MacGowan A P, Bowker K E
Bristol Centre for Antimicrobial Research and Evaluation, Southmead Health Services NHS Trust, England.
Clin Pharmacokinet. 1998 Nov;35(5):391-402. doi: 10.2165/00003088-199835050-00004.
There are considerable laboratory data and information from animal and continuous culture in vitro models to support continuous infusion therapy for penicillins and cephalosporins, but, as yet, the only existing clinical data relate to cephalosporins. Penicillins do not exert concentration-dependent killing in the therapeutic range but have a post-antibiotic effect (PAE) against Gram-positive cocci but not Gram-negative rods. Animal models indicate the time (T) during which the serum concentrations exceed the minimum inhibitory concentration (MIC) of the pathogen [T > MIC] determines outcomes. Pharmacokinetic studies in humans indicate that continuous infusion with penicillins is possible but there are no clinical data on efficacy. Cephalosporins have similar pharmacodynamic properties to penicillins; T > MIC determines outcome. Data related to ceftazidime indicate that the drug concentration at steady-state (Css) should exceed the pathogen MIC by > 1-fold and perhaps by 4- to 5-fold or more. Human pharmacokinetics of ceftazidime administered by continuous infusion to a wide variety of patient groups indicates that Css of > 20 mg/L can easily be achieved using conventional daily doses. Clinical data indicate increased effectiveness of a continuous regimen in neutropenic patients with Gram-negative infection. Furthermore cefuroxime administration by continuous infusion has resulted in lower doses and shorter course durations. Little is known of the pharmacodynamics of monobactams and there are few clinical data on continuous infusion therapy. Carbapenems have different pharmacodynamics to other beta-lactams as they have concentration-dependent killing and a PAE with both Gram-positive and Gram-negative bacteria. While T > MIC has a role in determining outcomes, the proportion of the dosing interval for which serum drug concentrations should exceed the pathogen MIC is less than for other beta-lactams. In vitro models have shown that continuous infusion is effective, as is less frequent dosing. There are few data on continuous infusion of carbapenems but some patients have been treated with once-daily dosing. Clinically, continuous infusion therapy with penicillins and cephalosporins should be considered in patients infected with susceptible Gram-negative rods not responding to conventional therapy. As an approximation, the same total daily dose should be given but a bolus intravenous injection should be give at the start of continuous infusion to ensure Css is reached rapidly. The Css may be difficult to predict and determination of serum drug concentrations may be indicated. Ideally, the Css should be calculated based on the MIC of the potential pathogen and may be higher or lower than the Css achieved by a conventional daily dose.
有大量来自动物实验和体外连续培养模型的实验室数据及信息支持青霉素和头孢菌素的持续输注疗法,但目前仅有的临床数据与头孢菌素相关。青霉素在治疗范围内不呈现浓度依赖性杀菌作用,不过对革兰氏阳性球菌有抗生素后效应(PAE),对革兰氏阴性杆菌则没有。动物模型表明血清浓度超过病原体最低抑菌浓度(MIC)的时间(T)[T > MIC]决定治疗结果。人体药代动力学研究表明青霉素持续输注是可行的,但尚无关于疗效的临床数据。头孢菌素具有与青霉素相似的药效学特性;T > MIC决定治疗结果。与头孢他啶相关的数据表明稳态时的药物浓度(Css)应超过病原体MIC的1倍以上,或许为4至5倍或更高。对各类患者群体持续输注头孢他啶的人体药代动力学研究表明,使用常规日剂量很容易实现Css > 20 mg/L。临床数据表明持续给药方案对革兰氏阴性菌感染的中性粒细胞减少患者疗效更佳。此外,持续输注头孢呋辛可降低剂量并缩短疗程。关于单环β-内酰胺类药物的药效学知之甚少,持续输注疗法的临床数据也很少。碳青霉烯类药物与其他β-内酰胺类药物的药效学不同,因为它们具有浓度依赖性杀菌作用,且对革兰氏阳性菌和革兰氏阴性菌均有PAE。虽然T > MIC在决定治疗结果方面有作用,但血清药物浓度应超过病原体MIC的给药间隔比例低于其他β-内酰胺类药物。体外模型表明持续输注是有效的,较少频次给药也是如此。关于碳青霉烯类药物持续输注的数据很少,但已有一些患者接受每日一次给药治疗。临床上,对于感染了对常规治疗无反应的敏感革兰氏阴性杆菌的患者,应考虑采用青霉素和头孢菌素持续输注疗法。大致而言,应给予相同的每日总剂量,但在持续输注开始时应静脉推注一次以确保迅速达到Css。Css可能难以预测,可能需要测定血清药物浓度。理想情况下,应根据潜在病原体的MIC计算Css,其可能高于或低于常规日剂量所达到的Css。