LOSARTAN POTASSIUM

Losartan Potassium is chemically described as 2-butyl-4-chloro-1-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]imidazole-5-methanol monopotassium salt. 
Losartan Potassiums empirical formula is C22H23ClKN6O , and its molecular weight is 422.9.
Losartan is generally marketed as the (basic) potassium salt of the aromatized negatively charged tetrazole, called "losartan potassium".

CAS Number: 124750-99-8
Molecular Formula: C22H23ClKN6O
Molecular Weight: 462.01
EINECS Number: 200-287-4

Synonyms:LOSARTAN POTASSIUM, 124750-99-8, Cozaar, Losacar, Losaprex, Losata, Tancin, Nu-Lotan, Losartan monopotassium salt, Aradois, Zaart, DuP 753, DuP-753, Presartan-50, MK-0954, DuP753, MK0954, L-158086, DU PONT-753, 3ST302B24A, E-3340, DTXSID3044209, 2-butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol, monopotassium salt, Potassium, Losartan, Monopotassium Salt, Losartan, Salt, Losartan Monopotassium, Losatan Potassium, Losortan Potassium, Losartan Potatssium, 2-Butyl-4-chloro-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-1H-imidazole-5-methanol, Monopotassium Salt, losartan potassium tablet, DTXCID1024209, LOSARTAN POTASSIUM 25 mg, LOSARTAN POTASSIUM 50 mg, LOSARTAN POTASSIUM 100 mg, Losartan Potassium Tablets, 25 mg, Losartan Potassium Tablets, 50 mg, Losartan Potassium Tablets, 100 mg, 658-044-7, Monopotassium 5-((4'-(2-butyl-4-chloro-5-hydroxymethyl-1H-imidazol-1-yl)methyl)biphenyl-2-yl)-1H-tetrazol-1-ide, losartan potassium salt, Lorzaar, MK 954, Lortaan, Losartan Potassium (DuP 753), MK-954, 2-Butyl-4-chloro-1-(p-(o-1H-tetrazol-5-ylphenyl)benzyl)imidazole-5-methanol, monopotassium salt, 124750-99-8 (Ka+), Lifezar, Lorzaan, Losacor, Tenopres, Lotim, Niten, Ocsaar, Neo Lotan, Du Pont 753, Losartan potassium [USAN], Covance, UNII-3ST302B24A, losartanpotassium, Losartan potassium [USAN:USP], 1H-Imidazole-5-methanol, 2-butyl-4-chloro-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-, monopotassium salt, 1H-Imidazole-5-methanol, 2-butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, monopotassium salt, Losartan potassium,  Potassium 5-[4'-[[2-butyl-4-chloro-5-(hydroxymethyl)-1H-imidazol-1-yl]methyl]biphenyl-2-yl]tetrazol-1-ide, Losartan Potassium?, Cozaar (TN), ARBLI, MK 0954, CHEMBL995, SCHEMBL42079, EPO, MLS001401407, potassium, [2-butyl-5-chloro-3-[[4-[2-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol, Ex-89, orb1310826, LOSARTAN POTASSIUM [JAN], Losartan potassium (JP17/USP), LOSARTAN POTASSIUM [HSDB], HMS2051M12, HMS2090O22, HMS2235F20, HMS3369F08, HMS3393M12, LOSARTAN POTASSIUM [VANDF], LOSARTAN POTASSIUM [MART.], BCP05332, BCP29397, LOSARTAN POTASSIUM [USP-RS], LOSARTAN POTASSIUM [WHO-DD], MSK10415, AKOS015955543, AKOS025310168, AC-1072, CCG-100869, FL24945, Losartan potassium - Bio-X trade mark, Losartan potassium, analytical standard, NC00119, 2-Butyl-4-chloro-1-(2'-(tetrazol-5-yl)biphenyl-4-ylmethyl)-1H-imidazole-5-methanol potassium, LOSARTAN MONOPOTASSIUM SALT [MI], LOSARTAN POTASSIUM [ORANGE BOOK], LOSARTAN POTASSIUM [EP MONOGRAPH], 2-Butyl-4-chloro-1-[[2'-(1H-tetrazol-5yl)-1,1'-biphenyl-4-yl]methyl]imidazole-5-methanol Potassium Salt, BL164642, HYZAAR COMPONENT LOSARTAN POTASSIUM, LOSARTAN POTASSIUM [USP MONOGRAPH], potassium 5-(4'-((2-butyl-4-chloro-5-(hydroxymethyl)-1H-imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-yl)tetrazol-1-ide, SMR000469593, L0232, NS00076270, D00357, AB01275507-01, SR-05000001514, SR-05000001514-1, Q27257991, Losartan potassium, European Pharmacopoeia (EP) Reference Standard, Losartan Potassium is known as a potent, synthetic AT1 receptor antagonist., Losartan potassium, United States Pharmacopeia (USP) Reference Standard, Losartan Potassium, Pharmaceutical Secondary Standard,  Certified Reference Material, 2-Butyl-4-chloro-1-[[2'-(1H-tetrazol-5yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol potassium, Cozaar, MK-954, 2-Butyl-4-chloro-1-2'-(1H-tetrazol-5yl)1,1'-biphenyl-4-ylmethyl-1H-imidazole-5-methanol potassium salt, Cozaar, MK-954, 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, LOSARTAN MONOPOTASSIUM SALT, LOSARTAN POTASSIUM, LOSARTAN POTASSIUM SALT, MK 954, 1h-imidazole-5-methanol,2-butyl-4-chloro-1-((2’-(1h-tetrazol-5-yl)(1,1’-biphe

