I-Rosuvastatin (igama lomkhiqizo i-Crestor, emakethe yi-AstraZeneca) ingenye yezidakamizwa ezivame ukusetshenziswa kakhulu.Njengamanye ama-statins, i-rosuvastatin inqunyelwe ukuthuthukisa amazinga e-lipid egazi lomuntu kanye nokunciphisa ingozi yenhliziyo nemithambo yegazi.

Phakathi neminyaka eyishumi yokuqala noma ngaphezulu lapho i-rosuvastatin yayisemakethe, yayaziwa kabanzi ngokuthi "i-statin yesizukulwane sesithathu," futhi yingakho iphumelela kakhulu futhi okungenzeka ibangele imiphumela emibi embalwa kunezinye izidakamizwa eziningi.Njengoba iminyaka isihambile futhi njengobufakazi obuvela ezivivinyweni zomtholampilo buye banqwabelana, isasasa elikhulu lale statin ethize liye lancishiswa.

Ochwepheshe abaningi manje babheka ubungozi obuhlobene kanye nezinzuzo ze-rosuvastatin njengokufana kakhulu nezamanye ama-statins.Kodwa-ke, kunezimo ezimbalwa zomtholampilo lapho i-rosuvastatin ingakhethwa khona.

Ukusetshenziswa kwe-rosuvastatin

Izidakamizwa ze-statin zenzelwe ukunciphisa i-cholesterol yegazi.Le mithi ibophezela ngokuncintisana kwi-enzyme yesibindi ebizwa ngokuthi i-hydroxymethylglutaryl (HMG) CoA reductase.I-HMG CoA reductase idlala indima yokukhawulela izinga ekuhlanganiseni kwe-cholesterol yisibindi.

Ngokuvimbela i-HMG CoA reductase, ama-statins anganciphisa kakhulu ukukhiqizwa kwe-cholesterol ye-LDL (“embi”) esibindini, futhi ngaleyo ndlela anganciphisa amazinga e-cholesterol e-LDL egazini ngendlela efinyelela ku-60%.Ngaphezu kwalokho, ama-statins ehlisa ngokuzithoba amazinga e-triglyceride egazi (cishe ngo-20-40%), futhi akhiqize ukwanda okuncane (cishe ngo-5%) emazingeni egazi we-HDL cholesterol ("i-cholesterol enhle").

Ngaphandle kwama-PCSK9 inhibitors asanda kwakhiwa, ama-statins ayimithi enamandla kakhulu yokunciphisa i-cholesterol etholakalayo.Ngaphezu kwalokho, ngokungafani namanye amakilasi ezidakamizwa ezinciphisa i-cholesterol, ukuhlolwa kwemitholampilo kuye kwabonisa ukuthi izidakamizwa ze-statin zingathuthukisa kakhulu imiphumela yesikhathi eside yabantu abane-coronary artery disease (CAD), kanye nabantu abasengozini elinganiselwe noma ephezulu yokuthuthukisa i-CAD. .

Ama-statin anciphisa ngokuphawulekayo ingozi yokuhlaselwa yinhliziyo okulandelayo, futhi anciphise ingozi yokufa ngenxa ye-CAD.(Ama-PCSK9 inhibitor amasha nawo manje asebonisiwe kuma-RCT amakhulu ukuze kuthuthukiswe imiphumela yomtholampilo.)

Leli khono lama-statins okuthuthukisa kakhulu imiphumela yomtholampilo kucatshangwa ukuthi liphumela, okungenani ngokwengxenye, kwezinye noma zonke izinzuzo zawo ezingeyona i-cholesterol.Ngaphezu kokunciphisa i-cholesterol ye-LDL, ama-statins anezindawo zokulwa nokuvuvukala, imiphumela elwa nokujiya kwegazi, kanye nezakhiwo zokuzinzisa ama-plaque.Ngaphezu kwalokho, le mithi inciphisa amazinga amaprotheni e-C-reactive, ithuthukise ukusebenza kwemithambo yonke, futhi inciphise ingozi ye-arrhythmia yenhliziyo esongela ukuphila.

Kungenzeka kakhulu ukuthi izinzuzo zomtholampilo eziboniswa yizidakamizwa ze-statin zibangelwa inhlanganisela yemiphumela yazo yokwehlisa i-cholesterol kanye nezinhlobonhlobo zazo zemiphumela engeyona i-cholesterol.

