Lorista HD coated pills 100mg + 25mg N60
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Active ingredients
Losartan + Hydrochlorothiazide
Release form
Pills
Composition
Potassium losartan 100 mg hydrochlorothiazide 25 mg adjuvants: pregelatinized starch - 69.84 mg, microcrystalline cellulose - 175.4 mg, lactose monohydrate - 126.26 mg, magnesium stearate - 3.5 mg. (e104) - 0.11 mg, titanium dioxide (e171) - 2.89 mg, talc - 1 mg.
Pharmacological effect
Combined antihypertensive drug. Losartan is a selective antagonist of angiotensin II receptor type AT1 of non-protein nature. In vivo and in vitro losartan and its biologically active carboxylic metabolite (EXP-3174) block all physiologically significant effects of angiotensin II on AT1 receptors regardless of the way it is synthesized, regardless of its synthesis pathway leads to an increase in plasma renin activity, reduces the concentration of aldosterone in the blood plasma. Losartan indirectly causes activation of the AT2 receptor by increasing the level of angiotensin II. Losartan does not inhibit the activity of kininase II, an enzyme that is involved in the metabolism of bradykinin. It reduces PRSP, pressure in the pulmonary circulation; reduces afterload, has a diuretic effect. Prevents the development of myocardial hypertrophy, increases exercise tolerance in patients with chronic heart failure. Taking losartan 1 time / day leads to a statistically significant decrease in systolic and diastolic blood pressure. During the day, losartan evenly controls blood pressure, with the antihypertensive effect consistent with the natural circadian rhythm. The decrease in blood pressure at the end of the dose of the drug was approximately 70-80% of the effect at the peak of the drug action, 5-6 hours after administration. Cancellation syndrome is not observed; also, losartan does not have a clinically significant effect on heart rate. Losartan is effective in men and women, as well as in elderly (≥65 years) and younger patients (≤65 years). Hydrochlorothiazide is a thiazide diuretic, the diuretic effect of which is associated with impaired reabsorption of sodium ions , chlorine, potassium, magnesium, water in the distal nephron; delays the excretion of calcium ions, uric acid. It has antihypertensive properties; hypotensive effect develops due to the expansion of arterioles.Virtually no effect on normal blood pressure. The diuretic effect occurs after 1-2 hours, reaches a maximum after 4 hours and lasts 6-12 hours. The antihypertensive effect occurs after 3-4 days, but it may take 3-4 weeks to achieve the optimal therapeutic effect.
Pharmacokinetics
The pharmacokinetics of losartan and hydrochlorothiazide with simultaneous use does not differ from that with their separate use. Losartan AbsorptionGoodly absorbed from the gastrointestinal tract. Taking the drug with food does not have a clinically significant effect on its serum concentrations. Cmax of losartan in the blood plasma is achieved 1 hour after ingestion. Bioavailability is about 33%. Distribution Over 99% of losartan and EXP-3174 binds to plasma proteins, primarily albumin. Vd losartan is equal to 34 liters. Practically does not penetrate through the BBB. Metabolism Exposure to significant metabolism during the first passage through the liver, forming the active metabolite EXP-3174 (14%) and a number of inactive metabolites, including 2 major metabolites, formed by hydroxylation of the butyl group of the chain and a less significant metabolite, N-2- tetrazole glucuronide. Cmax of EXP-3174 is reached 3-4 hours after taking the drug inside. Injection The plasma clearance of losartan and EXP-3174 is approximately 10 ml / s (600 ml / min) and 0.83 ml / s (50 ml / min), respectively. Renal clearance of losartan and EXP-3174 is about 1.23 ml / s (74 ml / min) and 0.43 ml / s (26 ml / min), respectively. T1 / 2 of losartan and EXP-3174 are 2 h and 6-9 h, respectively. About 58% of the drug is excreted in the bile, 35% in the urine. Hydrochlorothiazide Absorption and distribution After oral administration, the absorption of hydrochlorothiazide is 60-80%. Cmax in the blood is achieved in 1.5-5 hours. Plasma protein binding - 64% Metabolism and excretionHydrochlorothiazide is not metabolized and is rapidly excreted by the kidneys. T1 / 2 is 5-15 hours.
Indications
- arterial hypertension (to patients for whom combination therapy is indicated); - reduction of the risk of cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy.
Contraindications
- anuria; - pronounced renal dysfunction (CC <30 ml / min); - hyperkalemia; - dehydration (including during the administration of diuretics in high doses); - pronounced hepatic dysfunction; - refractory hypokalemia; - arterial hypotension - deficiency of lactase; - galactosemia or glucose / malabsorption syndrome; - pregnancy; - lactation period; - age up to 18 years (efficacy and safetynot found single kidney, diabetes mellitus, hypercalcemia, hyperuricemia, and / or gout, with a severe allergic history (some patients have angioedema developed earlier when taking other drugs, including ACE inhibitors) and bronchial asthma, systemic blood diseases (including those with SLE), simultaneously with NSAIDs (including COX-2 inhibitors).
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
Data on the use of losartan during pregnancy is not. Renal perfusion of the fetus, which depends on the development of the renin-angiotensin system, begins to function in the third trimester of pregnancy. The risk to the fetus increases when taking losartan in the II and III trimesters, because taking drugs directly acting on the renin-angiotensin system during the II and III trimesters of pregnancy can lead to fetal death. It is not recommended to prescribe diuretics during pregnancy due to the risk of jaundice in the fetus and newborn, thrombocytopenia in the mother. Diuretic therapy does not prevent the development of toxemia of pregnancy. When establishing pregnancy, Lorista HD therapy should be stopped immediately. If you need to use the drug during lactation, breastfeeding should be stopped.
