Yu K W, Briones F, Chin N X, Neu H C
Department of Medicine, College of Physicians and Surgeons, Columbia University, New York, New York.
Diagn Microbiol Infect Dis. 1991 Jul-Aug;14(4):331-5. doi: 10.1016/0732-8893(91)90024-a.
The activity of rokitamycin, a 16-membered macrolide, was compared with other macrolides and agents used to treat respiratory infections. Rokitamycin had in vitro activity against streptococci and Streptococcus pneumoniae comparable to the other macrolides, inhibiting most organisms at less than 0.03 to 0.5 microgram/ml. It was the most active macrolide agent against Staphylococcus aureus, inhibiting 90% at 1 microgram/ml. Macrolide-resistant streptococci and staphylococci in which resistance was inducible were inhibited, but constitutively resistant Gram-positive bacteria were resistant. Rokitamycin was less active than erythromycin against Haemophilus influenzae, but had activity comparable to erythromycin against Moraxella catarrhalis and Neisseria gonorrhoeae. It inhibited Clostridium spp. and peptostreptococci, but had poor activity against Bacteroides species. Rokitamycin was bactericidal for streptococci and staphylococci, but not for enterococci. Overall rokitamycin has in vitro activity comparable to currently available 14-membered macrolides. Its clinical utility will be influenced by the degree of metabolism to less active metabolites since 70% is rapidly metabolized.
将16元大环内酯类药物罗他霉素的活性与其他大环内酯类药物及用于治疗呼吸道感染的药物进行了比较。罗他霉素对链球菌和肺炎链球菌的体外活性与其他大环内酯类药物相当，对大多数菌株的抑制浓度低于0.03至0.5微克/毫升。它是对金黄色葡萄球菌活性最强的大环内酯类药物，在1微克/毫升时可抑制90%的菌株。对大环内酯类耐药的链球菌和诱导型耐药的葡萄球菌可被抑制，但组成型耐药的革兰氏阳性菌具有耐药性。罗他霉素对流感嗜血杆菌的活性低于红霉素，但对卡他莫拉菌和淋病奈瑟菌的活性与红霉素相当。它可抑制梭菌属和消化链球菌，但对拟杆菌属的活性较差。罗他霉素对链球菌和葡萄球菌具有杀菌作用，但对肠球菌无杀菌作用。总体而言，罗他霉素的体外活性与目前可用的14元大环内酯类药物相当。由于70%的罗他霉素会迅速代谢，其临床效用将受到代谢为活性较低代谢产物程度的影响。
