Losartan, 12.5 mg, film-coated tablets, 30 pcs.

Losartan

Hypersensitivity reactions

In patients with a history of angioedema (swelling of the face, lips, pharynx/larynx and/or tongue), monitoring of the use of the drug is necessary.

Embryotoxicity

The use of drugs that affect the RAAS during the second and third trimester of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and mortality. The development of oligohydramnios may be associated with fetal lung hypoplasia and skeletal deformation. Possible adverse events in neonates include calvarial hypoplasia, anuria, hypotension, renal failure and death. If pregnancy is established, losartan should be discontinued immediately (see Use during pregnancy and breastfeeding).

Arterial hypotension and water-electrolyte imbalance or decreased circulating blood volume (CBV)

In patients with reduced blood volume (for example, those receiving treatment with large doses of diuretics), symptomatic arterial hypotension may occur. Correction of such conditions must be carried out before prescribing losartan or starting treatment with a lower dose of the drug (see Dosage and Administration). Fluid and electrolyte imbalance is common in patients with impaired renal function with or without diabetes mellitus, so careful monitoring of these patients is necessary.

During treatment with losartan, it is not recommended to take potassium-sparing diuretics, potassium supplements, or potassium-containing salt substitutes without prior consultation with your doctor.

Aortic or mitral stenosis, hypertrophic obstructive cardiomyopathy

Like all drugs that have a vasodilating effect, ARA II should be prescribed with caution to patients with aortic or mitral stenosis or hypertrophic obstructive cardiomyopathy.

Coronary heart disease and cerebrovascular diseases

Like all drugs that have a vasodilating effect, ARA II should be prescribed with caution to patients with coronary heart 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.

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 dysfunction. Since there is insufficient experience with the use of losartan in patients with heart failure and concomitant severe renal impairment, in patients with severe heart failure (NYHA functional class IV), as well as in patients with heart failure and symptomatic life-threatening arrhythmias, losartan should be prescribed with caution in patients of these groups.

Primary hyperaldosteronism

Since patients with primary hyperaldosteronism generally do not respond well to therapy with antihypertensive drugs that act by inhibiting the RAAS, the use of losartan is not recommended in this group of patients.

Liver dysfunction

Data from pharmacokinetic studies indicate that plasma concentrations of losartan in patients with liver cirrhosis are significantly increased, so patients with a history of impaired liver function should be prescribed the drug at a lower dose. There is no experience with the use of losartan in patients with severe liver dysfunction, so the drug should not be used in this group of patients).

Renal dysfunction

Due to inhibition of the RAAS, changes in renal function, including the development of renal failure, have been observed in some susceptible patients. These changes in renal function may return to normal after treatment is stopped.

Some drugs that affect the RAAS may increase blood urea and serum creatinine concentrations in patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney. Similar effects have been reported with losartan.

Such renal dysfunction may be reversible after discontinuation of therapy.

Dual blockade of the renin-angiotensin-aldosterone system (RAAS)

The simultaneous use of angiotensin II receptor antagonists with drugs containing aliskiren is contraindicated in patients with diabetes mellitus and/or with moderate or severe renal impairment (GFR less than 60 ml/min/1.73 m2 body surface area) and is not recommended in other patients.

Concomitant use of angiotensin II receptor antagonists with ACE inhibitors is contraindicated in patients with diabetic nephropathy and is not recommended in other patients.

Special patient groups

Race

The ability of losartan, compared with atenolol, to reduce the risk of stroke and myocardial infarction, as well as reduce cardiovascular mortality in patients with hypertension and left ventricular hypertrophy, does not apply to black patients, although both treatment regimens effectively reduced blood pressure in these patients.

Children and teenagers

The effectiveness and safety of losartan in children and adolescents under 18 years of age have not been established.

If oliguria or arterial hypotension develops in newborns whose mothers took losartan during pregnancy, symptomatic therapy aimed at maintaining blood pressure and renal perfusion is necessary. Blood transfusions or dialysis may be required to prevent hypotension and/or maintain renal function.