Ihluke kanjani i-Rosuvastatin?

I-Rosuvastatin iyisidakamizwa esisha, esibizwa ngokuthi "isizukulwane sesithathu" sezidakamizwa.Empeleni, umuthi wama-statin onamandla kakhulu emakethe.

Amandla ayo ahlobene atholakala ezicini zayo zamakhemikhali, eziyivumela ukuthi ibophe iqine kakhudlwana ku-HMG CoA reductase, ngaleyo ndlela ibangele ukuvinjelwa okuphelele kwale enzyme.I-molecule ye-molecule, i-rosuvastatin ikhiqiza i-LDL-cholesterol-yehlisa kakhulu kunezinye izidakamizwa ze-statin.Kodwa-ke, ubukhulu obufanayo bokwehlisa i-cholesterol bungafinyelelwa ngokusebenzisa imithamo ephezulu yezinye eziningi zama-statins.

Lapho ukwelashwa kwe-statin "okujulile" kuyadingeka ukuze kuncishiswe amazinga e-cholesterol, i-rosuvastatin iwumuthi osetshenziswa kodokotela abaningi.

Ukusebenza kwe-rosuvastatin

I-Rosuvastatin isizuze idumela lokusebenza ngempumelelo ikakhulukazi phakathi kwezidakamizwa ze-statin, ikakhulukazi ngokusekelwe emiphumeleni yokuhlolwa okubili komtholampilo.

Ngo-2008, ukushicilelwa kocwaningo lwe-JUPITER kwaqashelwa odokotela benhliziyo yonke indawo.Kulolu cwaningo, abantu abangaphezu kwe-17,000 abanempilo ababenamazinga ajwayelekile e-cholesterol e-LDL egazini kodwa amazinga e-CRP aphakeme ayenziwe ngokungahleliwe ukuze bathole noma i-20 mg ngosuku ye-rosuvastatin noma i-placebo.

Ngesikhathi sokulandelela, abantu abahlelwe ngokungahleliwe ku-rosuvastatin abazange nje banciphise kakhulu amazinga e-cholesterol ye-LDL namazinga e-CRP, kodwa futhi babe nezenzakalo ezimbalwa zenhliziyo nemithambo yegazi (okuhlanganisa ukuhlasela kwenhliziyo, unhlangothi, isidingo senqubo yokuvuselela imithambo efana nokuhlinzwa kwe-stent noma i-bypass, kanye nenhlanganisela yokuhlaselwa yisifo senhliziyo, noma ukufa kwenhliziyo nemithambo yegazi), kanye nokunciphisa ukufa okuyimbangela.

Lolu cwaningo lwaluphawuleka hhayi kuphela ngenxa yokuthi i-rosuvastatin iye yathuthukisa kakhulu imiphumela yomtholampilo kubantu ngokusobala abanempilo, kodwa futhi ngoba laba bantu babengenawo amazinga e-cholesterol aphakeme ngesikhathi sokubhaliswa.

Ngo-2016, uhlolo lwe-HOPE-3 lwashicilelwa.Lolu cwaningo lubhalise abantu abangaphezu kwe-12,000 okungenani engozini eyodwa ye-atherosclerotic vascular disease, kodwa akukho CAD ecacile.Abahlanganyeli bahlelwe ngokungahleliwe ukuze bathole i-rosuvastatin noma i-placebo.Ekupheleni konyaka, abantu abathatha i-rosuvastatin babe nokuncipha okukhulu komphumela womphumela oyinhlanganisela (okuhlanganisa ukuhlasela kwenhliziyo okungabulali noma unhlangothi, noma ukufa ngenxa yesifo senhliziyo).

Kuzo zombili lezi zivivinyo, i-randomization ku-rosuvastatin yenze ngcono kakhulu imiphumela yomtholampilo yabantu ababenesici esiyingozi esisodwa noma ngaphezulu, kodwa kungekho zimpawu zesifo senhliziyo esisebenzayo.

Kufanele kuqashelwe ukuthi i-rosuvastatin yakhethwa kulezi zivivinyo hhayi ngenxa yokuthi yayinamandla kakhulu ezidakamizwa ze-statin, kodwa (okungenani ingxenye enkulu) ngenxa yokuthi ukuhlolwa kwakuxhaswe ngu-AstraZeneca, umenzi we-rosuvastatin.

