Losartan
Losartan: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Losartan
ATX code: C09CA01
Active ingredient: losartan (losartan)
Manufacturer: Pharmaceutical Plant Teva Private Co. Ltd. (Israel)
Description and photo update: 2019-13-08
Prices in pharmacies: from 37 rubles.
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Losartan is a drug with an antihypertensive effect.
Release form and composition
Losartan is produced in the form of film-coated tablets: round, biconvex, a slight surface roughness is permissible; at the break - white with a yellowish tinge or white; 12.5 and 25 mg - white with a grayish tinge or white, 50 mg - pink, 100 mg - yellow (in blisters of 10 pcs., 3 blisters in a cardboard box; in blisters of 15 pcs., 2, 4, 6 blisters in a cardboard box; in blister packs of 10, 30 pcs., 1-6, 10 packs in a cardboard box; in a blister strip of 20 pcs., 1, 3 packs in a cardboard box; in blister packs of 7 pcs., 1-4 packs in a cardboard box; in cans (jars) of 10, 20, 30,40, 50, 60, 100 pcs., 1 can in a cardboard box).
The composition of 1 tablet includes:
- Active ingredient: potassium losartan - 12.5 mg, 25 mg, 50 mg or 100 mg;
- Excipients (tablets of 12.5 / 25/50/100 mg, respectively): lactose monohydrate (milk sugar) - 114.63 / 149.5 / 270.6 / 115 mg, microcrystalline cellulose - 5.72 / 12.24 / 26.6 / 40 mg, croscarmellose sodium (primellose) - 4.29 / 9.18 / 15.2 / 11.2 mg, colloidal silicon dioxide (aerosil) - 1.43 / 2.04 / 3.8 / 2 mg, povidone (low molecular weight polyvinylpyrrolidone) - 0/0/0/9 mg, magnesium stearate - 1.43 / 2.04 / 3.8 / 2.8 mg.
Shell composition:
- 12.5 and 25 mg (respectively): Opadry II white (polyvinyl alcohol (E1203) - 40%, titanium dioxide (E171) - 25%, polyethylene glycol (macrogol) (E1521) - 20.2%, talc (E553b) - 14.8%) - 2.983 / 3.975 mg, simethicone emulsion 30% (water - 50-69.5%, polydimethylsiloxane - 25.5-33%, polyethylene glycol sorbitan tristearate - 3-7%, methylcellulose - 1-5%, silica gel - 1-5%) - 0.017 / 0.025 mg;
- 50 mg: Opadry II pink (polyvinyl alcohol (E1203) - 40%, titanium dioxide (E171) - 24.18%, talc (E553b) - 14.8%, polyethylene glycol (macrogol) (E1521) - 20.2%, dye carmine red (E120) - 0.54%, aluminum varnish based on charming red dye (E129) - 0.08%, aluminum varnish based on sunset yellow dye (E110) - 0.15%, aluminum varnish based on dye quinoline yellow (E104) - 0.05%) - 9.923 mg, simethicone emulsion 30% (water - 50-69.5%, polyethylene glycol sorbitan tristearate - 3-7%, polydimethylsiloxane - 25.5-33%, methylcellulose - 1 -5%, silica gel - 1-5%) - 0.077 mg;
- 100 mg: (hypromellose - 4.8 mg, talc - 1.6 mg, titanium dioxide - 0.826 mg, polyethylene glycol 4000 (macrogol 4000) - 0.72 mg, yellow iron oxide (iron oxide) - 0.054 mg) or (dry a mixture for a film coating containing: hypromellose - 60%, talc - 20%, titanium dioxide - 10.33%, macrogol 4000 (polyethylene glycol 4000) - 9%, yellow iron oxide (iron oxide) - 0.67%) - 8 mg.
Pharmacological properties
Pharmacodynamics
Losartan is a specific angiotensin II receptor antagonist (AT 1 -subtype) intended for internal administration. This substance does not inhibit the angiotensin-converting enzyme (kininase II), which is a catalyst for the reaction of obtaining angiotensin II from angiotensin I.
