Losartan-Teva - Instructions For Use, Price, Reviews, Analogs Of Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Losartan-Teva

Losartan-Teva: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Losartan-Teva

ATX code: C09CA01

Active ingredient: losartan (Losartan)

Producer: TEVA Pharmaceutical Works Private Limited Company (Hungary)

Description and photo update: 2019-08-10

Prices in pharmacies: from 162 rubles.

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Losartan-Teva is an antihypertensive drug.

Release form and composition

The drug is produced in the form of film-coated tablets: biconvex, oval, white; tablets with a dosage of 12.5 mg - on one side with an engraving L; dosage of 25 mg - with a line on both sides, on one of the sides engraved with "2" above the line and "5" below the line; dosage of 50 and 100 mg - on one side with a dividing line, on the other - with engraving "50" or "100", respectively (12.5; 25, 50 and 100 mg - 10 pcs. in a blister, in a cardboard box 3 blisters; 25 mg - 10 pcs. in a blister, in a cardboard box 5 blisters; 50 mg - 14 pcs. in a blister, in a cardboard box 1 blister. Each pack also contains instructions for the use of Losartan-Teva).

1 tablet contains:

• active substance: losartan potassium - 12.5 / 25/50/100 mg;
• auxiliary components: microcrystalline cellulose, lactose monohydrate, magnesium stearate, pregelatinized starch;
• film casing: Opadry II 85F18422 white (macrogol, titanium dioxide, talc, partially hydrolyzed polyvinyl alcohol).

Pharmacological properties

Pharmacodynamics

Losartan belongs to specific antagonists of angiotensin II receptors (AT ₁ subtype) for oral administration. Angiotensin II selectively binds to AT ₁ -receptors localized in many tissues (in the smooth muscles of the vascular walls, kidneys, adrenal glands, and heart), and performs a number of important biological functions such as vasoconstriction and aldosterone release. Also, angiotensin II stimulates the proliferation of smooth muscle cells.

The active substance of Losartan-Teva and its metabolite (E 3174), which exhibits pharmacological activity, both in vitro and in vivo, suppress all physiological effects of angiotensin II, regardless of the pathway and source of production. Selectively binding to AT ₁ -receptors, losartan does not interact and does not inhibit the receptors of other hormones and ion channels responsible for regulating the function of the cardiovascular system. In addition, losartan does not suppress the angiotensin-converting enzyme (ACE) - kininase II, as a result of which it does not counteract the destruction of bradykinin and rarely leads to the development of side effects indirectly associated with the latter, including the appearance of angioedema.

When losartan is used, the absence of negative feedback on renin production causes an increase in the plasma activity of blood renin, which in turn leads to an increase in the content of angiotensin II in the blood plasma. At the same time, the antihypertensive effect and a decrease in the level of aldosterone in the plasma persist, which is a confirmation of the effective blockade of angiotensin II receptors.

Losartan and its active metabolite (E 3174) are distinguished by a greater degree of affinity for angiotensin I receptors than for angiotensin II receptors. The main metabolite of losartan demonstrates an activity 10–40 times higher than that of the main substance. After a single oral administration of Losartan-Teva, the hypotensive effect [decrease in systolic and diastolic blood pressure (BP)] reaches a maximum after 6 hours, after which it gradually decreases over 24 hours. The maximum hypotensive effect is observed 3–6 weeks after the start of the course of therapy.

In the presence of arterial hypertension without diabetes mellitus with proteinuria (over 2000 mg / day), treatment with the drug reliably provides a decrease in proteinuria, excretion of albumin and immunoglobulin G. reflexes.

In patients with arterial hypertension, the use of losartan in a daily dose of 150 mg does not lead to a change in the serum concentration of high density lipoprotein cholesterol (HDL), total cholesterol and triglycerides in the blood. Also, taking the drug in a similar dose does not change the fasting blood glucose level.

