78.承上題,該藥品須降低劑量的原因為下列何種酵素被抑制?
(A) CYP3A4
(B) monoamine oxidase
(C) xanthine oxidase
(D) aldehyde dehydrogenase
統計: A(166), B(63), C(3714), D(36), E(0) #882705
詳解 (共 3 筆)
B) Monoamine Oxidase Inhibitors, MAOIs(單胺氧化酶抑制) 為一類抑制單胺氧化酶作用的藥物。該類藥品在抑鬱症的治療中已有很長的一段歷史。 單胺是指Norepinephrine(NE)、Epinephrine、Serotonine(5-HT)、Tyramine
另外Azathioprine、 Mercaptopurine (6-MP)、Didanosine、Theophylline衍生物等,都是黃嘌呤氧化酶受質,合併使用Allopurinol或Febuxostat會提高上述藥物濃度。
D)抑制aldehyde dehydrogenase 的作用,可作為戒酒藥。如:Disulfiram
Allopurinol + azathioprine
Allopurinol,因抑制Xanthine Oxidase,可導致Azathioprine衍生物濃度上升
AZA代謝途徑包括XO,與allopurinol 並用會增加AZA 濃度
the metabolism of mercaptopurine (MP), or its prodrug azathioprine (AZA), occurs via 3 primary pathways: oxidation to inactive thiouric acid catalyzed by xanthine oxidase (XO); methylation to inactive methyl-mercaptopurine catalyzed by thiopurine S-methyl transferase (TPMT); and activation to thioguanine nucleotides in a process initiated by hypoxanthine-guanine phosphoribosyl transferase.
Inhibition of XO by allopurinol may increase systemic MP exposure and toxicity, particularly via inhibition of its presystemic metabolism.
US prescribing information for most MP and AZA products recommends a dose reduction of two-thirds to three-quarters when used with allopurinol in order to reduce this risk of toxicity.
UpToDate Lexicomp Azathioprine / Allopurinol