Instruction for use: LosarelI want this, give me price
Dosage form: film coated tablets
Active substance: Losartanum
Angiotensin II receptor antagonists (AT1 subtype)
Nosological classification (ICD-10)
I10 Essential (primary) hypertension: hypertension; Arterial hypertension; Arterial hypertension crisis course; Essential Hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Primary hypertension; Arterial hypertension, complications of diabetes; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; arterial Hypertension; malignant Hypertension; Hypertonic disease; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; Isolated systolic hypertension
I15 Secondary hypertension: Arterial hypertension, complications of diabetes; hypertension; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; hypertension; arterial Hypertension; malignant Hypertension; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; hypertension; Arterial hypertension; Arterial hypertension crisis course; renovascular hypertension; Hypertension symptomatic; Renal hypertension; Renovascular hypertension; renovascular hypertension; Symptomatic hypertension
I50.0 Congestive heart failure: anasarca heart; Decompensated congestive heart failure; Congestive heart failure; Congestive heart failure with high afterload; Congestive chronic heart failure; Cardiomyopathy with severe chronic heart failure; Compensated chronic heart failure; Swelling with circulatory failure; Edema of cardiac origin; Swelling of the heart; Edematous syndrome in diseases of the heart; Edematous syndrome in congestive heart failure; Edematous syndrome in heart failure; Edematous syndrome in heart failure or liver cirrhosis; right ventricular failure; Congestive Heart Failure; Heart failure stagnant; Heart failure with low cardiac output; Heart failure is a chronic; Cardiac edema; Chronic decompensated heart failure; Chronic Congestive Heart Failure; Chronic heart failure; Change of liver function in heart failure
I50.1 Left ventricular failure: Cardiac asthma; Asymptomatic dysfunction of the left ventricle; Asymptomatic left ventricular heart failure; Diastolic dysfunction of the left ventricle; Left ventricular dysfunction; Changes in the left ventricle with myocardial infarction; Left ventricular heart failure; Violation of the function of the left ventricle; Acute left ventricular failure; Acute cardiac left ventricular failure; Cardiac asthma; Heart failure of left ventricular; Changes in the lungs with left ventricular failure; Precordial abnormal pulsation; Lack of left ventricle
N08.3 Glomerular lesions in diabetes mellitus (E10-14 + with common fourth sign .2): Nephropathy diabetic; Diabetic Nephropathy; Diabetic nephropathy in the background of type 1 diabetes mellitus; Diabetic nephropathy in patients with type I diabetes; Proteinuria in patients with type 2 diabetes mellitus
N39.1 Persistent proteinuria, unspecified: Severe proteinuria; Proteinuria; Nephrotic-proteinuric syndrome
Composition and release form
Tablets covered with a film coating.
active substance: Losartan potassium 50 mg
Auxiliary substances: MCC; Lactose monohydrate; Pregelatinized starch; Silicon dioxide colloidal anhydrous; Magnesium stearate
Film membrane: hypromellose; Giprolose; Macrogol 400; Titanium dioxide (E171); talc
In the blister 10 pcs .; In a pack of cardboard 3 blisters.
Description of dosage form
Tablets: round, biconvex, white or white with a yellowish tinge color, covered with a film sheath, with a risk on one side.
Losartan is a specific antagonist of angiotensin II (type AT1) receptors.
Mode of action - antihypertensive, blocking AT1-receptors.
Angiotensin II selectively binds to the AT1 receptors found in many tissues (in the smooth muscle tissues of the vessels, adrenal glands, kidneys and heart) and causes vasoconstriction and release of aldosterone, smooth muscle proliferation.
In vitro and in vivo studies have shown that losartan and its pharmacologically active metabolite block all physiologically important effects of angiotensin II, regardless of the source or route of its synthesis.
Reduces OPSS, concentration in the blood of aldosterone, blood pressure, pressure in a small circle of blood circulation; Reduces afterload, has a diuretic effect. Prevents development of myocardial hypertrophy, increases exercise tolerance in patients with chronic heart failure (CHF). After a single oral intake, the antihypertensive effect (decreases SAD and DAD) reaches a maximum after 6 hours, then gradually decreases within 24 hours. The maximum hypotensive effect develops in 3-6 weeks after regular intake of the drug. It does not inhibit ACE and, accordingly, does not interfere with the destruction of bradykinin, therefore, Losartan has no side effects, indirectly associated with bradykinin (eg, angioedema).
In patients with arterial hypertension without concomitant diabetes mellitus with proteinuria (more than 2 g / day), the use of the drug significantly reduces proteinuria, albumin and immunoglobulin G excretion.
