Ngaphandle kwe-cholesterol, umzimba womuntu awunakuba khona ngokuphelele. Le nto iyingxenye yolwelwesi lweseli, ngaphezu kwalokho, ngaphandle kwawo, umsebenzi wesistimu yezinzwa nezinye izitho ezibalulekile zomzimba womuntu ngeke kwenzeke.
Ngokuqukethwe okweqile kwalolutho kusho ukuthi i-cholesterol embi, yona kanye ne-protein kwakha i-compact entsha - i-lipoprotein. Ibuye ibe khona ngezindlela ezimbili: i-low density and high density. I-lipensrensin ephezulu yokulimala ayinabungozi emzimbeni, ngokungafani nezinhlobonhlobo zayo zesibili. Uma isimo singasasebenzi futhi izinga lale lipoprotein esegazini alibaluleki, kuzokwanela isiguli ukuthi siguqule ekudleni kokudla singene emisebenzini yaso yokuphila.
Kodwa lezi zinyathelo azihlali zinikeza umphumela oyifunayo, kwezinye izimo, isiguli singadinga ukuhlanzwa kwezokwelapha kwemikhumbi.
Sekuyisikhathi eside ososayensi basebenzela ukwakha umuthi ofanele wokunciphisa i-cholesterol "embi".
Isixazululo esikahle asikatholakali, amaqembu amaningi emithi edaliwe ukunciphisa i-cholesterol, ngalinye lawo linama-nuances alo amahle futhi angalungile.
Izimpawu ziphakathi kwezidakamizwa ezihamba phambili ze-lipoprotein ephezulu yegazi, kodwa ngenxa yamaphutha amaningi nokubakhona kwemiphumela eyingozi emzimbeni, ikakhulukazi uma usebenzisa imithamo ephezulu yomuthi, azihlali zishesha ukunquma.
Isimo se-Cholesterol Absorption Inhibitors
Lapho welapha i-cholesterol ephezulu yegazi, ama-static awaxubeki ne-nicotinic acid kanye nama-fibrate, okuyizidakamizwa zesigaba esehlukile, ngenxa yokuthi akuphephile ngokwanele futhi kungadala ukukhula kwezinye izifo. Isibonelo, ukuhlanganiswa kwama-fibrate nama-statins kukhulisa ubungozi be-myopathy, into efanayo ingenzeka ngokuhlanganiswa kwe-nicotinic acid nama-statins, ngaphezu kwalokho konke isibindi kungathinteka.
Kepha osokhemisi bathole isixazululo, bathuthukisa imishanguzo eqondiswe kwezinye izindlela zokwenziwa kwe-hypercholesterolemia, ikakhulukazi, ekufakweni kwe-cholesterol emathunjini. Omunye wale mishanguzo yi-Ezithimibe noma i-Ezeterol.
Inzuzo yomuthi ukuthi iphephe kakhulu ngenxa yokuthi izingxenye zayo azingene egazini. Lokhu kubaluleke kakhulu ngoba umuthi uzotholakala ezigulini ezinesifo sezinhlungu zesibindi kanye nalabo abaphikiselwe ukusetshenziswa kwama-statins ngenxa yezizathu eziningi. Ukuhlanganiswa kwe-ezeterol ngama-statins kungahle kube nomthelela ekwandiseni umphumela wokwelapha okuhloswe ngawo ukwehlisa i-cholesterol emzimbeni.
Mayelana nobubi bomuthi, izindleko zawo eziphakeme ziyahlukaniswa futhi, esimweni sokubumba, umphumela omncane wokusetshenziswa, uma uqhathaniswa nemiphumela yokwelashwa ngama-statins.
Izinkomba zokusetshenziswa kwomuthi
Kunconywa nini ukunquma lesi sidakamizwa? Kuboniswa i-hypercholesterolemia eyinhloko, i-Ezithimibe isetshenziswa ngokuzimela ngaphezu kokudla kokudla, noma ngokuhlanganiswa nama-statins.
Lesi sidakamizwa sisiza ukwehlisa hhayi kuphela izinga le-cholesterol ephelele, kodwa futhi ne-apolipoprotein B, i-triglycerides, i-cholesterol ye-LDL, kanye nokukhulisa i-cholesterol ye-HDL.
