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, being part of antihypertensive therapy. Treatment of chronic heart failure (in patients aged 60 years and above), if treatment with ACE inhibitors is not indicated because of incompatibilities, especially cough or contraindications; treatment with Losartan should not be changed in patients with heart failure who have stabilized the clinical condition when ACE inhibitors are given; ejection fraction of the left ventricle should be ≤40% and the clinical condition of patients should be stabilized during treatment of chronic heart failure. Reduction of risk of stroke in patients with hypertension and left ventricular hypertrophy documented in electrocardiogram.

1 tabl powl. contains 50 mg of potassium losartan. The tablets contain 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 and 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 urine (35%) and faeces (58%). 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).

Patients with a history of angioneurotic edema (swelling of the face, lips, throat and / or tongue) should be closely monitored. In patients with reduced intravascular volume and / or reduced sodium levels due to intense 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 (6-18 years). Patients with renal dysfunction with or without diabetes mellitus often have electrolyte imbalance - regular monitoring of potassium and blood creatinine clearance, especially in patients with heart failure and blood creatinine 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; Renal function changes may resolve after discontinuation - these should be used with caution.During treatment of children with impaired renal function, renal function should be monitored regularly as it may worsen, particularly when other conditions are present, such as fever or 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 cumulative administration is not recommended. Lack of experience in patients after 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 a risk of severe hypotension and (often acute) renal failure. There is insufficient experience in the clinical 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. Angiotensin II receptor antagonists are less effective in the treatment of hypertension in the black population. 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. The use of losartan in children below 6 years is not recommended. 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) - in the case when exposure to the drug occurred from the second trimester of pregnancy, ultrasound examination of fetal skull and kidneys is recommended; newborns whose mothers took the drug during pregnancy should be closely monitored for hypotension. The use of losartan is not recommended during breastfeeding, especially when breastfeeding a newborn or a premature baby.

Hypertension. Common: dizziness of central and labyrinthic origin, hyperkalemia. Uncommon: drowsiness, headache, sleep disturbances, palpitations, angina pectoris, orthostatic hypotension, 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, dose-dependent orthostatic symptoms, renal failure, renal dysfunction, increased urea and creatinine in the blood, hyperkalemia.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, dose-related orthostatic symptoms, weakness, fatigue, hypoglycaemia, hyperkalemia. In addition, post-marketing experience has been reported: rarely - hypersensitivity reactions, anaphylactic reactions, angioneurotic edema (including laryngeal and glottal edema, face, lips, throat and / or tongue; in some of these patients, angioneurotic edema occurred in the past due to using other drugs, including ACE inhibitors), vasculitis (including Schonlein-Henoch purpura), hepatitis; frequency unknown - anemia, thrombocytopenia, depression, migraine, dysgeusia, tinnitus, cough, diarrhea, pancreatitis, liver dysfunction, urticaria, pruritus, rash, allergic reaction to light, muscle pain, joint pain, rhabdomyolysis, erectile dysfunction / impotence, malaise, hyponatremia. In patients at risk, renal function disorders have been reported, including renal failure, resulting from the inhibition of the angiotensin-renin-aldosterone system; such changes in renal function may be reversible after discontinuation of therapy. The profile of side effects in children appears to be similar to that seen in adult patients.

Orally.Hypertension. Adults: The usual starting and maintenance dose is 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 in combination with other antihypertensive agents, mainly with diuretics (eg hydrochlorothiazide). Children: no clinical experience regarding the efficacy and safety of losartan in the treatment of hypertension in children and adolescents from 6 to 16 years. Limited pharmacokinetic data are available for hypertensive children over 1 month. For patients who can swallow tablets, o. 20-50 kg the recommended dose is 25 mg once a day. In exceptional cases, the dose may be increased to a maximum of 50 mg once a day. In patients with bw > 50 kg the usual dose is 50 mg once a day. In exceptional cases, the dose may be increased up to a maximum of 100 mg once a day. No studies on the use in children of doses> 1.4 mg / kg have been performed. (or more than 100 mg) daily.Patients with hypertension and type II diabetes mellitus with proteinuria ≥0.5 g / day. The usual starting dose is 50 mg once a day. After a month from the start of treatment, depending on the value of your blood pressure, the dose may be increased to 100 mg once a day. The preparation can be used simultaneously with other antihypertensive drugs (eg diuretics, Calcium antagonists, α- or β-blockers and centrally acting drugs), as well as with insulin and other commonly used hypoglycemic agents (eg, sulphonylureas, glitazones and glucosidase inhibitors) ).Heart failure. The usual starting dose is 12.5 mg once a day. The dose should be increased gradually at weekly intervals (ie 12.5 mg / day, 25 mg / day, 50 mg / day) until the usual maintenance dose of 50 mg is achieved once daily, depending on the patient's condition.Reduction of risk of stroke in patients with hypertension and left ventricular hypertrophy confirmed in ECG. The usual starting dose is 50 mg once a day. Depending on changes in blood pressure, you should add hydrochlorothiazide low dose and / or increase the dose of losartan to 100 mg once a day.Special groups of patients. In patients with a reduced volume of intravascular (eg high-dose diuretic treatment), a starting dose of 25 mg once a day should be considered. No adjustment of the initial dose is required in patients with renal impairment or hemodialysis. A lower dose should be considered in patients with a history of liver dysfunction. In elderly patients, dosage adjustment is not usually necessary, however, in patients> 75 years, consideration should be given to starting treatment with a 25 mg dose.The tablets can be taken with or without a meal, with a glass of water.