Buy Losartan Vertex tablet coated 100mg N30
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Losartan Vertex pill coated 100mg N30

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Active ingredients

Losartan

Release form

Pills

Composition

Losartan potassium 100 mg; Excipients: lactose monohydrate - 115 mg, microcrystalline cellulose - 40 mg, croscarmellose sodium - 11.2 mg, povidone (low molecular weight polyvinylpyrrolidone) - 9 mg, silicon dioxide, colloidal - 2 mg, magnesium stearate - 2.8 mg., Mg. .. film coat: (hypromellose - 4.8 mg, talc - 1.6 mg, titanium dioxide - 0.826 mg, macrogol 4000 (polyethylene glycol 4000) - 0.72 mg, ferric oxide yellow (iron oxide) - 0.054 mg) or (dry mix for film coating containing hypromellose 60%, talc 20%, titanium dioxide 10.33%, macrogol 4000 (polyethylene glycol eh 4000) 9%, yellow iron oxide (iron oxide), 0.67%) - 8 mg.

Pharmacological effect

Losartan is a specific angiotensin II receptor antagonist (AT1 tin) for oral administration. Angiotensin II binds selectively to AT1 receptors found in many tissues (in vascular smooth muscle tissue, adrenal glands, nights, 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 (E 3174) both in vitro and in vivo block all the physiological effects of angiotensin II, regardless of the source or route of synthesis. Losartan binds selectively to AT1 receptors: it 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), which contributes to the degradation of bradykinin, so side effects indirectly associated with bradykinin (eg, angioedema) occur rarely.; When losartan is used, the negative effect of negative feedback on renin secretion leads to an increase plasma renin activity. Increased renin activity leads to an increase in plasma angiotensin II concentration. However, antihypertensive activity and a decrease in the concentration of aldosterone in blood plasma persist, indicating an effective blockade of angiotensin II receptors. After the abolition of losartan, plasma renin activity and the concentration of angiotensin II decreased to baseline values ​​for 3 days,observed before starting the drug.; Losartan and its active metabolite have a high affinity for angiotensin II receptors (type AT1); The concentrations of losartan and its active metabolite in plasma, as well as the antihypertensive effect of losartan increase with increasing dose of the drug.; Maximum antihypertensive effect develops 3-6 weeks after starting 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, excretion of albumin and immunoglobulin G (IgG) .; In women in the post-honeous period with arterial hypertension, who took losartan at a dose of 50 mg / day for 4 weeks, there was no effect of the therapy on the renal and systemic levels of prostaglandins; vegetative reflexes and does not have a long-lasting effect on the level of norepinephrine in the blood plasma. In patients with arterial hypertension, losartan in doses up to 150 mg per day does not cause clinically significant changes in the concentration of triglycerides, cholesterol and high density lipoprotein cholesterol. In the same doses, losartan does not affect the fasting blood glucose concentration. Losartan caused a decrease in the serum concentration of uric acid (usually less than 0.4 mg / dL), which was maintained 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.

Pharmacokinetics

Absorption; When ingested, losartan is well absorbed from the gastrointestinal tract. Systemic bioavailability of losartan is approximately 33%, food intake does not affect the bioavailability of losartan. The average maximum concentrations of losartan and its active metabolite are reached after 1 h and 3-4 h, respectively.; Distribution; Losartan and its active metabolite are associated with plasma proteins (mainly albumin) by more than 99%. The volume of distribution of losartan is 34 liters. Losartan practically does not penetrate the blood-brain barrier.; Metabolism; Losartan undergoes the effect of “primary passage” through the liver, it is metabolized with the participation of the cytochrome P450 isoenzyme CYP2C9. Approximately 14% of a dose of losartan, administered intravenously or orally, is converted to its active metabolite (EXP3174) with a carboxyl group.Biologically inactive metabolites are also formed: the two main (as a result of hydroxylirovania side butyl chain) and less significant - N-2-tetrazole-glucuronide.; Withdrawal; The plasma clearance of losartan and its active metabolite is 600 ml / min and 50 ml / min, respectively. The renal clearance of losartan and its active metabolite is approximately 74 ml / min and 26 ml / min, respectively. When losartan is taken orally, about 4% of the dose is excreted unchanged by the kidneys and, within 6% of the dose, excreted by the kidneys as an active metabolite. Losartan and its active metabolite have linear pharmacokinetics when ingested losartan in doses up to 200 mg. After ingestion, plasma concentrations of losartan and its active metabolite decrease polyexponentially with end T1 / 2 of approximately 2 and 6–9 h, respectively; elimination of losartan and its metabolites occurs in the bile and kidneys. After ingestion of losartan, labeled with 14C, about 35% of the radioactive label is detected in the urine and 58% in the feces.; Pharmacokinetics in special groups of patients; The concentrations of losartan and its active metabolite in the blood plasma of elderly male patients with arterial hypertension do not significantly differ from these indicators in younger male patients with arterial hypertension.; plasma levels of losartan were 2 times higher in women with hypertension compared with men with hypertension enziey. The concentrations of the active metabolite in men and women did not differ. This apparent pharmacokinetic difference has no clinical significance. When taking losartan orally, the Nazis with cirrhosis of the liver had an alcoholic origin of mild to moderate severity of losartan and its active metabolite in plasma were 5 and 1.7 times (respectively) higher than young healthy male volunteer volunteers.; Plasma losartan concentrations in patients with creatinine clearance above 10 ml / min did not differ from those in patients with normal renal function. In patients requiring hemodialysis, the area under the concentration-time curve (AUC) is approximately 2 times greater than in patients with normal renal function. Plasma concentrations of the active metabolite do not change in patients with impaired renal function or in patients on hemodialysis. Losartan and its active metabolite are not removed from the bloodstream by hemodialysis.

