All about lorist tablets n. What is Lorista medicine for and how to take it

24.10.2018

Lorista is a drug used in the treatment arterial hypertension and heart failure. The active ingredient is losartan.

It increases the physical endurance of a person when doing hard work, prevents hypertrophy (thickening, enlargement) of the myocardium and heart.

Hypertrophy of the heart muscle or left ventricle is a dangerous disease that often affects even young people (up to 40 years old) and threatens sudden lethal outcome. There are medical assumptions that the disease is hereditary or it is caused by a mutation in the genes of myocardial cells.

With the development of this pathology, various symptoms begin to appear: general weakness, pain in the heart, arrhythmia, angina pectoris, increased blood pressure for unknown reasons.

To reduce the risk of developing cardiac hypertrophy, the risk of stroke in arterial hypertension, to protect the kidneys of diabetic patients, Lorista is prescribed. With cardiac chronic insufficiency this medicine is used together with diuretics, glycosides according to a strictly developed scheme.

The use of the drug involves a mandatory consultation with a doctor, the selection of a dose and a schedule for a particular patient. With hypotension ( low rates AD), hyperkalemia, dehydration or high sensitivity to the active ingredients of the drug Lorista is not prescribed.

Release form and composition

The main active ingredients in the preparation are: losartan and hydrochlorothiazide . Auxiliary components: cellactose, starch, magnesium stearate, silicon dioxide.

Losartan potassium blocks receptors angiotensin 2 in the vessels, heart, kidneys, which reduces the narrowing of the lumen of the vessels. This reduces the overall resistance of blood vessels - as a result, blood pressure.

Hydrochlorothiazide gives a diuretic effect, affecting the 2nd phase of the process of urination, its hypotensive effect is also explained by the expansion of arterioles.

Tablets are oval, biconvex, coated with a white or yellowish shell with a risk on one side. Dosage 12.5; 25; 50 or 100 mg. Shelf life - 3-5 years (indicated on the package). Store at a temperature not exceeding 30 about S.

pharmachologic effect

The drug is selective blocker angiotensin 2 receptors (type AT1) of a non-protein nature, activates AT2 receptors, reduces the amount of aldosterone, increases renin activity in blood plasma.

Main tasks: reduction of blood pressure in the small circle and OPSS, reduces the load and gives a diuretic (diuretic) effect. The endurance of physical activity of patients with chronic heart failure increases, the risk of developing hypertrophy of the heart muscle (myocardium) decreases.

The dose of the drug is 50 mg / day, sometimes the dose is increased to 100 mg / day. If the patient is also taking diuretics, then the dose of Lorista is reduced to 25 mg / day.

Lorista is rapidly absorbed in the housing and communal services, the maximum effect occurs within an hour. Excreted with bile (58%) and urine (35%).

Taking a lorist pressure pill gives a stable decrease in pressure (systolic and diastolic), while not having a noticeable effect on heart rate (heart rate). Effective for patients of both sexes, for young patients and those over 65 years of age.

Indications for use

  • arterial hypertension of the 1st-2nd degree;
  • reduced risk of stroke in patients with high pressure and having left ventricular hypertrophy;
  • in the combined treatment of heart failure (with intolerance to ACE inhibitors);
  • protecting the kidneys of patients diabetes according to the 2nd type, decrease in proteinuria, decrease in the development of kidney damage, to prevent the need for dialysis.

Dosage and how to take

The drug is taken orally with water, preferably at the same time (it does not depend on food intake). Well absorbed in the gastrointestinal tract, absorbed about 33%, an hour after ingestion begins to act, after 3-4 hours - the maximum concentration in the blood plasma. Excreted with bile - 58%, with urine - 35%.

At daily intake during the day the effect of pressure reduction lasts, diuretic - 12 hours. The daily dose is 50 mg, to achieve the maximum effect, take 3-6 weeks. The attending physician may, if necessary, increase the dose (up to 100 mg per day).

When taking large doses of diuretics, start taking lorista with smaller doses, the initial dose is 25 mg / day. Elderly patients, with impaired renal function, patients on hemodialysis do not require a reduction in the initial dose. In smaller doses, it is also prescribed for violations of the liver.

Typically, lorista is started at a dose of 12.5 mg/day. during the 1st week, 2nd week - 25 mg / day, 3rd and 4th week - 50 mg / day. It is taken in combination with cardiac glycosides and diuretics.

There are also combined preparations with active substances: losartan and hydrochlorothiazide:

  • Lorista N (50 mg losartan, 12.5 mg hydrochlorothiazide);
  • Lorista H 100 (100 mg losartan, 12.5 mg hydrochlorothiazide);
  • Lorista ND (100 mg losartan, 25 mg hydrochlorothiazide).

Sold in packs of 30, 60, 90 tablets.

Treatment with these drugs involves not exceeding the maximum dose - 1 tablet per day (100/25 mg).

Side effects

When taken, side effects of the drug may occur. in various systems of the human body.

Nervous system:

  • headache, migraine;
  • dizziness;
  • asthenia exhaustion nervous system(impotence, chronic fatigue);
  • sleep disturbances (insomnia at night or drowsiness during the day);
  • memory disorders;
  • tremor (involuntary muscle twitching);
  • depression;
  • ataxia (coordination disorder);
  • syncope (short-term fainting).

