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加雷沙星甲磺酸水合物是一种新型的、口服的、喹诺酮母核6位去氟的抗生素,它对常见的呼吸道致病菌,包括耐药菌有着良好的抗菌活性。临床研究中显示,对于细菌性肺炎、支原体肺炎、衣原体肺炎和急性支气管炎,加雷沙星的临床有效率为92%~96%;对于慢性呼吸道疾病的急性感染性发作有效率为85%;对于耳鼻咽喉感染的有效率则为81%~95%。加雷沙星对于各种细菌清除率分别如下:金黄色葡萄球菌为90.9%;肺炎链球菌为99.2%;流感嗜血菌为98.2%;黏膜炎莫拉菌为96.6%;耐青霉素的肺炎链球菌为100%。对于耐阿莫西林的流感嗜血菌株中产β-内酰胺酶的阴性菌株和流感嗜血菌株中产β-内酰胺酶的阳性菌株,加雷沙星的细菌清除率为100%,而对黏膜炎莫拉菌中的产β-内酰胺酶的阳性菌株,则为96.2%。使用加雷沙星每天400mg,加雷沙星在血浆和组织中的浓度大大高于其对主要病原菌的MIC90。在血浆中Cmin为1.92μg/mL,大大高于菌株防耐药变异浓度,暗示加雷沙星在治疗过程中不会导致耐药菌株突变。在临床试验中,加雷沙星未出现氟喹诺酮类药物常见的不良反应,如QTc延长,血糖异常以及严重的肝脏损害。在治疗期间尚未出现严重的不良反应。试验结果显示加雷沙星在治疗上下呼吸道感染方面非常有效。
Galefloxacin mesylate hydrate is a novel, oral, quinolone core 6-defluorinated antibiotic that has good antibacterial activity against common respiratory pathogens, including resistant bacteria. Clinical studies have shown that the clinical effective rate of galebsicate is 92% -96% for bacterial pneumonia, mycoplasma pneumonia, chlamydia pneumonia and acute bronchitis, 85% for acute infectious seizure of chronic respiratory diseases, The effective rate for otolaryngological infections is 81% to 95%. The clearance rates of galeadine for various bacteria were as follows: 90.9% for Staphylococcus aureus; 99.2% for Streptococcus pneumoniae; 98.2% for Haemophilus influenzae; 96.6% for Moraxella catarrhalis; Cocci is 100%. For the amoxicillin-producing strains of β-lactamase-producing strains of Haemophilus influenzae strains and β-lactamase-producing strains of Haemophilus influenzae strains, the clearance rate of galefloxacin was 100%, and for mucositis Moraceae β-lactamase-producing strains of positive, then 96.2%. With 400 mg of galefloxacin per day, galebsofloxacin concentrations in plasma and tissues are much higher than their MIC90 for the major pathogen. Cmin in plasma was 1.92μg / mL, which was much higher than that of drug-resistant strains. This suggests that galefloxacin does not cause mutations in drug-resistant strains during the course of treatment. In clinical trials, galephafloxacin did not appear common adverse reactions of fluoroquinolones, such as prolonged QTc, abnormal blood glucose and severe liver damage. No serious adverse reactions have occurred during treatment. Test results show that galefloxacin in the treatment of upper and lower respiratory tract infection is very effective.