METAMPICILLIN - ANTIBACTERIAL ACTIVITY AND ABSORPTION AND EXCRETION IN MAN
METAMPICILLIN - ANTIBACTERIAL ACTIVITY AND ABSORPTION AND EXCRETION IN MAN
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DOI：
10.1159/000220849
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发表时间：
1972-01-01
期刊：
影响因子：
3.3
通讯作者：
ELSON, S
中科院分区：
文献类型：
--
作者：
SUTHERLAND, R;CROYDON, EAP;ELSON, S
氨苄西林是由氨苄西林与甲醛反应而成的青霉素，在水溶液中水解制得氨苄西林。在酸性条件下，水解率较高，中性介质中水解率较低，在人血清中则不完全。在体外，氨苄西林显示出与氨苄西林相似的光谱和活性水平，两种化合物对青霉素酶产生菌都没有活性。人血清对氨苄西林的活性有明显的抑制作用，在人血清存在下，该化合物的活性低于氨苄西林。口服甲氨苄西林后，在血液和尿液中均未检测到甲氨苄西林，在这些受试者中仅检测到氨苄西林。口服甲氨苄西林后产生的氨苄西林血药浓度略低于同等剂量的氨苄西林。肌注美他西林(肌肉注射)给志愿者服用药物后，受试者的血液中同时出现了氨苄西林和甲氨西林，而尿液中只出现了氨苄西林。
Metampicillin, the penicillin prepared by the reaction of ampicillin with formaldehyde, hydrolysed in aqueous solution with the formation of ampicillin. Hydrolysis was rapid under acid conditions, less rapid in neutral medium, and was incomplete in human serum. Metampicillin showed a spectrum and level of activity similar to that of ampicillinin vitro,and both compounds were inactive against penicillinase-producing strains of bacteria. The activity of metampicillin was markedly reduced by human serum, and the compound was less active than ampicillin in the presence of human serum. Following the oral administration of metampicillin to man, metampicillin was not detected in the blood stream nor in urine, and ampicillin alone was demonstrated in these subjects. The serum concentrations of ampicillin that were produced following the oral administration of metampicillin were somewhat lower than those obtained with equivalent doses of ampicillin. Adminstration of metampicillin by the intramuscular (i.m.) route to volunteers resulted in the appearance of both ampicillin and metampicillin in the blood, and of ampicillin alone in the urine of these subjects.