Avilés Santa M L, Ramírez-Ronda C H
Infectious Diseases Program, University of Puerto Rico School of Medicine, San Juan VA Medical Center 00927-5800.
Bol Asoc Med P R. 1992 Jan;84(1):21-5.
After almost forty years of its introduction, erythromycin will not be the exclusive member of the macrolide group of antibiotic agents, but a new generation of its derivatives which surpass it in pharmacological properties and clinical efficacy will also be available. Clarithromycin, a 14-membered derivative, has shown acid stability, longer half-life, lower protein binding and higher lung tissue penetration. Its exceedingly high activity against erythromycin-susceptible gram-positive cocci, Mycoplasma pneumoniae, and Legionella pneumophila makes it and important alternative choice in the therapy of respiratory tract infections. Also, it has shown high activity against Chlamydia trachomatis, and high urinary clearance of this unmetabolized molecule, important properties which would render it a special role in the treatment of genitourinary tract infections. Azithromycin, a 15-membered derivative has shown enhanced basicity (due to the nitrogen atom in its lactone ring), longer half-life and lower protein bindings. Its exceptional activity against Hemophilus influenzae, Branhamella catarrhalis, Neisseria gonorrhoeae, Ureaplasma urealyticum and gram-negative bacteria, and its high concentration in tonsillar, pulmonary, prostatic and female reproductive tract tissues, assigns it an honorific place among the macrolides in the therapy against respiratory tract and genitourinary tract infections. Its role against T. gondii deserves further study, but points out this agent as a promise against this parasite.
在引入近四十年后,红霉素将不再是大环内酯类抗生素中的唯一成员,新一代在药理特性和临床疗效上优于它的衍生物也将问世。克拉霉素,一种14元环衍生物,已显示出酸稳定性、更长的半衰期、更低的蛋白结合率以及更高的肺组织穿透力。它对红霉素敏感的革兰氏阳性球菌、肺炎支原体和嗜肺军团菌具有极高活性,使其成为呼吸道感染治疗中的重要替代选择。此外,它对沙眼衣原体显示出高活性,且该未代谢分子的尿清除率高,这些重要特性使其在泌尿生殖道感染治疗中具有特殊作用。阿奇霉素,一种15元环衍生物,已显示出增强的碱性(由于其内酯环中的氮原子)、更长的半衰期和更低的蛋白结合率。它对流感嗜血杆菌、卡他布兰汉菌、淋病奈瑟菌、解脲脲原体及革兰氏阴性菌具有特殊活性,且在扁桃体、肺、前列腺和女性生殖道组织中浓度高,这使其在治疗呼吸道和泌尿生殖道感染的大环内酯类药物中占据重要地位。其对弓形虫的作用值得进一步研究,但表明该药物有望对抗这种寄生虫。