Zogulitsa

(+)-(3R,5S), tert-Butyl 7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulphonylamino)-pyrimidin-5-yl]-3,5 -dihydroxy-6(E) -heptenate, yomwe imadziwikanso kuti R1.5 kapena tert-butyl-rosuvastatin, ndi mankhwala omwe amatha kugwiritsidwa ntchito pamakampani opanga mankhwala.Rosuvastatin ndi mankhwala odziwika bwino ochepetsa cholesterol omwe ali m'kalasi mankhwala otchedwa statins.Imagwira ntchito poletsa enzyme yotchedwa HMG-CoA reductase, yomwe imagwira ntchito yopanga cholesterol m'thupi.R1.5 ndi yochokera ku rosuvastatin yomwe ili ndi gulu la tert-butyl lomwe limagwirizanitsidwa ndi molekyulu, kupereka zowonjezera zowonjezera ndi zopindulitsa.Mmodzi zotheka kugwiritsa ntchito R1.5 ndi monga mankhwala opangira mankhwala ochizira hyperlipidemia ndi kupewa matenda a mtima.Monga rosuvastatin, R1.5 ingagwiritsidwe ntchito kuchepetsa LDL cholesterol, yomwe imadziwikanso kuti "zoipa" cholesterol, ndi triglycerides m'magazi.Pharmacokinetic imatha kuwonetsa zinthu zabwino za pharmacokinetic, monga kuchuluka kwa bioavailability kapena kukhazikika kokhazikika, poyerekeza ndi mankhwala a kholo.Kuonjezera apo, gulu la tert-butyl likhoza kuthandizira kusungunuka kwapawiri ndi kupangika kosasunthika, zomwe zimapangitsa kuti zikhale zoyenera machitidwe osiyanasiyana operekera mankhwala.Gulu la tert-butyl limatha kukhala ngati gulu loteteza, lolola kuti rosuvastatin itulutsidwe m'magulu kapena ziwalo zina, monga chiwindi.Njirayi ikhoza kupititsa patsogolo mphamvu ya mankhwalawa ndikuchepetsa zotsatira zomwe zingatheke powonjezera ndende yake pamalo omwe akuyembekezeredwa komanso kuchepetsa kukhudzidwa kwa minofu yomwe siinapangidwe.Mapangidwe ovuta a pawiriwa amapereka nsanja yosinthira zina ndi zina.Ofufuza atha kugwiritsa ntchito R1.5 ngati chinthu chotsogolera kuti afufuze maubwenzi ochita kupanga ndikupanga ma analogi atsopano okhala ndi potency yowonjezereka, kusankha bwino, kapena mbiri yachipatala.Maphunziro oterowo angathandize kuti pakhale ma statins atsopano komanso othandiza kwambiri kapena othandizira ena ochepetsa mafuta m'thupi. -2-(N-methyl-N-methylsulphonylamino)-pyrimidin-5-yl]-3,5-dihydroxy-6(E)-heptenate (R1.5 kapena tert-butyl-rosuvastatin) imakhala ndi lonjezo ngati mankhwala opangira mankhwala. chithandizo cha hyperlipidemia ndi matenda amtima.Mapangidwe ake apadera, ophatikizidwa ndi gulu la tert-butyl, atha kupereka maubwino monga kuwongolera kwa pharmacokinetics, kaperekedwe ka mankhwala omwe akutsata, komanso mwayi wopititsa patsogolo mankhwala.Kufufuza kwina ndi chitukuko ndizofunikira kuti mufufuze mokwanira kuthekera kwa R1.5 pazamankhwala.