Kāpae

ʻO Atorvastatin Calcium kahi mea paʻa ikaika o ka HMG-CoA reductase me ka waiwai IC50 o 150 nM [1].
ʻO HMG-CoA reductase ka enzyme nui o ke ala mevalonate e hoʻopuka ai i ka cholesterol. ʻO ka HMG-CoA ka enzyme e kaupalena ana i ka helu a he mea nui ia no ka hoʻohaʻahaʻa ʻana i nā pae cholesterol koko. Aia ka HMG-CoA reductase i loko o ka endoplasmic reticulum a loaʻa iā ia ʻewalu mau kikowaena transmembrane. Hiki i nā inhibitors o HMG-CoA reductase ke hoʻoulu i ka LDL (low density lipoprotein) i hōʻike ʻia i loko o ke ake. Ke alakaʻi nei ia i ka hoʻonui ʻana i nā pae catabolism o ka LDL plasma a hoʻohaʻahaʻa i ka ʻike o ka cholesterol plasma kahi mea koʻikoʻi e hoʻoholo ai i ka atherosclerosis. He kuleana koʻikoʻi ka HMG-CoA reductase i ka hana ʻana o ka cholesterol. ʻO ka HMG-CoA ka pahuhopu no nā lāʻau hoʻohaʻahaʻa cholesterol. ʻO ka HMG-CoA reductase kekahi enzyme koʻikoʻi no ka hoʻomohala ʻana. Pili ka hana o ka HMG-CoA reductase i nā hemahema o ka neʻe ʻana o ka germ cell. ʻO ka pale ʻana i kāna hana hiki ke alakaʻi i ka hemorrhage intracerebral [1].
ʻO Atorvastatin kahi mea hoʻopaneʻe HMG-CoA reductase me ka waiwai IC50 o 154 nM. He kūpono ia i ka mālama ʻana i kekahi mau dyslipidemias a me hypercholesterolemia [1]. ʻO ka mālama ʻana iā Atorvastatin ma 40 mg e hoʻemi ana i ka kolamu piha o 40% ma hope o 40 mau lā.[1] Hoʻohana ʻia no ka mālama ʻana i nā maʻi maʻi coronary a i ʻole nā ​​​​maʻi maʻi me nā pae cholesterol maʻamau.[2] Hoʻemi pū ʻo Atorvastatin i ka apheresis lipoprotein haʻahaʻa haʻahaʻa i nā mea maʻi ma o ka hoʻoulu ʻana i ka hōʻike LDL-receptors.
Hoʻopili ʻia ia i kekahi mau metabolites i mea nui no ka hopena o nā hana therapeutic e CYP3A4 (cytochrome P450 3A4).[3]
Kuhikuhi:
[1]. van Dam M, Zwart M, de Beer F, Smelt AH, Prins MH, Trip MD, Havekes LM, Lansberg PJ, Kastelein JJ: ʻO ka hopena lōʻihi a me ka palekana o ka atorvastatin i ka mālama ʻana i ke ʻano koʻikoʻi III a me ka dyslipidemia i hui pū ʻia. Puuwai 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: Ka pale ʻana i nā hanana coronary a me ka hahau ʻana me ka atorvastatin i nā maʻi hypertensive i loaʻa ka awelika a haʻahaʻa paha. -ʻo ka nui o ka cholesterol maʻamau, ma ka Anglo-Scandinavian Cardiac Outcomes Trial--Lipid Lowering Arm (ASCOT-LLA): a multicentre randomized controlled trial. Lancet 2003, 361(9364):1149-1158.
[3]. Lennernas H: Nā lāʻau lapaʻau lapaʻau o ka atorvastatin. Clin Pharmacokinet 2003, 42 (13): 1141-1160.

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