Aminoglycosides/Broad Spectrum Abx (Lec 15) Flashcards
Aminoglycoside Abx structure?
Have amino surgar in glycosidic link
Polar (polycations)
Aminoglycoside polarity responsible for what?
pharmacokinetic properties
Aminoglycoside mechanism of action?
irreversibly inhibit protein synth:
block initiation of mRNA translation,
bactericidal
Aminoglycosides req what for activation?
aerobic conditions,
O2 req for abx transport to 30S subunit
Aminoglycoside active against?
aerobic G- enteric rods
Aminoglycosides are drug class of choice for what conditions?
sepsis
endocarditis
Streptomycin (aminoglycoside) used to treat?
b. plague
TB
endocarditis (in combo therapy)
Aminoglycosides + antipseud PCN used to treat what?
p. aeruginosa
Neomycin (aminoglycoside) used to treat?
G- skin infections
topical application
Gentamicin (aminoglycoside) used to treat what?
tularemia
DOC for Enterococci (G+ cocci)?
aminoglycoside + PCN
Aminoglycosides are what-dependent killers?
Concentration-dependent:
↑ concentration of drug kills more bacteria at more rapid rate
Aminoglycoside post-abx effect?
stays active beyond measurable [ ]
Aminoglycoside toxicity?
ototoxic
nephrotoxic
large dose less toxic than multiple small doses
Aminoglycoside administration?
IM
IV
topical
NOT oral - GI can’t absorb
Aminoglycosides are used primarily how?
in combo w/ other abx
3 types of Broad Spectrum Abx (BSA)?
1) chloramphenicol
2) tetracyclines
3) glycylcyclines
Chloramphenicol (BSA) mechanism of action?
reversibly binds 50S, preventing peptide bonds ->
inhibits protein synth
*also inhibits mitochondrial protein synth
Chloramphenicol is -static or -cidal?
bacteriostatic
can be -cidal to mengeal pathogens
Chloramphenicol spectrum?
G-, G+, aerobic, anaerobic, atypical
Chloramphenicol used only in what cases?
Life threatening infections
NEVER DOC
Chloramphenicol would be used to treat what life threatening infections?
typhoid fever
meningitis
Chloramphenicol administered how?
parenteral
What is Chloramphenicol not administered orally?
causes aplastic anemia
Chloramphenicol distribution?
ALL tissues
CNS penetration
Chloramphenicol metabolized how?
Conjugated w/ glucuronic acid in liver
Chloramphenicol toxicity (dose-dependent)?
bone marrow suppression
can be reversed by stopping med
Chloramphenicol toxicity (dose-independent)?
fatal aplastic anemia
Chloramphenicol toxicity to newborns?
Gray Baby Synd:
inadequate glucuronyl transferase activity in liver
What enzyme causes Chloramphenicol resistance in bacteria?
acetyl transferase
Tetracyclines (BSA) mechanism of action?
reversibly binds 30S ribosome, blocking tRNA attachment->
inhibits proetin synth
Tetracyclines are -static or -cidal?
bacterostatic
Tetracyclines spectrum?
G-, G+, aerobic, anaerobic, atypical
3 organisms resistant to Tetracyclines?
1) b. fragilis
2) proteus
3) pseudomonas
Tetracyclines is DOC for?
cholera m. pneumonia chlamydia b. burgdorferi (Lyme, early) vibrio rickettsii (Rocky Mnt Spotted)
Tetracycline resistance U from?
efflux pumps
Tetracyclines administration?
oral
chelation
Tetracyclines distribution?
all tissues except joints and CNS
Deposit in bone and teeth (chelate Ca2+)
Doxycycline (TCN family) metabolized?
NOT in liver
excreted thru feces
Tetracyclines side effects?
GI
bone/teeth
Glycylcycline (BSA) prototype drug?
Tigecycline
Tigecycline method of action?
binds 30S
bacteriostatic
Tigecycline spectrum?
same as TCN
AND also active against MRSA, MRSE, PRSP, VRE
Tigecycline primarily used to treat what type of infections?
complicated skin and skin-structure,
complicated intra-abdominal
Tigecycline administration?
IV
Tigecycline elimination?
2/3 fecal
1/3 renal
Tigecycline side effects?
similar to TCN