Stabilizes the level of urea in the blood plasma. Does not affect vegetative reflexes and does not have a long-term effect on the level of norepinephrine in the blood plasma.
In a dose up to 150 mg once a day does not affect the level of triglycerides, total cholesterol and HDL cholesterol in the blood serum in patients with arterial hypertension. At the same dose, losartan does not affect the fasting blood glucose level.
When ingested, losartan is well absorbed and is metabolized at the first passage through the liver by carboxylation with the participation of cytochrome P450 2S9 isoenzyme with the formation of an active metabolite. Systemic bioavailability of losartan is about 33%. Cmax of losartan and its active metabolite is reached in the blood serum approximately after 1 hour and 3-4 hours after ingestion, respectively. Eating does not affect the bioavailability of losartan.
More than 99% of losartan and its active metabolite binds to blood plasma proteins, mainly with albumins. Vd Losartan - 34 liters. Losartan practically does not penetrate the BBB.
Approximately 14% of losartan administered to the patient in / in or inside is converted to an active metabolite.
The plasma clearance of losartan is 600 ml / min, and the active metabolite 50 ml / min. The renal clearance of losartan and its active metabolite is 74 and 26 ml / min, respectively. When administered orally, approximately 4% of the dose taken is excreted by the kidneys unchanged and about 6% is excreted by the kidneys in the form of an active metabolite. Losartan and its active metabolite is characterized by linear pharmacokinetics when ingested at doses up to 200 mg. After oral administration, plasma concentrations of losartan and its active metabolite decrease polyexponentially with a final T1 / 2 losartan for about 2 hours and an active metabolite about 6-9 hours. When taking the drug at a dose of 100 mg / day, neither losartan nor the active metabolite significantly cumulate Blood plasma.
Losartan and its metabolites are excreted through the intestine and the kidneys.
Pharmacokinetics in specific patient groups
In patients with alcoholic liver cirrhosis of mild and moderate severity, the concentration of losartan was 5 times, and the active metabolite was 1.7 times higher than in healthy male volunteers.
With Cl creatinine above 10 ml / min, the concentration of losartan in the blood plasma does not differ from that with normal kidney function. In patients who need hemodialysis, the AUC value is approximately 2 times higher than in patients with normal renal function.
Neither losartan nor its active metabolite is removed from the body by hemodialysis.
The concentrations of losartan and its active metabolite in blood plasma in elderly men with arterial hypertension do not differ significantly from the values of these parameters in young men with arterial hypertension. Values of plasma concentrations of losartan in women with arterial hypertension are 2 times higher than the corresponding values for men suffering from hypertension. The concentration of active metabolite in men and women does not differ. This pharmacokinetic difference is not clinically relevant.
Indications of the drug Losarel
CHF (with ineffective treatment with ACE inhibitors);
Nephropathy in type 2 diabetes mellitus (reduced risk of hypercreatininemia and proteinuria);
Reduction in the risk of cardiovascular complications and mortality in patients with hypertension and left ventricular hypertrophy.
Hypersensitivity to the components of the drug;
Age under 18 years (effectiveness and safety not established);
Lactose intolerance, galactosemia or the syndrome of impaired glucose / galactose absorption.
Hepatic and / or renal insufficiency;
Decrease in BCC;
Violation of water and electrolyte balance;
Bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney.
Usually side effects are weak and transient, do not require discontinuation of treatment.
The incidence of side effects is characterized as follows: very often -> 10%; Often -> 1, <10%, sometimes -> 0.1, <1%; Rarely -> 0.01, <0.1% and very rarely, including individual reports - <0.01%.
From the CVS: sometimes - orthostatic hypotension (dose-dependent), epistaxis, palpitations, tachycardia, bradycardia, arrhythmia, angina pectoris, myocardial infarction, vasculitis.
From the digestive tract: often - nausea, diarrhea, dyspeptic phenomena, abdominal pain; Sometimes - anorexia, a taste disorder, dry mouth, toothache, vomiting, flatulence, gastritis, constipation, hepatitis, a violation of liver function.
From the skin: sometimes - dry skin, erythema, subcutaneous hemorrhage, photosensitivity, increased sweating, alopecia.
Allergic reactions: sometimes - hives, skin rash, itching, angioedema.
On the part of the blood and hematopoiesis system: sometimes - anemia, thrombocytopenia, eosinophilia, purple Shenlaine-Genocha.
From the musculoskeletal system: often - convulsions, myalgia, pain in the back, chest, legs; Sometimes - arthralgia, arthritis, fibromyalgia; Rarely - rhabdomyolysis.