Ochwepheshe abaningi be-lipid bakholelwa ukuthi imiphumela yalokhu kuhlolwa ibizofana ukube bekusetshenziswe enye i-statin ngemithamo eyanele, futhi empeleni, izincomo zamanje zokwelashwa ngezidakamizwa ze-statin ngokuvamile zivumela ukusetshenziswa kwanoma yimiphi imithi ye-statin inqobo nje uma umthamo uphakeme ngokwanele ukuze ufinyelele izinga elifanayo lokwehlisa i-cholesterol njengoba lingafinyelelwa ngomthamo ophansi we-rosuvastatin.(Okuhlukile kulo mthetho ojwayelekile kwenzeka lapho kudingeka “ukwelashwa okunamandla ngama-statins”. Ukwelashwa okujulile ngama-statin kuqondwa njengokusho i-rosuvastatin yomthamo omkhulu noma i-atorvastatin yomthamo omkhulu, okuyi-statin enamandla kakhulu etholakalayo.)

Kodwa ngenxa yokuthi i-rosuvastatin ngempela kwakuyisidakamizwa esasetshenziswa kulezi zivivinyo ezimbili ezibalulekile zomtholampilo, odokotela abaningi baye bahluleka ukusebenzisa i-rosuvastatin njengesithako sabo abazikhethela sona.

Izinkomba Zamanje

Ukwelashwa kwe-Statin kuboniswa ukuthuthukisa amazinga e-lipid egazi angajwayelekile (ikakhulukazi, ukwehlisa i-cholesterol ye-LDL kanye/noma amazinga e-triglyceride), nokuvimbela isifo senhliziyo nemithambo yegazi.I-Statins inconywa kubantu abanesifo senhliziyo esimisiwe, abantu abanesifo sikashukela, kanye nabantu abasengozini yeminyaka eyi-10 yokuba nesifo senhliziyo ingaphezu kuka-7.5% kuya ku-10%.

Nakuba, ngokuvamile, izidakamizwa ze-statin zithathwa njengezingashintshaniswa ngokuya ngokusebenza kwazo kanye nengozi yazo yokudala izehlakalo ezimbi, kungase kube nezikhathi lapho i-rosuvastatin ingakhethwa khona.Ikakhulukazi, lapho ukwelashwa kwe-statin "okunamandla aphezulu" kuhloselwe ukwehlisa i-cholesterol ye-LDL ibe emazingeni aphansi kakhulu ngangokunokwenzeka, i-rosuvastatin noma i-atorvastatin emazingeni azo aphezulu emithamo ngokuvamile ayanconywa.

Ngaphambi Kokuthatha

Ngaphambi kokuthi unikezwe noma yisiphi isidakamizwa se-statin, udokotela wakho uzokwenza ukuhlolwa kwengozi okusemthethweni ukuze alinganise ubungozi bakho bokuthola isifo senhliziyo futhi uzokala amazinga akho e-lipid yegazi.Uma usuvele unesifo senhliziyo nemithambo yegazi noma usengozini ephakeme kakhulu yokuba naso, udokotela wakho cishe uzoncoma umuthi wama-statin.

Eminye imishanguzo ye-statin evame ukunikezwa ihlanganisa i-atorvastatin, i-simvastatin, i-fluvastatin, i-lovastatin, i-pitavastatin, ne-pravastatin.

I-Crestor, uhlobo lwegama lomkhiqizo we-rosuvastatin e-US, ibiza kakhulu, kodwa izinhlobo ezijwayelekile ze-rosuvastatin seziyatholakala.Uma udokotela wakho efuna ukuthi uphuze i-rosuvastatin, buza ukuthi ungakwazi yini ukusebenzisa ijenerikhi.

I-Statins akufanele isetshenziswe kubantu abangazwani nama-statins nanoma yiziphi izithako zabo, abakhulelwe noma abancelisayo, abanesifo sesibindi noma ukwehluleka kwezinso, noma abaphuza utshwala ngokweqile.Ucwaningo lukhombisa ukuthi i-rosuvastatin ingasetshenziswa ngokuphepha ezinganeni ezingaphezulu kweminyaka eyi-10.

