Losartan Canon, 50 mg 60 pcs

Pharmacotherapeutic group:

Angiotensin II receptor antagonist.

Chronic code: C09CA01

Indications

Hypertension (high blood pressure), Heart failure, Prevention of heart attacks and strokes

• Arterial hypertension.
• Risk reduction for cardiovascular disease and mortality in patients with hypertension and left ventricular hypertrophy.
• Chronic heart failure (as part of combined therapy, with intolerance or ineffectiveness of ACE inhibitor therapy).
• In patients with diabetes mellitus type 2 with proteinuria to slow down the progression of renal failure, manifested by decreased incidence of hypercreatininemia, the rate of end-stage chronic renal failure requiring dialysis or renal transplantation, mortality rates, and decreased proteinuria

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Active ingredient

Losartan

Composition

1 film-coated tablet, 50 mg contains:

active ingredient: losartan potassium 50 mg;

auxiliary substances:

corn starch 25.4 mg,

croscarmellose sodium 5.5 mg,

mannitol 30 mg,

Magnesium stearate 1 mg,

Povidone 3.1 mg,

Microcrystalline cellulose 25 mg;

The film coating:

Opadray white 4 mg, including: hypromellose (hydroxypropyl methylcellulose) 1.35 mg, hyprolose (hydroxypropyl cellulose) 1.35 mg, talc 0.8 mg, titanium dioxide 0.5 mg.

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How to take, the dosage

Overly, regardless of meals. Tablets are swallowed without chewing, with water. Frequency of intake is 1 time per day, preferably at the same time, in the morning.

Hypertension

The starting and maintenance dose is 50 mg/day. If necessary, the daily dose may be increased to a maximum of 100 mg. If a single dose does not give the target BP, the daily dose should be divided into 2 doses: 25 mg (25 mg lozartan or 50 mg lozartan with rice) 2 times daily or 50 mg 2 times daily.

Lowering cardiovascular risk and mortality in patients with arterial hypertension and left ventricular hypertrophy

The initial dose of the drug is 50 mg once daily. Subsequently, hydrochlorothiazide may be added in low doses or the dose of Lozartan Canon may be increased to a maximum of 100 mg in one or two doses with regard to BP reduction.
Chronic Heart Failure

The initial dose for patients with chronic heart failure is 12.5 mg (Lozartan in 25 mg tablets with rice is possible) 1 time/day. The dose is titrated 2 times, depending on patient tolerance, at weekly intervals, i.e., 12.5 mg/day, 25 mg/day, 50 mg/day to an average maintenance dose of 50 mg/day. No dose adjustment is required in elderly patients with renal insufficiency.

In patients with type 2 diabetes mellitus with proteinuria to slow the progression of renal failure
The initial dose is 50 mg once daily with further increase to a maximum dose of 100 mg/day (depending on the degree of BP reduction) in one or two doses.

Particular patient groups

In patients with decreased circulating blood volume (RBC) (e.g., when taking high-dose diuretics), the recommended starting dose of Losartan Canon is 25 mg (losartan 25 mg tablets or 50 mg tablets with a rice may be used).

Patients with hepatic impairment (less than 9 points on the Child-Pugh scale), hemodialysis procedures, and patients older than 75 years are recommended a lower starting dose of 25 mg (the use of losartan in 25 mg tablets or in 50 mg tablets with a ribbon is possible) once daily.

There is insufficient experience in using the drug in patients with severe hepatic impairment; therefore, the drug is not recommended in this category of patients (see section “Contraindications”).

In patients with moderate renal impairment (CKR 20-30 ml/min), no dose adjustment is required.

Interaction

Can be used concomitantly with other hypotensive agents.

No clinically significant drug interactions of losartan with hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole and erythromycin have been reported. Rifampicin and fluconazole have been reported to decrease plasma concentrations of the active metabolite. The clinical significance of these interactions is not yet known.
As with other agents that block angiotensin II formation and effects, concomitant administration of potassium-saving diuretics (spironolactone, triamterene, amiloride), potassium supplements and salts containing potassium may result in increased serum potassium ions.