The cardiovascular system:

  • orthostatic hypertension. With a sharp change in body position, fainting may occur. There is dizziness with a sharp rise, this condition provokes acute vascular insufficiency;
  • tachycardia;
  • arrhythmia;
  • bradycardia;
  • vasculitis.

Respiratory system:

  • nasal congestion, swelling of the nasal mucosa;
  • cough or upper respiratory infections;
  • pharyngitis;
  • bronchitis;
  • dyspnea (shortness of breath).

Digestive system:

  • nausea, vomiting;
  • diarrhea;
  • flatulence, constipation, abdominal pain;
  • gastritis;
  • disorders in the liver;
  • dry mouth;
  • very rarely hyperbilirubinemia;

Urinary system:

  • irresistible sudden urge to urinate;
  • violations of the kidneys;
  • increased content of urea, creatinine in blood serum;
  • urinary tract infections.

reproductive system:

  • impotence;
  • decreased libido;

Hematopoietic system:

  • purpura of Shenlein-Henoch;
  • anemia.

Musculoskeletal system:

  • back or chest pain;
  • convulsions;
  • myalgia (muscle pain);

Other side effects:

  • visual disturbances, taste disorders;
  • tinnitus;
  • increased sweating;
  • dry skin;
  • erythema
  • alopecia;
  • hyperkalemia;
  • gout.

Sometimes allergic reactions are possible: rash on the skin, swelling of the face, tongue, larynx. It should be noted that the listed side effects are rare, mild and pass quickly. Usually Lorista is well tolerated by patients, withdrawal is not required. Patients with impaired water and electrolyte balance, who have a reduced volume of circulating blood, prescribe the drug with extreme caution and under the supervision of a physician.

Contraindications

The drug is not prescribed in the following cases:

  • arterial hypotension;
  • hyperkalemia (increased plasma potassium concentration);
  • lactose intolerance;
  • dehydration (lack of water in the body);
  • galactosemia (impaired absorption of glucose / galactose);
  • pregnancy;
  • breast-feeding;
  • age (up to 18 years) - the impact has not been studied;
  • hypersensitivity to the components of the drug.

In crises, for the treatment of high degrees of hypertension, for emergency and immediate care is not used. A stable effect of pressure stabilization at the required level is achieved in the vast majority of patients who take Lorista for a long time. Side effects observed in about 1% of patients. If you feel worse, you should consult a doctor to change the dose, treatment regimen or choose another drug.

Combination with other drugs

Taking lorista with diuretics (for example, triamterene) increases the risk of hyperkalemia (plasma potassium more than 5 mmol / l), which leads to disruption of the myocardium and muscle weakness.

Co-administration with anti-inflammatory nonsteroidal drugs, reduces the diuretic and hypotensive effect of drugs that reduce pressure.

Simultaneous administration of lorista and thiazide diuretics gives an additive effect (increased mutual influence).

Taking the drug with cholestyramine can lead to a deterioration in the absorption of the drug and reduces the hypertensive effect.

Analogues

Among drugs that have the same therapeutic effect and give similar side effects can be called:

  1. "Kozaar". The manufacturer is the Dutch company Merck Sharp and Dome B.V., tablets of 50 or 100 mg losertan potassium.
  2. Gizaar and Gizaar forte of the same campaign are combined forms of lorist analogues: potassium losartan (50, 100 ml) + hydrochlorothiazide (12.5 mg). Both drugs are designed to reduce pressure with a mild diuretic effect.
  3. The drug "Lozap plus". Producer "Zentiva a.s." (Czech). Oblong tablets with a light yellow coating and a notch on both sides. Active ingredients: losartan potassium (50 mg), hydrochlorothiazide (12.5 mg).
  4. "Vazotenz N" is an analogue of the drug "Lorista N". Production of the Icelandic company "Actavis group a.o.", losartan potassium (50.100 mg) + hydrochlorothiazide (12.5, 25 mg).

IN lorista instructions for use recommendations, at what pressuredrink and dose. The main thing is to follow the doctor's prescription.

At the beginning of treatment, blood pressure decreases and the condition of patients improves. The effect manifests itself with the accumulation process medicinal product in organism. Sometimes, due to addiction to the drug, its effectiveness may decrease, and the doctor resorts to increasing the dosage.

In some patients (after an initial improvement in the condition), as a manifestation side effects in the evening, bursts of emotions and an increase in blood pressure were observed. Then the treatment with lorista is canceled.

Patients (overwhelmingly) perceive this drug well and respond positively to its action. Pressure stabilization usually occurs with regular use for a month (or 2-3 weeks).

Lorista N contains 2 times more losartan (50 mg) and the same amount (12.5 mg). If the patient has a reduced volume of circulating blood, then Lorista N can be taken only after its correction, as well as the abolition of diuretics. Lorista H is prescribed if treatment with losartan has not helped stabilize blood pressure.

Lorista ND contains the same components, but 2 times more (losartan - 100 mg and hydrochlorothiazide - 25 mg).

