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%.
Losartan tablets p/o 50 mg No. 10x3
Name
Losartan tablets, 50 mg, 30 pcs.
Description
Film-coated tablets, white or white with a yellowish tint, round, biconvex. The film coating on the surface of the tablets may be uneven.
Main active ingredient
Losartan.
Release form
Pills.
Dosage
50 mg.
pharmachologic effect
Losartan is a synthetic angiotensin II receptor (AT1 type) antagonist for oral use. Losartan does not have an agonistic effect and does not block other hormone receptors or ion channels that are involved in the regulation of the cardiovascular system. Moreover, losartan does not inhibit ACE (kinase II), an enzyme that promotes the breakdown of bradykinin. As a result, there is no potentiation for bradykinin-mediated side effects. During the use of losartan, elimination of the negative feedback reaction of angiotensin II on renin secretion leads to an increase in the level of angiotensin II in the blood plasma. Despite this increase, 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 levels return to baseline within 3 days. Both losartan and its active metabolite have a higher affinity for AT1 receptors than for AT2. The active metabolite is 10-40 times more active than losartan (based on weight).
Indications for use
Treatment of essential hypertension. Treatment of kidney disease in adult patients with arterial hypertension and type 2 diabetes mellitus with proteinuria ≥ 0.5 g / day - as part of antihypertensive therapy. Reducing the risk of stroke in adult patients with arterial hypertension and left ventricular hypertrophy confirmed by ECG.
Directions for use and doses
Losartan is taken orally with a glass of water. Losartan is taken orally regardless of food intake. Arterial hypertension The usual initial and maintenance dose for most patients is 50 mg once daily. The maximum antihypertensive effect is achieved 3-6 weeks after the start of treatment. In some patients, increasing the dose to 100 mg per day (in the morning) may be more effective. Losartan may be taken in combination with other antihypertensive drugs, especially diuretics (eg, hydrochlorothiazide). Patients with hypertension and type 2 diabetes mellitus (proteinuria ≥ 0.5 g/day) The usual starting dose is 50 mg once daily. The dose can be increased to 100 mg once daily, depending on blood pressure readings one month after the start of treatment. Losartan can be used with other antihypertensive drugs (eg, diuretics, calcium channel blockers, alpha- or beta-receptor blockers, centrally acting drugs), as well as with insulin and other commonly used hypoglycemic drugs (eg, sulfonylureas, glitazones and glucosidase inhibitors). Reducing the risk of stroke in patients with arterial hypertension and left ventricular hypertrophy confirmed by ECG The usual starting dose is 50 mg of losartan once daily. Depending on the decrease in blood pressure, a low dose of hydrochlorothiazide should be added to treatment and/or the dose of losartan should be increased to 100 mg once daily. Selected patient groups When prescribing the initial dose
Use during pregnancy and lactation
Pregnancy. Drugs that act directly on the renin-angiotensin system can cause fetal malformations or death. If pregnancy is diagnosed, Losartan should be discontinued immediately. The use of losartan is not recommended during the first trimester of pregnancy and is contraindicated during the second and third trimesters of pregnancy. Epidemiological data regarding the risk of teratogenicity after use of ACE inhibitors during the first trimester of pregnancy are inconclusive, but a slight increase in risk cannot be excluded. Since there are no controlled epidemiological data regarding the risk of angiotensin II receptor antagonists (ARAII), similar risks may exist for this class of drugs. Unless continued therapy with ARB II is considered necessary, patients planning pregnancy should be prescribed an alternative hypertensive therapy with an established safety profile for use during pregnancy. If pregnancy is diagnosed, treatment with losartan should be stopped immediately and, if necessary, alternative treatment should be initiated. It is known that the use of APAII during the second and third trimesters of pregnancy induces fetotoxicity (weakened renal function, oligohydramnios, delayed ossification of the skull bones) and neonatal toxicity (renal failure, hypotension, hyperkalemia). If losartan was used during the second trimester of pregnancy, an ultrasound examination is recommended to check kidney function and the condition of the skull bones. The condition of newborns whose mothers have used losartan should be frequently monitored for the occurrence of arterial hypotension. Lactation. Since there is no information regarding the use of losartan during breastfeeding, it is not recommended to use this drug during lactation. It is preferable to alternative treatment with drugs with a better studied safety profile for use during breastfeeding, especially when feeding newborns and premature infants.