Hypotensive agents may increase the antihypertensive effects of losartan.Also, tricyclic antidepressants, neuroleptics, baclofen, and amifostine may increase the antihypertensive effects of losartan, which lower blood pressure as a primary or side effect and may increase the risk of arterial hypotension.

The simultaneous use of angiotensin II receptor antagonists and nonsteroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase-2 inhibitors, acetylsalicylic acid as an anti-inflammatory agent) may decrease the antihypertensive effects of losartan. In patients with impaired renal function, concomitant use of angiotensin II antagonists or diuretics and NSAIDs may cause further impairment of renal function, including acute renal failure and increased serum potassium. This combination should be used with caution, especially in elderly patients.

When concomitant use of lithium with ACE inhibitors a reversible increase in serum lithium concentration and development of toxicity has been reported; in very rare cases this has been observed with angiotensin II receptor antagonists. Caution should be exercised when using lithium concomitantly with losartan. If this combination is necessary, it is recommended that serum lithium concentrations be monitored.

Mutually enhances the effect of beta-adrenoblockers and sympatholytics; coadministration of losartan with diuretics causes an additive effect.

Dual RAAS blockade (e.g., by combining an angiotensin II receptor antagonist with ACE inhibitors or aliskiren) in patients with diagnosed atherosclerosis, heart failure or diabetes mellitus with target organ damage is associated with a higher incidence of arterial hypotension, syncope, hyperkalemia and renal dysfunction (including the development of acute renal failure) compared to the use of single RAAS blockade. Double RAAS blockade should be controlled individually in each case with careful monitoring of blood pressure, blood water-electrolyte balance and renal function.

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Special Instructions

Patients with decreased RBC (e.g., those receiving high doses of diuretics) may experience symptomatic arterial hypotension, so replete the RBC or initiate lower-dose treatment with losartan canon before starting treatment.

In patients with cirrhosis, plasma concentrations of losartan are significantly increased, so it should be prescribed in lower doses if there is a history of liver disease.

Pharm plasma potassium and creatinine clearance should be monitored regularly during therapy, especially in elderly patients, patients with impaired renal function, patients with type 2 diabetes complicated by nephropathy; and these parameters should be monitored particularly carefully in patients with heart failure with concomitant renal impairment.

Preventive RAAS medications can increase urate and serum creatinine concentrations in patients with bilateral renal artery stenosis or arterial stenosis of the sole kidney.

There is no experience with losartan in patients after renal transplantation.

In patients with severe chronic heart failure, drugs that affect the RAAS can lead to severe arterial hypotension and acute renal failure. There are isolated reports of the development of oliguria and/or increasing azotemia and acute renal failure, including death.

There is insufficient experience with losartan in patients with heart failure with concomitant severe renal failure, in patients with severe chronic heart failure (NYHA functional class IV), in patients with heart failure with life-threatening arrhythmias. In these groups, caution should be exercised when using Lozartan Canon with beta-adrenoblockers.

As with all drugs with vasodilatory effects, Losartan Canon should be administered with caution in patients with aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy.

In patients with cerebrovascular disease of ischemic nature, excessive BP reduction may lead to stroke. Physician supervision is recommended when titrating the dose.

Caution should be exercised when prescribing Lozartan Canon in patients with a history of angioedema, including when taking other medications, including ACE inhibitors.
Patients with primary hyperaldosteronism usually do not respond to hypotensive agents acting through inhibition of the renin-angiotensin system. Therefore, the use of Lozartan Canon is not recommended for the treatment of such patients.

Impact on driving and operating machinery

There have been no studies to evaluate the effect of the drug on driving and operating machinery.
Drowsiness and dizziness may occur, so caution should be exercised when performing tasks requiring increased attention, especially at the beginning of treatment, when increasing the drug dose and when driving vehicles.

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Contraindications

• High sensitivity to the active substance or other components of the drug.
• Arterial hypotension.
• Severe hepatic insufficiency (more than 9 points on the Child-Pugh scale).
• Primary hyperaldosteronism.
• Simultaneous use with aliskiren in patients with diabetes and patients with renal impairment (creatinine clearance less than 60 ml/min).
• Pregnancy, period of breastfeeding.
• Age under 18 years of age (efficacy and safety not established).

