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[答]磺胺类药吸收到体内后,一部分在肝脏中代谢,通过乙酰基转移酶将乙酰辅酶A的乙酰基团转移到药物上,变成乙酰化磺胺,有少量在血液或肾脏内乙酰化。各种磺胺药乙酰化的程度占摄入体内的磺胺药总量的百分比称之为磺胺药的乙酰化率。磺胺药乙酰化程度是评价磺胺药优缺点的一个重要指标。因为:①磺胺药乙酰化以后变成乙酰磺胺,即失去抗菌作用,乙酰化率高的磺胺药在体内抗菌作用减弱;②乙酰磺胺在尿中溶解度多降低,容易在肾小管析出结晶,引起结晶尿、血尿。因此,乙酰化率低的磺胺药在尿中溶解度较高,对肾脏损害小。现将常用的几种磺胺药在体内的乙酰化率概述如下:
[Answer] Sulfa drugs absorbed into the body, part of the metabolism in the liver, by acetyltransferase acetyl acetyl CoA acetyl group transferred to drugs, into acetylated sulfonamides, a small amount of acetylation in the blood or kidneys . The degree of acetylation of various sulfonamides accounts for the percentage of total sulfonamide intake in the body as the acetylation rate of sulfonamides. The degree of acetylation of sulfa drugs is an important indicator to evaluate the advantages and disadvantages of sulfa drugs. Because: sulfonamides after acetylsalicylic acid into the loss of antibacterial effect, the high rate of acetylation sulfa drugs in vivo antibacterial effect weakened; (2) acetaminophen in the urine more soluble, easy to precipitate in the renal tubular crystallization, causing crystallization Urine, hematuria. Therefore, the low rate of acetylation sulfa drugs in the urine of high solubility, damage to the kidneys small. Now several commonly used sulfonamides in vivo acetylation rate is summarized as follows: