论文部分内容阅读
一些带有伯氨基或肼基的药物,在机体内可直接通过N-乙酰化途径进行代谢。乙酰化过程在乙酰辅酶A依赖的N-乙酰基转移酶催化下进行。六十年代以来,逐步发现药物在体内的乙酰化有两种类型。一类以异烟肼为代表,包括异烟肼、肼苯哒嗪、普鲁卡因酰胺、磺胺二甲嘧啶、氨苯砜和苯乙肼等,乙酰化速率在个体间差异较大,在人群中具有多型乙酰化机理(Poly-morphic acetylation)。另一类如氨基水杨酸、对氨基苯甲酸和某些磺胺药,乙酰化速率在个体之间差异不大,没有多型乙酰化机理。
Some drugs with primary or hydrazino groups can be directly metabolized by the N-acetylation pathway in the body. Acetylation is catalyzed by acetyl-CoA-dependent N-acetyltransferase. Since the 1960s, two types of drugs have been gradually found to be acetylated in the body. A class of isoniazid, including isoniazid, hydralazine, procaine amide, sulfamethazine, dapsone and phenelzine, the acetylation rate varies widely between individuals, in the The population has a polytype acetylation mechanism (Poly-morphic acetylation). Another group such as aminosalicylic acid, p-aminobenzoic acid and some sulfonamides, acetylation rate was not significantly different among individuals, there is no multi-type acetylation mechanism.