I-Rosuvastatin (igama le-brand Crestor, elithengiswa yi-AstraZeneca) yenye yezona ziyobisi zisetyenziswa ngokuqhelekileyo.Njengamanye ama-statins, i-rosuvastatin imiselwe ukuphucula amanqanaba e-lipid yegazi kunye nokunciphisa umngcipheko we-cardiovascular.
Ngexesha leshumi leminyaka okanye ngoko ke i-rosuvastatin yayikwimarike, yayichazwa ngokubanzi njenge "statin yesizukulwana sesithathu," kwaye ngenxa yoko isebenza ngakumbi kwaye inokubangela iziphumo ezibi ezimbalwa kunezinye iziyobisi ezininzi.Njengoko iminyaka ihambile kwaye njengoko ubungqina obuvela kulingo lwezonyango buye baqokelelana, uninzi lomdla wokuqala wale statin ithile iye yamodareyithwa.
Uninzi lweengcali ngoku zithathela ingqalelo imingcipheko enxulumeneyo kunye neenzuzo zerosuvastatin ukuba zifane kakhulu nezo zezinye iistatins.Nangona kunjalo, kukho iimeko ezimbalwa zeklinikhi apho i-rosuvastatin inokukhethwa khona.
Ukusetyenziswa kweRosuvastatin
Iziyobisi ze-statin zenzelwe ukunciphisa i-cholesterol yegazi.La machiza abopha ngokukhuphisanayo kwi-enzyme yesibindi ebizwa ngokuba yi-hydroxymethylglutaryl (HMG) CoA reductase.I-HMG CoA reductase idlala indima yokunciphisa izinga kwi-synthesis ye-cholesterol ngesibindi.
Ngokuthintela i-HMG CoA reductase, i-statins inokunciphisa kakhulu i-LDL ("embi") imveliso ye-cholesterol esibindini, kwaye ngoko inokunciphisa amanqanaba egazi le-LDL ye-cholesterol malunga ne-60%.Ukongezelela, i-statins iyancipha ngokuthobekileyo amanqanaba e-triglyceride yegazi (malunga ne-20-40%), kwaye ivelise ukunyuka okuncinci (malunga ne-5%) kumanqanaba egazi le-HDL cholesterol ("i-cholesterol enhle").
Ngaphandle kwee-PCSK9 inhibitors ezisanda kuphuhliswa, i-statins ngawona machiza anamandla okunciphisa i-cholesterol akhoyo.Ukongezelela, ngokungafaniyo nezinye iiklasi zeziyobisi ezinciphisa i-cholesterol, izilingo zeklinikhi ziye zabonisa ukuba iziyobisi ze-statin zinokuphucula kakhulu iziphumo zexesha elide zabantu abane-coronary artery disease (CAD), kunye nabantu abasengozini enkulu okanye ephezulu yokuphuhlisa iCAD. .
Kwakhona iiStatins ziwunciphisa ngokuphawulekayo umngcipheko wokuhlaselwa yintliziyo okulandelayo, yaye zinciphisa umngcipheko wokufa ngenxa yeCAD.(I-PCSK9 inhibitors entsha nayo ngoku iboniswe kwii-RCT ezinkulu zokuphucula iziphumo zekliniki.)
Esi sikhundla se-statins sokuphucula kakhulu iziphumo zeklinikhi kucingelwa ukuba sisiphumo, ubuncinci ngokuyinxenye, kwezinye okanye kuzo zonke izibonelelo zabo ezingezizo i-cholesterol-ehlisa.Ukongeza ekunciphiseni i-cholesterol ye-LDL, i-statins nayo inezixhobo ezichasayo, i-anti-blood clotting effects, kunye ne-plaque-stabilizing properties.Ngaphezu koko, la mayeza anciphisa amanqanaba eprotheyini e-C-reactive, aphucule umsebenzi we-vascular, kwaye anciphise umngcipheko we-arrhythmias ye-cardiac esongela ubomi.
Kunokwenzeka ukuba izibonelelo zeklinikhi ezibonakaliswe ngamachiza e-statin zibangelwa yindibaniselwano yeziphumo zabo zokunciphisa i-cholesterol kunye neentlobo zazo ezahlukeneyo zemiphumo engeyiyo i-cholesterol.
Yahluke njani iRosuvastatin?