Dosage and administration
The drug is taken orally, regardless of the meal.Loristu ND can be combined with other antihypertensive agents. In case of arterial hypertension, the initial and maintenance dose is 1 tab. (100/25 mg) 1 time / day. As a rule, the drug is prescribed in the absence of an adequate therapeutic effect Loristy N (50 / 12.5 mg). The maximum antihypertensive effect is achieved within 3 weeks of therapy. The maximum daily dose - 1 tab. Lorists ND.If reduced BCC (for example, against the background of receiving diuretics in high doses), the recommended initial dose of losartan in patients with hypovolemia is 25 mg 1 time / day. In this regard, Lorista HD therapy should be started after discontinuation of diuretics and correction of hypovolemia. Elderly patients and patients with moderate renal insufficiency (CC 30-50 ml / min), including those on dialysis, do not require correction of the initial dose of the drug. To reduce the risk of cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy, the standard initial dose of losartan is 50 mg 1 time / day. Patients who failed to achieve the target level of blood pressure while receiving losartan 50 mg / day require therapy by combining losartan with low doses of hydrochlorothiazide (12.5 mg), and, if necessary, increase the dose of losartan to 100 mg in combination with hydrochlorothiazide dose of 12.5 mg / day, in the future - to increase the dose of hydrochlorothiazide, prescribing Lorista HD 1 tablet / day.
Side effects
From the side of the central nervous system: often - headache, systemic and non-systemic dizziness, insomnia, fatigue; sometimes - migraine. From the cardiovascular system: often - orthostatic hypotension (dose-dependent), palpitations, tachycardia; rarely - vasculitis. Respiratory system: often - cough, infections of the upper respiratory tract, pharyngitis, swelling of the nasal mucosa. On the part of the digestive system: often - diarrhea, dyspepsia, nausea, vomiting, abdominal pain; rarely - hepatitis, abnormal liver function; very rarely - increased activity of liver enzymes and bilirubin. For the musculoskeletal system: often - myalgia, back pain; sometimes - arthralgia. From the hemopoietic system: infrequently - anemia, Schönlein-Genoh purpura. From laboratory parameters: often - hyperkalemia, hemoglobin and hematocrit increase (clinically insignificant); sometimes - a moderate increase in the level of urea and serum creatinine. Allergic reactions: sometimes - urticaria,pruritus; rarely - anaphylactic reactions, angioedema (including swelling of the larynx and tongue, causing obstruction of the respiratory tract and / or swelling of the face, lips, pharynx). Other: often - asthenia, weakness, peripheral edema, chest pain.
Overdose
Lozartan: symptoms of abdominal pain With simultaneous intake of cardiac glycosides, hypokalemia may aggravate the course of arrhythmias. Treatment: symptomatic therapy
Interaction with other drugs
Lozartan In clinical studies triamterene, amiloride), potassium-containing additives or potassium salts can lead to hyperkalemia. NSA, incl. selective COX-2 inhibitors may decrease the effectiveness of diuretics and other antihypertensive drugs, including losartan. In patients with impaired renal function who received NSAID therapy (including COX-2 inhibitors), therapy with angiotensin II receptor antagonists can lead to a further deterioration in renal function, including acute renal failure, which is usually reversible. The hypotensive effect of losartan, like other antihypertensive drugs, can be reduced by taking indomethacin. Hydrochlorothiazide When used simultaneously with ethanol, barbiturates and narcotic drugs may potentiate the risk of orthostatic hypotension. If used concomitantly with hypoglycemic agents (for ingestion and insulin), dosage adjustment of hypoglycemic agents may be necessary. When used in combination with other antihypertensive drugs, an additive effect is noted. violate the absorption of hydrochlorothiazide. When used simultaneously with GCS, ACTH there is a marked decrease in electrolyte levels, in h asthenia,hypokalemia. Hydrochlorothiazide reduces the severity of the response to the use of pressor amines (eg, epinephrine, norepinephrine). Hydrochlorothiazide enhances the effect of muscle relaxants of a non-depolarizing type of action (eg, tubocurarine). NSAIDs (including COX-2 inhibitors) can reduce the diuretic, natriuretic and hypotensive effects of diuretics. Due to the effect on calcium metabolism, thiazide intake diuretics may distort the results of the research function of the parathyroid glands.
special instructions
It can be prescribed together with other antihypertensive drugs. There is no need for a special selection of the initial dose in elderly patients. The drug can increase the concentration of urea and creatinine in the blood plasma of patients with bilateral renal artery stenosis or anemia of the kidney artery. glucose tolerance, reduce urinary calcium excretion and cause a transient, insignificant increase in plasma calcium concentration, increase concentration cholesterol and TG, to provoke the occurrence of hyperuricemia and / or gout. Lorista HD contains lactose, so the drug is not prescribed to patients with lactase deficiency, galactosemia or malabsorption syndrome glucose / galactose. NDs can perform actions that require increased attention (for example, driving a car or hazardous technical equipment). In some individuals, at the beginning of therapy, the drug can cause arterial hypotension and dizziness and, thus, indirectly affect their psychophysical condition. For safety reasons, before starting an activity requiring increased attention, patients should first evaluate their response to treatment.