Losartan film-coated tablets 25 mg 30 pcs. in Moscow

Losartan film-coated tablets 25 mg 30 pcs. in Moscow

Losartan is a specific angiotensin II receptor (AT1 type) antagonist for oral administration. Angiotensin II selectively binds to AT1 receptors found in many tissues (vascular smooth muscle, adrenal glands, kidneys and heart) and performs several important biological functions, including vasoconstriction and aldosterone release. Angiotensin II also stimulates the proliferation of smooth muscle cells.

Losartan and its pharmacologically active metabolite (E 3174) both in vitro and in vivo block all physiological effects of angiotensin II, regardless of the source or route of synthesis. Losartan selectively binds to AT1 receptors: it does not bind to or block the receptors of other hormones and ion channels that play an important role in regulating the function of the cardiovascular system. In addition, losartan does not inhibit angiotensin-converting enzyme (ACE), which promotes the degradation of bradykinin, so side effects indirectly related to bradykinin (for example, angioedema) are rare.

When using losartan, the absence of negative feedback influence on renin secretion leads to an increase in plasma renin activity. An increase in renin activity leads to an increase in the concentration of angiotensin II in the blood plasma.

However, antihypertensive activity and a decrease in plasma aldosterone concentrations persist, indicating effective blockade of angiotensin II receptors. After discontinuation of losartan, plasma renin activity and angiotensin II concentration decreased within 3 days to the initial values ​​observed before starting the drug.

Losartan and its active metabolite have a high affinity for angiotensin II receptors (type AT1).

Plasma concentrations of losartan and its active metabolite, as well as the antihypertensive effect of losartan, increase with increasing dose of the drug.

The maximum antihypertensive effect develops 3-6 weeks after starting the drug.

In patients with arterial hypertension, proteinuria (more than 2 g per day), without diabetes mellitus, the use of the drug significantly reduces proteinuria, albumin and immunoglobulin G (IgG) excretion.

In postmenopausal women with arterial hypertension who took losartan at a dose of 50 mg/day for 4 weeks, there was no effect of therapy on the renal and systemic levels of prostaglandins.

Losartan does not affect autonomic reflexes and does not have a long-term effect on the level of norepinephrine in the blood plasma.

In patients with arterial hypertension, losartan in doses up to 150 mg per day does not cause clinically significant changes in the concentration of triglycerides, total cholesterol and high-density lipoprotein cholesterol. At the same doses, losartan has no effect on fasting blood glucose concentrations. Losartan caused a decrease in serum uric acid concentration (usually less than 0.4 mg/dL), which persisted during long-term therapy. In controlled clinical studies involving patients with arterial hypertension, there were no cases of drug withdrawal due to an increase in creatinine or potassium in the blood serum.

Instructions for use LOSARTAN

Hypersensitivity

Patients with a history of angioedema (swelling of the face, lips, larynx and/or tongue) should be closely monitored.

Arterial hypotension and water-electrolyte balance

In patients with reduced blood volume and/or sodium content, symptomatic hypotension may develop as a result of enhanced diuretic therapy, salt restriction, diarrhea and vomiting. These conditions should be corrected before starting the use of losartan or the initial dose of the drug should be reduced.

Double blockade of the RAAS

Dual blockade of the RAAS is accompanied by an increased risk of arterial hypotension, hyperkalemia and renal dysfunction (including acute renal failure) compared with monotherapy.

Dual blockade of the RAAS using an ACE inhibitor, an angiotensin II receptor antagonist and aliskiren cannot be recommended for any patient, especially patients with diabetic nephropathy.

In some cases, when the combined use of an ACE inhibitor and an angiotensin II receptor antagonist is absolutely indicated, careful supervision by a specialist and mandatory monitoring of renal function, water-electrolyte balance, and blood pressure are necessary. This applies to the prescription of candensartan or valsartan as adjunctive therapy to ACE inhibitors in patients with chronic heart failure. Carrying out double blockade of the RAAS under the careful supervision of a specialist and mandatory monitoring of renal function, water-electrolyte balance and blood pressure is possible in patients with chronic heart failure with intolerance to aldosterone antagonists (spironolactone), who have persistence of symptoms of chronic heart failure, despite other adequate therapy .

Electrolyte imbalance

It should be taken into account that electrolyte imbalances are common in patients with impaired renal function (with or without diabetes mellitus). According to data from a clinical study involving patients with type 2 diabetes mellitus and nephropathy, the incidence of hyperkalemia in the group receiving losartan was higher compared to the group receiving placebo. Therefore, potassium levels in the blood plasma and creatinine clearance should be carefully monitored, especially in patients with heart failure and creatinine clearance 30-50 ml/min.