Impact on the ability to drive a car and potentially dangerous mechanisms
There is no data regarding the effect of the drug on the ability to drive vehicles and other mechanisms. However, when driving vehicles and other mechanisms, you should remember the possibility of developing such adverse reactions as dizziness and drowsiness, especially at the beginning of treatment and when increasing the dose of the drug.
Precautionary measures
Fetal toxicity. Use of drugs that affect the renin-angiotensin system during the second and third trimesters of pregnancy impairs fetal renal function and increases the incidence of fetal and neonatal morbidity and mortality. The development of oligohydramnios may be associated with pulmonary hypoplasia and skeletal deformities in the fetus. Potential neonatal adverse reactions include calvarial hypoplasia, anuria, hypotension, renal failure and death. If pregnancy is established, use of the drug Losartan should be stopped immediately. Hypersensitivity. Angioedema. Patients with a history of angioedema (swelling of the face, lips, throat and tongue) should be monitored frequently. Arterial hypotension and water-electrolyte imbalance. Symptomatic hypotension, especially after the first dose of the drug or after dose increases, may occur in patients with reduced intravascular volume and/or sodium deficiency caused by the use of strong diuretics, dietary salt restriction, diarrhea or vomiting. Before starting treatment with losartan, such conditions should be corrected or the drug should be used at a lower initial dose. The same recommendations apply to children aged 6 to 18 years. Electrolyte imbalance. Electrolyte imbalance is often observed in patients with impaired renal function (with or without diabetes mellitus) and should be taken into account. It has been shown that when losartan was used in patients with type 2 diabetes mellitus and nephropathy, a high incidence of hyperkalemia was observed. Therefore, plasma potassium concentrations and creatinine clearance values should be checked frequently, especially in patients with heart failure and a creatinine clearance of 30-50 ml/min. The simultaneous use of losartan and potassium-sparing diuretics, potassium supplements and potassium-containing salt substitutes is not recommended. Liver dysfunction. Taking into account pharmacokinetic data indicating a significant increase in plasma concentrations of losartan in patients with cirrhosis, a dose reduction of the drug should be considered in patients with a history of impaired liver function. There is no experience with the use of losartan in patients with severe liver dysfunction. Therefore, losartan should not be used in patients with severe hepatic impairment. Losartan is not recommended for use in children with impaired liver function. Renal dysfunction. Changes in renal function, including renal failure, associated with inhibition of the renin-angiotensin system have been reported (especially in patients with renal function dependent on the renin-angiotensin-aldosterone system, that is, patients with severely impaired cardiac function or with pre-existing impaired renal function). As with other drugs that affect the renin-angiotensin-aldosterone system, increases in blood urea and serum creatinine levels have been reported in patients with bilateral renal artery stenosis or with 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 patients with bilateral renal artery stenosis or arterial stenosis of a solitary kidney. Use in children with impaired renal function. The drug is not recommended for use in children with glomerular filtration rate
Interaction with other drugs
Other antihypertensive drugs may enhance the hypotensive effect of losartan. Concomitant use with other drugs that can induce arterial hypotension as an adverse reaction (tricyclic antidepressants, antipsychotropic drugs, baclofen and amifostine) may increase the risk of hypotension. Losartan is metabolized primarily through the cytochrome P450 (CYP) 2C9 system to an active carboxylic acid metabolite. Fluconazole (a CYP2C9 inhibitor) was found to reduce exposure to the active metabolite by approximately 50%. It has been established that simultaneous treatment with losartan and rifampicin (an inducer of metabolic enzymes) leads to a 40% decrease in the concentration of the active metabolite in the blood plasma. The clinical significance of this effect is unknown. There is no difference in exposure when losartan is co-administered with fluvastatin (a weak CYP2C9 inhibitor). As with other drugs that block angiotensin II or its effects, concomitant use of drugs that retain potassium in the body (eg, potassium-sparing diuretics: spironolactone, triamterene, amiloride) or may increase potassium levels (eg, heparin), and Also, potassium supplements or potassium-containing salt substitutes may lead to increased serum potassium levels. The simultaneous use of such drugs is not recommended. A reversible increase in serum lithium concentrations, as well as toxicity, has been reported during concomitant use of lithium with ACE inhibitors. This adverse reaction has also been very rarely reported with the use of angiotensin II receptor antagonists (ARAII). Concomitant treatment with lithium and losartan should be carried out with caution. If use of such a combination is considered necessary, it is recommended that serum lithium levels be monitored during coadministration. With the simultaneous use of APAII and non-steroidal anti-inflammatory drugs (for example, selective cyclooxygenase-2 (COX-2) inhibitors, acetylsalicylic acid in doses that have an anti-inflammatory effect, non-selective NSAIDs), the antihypertensive effect may be weakened. Concomitant use of angiotensin II antagonists or diuretics with NSAIDs may lead to an increased risk of deterioration of renal function, including the possibility of acute renal failure, as well as an increase in serum potassium levels, especially in patients with existing renal impairment. This combination should be prescribed with caution, especially in elderly patients. Patients should be adequately hydrated and consideration should be given to monitoring renal function after initiation of concomitant therapy and periodically thereafter. Double blockade of the renin-angiotensin-aldosterone system. Clinical trial data have shown that dual blockade of the renin-angiotensin-aldosterone system (RAAS) due to concomitant use of ACE inhibitors, angiotensin II receptor blockers or aliskiren is associated with an increased incidence of hypotension, hyperkalemia and decreased renal function (including acute renal failure), including comparison with monotherapy with a drug acting on the RAAS.
