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罗红霉素。其抗菌活性、药代动力学特性及治疗用途的最新进展。

Roxithromycin. An update of its antimicrobial activity, pharmacokinetic properties and therapeutic use.

作者信息

Markham A, Faulds D

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1994 Aug;48(2):297-326. doi: 10.2165/00003495-199448020-00011.

Abstract

Roxithromycin is a derivative of the macrolide antibacterial erythromycin with in vitro antibacterial activity resembling that of the parent compound. The drug has activity against some Staphylococcus spp., many Streptococcus spp., Moraxella (Branhamella) catarrhalis, Mycoplasma pneumoniae, Legionella pneumophila and Chlamydia trachomatis as well as many less common organisms. Measured using recently proposed guidelines, roxithromycin has in vitro activity against Haemophilus influenzae. In comparison with that of its parent compound, the pharmacokinetic profile of roxithromycin is characterised by high plasma, tissue and body fluid concentrations and a long half-life permitting an extended dosage interval. Roxithromycin has proven clinical efficacy in upper and lower respiratory infections, skin and soft tissue infections, urogenital infections and orodental infections, and appears to be as effective as more established treatments including erythromycin, amoxicillin/clavulanic acid and cefaclor. The drug has also shown promise in a variety of more specialised indications including opportunistic infections in human immunodeficiency virus (HIV)-positive patients and as part of a Helicobacter pylori eradication regimen. Roxithromycin is very well tolerated with an overall incidence of adverse events of approximately 4%. Thus, roxithromycin is an attractive therapeutic alternative in its established indications, especially when the option of once-daily administration is considered.

摘要

罗红霉素是大环内酯类抗菌药物红霉素的衍生物,其体外抗菌活性与母体化合物相似。该药物对一些葡萄球菌属、许多链球菌属、卡他莫拉菌(布兰汉菌属)、肺炎支原体、嗜肺军团菌和沙眼衣原体以及许多不太常见的微生物具有活性。按照最近提出的指南进行测定,罗红霉素对流感嗜血杆菌具有体外活性。与母体化合物相比,罗红霉素的药代动力学特征是血浆、组织和体液浓度高,半衰期长,允许延长给药间隔。罗红霉素在上、下呼吸道感染、皮肤和软组织感染、泌尿生殖系统感染和口腔感染方面已证明具有临床疗效,并且似乎与包括红霉素、阿莫西林/克拉维酸和头孢克洛在内的更成熟治疗方法一样有效。该药物在包括人类免疫缺陷病毒(HIV)阳性患者的机会性感染等各种更特殊的适应症以及作为幽门螺杆菌根除方案的一部分方面也显示出前景。罗红霉素耐受性良好,不良事件的总体发生率约为4%。因此,罗红霉素在其既定适应症中是一种有吸引力的治疗选择,尤其是考虑到每日一次给药的选择时。

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