Take orally, regardless of food intake, the frequency of admission is 1 time per day. Arterial hypertension: medium daily dose is 50 mg. The maximum antihypertensive effect is achieved within 3-6 weeks of therapy. In some patients, a more pronounced effect can be achieved by increasing the dose of the drug to 100 mg per day in two doses or in one dose. Against the background of taking large doses of diuretics, it is recommended to start therapy with 25 mg per day in one dose. In elderly patients, as well as in patients with impaired renal function, including patients on hemodialysis, no initial dose adjustment is required. Dose adjustment is not required in elderly patients or patients with impaired renal function, including patients on hemodialysis. Patients with impaired liver function should be given lower doses of the drug. Chronic heart failure: the initial dose is 12.5 mg per day in one dose. In order to reach the usual maintenance dose of 50 mg per day, the dose of the drug must be increased gradually, at intervals of one week (for example, 12.5 mg, 25 mg, 50 mg once a day). The drug is usually prescribed in combination with diuretics and cardiac glycosides. The dose of the drug should be increased according to the following scheme: 1 week: from 1 to 7 days - 1 tablet of 12.5 mg once a day. 2 weeks: from 8 to 14 days - 1 tablet of 25 mg once a day. 3 weeks: from 15 to 21 days - 1 tablet of 50 mg once a day. 4 weeks: from 22 to 28 days - 1 tablet of 50 mg once a day. Reducing the risk of stroke in patients with arterial hypertension and left ventricular hypertrophy: the standard initial dose of the drug is 50 mg per day in one dose. In the future, low-dose hydrochlorothiazide can be added and / or the dose of the drug can be increased to 100 mg per day. Renal protection in patients with type 2 diabetes mellitus with proteinuria: the standard initial dose of the drug is 50 mg per day in one dose. The dose of the drug can be increased to 100 mg per day, taking into account the decrease in blood pressure. Application in pediatrics. The safety and efficacy of the drug in children have not been established.

INN: Hydrochlorothiazide, Losartan

Manufacturer: Krka, d.d., Novo Mesto

Anatomical-therapeutic-chemical classification: Losartan in combination with diuretics

Registration number in the Republic of Kazakhstan: No. RK-LS-5 No. 019289

Registration period: 24.10.2017 - 24.10.2022

Instruction

Tradename

Lorista® H 100

International non-proprietary name

Dosage form

Film-coated tablets, 100 mg / 12.5 mg

Composition

One tablet contains

active substances: losartan potassium - 100.00 mg

hydrochlorothiazide - 12.50 mg,

Excipients: pregelatinized starch, microcrystalline cellulose, lactose monohydrate, magnesium stearate,

shell composition: hypromellose, macrogol 4000, titanium dioxide (E171), talc

Description

Oval-shaped, biconvex, film-coated tablets, white

Pharmacotherapeutic group

Drugs affecting the renin-angiotensin system.

Angiotensin II antagonists in combination with diuretics

ATC code С09DA01

Pharmacological properties

Pharmacokinetics

Suction

Losartan well absorbed from gastrointestinal tract. It undergoes significant metabolism during its first pass through the liver, forming an active metabolite with carboxylic acid and other inactive metabolites. Systemic bioavailability is approximately 33%. Taking the drug with food does not have a clinically significant effect on its serum concentrations. Losartan reaches maximum concentrations after 1 hour, and its active metabolite (E3174) - 3-4 hours after ingestion.

Hydrochlorothiazide absorbed mainly in the duodenum and in the upper sections small intestine. The degree of absorption is 70% and it increases by another 10% when hydrochlorothiazide is taken with food. Peak serum concentrations are reached within 1.5 to 5 hours.

Distribution

Losartan: more than 99% of losartan and E3174 bind to plasma proteins, mainly albumin. The volume of distribution of losartan is 34 liters. Losartan crosses the blood-brain barrier very poorly or does not penetrate at all.

Hydrochlorothiazide: the volume of distribution is approximately

3 l/kg. About 40% of the substance binds to plasma proteins. Hydrochlorothiazide accumulates in erythrocytes, but the mechanism of this phenomenon remains unknown.

breeding

Losartan: about 35% of orally administered losartan is excreted by the kidneys and 65% in the feces. With preserved kidney function, only about 5% of losartan is excreted by the kidneys unchanged and another 6% as an active metabolite. The total serum clearance of losartan and its active metabolite is approximately 600 ml/min and 50 ml/min, respectively. The renal clearance of losartan is 75 ml/min, and its active metabolite is 26 ml/min. If losartan is administered orally, about 4% of the dose taken is excreted in the urine unchanged and another 6% as the active metabolite. The half-life of losartan is 1.5 to 2 hours, and its active metabolite is 6 to 9 hours.

It is not known whether losartan and E3174 are excreted in breast milk. They are not removed from the body during hemodialysis.

Hydrochlorothiazide: elimination of hydrochlorothiazide is the result of tubular secretion. Renal clearance is approximately 33 ml/minute. Tubular secretion of hydrochlorothiazide can be competitively reduced by endogenous acid metabolites (usually formed in patients with liver or kidney damage), as well as weak exogenous acids (eg, probenecid, salicylates, and penicillin). Hydrochlorothiazide has a biphasic elimination profile. The plasma half-life is approximately 2.5 hours. total time half-life - from 5.6 to 14.8 hours. More than 95% of unchanged hydrochlorothiazide is excreted in the urine.

Hydrochlorothiazide crosses the placental barrier and is excreted into mother's milk. Serum concentrations of hydrochlorothiazide in the umbilical vein are almost the same as in the mother's blood. The content of this substance in the amniotic fluid exceeds the serum concentrations from the umbilical vein (up to 19 times). The content of hydrochlorothiazide in breast milk very low.

Pharmacodynamics

Losartan is oral selective antagonist angiotensin II receptors (type AT1). Angiotensin II binds to AT1 receptors found in various tissues (eg, vascular smooth muscle tissue, adrenal glands, kidneys, and heart) and causes vasoconstriction and aldosterone release. Angiotensin II also stimulates the proliferation of smooth muscle cells.