Contraindications
Hypersensitivity to the active substance and any excipient included in the drug. Severe liver dysfunction. Second and third trimesters of pregnancy. Concomitant use of the drug Losartan with drugs containing aliskiren is contraindicated in patients with diabetes mellitus or impaired renal function (GFR).
Compound
Each tablet contains: active ingredient: losartan potassium salt - 50 mg; excipients: pregelatinized starch, croscarmellose sodium, colloidal anhydrous silicon dioxide, calcium stearate (E572), microcrystalline cellulose (E460), opadry II white (85F). Composition of opdray II white (85F) per 1 tablet: polyvinyl alcohol, partially hydrolyzed, macrogol/polyethylene glycol 3350, talc (E553b); titanium dioxide (E171).
Overdose
Symptoms. There is insufficient data on cases of drug overdose. The most likely manifestations of an overdose may be arterial hypotension and tachycardia. Bradycardia may occur due to parasympathetic (vagal) stimulation. Treatment. If hypotension occurs, supportive treatment should be provided. Treatment depends on the length of time after taking the drug and the nature and severity of symptoms. The priority measure should be to stabilize the cardiovascular system. After oral administration of the drug, the use of activated carbon in an appropriate dose is indicated. Later, vital signs should be monitored frequently and adjusted if necessary. Losartan and the active metabolite are not excreted from the body by hemodialysis. The drug is not recommended for children with glomerular filtration rate
Side effect
The frequency of the adverse reactions listed below is defined as the following: very common: 1/10; often: from 1/100 to
Storage conditions
Store in a place protected from moisture and light at a temperature not exceeding 25°C. Keep out of the reach of children.
Buy Losartan tablet p/o 50 mg in container pack No. 10x3 in the pharmacy
Price for Losartan tablet p/o 50 mg in container pack No. 10x3
Instructions for use for Losartan tablet p/o 50 mg in container pack No. 10x3
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.
