Index of drugs

Treatment of primary hypertension. Treatment of kidney disease in patients with hypertension and type 2 diabetes mellitus with proteinuria ≥ 0.5 g / day as a component of antihypertensive therapy. Treatment of chronic heart failure (in patients ≥ 60 years of age) when treatment with ACE inhibitors does not seem adequate due to adverse reactions or contraindications to use; in patients with heart failure whose condition has been stabilized with an ACE inhibitor, therapy should not be changed to losartan; ejection fraction of the left ventricle in patients should be ≤ 40% and their condition should be stabilized during treatment of chronic heart failure. Reduction of the risk of stroke in patients with hypertension and left ventricular hypertrophy confirmed by ECG.

1 tabl powl. contains 50 mg of Losartan potassium (and lactose).

Angiotensin II receptor antagonist (AT type₁). Selectively binds to the AT receptor₁ blocking the effects of angiotensin II. It has no agonist activity towards the AT receptor₁it does not bind or block other hormone receptors or ion channels important for regulation in the circulatory system. It is not an ACE inhibitor (kinase II), so it does not increase the effects of bradykinin-dependent effects. Losartan is well absorbed from the gastrointestinal tract and undergoes a first-pass effect, resulting in the active metabolite - carboxylic acid and other inactive metabolites. The bioavailability of losartan is approximately 33%. The mean maximum concentrations of losartan and its active metabolite occur respectively after 1 hour and 3-4 hours. Losartan and its active metabolite are approximately 99% bound to plasma proteins. About 14% of the losartan dose is converted to the active metabolite. Losartan and its metabolites are excreted in the bile and in the urine. T_0,5 is about 2 h for losartan and 6-9 h for the active metabolite.

Hypersensitivity to the active substance or to any of the excipients. Severe liver dysfunction. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (glomerular filtration rate, GFR <60 ml / min / 1.73 m²). II and III trimester of pregnancy.

Patients with a history of angioedema should be closely monitored. Symptomatic hypotension, especially after the first dose and after increasing the dose, may occur in patients with circulating and / or sodium-depleted blood volume due to intensive diuretic therapy, reduced salt intake, diarrhea or vomiting - these deficiencies should be corrected before administration of the preparation or use a lower starting dose; this also applies to children. In patients with impaired renal function, with or without diabetes mellitus, electrolyte imbalance often needs to be compensated. During treatment with Losartan, the concentration of potassium in the blood and the creatinine clearance should be monitored; particular attention should be paid to patients with heart failure and creatinine clearance 30-50 ml / min. Due to the risk of hyperkalemia, concomitant use of losartan and potassium-sparing diuretics, potassium supplements and potassium-containing salt substitutes is not recommended. A decrease in the dose of losartan should be considered in patients with a history of liver dysfunction. Losartan is not recommended in children with impaired liver function. As a consequence of the inhibition of the renin-angiotensin-aldosterone system (RAA), renal dysfunction has been observed, including renal insufficiency (especially in patients whose renal function depends on RAA activity, such as patients with severe heart failure or previous renal dysfunction) ). Increases in urea and creatinine in the blood have been observed in patients with bilateral renal artery stenosis or stenosis of the artery to the sole active kidney; these changes usually disappear after treatment - losartan should be used with caution in these patients. Losartan is not recommended for use in children whose glomerular filtration rate is <30 ml / min / 1.73 m². During treatment with losartan, renal function should be monitored regularly, especially when losartan is given in existing conditions (fever, dehydration) that may affect kidney function.Co-administration of losartan and ACE inhibitors has been shown to interfere with renal function, therefore it is not recommended to use them at the same time. There is no experience with the use of losartan in patients after recent kidney transplantation. It should not be used in patients with primary hyperaldosteronism, as they usually do not respond to the administration of antihypertensive drugs acting by inhibiting the activity of the RAA system. Because of the risk of myocardial infarction and stroke, use caution in patients with ischemic heart disease and cerebrovascular disorders. In patients with heart failure, with or without renal impairment, there is a risk of severe hypotension and (often acute) renal failure. There is insufficient therapeutic experience in the use of losartan in patients with heart failure and severe renal impairment, in patients with severe heart failure (NYHA stage IV), as well as in patients with heart failure and symptomatic, life-threatening cardiac arrhythmias - losartan should be use with caution in these patient groups. The combination of losartan and β-blocker should be used with caution. Special caution should be exercised in patients with aortic or mitral stenosis or hypertrophic cardiomyopathy with narrowing of the outflow route. Losartan and other angiotensin antagonists are definitely less effective in reducing blood pressure in black patients than non-black patients. The concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren increases the risk of hypotension, hyperkalaemia and renal dysfunction (including acute renal failure) - therefore, dual blocking of the RAA system is not recommended by concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren. If the use of a dual RAA blockade is absolutely necessary, it should only be carried out under the supervision of a specialist, and the vital parameters of the patient, such as kidney function, electrolyte concentration and blood pressure should be closely monitored. In patients with diabetic nephropathy, ACE inhibitors and angiotensin II receptor antagonists should not be used concurrently. Losartan is not recommended for use in children under 6 years of age because limited data are available for use in this patient group. Due to the lactose content, the preparation should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

The use of losartan in the first trimester of pregnancy is not recommended (there is a risk of teratogenicity). Use in the second and third trimester of pregnancy is contraindicated. Losartan used in the second and third trimester of pregnancy is toxic to fetal development (deterioration of renal function, oligohydramnios, delayed ossification of the skull) and newborn (renal failure, hypotension, hyperkalemia) - when exposure to the drug occurred from the second trimester of pregnancy, it is recommended ultrasound examination of fetal skull and kidneys; newborns whose mothers took the drug during pregnancy should be closely monitored for hypotension. The use of losartan during breastfeeding is not recommended. You should use a different treatment with an established safety profile during breastfeeding, especially when feeding a newborn or premature baby.

