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|Product Name:||Losartan Potassium||CAS:||124750-99-8|
|MW:||462.01||Shipping Method:||EMS, HKEMS, FEDEX, DHL, UPS, Aramex, ETC|
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Pharmaceutical Raw Steroid Powder Losartan Potassium CAS 124750-99-8 For for Hypertension Treatment
Losartan Potassium is a specific antagonist of the angiotensin II receptor subtype AT1. Antagonism of the AT1 receptor and interference of association between AT1 and angiotensin II produces vasodilation and reduction of hypertension. This antagonism has other downstream effects, including a correlated antagonism of the thromboxane A2 receptor, inhibition of platelet aggregation, and induction of peroxisome proliferator-actived receptor gamma (PPARγ) activity.
As with all angiotensin II type 1 receptor (AT1) antagonists, losartan is indicated for the treatment of hypertension. It may also delay progression of diabetic nephropathy and is associated with a positive clinical outcome in that regard. It is a suitable pharmacological agent for the reduction of renal disease progression in patients with type 2 diabetes, hypertension, and microalbuminuria or proteinuria.
Losartan is also available as losartan, acombination drug with a low-dose thiazide dluretic to achieve an additive antihypertensive effect.
|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|
1. Losartan potassium,Losartan is well absorbed following oral administration and undergoes significant first-pass metabolism to produce the 5-carboxylic acid metabolite, designated as EXP3174. About 14% of an oral dosage is converted to this metabolite, which is long-acting (6 to 8 hr) and a noncompetitive antagonist at the AT1 receptor, contributing to the pharmacological effects of losartan. EXP3174 is 10-40 times more potent in blocking AT1 receptors than losartan. Losartan's bioavailability is about 32%.
2. Losartan potassium,Metabolism is primarily by cytochrome P450 isoenzymes CYP2C9 and CYP3A4. Peak plasma concentrations of losartan and EXP3174 occur about one hour and three to four hours, respectively, after an oral dose. Both losartan and EXP3174 are more than 98% bound to plasma proteins. Losartan is excreted in the urine, and in the feces via bile, as unchanged drug and metabolites. About 4% of an oral dose is excreted unchanged in urine, and about 6% is excreted in urine as the active metabolite. The terminal elimination half lives of losartan and EXP3174 are about 1.5 to 2.5 hours and 3 to 9 hours, respectively.
|A||Losartan Tablet is indicated for the treatment of hypertension.|
|A||Patients who are hypersensitive to any component of this product.|
|B||Safety and efficacy has not been established in children.|
|C||The use of Losartan Tablet during pregnancy and lactation is contra-indicated.
Losartan Tablet should be discontinued as soon as possible, when pregnancy is suspected.
|A||Women of childbearing age should ensure adequate contraception.|
|B||Symptomatic hypotension may occur after initiation of Losartan Tablet.|
|C||Reduced doses must be considered in patients with hepatic impairment.|
|D||Losartan Tablet is contra-indicated in pregnancy and should be used with care,
if at all, during breast-feeding.
|E||Losartan Tablet should be used with caution in patients with bilateral renal artery stenosis
or stenosis of an artery to a single kidney, aortic valve stenosis, and hypertrophic
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