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第三代头孢菌素头孢三嗪(Ceftriaxone,Ⅰ)和头孢噻肟(Cefotaxime,Ⅱ)均具有较广的抗菌谱,但药代动力学表现有很大差别。实验显示,静注1g 药物后,Ⅱ血浓度达100 μg/ml,1 h 和2 h 血浓度分别迅速下降至15和5 μg/ml,t1/2β为1.1 h;而Ⅰ峰浓度达150～170μg/ml,2h 和12h 分别为100和35 μg/ml,24h 仍有10 μg/ml,t1/2β为8～9h。Wise 等比较了Ⅰ和Ⅱ的组织渗透性,给1 gⅡ后1 h,皮肤水泡中最高浓度为7μg/ml;给0.5g Ⅰ则在6h 达峰浓度32μg/ml,24h 仍有10μg/ml。作者测定了两种抗生素在血清和腹水的浓度,静注15mg/kg 时,Ⅰ血清峰浓度为177μg/ml,2 h 97μg/ml,24 h 16 μg/ml,平均t1/2β芦为13h,其腹水
The third generation ceftriaxone (Ceftriaxone, Ⅰ) and cefotaxime (Cefotaxime, Ⅱ) have a broad antibacterial spectrum, but the performance of pharmacokinetics are very different. The experimental results showed that after intravenous injection of 1 g of drug, the blood concentration of Ⅱ reached 100 μg / ml, the serum concentrations of 1 and 2 h dropped rapidly to 15 and 5 μg / ml, respectively, and the t1 / 2β was 1.1 h; 170μg / ml, 2h and 12h respectively 100 and 35 μg / ml, 24h still 10 μg / ml, t1 / 2β for 8 ~ 9h. Wise et al compared the tissue permeability of Ⅰ and Ⅱ, 1 h after 1 g Ⅱ, the highest concentration in skin blisters was 7 μg / ml; 0.5 g Ⅰ reached the peak concentration of 32 μg / ml at 6 h and 10 μg / ml at 24h. The authors measured the serum and ascitic fluid concentrations of two antibiotics at a dose of 15 mg / kg iv. Peak I serum concentrations were 177 μg / ml, 97 μg / ml for 2 h, 16 μg / ml for 24 h, 13 h for average t1 / Its ascites