Expiration date: 06/2025
Pharmacological action:
Antihypertensive
Blocks the angiotensin II receptor (subtype AT1) in various tissues, including cortical substance of adrenal glands, brain, kidney, liver, vascular smooth muscles, heart and prevents the development of effects of angiotensin II. Reduces arterial vasoconstriction, peripheral vascular resistance, the pressure in the pulmonary circulation, lowers blood pressure jamming in the pulmonary vessels, inhibits the release of aldosterone, prevents retention of sodium and water in the body. Increases tolerance to physical load in patients with heart failure.
After receiving a single antihypertensive effect (reduction in SBP and DBP) reaches a maximum at 6 h and gradually (over 24 h) decreases. Stable lower blood pressure most patients have to a 3-6 week course.
In experiments on rats and mice for 2 years, receiving the maximum tolerated dose (200 mg/kg/day) of carcinogenic action is not detected. However, in female rats revealed a slight increase in the incidence of adenomas of the acini of the pancreas. In vitro and in vivo mutagenic properties are not detected. Fertility and reproductive function of male rats receiving inside doses up to 150 mg/kg/day, did not change. When administered to female rats doses of 100 mg/kg/day or more was observed reduction in the number of yellow bodies, implants and embryos.
Rapidly absorbed from the gastrointestinal tract. Bioavailability is small (approximately 33%) because the "first pass" through the liver losartan biotransformation by carboxylation with the participation of cytochrome P450 2C9 and 3A4 with the formation of the main metabolite is 10-40 times more active, than initial substance. Cmax achieved within 1 h (losartan) and 3-4 hrs (active metabolite), the plasma protein binds to the 98.7% (losartan) and 99.8% (metabolite), T1/2 is 1.5–2 h and 6-9 h respectively. In addition to the active carboksiproizvodnyi formed several inactive metabolites. Excreted kidneys approximately 35% (4% unchanged and 6% as active metabolite), faeces — about 60%.
Indications :
Hypertension.
Reducing the risk associated cardiovascular morbidity and mortality in patients with hypertension and left ventricular hypertrophy, manifested by a decline in the aggregate frequency of cardiovascular mortality, stroke and myocardial infarction.
Protection of kidneys in patients with diabetes mellitus type 2 with proteinuria - slowing the progression of renal failure, manifested by a reduced frequency
gipercreatininemia, the incidence of ESRD requiring hemodialysis or renal transplantation,
mortality and reduction of proteinuria.
Chronic heart failure when treatment failure with ACE inhibitors.
Dosing regimen:
The average ingestion dose is 50 mg 1 times/day.
If necessary, the dose may be reduced to 25 mg or increased to 100 mg/day, in the latter case, it is possible to use 2 times/day.
Side effects:
From the side of cardiovascular system: dizziness, orthostatic hypotension.
From the metabolic: hyperkalemia.
Allergic reactions: angioedema (including swelling of the face, lips, pharynx and/or tongue), urticaria.
From the digestive system: diarrhea, increased ALT activity.
CNS: headache.
Dermatological reactions: itching.
Other: renal dysfunction, myalgia.
Contraindications:
Pregnancy, lactation, childhood and adolescence to 18 years, increased sensitivity to losartan.
Application of pregnancy and breast-feeding:
Contraindicated during pregnancy and lactation.
Application for violations of liver function:
Patients with the history of liver disease, losartan should be used in low doses. In liver cirrhosis the concentration of losartan in blood plasma increases considerably.
Application for violations of renal function:
If impaired renal function may require a dose reduction of losartan.
Use in children:
The safety and efficacy of losartan in children have not been established.
Use in elderly patients:
The elderly patients during treatment should regularly monitor the level of potassium in the blood.
Special instructions:
With care use hypotension, a decrease in BCC, violations vodno-elektrolitnogo balance, bilateral renal artery stenosis or stenosis of artery only kidneys, the kidney/liver failure
Patients who have a deficiency of fluid and/or sodium before treatment is necessary to correct water and electrolyte imbalance or use a lower initial dose.
In patients with dehydration (for example, receiving treatment dioretikami in high doses) at the beginning of treatment with losartan may experience symptomatic hypotension.
If impaired renal function may require a dose reduction of losartan.
Patients with the history of liver disease, losartan should be used in low doses. In liver cirrhosis the concentration of losartan in blood plasma increases considerably.
During treatment should regularly monitor the level of potassium in the blood, especially in elderly patients when impaired renal function.
Should avoid the simultaneous use of losartan with potassium-sparing diuretics.
The safety and efficacy of losartan in children have not been established.
Drug interactions:
While the use of diuretics in high doses, possible hypotension.
At simultaneous application with preparations of potassium, kalisberegatmi dioretikami increased risk of giperkaliemii.
While the use of indomethacin may decrease the effectiveness of losartan.
There are reports about the development of lithium toxicity while the use of lithium carbonate.
While the use of orlistat reduces the antihypertensive effect of losartan, which may lead to a significant increase in blood pressure, the development of hypertensive crisis.
At simultaneous application with rifampicin increased clearance of losartan and decreases its effectiveness.
Terms of release:
A drug dispensed by prescription.
Storage conditions:
In a dry, protected from light place, at temperature not above 25 °C.
Keep out of reach of children.