Losartan and its pharmacologically active metabolite (E3174) block all physiological effects of angiotensin II, regardless of its source and biosynthesis pathway; at the same time, they do not affect autonomic reflexes and do not have a permanent effect on the content of norepinephrine in plasma.

Losartan selectively binds to AT1 receptors and does not block other hormone receptors or ion channels that respond to activity regulation. of cardio-vascular system. Moreover, losartan does not inhibit the activity of angiotensin-converting enzyme (kinase II), an enzyme that is involved in the breakdown of bradykinin. As a result, with losartan therapy, effects indirectly associated with the blockade of AT1 receptors, such as potentiation of bradykinin effects or the development of edema, rarely develop.

Losartan potassium is equally effective in men and women, as well as in older (≥ 65 years) and younger patients (≤ 65 years). Its maximum effect develops 6 hours after administration. The therapeutic effect of losartan lasts 24 hours, so it is enough to take it once a day. The antihypertensive effect develops during the first week of therapy, and then gradually increases and stabilizes after 3-6 weeks.

Hydrochlorothiazide is a diuretic. Thiazide diuretics predominantly inhibit the dilution ability of the kidneys in the distal tubules, preventing the reabsorption of sodium and chloride ions in this part of the nephron. Thus, they increase the excretion of sodium, potassium, chloride and water.

At the beginning of hydrochlorothiazide therapy, the volume of fluid circulating in the vessels decreases due to increased excretion of water and salts, which leads to a decrease in blood pressure and a decrease in cardiac output. The diuretic effect occurs approximately 2 hours after the administration of hydrochlorothiazide and reaches its maximum after 3-4 hours. The diuretic effect persists for 6-12 hours. The hypotensive effect develops after 3-4 days from the start of therapy and reaches a maximum after 3-4 weeks. It persists up to 7 days after discontinuation of treatment.

The frequency of development of adverse effects when taking thiazide diuretics depends on their dose, so mild and moderate arterial hypertension is currently treated with lower doses of thiazide diuretics than in the past.

When taking Lorist® H 100, an additive effect on blood pressure is achieved (pressure reduction is greater than when taking each of the drugs separately).

Due to the diuretic effect of hydrochlorothiazide, plasma renin activity, aldosterone secretion and serum angiotensin II concentrations increase, and the serum potassium content decreases, which partially levels the effectiveness of treatment. Since aldosterone secretion is reduced, losartan reduces potassium excretion, which is usually increased when taking hydrochlorothiazide.

Despite a significant decrease in blood pressure, the use of Lorist® H 100 does not significantly affect the heart rate.

Indications for use

Arterial hypertension in patients not responding to monotherapy

losartan or hydrochlorothiazide - reducing the risk of stroke and cardiovascular mortality in arterial

al hypertension in patients with left ventricular hypertrophy.

Dosage and administration

The drug may be administered with other antihypertensive agents. The tablets can be taken with or without food, with a glass of water.

hypertension Losartan and hydrochlorothiazide are not intended for use as initial therapy, except in patients whose blood pressure does not respond to losartan or hydrochlorothiazide monotherapy. When clinically necessary, in patients whose blood pressure is not adequately controlled, a direct change from monotherapy to a fixed combination may be considered.

The usual maintenance dose is 1 tablet of Lorista® H (losartan 50 mg/hydrochlorothiazide 12.5 mg) once daily. If there is insufficient therapeutic response, the dose of Lorist® H may be increased to one tablet of Lorist® HD (losartan 100 mg / hydrochlorothiazide 25 mg) once a day. The maximum dose is one tablet of Lorista® HD (losartan 100 mg/hydrochlorothiazide 25 mg) once daily. In general, the antihypertensive effect is achieved within three to four weeks after the start of therapy.

Lorista® H 100 (losartan 100 mg / hydrochlorothiazide 12.5 mg) is indicated for patients who have been dosed up to 100 mg losartan and who require additional blood pressure control.

Reduction cardiovascular risk morbidity and mortality in patients with arterial hypertension with left ventricular hypertrophy The usual starting dose is 50 mg losartan once daily.

If the desired blood pressure level is not achieved with losartan 50 mg, treatment should be changed using a combination of losartan with a low dose of hydrochlorothiazide (12.5 mg) and, if necessary, the dose should be increased to 100 mg losartan / 12.5 mg hydrochlorothiazide once per day. If necessary, the dose should be increased to 100 mg of losartan and 25 mg of hydrochlorothiazide once a day.

Lorista H® (50 mg/12.5 mg), Lorista H®100 (100 mg/12.5 mg) and Lorista® HD (100 mg/25) are suitable alternative formulations for patients treated concomitantly with losartan and hydrochlorothiazide .

Usage in patients with kidney failure And patients on hemodialysis There is no need to adjust the dose in patients with a slight decrease in renal function (creatinine clearance 30-50 ml / min). Losartan/hydrochlorothiazide tablets are not recommended for patients on hemodialysis and should not be used in patients with a significant decrease in renal function (creatinine clearance<30 мл/мин).

In patients with hypovolemia The recommended starting dose of losartan is 25 mg once daily. In this regard, therapy with losartan / hydrochlorothiazide tablets should be started after discontinuation of diuretics and correction of hypovolemia. Patients with impaired liver function Losartan/hydrochlorothiazide is contraindicated in patients with severe hepatic impairment. Elderly patients For elderly patients, dose adjustment is not required.