I-Rosuvastatin liyeza elitsha, elibizwa ngokuba "kwisizukulwana sesithathu" ichiza le-statin.Ngokusisiseko, lelona chiza linamandla le-statin kwimarike.
Amandla ayo ahambelanayo avela kwiimpawu zayo zeekhemikhali, ezivumela ukuba zibophe ngokuthe gqolo kwi-HMG CoA reductase, ngaloo ndlela isebenze inhibition epheleleyo ngakumbi yale enzyme.I-molecule ye-molecule, i-rosuvastatin ivelisa i-LDL-cholesterol-ehlisa ngaphezu kwamanye amachiza e-statin.Nangona kunjalo, ubukhulu obufanayo bokwehliswa kwe-cholesterol bunokufezekiswa ngokusebenzisa iidosi eziphezulu zezinye i-statins.
Xa unyango lwe-statin "olunzulu" lufuneka ukutyhala amanqanaba e-cholesterol asezantsi kangangoko, i-rosuvastatin liyeza lokuya koogqirha abaninzi.
Ukusebenza kweRosuvastatin
I-Rosuvastatin ifumene udumo lokusebenza ngokukodwa phakathi kwamachiza e-statin, ngokukodwa ngokusekelwe kwiziphumo zolingo lwezonyango ezimbini.
Kwi-2008, upapasho lophononongo lweJUPITER lwafumana ingqalelo yee-cardiologists kuyo yonke indawo.Kulo pho nonongo, abantu abangaphezu kwe-17,000 abanempilo abanamaqondo aqhelekileyo e-LDL yegazi le-cholesterol kodwa amanqanaba aphezulu e-CRP ayenziwa ngokungaqhelekanga ukufumana i-20 mg ngosuku lwe-rosuvastatin okanye i-placebo.
Ngethuba lokulandelwa, abantu abakhethiweyo kwi-rosuvastatin abazange banciphise kakhulu amanqanaba e-cholesterol ye-LDL kunye namanqanaba e-CRP, kodwa nabo babeneziganeko ezincinci ze-cardiovascular (kubandakanywa nesifo senhliziyo, ukubetha, imfuno yenkqubo ye-revascularization efana ne-stent okanye utyando lwe-bypass, kunye nokudityaniswa kokuhlaselwa yintliziyo, okanye ukufa kwentliziyo), kunye nokuncipha kokusweleka kwezinto zonke.
Olu pho nonongo lwaluphawuleka kungekuphela nje ngenxa yokuba i-rosuvastatin iphucule kakhulu iziphumo zeklinikhi kubantu ababonakala besempilweni, kodwa nangenxa yokuba aba bantu babengenawo amanqanaba aphezulu e-cholesterol ngexesha lokubhalisa.
Ngo-2016, ulingo lwe-HOPE-3 lwapapashwa.Olu phononongo lubhalise abantu abangaphezu kwe-12,000 ubuncinane umngcipheko omnye we-atherosclerotic vascular disease, kodwa akukho CAD engaphezulu.Abathathi-nxaxheba bahlelwe ukuba bafumane i-rosuvastatin okanye i-placebo.Ekupheleni konyaka, abantu abathatha i-rosuvastatin baye bancipha kakhulu kwisiphumo sesiphumo esihlanganisiweyo (kubandakanya ukuhlaselwa kwentliziyo okungapheliyo okanye ukubetha, okanye ukufa ngenxa yesifo senhliziyo).
Kuzo zombini ezi zilingo, i-randomization kwi-rosuvastatin iphucule kakhulu iziphumo zeklinikhi zabantu abanomngcipheko omnye okanye ngaphezulu, kodwa akukho zimpawu zesifo senhliziyo esisebenzayo.
Kufuneka kuqatshelwe ukuba i-rosuvastatin ikhethwe kwezi zilingo kungekhona ngenxa yokuba yayiyeyona nto inamandla yezidakamizwa ze-statin, kodwa (ubuncinci inxalenye enkulu) kuba iimvavanyo zaxhaswa ngu-AstraZeneca, umenzi we-rosuvastatin.