It is not recommended to take losartan with potassium-sparing diuretics, potassium supplements, or potassium-containing salt substitutes.

Liver dysfunction

According to pharmacokinetic data, a significant increase in plasma concentrations of losartan was detected in patients with liver cirrhosis; therefore, patients with impaired liver function should be prescribed the drug in lower doses. Losartan should not be used in patients with severe liver dysfunction.

Renal dysfunction

Due to inhibition of the RAAS, renal dysfunction, including renal failure, has been reported with the drug (particularly in patients whose renal function is dependent on the activity of the RAAS, such as patients with severe heart failure or patients with existing renal impairment). As with the use of other drugs that affect the RAAS, increased serum urea and creatinine concentrations have been reported in patients with bilateral renal artery stenosis or arterial stenosis of a solitary kidney; these changes in renal function may be reversible after discontinuation of therapy. Losartan should be used with caution in the treatment of patients with bilateral renal artery stenosis or arterial stenosis of a solitary kidney.

When treating with losartan, renal function should be regularly monitored, because its violation is possible. This is especially true when losartan is used against the background of other pathological conditions (fever, dehydration) that may affect kidney function.

The simultaneous use of losartan and ACE inhibitors worsens renal function, so this combination is not recommended.

Kidney transplant

There is no experience using the drug to treat patients who have recently undergone kidney transplantation.

Primary hyperaldosteronism

In patients with primary hyperaldosteronism, antihypertensive drugs that act by inhibiting the RAAS are generally ineffective. Therefore, the use of losartan is not recommended.

IHD and cerebrovascular diseases

As with the use of other antihypertensive drugs, an excessive decrease in blood pressure in patients with coronary artery disease and cerebrovascular diseases can lead to the development of myocardial infarction or stroke.

Heart failure

As with other drugs that affect the RAAS, patients with heart failure with or without renal impairment are at risk of developing severe hypotension and (often acute) renal impairment.

There is insufficient therapeutic experience with losartan in patients with heart failure and concomitant severe renal impairment, in patients with severe heart failure (NYHA class IV), and in patients with heart failure and symptomatic, life-threatening cardiac arrhythmia. Therefore, losartan should be used with caution in this group of patients. Losartan should be used with caution in combination with beta-blockers.

Stenosis of the aortic and mitral valves, obstructive hypertrophic cardiomyopathy

As with the use of other vasodilators, the drug should be prescribed with extreme caution to patients with aortic or mitral valve stenosis or obstructive hypertrophic cardiomyopathy.

Lactose intolerance

The drug contains lactose. The drug should not be prescribed to patients with such rare hereditary pathologies as galactose intolerance, lapp lactase deficiency or glucose-galactose malabsorption.

Use in pediatrics

Losartan is contraindicated in children and adolescents under 18 years of age.

, since there is insufficient data regarding the use of the drug in this group of patients.

Ethnic differences

It has been established that ACE inhibitors, losartan and other angiotensin antagonists are significantly less effective in reducing blood pressure in patients of the Negroid race than in representatives of other races; This may be due to the fact that among black patients suffering from arterial hypertension, individuals with low renin activity predominate.

Impact on the ability to drive vehicles and operate machinery

Studies of the effect of the drug on the ability to drive a car and operate machinery have not been conducted. However, when driving or operating machinery, it is necessary to take into account that when using antihypertensive drugs, sudden onset of dizziness or drowsiness is possible, especially at the beginning of treatment or when the dose is increased.

Losartan tablets ppo 50 mg No. 90

Compound

1 film-coated tablet contains:

Pharmacokinetics

The antihypertensive drug is a specific antagonist of angiotensin II (type AT1) receptors. Does not inhibit kininase II, an enzyme that destroys bradykinin. Reduces total peripheral vascular resistance (TPVR), blood concentrations of norepinephrine and aldosterone, blood pressure (BP), pressure in the “lesser” 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 dose, the antihypertensive effect (systolic and diastolic blood pressure decreases) reaches a maximum after 6 hours, then gradually decreases over 24 hours.

The maximum antihypertensive effect develops 3-6 weeks after starting the drug. The concentration of losartan and its active metabolite in the blood plasma, as well as the antihypertensive effect of losartan, increases with increasing dose of the drug. Since losartan and its active metabolite are angiotensin II receptor antagonists (ARA II), they both contribute to the antihypertensive effect.