Lorista H® 100 can be taken with or without food. In order not to miss taking the drug, the tablets should be taken at the same time every day. If the patient forgets to take a tablet, do not double the next dose. At the next appointment, the patient should take the usual dose of the drug at the prescribed time.

The duration of treatment is not limited.

Side effects

Often (>1/100 to<1/10):

Headache, dizziness, cephalalgia

Cough, upper respiratory tract infection, nasal congestion,

sinusitis, sinus disease

Abdominal pain, nausea, diarrhea, dyspepsia

- muscle cramps, back pain, leg pain, muscle pain

Asthenia, fatigue, chest pain

Hyperkalemia, slight decrease in hematocrit and hemoglobin

Not often(>1/1,000 up to<1/100):

Anemia, agranulocytosis, aplastic anemia, hemolytic anemia,

leukopenia, purpura, thrombocytopenia

Anorexia, hyperuricemia, hypokalemia, hyponatremia

Insomnia, anxiety, anxiety disorder, panic disorder

mental illness, confusion, depression, painful dreams, sleep disturbances,

drowsiness, memory impairment

Nervousness, paresthesia, peripheral neuropathy, tremor, migraine,

Temporary blurred vision, burning sensation or sharp pain in the eyes,

conjunctivitis, decreased visual acuity, xanthopsia

Vertigo, tinnitus

Hypotension, orthostatic hypotension, sternalgia, angina,

AV block II degree, cerebrovascular disorder, myocardial infarction,

palpitations, arrhythmia (atrial fibrillation, sinus

bradycardia, tachycardia, ventricular tachycardia, ventricular fibrillation

Necrotizing angiitis (vasculitis, cutaneous vasculitis)

pharyngeal discomfort, pharyngitis, laryngitis, difficulty breathing,

bronchitis, epistaxis, rhinitis, respiratory congestion, pneumo-

nit, pulmonary edema

Dry mouth, flatulence, gastritis, vomiting, sialadenitis, constipation, spasms,

stomach irritation, nausea, diarrhea

Alopecia, dermatitis, dry skin, erythema, hyperemia, photosensitive

ness, itching, rash, urticaria, sweating, urticaria, toxic epi-

dermal necrolysis

Arm pain, joint swelling, knee pain, musculoskeletal pain,

shoulder pain, stiffness, arthralgia, arthritis, coxalgia, fibromyalgia

gia, muscle weakness, muscle cramps

Jaundice (intrahepatic cholestasis), pancreatitis

Nocturia, frequent urination, urinary tract infections,

glucosuria, interstitial nephritis, renal failure

Decreased libido, impotence

Facial swelling, fever

Slight increase in serum urea and creatinine levels

Seldom(>1/10,000 to<1/1 000) :

Hyperkalemia, elevated ALT

Anaphylactic reactions, angioedema, allergic rash

Very rarely (<1/10 000):

Increased liver enzymes and bilirubin

Henoch-Schonlein disease, ecchymosis, hemolysis

Gout

Contraindications

Hypersensitivity to the components of the drug

Severe arterial hypotension, hypovolemia

Hypokalemia or hypercalcemia not responding to treatment

Refractory hyponatremia

Symptomatic hyperuricemia/gout

severe liver failure; cholestasis and biliary obstruction

Severe renal failure (creatinine clearance< 30 мл/мин)

Pregnancy and lactation

Children and adolescents up to 18 years of age (efficacy and safety

not studied)

Drug Interactions

Losartan Rifampicin and fluconazole have low levels of active metabolites. The clinical implications of these interactions have not been evaluated. As with other drugs that block angiotensin II or its action, moderate potassium diuretics (eg, spironolactone, triamtirene, amiloride), potassium supplements, or potassium-based salt substitutes may increase

potassium in blood serum.

As with other drugs that affect sodium excretion, lithium excretion may be reduced. Therefore, serum lithium levels should be carefully monitored if lithium salts are administered concomitantly with angiotensin II receptor antagonists. non-steroidal anti-inflammatory drugs, there may be a decrease in the antihypertensive effect. The combined use of angiotensin II antagonists or diuretics and non-steroidal anti-inflammatory drugs may lead to an increased risk of impaired renal function, including possible acute renal failure, as well as an increase in serum potassium, especially in patients with poor renal function. The combination should be used with caution, especially in elderly patients. Patients should be adequately hydrated and renal function should be closely monitored after initiation of concomitant therapy, and periodically thereafter.

In some patients with impaired renal function who are treated with non-steroidal anti-inflammatory drugs, including selective inhibitors of cyclooxygenase-2, co-administration of angiotensin II receptor antagonists may lead to further deterioration of renal function. This effect is usually reversible.

Other substances that cause hypotension, such as tricyclic antidepressants, antipsychotics, baclofen, amifostine, which lower blood pressure as a main or side effect, which may increase the risk of hypotension.

Hydrochlorothiazide Drugs that have an effect when used together with thiazide diuretics.

Alcohol, barbiturates, drugs or antidepressants:

may increase orthostatic hypotension.

Antidiabetic medicines (oral drugs and insulin): thiazide treatment may affect glucose tolerance. The dosage of the antidiabetic drug may need to be adjusted. Metformin should be used with caution due to the risk of lactic acidosis caused by possible renal impairment associated with hydrochlorothiazide.

