Rosenblatt J E, Edson R S
Division of Infectious Diseases and Internal Medicine, Mayo Clinic.
Mayo Clin Proc. 1987 Nov;62(11):1013-7. doi: 10.1016/s0025-6196(12)65074-5.
Metronidazole, a nitroimidazole derivative, is a unique antimicrobial agent that is active against both bacterial and parasitic organisms, although only the anaerobic members of these groups are susceptible. It has been used for the treatment of trichomoniasis for almost 30 years and is also effective in amebiasis and giardiasis. More recently, metronidazole has emerged as a principal agent for the treatment of anaerobic infections. It is highly effective against all species of anaerobes except certain non-spore-forming gram-positive bacilli and cocci and is the only agent rapidly bactericidal against the Bacteroides fragilis group. The hydroxy metabolite is 65% as effective as metronidazole and may play a major therapeutic role. Clinical studies have substantiated its efficacy for prophylaxis during elective colorectal surgical procedures and the treatment of deep abdominal sepsis (usually in combination with another agent such as an aminoglycoside). Metronidazole is the treatment of choice for bacterial vaginosis and seems to be as effective as vancomycin for treatment of Clostridium difficile-related diarrhea and colitis. Good blood levels are produced after both oral and intravenous administration, and side effects are infrequent and minimal. Metronidazole should not be taken during the first trimester of pregnancy because of concerns about mutagenicity. Tinidazole and ornidazole are recently developed nitroimidazole derivatives that have even greater antimicrobial activity than metronidazole.
甲硝唑是一种硝基咪唑衍生物,是一种独特的抗菌药物,对细菌和寄生虫均有活性,不过只有这些菌群中的厌氧菌敏感。它用于治疗滴虫病已有近30年历史,对阿米巴病和贾第虫病也有效。最近,甲硝唑已成为治疗厌氧菌感染的主要药物。它对除某些无芽孢革兰氏阳性杆菌和球菌外的所有厌氧菌均高度有效,是唯一对脆弱拟杆菌属有快速杀菌作用的药物。其羟基代谢产物的效力为甲硝唑的65%,可能起主要治疗作用。临床研究证实了其在择期结直肠手术期间预防感染以及治疗深部腹部脓毒症(通常与另一种药物如氨基糖苷类联合使用)方面的疗效。甲硝唑是细菌性阴道病的首选治疗药物,对于艰难梭菌相关性腹泻和结肠炎的治疗似乎与万古霉素一样有效。口服和静脉给药后均可产生良好的血药浓度,副作用很少且轻微。由于担心有致突变性,妊娠头三个月不应服用甲硝唑。替硝唑和奥硝唑是最近开发的硝基咪唑衍生物,其抗菌活性比甲硝唑更强。