Antimicrobials 4 Flashcards
MOA of aminoglycosides (there are two)
- irreversibly binds to ribosomenal subunit and causes codon to be misread, they are bactericidal unlike most protein synthesis inhibitors.
- disrupts biofilms (esp gram neg ones)–>displaces calcium and magnesium from the outer cell membrane which disrupts the LPS cross links and destabilizes the outer membrane
why do aminoglycosides have a post antibiotic effect
they irreversibly bind to the ribosomes and kill the bacteria right away
aminoglycosides are really great for what kind of bacteria? How does the drug get into these bacteria?
really great for gram negative bacteria. it gets in via porins in the outer membrane, and are then actively transported through the inner membrane (oxygen dependent, no not effective against anaerobes)
aminoglycosides are not good at disrupting biofilms of gram positive bacteria, UNLESS…
the aminoglycoside is administered with a cell-wall disrupting agent like a beta lactam; they are syngergistic with cell wall disrupting antimicrobials
list some general characteristics of aminoglycosides
- bactericidal
- concentration dependent
- oxygen dependent
- inactivated at low pH
- inactivated by necrotic debris/purulent material–>not good for abscesses
- inactivated by combining with other drugs in syringe
important PK considerations for aminoglycosides?
- not absorbed from GI (topical or injectable)
- not bound to proteins
- does not cross blood brarriers
- eliminated via kidney without prior metabolism
- accumulate in renal cortex ( do not give systemically to food animals)
what are the two big adverse effects of aminoglycosides?
-nephrotoxic: accumulates in renal cortex and damages prox tubule cells
ototoxic: accumulates in inner ear, effets auditory and vestibular, usually ocurs after nephrotoxicity
what are the two aminoglycosides i need to remember?
gentamicin, amikacin
aminoglycosides are important drugs for treating ______ infections, although some newer drugs can treat similar infections with fewer adverse effects (like 3rd gen cephalosporins)
aerobic gram neg
how are gentimycin and amikacin given and what are they commonly used for?
both can be given IV, IM, or SQ
most commonly used to treat joint infections in horses, often combined with local anestheitcs or steroids during routine joint injections as prophylaxsis. can also be used topically for eye and ear infections
how do gentamicin and amikacin differ?
both effective for gram neg, amikacin better for staph, both not good at crossing cell membranes
gentamicin and amikacin can be used topically for ear infections, but are ototoxic…how does this work?
before you put it topically in the ear, you should check to make sure the tympanic membrane is in tact but this isn’t always possible
which is broader spectrum, gentamicin or amikacin?
amikacin (since action against staphs as well as gram neg aerobes)
MOA of macrolides and lincosamides?
prevent polypeptide chain elongation
should you use a macrolide and a lincosamide together?
no! they will interfere with each otherand decrease their efficacy