Using microdialysis in a rabbit model of Streptococcus pneumoniae meningitis, the pharmacokinetics and pharmacodynamics of a new fluoroquinolone, A-80556, were determined. A-80556 (10 mg/kg iv) was administered to four rabbits. Saline was given to four separate control animals. A microdialysis probe perfused the CSF (2 microL/min) and effluent was collected at 0-0.25, 0.25-1, 1-2, 2-4, and 4-6 h after injection of A-80556. Seven blood samples were collected and analyzed by HPLC. At 0, 2, 4 and 6 h 300 microL of CSF was withdrawn for pharmacodynamic measurements. Plasma A-80556 concentrations demonstrated AUC0-infinity 2.40 +/- 0.272 micrograms.h/mL; T1/2 beta 1.07 +/- 0.011 h; Vd 6.35 +/- 0.50 L/kg; and Cl1 4.23 +/- 0.48 L/h.kg. Penetration into the CSF was 18.21%. Pharmacodynamics using time-kill curves showed a 3-log reduction in bacterial counts in CSF at 2 h after administration continuing for the remaining four hours of the experiment. These results demonstrate that microdialysis can be used for determination of drug penetration and efficacy in experimental S. pneumoniae meningitis.

01 May 1994·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

In vitro and in vivo evaluations of A-80556, a new fluoroquinolone

Q2 · MEDICINE

Article

Author: Alder, J ; Hensey, D ; Clement, J J ; Tanaka, S K ; Ramer, N ; Vojtko, C ; Beyer, J ; McDaniel, D ; Chu, D T

A-80556 is a novel fluoroquinolone with potent antibacterial activity against gram-positive, gram-negative, and anaerobic organisms. A-80556 was more active than ciprofloxacin, ofloxacin, lomefloxacin, and sparfloxacin against gram-positive bacteria. A-80556 was particularly active against Staphylococcus aureus (MIC for 90% of isolates [MIC90], 0.12 microgram/ml, relative to fluoroquinolone-susceptible strains) and Streptococcus pneumoniae (MIC90, 0.12 microgram/ml). A-80556 was also the most active of the quinolones tested against ciprofloxacin-resistant S. aureus, with an MIC90 of 4.0 micrograms/ml; that of ciprofloxacin was > 128 micrograms/ml. However, the significance of this activity is not known. A-80556 was slightly less active against Escherichia coli (MIC90, 0.06 microgram/ml) and other enteric organisms than ciprofloxacin (MIC90 for E. coli, < or = 0.03 microgram/ml). A-80556 was slightly less active against Pseudomonas aeruginosa (MIC90, 4.0 micrograms/ml) than ciprofloxacin (MIC90, 2.0 micrograms/ml) and more active against Acinetobacter spp. (respective MIC90s, 0.12 and 0.5 microgram/ml). A-80556 was also the most active compound against anaerobes. Against Bacteroides fragilis, the MIC90 of A-80556 was 2.0 micrograms/ml; that of ciprofloxacin was 16 micrograms/ml. The in vivo efficacy of A-80556 in experimental models with both gram-positive and gram-negative infections was consistent with the in vitro activity and pharmacokinetics and oral absorption in mice.

01 Jan 1994·Journal of Antimicrobial ChemotherapyQ2 · MEDICINE

In-vitro activity of quinolones and macrolides against mycobacteria

Q2 · MEDICINE

Article

Author: C. Y. Chan ; D. Lyon ; W. W. Yew ; M. S. K. Li ; A. F. B. Cheng ; L. J. V. Piddock

The activities of eight quinolones (ciprofloxacin, clinafloxacin, levofloxacin, ofloxacin, A-80556, sparfloxacin, temafloxacin and tosufloxacin) and three macrolides (azithromycin, clarithromycin and erythromycin) against 98 clinical isolates of Mycobacterium tuberculosis and 120 isolates of five different atypical mycobacterial species including 20 Mycobacterium kansasii, 25 Mycobacterium scrofulaceum, 25 Mycobacterium avium/intracellulare, 25 Mycobacterium chelonae and 25 Mycobacterium fortuitum were determined with the Middlebrook 7H9 broth macrodilution method. Sparfloxacin, clinafloxacin, levofloxacin, ciprofloxacin and ofloxacin were active against M. tuberculosis (MIC90 0.06-0.5 mg/L; MBC90 0.125-2.0 mg/L). However, higher MIC90S and MBC90S of these quinolones were obtained for strains of multi-drug resistant M. tuberculosis. The macrolides tested had poor activity against M. tuberculosis isolates (MIC90 > 8.0 mg/L). Furthermore, high MIC90S of the quinolones and macrolides (2.0 to 8.0 mg/L) were obtained for clinical isolates of atypical mycobacteria, with the exception of clarithromycin against M. kansasii (MIC90 = 1.0 mg/L) and sparfloxacin against M. scrofulaceum (MIC90 = 1.0 mg/L).

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Discovery	US	Abbott Laboratories (Philippines), Inc.	-

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