Vane F M, Buggé J L, Rodriguez L C
Research Division, Hoffmann-La Roche Inc., Nutley, NJ 07110.
Drug Metab Dispos. 1989 May-Jun;17(3):280-5.
Five metabolites were isolated from the blood of psoriatic patients on chronic therapy with etretinate (Tegison). The two major metabolites were the all-trans acid (acitretin) and the 13-cis acid (isoacitretin), both of which had been previously identified as major metabolites of etretinate in human blood. The other three metabolites had not been previously reported in human blood. One metabolite corresponded to isoacitretin with a hydroxy group on an aromatic methyl group. The other two metabolites had acid side chains shortened by one carbon and a reduced 11, 12-double bond. One of the two metabolites retained the aromatic methoxy group, whereas the other was the phenolic analog.
从长期服用依曲替酯(银屑灵)的银屑病患者血液中分离出了5种代谢产物。两种主要代谢产物是全反式酸(阿维A)和13 - 顺式酸(异阿维A),这两种产物先前已被确定为依曲替酯在人体血液中的主要代谢产物。另外三种代谢产物此前未在人体血液中报道过。一种代谢产物是在芳族甲基上带有羟基的异阿维A。另外两种代谢产物的酸侧链缩短了一个碳原子,且11、12位双键减少。这两种代谢产物中的一种保留了芳族甲氧基,而另一种是酚类类似物。