Losartan Canon
Losartan Canon: 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 Canon
ATX code: C09CA01
Active ingredient: losartan (Losartan)
Producer: CJSC "Kanonfarma Production" (Russia); CJSC "Raduga Production" (Russia); LLC "Plant named after academician V. P. Filatov "(Russia)
Description and photo update: 2019-05-07
Prices in pharmacies: from 87 rubles.
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Losartan Canon is an antihypertensive drug, angiotensin II receptor antagonist.
Release form and composition
The drug is available in the form of film-coated tablets: almost white or white, biconvex, round, the core of the tablet is white or almost white (tablets in blisters: 7 pcs., In a cardboard box 1, 2 or 4 packages; by 10 pcs., In a carton box 1, 3 or 6 packs; 28 pcs., In a carton box 1 or 2 packs; 30 pcs., In a cardboard box 1, 2 or 3 packs. Each pack also contains instructions for use Losartan Canon).
1 tablet contains:
- active substance: losartan potassium - 50 mg or 100 mg;
- auxiliary components: corn starch, povidone, croscarmellose sodium, magnesium stearate, mannitol, microcrystalline cellulose;
- composition of the film shell: white opadry [titanium dioxide, hypromellose (hydroxypropyl methylcellulose), talc, hyprolose (hydroxypropyl cellulose)].
Pharmacological properties
Pharmacodynamics
Losartan Canon is an antihypertensive drug. Its active ingredient, potassium losartan, is a selective angiotensin II receptor antagonist (type AT 1). Angiotensin II is a powerful vasoconstrictor, the main active hormone of the renin-aldosterone-angiotensin system (RAAS) and a decisive pathophysiological link in the development of arterial hypertension. As a result of the selective binding of angiotensin II to AT 1-receptors that are found in the smooth muscle tissues of blood vessels, in the heart, adrenal glands and kidneys, it narrows the lumen of blood vessels (especially arteries), releases aldosterone and performs other important biological functions. Angiotensin II also potentiates the proliferation of smooth muscle cells. Losartan, in contrast to individual peptide angiotensin II antagonists, does not have agonist effects. The action of the substance and its pharmacologically active metabolite (E-3174) is aimed at blocking all physiological effects of angiotensin II, in vitro and in vivo, regardless of the source or route of synthesis.
Losartan is characterized by selective binding to AT 1 -receptors; it does not affect the receptors of other hormones and ion channels, which are actively involved in the regulation of the function of the cardiovascular system. It does not inhibit the angiotensin-converting enzyme (ACE), which is responsible for the destruction of bradykinin. Therefore, the development of bradykinin-mediated and other effects not directly related to the blockade of AT 1 receptors are not related to the action of losartan. So peripheral edema was observed when taking losartan in 1.7% of cases, and in the placebo group in 1.9%.
When losartan is taken orally, OPSS (total peripheral vascular resistance), the concentration of aldosterone and norepinephrine in the blood, blood pressure (BP) and pressure in the pulmonary circulation decrease, and a diuretic effect is manifested. Afterload decreases, the risk of myocardial hypertrophy decreases, with chronic heart failure, exercise tolerance increases. Losartan increases the plasma activity of renin, causing an increase in plasma angiotensin II.
A single dose of Losartan Canon provides a maximum decrease in systolic and diastolic blood pressure after 6 hours, then within 24 hours the antihypertensive activity of the drug gradually decreases. In the process of regular use of losartan, hypotensive activity, and a decrease in the concentration of aldosterone in blood plasma is manifested after 14 and 42 days of therapy, this indicates an effective blockade of angiotensin II receptors. 3 days after replacing losartan with another agent, there is a decrease in plasma renin activity and angiotensin II level to the values noted before the start of treatment.
The activity of the metabolite E-3174 is 10–40 times higher than that of losartan. The affinity of the active substance and its active metabolite for the AT 1 type receptors is higher than for the AT 2 type receptors.