Pharmacokinetics

After oral administration of Losartan-Teva, the active substance is actively absorbed from the gastrointestinal tract (GIT) and undergoes biotransformation during the first passage through the liver through the carboxylation reaction, which occurs with the participation of the isoenzyme CYP2C9. As a result of the metabolism of losartan, a carboxy derivative is formed - an active metabolite. The bioavailability of losartan averages 33% and does not depend on the time of the meal. In blood serum, the maximum concentration of the drug and its active derivative is observed, respectively, 1 and 3-4 hours after oral administration.

The volume of distribution of funds is 34 liters. More than 99% of losartan and its main metabolite bind to blood plasma proteins, mainly albumin. Losartan-Teva practically does not pass through the blood-brain barrier.

On average, 14% of losartan administered orally or intravenously (iv) is converted to E 3174 (an active metabolite), the plasma clearance of which is approximately 50 ml / min. Plasma clearance of losartan is 600 ml / min. The renal clearance of the active substance and its carboxy derivative is approximately 74 and 26 ml / min, respectively. When taken orally, the kidneys excrete approximately 4% of the administered dose of the drug unchanged and 6% in the form of an active metabolite. When used orally in doses up to 200 mg, losartan and its main metabolite are characterized by linear pharmacokinetics. The terminal half-life of losartan is approximately 2 hours, and E 3174 is 6-9 hours. When taking Losartan-Teva in a daily dose of 100 mg, neither the active substance nor its active derivative accumulates.

Losartan and its metabolites are eliminated by the kidneys and through the intestines. After oral administration of ¹⁴ C- labeled losartan by healthy volunteers, approximately 35% of the radioactive label is detected in urine and 59% in feces.

In women with arterial hypertension, plasma levels of losartan are 2 times higher than those in men with a similar diagnosis. The values of the concentration in the blood of the active metabolite in men and women do not differ.

With indications of creatinine clearance (CC) more than 10 ml / min, the plasma content of losartan in the blood does not differ from that during normal renal activity.

In patients requiring hemodialysis, the area under the concentration-time curve (AUC) is, on average, 2 times greater than in those with normal renal function.

If patients have mild and moderate alcoholic cirrhosis of the liver, the level of losartan and its active derivative in the blood is 5 and 1.7 times higher, respectively, than in healthy male volunteers.

In elderly patients with arterial hypertension, the plasma concentrations of losartan and its active metabolite do not differ significantly from the values of these parameters in young men with the same disease.

Indications for use

• arterial hypertension;
• diabetic nephropathy or hypercreatininemia and proteinuria (the ratio of urine albumin and creatinine more than 300 mg per day) in patients with type 2 diabetes mellitus and arterial hypertension - in order to slow the progression of diabetic nephropathy to end-stage chronic renal failure (CRF);
• chronic heart failure (CHF) in case of ineffectiveness or intolerance of treatment with ACE inhibitors - as part of complex therapy;
• reducing the threat of developing cardiovascular lesions (including stroke) and mortality in patients with left ventricular hypertrophy (LVH) and arterial hypertension.

Contraindications

Absolute:

• severe hepatic impairment (above 9 points on the Child-Pugh scale);
• glucose-galactose malabsorption syndrome or lactase deficiency, hereditary galactose intolerance;
• combination therapy with aliskiren or drugs containing aliskiren in patients with diabetes mellitus and / or impaired renal function with a glomerular filtration rate (GFR) less than 60 ml / min / 1.73 m²;
• pregnancy and lactation;
• age up to 18 years;
• hypersensitivity to any component of the product.

Relative (it is required to use Losartan-Teva tablets with caution):

• arterial hypotension;
• mitral and aortic stenosis;
• severe CHF functional class IV according to the classification of the New York Heart Association (NYHA);
• ischemic heart disease (CHD);
• heart failure with life-threatening arrhythmias;
• obstructive hypertrophic cardiomyopathy;
• cerebrovascular diseases;
• violations of water and electrolyte balance;
• heart failure, accompanied by severe renal impairment;
• reduced volume of circulating blood (BCC);
• renal failure;
• stenosis of an artery of a single kidney or bilateral stenosis of the renal arteries (during the period of therapy, an increase in the concentration of urea in the blood and the level of serum creatinine is possible);
• condition after kidney transplantation;
• liver failure (below 9 points on the Child-Pugh scale);
• primary hyperaldosteronism;
• a history of angioedema.