Umthamo we-rosuvastatin

Lapho i-rosuvastatin isetshenziselwa ukwehlisa amazinga e-cholesterol aphakeme e-LDL, imvamisa imithamo ephansi iyaqalwa (5 kuya ku-10 mg ngosuku) futhi ilungiswe phezulu njalo ngenyanga noma ezimbili uma kunesidingo.Kubantu abane-hypercholesterolemia yomndeni, odokotela bavame ukuqala ngemithamo ethe xaxa (10 kuya ku-20 mg ngosuku).

Lapho i-rosuvastatin isetshenziselwa ukwehlisa ubungozi besifo senhliziyo nemithambo yegazi kubantu abasengozini ephakeme ngokumaphakathi, umthamo wokuqala uvame ukuba ngu-5 kuye ku-10 mg ngosuku.Kubantu ubungozi babo buthathwa buphezulu (ikakhulukazi, ubungozi babo beminyaka eyi-10 bulinganiselwa ukuthi bungaphezu kuka-7.5%), ukwelapha okunamandla kuvame ukuqalwa, ngo-20 kuya ku-40 mg ngosuku.

Uma i-rosuvastatin isetshenziselwa ukwehlisa ubungozi bezehlakalo ezengeziwe zenhliziyo nemithambo yegazi kumuntu onesifo senhliziyo esesivele esenziwe, ukwelashwa okuqinile kuvame ukusetshenziswa ngomthamo wama-20 kuye kwangama-40 mg ngosuku.

Kubantu abathatha i-cyclosporine noma izidakamizwa ze-HIV/AIDS, noma kubantu abanokwehla kokusebenza kwezinso, umthamo we-rosuvastatin udinga ukuhlelwa phansi, futhi ngokuvamile akufanele udlule ku-10 mg ngosuku.

Abantu bozalo lwase-Asia bavame ukuzwela kakhulu emithini ye-statin futhi bathambekele kakhulu emiphumeleni emibi.Ngokuvamile kunconywa ukuthi i-rosuvastatin iqalwe ngo-5 mg ngosuku futhi ikhuliswe kancane kancane ezigulini zase-Asia.

I-Rosuvastatin ithathwa kanye ngosuku, futhi ingathathwa ekuseni noma ebusuku.Ngokungafani neminye imishanguzo eminingi ye-statin, ukuphuza inani elincane lejusi yamagilebhisi kunomphumela omncane ku-rosuvastatin.

Imiphumela emibi ye-Rosuvastatin

Eminyakeni esanda kwakhiwa i-rosuvastatin, ochwepheshe abaningi bathi imiphumela emibi ye-statin izoba mbi kakhulu nge-rosuvastatin, ngoba imithamo ephansi ingasetshenziswa ukuze kufinyelelwe ukwehla okwanele kwe-cholesterol.Ngasikhathi sinye, abanye ochwepheshe bathi imiphumela emibi ye-statin izokhuliswa ngalo muthi, ngoba wawunamandla kakhulu kunamanye ama-statins.

Eminyakeni edlule, kuye kwabonakala ukuthi akukho ukugomela obekuyiqiniso.Kubukeka sengathi uhlobo nobukhulu bemiphumela emibi ngokuvamile icishe ifane ne-rosuvastatin njengoba injalo nangezinye izidakamizwa ze-statin.

Ama-Statin, njengeqembu, abekezelelwa kangcono kunezinye izidakamizwa ezinciphisa i-cholesterol.Kuhlaziyo lwemeta olwanyatheliswa ngo-2017 olwalubheka izivivinyo zemitholampilo ezingahleliwe ezingama-22, bangu-13.3% kuphela abantu ababengahleliwe emuthini we-statin abayeka umuthi ngenxa yemiphumela engemihle phakathi neminyaka engu-4, uma kuqhathaniswa no-13.9% wabantu abafakwe ngokungahleliwe ku-placebo.

