingredients of the drug;
• galactosemia.

Use with caution in case of arterial hypotension, decreased blood volume, water-electrolyte imbalance, bilateral renal artery stenosis or stenosis of the artery of a single kidney, and renal/liver failure.

Application Losartan-Richter 50 mg 30 pcs. film-coated tablets during pregnancy and breastfeeding

Contraindicated.

special instructions

For patients who have fluid and/or sodium deficiency, fluid and electrolyte disturbances should be corrected or a lower initial dose should be used before starting treatment.

In patients with dehydration (for example, those receiving high-dose diuretics), symptomatic hypotension may occur when losartan treatment is initiated.

If renal function is impaired, a dose reduction of losartan may be required.

In patients with a history of liver disease, losartan should be used in low doses. In liver cirrhosis, the concentration of losartan in the blood plasma increases significantly.

During treatment, potassium levels in the blood should be regularly monitored, especially in elderly patients with impaired renal function.

The simultaneous use of losartan with potassium-sparing diuretics should be avoided.

Overdose

Marked decrease in blood pressure, change in heart rate (HR) (tachycardia or bradycardia due to parasympathetic (vagal) stimulation).

Side effects Losartan-Richter 50 mg 30 pcs. film-coated tablets

From the hematopoietic system: rarely - anemia, thrombocytopenia.

From the nervous system: often - dizziness, headache, sleep disturbance, insomnia; uncommon - anxiety, drowsiness, memory impairment, peripheral neuropathy, paresthesia, hypoesthesia, migraine, tremor, ataxia, depression, syncope, acute cerebrovascular accident.

From the side of the organ of vision: infrequently - impaired visual acuity, conjunctivitis.

On the part of the hearing organ: infrequently - ringing in the ears.

From the cardiovascular system: often - palpitations, tachycardia, bradycardia, arrhythmia; infrequently - angina pectoris, orthostatic hypotension (dose-dependent).

From the respiratory system: often - cough, upper respiratory tract infections (pharyngitis, rhinitis, sinusitis, bronchitis), swelling of the nasal mucosa; infrequently - dyspnea.

From the digestive system: often - nausea, diarrhea, abdominal pain, dyspeptic disorders; uncommon - taste disturbance, anorexia, dry mouth, vomiting, flatulence, constipation, gastritis, liver dysfunction; rarely - hepatitis.

From the urinary system: uncommon - urinary tract infections, impaired renal function, urinary urgency, acute renal failure.

From the genital organs and mammary gland: infrequently - decreased libido, impotence.

From the skin and subcutaneous tissues: uncommon - dry skin, erythema, skin hyperemia, photosensitivity, increased sweating, alopecia.

From the musculoskeletal system: often - muscle cramps in the lower extremities, myalgia, pain in the back, chest, legs; uncommon - arthritis, arthralgia, fibromyalgia, rhabdomyolysis.

Allergic reactions: rarely - skin rash, urticaria, itching, angioedema (including swelling of the larynx and tongue), Quincke's edema, allergic vasculitis, Henoch-Schönlein purpura.

From laboratory and instrumental data: often - hypokalemia; infrequently - moderate increase in the concentration of urea and creatinine in the blood serum, hypoglycemia, hyponatremia, hyperuricemia; very rarely - increased activity of liver enzymes, hyperbilirubinemia.

Other: often - asthenia, increased fatigue.

Drug interactions

When used simultaneously with diuretics in high doses, arterial hypotension is possible.

When used simultaneously with potassium preparations and potassium-sparing diuretics, the risk of developing hyperkalemia increases.

When used simultaneously with indomethacin, the effectiveness of losartan may be reduced.

There is a report of the development of lithium intoxication when used simultaneously with lithium carbonate.

When used simultaneously with orlistat, the antihypertensive effect of losartan decreases, which can lead to a significant increase in blood pressure and the development of a hypertensive crisis.

When used simultaneously with rifampicin, the clearance of losartan increases and its effectiveness decreases.

Directions for use and doses

Orally, 1 time per day, regardless of meals.

