Ingemuva

I-Atorvastatin Calcium iyi-inhibitor enamandla ye-HMG-CoA reductase enevelu ye-IC50 engu-150 nM[1].
I-HMG-CoA reductase iyi-enzyme eyinhloko ye-mevalonate pathway ekhiqiza i-cholesterol. I-HMG-CoA iyi-enzyme enciphisa izinga futhi ibalulekile ekwehliseni amazinga e-cholesterol egazini. I-HMG-CoA reductase itholakala ku-endoplasmic reticulum futhi iqukethe izizinda eziyisishiyagalombili ze-transmembrane. Ama-inhibitor e-HMG-CoA reductase angadala ukubonakaliswa kwe-LDL (low density lipoprotein) esibindini. Kuholela ekwandiseni amazinga e-catabolism we-plasma LDL futhi kwehlise ukugcwala kwe-plasma cholesterol okuyisici esibalulekile se-atherosclerosis. I-HMG-CoA reductase idlala indima ebalulekile ekwakhiweni kwe-cholesterol. I-HMG-CoA iyinkomba eyodwa kuphela yezidakamizwa ezehlisa i-cholesterol. I-HMG-CoA reductase nayo iyi-enzyme ebalulekile ekuthuthukisweni. Umsebenzi we-HMG-CoA reductase uhlobene nokukhubazeka kokufuduka kwamangqamuzana amagciwane. Ukuvinjelwa komsebenzi wawo kungaholela ekopheni kwe-intracerebral[1].
I-Atorvastatin iyi-HMG-CoA reductase inhibitor enenani le-IC50 elingu-154 nM. Isebenza ngempumelelo ekwelapheni i-dyslipidemia ethile kanye ne-hypercholesterolemia[1]. Ukwelashwa kwe-Atorvastatin ngo-40 mg kwehlisa i-cholesterol ephelele ngama-40% ngemva kwezinsuku ezingu-40.[1] Iphinde isetshenziselwe ukwelapha iziguli zenhliziyo noma zohlangothi ezinamazinga ajwayelekile e-cholesterol.[2] I-Atorvastatin futhi yehlisa i-low density lipoprotein apheresis ezigulini ngokufaka inkulumo ye-LDL-receptors.
Icutshungulwa kuma-metabolite ambalwa abalulekile kumphumela wezenzo zokwelapha nge-CYP3A4 (cytochrome P450 3A4).[3]
Izithenjwa:
[1]. van Dam M, Zwart M, de Beer F, Smelt AH, Prins MH, Trip MD, Havekes LM, Lansberg PJ, Kastelein JJ: Ukusebenza kwesikhathi eside nokuphepha kwe-atorvastatin ekwelapheni uhlobo olunzima lwe-III kanye ne-dyslipidaemia ehlangene. Inhliziyo 2002, 88(3):234-238.
[2]. I-Sever PS, i-Dahlof B, i-Poulter NR, i-Wedel H, i-Beevers G, i-Caulfield M, i-Collins R, i-Kjeldsen SE, i-Kristinsson A, i-McInnes GT et al: Ukuvinjelwa kwemicimbi ye-coronary kanye ne-stroke nge-atorvastatin ezigulini ezinomfutho wegazi ophakeme ezinesilinganiso noma esiphansi kune -isilinganiso sokugxila kwe-cholesterol, ku-Anglo-Scandinavian Cardiac Outcomes Trial--Lipid Lowering Arm (ASCOT-LLA): isilingo esilawulwa ngokungahleliwe se-multicentre. I-Lancet 2003, 361(9364): 1149-1158.
[3]. I-Lennernas H: I-pharmacokinetics yomtholampilo ye-atorvastatin. I-Clin Pharmacokinet 2003, 42(13): 1141-1160.

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