Ihe ọmụma
Ezetimibe ntụ ntụ bụ ọgwụ dị ike na-ebelata cholesterol nke enwetala nlebara anya dị ukwuu na mpaghara ahụike maka usoro ọrụ ya pụrụ iche. N'adịghị ka ọgwụ cholesterol ọdịnala nke na-elekwasị anya n'ibelata mmepụta cholesterol n'ime imeju, ezetimibe na-arụ ọrụ site n'ichebe nnabata nke eriri afọ nke cholesterol. Usoro ọhụrụ a emeela ka ọ bụrụ ngwá ọrụ dị mkpa na njikwa hypercholesterolemia, ọnọdụ nke ọkwa cholesterol dị elu n'ime ọbara mara.
Kedu ihe bụ isi usoro eji eme ihe maka ezetimibe na mbelata cholesterol?
Ezetimibe ntụ ntụ na-arụ ọrụ site na usoro dị iche iche nke na-ekewapụ ya na ọgwụ ndị ọzọ na-eweda cholesterol. Ebumnuche ya bụ Niemann-Pick C1-dị ka 1 (NPC1L1), nke na-arụ ọrụ dị mkpa na nnabata cholesterol na eriri afọ. Site na igbochi protein a, ezetimibe na-ebelata nke ọma cholesterol nke na-abanye n'ọbara site na isi nri nri na bile acid.
Usoro a na-amalite mgbe ezetimibe na-abanye n'ime eriri afọ ma nweta glucuronidation na imeju. Mgbanwe nke metabolic a na-eme ka ike ọgwụ ahụ nwee ike ijikọ na protein NPC1L1. Ozugbo agbụ, ezetimibe ntụ ntụ na-egbochi protein site n'ịkwado ibufe cholesterol gafee mgbidi eriri afọ. N'ihi ya, obere cholesterol na-abanye n'ọbara, na-eduga n'ibelata ọkwa cholesterol n'ozuzu ya.
Ọ dị mkpa ịmara na ezetimibe anaghị elekwasị anya naanị cholesterol nri. Ọgwụ ahụ na-emetụtakwa mweghachi nke cholesterol site na bile acid, nke imeju na-emepụta wee banye n'ime eriri afọ iji nyere aka na mgbaze abụba. Site n'ibelata mweghachi nke cholesterol a, ezetimibe na-enye aka na-ebelata ọkwa cholesterol n'ime ahụ.
Akụkụ ọzọ dị mkpa nke usoro ezetimibe bụ nhọrọ ọ na-eme na nnabata cholesterol. N'adịghị ka ọgwụ ndị ọzọ nwere ike imetụta nnabata nke nri dị iche iche, ezetimibe na-elekwasị anya cholesterol kpọmkwem na-enweghị mmetụta dị ukwuu na mmịnye vitamin ma ọ bụ triglycerides na-agbaze abụba. Nhọrọ a na-enye aka na profaịlụ nchekwa ya dị mma ma mee ka ọ bụrụ nhọrọ bara uru maka ndị ọrịa nwere ike ọ gaghị anabata ma ọ bụ meghachi omume nke ọma na ọgwụgwọ ndị ọzọ na-ebelata cholesterol.
Usoro pụrụ iche nke ezetimibe nwekwara mmetụta maka homeostasis cholesterol nke anụ ahụ. Ka ọgwụ ahụ na-ebelata nnabata cholesterol, imeju na-azaghachi site na ịkwalite okwu nnabata LDL. Mmụba a nke ndị na-anabata LDL na-eme ka ike imeju nwee ike iwepụ LDL cholesterol n'ọbara, na-atụnyekwu ụtụ na mkpokọta cholesterol na-ewetu ọgwụ ahụ.
Kedu ka ezetimibe si dị irè ma e jiri ya tụnyere ọgwụ ndị ọzọ na-ebelata cholesterol?
Mgbe a na-enyocha ịdị irè nke ezetimibe ntụ ntụ, ọ dị mkpa ịtụle arụmọrụ ya ma e jiri ya tụnyere ọgwụ ndị ọzọ na-ebelata cholesterol, karịsịa statins, nke a na-ewerekarị dị ka ọkọlọtọ ọla edo na njikwa lipid. Ọ bụ ezie na ezetimibe nwere ike ọ gaghị enwe ike dị ka statins dị elu na mbelata LDL cholesterol, ọ na-enye ọtụtụ uru na-eme ka ọ bụrụ nhọrọ dị mkpa na ngwa ngwa ọgwụ maka ijikwa hypercholesterolemia.
Nnyocha egosiwo na ezetimibe, mgbe ejiri ya dị ka monotherapy, nwere ike ibelata ọkwa LDL cholesterol site na ihe dịka 15-20%. Mbelata a, ọ bụ ezie na ọ dị ntakịrị ma e jiri ya tụnyere mbelata 30-50% nke a na-enwetakarị na statins, ka dị mkpa n'ụlọ ọgwụ maka ọtụtụ ndị ọrịa. Ọzọkwa, ịdị irè ezetimibe na-apụta ìhè nke ọma na ndị ọrịa na-enweghị statin ma ọ bụ ndị na-enwetabeghị ọkwa LDL ebumnuche ha site na iji ọgwụgwọ statin naanị.
Otu n'ime isi ike nke ezetimibe bụ usoro mmekọ ya na statins. Ọ bụ ezie na statins na-arụ ọrụ site na igbochi njikọ cholesterol n'ime imeju, ezetimibe na-elekwasị anya nnabata cholesterol n'ime eriri afọ. Ụzọ abụọ a maka njikwa cholesterol na-ebutekarị mmetụta synergistic mgbe ejiri ọgwụ abụọ ahụ mee ihe. Nnyocha egosila na ịgbakwụnye ezetimibe na ọgwụgwọ statin nwere ike inye mbelata 15-20% ọzọ na ọkwa LDL cholesterol, na-enye ohere ka ndị ọrịa nwee ike iru ebumnuche lipid ha lekwasịrị anya.
Ezetimibe na-egosipụtakwa nkwa na ọnụ ọgụgụ ndị ọrịa kpọmkwem ebe statins nwere ike ịnwe oke. Dịka ọmụmaatụ, n'ime ndị ọrịa nwere ọrịa akụrụ na-adịghị ala ala, ezetimibe egosila na ọ dị irè n'ibelata ọkwa LDL cholesterol na-enweghị mmetụta ndị nwere ike ime gbasara akụrụ metụtara na ọgwụgwọ statin dị elu. N'otu aka ahụ, n'ime ndị ọrịa nwere ọrịa mkpụrụ ndụ ihe nketa na-emetụta metabolism nke cholesterol, dị ka hypercholesterolemia ezinụlọ, ezetimibe nwere ike inyekwu uru na-ebelata cholesterol mgbe ejikọtara ya na usoro ọgwụgwọ.
Akụkụ ọzọ ị ga-atụle mgbe ị na-atụnyere ezetimibe na ọgwụ ndị ọzọ na-ebelata cholesterol bụ mmetụta ya na paramita lipid na-abụghị LDL. Ọ bụ ezie na mmetụta ezetimibe bụ isi na LDL cholesterol, ọmụmụ egosiwokwa mmụba dị ntakịrị na akara lipid ndị ọzọ. Dịka ọmụmaatụ, e jikọtara ezetimibe na ntakịrị mmụba na HDL cholesterol (cholesterol "ezigbo") yana mbelata nke triglycerides, na-enye aka na mmụba n'ozuzu na profaịlụ lipid.
Ọ dị mma ịmara na ịdị irè nke ezetimibe na-agafe karịa mmụba ọnụọgụgụ na ọkwa lipid. Ọmụmụ ihe dị ogologo oge, dị ka nnwale MMUTA-IT, egosila na mgbakwunye nke ezetimibe na ọgwụgwọ statin nwere ike ime ka mbelata ọzọ na ihe omume obi obi ma e jiri ya tụnyere ọgwụgwọ statin naanị. Nke a na-egosi na usoro ihe pụrụ iche ezetimibe si eme nwere ike inye uru nke obi karịa nke enwere ike ịkọwa site na mbelata LDL naanị.
Enwere ike iji ezetimibe jikọtara ya na statins maka nsonaazụ kacha mma?
The Nchikota ezetimibe ntụ ntụ na statins apụtala dị ka atụmatụ siri ike na njikwa hypercholesterolemia, ọkachasị maka ndị ọrịa na-enwetabeghị ọkwa lipid ebumnuche ha na ọgwụgwọ statin naanị. Usoro njikọ a na-eme ka usoro mmekọ nke ọgwụ abụọ ahụ na-emekọ ihe iji nye nkwalite cholesterol na-ebelata nrụpụta na nsonaazụ obi ka mma.
Ebumnuche dị n'azụ ijikọta ezetimibe na statins bụ n'ụdị omume ha dị iche ma nwee mmekọrịta. Statins na-arụ ọrụ nke ọma site n'igbochi HMG-CoA reductase, enzyme na-egbochi ọnụego cholesterol njikọ, si otú a na-ebelata mmepụta imeju nke cholesterol. N'aka nke ọzọ, Ezetimibe na-elekwasị anya n'ibelata cholesterol n'ime eriri afọ. Site n'ịgbasa ma mmepụta na nnabata nke cholesterol n'otu oge, ọgwụgwọ ngwakọta a na-enye ụzọ zuru oke maka njikwa lipid.
Ọmụmụ ụlọ ọgwụ egosila mgbe niile ịdị mma nke nchikota ezetimibe-statin ma e jiri ya tụnyere statin monotherapy. Nnwale ENHANCE, dịka ọmụmaatụ, gosiri na ịgbakwụnye ezetimibe na simvastatin butere mbelata nke ukwuu na ọkwa LDL cholesterol ma e jiri ya tụnyere simvastatin naanị. Na nkezi, ọgwụgwọ nchikota nyere mbelata 15-20% nke LDL cholesterol karịa ihe enwetara na ọgwụgwọ statin. Mmetụta mgbakwunye a bara uru karịsịa maka ndị ọrịa na-erubeghị ebumnuche LDL ha n'agbanyeghị doses statin anabatara nke ukwuu.
