Sparfloxacin

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Chemical Structure| 110871-86-8 同义名 : CI-978; AT-4140; Zagam; Esparfloxacino; PD 131501; PD 1315-1; CP 103,826
CAS号 : 110871-86-8
货号 : A170693
分子式 : C19H22F2N4O3
纯度 : 99+%
分子量 : 392.4
MDL号 : MFCD00869619
存储条件:

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:

0.5% CMC+water 10 mg/mL suspension

生物活性
描述 Sparfloxacin, a synthetic, second generation, broad spectrum aminodifluoroquinolone antibiotic, has excellent penetration into respiratory tissues and has good activity against Gram-positive, Gram-negative, and atypical bacteria[3]. Sparfloxacin often induce photosensitive skin reactions, more often phototoxic reactions than photoallergic ones, and sometimes associated photo-onycholysis [4]. Plasma sparfloxacin concentrations reach a peak (Cmax) of approximately 0.7 mg/L at 3 to 5 hours after a 200mg oral dose. Sparfloxacin binds weakly to plasma protein (37%), and exhibits excellent tissue distribution and effective penetration into extracellular fluids[5]. The profile of adverse effects for sparfloxacin is generally similar to that of other quinolones: gastrointestinal discomfort and CNS effects are the most common in clinical trials [6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02099240 Osteomyelitis Early Phase 1 Recruiting September 2019 United States, Kentucky ... 展开 >> University of Louisville Recruiting Louisville, Kentucky, United States, 40202 Contact: Julio A Ramirez, MD    502-852-1148    jarami01@louisville.edu    Contact: David Seligson, MD    502-852-0923    d0seli01@louisville.edu    Sub-Investigator: Forest Arnold, DO          Sub-Investigator: Timothy Wiemkwn, PhD          Sub-Investigator: Robert Kelley, PhD          Sub-Investigator: James Summersgill, PhD          Sub-Investigator: Ruth Carrico, PhD          Sub-Investigator: Julie Harting, PharmD          Sub-Investigator: Paula Peyrani, MD          Principal Investigator: David Seligson, MD          Sub-Investigator: Craig Roberts, MD          Principal Investigator: Julio Ramirez, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.74mL

2.55mL

1.27mL

25.48mL

5.10mL

2.55mL

参考文献

[1]Pan XS, Fisher LM. Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: selective targeting of gyrase or topoisomerase IV by quinolones. Antimicrob Agents Chemother. 1997 Feb;41(2):471-4.

[2]Nakamura S, Minami A, et al. In vitro and in vivo antibacterial activities of AT-4140, a new broad-spectrum quinolone. Antimicrob Agents Chemother. 1989 Aug;33(8):1167-73.

[3]Yahya H. Sparfloxacin-induced nail pigmentation: A case of fixed drug eruption?. Ann Afr Med. 2018;17(1):40–42

[4]Pawar M, Singh M. Sparfloxacin-induced photo-onycholysis and photosensitivity characteristically sparing lepromatous skin lesions: an interesting observation. Acta Dermatovenerol Alp Pannonica Adriat. 2018;27(3):149–151

[5]Shimada J, Nogita T, Ishibashi Y. Clinical pharmacokinetics of sparfloxacin. Clin Pharmacokinet. 1993;25(5):358–369

[6]Goa KL, Bryson HM, Markham A. Sparfloxacin. A review of its antibacterial activity, pharmacokinetic properties, clinical efficacy and tolerability in lower respiratory tract infections. Drugs. 1997;53(4):700–725