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https://www.readbyqxmd.com/read/29532764/entresto-a-new-panacea-for-heart-failure
#1
Peter H Khalil, Ghazal Kabbach, Debabrata Mukherjee, Sarmad Said
Heart Failure (HF) is one of the main health care burdens in the United States and in the world. Many drugs are approved and used in practice for management of this condition; including beta blockers, diuretics, aldosterone antagonists, angiotensin converting enzyme inhibitors (ACEI's), and angiotensin receptor blockers (ARBs). Recently, the Food and Drug Administration (FDA) approved a drug with brand name Entresto (Sacubitril/Valsartan or LCZ696), an angiotensin receptor neprilysin inhibitor for the use in Heart Failure with Reduced Ejection Fraction (HFrEF) patients instead of ACEI's and ARBs...
March 13, 2018: Cardiovascular & Hematological Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29469206/impact-of-sacubitril-valsartan-combination-in-patients-with-chronic-heart-failure-and-sleep-apnoea-syndrome-the-entresto-sas-study-design
#2
Dany Jaffuel, Nicolas Molinari, Philippe Berdague, Atul Pathak, Michel Galinier, Marion Dupuis, Jean-Etienne Ricci, Jean-Pierre Mallet, Arnaud Bourdin, François Roubille
AIMS: Sleep-disordered breathing (SDB) is a highly prevalent co-morbidity in patients with chronic heart failure (CHF) and can play a detrimental role in the pathophysiology course of CHF. However, the best way to manage SDB in CHF remains a matter of debate. Sacubitril-valsartan has been included in the 2016 European Society of Cardiology guidelines as an alternative to angiotensin-converting enzyme inhibitors to further reduce the risk of progression of CHF, CHF hospitalization, and death in ambulatory patients...
June 2018: ESC Heart Failure
https://www.readbyqxmd.com/read/29398176/profound-vasoplegia-during-sacubitril-valsartan-treatment-after-heart-transplantation
#3
Aws Almufleh, Lisa M Mielniczuk, Radoslav Zinoviev, Andrew Moeller, Ross A Davies, Ellamae Stadnick, Vincent Chan, Sharon Chih
Vasoplegia occurs in up to 16% of patients who undergo heart transplantation (HT) and is associated with significant morbidity and mortality. We present a case of a 61-year-old man with ischemic cardiomyopathy receiving sacubitril/valsartan (Entresto; Novartis, Cambridge, MA) who developed profound hypotension after HT. He was treated with intravenous methylene blue and high-dose vasopressors, but developed acute kidney injury requiring dialysis and a prolonged stay in the intensive care unit. This case supports a potent vasodilatory effect of sacubitril/valsartan, and if confirmed by other studies, might warrant consideration for withholding treatment while awaiting HT, particularly in patients with risk factors for vasoplegia...
March 2018: Canadian Journal of Cardiology
https://www.readbyqxmd.com/read/29375230/prolonged-first-dose-hypotension-induced-by-sacubitril-valsartan
#4
Fu-Chih Hsiao, Pao-Hsien Chu
Entresto was recommanded by major guidelines as the frontline therapy for heart failure with reduced ejection fraction since its clinical benefit was proved by the PARADIGM-HF trial. Angiotensin converting enzyme inhibitors are the cornerstone of the treatment of HF. Varying incidences of first-dose hypotension have been reported and recognized as a potential limiting factor for prescribing. According to previous reports, the onset of hypotension mostly occur 3-5 hours after the first dose. However, the pattern of entresto-related hypotension has not been reported...
January 2018: Acta Cardiologica Sinica
https://www.readbyqxmd.com/read/29352367/continuous-manufacturing-of-co-crystals-challenges-and-prospects
#5
REVIEW
Rahul B Chavan, Rajesh Thipparaboina, Balvant Yadav, Nalini R Shastri
The last decade has witnessed extensive growth in the field of co-crystallization for mitigating the solubility and dissolution-related issues of poorly soluble drugs. This is largely because co-crystals can modify the physicochemical properties of drugs without any covalent modification in the drug molecules. The US Food and Drug Administration (FDA) now considers drug products that are designed to contain a new co-crystal, analogous to new polymorph of the active pharmaceutical ingredient (API). This positive change in regulatory perspective coupled with successful commercialization of valsartan-sacubitril co-crystal (Entresto, Novartis) has now brought co-crystals into focus, in both industries as well as academia...
January 19, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28944989/the-combination-of-valsartan-and-sacubitril-in-the-treatment-of-hypertension-and-heart-failure-an-update
#6
REVIEW
Peter Munch Nielsen, Daniela Grimm, Markus Wehland, Ulf Simonsen, Marcus Krüger
A novel antihypertensive drug, LCZ696 (Entresto®), has recently been introduced, which combines the action of an antagonist of the renin-angiotensin-aldosterone system (RAAS), effectively decreasing the blood pressure, with an inhibition of neprilysin, which is responsible for metabolizing natriuretic peptides exerting antihypertensive and antifibrotic effects. In this MiniReview, we describe the pharmacokinetics and pharmacodynamics, efficacy and side effects of the combined angiotensin receptor antagonist and neprilysin inhibitor LCZ696...
