Universal reference book for medicines
Product name: LORISTA ® (LORISTA ® )

Active substance: losartan

Type: Angiotensin II receptor antagonist

Manufacturer: КРКА-РУС (Russia)
Composition, form of production and packaging
The tablets covered with a film membrane
from light yellow to yellow color, oval, slightly biconcave, with a facet.

1 tab.

Losartan potassium 12.5 mg

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

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

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
10 pieces.
- packings cellular planimetric (9) - packs cardboard.
The tablets covered with a film membrane of yellow color, oval, slightly biconcave, with a risk on one side and a facet.

1 tab.

Losartan potassium 25 mg

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

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

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
10 pieces.
- packings cellular planimetric (9) - packs cardboard.
The tablets covered with a film membrane of white color, round, slightly biconcave, with a risk on one side, with a facet.

1 tab.

Losartan potassium 50 mg

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

Sheath composition: hypromellose, talc, propylene glycol, titanium dioxide (E171).

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
10 pieces.
- packings cellular planimetric (9) - packs cardboard.
The tablets covered with a film membrane of white color, oval, slightly biconcave.

1 tab.

Losartan Potassium 100 mg

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

Sheath composition: hypromellose, talc, propylene glycol, titanium dioxide (E171).

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
10 pieces.
- packings cellular planimetric (9) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

Selective antagonist of angiotensin II receptor type AT 1 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 AT 1 -receptors regardless of the route of its synthesis: leads to an increase in plasma renin activity, reduces the concentration of aldosterone in the blood plasma.

Losartan indirectly causes the activation of AT 2 -receptors 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.
Reduces OPSS, pressure in a small circle of blood circulation;
reduces afterload, has a diuretic effect.
It prevents the development of myocardial hypertrophy, increases tolerance to physical activity in patients with chronic heart failure.

The administration of losartan 1 time / day leads to a statistically significant decrease in systolic and diastolic blood pressure.
During the day, losartan evenly controls BP, while the antihypertensive effect corresponds to a natural circadian rhythm. 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, 5-6 hours after admission. The withdrawal 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 the elderly (? 65 years) and younger patients (? 65 years).

PHARMACOKINETICS

Suction

Losartan is well absorbed from the digestive tract.
The intake of the drug with food does not have a clinically significant effect on its serum concentrations.
Bioavailability is about 33%.
C max losartan in blood plasma is achieved 1 h after ingestion. C max EXP-3174 in blood plasma is achieved in 3-4 hours.
Distribution

More than 99% of losartan and EXP-3174 bind to plasma proteins, mainly albumin.

V d of losartan is 34 liters.
Very poorly penetrates the BBB.
Metabolism

It is subject to significant metabolism during the "first passage" through the liver, forming the active metabolite EXP-3174 (14%) and a number of inactive metabolites, including the 2 main metabolites formed by hydroxylation of the butyl group of the chain and a less significant metabolite, N-2-tetrazole glucuronide.

Excretion

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.
The 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. T 1/2 losartan is 2 h. T 1/2 active metabolite is 6-9 h. About 58% of the drug is excreted with bile, 35% - kidney.
INDICATIONS

- arterial hypertension;

- reduced risk of stroke in patients with hypertension and left ventricular hypertrophy;

- Chronic heart failure (as part of combination therapy, with intolerance or inefficiency of therapy with ACE inhibitors);

- Protection of kidney function in patients with type 2 diabetes mellitus with proteinuria in order to reduce proteinuria, decrease the progression of kidney damage, reduce the risk of developing the terminal stage (preventing the need for dialysis, the probability of increasing serum creatinine levels) or the onset of death.

DOSING MODE

The drug is taken inside, regardless of food intake, the frequency of reception - 1 time / day.

With arterial hypertension, the average daily dose is 50 mg.
The maximum antihypertensive effect is achieved within 3-6 weeks of therapy. It is possible to achieve a more pronounced effect by increasing the dose of the drug to 100 mg / day in two divided doses or in one dose.
Against the background of taking diuretics in high doses, it is recommended to start Loristoy's therapy with 25 mg / day in one session.

Elderly patients, patients with impaired renal function (including patients on hemodialysis) do not need correction of the initial dose of the drug.

Patients with impaired liver function should be given a lower dose.

In chronic heart failure, the initial dose of the drug is 12.5 mg / day in one session.
In order to reach the usual maintenance dose of 50 mg / day, the dose should be increased gradually, at intervals of 1 week (eg, 12.5 mg, 25 mg, 50 mg / day). Lorist ® is usually prescribed in combination with diuretics and cardiac glycosides.
The scheme for increasing the dose of the drug is presented in the table.

1 week (from 1 to 7 days) for 1 tab.
12.5 mg / day
2 week (from 8 to 14 days) for 1 tab.
25 mg / day
3 week (from 15 to 21 days) for 1 tab.
50 mg / day
4 week (from 22 to 28 day) for 1 tab.
50 mg / day
To reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy, the standard initial dose is 50 mg / day.
In the future, hydrochlorothiazide can be added at low doses and / or Lorista dose increased to 100 mg / day.
To protect the kidneys in patients with type 2 diabetes mellitus with proteinuria, the standard initial dose of Lorista is 50 mg / day.
The dose of the drug can be increased to 100 mg / day, taking into account the decrease in blood pressure.
SIDE EFFECT

From the central nervous system and peripheral nervous system :? 1% - dizziness, asthenia, headache, fatigue, insomnia;
<1% - anxiety, sleep disturbance, drowsiness, memory disorders, peripheral neuropathy, paresthesia, hypostases, migraine, tremor, ataxia, depression, syncope.
From the cardiovascular system: orthostatic hypotension (dose-dependent), palpitations, tachycardia, bradycardia, arrhythmias, angina pectoris, vasculitis.