Hypertension. Common: dizziness of central and labyrinthic origin, hyperkalemia. Uncommon: drowsiness, headache, sleep disturbances, palpitations, angina pectoris, orthostatic hypotension (including dose-related orthostatic symptoms, especially in patients with reduced circulating blood volume, e.g. in patients with severe heart failure or treated with high doses of medicines diuretic), rash, abdominal pain, constipation, weakness, fatigue, edema. Rare: increased ALT activity.Hypertension and hypertrophy of the left ventricle. Common: dizziness of central and labyrinthic origin, weakness, fatigue.Chronic heart failure. Common: anemia, dizziness, impaired renal function, renal failure, increased urea and creatinine in the blood, hyperkalemia.Uncommon: headache, orthostatic hypotension (including dose-related orthostatic symptoms, especially in patients with reduced circulating blood volume, e.g. in patients with severe heart failure or treated with high diuretics), shortness of breath, cough, diarrhea, nausea, vomiting, urticaria, pruritus, rash, weakness, fatigue. Rare: paraesthesia, fainting, atrial fibrillation, cerebrovascular accident.Hypertension and type 2 diabetes with kidney disease. Common: central dizziness, orthostatic hypotension (including dose-related orthostatic symptoms, especially in patients with reduced circulating blood volume, e.g. in patients with severe heart failure or treated with high diuretics), weakness, fatigue, hypoglycaemia, hyperkalemia . The following side effects have been reported in post-marketing experience: rare: hypersensitivity reactions, anaphylactic reactions, angioneurotic edema (including laryngeal, glottis, face, lip, throat, and / or laryngeal narrowing of the airways; in some of these patients, angioneurotic edema occurred in the past in connection with the use of other drugs, including ACE inhibitors), vasculitis (including Schoenlein-Henoch purpura), hepatitis; frequency unknown: anemia, thrombocytopenia, depression, migraine, taste disorders, tinnitus, cough, diarrhea, pancreatitis, liver dysfunction, urticaria, pruritus, rash, photosensitivity, muscle pain, arthralgia, rhabdomyolysis, erectile dysfunction / impotence , bad mood, hyponatremia. The following additional side effects were more common in patients receiving losartan than placebo: back pain, urinary tract infections, and flu-like symptoms. As a result of inhibition of the renin-angiotensin-aldosterone system, renal dysfunction has been observed, including renal failure in at-risk patients; these changes in kidney function may resolve after discontinuation of treatment. The profile of side effects in children appears to be similar to that seen in adult patients.

Orally.Hypertension: AdultsThe recommended initial and maintenance dose is usually 50 mg once a day. The maximum antihypertensive effect is obtained within 3-6 weeks from the start of treatment. In some patients it may be beneficial to increase the dose to 100 mg once a day (in the morning). The preparation can be used at the same time as other antihypertensive agents, especially diuretics (eg hydrochlorothiazide).Children≥6 years and about > 20 kg to <50 kg, which can swallow tablets: 25 mg once a day (in exceptional cases, the dose may be increased to 50 mg once a day); children about the month of > 50 kg: 50 mg once a day (in exceptional cases the dose may be increased to 100 mg once a day). There are no studies on the use of doses> 1.4 mg / kg. (or> 100 mg) per day of children. There are limited data on the efficacy and safety of losartan in the treatment of hypertension in children and adolescents from 6 to 16 years of age. The drug is not recommended for use in children under 6 years of age in children whose glomerular filtration rate is <30 ml / min / 1.73 m³ and in children with liver disorders.Hypertension and type 2 diabetes mellitus with proteinuria ≥0.5 g / dayThe usual starting dose is 50 mg once a day. The dose can be increased to 100 mg once a day depending on the value of your blood pressure, after the first month after starting treatment. It can be used at the same time as other antihypertensive medicines (eg diuretics, Calcium antagonists, α- or ß-blockers, central medicines), insulin and oral antidiabetes medicines (eg sulphonylureas, glitazones, glucosidase inhibitors).Heart failureThe usual starting dose is 12.5 mg once a day. The dose should generally be increased gradually every week (ie 12.5 mg / day, 25 mg / day, 50 mg / day) until the usual maintenance dose (50 mg once daily) is reached, if it is tolerated by the patient .Reduction of the risk of stroke in patients with hypertension and left ventricular hypertrophy confirmed by ECGThe usual starting dose is 50 mg once a day.Depending on changes in blood pressure, low-dose hydrochlorothiazide may be used and / or the dose of losartan may be increased to 100 mg once a day.Special groups of patients. For patients with reduced circulating blood volume (eg, treated with high diuretic doses), a starting dose of 25 mg once a day should be considered. Adjustment of the initial dose is not necessary in patients with renal impairment, hemodialysis, and the elderly (although patients> 75 years of age, 25 mg should be considered). A lower dose should be considered in patients with hepatic impairment; do not use the preparation in patients with severe hepatic impairment.Way of giving. The tablet can be divided. The drug can be taken with or without a meal, washed down with a glass of water.