January 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28895827/after-a-big-entrance-it-s-just-so-so-for-entresto
#7
Thomas Reinke
Some industry observers wonder why the wunderkind hasn't done more wonderfully on the market. As a brand name drug, Entresto costs substantially more than the generic ACE inhibitors and ARBs. GoodRx reports the average cash price for uninsured patients for Entresto is $504 per month, compared with $44 for enalapril.
July 2017: Managed Care
https://www.readbyqxmd.com/read/28890834/the-use-of-a-novel-heart-failure-agent-in-the-treatment-of-pregnancy-associated-cardiomyopathy
#8
Vamsi C Gaddipati, Aarti A Patel, Adam J Cohen
Peripartum cardiomyopathy is an uncommon, pregnancy-related form of dilated cardiomyopathy that is associated with development of new-onset left ventricular dysfunction. Its etiology is presently unknown, but current standard of care involves the use of typical drug therapy for the treatment of heart failure. Pregnancy-associated cardiomyopathy (PACM) is a similar condition that refers to patients who develop such symptoms prior to the last month of pregnancy. We report the case of a nulliparous Caucasian female who develops early, severe PACM during her first pregnancy with postpartum persistence of New York Heart Association class II-III symptoms despite medical therapy...
2017: Case Reports in Cardiology
https://www.readbyqxmd.com/read/28883863/the-evolution-of-natriuretic-peptide-augmentation-in-management-of-heart-failure-and-the-role-of-sacubitril-valsartan
#9
Srikanth Yandrapalli, Wilbert S Aronow, Pratik Mondal, David R Chabbott
Heart failure (HF) is one of the leading causes of morbidity, mortality, and health care expenditures in the US and worldwide. For three decades, the pillars of treatment of HF with reduced ejection fraction (HFrEF) were medications that targeted the sympathetic nervous system (SNS) and the renin-angiotensin-aldosterone system (RAAS). Prior attempts to augment the natriuretic peptide system (NPS) for the management of HF failed either due to lack of significant clinical benefit or due to the unacceptable side effect profile...
August 2017: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/28676030/heart-failure-with-preserved-ejection-fraction-entresto-a-possible-option
#10
Taylor Bramblett, Mohamed Teleb, Aymen Albaghdadi, Harsh Agrawal, Debabrata Mukherjee
BACKGROUND: Heart failure with preserved ejection fraction (HFpEF) makes up half of diagnosed heart failure (HF) cases and has similar outcomes compared to heart failure with reduced ejection fraction (HFrEF) but a discrepancy in knowledge and approach to treatment. HFpEF is diagnosed using the following criteria: symptoms, preserved ejection fraction (greater than 50%), and evidence of abnormal left ventricular filling or relaxation, or diastolic distensibility or stiffness. Studies conducted to examine the efficacy of angiotensin receptor blockers (ARB) (irbesartan and candesartan), thiazide diuretics (chlorthalidone), and angiotensin converting enzyme inhibitors (ACEI) (perindopril) in the treatment of HFpEF, showed moderate efficacy but no clear benefit...
2017: Cardiovascular & Hematological Disorders Drug Targets
https://www.readbyqxmd.com/read/28569442/first-derivative-emission-spectrofluorimetric-method-for-the-determination-of-lcz696-a-newly-approved-fda-supramolecular-complex-of-valsartan-and-sacubitril-in-tablets
#11
Marwa A A Ragab, Shereen M Galal, Mohamed A Korany, Aya R Ahmed
LCZ696 (sacubitril/valsartan, Entresto™) is a therapy lately approved by United States Food and Drug Administration (US FDA) as a heart failure therapy. It is claimed to decrease the mortality rate and hospitalization for patients with chronic heart failure. This study is considered as the first report to investigate the fluorimetric behavior of sacubitril in addition to pursuing all the different conditions that may affect its fluorescence. Various conditions were studied, for example studying the effects of organized media, solvents and pH, which may affect the fluorescence behavior of sacubitril...
December 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/28515501/ismp-medication-error-report-analysis-potential-issues-with-new-basal-insulin-glp-1-fixed-combinations-hydroxyzine-hydroxyurea-mix-up-concomitant-use-of-entresto-and-ace-inhibitors-can-lead-to-serious-outcomes-more-outpatient-oral-cancer-drugs-should-be-in
#12
Michael R Cohen, Judy L Smetzer
These medication errors have occurred in health care facilities at least once. They will happen again-perhaps where you work. Through education and alertness of personnel and procedural safeguards, they can be avoided. You should consider publishing accounts of errors in your newsletters and/or presenting them at your inservice training programs. Your assistance is required to continue this feature. The reports described here were received through the Institute for Safe Medication Practices (ISMP) Medication Errors Reporting Program...
