LCZ696(Sacubitril + Valsartan)
Whakaahuatanga
Ko te LCZ696 (Sacubitril/Valsartan), ko Valsartan (he ARB) me te Sacubitril (AHU377) i roto i te 1:1 molar ratio, he tuatahi-i roto i te-akomanga, whai-waha-a-waha, me te angiotensin receptor-neprilysin (ARN) mahi aukati-rua mo te whakaheke toto. me te ngoikore o te ngakau [1][2][3]. Ko te LCZ696 te whakapai ake i te cardiomyopathy mate huka ma te aukati i te mumura, te ahotea oxidative me te apoptosis.
Papamuri
Ko te LCZ696 he ARNi tuatahi i roto i te karaehe (angiotensin receptor neprilysin inhibitor) kei roto nga waahanga anionic o AR valsartan me te neprilysin inhibitor prodrug AHU377 (1:1 ōwehenga) mo te ngoikore o te ngakau me te whakaheke toto.
Ko nga kaikawe angiotensin ko nga kaiwhakawhiwhi G-protein-coupled. Ka takawaenga ratou i te mate ngakau me etahi atu paanga o te angiotensin II he peptide koiora o te punaha renin-angiotensin. Ko te Neprilysin he endopeptidase kūpapa e whakaheke ana i nga peptides vasoactive endogenous penei i nga peptides natriuretic. Ko te aukati i te neprilysin ka whakanui ake i te kukū o nga peptides natriuretic i whai waahi ki te tiaki ngakau, ngakau me nga whatukuhu. [1]
I roto i nga kiore Sprague-Dawley, ko te whakahaere a-waha o te LCZ696 i arahi ki te pikinga o te horopeta-whakaaro i te immunoreactivity o te peptide natriuretic atrial i hua mai i te aukati neprilysin. I roto i nga kiore whakaheke toto-rua, na LCZ696 i pa mai te whakahekenga o te pehanga toto totika. Ko nga kaiuru hauora, he rangahau matapōkere, rua-matapo, te rangahau placebo-whakahaere i whakapumautia e LCZ696 i whakarato i te aukati neprilysin i te wa kotahi me te aukati kaiawhina AT1. Ko te LCZ696 he haumaru me te pai o te manawanui ki te tangata. [2] [3]
Tohutoro:
McMurray JJ, Packer M, Desai AS et al. Angiotensin-neprilysin inhibition versus enalapril i te ngoikore o te ngakau. N Ingarihi J Med. 2014 Sep 11;371(11):993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S et al. Pharmacokinetics me pharmacodynamics o LCZ696, he pukapuka-rua-mahi angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14.
Langenickel TH, Dole WP. Angiotensin receptor-neprilysin inhibition with LCZ696: a novel approach for the treatment of heart failure, Drug Discov Today: Ther Strategies (2014),
Rokiroki
| Paura | -20°C | 3 tau |
| 4°C | 2 tau | |
| I roto i te whakarewa | -80°C | 6 marama |
| -20°C | 1 marama |
Hanganga matū
Tono18Ko nga kaupapa Aromātai Tauritenga Kounga kua whakaaetia4, a6kei te whakamanahia nga kaupapa.
Ko te punaha whakahaere kounga teitei o te ao kua whakatakoto he turanga pakari mo nga hoko.
Ko te tirotiro i te kounga ka haere i roto i te huringa ora katoa o te hua ki te whakarite i te kounga me te hua rongoa.
Ko te roopu Whakahaere Whakahaere Ngaio e tautoko ana i nga tono kounga i te wa o te tono me te rehitatanga.
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