Pharmacokinetics
After oral administration, the absorption of losartan from the gastrointestinal tract is good. At the same time, with the participation of the isoenzyme CYP2C9, the active substance is metabolized by carboxylation during the first passage through the liver to form the active metabolite E-3174.
Systemic bioavailability is approximately 33%. The maximum concentration (C max) in the blood serum of losartan is reached after 1 hour, the active metabolite - after about 3-4 hours. Concomitant food intake does not affect the bioavailability of losartan.
Plasma protein binding of losartan and E-3174 - 99% (mainly with albumin).
Vd (volume of distribution) - 34 liters.
Losartan practically does not overcome the blood-brain barrier.
In doses up to 200 mg, losartan and its active metabolite are characterized by linear pharmacokinetics. Against the background of therapy, 100 mg 1 time per day, there is no clinically significant accumulation in the blood plasma of either losartan or its active metabolite.
Approximately 14% of the dose of losartan is transformed into the active metabolite E-3174. In addition, as a result of hydroxylation of the butyl side chain, two main metabolites and one minor metabolite, N-2-tetrazole-glucuronide, are formed. They have no biological activity.
Plasma clearance of losartan is about 600 ml / min, E-3174 - 50 ml / min, renal clearance is 74 and 26 ml / min, respectively.
Through the kidneys, about 4% of the dose of losartan taken orally is excreted unchanged, including the form of an active metabolite - about 6%.
Plasma concentrations of the drug decrease poly-exponentially, the final half-life (T 1/2) of losartan is approximately 2 hours, E-3174 - 6-9 hours.
The drug is excreted through the intestines with bile up to 58% and kidneys - about 35%.
In elderly men with arterial hypertension, the concentration of losartan and the metabolite E-3174 in the blood plasma does not differ significantly from those in younger male patients with hypertension.
With arterial hypertension in women, the plasma concentration of losartan is 2 times higher than in men, and the level of the active metabolite in men and women is the same. This pharmacokinetic difference is not clinically significant.
In patients with mild and moderate alcoholic cirrhosis of the liver, the concentration of losartan in the blood plasma is 5 times higher than in young healthy male volunteers; for the active metabolite, this indicator is 1.7 times.
In case of impaired renal function with creatinine clearance (CC) above 10 ml / min, plasma concentrations of losartan are comparable to those in individuals with unchanged renal function. In patients on hemodialysis, the total concentration of losartan in the blood plasma increases by about 2 times. Plasma concentrations of the active metabolite in patients with impaired renal function or on hemodialysis do not change. The drug is not excreted by hemodialysis.
Indications for use
- arterial hypertension;
- arterial hypertension with concomitant left ventricular hypertrophy - to reduce the risk of cardiovascular disease and mortality;
- chronic heart failure - as part of combination therapy in patients with intolerance or ineffectiveness of therapy with ACE inhibitors;
- type 2 diabetes mellitus with proteinuria - in order to reduce the progression of renal failure (hypercreatininemia, development of end-stage chronic renal failure, requiring dialysis / kidney transplantation, reduce mortality rates) and reduce proteinuria.
Contraindications
Absolute:
- arterial hypotension;
- primary hyperaldosteronism;
- severe liver failure (more than 9 points on the Child-Pugh scale);
- simultaneous use of aliskiren for diabetes mellitus and renal failure (CC less than 60 ml / min);
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to the components of the drug.
With caution, Losartan Canon tablets should be prescribed during the period after kidney transplantation, with renal failure, bilateral renal artery stenosis or stenosis of a solitary kidney artery, heart failure with concomitant severe renal failure, chronic heart failure of functional class IV according to the NYHA classification (New York Heart Association), hypertrophic obstructive cardiomyopathy, aortic and mitral stenosis, ischemic heart disease, heart failure with life-threatening arrhythmias, disturbances in water and electrolyte balance (hypokalemia, hypomagnesemia, hyponatremia, hyperkalemia, hypochloremic alkalosis), with a decrease in circulating blood volume, insufficiency (less than 9 points on the Child-Pugh scale), cerebrovascular diseases,angioneurotic edema in history.
