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Sacubitril
Sacubitril (; INN) is an antihypertensive drug used in combination with valsartan. The combination drug sacubitril/valsartan, known during trials as ''LCZ696'' and marketed under the brand name ''Entresto'', is a treatment for heart failure. It was approved under the FDA's priority review process for use in heart failure on July 7, 2015. Side effects Sacubitril increases levels of bradykinin, which is responsible for the edema seen sometimes in patients with the medication. This is why the medication is not recommended for patients with a history of pulmonary edema with the usage of ACE inhibitors. Mechanism of action Sacubitril is a prodrug that is activated to sacubitrilat (LBQ657) by de- ethylation via esterases. Sacubitrilat inhibits the enzyme neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure–lowering peptides that work mainly by reducing blood volume. In addition, neprilysin degrades a variety of peptides ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sacubitril/valsartan
Sacubitril/valsartan, sold under the brand name Entresto among others, is a fixed-dose combination medication for use in heart failure. It consists of the neprilysin inhibitor sacubitril and the angiotensin receptor blocker valsartan. The combination is sometimes described as an "angiotensin receptor-neprilysin inhibitor" (ARNi). In 2016, the American College of Cardiology/American Heart Association Task Force recommended it as a replacement for an ACE inhibitor or an angiotensin receptor blocker in people with heart failure with reduced ejection fraction. Potential side effects include angioedema, nephrotoxicity, and low blood pressure. It was approved for medical use in the United States and in the European Union in 2015, and in Australia in 2016. In 2022, it was the 165th most commonly prescribed medication in the United States, with more than 3million prescriptions. It is available as a generic medication. Medical uses Sacubitril/valsartan can be used instead of an AC ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sacubitril Activation
Sacubitril (; INN) is an antihypertensive drug used in combination with valsartan. The combination drug sacubitril/valsartan, known during trials as ''LCZ696'' and marketed under the brand name ''Entresto'', is a treatment for heart failure. It was approved under the FDA's priority review process for use in heart failure on July 7, 2015. Side effects Sacubitril increases levels of bradykinin, which is responsible for the edema seen sometimes in patients with the medication. This is why the medication is not recommended for patients with a history of pulmonary edema with the usage of ACE inhibitors. Mechanism of action Sacubitril is a prodrug that is activated to sacubitrilat (LBQ657) by de- ethylation via esterases. Sacubitrilat inhibits the enzyme neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure–lowering peptides that work mainly by reducing blood volume. In addition, neprilysin degrades a variety of peptides i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neprilysin
Neprilysin (; also known as membrane metallo-endopeptidase (MME), neutral endopeptidase (NEP), cluster of differentiation 10 (CD10) and common acute lymphoblastic leukemia antigen (CALLA)) is an enzyme that in humans is encoded by the ''MME'' gene. Neprilysin is a zinc-dependent metalloprotease that cleaves peptides at the amino side of hydrophobic residues and inactivates several peptide hormones including glucagon, enkephalins, substance P, neurotensin, oxytocin, and bradykinin. It also degrades the amyloid beta peptide whose abnormal folding and aggregation in neural tissue has been implicated as a cause of Alzheimer's disease. Synthesized as a membrane-bound protein, the neprilysin ectodomain is released into the extracellular domain after it has been transported from the Golgi apparatus to the cell surface. Neprilysin is expressed in a wide variety of tissues and is particularly abundant in kidney. It is also a common acute lymphocytic leukemia antigen that is an imp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Valsartan
Valsartan, sold under the brand name Diovan among others, is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease. It belongs to a class of medications referred to as angiotensin II receptor blockers (ARBs). It is a reasonable initial treatment for high blood pressure. It is taken by mouth. Common side effects include feeling tired, dizziness, high blood potassium, diarrhea, and joint pain. Other serious side effects may include kidney problems, low blood pressure, and angioedema. Use in pregnancy may harm the baby and use when breastfeeding is not recommended. It is an angiotensin II receptor antagonist and works by blocking the effects of angiotensin II. Valsartan was patented in 1990, and came into medical use in 1996. It is available as a generic medication. In 2022, it was the 117th most commonly prescribed medication in the United States, with more than 5million prescriptions. Medical uses Valsartan is used to treat high blood ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sacubitrilat