Losartan FT
- Hypersensitivity reactions Patients with a history of angioedema (swelling of the face, lips, pharynx, tongue) should be under strict supervision (see sections “Side effects”, “Contraindications”). Hypotension and electrolyte imbalance When circulating blood volume decreases and/or blood sodium levels decrease (hyponatremia), such as due to intensive use of diuretics, dietary salt restriction, diarrhea or vomiting, symptomatic hypotension may occur, especially after taking the first dose of the drug and after increasing the dose. These conditions must be corrected before starting the use of the drug LOSARTAN FT, or the use of the drug LOSARTAN FT should be started with a lower dose (see section “Dosage and Administration”). This information also applies to children aged 6-18 years. Electrolyte imbalances Electrolyte imbalances are common in patients with impaired renal function with or without diabetes and should be looked out for. In patients with type II diabetes mellitus in combination with nephropathy, hyperkalemia may develop while using losartan (see section "Side effects"). Careful monitoring of plasma potassium concentrations and creatinine clearance is necessary, especially in patients with heart failure and creatinine clearance of 30-50 ml/min. The simultaneous use of the drug LOSARTAN FT with potassium-sparing diuretics, potassium supplements and potassium-containing salt substitutes is not recommended (see section “Interaction with other drugs and other forms of interaction”). Liver dysfunction In persons with liver cirrhosis, a significant increase in the concentration of losartan in the blood plasma was detected. A lower dose of losartan should be considered if there is a history of mild to moderate hepatic impairment. Due to the lack of experience in the therapeutic use of losartan in severe liver dysfunction, LOSARTAN FT is contraindicated in patients with severe liver dysfunction (see sections “Method of administration and dosage”, “Contraindications” and “Pharmacological properties”). The use of losartan in children with impaired liver function is not recommended (see section "Method of administration and dosage"). Renal Impairment As a consequence of inhibition of the renin-angiotensin-aldosterone system, renal impairment, including renal failure, has been reported (particularly in patients whose renal function is dependent on the activity of the renin-angiotensin-aldosterone system, e.g. who have severe heart failure or previously documented renal dysfunction). As with other drugs that affect the renin-angiotensin-aldosterone system, increases in blood urea and serum creatinine levels have been reported in patients with bilateral renal artery stenosis or solitary renal artery stenosis; These changes in renal function may be reversible after discontinuation of therapy. Losartan should be used with caution in patients with bilateral renal artery stenosis or arterial stenosis of a solitary kidney. The use of losartan in children with a glomerular filtration rate <30 ml/min/1.73 m2 is not recommended, since there are no available data on use in this category of patients (see also section “Dosage and Administration”). Renal function should be regularly monitored while using losartan, as renal function may deteriorate. This is especially necessary if losartan is used against the background of fever, dehydration and other conditions that can lead to impaired renal function. It has been shown that the simultaneous use of losartan and ACE inhibitors leads to renal dysfunction. Therefore, the simultaneous use of these drugs is not recommended (see section “Interaction with other drugs and other forms of interaction”). Kidney transplantation There is no experience with patients who have recently undergone kidney transplantation. Primary hyperaldosteronism In patients with primary hyperaldosteronism, therapy with antihypertensive agents that act through inhibition of the renin-angiotensin system is usually ineffective. Therefore, the use of the drug LOSARTAN FT is not recommended in this category of patients. Coronary heart disease and cerebrovascular disease As with any antihypertensive drug, losartan may cause an excessive decrease in blood pressure, which in patients with coronary heart disease and/or cerebrovascular disease can lead to myocardial infarction or stroke. Heart failure In patients with heart failure with or without renal impairment, as with other drugs acting on the renin-angiotensin system, there is a risk of severe hypotension and renal impairment (often acute). There is insufficient experience with the use of losartan in patients with heart failure in combination with severe renal impairment, in patients with severe heart failure (NYHA class IV), in patients with heart failure in combination with symptomatic, life-threatening arrhythmias. Therefore, losartan should be used with caution in these categories of patients. Concomitant use of losartan and a β-blocker also requires caution. Aortic and mitral valve stenosis, obstructive hypertrophic cardiomyopathy As with other vasodilators, special caution should be exercised in patients with aortic or mitral valve stenosis or obstructive hypertrophic cardiomyopathy. Auxiliary components This medicine contains lactose. Patients with rare hereditary disorders such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this medicine. Before starting use, you should definitely consult your doctor. Ethnicity Losartan and other angiotensin antagonists, like ACE inhibitors, appear to be less effective in lowering blood pressure in black patients compared to representatives of other races. This phenomenon may be due to the fact that low renin activity is more common in the population of blacks with hypertension. Pregnancy Do not start therapy with losartan during pregnancy. Unless continued use of losartan is considered absolutely necessary, patients planning pregnancy should switch to other antihypertensive agents that have a favorable safety profile when used during pregnancy. If pregnancy is detected while using losartan, the use of the drug should be stopped immediately and, if necessary, another drug should be prescribed (see sections “Contraindications”, “Fertility, Pregnancy and Lactation”). Dual blockade of the renin-angiotensin-aldosterone system There is evidence that concomitant use of ACE inhibitors, angiotensin II receptor blockers or aliskiren increases the risk of hypotension, hyperkalemia and deterioration of renal function (including the development of acute renal failure). In this regard, double blockade of the renin-angiotensin-aldosterone system through the simultaneous use of ACE inhibitors, angiotensin II receptor blockers or aliskiren is not recommended (see sections “Interaction with other drugs and other forms of interaction”, “Contraindications”). In cases where dual blockade of the renin-angiotensin-aldosterone system is considered absolutely necessary, such therapy should only be carried out under specialist supervision and with frequent close monitoring of renal function, electrolyte levels and blood pressure. In patients with diabetic nephropathy, ACE inhibitors and angiotensin II receptor blockers should not be coadministered.