Losartan Canon, instructions for use: method and dosage
Losartan Canon tablets are taken orally, swallowed whole and washed down with water, in the morning, before or after breakfast, preferably at the same time.
Recommended dosage:
- arterial hypertension: initial and maintenance dose - Losartan Canon 50 mg once a day, if necessary, it can be increased to 100 mg. If the target blood pressure level is not achieved with a single dose of the drug, then the daily dose should be divided into 2 doses: with a dosage regimen of 50 mg, take 25 mg 2 times a day, 100 mg - 50 mg 2 times a day. The maximum daily dose is 100 mg;
- arterial hypertension with concomitant left ventricular hypertrophy (reducing the risk of cardiovascular disease and mortality): initial dose - Losartan Canon 50 mg 1 time per day. Further, taking into account the decrease in blood pressure, it is possible to increase the daily dose to 100 mg in 1 or 2 doses or the concomitant administration of low doses of hydrochlorothiazide;
- chronic heart failure: initial dose - 12.5 mg once a day. The maintenance dose is selected by titration with an interval of 7 days, with good patient tolerance of the drug at a dose of 12.5 mg, after 7 days, 25 mg is prescribed once a day, then 50 mg;
- type 2 diabetes mellitus with proteinuria (to slow the progression of renal failure): the initial dose is 50 mg 1 time per day, followed by an increase to 100 mg per day in 1 or 2 doses (depending on the degree of blood pressure reduction).
With a reduced BCC (including patients taking high doses of diuretics), the initial dose of the drug should be 25 mg.
Dose adjustment is not required in elderly patients with renal insufficiency.
In hepatic impairment (less than 9 points on the Child-Pugh scale), during hemodialysis, or for patients over the age of 75, it is recommended to use an initial dose of 25 mg.
For the treatment of patients with moderate renal impairment (CC 20-30 ml / min), you can use the usual doses of Losartan Canon.
Side effects
- on the part of the hematopoietic system: rarely - thrombocytopenia, anemia;
- from the nervous system: often - insomnia, sleep disturbances, headache, dizziness; infrequently - drowsiness, anxiety, memory disorder, migraine, paresthesia, hypesthesia, peripheral neuropathy, tremor, ataxia, syncope, depression, acute cerebrovascular accident;
- on the part of the cardiovascular system: often - arrhythmia, palpitations, bradycardia, tachycardia; infrequently - orthostatic hypotension (dose-dependent), angina pectoris;
- on the part of the organ of vision: infrequently - conjunctivitis, impaired visual acuity;
- from the organ of hearing: infrequently - ringing in the ears;
- from the respiratory system: often - cough, swelling of the nasal mucosa, infectious diseases of the upper respiratory tract (rhinitis, sinusitis, pharyngitis, bronchitis); infrequently - dyspnea;
- from the digestive system: often - abdominal pain, nausea, dyspeptic disorders, diarrhea; infrequently - dry mouth, taste disturbance, vomiting, gastritis, flatulence, constipation, anorexia, liver dysfunction; rarely - hepatitis;
- from the urinary system: infrequently - an urgent urge to urinate, impaired renal function, acute renal failure, urinary tract infections;
- on the part of the genitals and breast: infrequently - decreased libido, impotence;
- dermatological reactions: infrequently - increased sweating, erythema, dry skin, skin flushing, alopecia, photosensitivity;
- from the musculoskeletal system: often - pain in the chest, back, legs, myalgia, cramps in the muscles of the lower extremities; infrequently - fibromyalgia, arthritis, arthralgia, rhabdomyolysis;
- allergic reactions: rarely - itching, skin rash, urticaria, Quincke's edema, angioedema (including edema of the tongue and larynx), allergic vasculitis, Shenlein's purpura - Genoch (hemorrhagic vasculitis);
- laboratory and instrumental parameters: often - hyperkalemia; infrequently - hypoglycemia, moderate increase in serum urea and creatinine levels, hyperuricemia, hyponatremia; very rarely - hyperbilirubinemia, increased activity of hepatic enzymes;
- others: often - increased fatigue, asthenia.