Uninzi lweengcali ze-lipid zikholelwa ukuba iziphumo zolu vavanyo beziya kuba ziyafana ukuba enye i-statin isetyenziswe kwidosi eyaneleyo, kwaye eneneni, iingcebiso zangoku kunyango ngamachiza e-statin ngokubanzi zivumela ukusetyenziswa kwazo naziphi na iziyobisi ze-statin ukuba nje Idosi iphezulu ngokwaneleyo ukufikelela kwinqanaba elifanayo le-cholesterol-ukwehlisa njengoko bekuya kuphunyezwa ngedosi esezantsi ye-rosuvastatin.(Imeko engafaniyo nalo mgaqo jikelele wenzeka xa “unyango lwe-statin olunzima” lubizwa. Unyango olunzulu lwe-statin luqondwa njenge-dose ephezulu ye-rosuvastatin okanye idosi ephezulu ye-atorvastatin, eyona statin ilandelayo inamandla akhoyo.)
Kodwa ngenxa yokuba i-rosuvastatin yayiyeyona nto yayisetyenziswa kolu lingo mbini lubalulekileyo lwezonyango, oogqirha abaninzi baye basilela ekusebenziseni i-rosuvastatin njengestatin yabo yokuzikhethela.
Iimpawu zangoku
Unyango lwe-Statin luboniswa ukuphucula amanqanaba egazi e-lipid engaqhelekanga (ngokukodwa, ukunciphisa i-cholesterol ye-LDL kunye / okanye amanqanaba e-triglyceride), kunye nokukhusela isifo senhliziyo.I-Statins icetyiswa kubantu abanesifo se-atherosclerotic ye-cardiovascular disease, abantu abanesifo seswekile, kunye nabantu abaqikelelwa ukuba umngcipheko we-10 wokufumana isifo senhliziyo ungaphezulu kwe-7.5 ukuya kwi-10%.
Ngelixa, ngokubanzi, iziyobisi ze-statin zithathwa njengokutshintshana ngokuhambelana nokusebenza kwazo kunye nomngcipheko wokubangela iziganeko ezimbi, kunokubakho amaxesha apho i-rosuvastatin inokukhethwa khona.Ngokukodwa, xa unyango lwe-statin "oluphezulu" lujoliswe ekunciphiseni i-cholesterol ye-LDL ukuya kumanqanaba aphantsi kunokwenzeka, mhlawumbi i-rosuvastatin okanye i-atorvastatin kwiindidi zabo eziphezulu zedosi ziyacetyiswa ngokubanzi.
Ngaphambi kokuthatha
Ngaphambi kokuba umiselwe nayiphi na iziyobisi ze-statin, ugqirha wakho uya kuqhuba uvavanyo lomngcipheko olusemthethweni ukuqikelela umngcipheko wakho wokuphuhlisa isifo senhliziyo kwaye uya kulinganisa amanqanaba egazi lakho.Ukuba sele unesifo se-cardiovascular disease okanye usemngciphekweni omkhulu wokusiphuhlisa, ugqirha wakho uya kuncomela ichiza le-statin.
Amanye amayeza e-statin amiselweyo abandakanya i-atorvastatin, i-simvastatin, i-fluvastatin, i-lovastatin, i-pitavastatin, kunye ne-pravastatin.
I-Crestor, uhlobo lwegama lebrand ye-rosuvastatin e-US, lubiza kakhulu, kodwa iindlela eziqhelekileyo ze-rosuvastatin ngoku ziyafumaneka.Ukuba ugqirha wakho ufuna ukuba uthathe i-rosuvastatin, cela ukuba ungayisebenzisa na igeneric.
I-Statins akufuneki isetyenziswe kubantu abachasene ne-statins okanye naziphi na izithako zabo, abakhulelweyo okanye abancancisayo, abanesifo sesibindi okanye ukusilela kwezintso, okanye abasela utywala ngokugqithisileyo.Uphononongo lubonisa ukuba i-rosuvastatin inokusetyenziswa ngokukhuselekileyo kubantwana abangaphezu kweminyaka eyi-10 ubudala.
Umthamo weRosuvastatin
Xa i-rosuvastatin isetyenziselwa ukunciphisa amanqanaba e-cholesterol e-LDL ephakamileyo, ngokuqhelekileyo i-dose ephantsi iqalwa (5 ukuya kwi-10 mg ngosuku) kwaye ihlengahlengiswa phezulu ngenyanga okanye ezimbini njengoko kuyimfuneko.Kubantu abane-hypercholesterolemia yosapho, oogqirha bahlala beqala ngeedosi eziphezulu (10 ukuya kwi-20 mg ngosuku).
