Macrolides and Fluroquinolones Flashcards
mechanisms of action for macrolides
inhibition of protein synthesis (bacteriostatic effect)
main adverse effects for macrolides (2)
-tissue irritation: pain on injection (all macrolides), nausea and vomiting (oral erythromycin)
-potentially fatal colitis in hindgut fermenters
first line macrolide
erythromycin
second line macrolide
newer macrolides
general spectrum for erythromycin
relatively broad
PK features for macrolides (4)
-concentrate in lung
-enter cells
-most newer macrolides have long half lives
-erythromycin: inhibits P450 enzymes and stimulates motilin receptors
general spectrum for newer macrolides
a mix but mainly gram -ve aerobes
MOA for fluoroquinolones
damage DNA; inhibition of DNA gyrases and topoisomerases
bactericidal effect
main adverse effects for fluoroquinolones (3)
-cartilage damage (immature animals)
-retinal damage/degeneration (enrofloxacin in cats)
-reduction in seizure threshold (can trigger seizures in epileptics)
line of use for fluoroquinolones
second line (ongoing prudent use problems)
general spectrum for for fluoroquinolones
similar to gentamicin
-many gram -ve, staph (gram +ve), atypical bacteria
PK features for fluoroquinolones
-most have long half lives
-oral absorption 100%
-concentrate in lung
what is the safest class of antibacterial drugs
macrolides
what do the generic names end in if they are macrolides
osin or mycin
is gentamicin a macrolide
no
2 important uses of macrolides
1) intracellular pathogens
2) respiratory infections
what is the name of a macrolide used for bacterial pnemonia in livestock
tilmicosin, effective against gram -ve aerobic lung pathogens
when is tilmicosin fatal
IV injection in cattle
always fatal to swine
what is tulathromycin approved for and in what species
in cattle and swine for bacterial pneumonia
examples of macrolides
-tilmicosin
-tulathromycin
-gamithromycin
what leads to resistance of macrolides
acquisition of plasmid-encoded efflux pump
what is an adverse effect of tilmicosin specifically
can cause rapid cardiac fatalities in species other than cattle when administered parenterally
Fluoroquinolones are best thought of as _________ drugs to be used for infections resistant to first-line
drugs
second line
examples of fluroquinolines (5)
- Enrofloxacin (Baytril®)
- Orbifloxacin (Orbax®)
- Marbofloxacin (Zeniquin®)
- Difloxacin (Dicural®)
- Danofloxacin (A180®)
what are all FQs ineffective against
obligate anaerobes
what type of drug is banned in food producing animals
chloramphenicol
what drugs should be avoided if possible due to human health? (3)
-FQs
-potentiated penicillin
-3rd generation cephalosporins