I-Ezetimibe yiyilisi ehlisa amanqanaba e-cholesterol . Kuye kwavunyelwa i-FDA ukususela ngo-2002, kwaye ithengiswa njengesisigxina sokuzimela (iZeta) ngokudibanisa ne-simvastatin (i- statin drug) njengeVitoin. Nangona kunjalo, i-ezetimibe ibe yinto ephikisanayo ngokusungulwa kwayo, kwaye iingcali ziphikisana nendawo yayo efanelekileyo kunyango lweengxaki ze lipid.
Ezetimibe
I-Ezetimibe isebenza ngokuthintela ukukhutshwa kwe-cholesterol emathunjini.
Ngokuqhelekileyo, i-cholesterol ephuma emathunjini ithathwa ngama-chylomicron kwisibindi, apho isetyenziselwa iinkqubo ezibalulekileyo ezibalulekileyo. Xa inani le-cholesterol elichithwe liyancitshiswa yi-ezetimibe, isibindi kufuneka sinike ukunikezwa kwe-cholesterol ngokususa kwiipoproteins ezijikelezayo kwigazi. Ngaloo ndlela, izinga legazi le-cholesterol linciphisa.
Ngokuqhelekileyo, i-ezetimibe ngokwayo okanye inxulumene nesimo sinciphisa inani le- cholesterol yeLDL egazini malunga ne-15%.
Iziphumo ezimbi ze-Ezetimibe
Ngokubanzi, i-ezetimibe iyakunyamezeleka. Isisindo, isifo sohudo, kunye nokuphendulwa komzimba kungenzeka. Nangona i-myopathy (i-side effects effects) ivakaliswe nge-ezetimibe, efana ne-myopathy ebonwe ngama-statins , iziganeko zaloo ngxaki zibonakala ziphantsi kakhulu kuneemimiselo. Enyanisweni, i-ezetimibe ingafakwa kwi-statin ye-dose ephantsi ukwenzela ukufezekisa ukunciphisa i-cholesterol ngaphandle kwe-myopathy ngezinye iinkalo kubonwa ngama-high-dose statins.
Ukuphikisana ne-Ezetimibe
Xa i-ezetimibe yavunywa kuqala, yayithengiswa kakhulu njengeVitoin (ezetimibe kunye ne-simvastatin), kwaye i-sales yandile. Unokukhumbula iimveliso zentengiso ngexesha elithelekisa umninazana wakho omnandi, u-rotund uSuzie kwisiqhekeza esikhulu se-strawberry shortcake kule mode. YayiyiVivinin.
Kuye kwenzeka ukuba, ngelixa ezo ntengiso zisebenza kwaye ngoxa uMerck wayethengisa iibhiliyoni zeedola zikaVytorin, ukushicilelwa kwakulibazisekile (okusolakileyo, abanye bathi) kwilingo le-clinic elixhaswe yi-Merck elibizwa ngokuba yi-ENHANCE. I-ENHANCE yayijoliswe ekuboniseni ukuba iVittorin iphucule i- atherosclerotic plaques ngaphezu kwe-simvastatin yedwa. Xa iziphumo zagqitywa ngo-2008, kwafunyanwa ukuba abantu baphathwa kunye noVytorin benza okubi kakhulu (kungekuhle) kunabo bafumana i-simvastatin yedwa.
Ngenxa yezi mpawu ezimbi (kunye nenyaniso yokuba abaninzi babecinga ukulibaziseka ekubhengezeni ezo ziphumo ukuba ubuncinci), ukuthengiswa kwe-ezetimibe itanki. Yaye ezo ntengiso zaphela ngokupheleleyo.
Inzala kwi-ezetimibe iye yavuselela ngokubanzi ukususela ngo-2014, xa iziphumo zovavanyo lwe-IMPROVE-IT zipapashwe. Kule vavanyo, izigulane ezine -coronary syndrome (ACS) eziqhelekileyo zazingenakulinganiswa ukufumana iVivtorin okanye i-simvastatin yodwa. Emva kweminyaka engama-6, izigulane ezitholayo iVittorin zenze ngcono ngokuthobekileyo iziphumo zeklinikhi (ezimbalwa ezifundwayo ze-ACS, kunye nesidingo esincinci sokuhlinzwa okanye i- stents esilandelayo ), kodwa kwakungenalohluko kwimpilo.
Uhlalutyo lwamagqabantshintshintshi-Uvavanyo lucetyiswa ukuba phantse yonke inzuzo ebonwa kwiqela lakwaVittorin lingabalwa ngabagulane abanesifo sikashukela.
Kubantu abanesifo sikashukela, akukho nzuzo yokongeza i-ezetimibe iboniswe.
I-Ezetimibe Kufanele Yenziwe Kuphi?
Ngokuqhelekileyo, ukusetyenziswa kwe-ezetimibe kufuneka kube nzima. Izikhokelo ezishicilelwe ngo-2013 nge-cholesterol azicebisi ukunyanga kwinqanaba le-cholesterol ethile. Kunoko, bagxila ekunqumeleni ukuba basebenzise i-statin drug okanye cha. Ngoko "izibilini" ze-cholesterol-ezinciphisa izidakamizwa ezifana ne-ezetimibe zinendawo encinane phantsi kwezi zikhokelo. Ngamanye amaxesha oogqirha banika i-ezetimibe kunye nemimiselo ephantsi-dose kubantu abafanele babe ngama-high-dose statins, kodwa abanako ukunyamezela iqondo eliphezulu.
Kwakhona, i-ezetimibe ngamanye amaxesha isetyenziselwa indawo esikhundleni seemimiselo kwizigulane ezingenakukwazi ukuthatha ama-statins kunoma yimuphi umthamo.
Ekugqibeleni, ngesiseko se-IMPROVE-IT, abaninzi abanomdla we-cardiologists babona kunengqondo ukusebenzisa i-ezetimibe kunye ne-statin kwizigulane zesifo sikashukela esine-ACS yakutshanje.
Ngaphandle kwezi meko ezimbalwa zeklinikhi, ngoku akukho sikhokelo esininzi sokuthatha i-ezetimibe.
> Imithombo:
> Cannon CP, Blazing MA, Giugliano RP, et al. I-Ezetimibe Yongezwe kwi-Statin Therapy emva kwe-Acon Coronary Syndromes. N Engl J Med 2015; 372: 2387.
> Kastelein JJ, Akdim F, Stroes ES et al .; Abaphandi: I-Simvastatin ene-Ezetimibe okanye engenayo i-Hypercholesterolemia. N. Engl. J. Med. 358, 1431-1443 (2008).