Other antihypertensive drugs: additive effect. Cholestyramine and colestipol resins: in the presence of anion exchange resins, the absorption of hydrochlorothiazide is impaired. A single dose of cholestyramine or colestipol resins binds hydrochlorothiazide and reduces its absorption from the gastrointestinal tract by up to 85% and 43%, respectively. Corticosteroids, adrenal cortex hormone: excretion of blood electrolytes, hypokalemia may develop.

Pressor amines (eg, adrenaline): some decrease in their effectiveness may occur, but not preclude use. Skeletal muscle relaxants, non-depolarizing (eg, tubocurarine): an increased response to muscle relaxants may be possible. Lithium: diuretics reduce renal clearance of lithium and increase the risk of developing it toxic effect, and therefore, their combined use is not recommended.

Medicines used to treat gout (probenecid, sulfinpyrazone and allopurinol): an adjustment (increase) in the dose of drugs that promote the excretion of uric acid may be necessary, since hydrochlorothiazide can increase the level of uric acid in the blood serum. The combined use of thiazide increases the risk of hypersensitivity reactions to allopurinol.

Anticholinergics (eg, atropine, biperiden): increased bioavailability of thiazide-type diuretics due to decreased gastrointestinal motility and gastric emptying rate. action. Salicylates: at high doses of salicylates, hydrochlorothiazide may increase the toxic effects of salicylates on the central nervous system. Methyldopa: there is some evidence of hemolytic anemia that occurs with the combined use of hydrochlorothiazide and methyldopa. Cyclosporine: combined treatment with cyclosporine may increase the risk of hyperuricemia and complications such as gout .

Digitalis glycosides: Hypokalemia or hypomagnesemia caused by hydrochlorothiazide may contribute to cardiac arrhythmias associated with digitalis.

Drugs that are affected by impaired serum potassium: during the use of losartan / hydrochlorothiazide with drugs that are affected by violations of serum potassium (for example, digitalis glycoside and antiarrhythmic drugs), periodic monitoring of serum potassium and electrocardiograms is recommended. When using drugs that cause flutter-flicker (ventricular tachycardia), hypokalemia is a predisposing factor to enhancing these effects; These include:

    class Ia antiarrhythmic drugs (such as quinidine, hydroquinidine, disopyramide)

    class III antiarrhythmics (amiodarone, sotalol, dofetilide, ibutilide)

    certain antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, sulpiride, sultopride, amisulpride, tiapride, pimozide, haloperidol, droperidol)

    others (such as bepridil, cisapride, diphemanil, erythromycin IV,

halofantrine, mizolastine, pentamidine, terfenadine, vincamine IV).

Calcium salts: due to decreased excretion, thiazide diuretics may increase serum calcium levels. If it is necessary to prescribe calcium supplements, it is necessary to monitor and adjust the level of calcium in the blood serum.

Impact on laboratory results: due to their effect on calcium metabolism, thiazides can interfere with the conduction

parathyroid function tests.

Carbamazepine: risk of symptomatic hyponatremia. Requires clinic

chesky and biological monitoring.

Iodine contrast agent: in the case of hypohydration caused by diuretics, there is an increased risk of acute renal failure, especially with high doses of an iodine preparation. Before use in patients

ents must be restored water balance.

AmphotericinB(parenteral), corticosteroids, adrenal hormones, or stimulant laxatives

Hydrochlorothiazide may exacerbate electrolyte imbalances, in particular hypokalemia.

special instructions

Losartan

Angioedema Patients who have had angioedema (swelling of the face, lips, throat and/or tongue) should be under close medical supervision.

Hypotension and depletion of intravascular volume

Symptomatic hypotension, especially after the first dose, may occur in patients with sodium depletion caused by increased diuretic therapy, dietary salt restriction, diarrhea, or vomiting. Before using losartan / hydrochlorothiazide, such symptoms must be eliminated.

Electrolyte imbalance

Electrolyte imbalance is widespread among patients with impaired renal function, diabetes or without, and this must be taken into account. Therefore, creatinine clearance levels and plasma potassium concentrations should be carefully monitored, especially in patients with heart failure and creatinine clearance of 30-50 ml / min.

The use of moderate potassium diuretics, potassium supplements, and potassium-based salt substitutes in conjunction with losartan/hydrochlorothiazide is not recommended.

Impaired liver function

Based on pharmacokinetic data showing a significant increase in plasma concentrations of losartan in patients with liver cirrhosis, losartan should be used with caution in patients with mild to moderate hepatic impairment. There are no therapeutic data on the use of losartan in patients with severe hepatic impairment. Therefore, the losartan/hydrochlorothiazide combination is contraindicated in patients with severe hepatic impairment.

Impaired kidney function

As a result of inhibition of the renin-angiotensin-aldosterone system, changes in renal function, including renal failure, have been observed (in particular, in patients whose kidney function depends on the renin-angiotensin-aldosterone system, with severe heart failure or pre-existing renal dysfunction).

As with other drugs that affect the renin-angiotensin-aldosterone system, increases in serum urea and creatinine have been observed in patients with bilateral renal artery stenosis or stenosis of an artery to one kidney, these changes in renal function may resolve after discontinuation of treatment. Losartan should be used with caution in patients with bilateral renal artery stenosis or single renal artery stenosis.

kidney transplant

There are no data on use in patients undergoing kidney transplantation.

