Incazelo

I-LCZ696 (Sacubitril/Valsartan), ehlanganisa i-Valsartan (an ARB) ne-Sacubitril (AHU377) ku-1:1 molar ratio, iyisigaba sokuqala, i-oral bioavailable, kanye ne-angiotensin receptor-neprilysin (ARN) inhibitor esebenza kabili ye-hypertension. kanye nokwehluleka kwenhliziyo[1][2][3].I-LCZ696 ithuthukisa i-cardiomyopathy yesifo sikashukela ngokuvimbela ukuvuvukala, ukucindezeleka okwenziwe nge-oxidative kanye ne-apoptosis.

Ingemuva

I-LCZ696 ingeyokuqala ekilasini i-ARNi (i-angiotensin receptor neprilysin inhibitor) ehlanganisa izingxenye ze-anionic ze-AR valsartan kanye ne-neprilysin inhibitor prodrug AHU377 (1:1 isilinganiso) sokuhluleka kwenhliziyo nomfutho wegazi ophezulu.

Ama-angiotensin receptors ama-G-protein-coupled receptors.Balamula imithambo yenhliziyo neminye imiphumela ye-angiotensin II okuyi-peptide esebenzayo yohlelo lwe-renin-angiotensin.I-Neprilysin iyi-endopeptidase engathathi hlangothi eyehlisa i-endo native vasoactive peptides njenge-natriuretic peptides.Ukuvinjelwa kwe-neprilysin kukhulisa ukugxila kwe-natriuretic peptides okube nomthelela ekuvikelweni kwenhliziyo, imithambo yegazi nezinso.[1]

Emagundaneni e-Sprague-Dawley, ukuphathwa ngomlomo kwe-LCZ696 kwaholela ekukhuphukeni okuncike kumthamo ku-immunoreactivity ye-atrial natriuretic peptide okubangelwa ukuvinjelwa kwe-neprilysin.Kumagundane e-hypertensive aphindwe kabili, i-LCZ696 ibangele ukwehla okuncike kumthamo kanye nokuqhubekayo kungcindezi ye-arterial.Abahlanganyeli abanempilo, ucwaningo olulawulwa ngokungahleliwe, oluyimpumputhe kabili, olulawulwa yi-placebo luqinisekisile ukuthi i-LCZ696 inikeze ukuvinjelwa kwe-neprilysin ngesikhathi esifanayo kanye nokuvinjelwa kwe-AT1 receptor.I-LCZ696 yayiphephile futhi ibekezelelwa kahle kumuntu.[2] [3]

Izithenjwa:
McMurray JJ, Packer M, Desai AS et al.I-Angiotensin-neprilysin inhibition ngokumelene ne-enalapril ekuhlulekeni kwenhliziyo.N Engl J Med.2014 Sep 11;371(11):993-1004.
U-Gu J, uNoe A, u-Chandra P, u-Al-Fayoumi S et al.I-Pharmacokinetics kanye ne-pharmacodynamics ye-LCZ696, inoveli esebenza kabili ye-angiotensin receptor-neprilysin inhibitor (ARNi).J Clin Pharmacol.2010 Apr;50(4):401-14.
Langenickel TH, Dole WP.I-Angiotensin receptor-neprilysin inhibition nge-LCZ696: indlela entsha yokwelapha ukuhluleka kwenhliziyo, iDrug Discov Today: Ther Strategies (2014),

Isitoreji

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