Alvarez-Elcoro S, Enzler M J
Division of Infectious Diseases and Internal Medicine, Mayo Clinic Jacksonville, Florida, USA.
Mayo Clin Proc. 1999 Jun;74(6):613-34. doi: 10.4065/74.6.613.
In addition to erythromycin, macrolides now available in the United States include azithromycin and clarithromycin. These two new macrolides are more chemically stable and better tolerated than erythromycin, and they have a broader antimicrobial spectrum than erythromycin against Mycobacterium avium complex (MAC), Haemophilus influenzae, nontuberculous mycobacteria, and Chlamydia trachomatis. All three macrolides have excellent activity against the atypical respiratory pathogens (C. pneumoniae and Mycoplasma species) and the Legionella species. Azithromycin and clarithromycin have pharmacokinetics that allow shorter dosing schedules because of prolonged tissue levels. Both azithromycin and clarithromycin are active agents for MAC prophylaxis in patients with late-stage acquired immunodeficiency syndrome (AIDS), although azithromycin may be the preferable agent because of fewer drug-drug interactions. Clarithromycin is the most active MAC antimicrobial agent and should be part of any drug regimen for treating active MAC disease in patients with or without AIDS. Although both azithromycin and clarithromycin are well tolerated by children, azithromycin has the advantage of shorter treatment regimens and improved tolerance, potentially improving compliance in the treatment of respiratory tract and skin or soft tissue infections. Intravenously administered azithromycin has been approved for treatment of adults with mild to moderate community-acquired pneumonia or pelvic inflammatory diseases. An area of concern is the increasing macrolide resistance that is being reported with some of the common pathogens, particularly Streptococcus pneumoniae, group A streptococci, and H. influenzae. The emergence of macrolide resistance with these common pathogens may limit the clinical usefulness of this class of antimicrobial agents in the future.
除红霉素外,美国目前可用的大环内酯类药物还包括阿奇霉素和克拉霉素。这两种新型大环内酯类药物在化学性质上比红霉素更稳定,耐受性更好,并且在抗鸟分枝杆菌复合群(MAC)、流感嗜血杆菌、非结核分枝杆菌和沙眼衣原体方面比红霉素具有更广泛的抗菌谱。所有三种大环内酯类药物对非典型呼吸道病原体(肺炎衣原体和支原体属)以及军团菌属均具有出色的活性。阿奇霉素和克拉霉素的药代动力学特性使得给药方案可以更短,因为其组织浓度维持时间更长。阿奇霉素和克拉霉素都是晚期获得性免疫缺陷综合征(AIDS)患者预防MAC的有效药物,不过由于药物相互作用较少,阿奇霉素可能是更优选的药物。克拉霉素是最有效的抗MAC抗菌药物,应成为治疗有或无AIDS患者的活动性MAC疾病的任何药物治疗方案的一部分。尽管阿奇霉素和克拉霉素在儿童中耐受性都很好,但阿奇霉素具有治疗方案更短和耐受性更好的优势,这可能会提高呼吸道以及皮肤或软组织感染治疗的依从性。静脉注射阿奇霉素已被批准用于治疗轻度至中度社区获得性肺炎或盆腔炎的成人患者。一个令人担忧的问题是,一些常见病原体,特别是肺炎链球菌、A组链球菌和流感嗜血杆菌,对大环内酯类药物的耐药性正在增加。这些常见病原体对大环内酯类药物耐药性的出现可能会限制这类抗菌药物在未来的临床应用。