Atorvastatin Calcium
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 kutaura muchiropa.Iyo inotungamira kuwedzera catabolism mazinga eplasma LDL uye kudzikisa kuwanda kweplasma cholesterol inova yakakosha dhizaini yeatherosclerosis.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 vanorwara nemoyo kana sitiroko vane mwero wakajairika cholesterol.[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. -average cholesterol concentrations, muAnglo-Scandinavia Cardiac Outcomes Trial--Lipid Lowering Arm (ASCOT-LLA): a multicentre randomized controlled trial.Lancet 2003, 361(9364):1149-1158.
[3].Lennernas H: Clinical pharmacokinetics ye atorvastatin.Clin Pharmacokinet 2003, 42(13):1141-1160.
Chimiro chemakemikari
Proposal18Quality Consistency Evaluation mapurojekiti akatenderwa4,uye6mapurojekiti ari pasi pekubvumidzwa.
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