Atorvastatin Calcium
Mbiri
Atorvastatin Calcium ndi inhibitor yamphamvu ya HMG-CoA reductase yokhala ndi IC50 mtengo wa 150 nM[1].
HMG-CoA reductase ndiye enzyme yofunikira ya njira ya mevalonate yomwe imatulutsa cholesterol.HMG-CoA ndiye puloteni yochepetsera mlingo ndipo ndiyofunikira kutsitsa kuchuluka kwa cholesterol m'magazi.HMG-CoA reductase ili mu endoplasmic reticulum ndipo ili ndi madera asanu ndi atatu a transmembrane.Ma inhibitors a HMG-CoA reductase amatha kupangitsa kuti LDL (low density lipoprotein) kuwoneka m'chiwindi.Zimathandizira kukulitsa kuchuluka kwa LDL m'magazi am'magazi ndikuchepetsa kuchuluka kwa cholesterol m'madzi am'magazi, chomwe ndi chofunikira kwambiri cha atherosulinosis.HMG-CoA reductase imagwira ntchito yofunika kwambiri pakupanga cholesterol.HMG-CoA ndiye chandamale chilichonse chamankhwala ochepetsa cholesterol.HMG-CoA reductase ndiyenso puloteni yofunikira pakukula.Ntchito ya HMG-CoA reductase imakhudzana ndi kuwonongeka kwa ma cell ma cell.Kulepheretsa ntchito yake kungayambitse kutulutsa magazi m'thupi [1].
Atorvastatin ndi HMG-CoA reductase inhibitor yokhala ndi IC50 mtengo wa 154 nM.Ndiwothandiza pochiza matenda ena a dyslipidemia ndi hypercholesterolemia [1].Mankhwala a atorvastatin pa 40 mg amachepetsa mafuta m'thupi ndi 40% pakadutsa masiku 40.[1]Amagwiritsidwanso ntchito pochiza odwala matenda amtima kapena sitiroko omwe ali ndi cholesterol yabwinobwino. [2]Atorvastatin imachepetsanso kachulukidwe kakang'ono ka lipoprotein apheresis mwa odwala mwa kuchititsa kuwonetsa kwa LDL-receptors.
Izo zimapukusidwa kuti angapo metabolites amene ali ofunika kwa zotsatira za zochita achire ndi CYP3A4 (cytochrome P450 3A4).[3]
Zolozera:
[1].van Dam M, Zwart M, de Beer F, Smelt AH, Prins MH, Trip MD, Havekes LM, Lansberg PJ, Kastelein JJ: Kugwiritsa ntchito nthawi yayitali komanso chitetezo cha atorvastatin pochiza matenda aakulu a mtundu wa III ndi dyslipidaemia.Mtima 2002, 88(3):234-238.
[2].Sever PS, Dahlof B, Poulter NR, Wedel H, Beevers G, Caulfield M, Collins R, Kjeldsen SE, Kristinsson A, McInnes GT et al: Kupewa zochitika za coronary ndi sitiroko ndi atorvastatin mwa odwala omwe ali ndi matenda oopsa kwambiri omwe ali ndi pafupifupi kapena otsika kuposa -avereji yamafuta a cholesterol, mu Anglo-Scandinavian Cardiac Outcomes Trial--Lipid Lowering Arm (ASCOT-LLA): kuyesa koyendetsedwa kosasinthika kosiyanasiyana.Lancet 2003, 361(9364):1149-1158.
[3].Lennernas H: Clinical pharmacokinetics ya atorvastatin.Clin Pharmacokinet 2003, 42 (13): 1141-1160.
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