Medication Description: Losartan
2-Butyl-4-chloro-1- [2- (1H-tetrazol-5-ylphenyl) benzyl] -imidazol-5-methanol.
Available in the form of potassium salt.
Synonym: Cozaar, Cozaar.
White or off-white crystalline powder. It is soluble in water and poorly in organic solvents.
The first non-peptide angiotensin II receptor blocker exhibiting high affinity and selectivity for the AT 1 receptor subtype.
-Angiotenzinovye blocking the AT 1 receptors, losartan decreases caused by arterial vasoconstriction by angiotensin II, aldosterone secretion, arginine vasopressin, norepinephrine, and endothelin-I, and the long-term use - and proliferative effects of angiotensin II in relation to cardiomyocytes, smooth muscle cells and fibroblasts of vascular wall.
Reduces total peripheral resistance (afterload), systemic arterial pressure and pressure in the pulmonary circulation.
Rapidly absorbed in the digestive tract, bioavailability is about 20-30%, C max - 1 h, T Ѕ - 1.5-2 h (metabolite - 6-9 h); undergoes biotransformation in the liver with the formation of an active metabolite, is excreted mainly with feces.
The antihypertensive effect lasts for more than 24 hours, which is caused by the metabolite action of losartan, which is 10–40 times more active than itself.
Applied with arterial hypertension and recently with congestive heart failure.
In case of arterial hypertension, they are usually used at 0.05 g (50 mg) once a day, if necessary, the daily dose can be increased in a few weeks to 0.1 g (the elderly reduce the liver and kidney problems).
In case of congestive heart failure, the initial dose is 0.0125 g (12.5 mg) once a day.
The effect of losartan develops slowly and reaches a maximum after 3-6 weeks.
Possible side effects: diarrhea, dizziness, headache, cough, impaired taste, peripheral neuropathy, arrhythmias, exacerbation of angina, allergic reactions, etc.
Losartan is contraindicated in hyperkalemia, pregnancy and lactation, in childhood.
Compatible with other antihypertensive drugs.
Product form: tablets of 0.0125 and 0.05 g (12.5 and 50 mg) (N. 7, 10, 14).
Gizaar - tablets containing losartan potassium 0.05 g (50 mg) and hydrochlorothiazide 0.0125 g (12.5 mg).
There is evidence that Gizaar is superior to losartan in antihypertensive efficacy and the ability to improve the quality of life.