Primary hyperaldosteronism

Patients with primary aldosteronism usually do not respond to antihypertensive drugs that act by inhibiting the renin-angiotensin system. Therefore, the use of losartan/hydrochlorothiazide tablets is not recommended.

Coronary heart disease and cerebrovascular accident

As with any antihypertensive drug, in patients with coronary artery disease and cerebrovascular disease, excessive lowering of blood pressure can lead to myocardial infarction or stroke.

Heart failure

In patients with heart failure, with impaired or normal liver function, there is, as well as with other drugs that act on the renin-angiotensin system, the risk of serious arterial hypertension, and impaired renal function (often acute).

Stenosis of the aortic valve, mitral valve, obstructive hypertrophic cardiomyopathy

As with other vasodilators, special attention should be paid to patients suffering from aortic or mitral valve stenosis or from obstructive hypertrophic cardiomyopathy.

Ethnic features

Angiotensin-converting enzyme inhibitors, losartan and other angiotensin antagonists, have been observed to be less effective in lowering blood pressure in blacks than in others, possibly due to the predominance of low-renin conditions in this hypertensive population.

Pregnancy

The losartan/hydrochlorothiazide combination should not be used during pregnancy. Patients planning pregnancy should be switched to alternative antihypertensive treatment, which should have an approved safety profile for use during pregnancy.

When pregnancy is diagnosed, losartan/hydrochlorothiazide combination therapy should be discontinued immediately and, if appropriate, alternative treatment initiated.

Hydrochlorothiazide

Hypotension and electrolyte/fluid imbalance

As with any antihypertensive treatment, some patients may experience symptomatic hypotension. Patients should be observed for clinical signs of fluid or electrolyte imbalance, such as sodium depletion, hyponatremia, hypochloremic alkalosis, hypomagnesemia, or hypokalemia, which may occur with occasional diarrhea or vomiting. In such patients, it is necessary to periodically, at appropriate intervals, determine the electrolytes of the blood serum. Dilutional hyponatremia may occur in patients prone to edema during the hot season.

Metabolic and endocrine effects

Thiazide treatment may impair glucose tolerance. Adjustment of dosages of antidiabetic agents, including insulin, may be required. With thiazide treatment, latent diabetes mellitus may occur. Thiazides may reduce urinary calcium excretion, and may cause intermittent slight increases in serum calcium. Severe hypercalcemia may indicate latent hyperparathyroidism. Thiazides should be discontinued before parathyroid tests are performed.

An increase in cholesterol and triglyceride levels may be associated with thiazide diuretic therapy.

In some patients, thiazide therapy may exacerbate hyperuricemia and/or gout. Since losartan reduces uric acid levels, losartan in combination with hydrochlorothiazide attenuates diuretic-induced hyperuricemia.

Liver failure

Thiazides should be used with caution in patients with impaired liver function or advanced liver disease, as they can cause intrahepatic cholestasis and, due to slight changes in fluid and electrolyte balance, can cause hepatic coma.

The losartan/hydrochlorothiazide combination is contraindicated in patients with severe hepatic impairment.

Other

In cases of the presence or absence of allergies or bronchial asthma in patients taking thiazides, a hypersensitivity reaction may occur. Exacerbation or activation of systemic lupus erythematosus has been observed after the use of thiazides.

Information about fillers

Lorista® H 100 contains lactose. Patients with rare congenital galactose intolerance, congenital lactose deficiency and malabsorption of glucose-galactose should not use this drug.

Features of the influence of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Studies of the effect on the ability to drive vehicles and work with mechanisms have not been conducted. However, when driving a vehicle or using various mechanisms, it must be borne in mind that sometimes dizziness or drowsiness may occur when taking antihypertensive drugs, in particular at the beginning of treatment or when the dosage is increased.

Overdose

Symptoms: tachycardia, hypotension, it is also possible to develop bradycardia due to the activation of parasympathetic (vagal) innervation. The main symptoms of overdose include symptoms caused by a decrease in the level of electrolytes (hypokalemia, hypochloremia, hyponatremia), as well as dehydration that occurs due to excessive urination.

Treatment - drug withdrawal. If the drug has been taken recently, perform a gastric lavage. It is necessary to control vital functions, if necessary - symptomatic therapy. Hemodialysis is ineffective.

Release form and packaging

Composition and form of release of the drug

Film-coated tablets from light yellow to yellow, oval, slightly biconvex, chamfered.

Excipients: cellactose (a mixture of lactose monohydrate and cellulose), pregelatinized starch, corn starch, microcrystalline cellulose, anhydrous colloidal silicon dioxide, magnesium stearate.

Shell composition: hypromellose, talc, propylene glycol, quinoline yellow dye (E104), titanium dioxide (E171).

10 pieces. - cellular contour packings (3) - packs of cardboard.
10 pieces. - cellular contour packings (6) - packs of cardboard.
10 pieces. - cellular contour packings (9) - packs of cardboard.

pharmachologic effect

Antihypertensive agent. It is a non-peptide blocker of angiotensin II receptors. It has high selectivity and affinity for AT 1 type receptors (with the participation of which the main effects of angiotensin II are realized). By blocking these receptors, losartan prevents and eliminates the vasoconstrictive effect of angiotensin II, its stimulating effect on the secretion of aldosterone by the adrenal glands, and some other effects of angiotensin II. It is characterized by a long action (24 hours or more), which is due to the formation of its active metabolite.