Losartan Potassium is a synthetic pharmaceutical compound that belongs to the class of drugs known as angiotensin II receptor antagonists, or more commonly, angiotensin receptor blockers (ARBs). 
Losartan Potassium is formulated as the potassium salt of losartan, which improves its stability and solubility for medicinal use. 
The molecule has an extended biphenyl group with a tetrazole which is being used in place of the carboxylic acid as a bioisostere.

This medication works by selectively blocking the binding of angiotensin II, a hormone that normally causes blood vessels to constrict, to the AT1 receptor subtype, which in turn leads to vasodilation, reduced vascular resistance, and decreased blood pressure. 
By interfering with this hormonal pathway, Losartan Potassium not only lowers high blood pressure but also reduces the workload on the heart and protects the kidneys from damage that can occur due to long-term hypertension or diabetes.
Losartan Potassium is an angiotensin II receptor blocker (ARB) used to treat hypertension.

Losartan Potassium inhibitors are used for a similar indication but are associated with a cough.3 When patients with ACE inhibitor associated coughs are switched to ARBs like losartan, they have an incidence of cough similar to placebo or hydrochlorothiazide.
Losartan Potassium is available as losartan potassium oral tablets as well as a combination tablet of losartan potassium and hydrochlorothiazide.
Patients taking losartan should have their renal function and potassium levels monitored.

Losartan Potassium was granted FDA approval on 14 April 1995.
As a angiotensin II receptor antagonist, Losartan Potassium is the potassium salt of losartan with antihypertensive activity, which is mainly used in the therapy of high blood pressure (hypertension) and diabetic nephropathy. 
Losartan Potassium functions by relaxing blood vessels so that blood can flow more easily. 

Losartan Potassium is also effective to help protect the kidneys from damage caused by diabetes and lower the risks of stroke in patients suffering from hypertension and myocardial enlargement. 
Besides, recent study has suggested that losartan is beneficial to reverse age related dysfunction in maintaining normal blood pressure and cellular energy usage on mitochondria and it can probably be used to treat left ventricular hypertrophy. 
Losartan Potassium may also be used as an alternative agent for the treatment of systolic dysfunction, myocardial infarction, coronary artery disease, and heart failure.

Angiotensin II is a hormone that plays an important role in regulating blood pressure. 
Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. 
Both of these effects are mediated by the angiotensin II type 1 (AT1) receptor. 

Losartan Potassium is an AT1 receptor antagonist with a Ki value of 5-20 nM. 
Losartan Potassium has an attenuating effect on vein graft atherosclerosis in rabbits and effectively reduces arterial blood pressure in rats. 
In humans, losartan controls hypertension while protecting renal function.

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. 
Losartan Potassium 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. 
Losartan Potassium 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.

Losartan Potassium is indicated to treat hypertension in patients older than 6 years, reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy (though this benefit may not extend to patients with African heritage), and to treat diabetic nephropathy with elevated serum creatinine and proteinuria in patients with type 2 diabetes and hypertension.
Losartan Potassium with hydrochlorothiazide is indicated to treat hypertension and to reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy (though this benefit may not extend to patients with African heritage).

Losartan Potassium is an angiotensin II receptor blocker used to treat hypertension, diabetic nephropathy, and to reduce the risk of stroke.
Losartan Potassium has a long duration of action as it is given once daily.
Patients taking losartan should be regularly monitored for hypotension, renal function, and potassium levels.

Losartan Potassium reversibly and competitively prevents angiotensin II binding to the AT1 receptor in tissues like vascular smooth muscle and the adrenal gland.
Losartan Potassium and its active metabolite bind the AT1 receptor with 1000 times more affinity than they bind to the AT2 receptor.

