Bakheit Ahmed H H, Al-Hadiya Badraddin M H, Abd-Elgalil Ahmed A
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia.
Department of Pharmaceutical Chemistry, College of Pharmacy, Taif University, TAIF, KSU.
Profiles Drug Subst Excip Relat Methodol. 2014;39:1-40. doi: 10.1016/B978-0-12-800173-8.00001-5.
Azithromycin is an azalide, a subclass of macrolide antibiotics. It is derived from erythromycin, with a methyl-substituted nitrogen atom incorporated into the lactone ring, thus making the lactone ring 15-membered. It prevents bacteria from growing by interfering with their protein synthesis. It binds to the 50S subunit of the bacterial ribosome and thus inhibits translation of mRNA. Azithromycin is used to treat or prevent certain bacterial infections, most often those causing middle ear infections, strep throat, pneumonia, typhoid, bronchitis, and sinusitis. In recent years, it has been used primarily to prevent bacterial infections in infants and those with weaker immune systems. It is also effective against certain sexually transmitted infections, such as nongonococcal urethritis, chlamydia, and cervicitis. Recent studies have indicated it also to be effective against late-onset asthma, but these findings are controversial and not widely accepted. The present study gives a comprehensive profile of azithromycin, including detailed physico-chemical properties, nomenclature, formulae, methods of preparation, and methods of analysis (including compendial, electrochemical, spectroscopic, and chromatographic methods of analysis). Developed validated stability-indicating (HPLC and biodiffusion assay methods under accelerated acidic, alkaline, and oxidative conditions, in addition to effect of different types of light, temperature, and pH. Detailed clinical applications also presented (mechanism of action, ADME profile, clinical uses and doses, side effects, and drug interactions). Each of the above stages includes appropriate figures and tables. More than 80 references were given as a proof of the above-mentioned studies.
阿奇霉素是一种氮杂内酯类药物,属于大环内酯类抗生素的一个亚类。它由红霉素衍生而来,在内酯环中引入了一个甲基取代的氮原子,从而使内酯环为15元环。它通过干扰细菌的蛋白质合成来阻止细菌生长。它与细菌核糖体的50S亚基结合,从而抑制mRNA的翻译。阿奇霉素用于治疗或预防某些细菌感染,最常见的是引起中耳感染、链球菌性咽喉炎、肺炎、伤寒、支气管炎和鼻窦炎的感染。近年来,它主要用于预防婴儿和免疫系统较弱者的细菌感染。它对某些性传播感染也有效,如非淋菌性尿道炎、衣原体感染和宫颈炎。最近的研究表明它对迟发性哮喘也有效,但这些发现存在争议,尚未被广泛接受。本研究全面介绍了阿奇霉素,包括详细的物理化学性质、命名、分子式、制备方法和分析方法(包括药典、电化学、光谱和色谱分析方法)。开发了经过验证的稳定性指示方法(在加速的酸性、碱性和氧化条件下的高效液相色谱法和生物扩散测定法,以及不同类型的光、温度和pH的影响)。还介绍了详细的临床应用(作用机制、药代动力学特征、临床用途和剂量、副作用及药物相互作用)。上述每个阶段都包含适当的图表。给出了80多篇参考文献以证明上述研究。