Losartan pills 50mg, 90pcs

Composition

One tablet contains:

Active ingredient:

losartan potassium-50,000 mg;

excipients:

lactose monohydrate-57,500 mg,

microcrystalline cellulose-20,000 mg,

croscarmellose sodium-5,600 mg,

povidone (polyvinylpyrrolidone low molecular weight) – 4,500 mg,

colloidal silicon dioxide-1,000 mg,

magnesium stearate-1,400 mg;

film coating:

[hypromellose − 2,400 mg, talc − 0,800 mg, titanium dioxide − 0,440 mg, macrogol 4000 (polyethylene glycol 4000) − 0,360 mg] or [dry mix for film coating containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] − 4,000 mg.

Pharmacological action

Losartan is a specific oral angiotensin II (AT1 type) receptor antagonist. Angiotensin II selectively binds to AT1 receptors found in many tissues (vascular smooth muscle, adrenal glands, kidneys, and heart) and performs several important biological functions, including vasoconstriction and aldosterone release. Angiotensin II also stimulates smooth muscle cell proliferation.

Losartan and its pharmacologically active metabolite (E 3174) both in vitroand in vivo block all physiological effects of angiotensin II, regardless of the source or route of synthesis. Losartan selectively binds to AT1 receptors; it does not bind or block the receptors of other hormones and ion channels that play an important role in regulating the function of the cardiovascular system. In addition, losartan does not inhibit the angiotensin-converting enzyme (ACE), which contributes to the degradation of bradykinin, so side effects indirectly associated with bradykinin (for example, angioedema) are quite rare.

When losartan is used, the absence of negative feedback on renin secretion leads to an increase in plasma renin activity. An increase in renin activity leads to an increase in the concentration of angiotensin II in blood plasma. However, antihypertensive activity and a decrease in plasma aldosterone concentration remain, which indicates an effective blockade of angiotensin II receptors. After discontinuation of losartan, plasma renin activity and angiotensin II concentration decreased for 3 days to the initial values observed before starting the drug. Losartan and its active metabolite have a high affinity for angiotensin II (AT1 type) receptors.

The plasma concentrations of losartan and its active metabolite, as well as the antihypertensive effect of losartan, increase with increasing dose.

The maximum antihypertensive effect develops in 3-6 weeks after the start of taking the drug.

In patients with arterial hypertension, proteinuria (more than 2 g per day), without diabetes mellitus, the use of the drug significantly reduces proteinuria, albumin and immunoglobulin G (IgG) excretion.

In postmenopausal women with arterial hypertension who took losartan at a dose of 50 mg / day for 4 weeks, there was no effect of therapy on renal and systemic prostaglandin levels.

Losartan has no effect on autonomic reflexes and does not have a long-term effect on the level of norepinephrine in blood plasma.

In patients with arterial hypertension, losartan at doses up to 150 mg per day does not cause clinically significant changes in the concentration of triglycerides, total cholesterol and high-density lipoprotein cholesterol. In the same doses, losartan does not affect the concentration of glucose in the fasting blood.

Losartan caused a decrease in the serum uric acid concentration (usually less than 0.4 mg / dl), which persisted during long-term therapy. In controlled clinical trials involving patients with arterial hypertension, there were no cases of drug withdrawal due to an increase in serum creatinine or potassium.

Indications

• hypertension;
• reduce the risk of associated cardiovascular morbidity and mortality in patients with hypertension and left ventricular hypertrophy, manifested by a reduction in the overall frequency of cardiovascular mortality, stroke and myocardial infarction;
• to protect the kidneys in patients with diabetes type 2 diabetes with proteinuria and slowing down the progression of renal failure, manifested by a decrease in the frequency of hypercreatininemia, the incidence of end-stage chronic renal disease (ESRD) requiring hemodialysis or kidney transplantation, mortality, and the reduction of proteinuria;
• chronic heart failure with failure of treatment with ACE inhibitors.

Contraindications

• hypersensitivity to any component of the drug;
• pregnancy and lactation;
• the age of 18;
• refractory hyperkalemia;
• lactose intolerance, lactase deficiency syndrome glucose-galactose malabsorption;
• dehydration;
• severe liver failure (no experience);
• concurrent use with aliskiren in patients with diabetes mellitus and/or impaired renal function (glomerular filtration rate less than 60 ml/min).