Xa i-rosuvastatin isetyenziselwa ukunciphisa umngcipheko wesifo senhliziyo kubantu abanomngcipheko ophezulu ophakamileyo, idosi yokuqala idla ngokuba yi-5 ukuya kwi-10 mg ngosuku.Kubantu abanomngcipheko obhekwa njengophakamileyo (ngokukodwa, umngcipheko we-10 iminyaka uqikelelwa ukuba ungaphezulu kwe-7.5%), unyango oluphezulu luhlala luqalwa, kunye ne-20 ukuya kwi-40 mg ngosuku.
Ukuba i-rosuvastatin isetyenziselwa ukunciphisa umngcipheko weziganeko ezongezelelweyo ze-cardiovascular kumntu osele esungulwe isifo se-cardiovascular disease, unyango olunzulu ludla ngokusetyenziswa umthamo we-20 ukuya kwi-40 mg ngosuku.
Kubantu abathatha i-cyclosporine okanye iziyobisi ze-HIV / AIDS, okanye kubantu abanokunciphisa umsebenzi wezintso, umthamo we-rosuvastatin kufuneka ulungelelaniswe phantsi, kwaye ngokuqhelekileyo akufanele udlule i-10 mg ngosuku.
Abantu bomnombo wase-Asiya bathanda ukuba novelwano ngakumbi kumachiza e-statin kwaye bathambekele ngakumbi kwiziphumo ebezingalindelekanga.Ngokuqhelekileyo kucetyiswa ukuba i-rosuvastatin iqaliswe kwi-5 mg ngosuku kwaye inyuswe ngokuthe ngcembe kwizigulane zase-Asia.
I-Rosuvastatin ithathwa kanye ngosuku, kwaye inokuthatyathwa nokuba kusasa okanye ebusuku.Ngokungafaniyo namanye amachiza e-statin, ukusela izixa ezithobekileyo zejusi yegrapefruit kunempembelelo encinci kwi-rosuvastatin.
Iziphumo ebezingalindelekanga zeRosuvastatin
Kwiminyaka ngokukhawuleza emva kokuba i-rosuvastatin iphuhlisiwe, iingcali ezininzi zachaza ukuba iziphumo zecala ze-statin ziya kuchazwa kancinci nge-rosuvastatin, ngenxa yokuba iidosi eziphantsi zingasetyenziselwa ukufezekisa ukunciphisa okwaneleyo kwe-cholesterol.Kwangelo xesha, ezinye iingcali zabanga ukuba iziphumo ebezingalindelekanga ze-statin ziyakukhuliswa ngeli chiza, kuba lalinamandla ngakumbi kunezinye iistatins.
Kwiminyaka engenelelayo, kuye kwacaca ukuba akukho nto ithethwayo ibichanekile.Kubonakala ngathi uhlobo kunye nobukhulu beziphumo ezibi ngokuqhelekileyo zifana ne-rosuvastatin njengoko kunjalo namanye amachiza e-statin.
I-Statins, njengeqela, inyamezeleke ngakumbi kunezinye iziyobisi zokunciphisa i-cholesterol.Kwi-meta-analysis epapashwe ngo-2017 ejonge izilingo zeklinikhi ezingama-22, kuphela i-13.3% yabantu abadityanisiweyo kwiyeza le-statin baye bayeka ichiza ngenxa yemiphumo emibi kwiminyaka eyi-4, xa kuthelekiswa ne-13.9% yabantu abangahleliwe kwi-placebo.
Sekunjalo, kukho iziphumo ezibi ezaziwayo ezibangelwa ngamachiza e-statin, kwaye ezi ziphumo bezingalindelekanga zisebenza ngokubanzi kwi-rosuvastatin kunye nayo nayiphi na enye i-statin.Ezona ziphawuleka kakhulu kwezi ziphumo bezingalindelekanga ziquka:
- Iziganeko ezimbi ezinxulumene nezihlunu.Ubuthi bemisipha bunokubangelwa ngama-statins.Iimpawu zingabandakanya i-myalgia (intlungu yemisipha), ubuthathaka bemisipha, ukuvuvukala kwemisipha, okanye (kwiimeko ezinqabileyo, ezinzima) i-rhabdomyolysls.I-Rhabdomyolysis kukusilela okubukhali kwezintso okubangelwa kukuqhekeka okukhulu kwemisipha.Kwiimeko ezininzi.Iziphumo zecala ezinxulumene nemisipha zinokulawulwa ngokutshintshela kwenye i-statin.I-Rosuvastatin iphakathi kwamachiza e-statin abonakala ebangela ubuthi obuncinci bezihlunu.Ngokwahlukileyo, i-lovastatin, i-simvastatin, kunye ne-atorvastatin zivame ukubangela iingxaki zemisipha.
