Losartan potassium

Description

Losartan potassium is the first potent and selective non-peptide angiotensin II (AT II) AT₁ receptor antagonist introduced to the market as a once-daily oral antihypertensive. It is efficacious and long lasting in controlling blood pressure in spontaneous hypertensive rats, in patients with essential hypertension in addition to those patients with renal impairment. Since losartan functions by competitive antagonism at the level of receptor, which represents the most direct way of selectively inhibiting the renin-angiotensin system (RAS) independent of the source of AT II, its use has been reported to be free of the coughing side effect exhibited by the ACE inhibitors. In contrast to calcium channel blockers, losartan does not appear to cause ankle edema, headache and tachycardia. It is also reported to be in clinical trials for the treatment of heart failure. Other reports indicate that losartan may have potential efficacy as an anxiolytic, an antiglaucoma agent, in addition to in providing protection against stroke and in preventing the myointimal proliferative response of the vascular wall after coronary angioplasty and surgery.

The Uses of Losartan potassium

A nonpeptide angiotensin II AT1-receptor antagonist. Antihypertensive.

What are the applications of Application

Losartan Potassium is a specific antagonist of the AT1 receptor with significant downstream effects.

Chemical Properties

Losartan potassium is a white to off-white free-flowing crystalline powder.Oxidation of the 5-hydroxymethyl group on the imidazole ring results in the active metabolite of losartan.

Metabolism

Losartan potassium is an orally active agent that undergoes substantial first-pass metabolism by cytochrome P450 enzymes. It is converted, in part, to an activecarboxylic acid metabolite that is responsible for most of the angiotensin II receptor antagonism that follows losartan treatment. About 14% of an orally-administereddose of losartan is converted to the active metabolite. In addition to the active carboxylic acid metabolite, several inactive metabolites are formed. In vitro studiesindicate that cytochrome P450 2C9 and 3A4 are involved in the biotransformation of losartan to its metabolites.

Side Effects

Side effects of Losartan potassium include:

diarrhea

stomach pain

muscle cramps

leg or back pain

dizziness

headache

sleep problems (insomnia)

tiredness, and

cold or flu symptoms such a stuffy nose, sneezing,sore throat, fever, and cough