Zhanel George G, Ketter Nzeera, Rubinstein Ethan, Friedland Ian, Redman Rebecca
Department of Medical Microbiology and Infectious Diseases, Faculty of Medicine, University of Manitoba, Winnipeg, Manitoba, Canada.
Drug Saf. 2009;32(9):709-16. doi: 10.2165/00002018-200932090-00001.
The seizure-inducing potential of carbapenems has been debated since the introduction of imipenem/cilastatin over 20 years ago. Doripenem is a new carbapenem, recently approved in the US for the treatment of adults with complicated urinary tract infections (cUTI) or complicated intra-abdominal infections (cIAI), and additionally in the EU for nosocomial pneumonia, including ventilator-associated pneumonia. Here, the seizure-inducing potential of doripenem is evaluated, using data from in vitro and in vivo animal studies, doripenem clinical trials and doripenem postmarketing reports of seizures. Animal studies indicate that doripenem has low binding affinity for GABA receptors and does not induce seizures at doses greater than seizure-inducing doses of imipenem or meropenem. In clinical studies of cUTI or cIAI, no seizures were reported in the 1332 patients treated with doripenem (500-mg infusion every 8 hours). In two studies, patients with nosocomial pneumonia were treated with doripenem 500 mg (1- or 4-hour infusion every 8 hours), and the incidence of seizures was lower for doripenem (1.2% [6/485]) than imipenem (3.8% [10/263]) or piperacillin/tazobactam (2.7% [6/221]). For patients with seizure-predisposing conditions, seizures occurred during treatment for 3/193 (1.5%) in doripenem, 1/66 (1.5%) in piperacillin/tazobactam and 6/116 (5.2%) in the imipenem group. The review of data from both clinical trials and postmarketing surveillance supports the low seizure-inducing potential of doripenem. The seizure potential of doripenem should be evaluated further in patients at increased risk for seizure.
自20多年前亚胺培南/西司他丁问世以来,碳青霉烯类药物的致癫痫潜力一直存在争议。多利培南是一种新型碳青霉烯类药物,最近在美国被批准用于治疗患有复杂性尿路感染(cUTI)或复杂性腹腔内感染(cIAI)的成人患者,在欧盟还被批准用于治疗医院获得性肺炎,包括呼吸机相关性肺炎。在此,利用来自体外和体内动物研究、多利培南临床试验以及多利培南上市后癫痫报告的数据,对多利培南的致癫痫潜力进行评估。动物研究表明,多利培南对GABA受体的结合亲和力较低,在高于亚胺培南或美罗培南致癫痫剂量的情况下不会诱发癫痫。在cUTI或cIAI的临床研究中,接受多利培南治疗的1332例患者(每8小时静脉输注500 mg)均未报告癫痫发作。在两项研究中,医院获得性肺炎患者接受多利培南500 mg治疗(每8小时输注1或4小时),多利培南组的癫痫发生率(1.2%[6/485])低于亚胺培南组(3.8%[10/263])或哌拉西林/他唑巴坦组(2.7%[6/221])。对于有癫痫诱发因素的患者,多利培南治疗期间癫痫发作的发生率为3/193(1.5%),哌拉西林/他唑巴坦组为1/66(1.5%),亚胺培南组为6/116(5.2%)。对临床试验和上市后监测数据的审查支持多利培南致癫痫潜力较低的观点。对于癫痫风险增加的患者,应进一步评估多利培南的癫痫发作潜力。