Losartan-Teva, instructions for use: method and dosage

Losartan-Teva is taken orally, regardless of the time of the meal, once a day (when using a dose of 100 mg, it is possible to take it 2 times a day). The tablets should be swallowed whole, without crushing or chewing, with water.

The recommended dosage regimen of Losartan-Teva, taking into account the indications:

• arterial hypertension: the average daily dose is 50 mg, to achieve a more pronounced therapeutic effect, the daily dose can be increased to 100 mg in 1 dose;
• reducing the threat of developing cardiovascular lesions (including stroke) and mortality in patients with LVH and arterial hypertension: the initial daily dose is 50 mg; in the course of further therapy, it is possible to add low doses of hydrochlorothiazide to the treatment or increase the daily dose of losartan to 100 mg (with taking into account changes in blood pressure), taken in 1 or 2 doses;
• CHF: initial daily dose - 12.5 mg (you can use ½ tablet with a dosage of 25 mg); usually, the dose can be increased at weekly intervals (12.5; 25 and 50 mg per day) to an average maintenance daily dose of 50 mg per dose, depending on the individual tolerance of the drug; dose adjustment for elderly patients is not required;
• proteinuria in patients with arterial hypertension and concomitant type 2 diabetes mellitus: the initial daily dose is 50 mg, in the future it is possible to increase the dose to 100 mg (taking into account the degree of decrease in blood pressure) in 1 or 2 doses.

In patients with reduced BCC (for example, when using diuretics in high doses), it is recommended to take Losartan-Teva at an initial dose of 25 mg once a day.

Side effects

As a rule, against the background of drug treatment, there may be transient and not requiring its withdrawal side reactions. In the case of taking Losartan-Tev for the treatment of arterial hypertension in the course of controlled studies, only the frequency of occurrence of dizziness differed from placebo by more than 1% (4.1 versus 2.4%). The dose-dependent hypotensive effect characteristic of antihypertensive drugs during the period of losartan use was observed in less than 1% of patients.

Adverse reactions recorded during clinical trials and post-registration observations with a frequency of more than 1% (often):

• respiratory system: nasal congestion, sinusitis, pharyngitis, cough, bronchitis, upper respiratory tract infections;
• musculoskeletal system: pain in the legs, back, cramps of the calf muscles;
• cardiovascular system: palpitations, tachycardia;
• digestive system: dyspeptic disorders, nausea, abdominal pain, diarrhea;
• neurology / psychiatry: insomnia, headache, dizziness;
• general symptoms: fatigue, asthenia, peripheral edema, chest pain.

Side effects noted with a frequency of less than 1% (infrequently):

• hematopoietic system: thrombocytopenia, anemia (decrease in hemoglobin and hematocrit by about 0.11 g% and 0.09 volume%, respectively, in rare cases of clinical significance), eosinophilia, Shenlein-Genoch purpura;
• nervous system and sensory organs: drowsiness, sleep disorders, anxiety, memory impairments, tremors, ataxia, taste disturbances, visual impairments, ringing in the ears, conjunctivitis, migraines, peripheral neuropathy, hyposthesia, paresthesias, fainting, depression;
• skin: increased sweating, dry skin, ecchymosis, alopecia, erythema, photosensitivity;
• digestive system: dryness of the oral mucosa, toothache, anorexia, flatulence, vomiting, constipation, gastritis, liver dysfunction, hepatitis;
• cardiovascular system: epistaxis, orthostatic hypotension (dose-dependent), arrhythmias, bradycardia, angina pectoris, myocardial infarction, vasculitis;
• genitourinary system: urgency to urinate, impaired renal function, urinary tract infections;
• reproductive system: impotence, decreased libido;
• musculoskeletal system: pain in the shoulder, knee, fibromyalgia, arthralgia, arthritis;
• allergic reactions: skin rash, itching, urticaria, angioedema, including edema of the larynx and tongue, leading to airway obstruction and / or swelling of the lips, face, pharynx;
• others: gout.