Indications for use

Arterial hypertension. Reduced risk of cardiovascular disease and mortality in patients with arterial hypertension and left ventricular (LV) hypertrophy, manifested by a cumulative reduction in the incidence of cardiovascular mortality, stroke and myocardial infarction; type 2 diabetes mellitus with proteinuria (reducing the risk of developing hypercreatininemia and proteinuria); CHF (if treatment with angiotensin-converting enzyme (ACE) inhibitors is ineffective).

Contraindications

Hypersensitivity to any component of the drug, severe liver dysfunction (more than 9 points on the Child-Pugh scale) (no experience with use), pregnancy, breastfeeding, age under 18 years (efficacy and safety of use have not been established), simultaneous use with aliskiren or aliskiren-containing drugs in patients with diabetes mellitus and/or impaired renal function (glomerular filtration rate (GFR) less than 60 ml/min/1.73 m2), lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (the drug contains lactose).

With caution: Hypotension, fluid and electrolyte imbalance, hyperkalemia, decreased circulating blood volume (CBV), liver dysfunction (less than 9 points on the Child-Pugh scale), severe renal dysfunction, bilateral renal artery stenosis or stenosis of the artery of a single kidney (presented in the “Special Instructions” section, condition after kidney transplantation (no experience with use), aortic or mitral stenosis, hypertrophic obstructive cardiomyopathy, heart failure with concomitant severe renal impairment, severe CHF IV functional class according to the NYHA classification, heart failure with threatening arrhythmias, coronary heart disease, cerebrovascular diseases, primary hyperaldosteronism, history of angioedema.

Directions for use and doses

Orally, regardless of food intake, the frequency of administration is 1 time per day.

For arterial hypertension, the average daily dose is 50 mg. If necessary, the daily dose can be increased to a maximum daily dose of 100 mg once a day.

Reducing the risk of cardiovascular disease and mortality in patients with arterial hypertension and LV hypertrophy: initial dose - 50 mg 1 time per day, subsequently it is recommended to additionally prescribe hydrochlorothiazide in low doses or increase the dose to 100 mg 1 time per day (taking into account the degree decrease in blood pressure).

Diabetes mellitus type 2 with proteinuria: initial dose - 50 mg 1 time per day with a further increase in dose to 100 mg/day (taking into account the degree of blood pressure reduction). CHF: the initial dose for patients with CHF is 12.5 mg 1 time per day.

As a rule, the dose is doubled at weekly intervals (i.e. 12.5, 25, 50 mg/day) to an average maintenance dose of 50 mg/day, 100 mg/day to a maximum (for this indication only) dose of 150 mg/day depending on individual tolerance.

Special groups of patients: When prescribed to patients receiving high doses of diuretics, the initial dose should be reduced to 25 mg/day. Patients with a history of impaired liver function should be prescribed lower doses of LOSARTAN.

In elderly patients, as well as those with impaired renal function (including those on dialysis), there is no need to adjust the initial dose. Losartan can be prescribed together with other antihypertensive drugs.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children.

Best before date

3 years.
Do not use after the expiration date stated on the package.

special instructions

In patients with dehydration (for example, those receiving treatment with high doses of diuretics), symptomatic arterial hypotension may occur at the beginning of treatment with LOSARTAN (dehydration must be corrected before prescribing LOSARTAN or starting treatment with a lower dose).

In patients with liver cirrhosis, the plasma concentration of LOSARTAN increases significantly, and therefore, in the presence of a history of liver disease, it should be prescribed in lower doses. Drugs that affect the kinin-angiotensin system may increase blood urea and serum creatinine concentrations in patients with bilateral renal stenosis or arterial stenosis of a solitary kidney. Condition after kidney transplantation. There is no experience with the use of the drug LOSARTAN in patients with a condition after kidney transplantation.

Aortic or mitral stenosis, hypertrophic obstructive cardiomyopathy. As with all drugs that have a vasodilating effect, angiotensin II receptor antagonists (ARA II) should be administered with caution to patients with aortic or mitral stenosis, or hypertrophic obstructive cardiomyopathy. Chronic heart failure. As with the use of other drugs that act on the RAAS, in patients with CHF and with or without impaired renal function, there is a risk of developing severe arterial hypotension or acute renal failure. There is no experience with the use of LOSARTAN in patients with heart failure and concomitant severe renal failure, in patients with severe heart failure (NYHA functional class IV), as well as in patients with heart failure and symptomatic life-threatening arrhythmias. Therefore, LOSARTAN should be prescribed with caution to patients in these groups. Coronary heart disease (CHD), cerebrovascular diseases. Like all drugs that have a vasodilating effect, ARA II should be prescribed with caution to patients with coronary artery disease or cerebrovascular diseases, since an excessive decrease in blood pressure in this group of patients can lead to the development of myocardial infarction or stroke.

