PHARMACOLOGY
Mode of Action
Like other fluoroquinolones, Prulifloxacin prevents bacterial DNA replication,
transcription, repair and recombination through inhibition of bacterial DNA
gyrase.
Antibacterial Spectrum
Prulifloxacin is the prodrug of ulifloxacin. Prulifloxacin is immediately and
quantitatively transformed into the active metabolite ulifloxacin. Therefore, the in
vitro
antimicrobial activity studies were performed using ulifloxacin (UFX).
Prulifloxacin showed potent and broad-spectrum antibacterial activity against
Gram-negative and Gram-positive bacteria.
Gram negative bacteria including community and nosocomial isolates of:
Escherichia coli
Klebsiella spp.
Proteus spp.
Providencia spp.
Moraxella catarrhalis
Morganella spp.
Haemophilus spp.
Pseudomonas aeruginosa (Activity varies between countries).
Gram-positive organisms, including:
Methicillin- or Oxacillin-susceptible Staphylococcus aureus,
Enterococcus spp.
Streptococcus pneumoniae
Pharmacokinetics
After administration of a single oral dose of prulifloxacin 600mg in young healthy
volunteers the peak plasma concentration (Cmax) of ulifloxacin (1.6μg/mL) was
achieved in a median time to Cmax (tmax) of 1 hour. The area under the plasma
concentration-time curve from zero to infinity (AUC∞) was 7.3 μg • h/mL, and
AUC∞ values showed linearity over a dose range of 300–600mg.
Ulifloxacin is ≈45% bound to serum proteins in vivo. It is extensively distributed
throughout tissues, with an apparent volume of distribution of 1231L after a
single dose of prulifloxacin 600mg, and shows good penetration into many body
tissues.
The elimination half-life (t1/2) of ulifloxacin after single-dose prulifloxacin 300–
600mg ranged from 10.6 to 12.1 hours.
After absorption from the gastrointestinal tract, prulifloxacin undergoes extensive
first-pass metabolism (hydrolysis by esterases, mainly paraoxonase to form
ulifloxacin, the active metabolite).Unchanged ulifloxacin is predominantly
eliminated by renal excretion.
Mode of Action
Like other fluoroquinolones, Prulifloxacin prevents bacterial DNA replication,
transcription, repair and recombination through inhibition of bacterial DNA
gyrase.
Antibacterial Spectrum
Prulifloxacin is the prodrug of ulifloxacin. Prulifloxacin is immediately and
quantitatively transformed into the active metabolite ulifloxacin. Therefore, the in
vitro
antimicrobial activity studies were performed using ulifloxacin (UFX).
Prulifloxacin showed potent and broad-spectrum antibacterial activity against
Gram-negative and Gram-positive bacteria.
Gram negative bacteria including community and nosocomial isolates of:
Escherichia coli
Klebsiella spp.
Proteus spp.
Providencia spp.
Moraxella catarrhalis
Morganella spp.
Haemophilus spp.
Pseudomonas aeruginosa (Activity varies between countries).
Gram-positive organisms, including:
Methicillin- or Oxacillin-susceptible Staphylococcus aureus,
Enterococcus spp.
Streptococcus pneumoniae
Pharmacokinetics
After administration of a single oral dose of prulifloxacin 600mg in young healthy
volunteers the peak plasma concentration (Cmax) of ulifloxacin (1.6μg/mL) was
achieved in a median time to Cmax (tmax) of 1 hour. The area under the plasma
concentration-time curve from zero to infinity (AUC∞) was 7.3 μg • h/mL, and
AUC∞ values showed linearity over a dose range of 300–600mg.
Ulifloxacin is ≈45% bound to serum proteins in vivo. It is extensively distributed
throughout tissues, with an apparent volume of distribution of 1231L after a
single dose of prulifloxacin 600mg, and shows good penetration into many body
tissues.
The elimination half-life (t1/2) of ulifloxacin after single-dose prulifloxacin 300–
600mg ranged from 10.6 to 12.1 hours.
After absorption from the gastrointestinal tract, prulifloxacin undergoes extensive
first-pass metabolism (hydrolysis by esterases, mainly paraoxonase to form
ulifloxacin, the active metabolite).Unchanged ulifloxacin is predominantly
eliminated by renal excretion.
