Estey E H, Weaver S S, LeBlanc B M, Brown N, Ho D H, Bodey G P
Clin Pharmacol Ther. 1981 Sep;30(3):396-403.
Pharmacologic studies of the semisynthetic cephalosporin ceforanide were conducted in 29 cancer patients. Intravenous doses of 500 mg over 30 min every 6 hr to 10 patients induced mean peak serum concentrations between 44.7 and 51.5 micrograms/ml, while in 10 patients receiving 1 gm over 30 min every 12 hr mean peak serum concentrations varied from 73.4 to 91.8 micrograms/ml. Twelve hours after 1 gm of drug, mean serum concentrations varied between 5.6 and 6.5 micrograms/ml. After a 500-mg loading dose, continuous infusion of 500 mg every 4 hr, 10 patients maintained serum concentrations above 34.2 micrograms/ml for 7 or 8 days. Most of the drug was excreted in the urine in the initial 6 hr after administration and mean urinary concentration of 1,315 micrograms/ml were obtained during this time. Serum half-life ranged between 2.2 and 2.9 hr on all schedules and therefore wa longer than that of other cephalosporins. No serious toxicity was noted. The relatively broad spectrum of activity in addition to the long half-life suggests clinical utility for this drug.
对29名癌症患者进行了半合成头孢菌素头孢雷特的药理学研究。10名患者每6小时静脉注射500毫克,持续30分钟,诱导的血清平均峰值浓度在44.7至51.5微克/毫升之间,而10名患者每12小时静脉注射1克,持续30分钟,血清平均峰值浓度在73.4至91.8微克/毫升之间变化。注射1克药物12小时后,血清平均浓度在5.6至6.5微克/毫升之间变化。给予500毫克负荷剂量后,每4小时持续输注500毫克,10名患者的血清浓度在7天或8天内维持在34.2微克/毫升以上。大部分药物在给药后的最初6小时内从尿液中排出,在此期间尿平均浓度达到1315微克/毫升。在所有给药方案下,血清半衰期在2.2至2.9小时之间,因此比其他头孢菌素的半衰期长。未观察到严重毒性。除半衰期长外,相对广泛的活性谱表明该药物具有临床应用价值。