Overdose
- symptoms: a significant decrease in blood pressure, tachycardia; as a result of parasympathetic (vagal) stimulation, bradycardia may develop;
- therapy: forced diuresis, the appointment of symptomatic treatment; hemodialysis is not effective.
special instructions
Due to the increased risk of symptomatic arterial hypotension during the use of Losartan Canon in patients with reduced BCC (including patients taking high-dose diuretics), the BCC should be replenished before treatment is started or treatment should be started with low doses of losartan.
Patients with a history of liver disease are advised to prescribe a lower daily dose of Losartan Canon.
Treatment should be accompanied by regular monitoring of CC and plasma potassium levels, especially in the following cases: with impaired renal function; with type 2 diabetes mellitus complicated by nephropathy; in elderly patients. The most careful monitoring of these indicators is required in patients with heart failure and concomitant renal impairment.
It should be borne in mind that with bilateral renal stenosis or stenosis of an artery of a single kidney, losartan can cause an increase in serum creatinine and blood urea concentration.
Particular care is required in patients with severe chronic heart failure. This is due to the fact that taking drugs that affect the RAAS can cause in this category of patients the development of severe arterial hypotension, acute renal failure, increasing azotemia and / or oliguria, including with a lethal outcome.
There is no sufficient experience with the use of Losartan Canon in heart failure with concomitant severe renal failure, life-threatening arrhythmias, severe chronic heart failure. In these groups, the drug should be used with caution in combination with beta-blockers.
Dose titration in patients with cerebrovascular ischemic diseases is recommended to be performed under medical supervision, since a significant decrease in blood pressure can lead to stroke.
Influence on the ability to drive vehicles and complex mechanisms
In connection with the possible development of drowsiness and dizziness, care should be taken when performing work requiring increased attention, including driving vehicles, especially at the beginning of treatment or when increasing the dose of Losartan Canon.
Application during pregnancy and lactation
The use of Losartan Canon is contraindicated during the period of gestation and breastfeeding.
When the fact of conception is established, the use of losartan should be stopped immediately.
In the first trimester of pregnancy, the exception is those women for whom it is not possible to use other antihypertensive drugs. The appointment of Losartan Canon in this case is allowed only under close medical supervision, including a weekly fetal ultrasound examination. Treatment should be discontinued if signs of oligohydramnios are found. The risk to the fetus in the first trimester is lower than in the later period, since the RAAS-dependent renal perfusion in the fetus appears in the second trimester.
Reception of Losartan Canon in the II or III trimester of pregnancy causes a developmental disorder, a decrease in kidney function in a child, a slowdown in the ossification of the skull bones, the development of oligohydramnios and can lead to fetal death. In newborns exposed to the toxic effects of an angiotensin II receptor antagonist in the womb in the second or third trimester, renal failure, arterial hypotension, and hyperkalemia may occur.
It should be borne in mind that newborns and infants who have been exposed to an angiotensin II receptor antagonist in utero need to be closely monitored for the timely detection of oliguria, hyperkalemia, and a significant decrease in blood pressure.
If it is necessary to use Losartan Canon during lactation, breastfeeding should be discontinued.
Pediatric use
The appointment of Losartan Canon under the age of 18 is contraindicated due to the lack of information on the efficacy and safety of the drug in children and adolescents.
With impaired renal function
Caution should be exercised when prescribing Losartan Canon for patients with renal failure, bilateral renal artery stenosis or stenosis of an artery of a single kidney, as well as in the period after kidney transplantation.
With moderate impairment of renal function (CC 20-30 ml / min), you can use the usual doses of the drug. The starting dose for patients on hemodialysis should be 25 mg.
For violations of liver function
The use of Losartan Canon for the treatment of patients with severe hepatic failure (more than 9 points on the Child-Pugh scale) is contraindicated.
In case of liver failure less than 9 points on the Child-Pugh scale, Losartan Canon should be prescribed with caution. The initial dose should not exceed 25 mg.
