Clinical Overview of Enoxacin

Abstract

Enoxacin is a new fluoroquinolone that will be available as oral and intravenous preparations. This drug is bactericida/for a wide range of organisms, including Staphylococcus aureus, S. epidermidis, Enterobacteriaceae and Pseudomonas aeruginosa. In addition, Neisseria gonorrhoeae is exquisitely susceptible. as is Branhamella catarrhal is. The evaluation of the clinical activity of enoxacin is still relatively new. but published studies reveal a good deal of potential in the treatment of infections caused by susceptible bacteria in the urinary tract. upper and lower respiratory tracts. bones and joints. and the gastrointestinal tract. The general use of this drug has been associated with few adverse reactions. Further published data. as well as the results of comparative trials now in progress. will permit a thorough clinical evaluation of this useful drug.Enoxacin (l-ethyl-6-fluoro-l, 4-hydro-4-oxl-7-piperazin-l-yl-I,8-naphthyridine-3-carboxylic acid) is a synthetic antibacterial drug of the fluoroquinolone class. The fluoroquinolones, derivatives of nalidixic acid, have been introduced in the past few years with the promise of broad spectrum antibacterial activity, widespread distribution into tissues and body fluids, favourable pharmacok'inetics and excellent absorption after oral administration. Like other fluoroquinolones, enoxacin is rapidly bactericidal against a broad spectrum of bacteria. Enoxacin shows rapid concentration-dependent bacterial killing (similar to that of the aminoglycosides), with a long postantibiotic effect and activity against organisms in their stationary phase. The mechanism of action of enoxacin is the inhibition of the A-subunit of bacterial DNA gyrase, the enzyme responsible for the negative supercoiling of bacterial DNA.The antibacterial spectrum of enoxacin [defined as including organisms with a minimum inhibitory concentration (MIC) ~ 2.0 mgJL] includes Enterobacteriaceae such as Escherichia coli (MICqo = 0.25 mg/L), Salmonella and Shigella species (MICqo = 0.25 mg/L), Klebsiella and Enterobacter species (MICqo = I mg/L), Proteus species (MICqo = 0.5 mgfL), Serratia marcescens (MICqo = I mg/L), etc.; Pseudomonas aeruginosa (MICqo = 2 mgJL), Yersinia species (MICqo = 0.25 mg/L), Neisseria gonorrhoeae (MICqo = 0.015 mg/L), N. meningitidis (MICqo = 0.06 mgJL), Haemophilus influenzae (MICqo = 0.12 mg/L); Legionella species (MICqo = 0.25 mg/L), Branhamella catarrhalis (MICqo = 0.25 mg/L), methicillin-susceptible Staphylococcus aureus (MICqo = I mg/L), methicillinresistant S. aureus (MICqo = 2 mg/L) and S. epidermidis (MICqo = I mg/L). Other Gram-positive cocci including Streptococcus pneumoniae, S. pyogenes and Enterococcus faecalis (s. faecalis), as well as Listeria monocytogenes, Bacteroidesfragilis and other anaerobic Gram-negative rods, are less susceptible or resistant to enoxacin. In vitro activ-

Toxicity of quinolone antimicrobial agents

“…In contrast to these experimental findings, there are few reports of adverse effects of quinolones on the cardiovascular system in human clinical use (Shah & Mulert, 1990;Norrby, 1991;Zinner, 1989;Smythe & Rybak, 1989;Paton & Reeves, 1991;Geddes, 1993). The hypotensive effects observed in animals, especially in dogs and cats, may thus be species selective.…”

“…In humans, quinolones are reported to induce adverse CNS reactions such as dizziness, restlessness, confusion, depression, insomnia, drowsiness, somnolence, anxiety, sleep disorders, tremors, tremulousness, headache, and seizures (Christ et al, 1988;Zinner, 1989;Smythe & Rybak, 1989;Shah & Mulert, 1990;Norrby, 1991;Paton & Reeves, 1991;Geddes, 1993).…”

“…State University] at 13:18 14 October 2012 dyspepsia, and heartburn (Christ et al, 1988;Zinner, 1989;Smythe & Rybak, 1989;Shah & Mulert, 1990;Paton & Reeves, 1991).…”

Fabrication of an electrochemical sensor based on magnetic multi-walled carbon nanotubes for the determination of ciprofloxacin

“…3 CF works by inhibiting both the A-subunit of bacterial DNA gyrase (topoisomerase II) and an essential enzyme that maintains the super helical twists in the bacterial DNA, which affects the growth and reproduction of bacteria. 4 Because of its low toxicity, very wide spectrum of antibacterial effect, and the poor resistance of bacteria to the compound, CF has been widely used in clinical practice. Due to its widespread clinical use, routine pharmaceutical analyses, pharmacological and pharmaceutical dynamic studies, CF requires a simple, selective and sensitive method for the determination of its presence in pharmaceutical formulations and biological uids.…”

Synchronous fluorescence determination of ciprofloxacin in the pharmaceutical formulation and human serum based on the perturbed luminescence of rare-earth ions

“…Similar to other fluoroquinolones (FQs), ciprofloxacin is used in the treatment of systemic infections including urinary tract, respiratory, gastrointestinal and cutaneous infections. Its drug function works by inhibiting both a-subunit of bacterial DNA gyrase (topoisomerase II) and an essential enzyme that maintains the superhelical twists in the bacterial DNA, to affect the growth and reproduction of bacteria [1]. Because of its low toxicity, very wide spectrum of antibacterial effect, and low ability to cause the resistance of bacteria to the compound, CPFX has been widely used in clinical practice.…”