Aminoglycosides - Gentamicin Flashcards
What is gentamicin used for?
- sever sepsis (unidentified source)
- pyelonephritis and complicated UTI
- biliary and intra-abdo sepsis
- endocarditis
What bacteria is gentamicin particularly effective against?
- gram - negative aerobes
including Pseudomonas aeruginosa
(severe infections)
Why are aminoglycosides like gentamicin combined with penicillin and/or metronidazole?
Aminoglycosides like gentamicin have no activity against streptococci and anaerobes so should be combined with penicillin and metronidazole when the organism is unkown.
How do aminoglycosides like gentamicin work?
They are bactericidal- bind irreversibly to bacterial ribosomes (30S subunit) and inhibit protein synthesis.
They enter bacterial cells via an oxygen-dependant transport system.
What is the spectrum of activity of aminoglycosides like gentamicin>
- Gram negative aerobic bacteria
- staphylococci
- mycobacteria
How do aminoglycosides such as gentamicin enter the bacterial cell?
Gentamicin enters bacterial cells via an oxygen-dependant transport system.
Why are aminoglycosides inneffective towards streptococci and anaerobic bacteria?
Aminoglycosides enter the bacterial cell via oxygen-dependant transport system. They then bind to 30S subunits and prevent protein synthesis.
Streptoccoci and anaerobes dont have this oxygen dependant transport system,
How do penicillins enhance gentamicin uptake?
- some baceria acquire resistance to aminoglycosides by reducing cell membrane permeability.
- Penicillins help uptake of gentamicin by weakening the bacterial cell walls.
What are the side effects of gentamicin?
- nephrotoxicity
- ototoxicity
(aminoglycosides accumulate in renal tbubular epithelial cells and cochlear/vestibular hair cells and trigger apoptosis and cell death)
How does gentamicin cause nephrotoxicity and ototoxicity?
Gentamicin accumulates in the renal tubular epithelial cells and the cochlear/vestibular cells - here they trigger apoptosis and cell death.
How does nephrotoxicity present?
- reduced urine output
- rising serum creatinine
- risinf urea
(can be reversible
How does otoxicity present?
after acute infection cleared - hearing loss - tinnitus - vestibular damage (may be irreversible)
How are aminoglycosides excreted?
renally excreted
Who are most susceptible to renal / ototoxicity?
Monitor levels of aminoglycosides carefully in:
- elderly
- neonates
- renal impairment
why are aminoglycosides contraindicated in myasthenia gravis?
aminoglycosides can impair neuromuscular transmission.