Dunn C J, Barradell L B
Adis International Limited, Auckland, New Zealand.
Drugs. 1996 Mar;51(3):483-505. doi: 10.2165/00003495-199651030-00013.
The azalide antibacterial agent azithromycin is a semisynthetic acid-stable erythromycin derivative with an expanded spectrum of activity and improved tissue pharmacokinetic characteristics relative to erythromycin. The drug is noted for its activity against some Gram-negative organisms associated with respiratory tract infections, particularly Haemophilus influenzae. Azithromycin has similar activity to other macrolides against Streptococcus pneumoniae and Moraxella catarrhalis, and is active against atypical pathogens such as Legionella pneumophila, Chlamydia pneumoniae and Mycoplasma pneumoniae. Once-daily administration of azithromycin is made possible by the long elimination half-life of the drug from tissue. Azithromycin is rapidly and highly concentrated in a number of cell types after absorption, including leucocytes, monocytes and macrophages. It undergoes extensive distribution into tissue, from where it is subsequently eliminated slowly. A 3-day oral regimen of once-daily azithromycin has been shown to be as effective as 5- to 10-day courses of other more frequently administered antibacterial agents [such as erythromycin, amoxicillin-clavulanic acid and phenoxymethylpenicillin (penicillin V)] in patients with acute exacerbations of chronic bronchitis, pneumonia, sinusitis, pharyngitis, tonsillitis and otitis media. Adverse effects of azithromycin are mainly gastrointestinal in nature and occur less frequently than with erythromycin. Azithromycin is likely to prove most useful as a 3-day regimen in the empirical management of respiratory tract infections in the community. Its ease of administration and 3-day duration of therapy, together with its good gastrointestinal tolerability, should optimise patient compliance (the highest level of which is achieved with once-daily regimens). Azithromycin is also likely to be useful in the hospital setting, particularly for outpatients and for those unable to tolerate erythromycin.
氮杂内酯类抗菌药物阿奇霉素是一种半合成的、对酸稳定的红霉素衍生物，其抗菌谱比红霉素更广，组织药代动力学特性也有所改善。该药物以对一些与呼吸道感染相关的革兰氏阴性菌具有活性而闻名，尤其是流感嗜血杆菌。阿奇霉素对肺炎链球菌和卡他莫拉菌的活性与其他大环内酯类药物相似，并且对非典型病原体如嗜肺军团菌、肺炎衣原体和肺炎支原体也有活性。由于该药物从组织中的消除半衰期较长，所以可以每日给药一次。阿奇霉素吸收后能迅速且高度集中于多种细胞类型中，包括白细胞、单核细胞和巨噬细胞。它在组织中广泛分布，随后从组织中缓慢消除。在慢性支气管炎急性加重、肺炎、鼻窦炎、咽炎、扁桃体炎和中耳炎患者中，每日一次服用阿奇霉素的3日口服方案已被证明与其他更频繁给药的抗菌药物（如红霉素、阿莫西林 - 克拉维酸和苯氧甲基青霉素（青霉素V））的5至10日疗程一样有效。阿奇霉素的不良反应主要是胃肠道方面的，且比红霉素发生的频率更低。在社区呼吸道感染的经验性治疗中，阿奇霉素作为3日疗程可能最为有用。其给药方便、疗程为3天，加上良好的胃肠道耐受性，应能优化患者的依从性（每日一次给药方案的依从性最高）。阿奇霉素在医院环境中也可能有用，特别是对于门诊患者以及那些不能耐受红霉素的患者。