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).
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.
Losartan, instructions for use
Losartan tablets must be taken orally without reference to meals. The drug is available in the form of tablets that should be swallowed without chewing once a day.
Instructions for the use of Losartan for various diseases:
- Patients with arterial hypertension are prescribed a daily dose of 50 mg once a day. At the discretion of the attending physician, the daily dose can be increased to 100 mg per day.
- For chronic heart failure, Losartan is prescribed initially at 12.5 mg per day, after which the dose is doubled at weekly intervals.
- If it is necessary to reduce the risk of developing diseases of the cardiovascular system, the drug is prescribed at a dose of 50 mg per day.
- In case of liver failure, taking this drug is recommended at a minimum dose of 25 mg per day. The same dosage is prescribed to patients over 75 years of age.
During treatment of any disease with the use of Losartan, strict monitoring of blood pressure is necessary.
To increase the therapeutic effect, this drug must be taken at the same time, which is usually determined by a specialist. If one dose is missed, the next one should be taken at the time closest to the scheduled one, followed by adjustment of the time of taking the next dose. It is not recommended to take a double dose of this medicine.
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.
Interaction with other drugs
When certain drugs are used concomitantly with Losartan, this may lead to negative drug interactions. An interaction may occur if the drug is taken with medications such as potassium supplements, potassium-sparing diuretics, or nonsteroidal anti-inflammatory drugs. In addition, the body metabolizes drugs differently, so taking them together with this drug may cause an extreme increase in the content of active substances.
Losartan potassium may potentially interact with a number of other medicines. Some of them are:
Drug interactions with ACE inhibitors
Losartan works similarly to ACE inhibitors, although it is not one. Therefore, combining these drugs may increase the risk of high potassium levels ( hyperkalemia ), the development of kidney failure, and dangerously low blood pressure.
Drug interactions with diuretics
The combination of this drug with diuretics can cause a severe decrease in blood pressure. To reduce the risk of such a manifestation, the attending physician should adjust the dose of Losartan.
Potassium supplements or potassium salt substitutes
If you take this drug with products that contain potassium or a potassium salt substitute, your blood potassium levels may become too high. This can cause serious problems, including those with the cardiovascular system.
Potassium-sparing diuretics
When taking Losartan and potassium-sparing diuretics at the same time, the body may absorb them differently than intended, which will ultimately lead to an increase in potassium levels in the blood.
Rifampicin
In this case, the absorption of Losartan will occur differently than expected, which may lead to a decrease in the level of the active substance of the drug in the body.
Lithium
The simultaneous use of Losartan and lithium-containing drugs can lead to changes in metabolism and an increase in the level of lithium in the blood.
Nonsteroidal anti-inflammatory drugs (NSAIDs)
If the patient has kidney disease or renal failure, simultaneous use of this drug and NSAIDs may worsen the health condition and worsen the course of the disease.
Losartan, 12.5 mg, film-coated tablets, 30 pcs.
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 (see "Side effects"
).
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 deformities. Possible adverse events in neonates include calvarial hypoplasia, anuria, hypotension, renal failure and death.
When diagnosing pregnancy, the drug LOSARTAN should be taken immediately.
Arterial hypotension and fluid disturbances
-
electrolyte balance or decreased circulating blood volume
In patients with reduced circulating blood volume (CBV) (for example, receiving treatment with large doses of diuretics), symptomatic arterial hypotension may occur. Correction of such conditions must be carried out before prescribing the drug LOSARTAN or starting treatment with a lower dose of the drug LOSARTAN (see " Method of administration and dosage"
»)
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. In clinical studies in patients with type 2 diabetes mellitus with proteinuria, the incidence of hyperkalemia was greater in the LOSARTAN group than in the placebo group. Several patients discontinued therapy due to hyperkalemia (see “ Side Effects”)
»).
During treatment with LOSARTAN, it is not recommended to take potassium-sparing diuretics, potassium supplements or potassium-containing salt substitutes.
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, patients with CHF and with or without impaired renal function are at risk of developing severe hypotension or acute renal impairment.