With caution

Hepatic insufficiency (less than 9 Child-Pugh scores), hypotension, reduced circulating blood volume (BCC), impaired water and electrolyte balance, hyperkalemia, bilateral renal artery stenosis or stenosis of the artery of a single kidney, renal failure, conditions after kidney transplantation, aortic and mitral stenosis, obstructive hypertrophic cardiomyopathy, a history of angioedema, severe heart failure (NYHA Functional Class IV), coronary heart disease, heart failure with life-threatening arrhythmias, cerebrovascular diseases, primary aldosteronism, heart failure with concomitant severe renal failure.

Side effects

From the cardiovascular system: dizziness, orthostatic hypotension.

From the side of metabolism: hyperkalemia.

Allergic reactions: angioedema (including swelling of the face, lips, pharynx and / or tongue), urticaria.

From the digestive system: diarrhea, increased ALT activity.

From the central nervous system: headache.

Dermatological reactions: itching.

Other services: impaired renal function, myalgia.

Interaction

When used concomitantly with high-dose diuretics, hypotension may occur.

When used concomitantly with potassium preparations, potassium-sparing diuretics, the risk of hyperkalemia increases.

Concomitant use with Indometacin may reduce the effectiveness of losartan.

Lithium intoxication has been reported with concomitant use with lithium carbonate.

When used concomitantly with orlistat, the antihypertensive effect of losartan decreases, which can lead to a significant increase in blood pressure, the development of a hypertensive crisis.

When used concomitantly with rifampicin, the clearance of losartan increases and its effectiveness decreases.

How to take, course of use and dosage

Inside, regardless of the meal.

The drug can be taken either as monotherapy or in combination with other antihypertensive drugs.

Arterial hypertension

The standard initial and maintenance dose for most patients is 50 mg once daily. The maximum antihypertensive effect is achieved after 3-6 weeks from the start of therapy.

In some patients, to achieve a greater effect, the dose may be increased to a maximum daily dose of 100 mg once a day.

In patients with reduced circulating blood volume (for example, when taking diuretics in large doses), the initial dose of the drug should be reduced to 25 mg once a day (see the section “Special instructions”).

There is no need to adjust the initial dose in elderly patients and in patients with renal insufficiency, including patients on dialysis.

Patients with hepatic insufficiency (less than 9 points on the Child-Pugh scale) during the hemodialysis procedure, as well as patients over 75 years of age, are recommended to prescribe the drug at a lower initial dose of 25 mg once a day.

Reducing the risk of associated cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy

The standard initial dose of the drug is 50 mg once a day. In the future, it is recommended to add hydrochlorothiazide or increase the dose of Losartan to 100 mg (taking into account the degree of reduction in blood pressure (BP)) in one or two doses.

Kidney protection in patients with type 2 diabetes mellitus and proteinuria

The standard initial dose of the drug is 50 mg once a day. In the future, it is recommended to increase the dose of Losartan to 100 mg once a day, taking into account the degree of reduction in blood pressure. Losartan can be prescribed together with other antihypertensive drugs (diuretics, slow calcium channel blockers, alpha-and beta-blockers, central-acting antihypertensive drugs), insulin, and other hypoglycemic drugs (sulfonylureas, glitazones, and glucosidase inhibitors).

Chronic heart failure

The initial dose of the drug is 12.5 mg once a day. As a rule, the dose is titrated at weekly intervals (i. e.12.5 mg once daily,25 mg once daily,50 mg once daily) to the usual maintenance dose of 50 mg once daily, depending on individual tolerance.

Overdose

Information about overdose of the drug is limited.

Most likely symptoms

Marked decrease in blood pressure and tachycardia; bradycardia may occur due to parasympathetic (vagal) stimulation.

Treatment

Forced diuresis, symptomatic therapy.

Neither losartan nor its active metabolite is eliminated from the body by hemodialysis.

Special instructions

It should be used with caution in patients with arterial hypotension, decreased BCC, impaired water-electrolyte balance, bilateral renal artery stenosis or stenosis of the artery of a single kidney, with renal / hepatic insufficiency

Patients who have a fluid and/or sodium deficiency should be corrected for water-electrolyte disorders before starting treatment, or a lower initial dose should be used.

In patients with dehydration (for example, those receiving high-dose diuretics), symptomatic hypotension may occur at the beginning of losartan treatment.

If renal function is impaired, it may be necessary to reduce the dose of losartan.

In patients with a history of liver disease, losartan should be used in low doses. With cirrhosis of the liver, the concentration of losartan in the blood plasma increases significantly.

During treatment, blood potassium levels should be regularly monitored, especially in elderly patients with impaired renal function.

Concomitant use of losartan with potassium-sparing diuretics should be avoided.

The safety and efficacy of losartan in children have not been established.

Form of production

Film-coated tablets

Active ingredient

Losartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Heart failure, Prevention of heart attacks and strokes, Hypertension