I-Ezetimibe yisidakamizwa esinciphisa amazinga e-cholesterol . Kuye kwaba yi-FDA evunyelwe kusukela ngo-2002, futhi ithengiswa njengesidakamizwa esimele (i-Zeta) ngokuhambisana nesimvastatin (isidakamizwa se- statin ) njengoVivinin. Kodwa-ke, i-ezetimibe ibilokhu iphikisana kakhulu kusukela isingeniso sayo, futhi ochwepheshe basaphikisana ngokuthi indawo yaso efanelekile ekwelapheni izifo ze-lipid.
Ezetimibe
I-Ezetimibe isebenza ngokuvimbela ukumuncwa kwe-cholesterol emathunjini.
Ngokuvamile, i-cholesterol yanyuka emathunjini ithathwa ngama-chylomicrons esibindi, lapho isetshenziselwa izinqubo ezimbalwa ezibalulekile. Lapho inani le-cholesterol elithintekayo liyancishiswa yi-ezetimibe, isibindi kufanele sithole ukutholakala kwe-cholesterol ngokuyisusa kuma- lipoproteins ajikeleza egazini. Ngakho, amazinga wegazi we-cholesterol ancipha.
Ngokuvamile, i-ezetimibe mhlawumbe noma ihlanganiswe nesimiso sincipha inani le- LDL cholesterol egazini cishe ngo-15%.
Imiphumela emibi ye-Ezetimibe
Ngokuvamile, i-ezetimibe ibekezelela kahle. I-nausea, isifo sohudo, kanye nokuphendula okwenziwe ukugula kungase kwenzeke. Ngenkathi i-myopathy (imizimba emibi yemisipha) ibikwa nge-ezetimibe, efana ne-myopathy ebonwe ngezithombe , izimo zalesi nkinga zibonakala ziphansi kakhulu kunama-statins. Eqinisweni, i-ezetimibe ingafakwa kwisimiso se-dose esincane ukuze kutholakale ukunciphisa kwe-cholesterol okungafunwa ngaphandle kwe-myopathy ngezinye izikhathi kuboniswe ngezithombe eziphezulu.
Ukungqubuzana Ne-Ezetimibe
Ngesikhathi i-ezetimibe ivunyelwa okokuqala, yayithengiswa kakhulu njengeVitoin (i-ezetimibe ne-simvastatin), futhi ukuthengiswa kwakunzima. Ungase ukhumbule izimakethe eziningi ngesikhathi ufanisa umama wakho omnandi, u-rotund u-Suzie esiqenjini esikhulu sokwephuza isitrobheli i-mode. Lokho kwakunguVytorin.
Kuvela ukuthi, ngenkathi lezo zentengiso zigijima kanti ngenkathi uMerck ethengisa izigidigidi zamaRandi aseVytorin, ukushicilelwa kwakubekwe ukubambezeleka (okusobala, abanye bathi) kwesilingo somtholampilo esixhaswe nguMerck esibizwa ngokuthi isifundo se-ENHANCE. I-ENHANCE yayihlose ukufakazela ukuthi iVivtorin ithuthukise ama- atherosclerotic plaques ngaphezu kwe-simvastatin yedwa. Lapho ekugcineni kukhishwa imiphumela ngo-2008, kwafundwa ukuthi abantu abaphathwa ngeVivtorin benza okubi kakhulu (hhayi okungcono) kunelabo abathola i-simvastatin kuphela.
Ngenxa yale miphumela emibi (futhi iqiniso lokuthi abaningi babhekene nokulibaziseka ekubikeni lezo miphumela okungenani ngokungabonakali), ukuthengisa kwe-ezetimibe tanked. Futhi izimakethe zanyamalala ngokuphelele.
Intshisekelo ku-ezetimibe iye yavuselela kusukela ngo-2014, lapho imiphumela ye-IMPROVE-IT ishicilelwe. Kulesi sivivinyo, iziguli ezine -coronary syndrome (ACS) ezinzima zenzelwe ukuthola i-Vytorin noma i-simvastatin yodwa. Ngemuva kweminyaka engama-6, iziguli ezithola iVittorin zazithuthukisa ngokuthobeka imiphumela yomtholampilo (ukufundwa okumbalwa kwe-ACS, nesidingo esincane sokuhlinzwa okudlulayo noma ama-stents ), kodwa kwakungekho umehluko ekusindeni.
Ukuhlaziywa kwamagqabha we-IMPROVE-Ukuhlolwa kwaphakamisa ukuthi cishe yonke inzuzo ebonwe eqenjini leVavtorin lingabalwa yiziguli ezine-sikashukela.
Kubantu abangenayo isifo sikashukela, akukho nzuzo ekungezeni i-ezetimibe ingaboniswa.
U-Ezetimibe Kufanele Usetshenziswe Nini?
Ngokuvamile, ukusebenzisa i-ezetimibe kufanele kube mncane kakhulu. Imihlahlandlela eyashicilelwe ngo-2013 nge-cholesterol ayincoma ukuphatha kunoma yikuphi izinga le-cholesterol elibhekiswe kulo. Kunalokho, bagxila ekunqumeni ukuthi ngabe basebenzise izidakamizwa zesimiso noma cha. Ngakho-ke izidakamizwa ezinciphisa i-cholesterol ezinjenge-ezetimibe zinendawo encane ngaphansi kwale mihlahlandlela. Ngesinye isikhathi odokotela banikeza i-ezetimibe kanye nesimiso esincane sezitho zomuntu kubantu okufanele babe sezitho zomzimba eziphezulu, kodwa abakwazi ukubekezelela umthamo ophezulu.
Futhi, i-ezetimibe ngezinye izikhathi isetshenziselwa esikhundleni sezimiso ezigulini ezingenakukwazi ukuthatha izitho zomzimba nganoma yisiphi isisindo.
Okokugcina, ngesisekelo socwaningo lwe-IMPROVE-IT, abaningi be-cardiologists babheka ukuthi kunengqondo ukusebenzisa i-ezetimibe kanye nesimiso esiphethwe iziguli zesifo sikashukela esine-ACS yakamuva.
Ngaphandle kwezimo ezimbalwa zemitholampilo, okwamanje asikho isizathu esiningi sokuthatha i-ezetimibe.
> Imithombo:
> Cannon CP, Blazing MA, Giugliano RP, et al. I-Ezetimibe Yengezwe ku-Statin Therapy emva kwe-Acute Coronary Syndromes. N Engl J Med 2015; 372: 2387.
> Kastelein JJ, Akdim F, Stroes ES et al .; Abahloli: I-Simvastatin ene-Ezetimibe noma engenayo e-Hypercholesterolemia ejwayelekile. N. Engl. J. Med. 358, 1431-1443 (2008).