There may also be violations of laboratory parameters: often - hyperuricemia (plasma potassium levels in the blood above 5.5 mmol / l); infrequently - an increase in the content of urea, residual nitrogen, creatinine in the blood serum; extremely rarely - a moderate increase in the activity of alanine aminotransferase (ALT) and aspartate aminotransferase (ACT), hyperbilirubinemia.

Overdose

Symptoms of an overdose of Losartan-Teva may include a significant decrease in blood pressure and tachycardia; as a result of parasympathetic stimulation, bradycardia may develop. In this condition, forced diuresis and symptomatic therapy are recommended. Neither losartan nor its active metabolite can be removed from the body with the help of hemodialysis.

special instructions

Before starting the course of treatment with Losartan-Teva, it is required to correct the BCC or start taking the drug at a lower initial dose.

If there is a history of angioedema (face, lips, tongue and / or pharynx), patients need to use the drug with extreme caution under strict supervision.

During therapy, it is recommended to regularly monitor the concentration of potassium in the blood, especially in elderly patients and in the presence of impaired renal function.

There are no data on the safety of drug therapy in patients who have recently undergone kidney transplantation.

As with the use of other antihypertensive drugs, an excessively sharp decrease in blood pressure in patients with cerebrovascular lesions and ischemic heart disease can provoke myocardial infarction or ischemic stroke.

There is practically no therapeutic experience with the use of losartan in the treatment of patients with heart failure and severe renal impairment, in those with severe CHF (class IV according to the NYHA classification), as well as in patients with heart failure and life-threatening arrhythmias. As a result, Losartan-Teva should be taken with extreme caution in these categories of patients. It has been established that in the presence of heart failure with or without concomitant renal impairment during treatment with drugs acting on the renin-angiotensin-aldosterone system (RAAS), the risk of severe arterial hypotension and acute renal failure is aggravated.

According to the available data, patients with primary hyperaldosteronism, as a rule, show resistance to the action of antihypertensive drugs that affect the RAAS. Therefore, Losartan-Teva is not recommended for this group of patients.

Influence on the ability to drive vehicles and complex mechanisms

There have been no special studies evaluating the effect of Losartan-Teva on the ability to drive vehicles and other complex, moving mechanisms, however, during the period of therapy, the risk of drowsiness and dizziness should be taken into account. When performing potentially hazardous work that requires increased attention, and driving vehicles, care should be taken, especially at the beginning of the course and when the dose of an antihypertensive drug is increased.

Application during pregnancy and lactation

The use of Losartan-Teva during pregnancy is contraindicated. According to research results, the use of drugs that affect the RAAS during the II and III trimesters of pregnancy can induce developmental defects and mortality of the fetus and newborn. The occurrence of oligohydramnios (oligohydramnios) can cause hypoplasia of the fetal lungs and deformation of the bones of the skeleton. Possible reactions that occur in the fetus as a result of exposure to these drugs include: arterial hypotension, anuria, delayed ossification of the skull bones, renal failure, death. As a result, upon confirmation of pregnancy, drug therapy should be immediately canceled. If during the period starting from the second trimester of pregnancy,the woman was prescribed antihypertensive treatment with drugs acting on the RAAS due to the impossibility of conducting alternative therapy; it is required to periodically perform ultrasound examinations (ultrasound) to assess the intra-amniotic space. Also, taking into account the week of pregnancy, appropriate fetal tests should be performed.

Whether losartan is excreted in breast milk has not been established, therefore, its use during lactation is contraindicated. If the use of Losartan-Teva is necessary during lactation, then the child should be transferred to artificial feeding.

Pediatric use

In patients under 18 years of age, the use of Losartan-Teva is contraindicated due to the lack of information confirming the safety and efficacy of losartan treatment in children and adolescents.