The active metabolite of losartan is 10-40 times more potent by weight than unmetabolized losartan as an inhibitor of AT1 and is a non-competitive inhibitor.
Losartan Potassium's prevention of angiotensin II binding causes vascular smooth muscle relaxation, lowering blood pressure.

Melting point: 263–265 °C
Storage temperature: Inert atmosphere, Room Temperature
Solubility: Freely soluble in water and methanol, slightly soluble in acetonitrile
Form: Powder or crystals
Color: Off-white
Water solubility: H2O: 2 mg/mL, clear
Merck number: 14,5583
BRN number: 5845770
BCS Class: 1
Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20 °C for up to 2 months
InChI: InChI=1S/C22H22ClN6O.K/c1-2-3-8-20-24-21(23)19(14-30)29(20)13-15-9-11-16(12-10-15)17-6-4-5-7-18(17)22-25-27-28-26-22,/h4-7,9-12,30H,2-3,8,13-14H2,1H3,/q-1,+1
InChIKey: OXCMYAYHXIHQOA-UHFFFAOYSA-N
SMILES: C1(C=CC=CC=1C1=CC=C(CN2C(CO)=C(Cl)N=C2CCCC)C=C1)C1=NN=NN1[K]

Losartan Potassium blocks receptors in your body that normally bind to a hormone called angiotensin II. 
When angiotensin II binds to these receptors, it causes your blood vessels to constrict and the body to release a hormone that tells your kidneys to keep sodium. 
Blocking these receptors help your blood vessels relax so that blood can move through them more easily. 

Blocking these receptors also causes your body to get rid of sodium and water. 
These effects can help your heart work better, lower blood pressure, and may reduce your risk for heart attack, stroke, and kidney damage progression. 
Losartan Potassium is recognized as the first drug of its kind approved for therapeutic use, marking a significant advancement in cardiovascular treatment compared to older medications like ACE inhibitors, since it does not typically cause persistent dry cough, a common side effect of those drugs. 

In addition to its antihypertensive properties, Losartan Potassium also has proven efficacy in reducing the risk of stroke in patients with left ventricular hypertrophy, and it provides kidney protection in patients with type 2 diabetes and proteinuria. 
Because of these multiple benefits, it is considered a cornerstone treatment for a wide range of cardiovascular and renal conditions.
Losartan Potassium, sold under the brand name Cozaar among others, is a medication used to treat high blood pressure (hypertension).

Losartan Potassium is in the angiotensin receptor blocker (ARB) family of medication, and is considered protective of the kidneys. 
Besides hypertension, it is also used in diabetic kidney disease, heart failure, and left ventricular enlargement.
Losartan Potassium comes as a tablet that is taken by mouth.

Losartan Potassium may be used alone or in addition to other blood pressure medication.
Up to six weeks may be required for the full effects to occur.
Common adverse effects include muscle cramps, stuffy nose, dizziness, cough, high blood potassium, and anemia.

Severe adverse effects may include angioedema, low blood pressure, and kidney problems.
Use during pregnancy may result in harm to the baby, use is not recommended during breastfeeding.
Losartan Potassium works by blocking angiotensin II.

Losartan Potassium was patented in 1986, and approved for medical use in the United States in 1995.
Losartan Potassium is on the World Health Organization's List of Essential Medicines.
It is available as a generic medication.[7] In 2023, it was the eighth most commonly prescribed medication in the United States, with more than 56 million prescriptions.

A version combined with hydrochlorothiazide is available which, in 2023, was the 65th most commonly prescribed medication in the United States, with more than 9 million prescriptions.
The most common adverse effects for losartan in adults are upper respiratory infections, dizziness, and back pain.
eople with type 2 diabetes and kidney disease may experience diarrhea, fatigue, low blood pressure, low blood glucose, elevated potassium, chest pain, or allergic reaction.

Losartan Potassium should not be taken by people who are diabetic and taking aliskiren.
Anemia may occur, due to inhibition of the renin–angiotensin system, as with other angiotensin receptor blockers, losartan may injure the liver, although this effect appears to be rare.
Electrolyte imbalances may occur in people with kidney problems who take losartan, adverse outcomes do not differ by sex, age, or race.

Losartan Potassium 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 hours) and a noncompetitive antagonist at the AT1 receptor, contributing to the pharmacological effects of losartan. 

Losartan Potassium is 10–40 times more potent in blocking AT1 receptors than losartan. 
In addition, the binding to the target enzyme is pH-sensitive, and the negatively charged tetrazole ring, which is similar in size to the negative carboxylic acid derivative, may contribute to the activity of the drug.