Pharmacokinetics

After oral administration, losartan is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 33%. It is metabolized during the "first pass" through the liver with the formation of a carboxyl metabolite, which has a more pronounced pharmacological activity than losartan, and a number of inactive metabolites. C max in the blood of losartan and the active metabolite is achieved after 1 hour and 3-4 hours, respectively. Plasma protein binding of losartan and the active metabolite is high - more than 98%.

T 1/2 of losartan and the active metabolite in the final phase is about 1.5-2.5 hours and 3-9 hours, respectively. Losartan is excreted in the urine and feces (with bile) unchanged and as metabolites. About 35% is excreted in the urine and about 60% in the feces.

Indications

Reducing the risk of associated cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy, manifested by a decrease in the combined incidence of cardiovascular mortality, stroke and myocardial infarction.

Dermatological reactions: itching.

Others: renal dysfunction, myalgia.

drug interaction

With simultaneous use with diuretics in high doses, arterial hypotension is possible.

With simultaneous use with potassium preparations, potassium-sparing diuretics, the risk of developing hyperkalemia increases.

With simultaneous use with indomethacin, a decrease in the effectiveness of losartan is possible.

There is a report on the development of lithium intoxication with simultaneous use with lithium carbonate.

With simultaneous use with decreases the antihypertensive effect of losartan, which can lead to a significant increase in blood pressure, the development of a hypertensive crisis.

With simultaneous use with rifampicin, the clearance of losartan increases and its effectiveness decreases.

special instructions

It should be used with caution in case of arterial hypotension, decrease in BCC, disturbances in water and electrolyte balance, bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney, in renal / hepatic insufficiency

Patients who are deficient in fluid and / or sodium, before starting treatment, it is necessary to correct water and electrolyte disorders or use a lower initial dose.

In patients with dehydration (for example, treated with high doses of diuretics), symptomatic arterial hypotension may occur at the beginning of treatment with losartan.

During the period of treatment, the level of potassium in the blood should be regularly monitored, especially in elderly patients, with impaired renal function.

The simultaneous use of losartan with potassium-sparing diuretics should be avoided.

Pregnancy and lactation

Contraindicated for use during pregnancy and lactation.

Application in childhood

The safety and efficacy of losartan in children have not been established.

For impaired renal function

In case of impaired renal function, a dose reduction of losartan may be required.

For impaired liver function

In patients with a history of liver disease, losartan should be used at low doses. With cirrhosis of the liver, the concentration of losartan in the blood plasma increases significantly.

Use in the elderly

In elderly patients during treatment should regularly monitor the level of potassium in the blood.

Arterial hypertension (for patients who are indicated for combination therapy). Reducing the risk of cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy.

Contraindications Lorista H tablets 12.5mg + 50mg

Hypersensitivity to losartan, to drugs that are derivatives of sulfonamides and other components of the drug, anuria, severe renal dysfunction (creatinine clearance (CC) less than 30 ml / min.), Hyperkalemia, dehydration (including against the background of taking high doses of diuretics) , severe liver dysfunction, refractory hypokalemia, pregnancy, lactation, arterial hypotension, age under 18 years (efficacy and safety have not been established), lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome. With caution: violations of the water and electrolyte balance of the blood (hyponatremia, hypochloremic alkalosis, hypomagnesemia, hypokalemia), bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney, diabetes mellitus, hypercalcemia, hyperuricemia and / or gout, aggravated allergic history (in some patients, angioedema developed earlier while taking other drugs, including ACE inhibitors) and bronchial asthma, systemic blood diseases (including systemic lupus erythematosus), simultaneous prescription of non-steroidal anti-inflammatory drugs (NSAIDs), including cyclooxygenase-II inhibitors (COX- 2 inhibitors). Use during pregnancy and lactation. There are no data on the use of losartan during pregnancy. Fetal renal perfusion, 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 second and third trimesters. When pregnancy is established, therapy should be discontinued immediately. If necessary, the appointment of the drug during lactation, it is necessary to stop breastfeeding.

Method of application and dosage Lorista H tablets 12.5mg + 50mg

Inside, regardless of the meal. The drug can be combined with other antihypertensive agents. Arterial hypertension. The initial and maintenance dose is 1 tablet of the drug (50/12.5 mg) 1 time per day. The maximum antihypertensive effect is achieved within three weeks of therapy. To achieve a more pronounced effect, it is possible to increase the dose of the drug up to 2 tablets (50/12.5 mg) 1 time per day. The maximum daily dose is 2 tablets of the drug. In patients with a reduced volume of circulating blood (for example, while taking high doses of diuretics), the recommended initial dose of losartan in patients with hypovolemia is 25 mg once a day. In this regard, therapy should be started after the abolition of diuretics and correction of hypovolemia. In elderly patients and patients with moderate renal insufficiency, including those on dialysis, no initial dose adjustment is required. Reducing the risk of cardiovascular morbidity and mortality in patients with arterial hypertension and left ventricular hypertrophy. The standard starting dose of losartan is 50 mg once daily. Patients who fail to achieve target blood pressure levels while taking losartan 50 mg / day require selection of therapy by combining losartan with low doses of hydrochlorothiazide (12.5 mg), and, if necessary, increase the dose of losartan to 100 mg per day. in combination with hydrochlorothiazide at a dose of 12.5 mg / day, in the future - increase to 2 tablets of the drug 50 / 12.5 mg in total (100 mg of losartan and 25 mg of hydrochlorothiazide once a day).