Nge-homozygous womndeni hypercholesterolemia, umuthi usetshenziswa njengesengezo kuma-statins ukuze wehlise i-cholesterol ephakemeyo, isamba kanye ne-LDL.
I-Ezeterol imiselwe i-sitomoolemia ye-homozygous. Ikuvumela ukuthi unciphise amazinga aphezulu we-campesterol ne-sitosterol.
Contraindication kanye nemiphumela emibi
Lo muthi awunqunyelwe ukusetshenziswa yiziguli ezinokukhubazeka okwengeziwe kwezinto zalo ezikhona.
Abesifazane abakhulelwe nangesikhathi sokuncelisa ibele futhi akunconywa ukuba basebenzise i-cholesterol ukumunca inhibitors.
Uma kunesidingo sokusetshenziswa kwe-ezeterol ngumama osancelayo, lapho-ke kuzodingeka ukuthi uthathe isinqumo sokuyeka ukuncelisa ibele.
Okunye ukuphikisana kufaka phakathi:
- iminyaka engaphansi kweminyaka eyi-18, ngoba ukuphepha kanye nokusebenza kahle kokusebenzisa umuthi akukasungulwa;
- ukuba khona kwanoma iyiphi i-pathologies yesibindi ngesikhathi sokuqhuma, kanye nokwanda komsebenzi wama-transaminases “wesibindi”;
- ukwehluleka okukhulu noma okulinganiselayo kokuhluleka kwesibindi, njengoba kukalwa ngezinga le-Child-Pyug;
- ukuntuleka kwe-lactose, ukungabekezelelani kwe-lactose, i-glucose-galactose malabsorption;
- ukusetshenziswa kwesidakamizwa kuhlangene ne-fibrate;
- Ukusetshenziswa kweziguli ezithola i-cyclosporine yezidakamizwa kufanele kwenziwe ngokuqapha kanye nokuqapha izinga lokuxineka kwe-cyclosporin egazini.
Endabeni ye-monotherapy, i-cholesterol ukumuncwa kwe-cholesterol kungadala imiphumela emibi efana nobuhlungu besisu, ukugayeka, ikhanda. Ngokwelashwa okuyinkimbinkimbi ngama-statins, ngaphezu kwe-migraines, izimpawu zingavela ngendlela yokukhathala, i-flatulence, izinkinga zesitulo (ukukhathazeka noma ukuqunjelwa), isicanucanu, i-myalgia, umsebenzi owandisiwe we-ALT, AST, ne-CPK. Futhi, ukubonakala kokuqhuma kwesikhumba, i-angioedema, i-hepatitis, i-pancreatitis, i-thrombocytopenia kanye nokwanda kwama-enzymes wesibindi akuhlanganisiwe emisebenzini yezokwelapha.
Ezimweni ezingavamile kakhulu, ukuthuthukiswa kwe-rhabdomyolysis kungenzeka.
Umgomo wokusebenza kwe-inhibitor
I-Ezetimibe ikhetha ukuvimbela ukumuncwa kwe-cholesterol nezinhlobo ezithile zezitshalo emathunjini amancane. Lapho, umuthi utholakala endaweni yamathumbu amancane futhi awuvumeli ukuba i-cholesterol imunce, ngaleyo ndlela kuncishiswe ukuhanjiswa kwe-cholesterol ngqo kusuka emathunjini kuya kwesinye isitho - isibindi, kwehlise izinqolobane zayo esibindini futhi kwandise ukuphuma kwe-plasma yegazi.
Ama-blocker we-cholesterol ukumunca awakhuphi ukuphuma kwe-bile acid futhi awavimbeli ukuvela kwe-cholesterol yesibindi, okungenakushiwo mayelana nama-statins. Ngenxa yomgomo ohlukile wokusebenza, izidakamizwa zalezi zifundo, ngenkathi zisetshenziswa ngama-statins, zingaqhubekisa ukwehlisa i-cholesterol. Ucwaningo lwe-preclinical lukhombisa ukuthi ukumuncwa kwe-14C-cholesterol kuvinjelwe yi-ezeterol.
I-bioavailability ephelele ye-ezeterol ayikwazi ukunqunywa ngoba le khompiyutha icishe ayinamanzi.