Primary hyperaldosteronism. Patients with primary hyperaldosteronism, as a rule, do not respond positively to therapy with antihypertensive drugs that act by inhibiting the RAAS, therefore the use of LOSARTAN is not recommended in this group of patients.

History of angioedema. In patients with a history of angioedema taking LOSARTAN, hypersensitivity reactions were observed in clinical practice in the post-marketing period: rarely observed angioedema involving the larynx and pharynx, causing airway obstruction, and/or angioedema of the face, lips, pharynx and/or tongue .

Children. The safety and effectiveness of the drug in children have not been established. Elderly patients Clinical trials have not revealed any differences in the safety and effectiveness of losartan in elderly patients.

Description

12.5 mg tablets are round, biconvex, white film-coated tablets. On cross-section, the tablet is white or almost white.

25 mg tablets are round, biconvex, white film-coated tablets, scored. On cross-section, the tablet is white or almost white.

Tablets 50 mg are round, biconvex, white film-coated tablets, scored. On cross-section, the tablet is white or almost white.

100 mg tablets are round, biconvex, yellow film-coated tablets with a score line. On a cross section, two layers are visible, the inner layer is white or almost white.

Conditions for dispensing from pharmacies

On prescription

Dosage form

Film-coated tablets.

Manufacturer and organization accepting consumer complaints

PRANAFARM, LLC

Pharmacodynamics

The antihypertensive drug is a specific antagonist of angiotensin II (type AT1) receptors. Does not inhibit kininase II, an enzyme that destroys bradykinin. Reduces total peripheral vascular resistance (TPVR), blood concentrations of norepinephrine and aldosterone, blood pressure (BP), pressure in the “lesser” 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 dose, the antihypertensive effect (systolic and diastolic blood pressure decreases) reaches a maximum after 6 hours, then gradually decreases over 24 hours.

The maximum antihypertensive effect develops 3-6 weeks after starting the drug. The concentration of losartan and its active metabolite in the blood plasma, as well as the antihypertensive effect of losartan, increases with increasing dose of the drug. Since losartan and its active metabolite are angiotensin II receptor antagonists (ARA II), they both contribute to the antihypertensive effect.

Side effects

Frequency of adverse events (AE): more than 10% - very common; more than 1% but less than 10% - frequent; more than 0.1% but less than 1% - infrequent; more than 0.01% but less than 0.1% - rare; less than 0.01% - very rare; frequency unknown—it is not possible to estimate the frequency based on the available data.

From the nervous system and sensory organs: frequent - systemic dizziness (vertigo), asthenia, increased fatigue, headache, insomnia; uncommon - anxiety, sleep disturbances, drowsiness, memory disorders, peripheral neuropathy, paresthesia, hypoesthesia, tremor, ataxia, loss of consciousness, ringing in the ears, changes in vision, conjunctivitis; rarely - fainting; frequency unknown - depression, migraine, taste disturbance.

From the respiratory system: common - nasal congestion, cough, upper respiratory tract infections (fever, sore throat, sinusopathy*, sinusitis, pharyngitis); Uncommon: shortness of breath, bronchitis, rhinitis.

From the digestive system: frequent - nausea, diarrhea*, dyspepsia*, abdominal pain; infrequently - loss of appetite, dryness of the oral mucosa, toothache, vomiting, flatulence, gastritis, constipation; rarely - hepatitis; frequency unknown - pancreatitis, liver dysfunction.

From the musculoskeletal system: frequent - convulsions, myalgia*, pain in the back, chest, legs; uncommon - arthralgia, pain in the shoulder, knee, arthritis, fibromyalgia.

From the cardiovascular system (CVS): uncommon - orthostatic hypotension (dose-dependent), palpitations, tachy- or bradycardia, arrhythmias, angina pectoris; rarely - atrial fibrillation, cerebrovascular accident; frequency unknown - anemia.

From the hematopoietic system: rarely - vasculitis (including Henoch-Schönlein purpura); frequency unknown - thrombocytopenia.

From the genitourinary system: infrequent - urinary urgency, urinary tract infections, renal dysfunction, decreased libido, erectile dysfunction / impotence.

