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 kuchuluka ndipo ndiyofunikira pakutsitsa 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. Zimayambitsa kuchulukitsa 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. Kuletsa 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 mtundu wa III woopsa komanso 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 mayeso a Anglo-Scandinavia Cardiac Outcomes--Lipid Lowering Arm (ASCOT-LLA): kuyeserera 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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