Arterial hypertension

In most cases, the initial and maintenance dose is 50 mg 1 time per day. The maximum antihypertensive effect is achieved after 3–6 weeks of taking the drug. If necessary, the dose of the drug can be increased to 100 mg/day (in 1–2 doses).

While taking large doses of diuretics, it is recommended to start therapy with Losartan-Richter with 25 mg (1/2 tablet of 50 mg each) per day in one dose.

No dose adjustment is required for elderly patients or patients with impaired renal function, including patients on hemodialysis.

Patients with impaired liver function should be prescribed lower doses of the drug.

Chronic heart failure (if therapy with ACE inhibitors is ineffective)

The initial dose of Losartan-Richter is 50 mg 1 time per day in one dose. In the future, hydrochlorothiazide may be added in low doses and/or the dose of Losartan-Richter may be increased to 100 mg per day.

Kidney protection in patients with type 2 diabetes mellitus with proteinuria

The initial dose of Losartan-Richter is 50 mg 1 time per day in one dose. During treatment, depending on blood pressure levels, the daily dose of the drug can be increased to 100 mg in 1–2 doses.

Chronic heart failure

For the treatment of chronic heart failure, the initial dose of the drug is 12.5 mg (losartan can be used in another dosage form - 12.5 mg tablets) in one dose.

In order to achieve the usual maintenance dose of 50 mg/day, the dose of Losartan-Richter must be increased gradually, at intervals of 1 week (for example, 12.5, 25, 50 mg once daily). Losartan-Richter is usually prescribed in combination with diuretics and cardiac glycosides.

The dose of the drug should be increased according to the following scheme:

- 1st week - from 1st to 7th day - 1 tablet. 12.5 mg 1 time per day;

- 2nd week - from the 8th to the 14th day - 1/2 tablet. 50 mg 1 time per day;

— 3rd week — from the 15th to the 21st day — 1 tablet. 50 mg 1 time per day;

— 4th week — from the 22nd to the 28th day — 1 tablet. 50 mg 1 time per day.

Losartan-Richter

Hypersensitivity reactions

Angioedema may occur.

Arterial hypotension and water-electrolyte imbalance

In the presence of hypovolemia (for example, during therapy with large doses of diuretics), symptomatic arterial hypotension may develop. This condition must be corrected before starting a course of therapy with LOSARTAN-RICHTER or starting therapy with a lower dose.

In kidney disease with or without diabetes mellitus, water and electrolyte imbalances often occur, which must be corrected. In clinical studies conducted in patients with type 2 diabetes mellitus with proteinuria, losartan therapy increased the incidence of hyperkalemia compared with placebo. However, the level of hyperkalemia required discontinuation of the drug in only a small number of cases.

Liver dysfunction

In case of liver cirrhosis, according to pharmacokinetic studies, the concentration of losartan in the blood plasma increases significantly, therefore, those patients who have a history of liver pathology should be prescribed the drug at a lower dose.

Renal dysfunction

The drug, due to the suppression of the renin-angiotensin system, may worsen renal function, especially in those patients in whom the functional state of the kidneys is largely dependent on the renin-angiotensin-aldosterone system, for example, in the presence of severe CHF or pre-existing renal dysfunction.

Drugs that affect the renin-angiotensin-aldosterone system may increase plasma residual nitrogen or creatinine levels in patients with bilateral renal artery stenosis or arterial stenosis of a solitary kidney.

These changes in renal function may disappear after discontinuation of therapy.

During treatment with LOSARTAN-RICHTER, special attention should be paid to patients who have severe renal failure and patients after kidney transplantation, since the development of anemia was noted in these patients.

Hyperkalemia and water-salt imbalance

. During treatment with losartan, serum potassium levels should be monitored, especially in elderly patients.

Lactose intolerance

If you are lactose intolerant, please note that a 50 mg tablet of LOSARTAN-RICHTER contains 1.050 mg of lactose, a 100 mg tablet contains 2.10 mg of lactose.

