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
interactions with fluoroquinilones
synergistic: b-lactam, aminoglycosides, Vancomycin, Metronidazole
Antagonist: Chloramphenical, Rifampicin
increases: Warfarin, caffein, theophylline & cyclosporin effect
prolonged QT, use antiarrhythmics
Indication of 2nd Generation Fluoroquinilones
UTI
Resp inf.
Dermatitis
sepsis
otitis
meningitis
1st choice: prostatitis
indication of 3rd & 4th G fluoroquinilones
Meningitis
Anaerob infection
meningoencephalitis
peritonitis
periodontitis
Enrofloxacin specie administration
Lactating cows
sus
poultry
smalls
Ciprofloxacin specie administration
Human
Danofloxacin specie administration
lactating cows
swine
poultry
marbofloxacin specie administration
large (injection)
orbifloxacin specie administration
smalls (orally)
Pradofloxacin specie administration
smalls (orally)
Nitroimidazoles drug
metronidazoles
metronidazole mode of action
destroys DNA in anaerobic conditions
(Bacteriacidal??)
metronidazole spectrum
obligate anaerobic bacteria
protozoa (trichomonas, histomonas, giardia, amoeba)
PK of metronidazole
Abs: Excellent
Distr: Excellent
Met: liver
excr: urine
metronidazole indication
anal sacculitis
gingivitis
paradonditis
oral cavity infection
protozoal
metronidazole banned from
Swine dysentery prevention
Fosfomycin mode of action
inhibition of peptidoglycan, bactericidal
spectrum of fosfomycin
Gram +
Gram -
(resistance develops rapidly)
PK of fosfomycin
distr: moderate
met: none
excr: faeces & urine
Administration and indication of fosfomycin
PO for UTI
Nitrofurans drugs
nitrofurantoin
mode of action of nitrofurantoin
bactericidal
spectrum of nitrofurantoin
broad Gram -
Enterobactericeae
resistance of nitrofurantoin
proteus & pseudomonas
PK of nitrofurans
abs: PO well
Furasolidone : met by liver (for enteral infections)
excr: Urine & nitrofurantoin
nitrofurantoin indication & species
UTI,
Ca & Fe
Toxicity of nitrofurantoin
low TI
GI irritation
neurotoxicity
NOT for FPA (mutagenic & carcinogenic)