Use in the elderly
In elderly patients, including with renal failure, dose adjustment is not required.
The initial daily dose of Losartan Canon for patients over the age of 75 years should not exceed 25 mg.
Drug interactions
With the simultaneous use of Losartan Canon:
- antihypertensive drugs: you can take other antihypertensive drugs, but you should take into account the increased action of losartan;
- digoxin, warfarin, hydrochlorothiazide, cimetidine, ketoconazole, erythromycin, phenobarbital: no clinically significant drug interactions with these substances were noted;
- rifampicin, fluconazole: a decrease in the concentration of the active metabolite of losartan in blood plasma was noted when combined with rifampicin and fluconazole, but the clinical significance of this interaction has not been established;
- potassium-sparing diuretics (spironolactone, amiloride, triamterene), potassium supplements, potassium-containing salts: the concomitant administration of these and other drugs that block the formation and effects of angiotensin II can cause an increase in the content of potassium ions in the blood serum;
- tricyclic antidepressants, amifostine, antipsychotics, baclofen: drugs that reduce blood pressure as a main or side effect can increase the risk of arterial hypotension, increasing the hypotensive effect of the drug;
- nonsteroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of cyclooxygenase-2, anti-inflammatory doses of acetylsalicylic acid: taking NSAIDs can help reduce the hypotensive effect of losartan, in patients with impaired renal function - cause deterioration of renal function, up to acute renal failure and an increase in potassium in serum. This combination should be used with caution, especially for elderly patients;
- lithium preparations: in very rare cases, the combination with lithium preparations can cause a reversible increase in the level of lithium in the blood serum and the development of toxicity. The combination of losartan with lithium should be accompanied by monitoring the concentration of the latter in the blood serum;
- beta-blockers, sympatholytics: there is a mutual enhancement of the effects of these funds and losartan;
- diuretics: taking diuretics has an additive effect.
Compared with the use of a single-component RAAS blockade, double RAAS blockade in patients with atherosclerosis, heart failure or diabetes mellitus with target organ damage increases the risk of arterial hypotension, hyperkalemia, renal dysfunction (including acute renal failure), and fainting. Therefore, the question of prescribing a combination of Losartan Canon with ACE inhibitors or aliskiren should be decided individually, treatment should be carried out under close monitoring of blood pressure, renal function and water-electrolyte balance of the blood.
Analogs
Losartan Canon analogs are Losartan, Renikard, Lozap, Zisakar, Lorista, Bloktran, Kozaar, Losakor, Lozarel, Karzartan, Vasotenz, Prezartan, Cardomin-Sanovel, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C, protected from moisture and light.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Losartan Canon
Patients, pointing out in reviews of Losartan Canon about its effectiveness, in some cases note the development of undesirable phenomena, including cough.
The price of Losartan Canon in pharmacies
The price of Losartan Canon for a package containing 30 tablets in a dose of 100 mg can be from 172 rubles, 60 tablets - from 291 rubles; at a dose of 50 mg: 90 tablets - from 285 rubles, 60 tablets - from 177 rubles.
Losartan Canon: prices in online pharmacies
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Drug name Price Pharmacy |
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Losartan Canon 50 mg film-coated tablets 30 pcs. RUB 87 Buy |
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Losartan Canon tablets p.o. 50mg 30 Pcs. 114 RUB Buy |
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Losartan Canon 100 mg film-coated tablets 30 pcs. 126 RUB Buy |
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Losartan Canon 50 mg film-coated tablets 60 pcs. 174 r Buy |
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Losartan Canon tablets p.o. 50mg 60 Pcs. 183 r Buy |
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Losartan Canon tablets p.o. 100mg 30 pcs. 230 RUB Buy |
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Losartan Canon tablets p.o. 50mg 90 Pcs. 249 r Buy |
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Losartan Canon 50 mg film-coated tablets 90 pcs. 249 r Buy |
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Losartan Canon 100 mg film-coated tablets 60 pcs. 266 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!