Noma kunjalo, kunemiphumela eyaziwa kahle ebangelwa ama-statins, futhi le miphumela emibi ngokuvamile isebenza ku-rosuvastatin kanye nanoma iyiphi enye i-statin.Okuphawuleka kakhulu kule miphumela engemihle ihlanganisa:

• Izehlakalo ezimbi ezihlobene nemisipha.Ubuthi bemisipha bungabangelwa ama-statins.Izimpawu zingase zihlanganise i-myalgia (ubuhlungu bemisipha), ubuthakathaka bemisipha, ukuvuvukala kwemisipha, noma (ezimweni ezingavamile, ezinzima) i-rhabdomyolysls.I-Rhabdomyolysis ukwehluleka kwezinso okukhulu okubangelwa ukuwohloka okukhulu kwemisipha.Ezimweni eziningi.imiphumela emibi ehlobene nemisipha ingalawulwa ngokushintshela kwenye i-statin.I-Rosuvastatin iphakathi kwezidakamizwa ze-statin ezibonakala zibanga ubuthi obuncane bemisipha.Ngokuphambene, i-lovastatin, i-simvastatin, ne-atorvastatin ijwayele ukudala izinkinga zemisipha.
• Izinkinga zesibindi.Cishe u-3% wabantu abathatha ama-statins bazoba nokwanda kwama-enzyme esibindi egazini labo.Kwabaningi balaba bantu, abukho ubufakazi bokulimala kwesibindi kwangempela okubonakala, futhi ukubaluleka kwalokhu kuphakama okuncane kuma-enzyme akucaci.Kubantu abambalwa kakhulu, ukulimala okukhulu kwesibindi kuye kwabikwa;akucaci, noma kunjalo, ukuthi izehlakalo zokulimala okukhulu kwesibindi ziphakeme kubantu abathatha ama-statins kunabantu abaningi.Akukho okukhombisa ukuthi i-rosuvastatin ikhiqiza izinkinga zesibindi eziningi noma ezimbalwa kunamanye ama-statins.
• Ukukhubazeka kwengqondo.Umbono wokuthi ama-statins angabangela ukukhubazeka kwengqondo, ukulahlekelwa inkumbulo, ukudangala, ukucasuka, ulaka, noma eminye imiphumela yesistimu yezinzwa ephakathi iye yaphakanyiswa, kodwa ayizange iboniswe ngokucacile.Ekuhlaziyweni kwemibiko yamacala ethunyelwe ku-FDA, izinkinga zokucabanga okusolwayo ezihlobene nama-statins zibonakala zivame kakhulu emithini ye-lipophilic statin, ehlanganisa i-atorvastatin, i-fluvastatin, i-lovastatin, ne-simvastatin.Izidakamizwa ze-hydrophilic statin, okuhlanganisa ne-rosuvastatin, ziye zathinteka kancane ngalesi sigameko esibi esingaba khona.
• Isifo sikashukela.Eminyakeni yamuva nje, ukwanda okuncane kokuthuthukiswa kwesifo sikashukela kuye kwahlotshaniswa nokwelashwa kwe-statin.Ukuhlaziywa kwemeta ka-2011 kwezivivinyo ezinhlanu zomtholampilo kuphakamisa ukuthi icala elilodwa elengeziwe lesifo sikashukela lenzeka kubo bonke abantu abangama-500 abalashwa ngama-statins anamandla kakhulu.Ngokuvamile, leli zinga lengozi libhekwa njengelamukelekayo inqobo nje uma i-statin ingalindelwa ukuthi yehlise kakhulu ingozi yenhliziyo nemithambo yegazi.

Eminye imiphumela emibi evame ukubikwa ngezidakamizwa ze-statin ihlanganisa isicanucanu, isifo sohudo, nobuhlungu bamalunga.

Ukusebenzisana

Ukuthatha izidakamizwa ezithile kungandisa ingozi yokuba nemiphumela engemihle nge-rosuvastatin (noma iyiphi i-statin).Lolu hlu lude, kepha izidakamizwa eziphawuleka kakhulu ezisebenzisana ne-rosuvastatin zihlanganisa:

• I-Gemfibrozil, okuyi-ejenti engeyona i-statin eyehlisa i-cholesterol
• I-Amiodarone, okuyisidakamizwa esilwa nokuvuvukala
• Imishanguzo eminingi ye-HIV
• Amanye ama-antibiotics, ikakhulukazi i-clarithromycin ne-itraconazone
• I-Cyclosporine, umuthi we-immunosuppressant

Izwi Elivela Kahle

Nakuba i-rosuvastatin iyi-statin enamandla kakhulu etholakalayo, ngokuvamile, ukusebenza kwayo kanye nephrofayili yobuthi ifana kakhulu nawo wonke amanye ama-statins.Noma kunjalo, kunezimo ezimbalwa zomtholampilo lapho i-rosuvastatin ingakhethwa kunezinye izidakamizwa ezingama-statin.