From the side of the central nervous system and sensory organs: often - dizziness, asthenia, headache, fatigue, insomnia; Sometimes - restlessness, sleep disturbance, drowsiness, memory disorders, peripheral neuropathy, paresthesia, hypoesthesia, tremor, ataxia, depression, syncope, ringing in the ears, visual impairment, conjunctivitis, migraine.
On the part of the respiratory system: often - nasal congestion, cough, upper respiratory tract infections, pharyngitis, dyspnoea, bronchitis, edema of the nasal mucosa.
On the part of the genitourinary system: sometimes - mandatory urges for urination, urinary tract infections, impaired renal function, decreased libido, impotence.
Laboratory indicators: often - hyperkalemia (the level of potassium in the blood plasma is more than 5.5 mmol / l); Sometimes - increased levels of urea and residual nitrogen or creatinine in the blood serum; Very rarely - a moderate increase in the activity of hepatic transaminases AST, ALT, hyperbilirubinemia.
There was no pharmacokinetic interaction of losartan with hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole and erythromycin.
Reportedly, rifampicin and fluconazole reduce the level of the active metabolite in the blood plasma. The clinical significance of these interactions is still unknown. As with other agents that inhibit angiotensin II or its effect, the combined use of losartan with potassium-sparing diuretics (eg spironolactone, triamterene, amiloride), potassium and potassium-containing preparations increases the risk of hyperkalemia.
NSAIDs, including selective inhibitors of COX-2, acetylsalicylic acid at a dose above 3 g / day, may reduce the effectiveness of angiotensin II receptor blockers. The combined use of angiotensin II receptor antagonists with NSAIDs, including selective inhibitors of COX-2, especially with reduced renal function, can lead to impaired renal function, including acute renal failure and increased potassium levels in the blood plasma. This effect is usually reversible.
With the combined use of antagonists of angiotensin II and lithium receptors, an increase in the concentration of lithium in the blood plasma is possible. Considering this, it is necessary to weigh the benefit and risk of joint use of losartan with lithium salts. In the event that it is necessary to apply the drugs together, it is necessary to regularly monitor the concentration of lithium in the blood plasma.
The combined use of losartan with diuretics has an additive effect. Strengthens (mutually) the effect of other antihypertensive drugs (diuretics, beta-blockers, sympatholytics).
Dosing and Administration
Inside, 1 time per day, regardless of food intake.
In most cases, the initial and maintenance dose is 50 mg once a day. If necessary, the dose of the drug can be increased to 100 mg / day (in 1 or 2 administration).
Against the background of taking large doses of diuretics, it is recommended to start therapy with Losarel with 25 mg (1/2 tablets 50 mg) per day in one session.
The initial dose is 12.5 mg / day, followed by a weekly increase in 2 times to 50 mg / day, depending on the tolerability of the drug.
Type 2 diabetes mellitus with proteinuria (reduced risk of hypercreatininemia and proteinuria)
The initial dose is 50 mg once a day in a single dose. During treatment, depending on blood pressure, you can increase the daily dose of the drug to 100 mg in 1 or 2 doses.
Reducing the risk of developing cardiovascular complications and mortality in patients with hypertension and left ventricular hypertrophy
The initial dose is 50 mg of the drug Losarel 1 time per day; If necessary, you can increase the dose of the drug Losarel to 100 mg / day.
Patients with impaired renal function (Cl creatinine less than 20 ml / min), liver disease in the history, dehydration, during dialysis, and patients older than 75 years are recommended a lower initial dose of the drug - 25 mg (1/2 table 50 Mg) once a day.
Symptoms: marked decrease in blood pressure and tachycardia; As a result of parasympathetic (vagal) stimulation, a bradycardia can develop.
Treatment: forced diuresis, symptomatic therapy. Hemodialysis is ineffective, because Losartan and its active metabolite are not excreted from the body by hemodialysis.
Safety and effectiveness of the drug in children are not established. Drugs that affect the renin-angiotensin-aldosterone system can increase the concentration of urea in the blood and serum creatinine in patients with bilateral renal artery stenosis or stenosis of the artery of a single kidney.
In patients with dehydration (eg receiving treatment with high doses of diuretics), at the beginning of treatment with Losarel, symptomatic arterial hypotension may occur (correction of dehydration before the administration of Losarel or starting treatment with a lower dose should be done).
Regular monitoring of the level of potassium in the blood plasma is necessary in patients taking long-term drug Losarel.
Effect on the ability to drive and work with machinery. Losartan does not affect the ability to drive or work with machinery.
Sandoz d.d., produced by Lek d.d. (Slovenia).
Conditions of supply of pharmacies
Storage conditions of the drug Losarel
At a temperature not higher than 25 ° C.
Keep out of the reach of children.
The shelf life of the drug Losarel
Do not use beyond the expiration date printed on the package.