Garey K W, Amsden G W
Department of Pharmacy, Bassett Healthcare, Cooperstown, NY 13326, USA.
Ann Pharmacother. 1999 Feb;33(2):218-28. doi: 10.1345/aph.18046.
To review the pharmacology, microbiology, chemistry, pharmacokinetics, efficacy, safety, tolerability, dosage, administration, and economic issues of intravenous azithromycin.
A MEDLINE search from 1978 to May 1998 of the English-language literature and an extensive review of journals and meeting abstracts was conducted. Due to the lack of published literature concerning the efficacy, safety, and pharmacokinetics of the intravenous formulation of azithromycin, the manufacturer was also contacted and requested to supply information concerning intravenous azithromycin.
In vitro and preclinical studies were included, as well as data from Phase II and III clinical trials. Efficacy, pharmacokinetic, safety, and tolerability data were also supplemented with information from the manufacturer, due to the lack of published reports.
Azithromycin, an azalide subclass of the macrolide antibiotics, is now available as an intravenous formulation. The intravenous form is approved for the treatment of community-acquired pneumonia caused by Chlamydia pneumoniae, Haemophilus influenzae. Legionella pneumophila, Moraxella catarrhalis, Mycoplasma pneumoniae, Staphylococcus aureus (methicillin-sensitive), and Streptococcus pneumoniae, and for the treatment of pelvic inflammatory disease caused by Chlamydia trachomatis, Neisseria gonorrhoeae, and Mycoplasma hominis in situations in which intravenous therapy is required. Its spectrum of activity, unique pharmacokinetics, and high and sustained tissue penetration allow for once-daily dosing with monotherapy in many cases. Clinical and bacteriologic response rates as well as the adverse event profile have been similar to or better than comparative agents.
Azithromycin offers advantages over other agents due to its unique pharmacokinetics, high and sustained tissue penetration, and spectrum of activity. This allows for monotherapy and once-daily intravenous dosing for mild-to-moderate community-acquired pneumonia or pelvic inflammatory disease in many instances. Future research should focus on total duration of antibiotic therapy and the need, or lack thereof, for extensive oral antibiotic follow-up.
综述静脉注射阿奇霉素的药理学、微生物学、化学、药代动力学、疗效、安全性、耐受性、剂量、给药方式及经济学问题。
检索了1978年至1998年5月的MEDLINE英文文献，并广泛查阅了期刊和会议摘要。由于缺乏关于阿奇霉素静脉制剂疗效、安全性和药代动力学的已发表文献，还联系了制造商并要求提供有关静脉注射阿奇霉素的信息。
纳入了体外和临床前研究以及II期和III期临床试验的数据。由于缺乏已发表的报告，疗效、药代动力学、安全性和耐受性数据还补充了制造商提供的信息。
阿奇霉素是大环内酯类抗生素的氮杂内酯亚类，现已制成静脉制剂。该静脉制剂被批准用于治疗由肺炎衣原体、流感嗜血杆菌、嗜肺军团菌、卡他莫拉菌肺炎支原体、金黄色葡萄球菌（对甲氧西林敏感）和肺炎链球菌引起的社区获得性肺炎，以及在需要静脉治疗的情况下，用于治疗由沙眼衣原体、淋病奈瑟菌和解脲脲原体引起的盆腔炎。其活性谱、独特的药代动力学以及高且持续的组织穿透力使得在许多情况下单药治疗时每日给药一次成为可能。临床和细菌学反应率以及不良事件情况与对照药物相似或更佳。
阿奇霉素因其独特的药代动力学、高且持续的组织穿透力以及活性谱，相较于其他药物具有优势。这使得在许多情况下，对于轻至中度社区获得性肺炎或盆腔炎可采用单药治疗且每日一次静脉给药。未来的研究应聚焦于抗生素治疗的总时长以及是否需要（或无需）进行广泛的口服抗生素后续治疗。