Sacubitrilat (INN; or LBQ657) is the active metabolite of the antihypertensive drug sacubitril, which is used in the treatment of heart failure Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome caused by an impairment in the heart's ability to Cardiac cycle, fill with and pump blood. Although symptoms vary based on which side of the heart is affected, HF .... References Antihypertensive agents Biphenyls Carboxylic acids Amides {{cardiovascular-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Atrial Natriuretic Peptide
Atrial natriuretic peptide (ANP) or atrial natriuretic factor (ANF) is a natriuretic peptide hormone secreted from the cardiac atria that in humans is encoded by the ''NPPA'' gene. Natriuretic peptides (ANP, BNP, and CNP) are a family of hormone/paracrine factors that are structurally related. The main function of ANP is causing a reduction in expanded extracellular fluid (ECF) volume by increasing renal sodium excretion. ANP is synthesized and secreted by cardiac muscle cells in the walls of the atria in the heart. These cells contain volume receptors which respond to increased stretching of the atrial wall due to increased atrial blood volume. Reduction of blood volume by ANP can result in secondary effects such as reduction of extracellular fluid (ECF) volume, improved cardiac ejection fraction with resultant improved organ perfusion, decreased blood pressure, and increased serum potassium. These effects may be blunted or negated by various counter-regulatory mechanism ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Edema
Edema (American English), also spelled oedema (British English), and also known as fluid retention, swelling, dropsy and hydropsy, is the build-up of fluid in the body's tissue (biology), tissue. Most commonly, the legs or arms are affected. Symptoms may include skin that feels tight, the area feeling heavy, and joint stiffness. Other symptoms depend on the underlying cause. Causes may include Chronic venous insufficiency, venous insufficiency, heart failure, kidney problems, hypoalbuminemia, low protein levels, liver problems, deep vein thrombosis, infections, kwashiorkor, angioedema, certain medications, and lymphedema. It may also occur in immobile patients (stroke, spinal cord injury, aging), or with temporary immobility such as prolonged sitting or standing, and during menstruation or pregnancy. The condition is more concerning if it starts suddenly, or pain or shortness of breath is present. Treatment depends on the underlying cause. If the underlying mechanism involve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mitsunobu Reaction
The Mitsunobu reaction is an organic reaction that converts an alcohol into a variety of functional groups, such as an ester, using triphenylphosphine and an azodicarboxylate such as diethyl azodicarboxylate (DEAD) or diisopropyl azodicarboxylate (DIAD). Although DEAD and DIAD are most commonly used, there are a variety of other azodicarboxylates available which facilitate an easier workup and/or purification and in some cases, facilitate the use of more basic nucleophiles. It was discovered by Oyo Mitsunobu (1934–2003). In a typical protocol, one dissolves the alcohol, the carboxylic acid, and triphenylphosphine in tetrahydrofuran or other suitable solvent (e.g. diethyl ether), cool to 0 °C using an ice-bath, slowly add the DEAD dissolved in THF, then stir at room temperature for several hours. The alcohol reacts with the phosphine to create a good leaving group then undergoes an inversion of stereochemistry in classic SN2 fashion as the nucleophile displaces it. A c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyridine
Pyridine is a basic (chemistry), basic heterocyclic compound, heterocyclic organic compound with the chemical formula . It is structurally related to benzene, with one methine group replaced by a nitrogen atom . It is a highly flammable, weakly alkaline, water-miscible liquid with a distinctive, unpleasant fish-like smell. Pyridine is colorless, but older or impure samples can appear yellow, due to the formation of extended, unsaturated Polymer, polymeric chains, which show significant electrical conductivity. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Historically, pyridine was produced from coal tar. As of 2016, it is synthesized on the scale of about 20,000 tons per year worldwide. Properties Physical properties Pyridine is diamagnetism, diamagnetic. Its critical point (thermodynamics), critical parameters are: pressure 5.63 MPa, temperature 619 K and volume 248 cm3/mol. In the temperatur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Succinic Anhydride
Succinic anhydride, is an organic compound with the molecular formula (CH2CO)2O. This colorless solid is the acid anhydride of succinic acid. Preparation In the laboratory, this material can be prepared by dehydration of succinic acid. Such dehydration can occur with the help of acetyl chloride or phosphoryl chloride, or thermally. Industrially, succinic anhydride is prepared by catalytic hydrogenation of maleic anhydride. Reactions Succinic anhydride hydrolyzes readily to give succinic acid: :(CH2CO)2O + H2O → (CH2CO2H)2 With alcohols (ROH), a similar reaction occurs, delivering the monoester: :(CH2CO)2O + ROH → RO2CCH2CH2CO2H Succinic anhydride is used in acylations under Friedel-Crafts conditions, as illustrated by the industrial route to the drug Fenbufen. Related compounds Maleic anhydride undergoes the Alder-ene reaction with alkenes to give alkenylsuccinic anhydrides. Such compounds are sizing agents in the paper industry. In this role, the anhydride is propos ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