Ukusetshenziswa kwomuthi ngokuhambisana nokudla akunathinti i-bioavailability yawo kumthamo ongekho ngaphezu kwe-10 mg.
Indlela yokusebenzisa, umthamo nezindleko
Ngaphambi kokuqala inkambo yokwelashwa, iziguli kudingeka zidle ngokudla nge-cholesterol ephezulu, kuzodingeka ukuthi ziqhubeke ukubonwa kuso sonke isikhathi sokudla umuthi. I-Ezeterol kumele ithathwe usuku lonke, kungakhathalekile ukuthathwa kokudla. Imvamisa, udokotela oholayo unquma ukuthi ungaphuzi umuthi we-10 mg ungadluli kanye ngosuku.
Ngokuqondene nomthamo ngokuhlanganiswa kwe-Ezithimibe ngama-statins, nokwelashwa okuyinkimbinkimbi, lo mthetho olandelayo kufanele unamathelwe: thatha umuthi kanye ngosuku ngama-statins, qiniseka ukuthi ulandela izincomo ezibekiwe zokwamukelwa.
Ekwelashweni okufanayo nokulandelana kwamafutha acid ne-Ezithimibe, kufanele kuthathwe ngomthamo we-10 mg kanye ngosuku, kepha kungabi isikhathi esingaphezu kwamahora amabili ngaphambi kokuthatha ama-sequestrants noma hhayi ngaphambi kwamahora amane ngemuva.
Uma kwenzeka ukungasebenzi kahle kwesibindi, iziguli ezisesimweni sokuhluleka kwesibindi esincane azidingi ukukhethwa komthamo. Futhi ezigulini ezinokwehluleka kwesibindi okulinganiselwe kuya kobunzima obukhulu, ngokuvamile akukalulekanga ukusebenzisa izithintelo zokufakwa kwe-cholesterol engenayo emathunjini omuntu.
Njengoba sekushiwo, intengo yama-inhibitors ayibizi ikakhulukazi, ephathelene nobubi bayo.
I-Ezetimibe kumthamo wamamiligremu ayi-10 (izingcezu ezingama-28) ingathengwa kusuka kuma-ruble ayi-1800 kuya kwangama-2000.
I-Ezithymibe ukweqisa nokuxhumana
Lapho uthatha inkambo yokwelapha ene-inhibitors, kubalulekile ukunamathela ngokuqinile ohlotsheni olunqunywe ngudokotela. Kepha uma kwenzeka kusetshenziswa i-overdose, iziguli kufanele zazi okulandelayo.
Ezimweni ezingavamile zokusebenzisa ngokweqile i-overdose, izehlakalo ezimbi ezivele ezigulini azizange zibe zimbi ngokwanele. Uma sikhuluma ngovivinyo lomtholampilo, khona-ke kwesinye saso lesi sidakamizwa sanikezwa izisebenzi zokuzithandela eziyi-15 ezinempilo enhle emthanjeni wama-50 mg nsuku zonke amasonto amabili.
Olunye ucwaningo lwalubandakanya izisebenzi zokuzithandela eziyi-18 ezinezimpawu ze-hypercholesterolemia; banqunyelwa ama-40 mg we-Ezithimibe izinsuku ezingaphezu kwezingama-50. Bonke ababambiqhaza esivivinyweni somtholampilo babenokubekezelela okuhle kulo muthi.
Ukuhlanganiswa kwe-Ezithimibe nokusetshenziswa kwama-antacid kungasiza ekwehliseni izinga lokufakwa kwezinto zomuthi wokuqala, kepha lokhu akuwuphazamisi umsebenzi wawo we-bioavailability. Ngokwelashwa okuhlanganyelwe nge-cholestyramine, izinga lokufaka inani lesamba le-eseterol lehliswa cishe ngamaphesenti angama-55.
Ngokulashwa okuyinkimbinkimbi ngama-fenofibrate, ngenxa yalokho, inani eliphelele le-inhibitor lenyuka cishe isikhathi esisodwa nesigamu. Ukusetshenziswa kwe-eseterol enama-fibrate akufundiswanga kahle, ngakho-ke ukusebenzisa kwabo kanyekanye odokotela akunconywa.
Ubungozi be-cholesterol ephezulu buchazwe kule vidiyo kulesi sihloko.