On the part of the respiratory system: 1% - nasal congestion, cough *, upper respiratory tract infections, pharyngitis, dyspnoea, bronchitis, edema of the nasal mucosa.

From the digestive system :? 1% - nausea, diarrhea *, dyspeptic phenomena *, abdominal pain;
<1% - anorexia, dry mouth, toothache, vomiting, flatulence, gastritis, constipation, hepatitis, a violation of liver function; very rarely - increased activity of liver enzymes, hyperbilirubinemia.
From the urinary system: <1% - mandatory urination, urinary tract infections, impaired renal function;
sometimes - a moderate increase in the level of urea and creatinine in the blood serum.
On the part of the reproductive system: <1% - decreased libido, impotence.

From the musculoskeletal system: 1% - convulsions, myalgia *, pain in the back, chest, legs;
<1% - arthralgia, arthritis, pain in the shoulder, knee, fibromyalgia.
From the senses: <1% - ringing in the ears, a violation of taste, visual impairment, conjunctivitis.

On the part of the system of hematopoiesis: infrequently - anemia, purple Shenlaine-Genocha.

Dermatological reactions: <1% - dry skin, erythema, photosensitivity, increased sweating, alopecia.

From the metabolism: giperkaliemia, gout.

Allergic reactions: <1% - urticaria, skin rash, itching, angioedema (including swelling of the larynx and tongue, causing airway obstruction and / or swelling of the face, lips, pharynx).
Sometimes angioedema has developed earlier when taking other medicines, including. ACE inhibitors.
* - side effects, the incidence of which is comparable to placebo.

In most cases, Lorista ® is well tolerated, side effects are mild and transient and do not require withdrawal of the drug.

CONTRAINDICATIONS

- arterial hypotension;

- Hyperkalemia;

- dehydration;

lactose intolerance;

- galactosemia or syndrome of impaired glucose / galactose absorption;

- Pregnancy;

- lactation period;

- age under 18 years (effectiveness and safety not established);

- hypersensitivity to losartan and / or other components of the drug.

Precautions should be taken with liver and / or renal failure, reduced bcc, water-electrolyte balance disorders, bilateral stenosis of the renal arteries, or stenosis of the artery of a single kidney.

PREGNANCY AND LACTATION

There are no data on the use of losartan in pregnancy.
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 with the use of losartan in the II and III trimesters. When establishing pregnancy, losartan should be discontinued immediately.
There is no data on the isolation of losartan with breast milk.
Therefore, the question of stopping breastfeeding or abolishing losartan therapy should be addressed, taking into account its importance for the mother.
APPLICATION FOR FUNCTIONS OF THE LIVER

With caution appoint losartan to patients with impaired renal function, bilateral stenosis of the renal arteries or unilateral stenosis of the artery of a single kidney.Regularly monitor the concentration of potassium, urea and creatinine in serum.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Patients with a history of liver disease are recommended therapy with lower doses.

APPLICATION FOR CHILDREN

The drug is contraindicated for the treatment of children and adolescents under the age of 18 , since there is no experience of using the drug in pediatrics.

APPLICATION IN ELDERLY PATIENTS

Older patients do not need to adjust the initial dose of the drug.

SPECIAL INSTRUCTIONS

In patients with reduced BCC (for example, when treating with large doses of diuretics) symptomatic arterial hypotension may develop.
Before starting losartan, it is necessary to eliminate the existing disorders, or start therapy with small doses.
In patients with mild and moderate cirrhosis of the liver, the concentration of losartan and its active metabolite in the blood plasma after ingestion is higher than in healthy ones.
Therefore, patients with a history of liver disease are recommended therapy in lower doses.
In patients with impaired renal function, with or without diabetes mellitus, hyperkalemia often develops, which should be borne in mind, but only in rare cases does it stop treatment.
During the treatment period, the concentration of potassium in the blood should be monitored regularly, especially in elderly patients, with renal dysfunction.
Drugs acting on the renin-angiotensin system can increase urea and creatinine in the serum in patients with bilateral renal artery stenosis or unilateral stenosis of the artery of a single kidney.
Changes in kidney function can be reversible after the abolition of therapy. During the treatment period, it is necessary to regularly monitor the serum creatinine concentration at regular intervals.
Use in Pediatrics

The drug is contraindicated for the treatment of children and adolescents under the age of 18 , since there is no experience of using the drug in pediatrics.

Impact on the ability to drive vehicles and manage mechanisms

Data on the effect of losartan on the ability to control transport or other technical means are not available.

OVERDOSE

Symptoms: marked decrease in blood pressure, tachycardia;
As a result of parasympathetic (vagal) stimulation, a bradycardia can develop.
Treatment: forced diuresis, symptomatic therapy.
Hemodialysis is ineffective.
DRUG INTERACTION

There was no clinically significant drug interaction with hydrochlorothiazide, digoxin, indirect anticoagulants, cimetidine, phenobarbital, ketoconazole and erythromycin.

During simultaneous administration with rifampicin and fluconazole, a decrease in the level of the active metabolite of potassium losartan was noted.
The clinical consequences of this phenomenon are unknown.
Simultaneous use with potassium-sparing diuretics (eg spironolactone, triamterene, amiloride) and potassium preparations increases the risk of hyperkalemia.

Simultaneous use of NSAIDs, including selective inhibitors of COX-2, can reduce the effect of diuretics and other antihypertensive agents.

If losartan is administered concomitantly with thiazide diuretics, a decrease in blood pressure is approximately additive.
Strengthens (mutually) the effect of other antihypertensive drugs (diuretics, beta-blockers, sympatholytics).
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored out of reach of children, dry place at a temperature of no higher than 30 ° C.
Shelf life - 5 years.
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