April 2017: Hospital Pharmacy
https://www.readbyqxmd.com/read/28492561/-sacubitril-valsartan-a-new-and-effective-treatment-for-heart-failure-with-reduced-ejection-fraction
#13
Michele Senni, Bruno Trimarco, Michele Emdin, Luciano De Biase
Despite significant therapeutic advances, patients with chronic heart failure and reduced ejection fraction (HFrEF) remain at high risk for heart failure progression and death. The PARADIGM-HF study, the largest outcome trial in HFrEF, has shown improved cardiovascular outcomes with sacubitril/valsartan (Entresto®, Novartis), previously known as LCZ696, compared with angiotensin-converting enzyme (ACE) inhibitor therapy, possibly leading us to a new era for heart failure treatment. Sacubitril/valsartan represents a first-in-class drug acting through inhibition of angiotensin receptor and neprilysin, thus modulating the renin-angiotensin-aldosterone system and vasoactive substances such as natriuretic peptides...
January 2017: Giornale Italiano di Cardiologia
https://www.readbyqxmd.com/read/27974807/long-term-neprilysin-inhibition-implications-for-arnis
#14
REVIEW
Duncan J Campbell
Neprilysin has a major role in both the generation and degradation of bioactive peptides. LCZ696 (valsartan/sacubitril, Entresto), the first of the new ARNI (dual-acting angiotensin-receptor-neprilysin inhibitor) drug class, contains equimolar amounts of valsartan, an angiotensin-receptor blocker, and sacubitril, a prodrug for the neprilysin inhibitor LBQ657. LCZ696 reduced blood pressure more than valsartan alone in patients with hypertension. In the PARADIGM-HF study, LCZ696 was superior to the angiotensin-converting enzyme inhibitor enalapril for the treatment of heart failure with reduced ejection fraction, and LCZ696 was approved by the FDA for this purpose in 2015...
March 2017: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/27929235/sacubitril-valsartan-entresto-for-heart-failure
#15
Judy Cheng
No abstract text is available yet for this article.
October 15, 2016: American Family Physician
https://www.readbyqxmd.com/read/27804100/rhabdomyolysis-after-coadministration-of-atorvastatin-and-sacubitril-valsartan-entresto%C3%A2-in-a-63-year-old-woman
#16
Eve S Faber, Madhavi Gavini, Ronald Ramirez, Richard Sadovsky
A 63-year-old woman previously stable on a regimen of atorvastatin 40 mg daily, carvedilol 25 mg twice daily, digoxin 0.125 mg daily, furosemide 40 mg daily, spironolactone 25 mg daily, rivaroxaban 15 mg daily, and enalapril 20 mg twice daily for heart failure developed rhabdomyolysis 26 days after enalapril was stopped and sacubitril/valsartan (Entresto™) started. The patient received sacubitril/valsartan at 24/26 mg twice daily for heart failure; however, after 26 days she developed muscle and skin pain...
December 2016: Drug Safety—Case Reports
https://www.readbyqxmd.com/read/27697814/european-drug-market-entries-2015-with-new-mechanisms-of-action
#17
Titus W P van den Heuvel, Adam F Cohen, Robert Rissmann
In this article, we consider the new drugs approved for the European market in 2015. We present a summary of the new mechanisms of action introduced and highlight three new mechanisms of action with a potentially high future impact: PCSK9 inhibition (alirocumab (Praluent®) and evolocumab (Repatha®)) for hypercholesterolaemia, neprilysin inhibition (sacubitril in combination with valsartan (Entresto®)) for heart failure, and interleukin-5 inhibition (mepolizumab (Nucala®)) for asthma.
October 2016: Clinical Medicine: Journal of the Royal College of Physicians of London
https://www.readbyqxmd.com/read/27668049/entresto-sacubitril-valsartan-first-in-class-angiotensin-receptor-neprilysin-inhibitor-fda-approved-for-heart-failure
#18
Loretta Fala
No abstract text is available yet for this article.
March 2016: American Health & Drug Benefits
https://www.readbyqxmd.com/read/27378659/angiotensin-receptor-neprilysin-inhibitor-arni-clinical-studies-on-a-new-class-of-drugs
#19
REVIEW
Mauro Gori, Maurizio Volterrani, Massimo Piepoli, Michele Senni
Sacubritil∗valsartan (Entresto, Novartis, still commonly referred to as LCZ696) is a combination drug described as a new class of dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). This combination drug has been successfully studied in patients with heart failure with both preserved (HFpEF) and reduced ejection fraction (HFrEF). In this review, the evidences in patients with HFpEF and HFrEF are summarized, including the results of more recent studies.
January 1, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/27377680/the-metalloprotease-neprilysin-degrades-and-inactivates-apelin-peptides
#20
Shaun M K McKinnie, Conrad Fischer, Kelvin M H Tran, Wang Wang, Fabricio Mosquera, Gavin Y Oudit, John C Vederas
The apelinergic system is a mammalian peptide hormone network with key physiological roles. Apelin isoforms and analogues are believed to be promising therapeutics for cardiovascular disease. Despite extensive studies on apelin-13 degradation patterns, only one protease, angiotensin-converting enzyme 2 (ACE2), had been implicated in its physiological regulation. Through use of a peptide-based fluorescent probe, we identified the metalloprotease neprilysin (NEP, a target for Entresto used in treatment of heart failure) as an enzyme that cleaves apelin isoforms...
August 17, 2016: Chembiochem: a European Journal of Chemical Biology
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