LCZ696 (Sacubitril + Valsartan)
Nkọwa
LCZ696 (Sacubitril/Valsartan), nke gụnyere Valsartan (ARB) na Sacubitril (AHU377) na 1: 1 molar ratio, bụ nke mbụ na klaasị, ọnụ ọnụ bioavailable, na dual-eme angiotensin receptor-neprilysin (ARN) inhibitor maka ọbara mgbali elu. na nkụda mmụọ obi[1][2][3].LCZ696 na-emeziwanye cardiomyopathy ọrịa shuga site na igbochi mbufụt, nrụgide oxidative na apoptosis.
ndabere
LCZ696 bụ nke mbụ na klaasị ARNi (angiotensin receptor neprilysin inhibitor) nke gụnyere moieties anionic nke AR valsartan na neprilysin inhibitor prodrug AHU377 (1: 1 ratio) maka nkụda obi na ọbara mgbali elu.
Ndị na-anabata angiotensin bụ G-protein jikọtara ọnụ.Ha na-agbazi obi na vaskụla mmetụta ndị ọzọ nke angiotensin II nke bụ peptide bioactive nke sistemu renin-angiotensin.Neprilysin bụ endopeptidase na-anọpụ iche nke na-eweda peptides endogenous vasoactive dị ka peptides natriuretic.Mgbochi nke neprilysin na-abawanye mkpokọta peptides natriuretic nke nyere aka na nchekwa obi, vaskụla na akụrụ.[1]
Na oke Sprague-Dawley, nchịkwa ọnụ nke LCZ696 butere ịrị elu dabere na dose na immunoreactivity nke peptide atrial natriuretic sitere na mgbochi neprilysin.N'ime oke oke transgenic okpukpu abụọ nke hypertensive, LCZ696 butere mbelata nke dabere na dose na nkwụsi ike na nrụgide akwara.Ndị sonyere na ahụike, nyocha nke enweghị usoro, kpuru okpukpu abụọ, ebe a na-achịkwa ebebo gosipụtara na LCZ696 nyere mgbochi neprilysin na-emekọ ihe yana mgbochi nnabata AT1.LCZ696 dị mma yana nnabata nke ọma n'ime mmadụ.[2] [3]
Ntụaka:
McMurray JJ, Packer M, Desai AS et al.Angiotensin-neprilysin inhibition na enalapril na nkụda obi.N Engl J Med.2014 Sep 11;371(11):993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S et al.Pharmacokinetics na pharmacodynamics nke LCZ696, akwụkwọ akụkọ abụọ na-eme angiotensin receptor-neprilysin inhibitor (ARNi).J Clin Pharmacol.2010 Eprel; 50 (4): 401-14 .
Langenickel TH, Dole WP.Angiotensin receptor-neprilysin inhibition na LCZ696: usoro ọhụụ maka ọgwụgwọ nke nkụda obi, Drug Discov Taa: Ther Strategies (2014)
Nchekwa
| Ntụ ntụ | -20°C | Afọ 3 |
| 4°C | afọ 2 | |
| Na ihe mgbaze | -80 Celsius | Ọnwa isii |
| -20°C | 1 ọnwa |
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