Background

Atorvastatin Calcium inhibitor ine simba yeHMG-CoA reductase ine IC50 kukosha kwe150 nM[1].
HMG-CoA reductase ndiyo yakakosha enzyme yemevalonate nzira inoburitsa cholesterol. HMG-CoA ndiyo chiyero-inomisa enzyme uye yakakosha pakudzikisa mazinga eropa cholesterol. HMG-CoA reductase iri mu endoplasmic reticulum uye ine sere transmembrane domains. Iyo inhibitors yeHMG-CoA reductase inogona kukurudzira iyo LDL (yakaderera density lipoprotein) inogamuchirwa muropa. Iyo inotungamira kuwedzera catabolism mazinga eplasma LDL uye kuderedza kuwanda kweplasma cholesterol inova yakakosha inogadzirisa atherosclerosis. HMG-CoA reductase inoita basa rakakosha mukuumbwa kwecholesterol. HMG-CoA ndiyo chete chinangwa chemishonga inoderedza cholesterol. HMG-CoA reductase zvakare yakakosha enzyme yekusimudzira. Chiitiko cheHMG-CoA reductase chine hukama negerm cell migration defects. Kudziviswa kwekuita kwayo kunogona kutungamirira kune intracerebral hemorrhage[1].
Atorvastatin iHMG-CoA reductase inhibitor ine IC50 kukosha kwe154 nM. Inoshanda mukurapa mamwe dyslipidemias uye hypercholesterolemia[1]. Kurapwa kweAtorvastatin ne40 mg kunoderedza cholesterol yese ye40% mushure memazuva makumi mana.[1] Inoshandiswawo kurapa varwere vane moyo kana sitiroko vane mwero wecholesterol wakajairika.[2] Atorvastatin zvakare inoderedza yakaderera density lipoprotein apheresis muvarwere nekuita LDL-receptors kutaura.
Inogadziriswa kune akawanda metabolites ayo akakosha pamhedzisiro yezviito zvekurapa neCYP3A4 (cytochrome P450 3A4).[3]
References:
[1]. van Dam M, Zwart M, de Beer F, Smelt AH, Prins MH, Rwendo MD, Havekes LM, Lansberg PJ, Kastelein JJ: Kushanda kwenguva refu uye kuchengetedzwa kwe atorvastatin mukurapa kwemhando yakaoma III uye yakabatanidzwa dyslipidaemia. Mwoyo 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: Kudzivirirwa kwezviitiko zve coronary uye sitiroko ne atorvastatin muvarwere vane hypertension vane pakati kana pasi-kupfuura. -avhareji yecholesterol yakawandisa, muAnglo-Scandinavia Cardiac Outcomes Trial--Lipid Lowering Arm (ASCOT-LLA): muyedzo wakawanda wakasarudzika unodzorwa. Lancet 2003, 361(9364):1149-1158.
[3]. Lennernas H: Clinical pharmacokinetics ye atorvastatin. Clin Pharmacokinet 2003, 42(13):1141-1160.

Chimiro chemakemikari