Indications

- arterial hypertension; - reducing the risk of associated cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy, manifested by a decrease in the cumulative incidence of cardiovascular mortality, the incidence of stroke and myocardial infarction; - kidney protection in patients with diabetes mellitus type 2 with proteinuria - slowing the progression of renal failure, manifested by a decrease in the frequency of hypercreatininemia, the incidence of end-stage chronic renal failure (CRF) requiring hemodialysis or kidney transplantation, mortality rates, and a decrease in proteinuria; - chronic heart failure with the ineffectiveness of treatment with ACE inhibitors.

Contraindications

- Hypersensitivity to any of the components of the drug; - pregnancy and breastfeeding period; - age up to 18 years; - refractory hyperkalemia; - lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome; - dehydration; - severe liver failure (no experience with the application); - simultaneous use with aliskiren in patients with diabetes mellitus and / or with impaired renal function (glomerular filtration rate less than 60 ml / min); With caution: liver failure (less than 9 points in Child-Pugh), hypotension, reduced circulating volume of blood (BCC), impaired water and electrolyte balance, hyperkalemia, bilateral renal artery stenosis or single renal artery stenosis, renal failure, conditions after kidney transplantation, aortic and mitral stenosis, obstructive g history of hypertrophic cardiomyopathy, angioedema, severe heart failure (NYHA functional class IV), ischemic heart disease, heart failure with life-threatening arrhythmias, cerebrovascular disease, primary aldosteronism, heart failure with concomitant severe renal failure.

Use during pregnancy and lactation

The use of Losartan in pregnancy is contraindicated.; Preparations directly affecting the renin-angiotensin-aldosterone system (RAAS), when used in the second and third trimesters of pregnancy, can cause a developmental defect or even death of a developing fetus.Therefore, when diagnosing pregnancy, Losartan should be stopped immediately. In experimental studies, it has been shown that the drug causes developmental defects and leads to death of the fetus or newborn. It is believed that the mechanism of such exposure is pharmacologically mediated effect on the RAAS. Renal perfusion of the human fetus, depending on the development of the RAAS, begins in the second trimester. The risk to the fetus increases if Lozartan is taken in the II or III trimester of pregnancy. The use of angiotensin II receptor antagonists in the II or III trimester of pregnancy has a toxic effect on the fetus (decreased renal function, development of oligohydramnios, delayed ossification of the skull) and the newborn (renal failure, arterial hypotension, hyperkalemia). If Losartan was used in the second trimester of pregnancy and later, an ultrasound of the bones of the skull is recommended and kidney function is evaluated.; It is not known whether Losartan is excreted in breast milk. When using Losartan during breastfeeding, a decision should be made either to stop breastfeeding or to discontinue treatment with the drug, taking into account its importance to the mother.

