Leigh D A, Reeves D S, Simmons K, Thomas A L, Wilkinson P J
Br Med J. 1976 Jun 5;1(6022):1378-80. doi: 10.1136/bmj.1.6022.1378.
Talampicillin is a thiazolide carboxylic ester of ampicillin and is hydrolysed in the intestinal mucosa to release free ampicillin. The mean peak serum concentration of ampicillin occurred one hour after a dose of talampicillin and was about twice that attained by an equivalent dose of ampicillin. The presence of food in the stomach reduced and delayed the peak blood levels but did not affect the total amount of antibiotic absorbed or the urinary recovery. Talampicillin had less effect on the faecal flora in volunteers than ampicillin, and no overgrowth with Candida spp or Staphylococcus aureus was seen. Thirty-eight out of 47 urinary infections were eradicated by a seven-day course of talampicillin.
酞氨苄青霉素是氨苄青霉素的噻唑羧酸酯,在肠黏膜中水解后释放出游离的氨苄青霉素。服用酞氨苄青霉素后,氨苄青霉素的血清平均峰值浓度在1小时后出现,约为等量氨苄青霉素峰值浓度的两倍。胃内有食物会降低并延迟血药峰值水平,但不影响吸收的抗生素总量或尿回收率。与氨苄青霉素相比,酞氨苄青霉素对志愿者粪便菌群的影响较小,未观察到念珠菌属或金黄色葡萄球菌过度生长的情况。47例泌尿系统感染中有38例通过为期7天的酞氨苄青霉素疗程得以根除。