Ọzọkwa, nchikota ezetimibe-statin egosila uru karịa iwetulata lipid nkịtị. Nnwale a na-eme ka ọ dị mma gosipụtara na mgbakwunye ezetimibe na simvastatin na ndị ọrịa nwere nnukwu ọrịa obi na nso nso a ọ bụghị naanị na profaịlụ lipid ka mma kamakwa belata ohere nke ihe omume obi. Ọmụmụ ihe a nyere ihe akaebe dị mkpa na iwetuwanye LDL cholesterol site na mgbakwunye ezetimibe na-asụgharị n'ime uru ụlọ ọgwụ, na-akwado echiche "dị ala ka mma" na njikwa cholesterol.
Usoro ọgwụgwọ ngwakọta na-enyekwa uru n'ihe gbasara mgbanwe dosing na njikwa mmetụta. Maka ndị ọrịa nwere mmetụta dị n'akụkụ ya na ọgwụgwọ statin dị elu, mgbakwunye ezetimibe na-enye ohere maka mbelata LDL nha ma ọ bụ karịa mgbe ị na-eji obere statin dose. Usoro a nwere ike ịba uru karịsịa maka ndị ọrịa na-enwekarị mgbaàmà nke muscle statin ma ọ bụ ndị nwere mmetụta ndị ọzọ metụtara statin.
Ọzọkwa, nchikota ezetimibe-statin egosila nkwa n'ime ụfọdụ ndị ọrịa. N'ime ndị ọrịa nwere hypercholesterolemia ezinụlọ, ọrịa mkpụrụ ndụ ihe nketa nke ọkwa cholesterol dị oke elu, usoro ọgwụgwọ njikọta nwere ike inye mbelata LDL agbakwunyere mgbe ọgwụgwọ statin dị elu ezughị oke. N'otu aka ahụ, na ndị ọrịa nwere ọrịa akụrụ na-adịghị ala ala ma ọ bụ ọrịa shuga, ebe iwetulata egbugbere ọnụ ike na-adịkarị mkpa, ụzọ nchikota nwere ike inye aka nweta ọkwa lipid lekwasịrị anya nke ọma.
Ọ dị mkpa ịmara na ọ bụ ezie na a na-anabatakarị ngwakọta ezetimibe-statin nke ọma, a ga-enyocha ndị ọrịa maka mmetụta ndị nwere ike ime. Ọ bụ ezie na ọ dị ụkọ, nchikota nwere ike ịbawanye ohere nke ụfọdụ mmetụta ndị metụtara statin. Agbanyeghị, profaịlụ nchekwa n'ozuzu nke usoro ọgwụgwọ nchikota ka na-adị mma, ọkachasị mgbe a tụlere ya megide oke iwetulata lipid na uru obi ya.
Na ngwụcha, Ezetimibe ntụ ntụ na-anọchite anya ọganihu dị ukwuu na ngalaba njikwa cholesterol. Usoro ọrụ ya pụrụ iche, nke na-ezubere mbanye cholesterol n'ime eriri afọ, na-enye usoro nkwado maka atụmatụ iweda cholesterol ọdịnala. Ọ bụ ezie na ezetimibe nwere ike ọ gaghị enwe ike dị ka statins dị elu mgbe ejiri ya naanị ya, ezigbo uru ya dabere na ikike ya ịkwalite nrụpụta ọgwụgwọ statin na-enye ihe ọzọ maka ndị ọrịa na-adịghị anabata statin.
Ịdị irè nke ezetimibe, ma dị ka monotherapy yana yana statins, edepụtala nke ọma n'ọtụtụ ule ụlọ ọgwụ. Ikike ya inyekwu mbelata cholesterol LDL, melite profaịlụ lipid n'ozuzu ya, na itinye aka na mbelata ihe egwu obi na-eme ka ọ bụrụ ngwa bara uru na njikwa hypercholesterolemia.
Ka nghọta anyị banyere metabolism lipid na ọrịa obi na-aga n'ihu, ọrụ ezetimibe na njikwa cholesterol nwere ike gbasaa. Usoro ya pụrụ iche nke omume, profaịlụ nchekwa dị mma, yana arụmọrụ egosipụtara na ọgwụgwọ ngwakọta na-etinye ya dị ka onye bụ isi na mbọ a na-aga n'ihu iji belata ibu ọrịa obi n'ụwa niile.
Ọ bụrụ na ị nwekwara mmasị na ngwaahịa a ma chọọ ịmatakwu nkọwa ngwaahịa, ma ọ bụ chọọ ịmata maka ngwaahịa ndị ọzọ metụtara, biko nweere onwe gị ịkpọtụrụ. iceyqiang@aliyun.com.
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