LOSARTAN PILLS 50MG
LOSARTAN PILLS 50MG - 30 tabs
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1 pill contains Losartan potassium 50 mg
Mechanism of action
Losartan is a specific angiotensin II receptor antagonist (subtype AT1) for oral administration. Angiotensin II selectively binds to AT1-receptors found in many tissues (in vascular smooth muscle tissue, adrenal glands, kidneys, and heart) and performs several important biological functions, including vasoconstriction and aldosterone release. Angiotensin II also stimulates the growth of smooth muscle cells.
Losartan and its pharmacologically active metabolite (Е 3174), both in vitro and in vivo, block all physiological effects of angiotensin II, regardless of the source or route of synthesis. Losartan selectively binds to AT1-receptors and does not bind or block the receptors of other hormones and ion channels, which play an important role in regulating the function of the cardiovascular system. In addition, losartan does not inhibit angiotensin-converting enzyme (ACE) - kininase II, and, accordingly, does not prevent the destruction of bradykinin, therefore side effects indirectly associated with bradykinin (eg, angioedema) occur quite rarely.
When using losartan, the lack of influence of negative feedback on renin secretion leads to an increase in plasma renin activity. Increased renin activity leads to an increase in plasma angiotensin II concentration. However, antihypertensive activity and a decrease in plasma aldosterone concentration remain, indicating an effective blockade of angiotensin receptors P. Losartan and its active metabolite have a greater affinity for angiotensin I receptors than angiotensin I receptors. The active metabolite is 10-40 times more active than losartan.
After a single intake, the hypotensive effect (systolic and diastolic blood pressure decreases) reaches a maximum after 6 hours, then gradually decreases within 24 hours. The maximum hypotensive effect develops 3-6 weeks after starting the drug.
In patients with arterial hypertension without concomitant diabetes mellitus with proteinuria (more than 2 g / day), the use of the drug significantly reduces proteinuria, the excretion of albumin and immunoglobulin G. Stabilizes the content of urea in the blood plasma. Does not affect the autonomic reflexes, and does not have a long-term effect on the concentration of norepinephrine in the blood plasma.
Indications and usage
- arterial hypertension;
- chronic heart failure (as part of combination therapy, with intolerance or failure of therapy with ACE inhibitors);
- reducing the risk of cardiovascular diseases (including stroke) and mortality in patients with arterial hypertension and left ventricular hypertrophy;
- diabetic nephropathy or hypercreatininemia and proteinuria (the ratio of urine albumin to creatinine is more than 300 mg / day) in patients with type 2 diabetes and concomitant arterial hypertension (reduced progression of diabetic nephropathy to terminal chronic renal failure).
Hypersensitivity to the drug; severe liver failure (more than 9 points on the Child-Pugh scale); age up to 18 years; hereditary intolerance to galactose, lactase deficiency or glucose-galactose malabsorption syndrome; pregnancy and lactation.
Pregnancy and Breastfeeding
The use of the drug Losartan-Richter during pregnancy is contraindicated. It is known that drugs acting directly on the renin-angiotensin-aldosterone system (RAAS), when used in the second and third trimesters of pregnancy, can cause developmental defects or even death of the developing fetus. Therefore, when diagnosing pregnancy, taking the drug Lozartan-Richter should be immediately stopped.
It is not known whether losartan is excreted in breast milk. It is not recommended to take the drug Losartan-Richter during lactation. If taking Lozartan-Richter is necessary during lactation,then breastfeeding must stop.
Dosage and administration
Lozartan-Richter drug is taken orally, regardless of the meal.
Tablets are swallowed, without chewing, with water. Frequency of admission - 1 time per day.
In hypertension, the average daily dose is 50 mg 1 time / day. To achieve a greater therapeutic effect, the dose is increased to 100 mg 1 time per day.
Chronic heart failure
The initial dose for patients with chronic heart failure is 12.5 mg 1 time per day. Typically, the dose increases with a weekly interval (that is, 12.5 mg / day, 25 mg / day and 50 mg / day) to an average maintenance dose of 50 mg 1 time per day, depending on the patient's tolerance of the drug.
No dose adjustment is required in elderly patients.
Reducing the risk of developing cardiovascular diseases (including stroke) and mortality in patients with arterial hypertension and left ventricular hypertrophy
The initial dose of the drug is 50 mg 1 time / day. In the future, hydrochlorothiazide may be added in low doses or the dose of Lozartan-Teva may be increased to 100 mg in one or two doses, taking into account the reduction in blood pressure (BP).