Dosage and administration

Inside, regardless of the meal.; The drug can be taken both as monotherapy and in combination with other antihypertensive drugs.; Hypertension; The standard initial and maintenance dose for most patients is 50 mg 1 time per day. The maximum antihypertepzivny 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 1 time per day.; In patients with a reduced volume of circulating blood (for example, while taking diuretics in large doses) the initial dose of the drug should be reduced to 25 mg 1 time per day (see section "Special instructions"); There is no need to select the initial dose in elderly patients and patients with renal insufficiency, including the patient s 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 old are recommended to prescribe the drug at a lower initial dose of 25 mg 1 time per day.; Reduce the risk of associated cardio -vascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy; The standard initial dose of the drug is 50 mg 1 time per 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 arterial pressure reduction (BP)) in one or two doses.; Kidney protection in patients with type 2 diabetes and proteinuria; Standard dosage 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 blood pressure reduction. Losartan can be prescribed in conjunction with other antihypertensive drugs (diuretics, slow calcium channel blockers, alpha and beta adrenoblockers, centrally acting hypotensive drugs), insulin and other hypoglycemic drugs (sulfonylurea derivatives, glycosides, and glucosidoside inhibitors;),); insufficiency; The initial dose of the drug is 12.5 mg once a day. As a rule, the dose is titrated with a weekly interval (that is, 12.5 mg 1 time per day. 25 mg 1 time per day. 50 mg 1 time per day) to the usual maintenance dose of 50 mg 1 time per day, depending on the individual portability.

Side effects

In most cases, losartan is well tolerated, side effects are mild and transient, and do not require discontinuation of the drug. Side effects observed when taking the drug are classified into categories depending on the frequency of their occurrence: very often> 1/10 (10%); often> 1/100 (1%) <1/10 (10%); sometimes> 1/1000 (0.1%), <1/100 (1%): rarely> 1/10000 (0.01%), <1/1000 (0.1%); very rarely <1/10000 (0.01%), including individual events.; Side effects occurring with a frequency of more than 1%; General disorders: asthenia, weakness, fatigue, pain in the chest, peripheral edema.; Cardio- vascular system: feeling of palpitations, tachycardia. On the part of the digestive system: abdominal pain, diarrhea, dyspepsia, nausea.; On the part of the musculoskeletal system: pain in the back, legs, muscle cramps.; From the central nervous system (CNS) : dizziness, headache, insomnia.; With one hundred rons of the respiratory system: cough, bronchitis, swelling of the nasal mucosa, pharyngitis, sinusitis, infections of the upper respiratory tract.; Side effects occurring with a frequency of less than 1%; Cardiovascular system: angina, symptomatic arterial hypotension (especially in patients intravascular dehydration, for example, patients with severe heart failure or when taking diuretics in high doses), dose-dependent orthostatic hypotension, bradycardia.arrhythmias, myocardial infarction, vasculitis. From the digestive system: anorexia, dry oral mucosa, toothache, meteorism, gastritis, constipation, hepatitis, abnormal liver function, vomiting.; From the skin: dry skin, ecchymosis, erythema ; photosensitization, increased sweating, alopecia; Allergic reactions: urticaria, pruritus, skin rash, angioedema (including laryngeal edema, vocal fold, causing obstruction of the respiratory tract, and / or swelling of the face, lips, pharynx and / or tongue) .; From the system side etvoreniya: anemia, thrombocytopenia, eosinophilia, Schonlein-Henoch purpura, the nervous system and sensory organs:. anxiety, sleep disturbance. drowsiness., memory impairment, peripheral neuropathy, paresthesia, hypostezia. tremor, ataxia, depression, syncope, tinnitus, taste disturbance, visual impairment, conjunctivitis, migraine. From the musculoskeletal system: arthralgia, arthritis, pain in the shoulder and knee, fibromyalgia.; From the urethral system: imperative urge to urinate, urinary tract infections, impaired kidney function; From the reproductive system: decreased libido, impotence; Other: exacerbation of gout, nosebleeds. From laboratory indicators:; often - hyperkalemia (potassium content is more than 5.5 mmol / l); infrequently - an increase in the concentration of urea, residual nitrogen, serum creatinine; very rarely - a moderate increase in the activity of grapsaminases (aspartate-aminopotransferase, alanine aminotransferase), hyperbilirubinemia. Attention! If any of the side effects indicated in the instructions are aggravated or you notice any other side effects that are not indicated and instructions, inform your doctor.

Overdose

Information on overdose of the drug is limited.; The most likely symptoms; A marked reduction 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 not excreted by hemodialysis.