Angiotensin II selectively interacts with AT 1 -receptors of many tissues (vascular smooth muscle tissue, kidney tissue, heart and adrenal gland), performing important biological functions, including vasoconstriction, release of aldosterone, etc. Angiotensin II also stimulates the process of proliferation of smooth muscle cells. In vitro and in vivo Losartan and E 3174 (pharmacologically active metabolite of Losartan) block the physiological effect of angiotensin II regardless of the pathway or source of synthesis. Losartan selectively interacts with AT 1-receptors and does not bind to receptors of other hormones or ion channels, which play an important role in the regulation of the functions of the cardiovascular system. Losartan does not suppress the angiotensin-converting enzyme (kininase II) and does not prevent the destruction of bradykinin, therefore, side effects indirectly caused by interaction with bradykinin are quite rare.
In the case of losartan use, there is no negative feedback with the secretion of renin, which leads to an increase in its activity in the blood plasma. An increase in renin activity causes an increase in the content of angiotensin II, but at the same time both antihypertensive activity and a decrease in the concentration of aldosterone in the blood plasma remain, which indicates the effectiveness of blockade of angiotensin II receptors. Losartan and its active metabolite have a greater affinity for angiotensin I receptors than for angiotensin II receptors. The activity of losartan is 10–40 times less than that of its active metabolite.
A single oral administration of the drug causes an antihypertensive effect (decrease in systolic and diastolic blood pressure), which reaches a maximum after 6 hours, and then gradually decreases over 24 hours.
The maximum antihypertensive effect is observed after 3–6 weeks.
With arterial hypertension and the absence of diabetes mellitus, the use of the drug in patients with proteinuria (over 2 g / day) significantly leads to a decrease in proteinuria, the excretion of immunoglobulin G and albumin.
Losartan stabilizes the content of urea in blood plasma, does not affect autonomic reflexes and the content of noradrenaline in plasma.
In patients with arterial hypertension, a daily dose of Losartan in the amount of 150 mg does not change the concentration of total cholesterol, high-density lipoprotein cholesterol and triglycerides in the blood serum. Taking a similar dose of the drug on an empty stomach does not affect blood glucose.
Pharmacokinetics
When taken orally, losartan is well absorbed from the gastrointestinal tract and is metabolized during the first passage through the liver through carboxylation with the participation of the isoenzyme CYP2C9, resulting in the formation of an active metabolite.
The bioavailability of Losartan is about 33%. The maximum concentration of the active substance and its active metabolite in the blood serum is reached, respectively, 1 and 3-4 hours after ingestion. The bioavailability of losartan is independent of food intake.
Over 99% of losartan and its active metabolite binds to plasma proteins (mainly albumin). The volume of distribution is 34 liters. Studies on rats have shown that losartan hardly crosses the blood-brain barrier.
Approximately 14% of losartan administered intravenously or taken orally is converted into an active metabolite. Inactive metabolites are also formed, including one minor metabolite, N-2-tetrazole glucuronide, and two major metabolites, which are formed after hydroxylation of the butyl side chain.
The plasma clearance of losartan is 600 ml / min, its active metabolite is 50 ml / min. The renal clearance of losartan is 74 ml / min, its active metabolite is 26 ml / min. When taken orally, about 4% of the dose is excreted by the kidneys unchanged, and 6% - as an active metabolite. For losartan and its active metabolite, linear pharmacokinetics are characteristic when taken orally up to 200 mg of losartan. The half-life of losartan is 1.5–2 hours, its main metabolite is 6–9 hours. With a daily dose of the drug 100 mg, losartan and its active metabolite do not accumulate in the blood plasma.
Losartan and metabolites are excreted through the kidneys and through the intestines with bile.
With a creatinine clearance above 10 ml / min, the plasma content of losartan does not differ from that in patients with normal renal function.
Losartan and its active metabolite are not removed from the body by hemodialysis.
In patients on hemodialysis, the AUC (area under the concentration-time curve) is 2 times higher than in patients with normal renal function.
In alcoholic liver cirrhosis of moderate and mild severity, the content of losartan and its active metabolite is 5 and 1.7 times higher than those of healthy male volunteers, respectively.
In elderly men with arterial hypertension, the plasma concentrations of losartan and its active metabolite do not differ from the values of these parameters in young men with a similar diagnosis. In women suffering from arterial hypertension, plasma concentrations of losartan are twice as high as in men suffering from this disease. The content of the active metabolite differs in women and men. This pharmacokinetic difference is not clinically significant.
