A-25. Fluoroquinolones, other antibacterial agents (nitroimidazoles, nitrofurans, fosfomycin) Flashcards
2nd generation Fluoroquinolones
Ciprofloxacin
Enrofloxacin
marbofloxacin
3rd generation Fluoroquinilones
Levofloxacin
Sparfloxacin
4th generation fluoroquinilones
Pradofloxacin
moxifloxacin
AMEG Category of fluoroquinilones
3rd & 4th : Cat B
Structure of Fluoroquinilones
5th carbon attachment affects toxicity
3 & 4th carbon attachement affects effectiveness
3rd & 4th fluoroquinilones generation resistance
decreased efficacy or no efficacy against P. aeruginosa
2nd generation fluoroquinilones generation resistance
Anaerobic
streptococcus
enterococcus
2nd generation fluoroquinilones generation spectrum
P. aeruginosa (Ciprofloxacin, Enrofloxacin, marbofloxacin)
IC bacteria
Spectrum of 1st generation Fluoroquinilones
Enterobacteriaceae
fastidious bacteria
Aeromonas
Spectrum of 3rd generation Fluoroquinilones
Gram +
Streptococcus
IC bacteria
Spectrum of 4th generation Fluoroquinilones
Gram +
Streptococcus
IC bacteria
Anaerobs
mode of action of Fluoroquinilones
promotion of bacterial DNA cleavage : inhibition of DNA synthesis
Concentration dependent bactericidal
PAE : 2-5hrs
Resistance of fluoroquinilones
chromosomal resistance (E.Coli, Salmonella & Campylobacter)
Plasmid mediated (Enterobacteriaceae)
cross resistance between all generations
PK of fluoroquinilones
Abs: Excellent, PO (food delays) ; SC/IM : good
Distr: Excellent (special barriers, concentrated in phagocytic cells)
Met: Partially metabolized, metabolites may be active
Excr: Urine as active drug, partially bile
Toxicity of Fluoroquinilones
very safe (1st G most toxic)
long lasting administration & large dose : more SE
Side effects of Fluoroquinilones
Retinopathy in cats (enrofloxacin)
inhibition of cartilage dvlpmt
CNS seizures
Dysbacteriosis