Losartan potassium 124750-99-8 Hypertensive Treatment Powder

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Losartan potassium

Synonyms: 2-BUTYL-4-CHLORO-1-[[2'-(1H-TETRAZOL-5YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1H-IMIDAZOLE-5-METHANOL; 2-butyl-4-chloro-1-[[2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-imidazole-5-methanol monopotassium salt; 2-BUTYL-4-CHLORO-1-[[2'-(

1H-TETRAZOLE-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1H-IMIDAZOLE-5-METHANOL, POTASSIUM SALT; COZAAR; DUP 753; LOSARTAN MONOPOTASSIUM SALT;

LOSARTAN POTASSIUM; LOSARTAN POTASSIUM SALT

CAS: 124750-99-8

MF: C22H23ClKN6O

MW: 462.01

EINECS: 200-287-4

Product Categories: Hypertension; Intermediates & Fine Chemicals; Pharmaceuticals;

Losartan; APIS; Aromatics; Heterocycles; API Reference Standard; COZAAR;

Cardiovascular APIs; API

Appearance: White to Off-White Crystalline Powder

Usage: 1. Antihypertensive, AT1 angiotensin II antagonist2. Coronary vasodilator used in the diagnosis of coronary heart disease

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Pharmacological action

Losartan is a nonpeptide angiotensin II receptor antagonist with high affinity and selectivity for the AT1 receptor, without binding to or blocking other hormone receptors or ion channels important in cardiovascular regulation. Angiotensin II is a potent vasoconstrictor, a primary active hormone of the renin-angiotensin system and a major determinant of the pathophysiology of hypertension. Losartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by inhibiting the binding of angiotensin II to the AT1receptor.

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COA

Items of analysis	Specification	Results
Characters	White or off white crystalline powder	off white powder
Solubility	Free soluble in water and methanol, very slightly soluble in chloroform	Conforms
Infraed absorption	Must similar to reference standard	Conforms
Ultraviolet absorption	Must similar to reference standard	Conforms
Test for potassium	Must be positive	positive
Water	≤0.5%	0.20%
Heavy metals	≤10ppm	< 10ppm
Single impurity	≤0.2%	0.07%
Total impurity	≤0.5%	0.12%
Cyclohexane	≤1000ppm	＜LOQ(LOQ: 50ppm)
Isopropyl alcohol	≤2000ppm	234ppm
Assay	98.5-101%	99.8%
Conclusion	Qualified

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Pharmacodynamics

Losartan is a specific antagonist of the angiotensin II receptor type AT1; it does not inhibit ACE (kininase II), the enzyme that degrades bradykinin. Removal of angiotensin II negative feed back on renin secretion leads to increased plasma renin activity, during losartan administration. A 2 to 3-fold increase in angiotensin II in plasma comes as a result of increases in plasma renin activity. However, antihypertensive activity and suppression of plasma aldosterone concentration are apparent, indicating effective angiotensin II receptor blockade. After discontinuation of losartan, plasma renin activity and angiotensin levels declined.

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Indications

Losartan Tablet is indicated for the treatment of hypertension.