Indications for use
- Arterial hypertension;
- Protection of the kidneys in type 2 diabetes mellitus with proteinuria (the effect is manifested by a slowdown in the progression of renal failure, namely, a decrease in the incidence of hypercreatininemia, proteinuria, end stage chronic renal failure (requiring kidney transplantation or hemodialysis), mortality rates);
- Reducing the risk of associated cardiovascular morbidity and mortality in arterial hypertension and left ventricular hypertrophy (the effect is manifested by a decrease in the cumulative incidence of stroke, cardiovascular mortality and myocardial infarction);
- Chronic heart failure in case of ineffectiveness of the treatment with angiotensin-converting enzyme inhibitors.
Contraindications
Absolute:
- Severe hepatic impairment (due to lack of experience with use);
- Refractory hyperkalemia;
- Dehydration;
- Lactase deficiency, lactose intolerance and glucose-galactose malabsorption syndrome;
- Simultaneous use with aliskiren in patients with diabetes mellitus and / or with functional impairment of the kidneys (at a glomerular filtration rate of less than 60 ml per minute);
- Pregnancy and lactation;
- Age under 18;
- Hypersensitivity to drug components.
Relative (diseases / conditions in which Losartan must be used with caution):
- Renal failure;
- Violations of water and electrolyte balance;
- Liver failure (less than 9 points according to Child-Pugh);
- Cardiac ischemia;
- Arterial hypotension;
- Decreased volume of circulating blood;
- Hyperkalemia;
- Stenosis of an artery of a single kidney or bilateral stenosis of the renal arteries;
- Conditions after kidney transplantation;
- Mitral and aortic stenosis;
- Obstructive hypertrophic cardiomyopathy;
- Severe heart failure (NYHA functional class IV), history of angioedema;
- Heart failure, accompanied by life-threatening arrhythmias;
- Heart failure accompanied by severe renal failure;
- Primary aldosteronism;
- Cerebrovascular diseases.
Instructions for the use of Losartan: method and dosage
Losartan is taken orally, regardless of the meal time.
The drug can be used as monotherapy or simultaneously with other antihypertensive drugs.
If there are no other prescriptions, the daily dose is taken in 1 reception.
In most cases of arterial hypertension, the standard initial and maintenance daily dose is 50 mg. As a rule, the maximum antihypertensive effect is achieved within 3-6 weeks from the start of therapy. In some patients, to achieve a greater effect, it is possible to increase the dose to a maximum of 100 mg per day.
With a reduced volume of circulating blood (for example, when taking large doses of diuretics), Losartan is started at a dose of 25 mg per day.
There is no need for an individual selection of the initial dose in elderly patients and with renal insufficiency, including those on dialysis patients.
In liver failure (less than 9 points on the Child-Pugh scale) during the hemodialysis procedure, as well as in patients over 75 years old, the drug is recommended to be prescribed in a lower initial daily dose of 25 mg.
The standard daily starting dose of Losartan to reduce the risk of associated cardiovascular morbidity and mortality in patients with left ventricular hypertrophy and arterial hypertension is 50 mg. In the future, it is recommended to increase the dose of the drug by 2 times (in 1 or 2 doses, depending on the degree of lowering of blood pressure) or the addition of hydrochlorothiazide.
The standard starting daily dose of Losartan for kidney protection in patients with type 2 diabetes mellitus with proteinuria is 50 mg. In the future, depending on the degree of lowering of blood pressure, it is recommended to increase the dose of the drug by 2 times. Losartan can be used concurrently with other antihypertensive drugs (alpha and beta blockers, diuretics, centrally acting antihypertensive drugs, blockers of "slow" calcium channels), insulin and other hypoglycemic drugs (glucosidase inhibitors, glitazones and sulfonylurea derivatives).
In chronic heart failure, the initial daily dose of Losartan is 12.5 mg. Usually, the dose is titrated at weekly intervals to the usual maintenance dose of 50 mg once a day (depending on individual tolerance).
Side effects
Losartan, as a rule, is well tolerated, side effects are transient and mild and do not require discontinuation of therapy.