Since there is insufficient experience with the use of the drug 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, the drug LOSARTAN should be prescribed with caution to patients in these groups.
Primary hyperaldosteronism
Since patients with primary hyperaldosteronism, as a rule, do not respond positively 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 the concentration of losartan in the blood plasma in patients with cirrhosis of the liver is significantly increased, therefore patients with a history of impaired liver function should be prescribed the drug LOSARTAN at a lower dose. There is no experience with the use of the drug LOSARTAN in patients with severe liver dysfunction, so the drug should not be used in this group of patients (see “ Pharmacological properties. Pharmacokinetics
";
" Contraindications
";
" Method of administration and dosage
").
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 when taking the drug LOSARTAN. Such renal dysfunction may be reversible after discontinuation of therapy. LOSARTAN should be used with caution in patients with bilateral renal artery stenosis or renal artery stenosis of a solitary kidney.
Special patient groups
Race
Analysis of data from the entire population of patients included in the LIFE study to study the effect of losartan on reducing the incidence of the main composite criterion of the study in patients with hypertension and left ventricular hypertrophy (n = 9193) showed that 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 (by 13.0%. p = 0.021) does not apply to patients of the Negroid race, although both treatment regimens effectively reduced blood pressure in these patients. In this study, the drug LOSARTAN, compared with atenolol, reduced cardiovascular morbidity and mortality in patients with hypertension and left ventricular hypertrophy of all races except blacks (n = 8660, p = 0.003). However, in this study, black patients receiving atenolol had a lower risk of the study's primary composite endpoint (i.e., lower combined incidence of cardiovascular death, stroke, and myocardial infarction) compared with race-matched patients receiving losartan (p= 0.03).
Children and teenagers
The effectiveness and safety of the drug 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).
Double renin blockade
-
angiotensin
-
aldosterone system (RAAS)
Concomitant use of angiotensin II receptor antagonists with drugs containing aliskiren is contraindicated in patients with diabetes mellitus and/or moderate or severe renal failure (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.
Impact on the ability to drive vehicles and operate machinery
No studies have been conducted to evaluate the effect on the ability to drive or operate machines, but caution should be exercised when using antihypertensive therapy and driving or operating machines, as dizziness and drowsiness may develop, especially at the beginning of therapy or when the dose is increased.
Losartan's analogs
Level 4 ATC code matches:
Telmisartan
Irbesartan
Presartan
Nortivan
Candesartan
Kozaar
Aprovel
Teveten
Blocktran
Cardosal
Valsartan
Atakand
Diovan
Valsacor
Mikardis
Vazar
Valz
Lorista
Lorista
Lozap
There are quite a large number of analogues of Losartan. Analogues, or synonyms of a given drug, are medicines containing the same active substance and intended to treat the same diseases. Analogues of the drug include:
- Lorista
- Lozap
- Kozaar
- Blocktran
- Vasotens
- Presartan
- Renicard
- Losarel
- Karzartan
- Zisakar
- Cardomine
- Losakor
Losartan price
The price of Losartan, relative to its quality and truly effective effect on the body, is very low. In pharmacies, this drug can be purchased at a price of 120 to 300 rubles, depending on the number of tablets in the package.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
ZdravCity
- Losartan tablets p.p.o.
12.5 mg 30 pcs. Pranapharm LLC 48 rub. order - Losartan tablets p.p.o. 50 mg 30 pcs. OzonOzon LLC
124 RUR order
- Losartan N tablets p.p.o. 12.5mg+50mg 30 pcs. Ozone LLC
184 RUR order
- Losartan tablets p.p.o. 100 mg 30 pcs. Ozone LLC
136 RUR order
- Losartan tab. p/o captivity. 12.5 mg No. 30Ozon LLC
56 RUR order
Pharmacy Dialogue
- Losartan (tab.p.pl.vol. 12.5 mg No. 30) Ozone LLC
57 RUR order
- Losartan-Richter (tab.p.pl/vol. 50mg No. 30)Gedeon-Richter-RUS ZAO
RUB 181 order
- Losartan (tab.p/pl/vol. 50 mg No. 30) Ozone LLC
RUB 158 order
- Losartan (tablet p/o 25 mg No. 30)Vertex
123 RUR order
- Losartan-N (tablet p/o 50 mg + 12.5 mg No. 30) Ozon LLC
RUB 194 order
show more