Interaction with other drugs

May be administered with other antihypertensive drugs.; Clinically significant interaction of losartan with such drugs as hydrochlorothiazide, digoxin, warfarin, cimetidine and phenobarbital, ketoconazole and erythromycin is not observed.; Rifamycin and fluconazole reduce the level of active metabolite.The clinical significance of these interactions has not been established potassium supplements and salts containing potassium can lead to an increase in the serum potassium content.; As with the use of other agents that affect the excretion of sodium, treatment with losartan may be accompanied I decrease sodium excretion and increase the serum lithium concentration, therefore, with simultaneous treatment with lithium drugs, its serum concentration should be monitored. means. Therefore, the antihyperteptic effect of angiotensin II receptor antagonists or ACE inhibitors can be weakened while being used with NSAIDs, including with selective COX-2 inhibitors.; In some patients with impaired renal function who have been treated with NSAIDs, the simultaneous administration of apiotensin II antagonists may cause further deterioration of renal function. This effect is usually reversible. Other antihypertensive drugs may increase the severity of the antihypertensive effect of losartan. The simultaneous use of drugs (for example, tricyclic antidepressants, neuroleptics, baclofen, amifostine), which lower blood pressure as a main or side effect, may increase the risk of arterial hypotension; associated with an increased risk of arterial hypotension, syncope, hyperkalemia, and renal dysfunction (including acute renal failure) compared with monotherapy. Blood pressure, kidney function and water-electrolyte balance in patients taking losartan and other medications that affect the RAAS must be carefully monitored. Losartan is not recommended to be used simultaneously with aliskiren in patients with diabetes mellitus.Simultaneous use of Lozartan and aliskiren should be avoided in patients with renal insufficiency (glomerular filtration rate less than 60 ml / min); when used simultaneously with fluvastatin (a weak inhibitor of the isoenzyme CYP 2C9), no difference in exposure was detected. Losartan, and you are taking other medications, consult your doctor.

special instructions

Allergic reactions. In patients taking losartan, anaphylactic reactions, angioedema involving the larynx and pharynx, causing obstruction of the airways and / or swelling of the face, lips, pharynx and / or tongue, were rarely observed. Some of these patients had a history of indications of transferred angioedema when taking other medications, including ACE inhibitors. Therefore, in the appointment of the drug to patients with angioedema in the history of edema, special care should be taken. Arterial hypotension and impaired water-electrolyte balance or reduction of the BCC. In patients with reduced BCC (for example, receiving treatment with diuretics in high doses), symptomatic arterial hypotension may occur. Correction of such conditions should be carried out before the appointment of losartan or start treatment with the use of the drug in a lower dose (see the section "

Dosage and administration

"). Violation of water and electrolyte balance is characteristic of patients with renal failure with type 2 diabetes mellitus or without diabetes mellitus, therefore, when prescribing a drug for this category of patients, special care should be taken because of the risk of hyperkalemia (see the Side Effects section, indicators); During the period of treatment should regularly monitor the content of potassium in the blood, especially in elderly patients, with impaired renal function. During treatment with losartan, patients should not take potassium preparations or salt substitutes containing potassium without prior consultation with the physician. Aortic or mitral stenosis, obstructive hypertrophic cardiomyopathy. Like all drugs with a vasodilating effect, angiotensin II receptor antagonists should be administered with caution to patients with aortic or mitral stenosis or obstructive hypertrophic cardiomyopathy. Coronary heart disease and cerebrovascular disease.As with all drugs that have a vasodilating effect, angiotensin II receptor antagonists should be administered with caution to patients with coronary heart disease or cerebrovascular diseases, since an excessive reduction in blood pressure in this group of patients can lead to myocardial infarction or stroke; Chronic heart failure ( CHF). As with the use of other drugs that have an effect on the RAAS, in patients with CHF and with or without impaired renal function, there is a risk of developing severe arterial hypotension or acute renal failure.; There is insufficient experience with losartan in patients with heart failure and concomitant severe renal deficiency, in a patient with severe heart failure (functional class IV, NYHA classification), as well as in patients with heart failure and symptomatic threatening life arrhythmias. Therefore, losartan should be prescribed with caution by the Nazis in these groups. Primary hyper aldosteronism. In patients with primary heliraldosteronism, as a rule, there is no positive response to therapy with antihypertensive drugs that act by inhibiting the RAAS, therefore the use of losartan is not recommended in this group of patients. Liver dysfunction. These pharmacokinetic studies indicate that plasma concentration of losartan in patients with cirrhosis of the liver increases significantly, so patients with liver disease in history should use the drug in a lower dose (see the section "

Dosage and administration

"); Impaired function the kidneys. Due to inhibition of the RAAS, changes in renal function were observed in some predisposed patients, including the development of renal failure. These changes may occur after stopping treatment.; Some drugs that affect the RAAS may increase the concentration of urea in the blood and serum creatine in patients with bilateral renal artery stenosis or arterial stenosis of a single kidney. Changes in renal function may be reversible after therapy.During the period of treatment, it is necessary to regularly monitor the concentration of creatine serum at regular intervals. Patients of advanced age. Clinical studies did not reveal any differences in safety and efficacy of losartan in elderly patients. Influence on ability to drive vehicles and mechanisms; During treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions (dizziness is possible, especially in patients taking diuresic drugs and who are on drug therapy).

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