68.有關repaglinide藥品交互作用之敘述,下列何者錯誤?
(A)與clopidogrel併用,會造成repaglinide血中濃度上升
(B)與cyclosporine併用,會造成repaglinide血中濃度上升
(C)與digoxin併用,會造成digoxin血中濃度上升
(D)與gemfibrozil併用,會造成低血糖風險增加
統計: A(1044), B(472), C(1880), D(931), E(0) #2624813
詳解 (共 8 筆)
解題重要觀念
[Repaglinide主要由CYP3A4、CYP2C8代謝]
(A)因為Clopidogrel代謝物是2C8的抑制劑,所以Repaglinide血中濃度上升。
資料取自 Micromedex
Clopidogrel Metabolism 1.Hepatic: Extensive 2.Thiol derivative (major): Active; metabolism differs based on CYP2C19 genotype, affecting the degree of antiplatelet effect.(以前藥理藥化考這裡) A poor metabolizer has 2 nonfunctional alleles. The approximate frequencies of poor CYP2C19 metabolizer genotypes are 2% in white patients, 4% in Black patients, and 14% in Chinese patients 3.Clopidogrel: Substrate of CYP2C19, CYP1A2, CYP2B6, and CYP3A (現在臨藥考這裡) 4.Acyl-beta-glucuronide metabolite: Inhibitor of CYP2C8 (現在臨藥考這裡) |
(D)與gemfibrozil併用,會造成低血糖風險增加-->因為glucuronidation後的gemfibrozil是2C8的抑制劑,所以repaglinide血中濃度上升,低血糖風險增加。
主要由UGT2B7代謝, It undergoes oxidation of the ring methyl group in the liver to form an hydroxymethyl and a carboxyl metabolite. Inhibitor of CYP2C8,In vitro, gemfibrozil is only a weak inhibitor of CYP2C8, but glucuronidation converts gemfibrozil to a strong, irreversible, and selective CYP2C8 inhibitor. |
(B)