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甲磺酸加雷沙星一水合物是一个新的脱氟(6)喹诺酮类抗菌药,本品对包括耐药菌株在内的常见呼吸系致病菌,具有极好的抗菌活性。最大血药浓度(Cmax)、药时曲线下面积(AUC)药代动力学参数理想,对痰及耳鼻喉组织渗透性良好。对细菌性肺炎、支原体肺炎、立克次氏体性肺炎和急性支气管炎患者,有效率为92%～96%。对慢性呼吸系疾病急性感染加重发作,有效率为85%;对耳鼻喉感染,有效率为81%～95%。本品对金葡菌清除率为90.9%、肺炎链球菌清除率为99.2%、流感嗜血菌为98.2%、卡他莫拉菌为96.6%、耐青霉素的肺炎链球菌为100%、对β-内酰胺酶阴性耐氨苄西林流感嗜血菌和β-内酰胺酶阳性的流感嗜血菌为100%、对β-内酰胺酶阳性卡他莫拉菌为96.2%。加雷沙星400mg,每日1次,血药浓度和组织浓度高于主要致病菌的MIC90,血药谷浓度为1.92μg/mL,该浓度水平高于防耐药突变浓度。这些指标提示,在治疗过程中,加雷沙星不太可能诱导耐药突变菌株的选择能力。临床研究显示,加雷沙星不产生氟喹诺酮类副作用,如:QTc延长、血糖紊乱或严重的肝损伤。研究期间未观察到严重的不良反应。临床研究结果表明:治疗上下呼吸道感染患者,加雷沙星非常有效。
Garefulixacin mesylate monohydrate is a new fluoroquinolone antibacterial. It has excellent antibacterial activity against common respiratory pathogens including drug-resistant strains. Maximal plasma concentration (Cmax), the area under the curve (AUC) pharmacokinetic parameters ideal sputum and ENT tissue permeability well. Bacterial pneumonia, mycoplasma pneumonia, rickettsia pneumonia and acute bronchitis patients, the effective rate was 92% to 96%. Effective treatment of acute exacerbation of chronic respiratory diseases, the effective rate was 85%; ENT infection, the effective rate was 81% to 95%. The product of Staphylococcus aureus clearance rate of 90.9%, Streptococcus pneumoniae clearance rate of 99.2%, Haemophilus influenzae was 98.2%, Moraxella catarrhalis 96.6%, resistant to penicillin-resistant Streptococcus pneumoniae 100%, β - Lactamase-negative ampicillin-resistant Haemophilus influenzae and β-lactamase-positive Haemophilus influenzae are 100%, and β-lactamase-positive Moraxella catarrhalis is 96.2%. Galefloxacin 400mg, once daily, blood concentration and tissue concentration higher than the main pathogenic bacteria MIC90, blood trough concentration 1.92μg / mL, the concentration level higher than the concentration of anti-drug-resistant mutations. These indicators suggest that galebsine is less likely to induce selection of drug-resistant mutant strains during treatment. Clinical studies have shown that galefloxacin does not produce the side effects of fluoroquinolones, such as: QTc prolongation, blood glucose disorders or severe liver damage. No serious adverse reactions were observed during the study. Clinical studies have shown that galefloxacin is very effective in treating patients with upper and lower respiratory tract infections.