With caution

• Disorders of water-electrolyte balance of the blood (hyponatremia, hypochloremic alkalosis, hypomagnesemia, hypokalemia, hyperkalemia).
• Decrease in circulating blood volume (CBC).
• Bilateral stenosis of the renal arteries or stenosis of the artery of the sole kidney, renal failure
• Condition after renal transplantation (no experience of use).
• Aortic and mitral stenosis, hypertrophic obstructive cardiomyopathy, heart failure with concomitant severe renal failure, severe chronic heart failure (NYHA functional class IV), heart failure with life-threatening arrhythmias, ischemic heart disease.
• Cerebrovascular disease.
• Hepatic failure (less than 9 points on the Child-Pugh scale.
• Angeoneurotic edema in the history.

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Side effects

WHO Classification of frequency of side effects:
very often ≥1/10 appointments (>10%)
often ≥1/100 to < 1/10 appointments (>1% and < 10%)
infrequent ≥1/1000 to < 1/100 appointments (>01 % and < 1 %)
rarely from ≥1/10000 to < 1/1000 appointments (>0.01 % and < 0.1 %)
very rarely < 1/10000 appointments (< 0.01 %)
frequency is unknown on the available data it is impossible to determine the incidence.

Disorders of the blood and lymphatic system:
Rarely: anemia, thrombocytopenia.

Disorders of the immune system:
Rarely: skin rash, urticaria, pruritus, angioedema (including laryngeal and tongue edema), Quincke’s edema, allergic vasculitis, Schoenlein-Henoch purpura.

Nervous system disorders:
Often: dizziness, headache, sleep disturbance, insomnia.
Infrequent: restlessness, somnolence, memory disturbance, peripheral neuropathy, paresthesia, hypoesthesia, migraine, tremor, ataxia, depression, syncope, acute cerebrovascular disorders.

Visual organ disorders:
Infrequent: visual acuity disorders, conjunctivitis.

Hearing organ and labyrinth disorders:
Infrequent: tinnitus.

Taste organ disorders:
Infrequent: taste disturbance.

Heart disorders:
Often: palpitations, tachycardia, bradycardia, arrhythmia.
Infrequent: angina pectoris.

Vascular disorders:
Infrequent: orthostatic hypotension (dose-dependent).

Respiratory system, thoracic and mediastinal disorders:
Often: cough, upper respiratory tract infections (pharyngitis, rhinitis, sinusitis, bronchitis), nasal mucous edema.
Infrequently: dyspnea.

Gastrointestinal tract disorders:
Often: nausea, diarrhea, abdominal pain, dyspeptic disorders.
Infrequent: anorexia, dry mouth, vomiting, flatulence, constipation, gastritis.

Liver and biliary tract disorders:
Infrequent: impaired liver function.
Rarely: hepatitis.

Skin and subcutaneous tissue disorders:
Infrequent: dry skin, erythema, skin hyperemia, photosensitization, increased sweating, alopecia.

Muscular and connective tissue disorders:
Often: muscle cramps of the lower extremities, myalgia, back, chest and leg pain.
Infrequent: arthritis, arthralgia, fibromyalgia, rhabdomyolysis.

Renal and urinary tract disorders:
Infrequent: urinary tract infections, impaired renal function, urgent urge to urinate, acute renal failure.

Gender and mammary gland disorders:
Infrequent: decreased libido, impotence.

General disorders:
Often: asthenia, increased fatigue.

Laboratory and instrumental data:
Often: hyperkalemia.
Infrequent: moderate increase in serum urea and creatinine levels, hypoglycemia, hyponatremia, hyperuricemia.
Very rare: increased activity of “liver” enzymes, hyperbilirubinemia.

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Overdose

Symptoms: marked decrease in blood pressure (BP), tachycardia. Bradycardia may occur due to parasympathetic (vagus) stimulation.

Treatment: forced diuresis, symptomatic therapy. Hemodialysis is not effective.

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Similarities

Lozap, Lorista, Presartan, Bloctran, Lozartan