With impaired renal function

Patients with renal insufficiency, stenosis of an artery of a single kidney, or bilateral stenosis of the renal arteries should take Losartan-Teva tablets with caution.

When carrying out the hemodialysis procedure, the initial dose of losartan should be 25 mg once a day.

For violations of liver function

Due to the insufficient experience of using the drug in patients with severe hepatic impairment (above 9 points on the Child-Pugh scale), taking Losartan-Teva in this category of patients is contraindicated.

In patients with moderate hepatic impairment (below 9 points on the Child-Pugh scale), the initial daily dose of Losartan-Teva should not exceed 25 mg.

Use in the elderly

Patients over the age of 75 are advised to use Losartan-Teva at a lower initial daily dose of 25 mg.

Drug interactions

• ACE inhibitors, aliskiren (direct renin inhibitor): in comparison with monotherapy, the risk of hyperkalemia, arterial hypotension, fainting and functional renal impairment (including acute renal failure) is aggravated when these drugs are combined with angiotensin II receptor antagonists (ARA II), leading to double blockade of RAAS; it is required to constantly monitor blood pressure, renal function and the concentration of electrolytes in the blood; in patients with diabetes mellitus and / or with impaired renal function (GFR below 60 ml / min / 1.73 m²), the combination of the drug with aliskiren is contraindicated; for patients with diabetic nephropathy, the combined use of losartan with ACE inhibitors is also contraindicated, for the rest of the patients it is not recommended;
• other antihypertensive drugs: this combination is allowed;
• sympatholytics, beta-blockers: there is a mutual enhancement of the effect;
• diuretics: an additive effect is recorded;
• digoxin, hydrochlorothiazide, warfarin, phenobarbital, ketoconazole, cimetidine, erythromycin: no pharmacokinetic interactions detected;
• fluconazole, rifampicin: the plasma level of the active metabolite in the blood decreases; to date, the clinical significance of these interactions has not been established;
• potassium-sparing diuretics such as triamterene, spironolactone, eplerenone, amiloride; potassium preparations, salts containing potassium: the threat of hyperkalemia increases;
• non-steroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of piclooxygenase-2 (COX-2): weakening of the effect of diuretics and other antihypertensive drugs may be recorded;
• lithium preparations: the serum concentration of lithium increases, regular monitoring of its level in the blood serum is necessary; when prescribing this combination, it is required to correlate the benefits and risks of the combined use of losartan with lithium salts.

Analogs

Analogues of Losartan-Teva are: Bloktran, Vasotenz, Zisakar, Cardomin-Sanovel, Losartan, Losartan-Canon, Losartan-Richter, Losartan-McLeodz, Losartan-TAD, Lotor, Karzartan, Kozaar, Lozap, Renicard, Losakar, Losakar, Lorista, Lozarel and others.

Terms and conditions of storage

Store in a place protected from light, out of reach of children, at temperatures up to 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Losartan-Teva

According to reviews of Losartan-Teva found on medical websites, it is an effective drug that helps to normalize and control blood pressure values throughout the course of treatment. Many patients note that the drug gently reduces pressure, eliminates pain and a feeling of heaviness in the head, while being well tolerated. Also, the reviews indicate the gradual development of the drug's action, reaching its maximum only at 3-6 weeks of therapy. As a result, patients are warned that Losartan-Teva cannot be used as an ambulance, since it is not intended to relieve a hypertensive crisis.

The disadvantages of the remedy include the development of adverse reactions. In some reviews, there is no positive effect in drug treatment.

The price of Losartan-Teva in pharmacies

The price of Losartan-Teva for a package containing 30 film-coated tablets can be: dosage of 25 mg - 90 rubles, 50 mg - 160 rubles, 100 mg - 180 rubles.

Losartan-Teva: prices in online pharmacies

Drug name Price Pharmacy

Losartan-Teva 50 mg film-coated tablets 30 pcs. 162 RUB Buy

Losartan-Teva 100 mg film-coated tablets 30 pcs. 173 r Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!