Elderly patients

Clinical studies have not revealed any particularities regarding the safety and effectiveness of losartan in elderly patients (over 65 years of age).

Lactose

The drug contains lactose monohydrate. It must be taken into account that the use of the drug is contraindicated in patients with rare congenital galactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Features of the action of the drug at the first dose

Patients with reduced blood volume (for example, when taking high doses of diuretics, limiting salt intake, diarrhea or vomiting) may develop symptomatic hypotension, especially after taking the first dose and after increasing the dose of the drug.

Features of the action of the drug upon its withdrawal

You should not stop taking the drug without consulting a doctor, as symptoms may return.

Features of the actions of a doctor (paramedic) or patient when one or more doses of a drug are missed

If you miss a dose of the drug, you must take the next dose at your usual time. Do not take a double dose to make up for a missed dose.

pharmachologic effect

Losartan is a selective, competitive antagonist and AT1 receptor blocker in various tissues, including the brain, adrenal cortex, liver, kidneys, heart and vascular smooth muscle, reducing the effect of angiotensin II development.

Administration of the active substance of the drug leads to a decrease in total peripheral resistance (afterload) and cardiac venous return (preload). All physiological effects of angiotensin II, including stimulation of aldosterone , are blocked by the action of Losartan. A decrease in blood pressure occurs regardless of the state of the renin-angiotensin . As a result of the use of this drug, plasma renin activity increases due to the removal of angiotensin II.

The effect of this drug was confirmed during the Life study (Losartan Intervention For Endpoint reduction in hypertension study), which involved 9,193 people suffering from essential arterial hypertension . The age of the subjects was 55-80 years with a blood pressure of 160-200 mm Hg. After taking Losartan, this figure decreased by 13%, and mortality among such patients decreased by 25%.

Side effects of the drug Losartan Sandoz

For essential hypertension (arterial hypertension) in controlled clinical trials, dizziness was the only adverse reaction associated with the use of losartan, which occurred more often than with placebo (in ≥1% of patients). Dose-related orthostatic effects were observed in less than 1% of patients. The most common side effects associated with the use of losartan in patients with hypertension (arterial hypertension) and left ventricular hypertrophy were dizziness, asthenia, and fatigue. In patients with type II diabetes mellitus, the most common side effects associated with the use of the drug were asthenia, fatigue, dizziness, hypotension and hyperkalemia. In addition, the following side effects have been reported. Hypersensitivity reactions: rarely - angioedema, including swelling of the larynx, lips and tongue, which can lead to airway obstruction. Some of these patients had indications of angioedema with the use of other drugs, including a history of ACE inhibitors. Rare cases of vasculitis, including Henoch-Schönlein purpura, have been reported. Cardiovascular: palpitations, tachycardia. Gastrointestinal: diarrhea, dyspepsia, nausea; hepatitis (very rare), abnormal liver function tests (ALT returned to normal after discontinuation of the drug). Hematological: anemia. Musculoskeletal system: myalgia; back pain, muscle cramps. Nervous system: discomfort, headache, insomnia, migraine. Skin: urticaria, itching. Respiratory: cough, rhinitis, pharyngitis, sinusitis, upper respiratory tract infections. Other: abdominal pain, asthenia, fatigue, chest pain, edema. Effect on laboratory test results Rare: hyperkalemia (serum potassium level 5.5 mEq/L). The risk of hyperkalemia is increased in patients with type II diabetes mellitus.

Pharmacodynamics and pharmacokinetics

This drug has a hypotensive effect immediately after the first oral administration. The effect of the drug is expressed in a decrease in systolic and diastolic blood pressure, which is achieved at most 6 hours after administration. After a day, the effect of the drug decreases. A stable hypotensive effect is observed after 3-6 weeks of taking Losartan.

In people suffering from arterial hypertension, this drug reduces proteinuria albumin and immunoglobulin G excretion . In addition, the active substance helps stabilize the urea content in the blood plasma without affecting the content of norepinephrine in the blood plasma.

Losartan is characterized by excellent absorption from the gastrointestinal tract. Of no less importance is the ability of the active substance to be metabolized during a single passage through the liver by carboxylation with the participation of the CYP2C9 isoenzyme, which produces an active metabolite.

