Index of drugs

Treatment of primary hypertension in adults and children and adolescents from 6 to 18 years. Treatment of kidney disease in adult hypertensive patients with type 2 diabetes mellitus with proteinuria ≥0.5 g / day as a component of antihypertensive therapy. Treatment of chronic heart failure in adult patients when treatment with ACE inhibitors is not appropriate due to side effects, especially cough or contraindications; in patients with heart failure whose condition has been stabilized with the use of an ACE inhibitor, treatment 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 stroke risk in adult 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). Losartan selectively blocks the AT receptor₁. Both potassium losartan and its pharmacologically active metabolite (carboxylic acid) block all effects of angiotensin II, regardless of the origin or route of its synthesis. Losartan does not stimulate or block other hormone receptors or ion channels important for regulation in the circulatory system. Losartan is also not an inhibitor of kininase II (an enzyme that breaks down bradykinin), so it does not increase the effects of bradykinin-dependent effects. After oral administration, it is well absorbed from the gastrointestinal tract and undergoes a first-pass effect through the liver. About 14% of the losartan dose is converted to the active metabolite. Bioavailability is about 33%. C_max losartan in the blood occurs after about 1 hour and its active metabolite after 3-4 hours. Losartan and its metabolites are excreted in the urine (35% / 43%) and faeces (58% / 50%). T_0,5 is about 2 h for Losartan, about 6-9 h for the active metabolite.

Hypersensitivity to the components of the preparation. Severe liver dysfunction. II and III trimester of pregnancy. 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 angioneurotic edema (swelling of the face, lips, throat and / or tongue) should be closely monitored. In patients with circulating and / or sodium-depleted blood volume due to intensive diuretic therapy, dietary salt restriction, diarrhea or vomiting, symptomatic hypotension may occur, particularly after the first dose and after increasing the dose. Such deficiencies should be corrected before administration of the preparation or a lower starting dose. This also applies to children from 6 to 18 years old. Patients with impaired renal or non-diabetic function often have electrolyte imbalances that need to be compensated - potassium and blood creatinine clearance should be closely monitored, particularly in patients with heart failure and creatinine clearance 30-50 ml / min . The concomitant use of potassium-sparing diuretics, potassium supplements and potassium-containing salt substitutes is not recommended. Use with caution in adult patients with a history of liver dysfunction. Losartan is not recommended for use in children with impaired hepatic function. As a consequence of renin-angiotensin-aldosterone system inhibition, renal dysfunction with renal insufficiency has been observed (especially in patients whose renal function depends on the activity of the renin-angiotensin-aldosterone system, such as those with severe heart failure or pre-existing renal dysfunction ). There was also an increase in blood urea and creatinine in patients with bilateral renal artery stenosis or stenosis of the artery to the only kidney; these changes in renal function may resolve after discontinuation of the drug - these should be used with caution. During treatment of children with impaired renal function, renal function should be monitored regularly as it may worsen, especially in existing diseases that may affect kidney function (fever, dehydration). Due to the lack of data, the use of losartan is not recommended in children with glomerular filtration rate <30 ml / min / 1.73 m². The concomitant use of losartan and ACE inhibitors interfered with renal function, therefore concomitant use is not recommended. There are no experiences in patients after a recent kidney transplantation. Patients with primary hyperaldosteronism usually do not respond to antihypertensive drugs acting by inhibiting the activity of the renin-angiotensin system - the use of the preparation in this group of patients is not recommended. Excessive reduction of blood pressure in patients with ischemic heart disease and cerebrovascular disorders may result in myocardial infarction or stroke. In patients with heart failure and concomitant renal impairment, there is - as with other agents acting on the renin-angiotensin system - a risk of severe hypotension and (often acute) renal failure. The lack of sufficient therapeutic experience in the use of losartan in patients with heart failure and concomitant 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. Combined treatment with losartan and beta-blockers should be used with caution. Particularly cautiously use in patients with aortic or mitral stenosis or hypertrophic cardiomyopathy with narrowing of the outflow pathway. 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. Angiotensin II receptor antagonists are less effective in the treatment of hypertension in the black population. Due to lack of data, the use of losartan is not recommended in children with glomerular filtration rate <30 ml / min / 1.73 m². Due to the lactose content, the preparation should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) 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-dependent orthostatic symptoms), 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, orthostatic hypotension (including dose-related orthostatic symptoms), renal dysfunction, renal failure, hyperkalemia, increased urea and creatinine in the blood.Uncommon: headache, shortness of breath, cough, diarrhea, nausea, vomiting, urticaria, pruritus, rash, weakness, tiredness. Rare: paraesthesia, fainting, atrial fibrillation, cerebrovascular accident.Hypertension and type 2 diabetes with kidney disease. Common: central dizziness, orthostatic hypotension (including dose dependent orthostatic symptoms), asthenia, 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 aged 6 to 18 years. 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, 100 mg / day, up to a maximum of 150 mg once a day) until the usual dose is reached. maintenance (50 mg once a day) 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 drug can be taken with or without a meal, washed down with a glass of water.