Sacubitril is a/an
Correct Answer: Neutral endopeptidase inhibitor
Description: (B) Neuro-endopeptidase inhibitor[?]Sacubitril is a pro-drug used in combination with valsartan to reduce the risk of cardiovascular events in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction.oIt acts by inhibiting neprilysin (neutral endopeptidase) which is responsible for the degradation of atrial and brain natriuretic peptide.oANP & BNP are released under atrial and ventricle stress, which activate downstream receptors leading to vasodilation, natriuresis and diuresis.oInhibition of neprilysin leads to reduced breakdown and increased concentration of endogenous natriuretic peptides in addition to increased levels of vasoconstricting hormones such as angiotensin II.oIt is given in combination with valsartan which is an aangitensin receptor blocker, resulting in a decrease in vascular resistance and blood pressure.oMost common adverse reactions (>=5%) are hypotension, hyperkalemia, cough, dizziness, & renal failure.oCardiovascular & renal effects of sacubitril is a result of the increased levels of peptides that are normally degraded by neprilysin. PHARMACOKINETICS OF SACUBITRIL* ClassAntiotensin-receptor nepilysin inhibitor* ForumulationSacubitril/valsatran-24/26mg,49/51mg,97/103mg tablets* RouteOral* Tmax0.5 hrs (Sacubitril); 2 hours (LBQ657)*; 1.5 hrs (Valsartan)* EliminationSacubitril (52-68% urine 37-48% feces; Valsartan (-13% urine; 86% feces)* Half-life1.4 hrs (sacubitril); 11.5 hrs (LBQ657)*; 9.9 hrs (valsartan)* Active metabolite of sacubitril.[?]VALSARTANois mainly used for treatment of high blood pressure, congestive heart failure, & to increase the chances of living longer after a heart attack. It is an angiotensin II receptor antagonistoSACUBITRILoSacubitril blocks the activity of an enzyme called neprilysin. When neprilysin is active, it breaks down helpful peptides Sacubitril inhibits nepnlysin so peptide levels can go up. These peptides help relax blood vessels & decrease sodium and fluid in the body.[?]ACE inhibitoroAn angiotensin-converting-enzyme inhibitor (ACE inhibitor) is used primarily for the treatment of hypertension (elevated blood pressure) and congestive heart failure.[?]Renin inhibitorsoRenin inhibitors are used primarily in treatment of essential hypertension (high blood pressure).oThese drugs inhibit the first and rate-limiting step of the renin-angiotensin-aldosterone system (RAAS), namely the conversion of angiotensinogen to angiotensin[?]Angiotensin receptor antagonist: Angiotensin II receptor blockers (ARBs) are medications that block the action of angiotensin II by preventing angiotensin II from binding to angiotensin II receptors on muscles surrounding blood vessels
Category:
Pharmacology
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