Losartan-Richter tablet p/pl/o 50 mg N30 (Gedeon)

Losartan Richter is a specific angiotensin II receptor antagonist (type AT1). Angiotensin II selectively binds to AT1 receptors located in many tissues (vascular smooth muscle tissue, adrenal glands, kidneys and heart) and causes important biological effects, including. vasoconstriction and aldosterone release, as well as smooth muscle cell proliferation. In vitro and in vivo studies have shown that losartan and its pharmacologically active metabolite block all physiologically important effects of angiotensin II, regardless of the source or route of its synthesis. Does not inhibit kinase II, an enzyme that destroys bradykinin. Reduces total peripheral vascular resistance (TPVR), blood concentrations of norepinephrine and aldosterone, blood pressure (BP), pressure in the pulmonary circulation; reduces afterload and has a diuretic effect. Prevents the development of myocardial hypertrophy, increases exercise tolerance in patients with chronic heart failure (CHF). After a single oral dose, the hypotensive effect (decrease in systolic and diastolic blood pressure) reaches a maximum after 6 hours, then gradually decreases over 24 hours. Maximum hypotensive effect develops 3-6 weeks after the start of regular use of the drug. Losartan does not inhibit angiotensin-converting enzyme (ACE) and, accordingly, does not prevent the destruction of bradykinin, so losartan is not characterized by side effects indirectly associated with bradykinin (for example, angioedema). in patients with arterial hypertension with proteinuria (more than 2 g/day) without concomitant diabetes mellitus, the use of the drug significantly reduces proteinuria, excretion of albumin and immunoglobulins G. Losartan stabilizes the level of urea in the blood plasma. Does not affect autonomic reflexes. Losartan at a dose of up to 150 mg/day does not affect the level of triglycerides, total cholesterol and high-density lipoprotein (HDL) cholesterol in the blood serum in patients with arterial hypertension. At the same dose, losartan does not affect fasting blood glucose levels. Pharmacokinetics Absorption When taken orally, losartan is well absorbed and is metabolized during the “first pass” through the liver by carboxylation with the participation of the CYP2C9 isoenzyme of cytochrome P450 with the formation of a 10-40 times more active metabolite. Systemic bioavailability of losartan is about 33%. Cmax of losartan in blood plasma after oral administration is achieved after 1-1.5 hours, Cmax of its active metabolite - after 3-4 hours. Food intake does not affect the bioavailability of losartan. Distribution: 92% of losartan and 99% of its active metabolite are bound to blood plasma proteins, in mainly with albumins. Vd of losartan - 34 l. Losartan practically does not penetrate the blood-brain barrier. Metabolism: Approximately 14% of losartan taken orally by the patient is converted into an active metabolite. In a small number of patients (approximately 1%), a minimal amount of active metabolite is formed from losartan. Elimination: Plasma clearance of losartan is 600 ml/min, and of 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. Losartan and its active metabolite are characterized by linear pharmacokinetics when taken orally in doses up to 200 mg. After oral administration, plasma concentrations of losartan and its active metabolite decrease polyexponentially with a final T1/2 of losartan of about 2 hours, and of the active metabolite - about 6-9 hours. When taking the drug at a dose of 100 mg/neither losartan nor the active metabolite significantly accumulates in the blood plasma. Losartan and its metabolites are excreted from the body through the intestines and kidneys. 35% is excreted by the kidneys (of which 4% - unchanged and 6% - in the form of an active metabolite), the rest (60%) - through the intestines. In healthy volunteers, after ingestion of 14C isotope labeled losartan, the radioactive label was found in the urine in quantities about 35%, in feces - about 58%. Pharmacokinetics in special groups of patients In patients with mild to moderate alcoholic cirrhosis of the liver, the concentration of losartan was 5 times higher, and the active metabolite was 1.7 times higher than in healthy male volunteers. QC above 10 ml/min, the concentration of losartan in the blood plasma does not differ from that with normal renal function. In patients who require hemodialysis, the AUC value 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. Plasma concentrations of losartan and its active metabolite in the elderly men with arterial hypertension do not differ significantly from the values ​​of these parameters in young men with arterial hypertension. The values ​​of plasma concentrations of losartan in women with arterial hypertension are 2 times higher than the corresponding value in men with arterial hypertension. This pharmacokinetic difference is not clinically significant. The concentration of the active metabolite does not differ between men and women.