- Iingxaki zesibindi.Ngokumalunga ne-3% yabantu abathatha i-statins baya kuba nokwanda kwee-enzyme zesibindi egazini labo.Kuninzi lwaba bantu, akukho bungqina bomonakalo wesibindi obonakalayo, kwaye ukubaluleka kokunyuka kuncinci kwi-enzymes akucaci.Kubantu abambalwa kakhulu, ukulimala okukhulu kwesibindi kuye kwabikwa;akucaci, nangona kunjalo, ukuba iziganeko zokulimala kakhulu kwesibindi ziphezulu kubantu abathatha i-statins kunabantu bonke.Akukho nto ibonisa ukuba i-rosuvastatin ivelisa imiba yesibindi engaphezulu okanye encinci kunezinye ii-statins.
- Ukuphazamiseka kwengqondo.Ingcamango yokuba i-statins inokubangela ukuphazamiseka kwengqondo, ukulahlekelwa kwememori, ukudandatheka, ukucaphuka, ubundlobongela, okanye ezinye iziphumo zenkqubo ye-nervous ziye zaphakanyiswa, kodwa ayizange iboniswe ngokucacileyo.Kuhlalutyo lweengxelo zetyala ezithunyelwe kwi-FDA, iingxaki ezityholayo zengqondo ezinxulumene ne-statins zibonakala zixhaphake kakhulu kunye neziyobisi ze-lipophilic statin, kubandakanya i-atorvastatin, i-fluvastatin, i-lovastatin, kunye ne-simvastatin.Iziyobisi ze-hydrophilic statin, kubandakanywa ne-rosuvastatin, ziye zachaphazeleka ngokuphindaphindiweyo kwesi siganeko esibi.
- Isifo seswekile.Kwiminyaka yakutshanje, ukunyuka okuncinci kuphuhliso lweswekile kuye kwadityaniswa nonyango lwe-statin.Uhlalutyo lwe-meta luka-2011 lwezilingo ezintlanu zeklinikhi lubonisa ukuba enye imeko eyongezelelweyo yesifo seswekile yenzeka kubo bonke abantu abangama-500 abaphathwa ngama-statins aphezulu.Ngokubanzi, eli nqanaba lomngcipheko lithathwa njengelamkelekileyo ukuba nje i-statin inokulindeleka ukuba inciphise kakhulu umngcipheko wentliziyo.
Ezinye iziphumo ebezingalindelekanga eziye zaxelwa ngokuqhelekileyo ngamachiza e-statin zibandakanya isicaphucaphu, urhudo, kunye neentlungu ezidibeneyo.
Ukusebenzisana
Ukuthatha iziyobisi ezithile kunokunyusa umngcipheko wokuphuhlisa imiphumo emibi kunye ne-rosuvastatin (okanye nayiphi na i-statin).Olu luhlu lude, kodwa awona machiza abonakalayo asebenzisana ne-rosuvastatin abandakanya:
- I-Gemfibrozil, eyi-agent ye-non-statin-cholesterol-ehlisa
- I-Amiodarone, elichiza lokuchasana ne-arrhythmic
- Uninzi lwamachiza e-HIV
- Ezinye ii-antibiotics, ngakumbi i-clarithromycin kunye ne-itraconazone
- Cyclosporine, ichiza immunosuppressant
Ilizwi elivela Wellwell
Ngelixa i-rosuvastatin yeyona statin inamandla ekhoyo, ngokubanzi, ukusebenza kwayo kunye neprofayili yetyhefu ifana kakhulu nazo zonke ezinye iistatins.Nangona kunjalo, kukho iimeko ezimbalwa zeklinikhi apho i-rosuvastatin inokukhethwa ngaphezu kwamanye amachiza e-statin.
Ixesha lokuposa: Mar-12-2021