When using the drug, disturbances from some body systems may develop, manifesting themselves with varying frequency (> 1% - often; <1% - rarely):
- Digestive system: often - abdominal pain, dyspepsia, diarrhea, nausea; rarely - dryness of the oral mucosa, anorexia, flatulence, toothache, gastritis, constipation, liver dysfunction, hepatitis, vomiting;
- Cardiovascular system: often - palpitations, tachycardia; rarely - angina pectoris, symptomatic arterial hypotension (especially in patients with intravascular dehydration, for example, with severe heart failure or when taking high doses of diuretics), dose-dependent orthostatic hypotension, bradycardia, myocardial infarction, arrhythmias, vasculitis;
- Central nervous system and sensory organs: often - headache, dizziness, insomnia; rarely - anxiety, sleep disturbance, memory impairment, drowsiness, peripheral neuropathy, hyposthesia, paresthesia, tremor, depression, ataxia, fainting, conjunctivitis, taste and vision disorders, ringing in the ears, migraine;
- Urinary system: rarely - urinary tract infections, urge to urinate, functional kidney disorders;
- Respiratory system: often - cough, swelling of the nasal mucosa, bronchitis, sinusitis, pharyngitis, upper respiratory tract infections;
- Hematopoietic system: rarely - anemia, eosinophilia, thrombocytopenia, Schönlein-Henoch purpura;
- Reproductive system: rarely - impotence, decreased libido;
- Musculoskeletal system: often - muscle cramps, pain in the legs and back; rarely - arthritis, arthralgia, pain in the knee and shoulder, fibromyalgia;
- Skin: rarely - increased sweating, dry skin, erythema, ecchymosis, photosensitivity, alopecia;
- Allergic reactions: rarely - skin rash, urticaria, itching, angioedema (including edema of the vocal fold and larynx, causing airway obstruction, and / or edema of the lips, face, tongue and / or pharynx);
- General disorders: often - peripheral edema, asthenia, fatigue, weakness, pain in the chest area;
- Others: rarely - nosebleeds, exacerbation of the course of gout.
It is also possible to develop violations from laboratory parameters:> 1% and 0.1% and <1% - an increase in the concentration of residual nitrogen, urea, creatinine in the blood serum; <0.01% - a moderate increase in the activity of transaminases (alanine aminotransferase, aspartate aminotransferase), hyperbilirubinemia.
With the development or aggravation of these side effects, as well as with the development of uncharacteristic symptoms, you should consult a doctor.
Overdose
Symptoms: tachycardia, a marked decrease in blood pressure, bradycardia may develop.
In the treatment of overdose, the appointment of forced diuresis and symptomatic therapy is recommended. Losartan and its active metabolite are not removed from the bloodstream by hemodialysis.
special instructions
In rare cases, with the use of Losartan, disorders develop in the form of anaphylactic reactions, angioedema with involvement of the pharynx and larynx, causing airway obstruction, and / or edema of the face, lips, tongue and / or pharynx. Therefore, if there are indications of a history of angioedema, the drug should be taken with extreme caution.
In patients with a reduced volume of circulating blood (for example, receiving high doses of diuretics), symptomatic arterial hypotension may develop. Correction of these conditions should be carried out before the appointment of Losartan or therapy should be started with taking lower doses.
Violations of water and electrolyte balance are characteristic of patients with renal failure with or without type 2 diabetes mellitus. When prescribing Losartan in this category of patients, special care must be taken because of the risk of developing hyperkalemia.
During therapy, it is necessary to regularly monitor the potassium content in the blood, especially in elderly patients and with functional impairment of the kidneys. Potassium supplements or salt substitutes containing potassium should not be taken without first consulting your doctor.
If there is an indication of a history of liver disease, Losartan should be taken in lower doses, which is associated with an increase in the concentration of the drug in the blood plasma.
During the period of therapy, it is necessary to regularly monitor the concentration of creatinine in the blood serum at regular intervals.
Caution should be exercised when driving vehicles and performing other potentially hazardous work requiring increased concentration of attention and rapid psychomotor reactions, due to the possible development of dizziness, especially in patients who took diuretic drugs and switched to Losartan therapy.
Application during pregnancy and lactation
It is forbidden to use Losartan during pregnancy and lactation. It is known that the use of drugs that affect the renin-angiotensin-aldosterone system in the II or III trimesters of pregnancy can cause developmental defects or death of the developing fetus. As a result, when diagnosing pregnancy, the use of Losartan must be stopped immediately.