Patients with concomitanttype 2 diabetes with proteinuria: Lozartan-Richter is prescribed at the initial dose of 50 mg 1 time per day with a further increase in the dose to 100 mg / day (taking into account the degree of blood pressure reduction) in one or two doses.
In patients with reduced BCC (for example, when taking diuretics in high doses), the recommended initial dose of Lozartan-Teva is 25 mg 1 time / day.
Patients with hepatic insufficiency (less than 9 points on the Child-Pugh scale), during the hemodialysis procedure, as well as patients over 75 years old A lower initial dose of the drug is recommended - 25 mg 1 time per day.
The safety and efficacy of the drug in children under 18 have not been established. There is not enough experience in the use of the drug in patients with severe liver failure, so the drug is not recommended in this category of patients.
From the nervous system and sensory organs: 1% or more - dizziness, asthenia, fatigue, headache, insomnia; less than 1% - anxiety, sleep disturbances, drowsiness, memory disorders, peripheral neuropathies, paresthesias, hypoesthesia, migraines, tremors, ataxia, depression, loss of consciousness, tinnitus, taste disturbances, vision changes, conjunctivitis.
On the part of the respiratory system: 1% or more - nasal congestion, cough *, infections of the upper respiratory tract (increased body temperature, sore throat, sinusopathy *, sinusitis, pharyngitis); less than 1% dyspnea, bronchitis, rhinitis.
On the part of the digestive system: 1% or more - nausea, diarrhea *, dyspepsia *, abdominal pain; less than 1% - loss of appetite, dry mouth, toothache, vomiting, flatulence, gastritis, constipation.
On the part of the musculoskeletal system: 1% or more - seizures, myalgia *, pain in the back, chest, legs; less than 1% - arthralgia, pain in the shoulder, knee, arthritis, fibromyalgia.
On the part of the cardiovascular system: less than 1% - orthostatic hypotension (dose-dependent), palpitations, tachy- or bradycardia, arrhythmias, angina pectoris, anemia.
On the part of the urogenital system: less than 1% - imperative urge to urinate, urinary tract infections, renal dysfunction, decreased libido, reduced potency.
On the part of the skin: less than 1% - dryness, skin hyperemia, photosensitivity, increased sweating, alopecia.
Allergic reactions: less than 1% - urticaria, rash, itching, angioedema, including face, lips, pharynx and / or tongue.
Other: more than 1% - hyperkalemia; less than 1% - fever, gout, increased activity of liver transaminases and hyperbilirubinemia (* - side effects are marked, the incidence of which is comparable to placebo. The relationship of side effects occurring with a frequency of less than 1% of cases with losartan is not proven).
Prior to the use of the drug Lozartan-Richter, it is necessary to correct the BCC or begin treatment with the use of the drug in a lower dose.
Drugs that affect the RAAS can increase the concentration of urea in the blood and the concentration of serum creatinine in patients with bilateral renal artery stenosis or arterial stenosis of a single kidney.
During the period of treatment should regularly monitor the content of potassium in the blood, especially in elderly patients, in violation of renal function.
It can be used simultaneously with other antihypertensives. Mutually enhances the effect of beta-blockers and sympatholytic. The combined use of losartan with diuretics causes an additive effect. Pharmacokinetic interactions of losartan with hydrochlorothiazide, Digoxin , Warfarin , cimetidine, phenobarbital, Ketoconazole and Erythromycin were not observed. Rifampicin and Fluconazole are reported to decrease the plasma concentration of the active metabolite. The clinical significance of these interactions is not yet known.
As with the use of other agents inhibiting angiotensin II or its action, the combined use of losartan with potassium-saving diuretics (for example, spironolactone, triamterene, amiloride), potassium preparations, salts containing potassium, increases the risk of hyperkalemia.
Non-steroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase-2 inhibitors (COX-2), can reduce the effect of diuretics and other antihypertensive drugs.
The combined use of angiotensin II receptor antagonists and lithium may increase the plasma concentration of lithium. Given this, it is necessary to weigh the benefits and the risk of losartan combined with lithium salts. If necessary, the joint use of drugs, it is necessary to regularly monitor the concentration of lithium in the blood plasma.
Symptoms: pronounced decrease in blood pressure and tachycardia; bradycardia may occur due to parasympathetic stimulation.
Treatment: forced diuresis, symptomatic therapy; hemodialysis is not effective.
Store at a temperature not exceeding 25 ° C. Keep out of reach of children.