From the skin: infrequent - dryness, skin hyperemia, increased sweating, alopecia; frequency unknown photosensitivity. Allergic reactions: uncommon - urticaria, skin rash, itching, angioedema, incl. face, lips, pharynx and/or tongue.

Other: frequent - hyperkalemia, increased concentrations of creatinine, urea and potassium in the blood; uncommon - edema, fever, gout, increased activity of liver transaminases and hyperbilirubinemia; frequency unknown - rhabdomyolysis, hyponatremia, hypoglycemia. * - side effects are marked, the incidence of which is comparable to placebo. The association of side effects that occur in less than 1% of cases with the use of losartan has not been proven.

Use during pregnancy and breastfeeding

The use of drugs that affect the renin-angiotensin-aldosterone system (RAAS) in the II-III trimesters of pregnancy reduces renal function and increases the morbidity and mortality of the fetus and newborns. The development of oligohydramnios may be associated with fetal lung hypoplasia and skeletal bone deformities. Possible adverse events in neonates include calvarial hypoplasia, anuria, hypotension, renal failure and death.

If pregnancy is diagnosed, the drug should be discontinued immediately. The above-mentioned undesirable outcomes are usually caused by the use of drugs that affect the RAAS in the second and third trimester of pregnancy. Most epidemiological studies examining the development of fetal abnormalities after the use of antihypertensive drugs in the first trimester of pregnancy have not revealed differences between drugs affecting the RAAS and other antihypertensive drugs.

When prescribing antihypertensive therapy to pregnant women, it is important to optimize possible outcomes for the mother and fetus. If it is impossible to choose an alternative therapy instead of therapy with drugs that affect the RAAS, it is necessary to inform the patient about the possible risk of therapy to the fetus. Periodic ultrasound examinations are necessary to assess the condition of the intra-amniotic space. Depending on the week of pregnancy, appropriate fetal tests are necessary.

When prescribed during lactation, a decision should be made to stop breastfeeding or discontinue treatment with losartan.

Interaction

Strengthens (mutually) the effect of other antihypertensive drugs (diuretics, beta-blockers, sympatholytics). Increases the risk of hyperkalemia when used together with potassium-sparing diuretics (eplerenone, spironolactone, triamterene, amiloride) and potassium preparations (K+).

In patients with dehydration (previous treatment with large doses of diuretics), symptomatic arterial hypotension may occur. There were no clinically significant interactions with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, phenobarbital, or warfarin. Can be prescribed with other antihypertensive drugs, insulin and other hypoglycemic agents (sulfonylurea derivatives, glitazones and glucosidase inhibitors).

Reduces the excretion of lithium, therefore, when used simultaneously with lithium preparations, it is necessary to carefully monitor the concentration of lithium in the blood serum. Concomitant use with non-steroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase-2 (COX-2) inhibitors, may weaken the effect of LOSARTAN, and simultaneous use of these drugs should be carried out with caution in patients with impaired renal function.

Dual blockade of the RAAS with the use of ARB II, ACE inhibitors or aliskiren (renin inhibitor) is associated with an increased risk of arterial hypotension, hyperkalemia and renal dysfunction (including the development of acute renal failure) compared with monotherapy. Monitoring of blood pressure, renal function and blood electrolyte levels is necessary in patients taking losartan and other drugs that affect the RAAS. LOSARTAN should not be used concomitantly with aliskiren or aliskiren-containing drugs in patients with diabetes mellitus and/or renal impairment (GFR less than 60 ml/min/1.73 m2). Rifampin, being an inducer of drug metabolism, reduces the concentration of the active metabolite of losartan in the blood. The clinical significance of this interaction has not been established. Fluconazole, an inhibitor of the CYP2C9 isoenzyme, reduces the concentration of the active metabolite of losartan, but the pharmacodynamic significance of the simultaneous use of losartan and inhibitors of the CYP2C9 isoenzyme has not been studied. It has been shown that patients who do not metabolize losartan into the active metabolite have a very rare and specific defect in the CYP2C9 isoenzyme. These data suggest that the metabolism of losartan to the active metabolite is carried out by the CYP2C9 isoenzyme, and not by the CYP3A4 isoenzyme.

Overdose

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

Treatment: forced diuresis, symptomatic therapy; hemodialysis is ineffective.

Impact on the ability to drive vehicles and operate machinery

No adverse effects of losartan on the ability to drive vehicles or operate machinery have been identified. However, it is known that the drug LOSARTAN can cause dizziness and drowsiness, as a result of which during its use it is necessary to exercise caution when performing work that requires increased attention and when driving vehicles.