EXTENT AND SPECTRUM OF THE ANTIMICROBIAL ACTIVITY OF CLARITHROMYCIN
EXTENT AND SPECTRUM OF THE ANTIMICROBIAL ACTIVITY OF CLARITHROMYCIN
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DOI：
10.1097/00006454-199312003-00002
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发表时间：
1993-12-01
影响因子：
3.6
通讯作者：
HARDY, DJ
中科院分区：
文献类型：
--
作者：
HARDY, DJ
克拉霉素是一种新的半合成大环内酯类药物，具有亲脂性，在组织中的浓度通常比血清中的浓度高10倍。克拉霉素对多种革兰氏阳性菌和革兰氏阴性菌、支原体、衣原体和分枝杆菌具有体外和体内活性。14-羟基克拉霉素是克拉霉素在人体内的主要代谢产物，对这些微生物的活性通常与克拉霉素相同，但在体外和体内对流感嗜血杆菌的活性高于克拉霉素。通过质粒或转座子编码的甲基化酶、大环内酯-林可酰胺-链阳性菌素耐药而对红霉素耐药的微生物也对克拉霉素耐药。然而，与旧的大环内酯类药物不同，克拉霉素具有体外和体内抗非典型分枝杆菌的活性。本文综述了克拉霉素和14-羟基克拉霉素的抗菌活性。
Clarithromycin, a new semisynthetic macrolide, is lipophilic and achieves concentrations in tissue that are generally 10 times greater than concentrations achieved in serum. Its binding to serum proteins is low and reversible.Clarithromycin has in vitro and in vivo activity against a variety of Gram-positive and Gram-negative bacteria, Mycoplasma, Chlamydia and mycobacteria. 14-Hydroxyclarithromycin, the major metabolite of clarithromycin in humans, is generally as active as clarithromycin against these organisms but is more active in vitro and in vive than clarithromycin against Haemophilus influenzae. Organisms resistant to erythromycin by plasmid or transposon-encoded methylase, macrolide-lincosamide-streptogramin resistance, are also resistant to clarithromycin. Unlike older macrolides, however, clarithromycin has in vitro and in vivo activity against atypical mycobacteria. The antimicrobial activities of clarithromycin and 14-hydroxyclarithromycin are reviewed in this article.