There are no data on the excretion of the drug in breast milk. If taking Losartan during lactation is necessary, then breastfeeding should be interrupted.
Pediatric use
According to the instructions, Losartan is prohibited for the treatment of patients under the age of 18 years.
With impaired renal function
In case of renal failure, the drug should be used with caution.
For violations of liver function
In liver failure (up to 9 points on the Child-Pugh scale), the drug should be used with caution.
Use in the elderly
When treating elderly patients, there is no need to select a dose of the drug.
Drug interactions
With the simultaneous use of Losartan with certain drugs, the following effects may occur:
- Rifampicin, fluconazole: decrease in the level of the active metabolite;
- Potassium-sparing diuretics (eg spironolactone, amiloride, triamterene, eplerenone) or drugs that increase potassium (eg heparin), potassium supplements, and potassium salts: increased serum potassium;
- Lithium preparations: a decrease in sodium excretion and an increase in serum lithium concentration (it is necessary to monitor its serum concentration);
- Non-steroidal anti-inflammatory drugs, including selective inhibitors of cyclooxygenase-2: reducing the antihypertensive effect; in patients with functional impairment of the kidneys receiving treatment with NSAIDs, further deterioration of renal function is possible;
- Other antihypertensive drugs: an increase in the severity of antihypertensive action;
- Medicines that lower blood pressure (for example, tricyclic antidepressants, antipsychotics, baclofen, amifostine): increased risk of arterial hypotension;
- Medicines affecting the renin-angiotensin-aldosterone system: increased risk of arterial hypotension, hyperkalemia, syncope and renal dysfunction (including acute renal failure); it is necessary to carefully monitor blood pressure, water and electrolyte balance and renal function.
Losartan can be used concurrently with other antihypertensive drugs.
Combined use with aliskiren for patients with diabetes mellitus and renal failure (at a glomerular filtration rate of less than 60 ml per minute) is not recommended.
Analogs
Analogues of Losartan are: Losartan Canon, Losartan Teva, Losartan Richter, Losartan Hydrochlorothiazide, Angizar, Brozaar, Bloktran, Hyperzar, Cardomin, Klosart, Kozaar, Ksartan, Lozap, Lorista, Losakar, Lotar, Presartan.
Terms and conditions of storage
Store in a dark place, 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
Reviews of Losartan are predominantly positive, but some users report the possible development of side effects.
The price of Losartan in pharmacies
The approximate price for Losartan is: 30 tablets of 25 mg - from 109 to 157 rubles, 30 tablets of 100 mg - 315 rubles.
Losartan: prices in online pharmacies
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Drug name Price Pharmacy |
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Losartan 12.5 mg film-coated tablets 30 pcs. RUB 37 Buy |
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Losartan 12.5 mg film-coated tablets 30 pcs. RUB 45 Buy |
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Losartan 12.5 mg film-coated tablets 30 pcs. RUB 49 Buy |
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Losartan Canon 50 mg film-coated tablets 30 pcs. RUB 87 Buy |
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Losartan 25 mg film-coated tablets 30 pcs. 89 RUB Buy |
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Losartan tablets p.p. 25mg 30 pcs. 114 RUB Buy |
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Losartan 50 mg film-coated tablets 30 pcs. 114 RUB Buy |
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Losartan 50 mg film-coated tablets 30 pcs. 115 RUB Buy |
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Losartan 100 mg film-coated tablets 30 pcs. 115 RUB Buy |
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Losartan Canon 100 mg film-coated tablets 30 pcs. 126 RUB Buy |
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Losartan 50 mg film-coated tablets 30 pcs. 130 RUB Buy |
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Losartan 100 mg film-coated tablets 30 pcs. 149 r Buy |
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Losartan Canon 50 mg film-coated tablets 60 pcs. 174 r Buy |
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Losartan N tablets p.o. 12.5mg + 50mg 30 pcs. RUB 181 Buy |
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Losartan Canon tablets p.o. 50mg 60 Pcs. 183 r Buy |
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Losartan 50 mg film-coated tablets 60 pcs. 199 RUB Buy |
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Hydrochlorothiazide + Losartan 50 mg + 12.5 mg film-coated tablets 30 pcs. 207 r Buy |
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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!