Systemic bioavailability of the active substance is approximately 33%. After approximately 60 minutes, the maximum concentration of the active substance in the blood serum is reached. The bioavailability of Losartan is not affected by food intake.

The degree of penetration of Losartan through the blood-brain barrier is minimal. Almost 99% of the substance binds to albumin and other blood plasma proteins.

Plasma clearance is approximately 600 ml/min and 50 ml/min. Renal clearance is approximately 74 ml/min and 26 ml/min. After taking the drug, approximately 4% of the dose taken is excreted through the kidneys unchanged and approximately 6% is excreted through the kidneys in the form of an active metabolite.

Basically, the active substance of this drug is excreted from the body through the kidneys and intestines.

Side effects

When taking this drug, side effects may occur, which can be classified into “common” and “rare”.

Common side effects include:

• pain in the abdominal area or stomach;
• state of anxiety;
• bladder pain;
• bloody spots in the urine;
• blurred vision;
• chills;
• cold sweat;
• coma;
• confusion of thoughts;
• pale skin;
• depression;
• difficulty breathing;
• painful urination;
• dizziness;
• cardiopalmus;
• frequent urge to urinate;
• headache;
• increased feeling of hunger;
• irregular heartbeat;
• pain in various parts of the body;
• nausea or vomiting ;
• numbness or tingling in the arms, legs, lips;
• convulsions;
• slurred speech;
• unstable breathing during exercise;
• sudden and causeless hematomas;
• state of fatigue or weakness ;
• heaviness in the legs.

The following side effects occur much less frequently when taking Losartan:

• chest pain or discomfort;
• chest tightness or heaviness;
• malaise;
• increased heart rate;
• inability to speak;
• pain or discomfort in the neck;
• sweating;
• swelling of the face;
• temporary blindness;
• instability or awkwardness.

Interactions of the drug Losartan Sandoz

The drug can be prescribed with other antihypertensive drugs (diuretics, calcium channel blockers, β-adrenergic receptor blockers, etc.). Currently, no clinically significant interactions of losartan with hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole and erythromycin have been identified. Rifampicin and fluconazole can reduce the concentration of the active metabolite of losartan in the blood plasma. The clinical consequences of these interactions have not been assessed. The simultaneous use of potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium salt preparations, including table salt substitutes, can lead to an increase in potassium levels in the blood serum. NSAIDs, including selective COX-2 inhibitors, may reduce the antihypertensive effect of angiotensin II receptor antagonists. In some patients with moderate renal impairment who are being treated with NSAIDs, including COX-2 inhibitors, concomitant use of angiotensin II receptor antagonists may result in a further deterioration of renal function. These effects are usually reversible. The simultaneous administration of losartan and ACE inhibitors has not been studied sufficiently.

Indications for use

Indications for the use of Losartan are as follows:

• arterial hypertension (a condition of the body when blood pressure rises above 140 mm Hg);
• chronic heart failure (a pathological condition in which the activity of the cardiovascular system does not provide oxygen to the body, first during physical activity and then at rest);
• the risk of developing diseases of the cardiovascular system, in particular stroke ;
• diabetic nephropathy (a term that combines a complex of lesions of the arteries, arterioles, tubules and glomeruli of the kidneys, which develop as a result of metabolic disorders in the kidney tissues).

Losartan: analogues and substitutes

Today, the drug Losartan, its analogs and substitutes based on the mechanism of action and composition are sold through pharmacy chains with a prescription from a cardiologist or therapist. The cost of medicines varies from 10-20 rubles and more. Analogues of the drug are produced mainly in the form of tablets and are produced in Russia and abroad.

Analogues can be prescribed by a general practitioner or cardiologist if there are only appropriate indications. The basis for replacement may be the insufficient effectiveness of Losartan, as well as the manifestation of severe negative side effects and allergic reactions.

These drugs are not combined with each other, but can be included in complex therapeutic measures. It is important to pay attention to the country of origin and excipients of the composition.