Uses:
Losartan Potassium is also used to decrease the risk of stroke in people who have high blood pressure and a heart condition called left ventricular hypertrophy (enlargement of the walls of the left side of the heart).
Losartan Potassium is widely prescribed in clinical medicine, and its uses extend beyond simple blood pressure control because of its unique ability to block angiotensin II at the receptor level, thereby influencing several cardiovascular and renal pathways. 
The primary use of Losartan Potassium is in the management of hypertension, where it helps lower elevated blood pressure, reducing the risk of serious complications such as stroke, myocardial infarction, and heart failure. 

By preventing vasoconstriction and promoting relaxation of the blood vessels, it improves blood circulation and lowers the strain on the cardiovascular system.
Another important therapeutic use of Losartan Potassium is in protecting the kidneys, particularly in patients who suffer from type 2 diabetes and diabetic nephropathy. 
In these individuals, high blood sugar and high blood pressure together can damage the filtering units of the kidneys, and Losartan Potassium has been shown to slow down this progression by lowering intraglomerular pressure and reducing proteinuria. 

This makes it a preferred choice for patients at risk of renal failure due to long-standing hypertension and diabetes.
Losartan Potassium is also indicated in patients with left ventricular hypertrophy, a condition in which the heart muscle becomes abnormally thick due to the chronic strain of high blood pressure. 
In this context, it not only lowers blood pressure but also reduces the risk of stroke, which is a common and serious complication in such patients. 

Furthermore, it can be used as part of combination therapy for congestive heart failure when other treatments alone are insufficient, thereby improving heart function and reducing hospitalizations.
In some clinical practices, Losartan Potassium is also considered beneficial for patients who are intolerant to ACE inhibitors, since it provides similar cardiovascular and renal protection without commonly causing side effects such as persistent dry cough or angioedema. 
Because of its safety profile and broad range of benefits, Losartan Potassium has become a cornerstone drug in modern cardiology and nephrology, used both as a monotherapy and in combination with other antihypertensive agents like diuretics or calcium channel blockers for more effective management of complex cases.

Coronary vasodilator used in the diagnosis of coronary heart disease (adenosine A2A agonist).
Losartan Potassium is used alone or in combination with other medications to treat high blood pressure in adults and children at least 6 years old.
Losartan Potassium is used for hypertension, including in people with left ventricular hypertrophy (enlarged heart muscle), and kidney dysfunction among type II diabetics.

Losartan Potassium may also delay progression of diabetic nephropathy. 
It is a suitable pharmacological agent for the reduction of kidney (renal) disease progression in patients with type 2 diabetes, hypertension, and microalbuminuria (>30 mg/24 hours) or proteinuria (>900 mg/24 hours).
Although evidence shows calcium channel blockers and thiazide-type diuretics are preferred first-line treatments for most people (due to both efficacy and cost), an angiotensin II receptor antagonist such as losartan is recommended as first-line treatment in people under the age of 55 who cannot tolerate an ACE inhibitor.

One study demonstrated losartan was superior to atenolol in the primary prevention of adverse cardiovascular events (myocardial infarction or stroke), with a reduction in cardiovascular morbidity and mortality for a comparable reduction in blood pressure. 
The maximal effects on blood pressure usually occur within 3–6 weeks of starting losartan.

Safety Profile:
Losartan Potassium, while considered relatively safe compared to many older antihypertensive drugs, still carries potential hazards that must be carefully considered, especially in long-term therapy or in vulnerable populations. 
One of the main hazards is the risk of excessive lowering of blood pressure (hypotension), which can lead to dizziness, fainting, blurred vision, or even falls in elderly patients if the dose is too high or if it is combined with other medications that also reduce blood pressure.

Another significant hazard is renal impairment or worsening kidney function in certain individuals, particularly those with bilateral renal artery stenosis (narrowing of the arteries supplying the kidneys). 
In such cases, Losartan Potassium can reduce glomerular filtration pressure too much, leading to acute kidney injury. 
While it is protective in many cases of diabetic nephropathy, it may be dangerous in patients with preexisting severe kidney disease if not closely monitored.

There is also a risk of hyperkalemia (elevated potassium levels in the blood), since Losartan Potassium decreases aldosterone secretion, a hormone that normally promotes potassium excretion. 
High potassium levels can be hazardous because they may cause muscle weakness, abnormal heart rhythms, or in severe cases, life-threatening cardiac arrhythmias. 
Patients taking potassium supplements, salt substitutes, or potassium-sparing diuretics are at greater risk of this complication.