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.
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White to Off-White Crystalline Powder
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A nonpeptide angiotensin II AT1-receptor antagonist. Antihypertensive.
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Selective non-peptide angiotensin AT 1 receptor antagonist. Inhibits the contractile effects of angiotensin II on rabbit aorta and jugular vein (pA 2 = 8.27). Orally active antihypertensive agent.
