モキシフロキサシン 化学特性,用途語,生産方法
効能
抗菌薬, 核酸合成阻害薬
使用
Moxifloxacin is an antibiotic for the treatment of bacterial infections like bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
定義
ChEBI: A quinolone that consits of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b
/ital>]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.
抗菌性
It displays good activity in vitro against Enterobacteriaceae and fastidious Gram-negative bacilli such as H. influenzae and Mor. catarrhalis, as well as against Grampositive cocci including Str. pneumoniae, but is poorly active against Enterococcus spp. Activity against non-fermentative Gramnegative bacilli is species dependent: Acinetobacter spp. (MIC 0.006–2.0 mg/L) and Sten. maltophilia (MIC 0.5–2.0 mg/L) are partially susceptible in vitro, but it has poor activity against Ps. aeruginosa and other non-fermenting Gram-negative rods. It displays good in-vitro activity against Ch. pneumoniae, C. trachomatis, mycoplasmas (including M. pneumoniae), L. pneumophila and B. fragilis. Although highly active against M. tuberculosis, it is less active against the M. avium complex, M. intracellulare, M. chelonei and M. fortuitum.
応用例（製薬）
fluoroquinolone substituted with an 8-methoxy group and a 7-diazabicyclononyl moiety, formulated as the hydrochloride for oral or intravenous use.
薬物動態学
absorption and distribution By the oral route, drug uptake is rapid, with moderate variability. As with all quinolones iron and antacids significantly reduce the bioavailability. No significant drug interactions with theophylline, itraconazole, probenecid or oral contraceptives have been found. In escalating dose studies (50–80 mg doses), Cmax and AUC values increased proportionally to the dose.
It is widely distributed throughout the body and into many tissues in concentrations exceeding those in plasma. Around 50–80% of plasma concentrations penetrate into CSF if the meninges are inflamed. The apparent plasma half-life is 15.6 h.
Metabolism and excretion Biliary elimination and metabolism are the main elimination pathways. About 19.3% of the administered dose is eliminated in the urine, with a bioavailability of 86.2%. Urinary excretion is via glomerular filtration and tubular reabsorption. Two main metabolites are recovered: M1 (a sulfocompound) and M2 (a glucuronide). M1 is mainly eliminated in feces (34.4%) and only 2.5% in urine： M2 is eliminated in urine (13.8%).
臨床応用
Acute bacterial exacerbations of chronic bronchitis and community
acquired pneumonia
Acute bacterial sinusitis
Treatment of complicated skin and soft-tissue infections caused by methicillin-susceptible Staph. aureus and Gram-negative rods (i.v. formulation)
Treatment of complicated intra-abdominal infections (i.v. formulation)
副作用
Adverse events are similar to those for other fluoroquinolones. Phototoxicity rates are not significantly above placebo levels. Gastrointestinal side effects are the most common, particularly nausea, diarrhea, abdominal pain and vomiting. Dizziness and headache may occur as well as allergic reactions. Attention has been drawn to a potential to cause lifethreatening hepatotoxicity. Moxifloxacin has the potential to prolong the QTc interval in some patients but the clinical significance of this phenomenon is unclear.
モキシフロキサシン 上流と下流の製品情報
原材料
準備製品