Portier H, Buisson M, Chavanet P
Service des maladies infectieuses et tropicales, CHU du Bocage, Dijon.
Rev Prat. 1994 Jun 15;44(12):1629-34.
The macrolides are still widely used in general practice and the new 14- or 15 membered-ring compounds-roxithromycin, clarithromycin, dirithromycin, azithromycin -may offer a new development. Their antibacterial activity is similar to erythromycin but azithromycin is more active against Gram negative strams. Roxythromycin exhibits high serum concentrations; azithromycin and dirithromycin present low serum concentrations but prolonged half-lives allowing a reduction of the duration of treatment particularly for pharyngitis (azithromycin). Macrolides are less useful for otitis and sinusitis treatment since their activity against H. influenzae and S. pneumoniae are weak. The activity against atypical bacteria justify their choice as first line treatment for benign atypical pneumonia of healthy young adults and for sexually transmitted diseases. In AIDS, these compounds are indicated in mycobacteriosis (clarithromycin), bacillary angiomatosis and excavated pneumonia due to Rhodococcus equi. Clinical tolerance is very good, particularly the gastro-intestinal one. The reported drug interactions are those of this class of antibiotics.
大环内酯类药物仍广泛应用于普通医疗实践中,新型的14或15元环化合物——罗红霉素、克拉霉素、地红霉素、阿奇霉素——可能代表了一个新的发展方向。它们的抗菌活性与红霉素相似,但阿奇霉素对革兰氏阴性菌更具活性。罗红霉素血清浓度较高;阿奇霉素和地红霉素血清浓度较低,但半衰期延长,尤其对于咽炎(阿奇霉素)而言,可缩短治疗疗程。大环内酯类药物对中耳炎和鼻窦炎的治疗效果欠佳,因为它们对流感嗜血杆菌和肺炎链球菌的活性较弱。其对非典型细菌的活性使其成为健康年轻成人良性非典型肺炎和性传播疾病一线治疗药物的选择。在艾滋病患者中,这些化合物可用于治疗分枝杆菌病(克拉霉素)、杆菌性血管瘤病以及由马红球菌引起的空洞性肺炎。临床耐受性非常好,尤其是胃肠道耐受性。所报道的药物相互作用是这类抗生素常见的。