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54 Cards in this Set

  • Front
  • Back
Examples of aminoglycosides
Examples of macrolide AB
Examples of streptogramins
Examples of tetracyclines
What is the basic mech behind broad spectrum abx
inhibits bacterial protein synth
MOA of aminoglycosides
cidal or static?
Biinds 30s ribosomal subunit, irreversibly interfering with protein synth
cidal (w killing being [] dependent)
also has post-abx effect, w antibacterial activity persisting beyond time that measurable amt of drug is present
What type of bacteria are aminoglycosides effective against?
gram - enteric bacteria , esp in bacteremia and sepsis
What can be combined with aminoglycosides to treat endocarditis? TB?
vancomycin or penicillin for both
MOR against aminoglycosides
inactivation of aminoglycosides by plasmid encodied transferase enzymes
impaired entry of aminoglycoside into cell
modification of ribosomal binding site
**transferase mediated R is main type**
Absorption of aminoglycosidES
poor from GI tract, give IM
highly polar that don't enter cells readily, largely excluded from CNS and eye
usually only high levels are found in UTI
Uses of SM?
2nd line agent for TB tx, used in combo with other agents to prevent R
What are tobramycin a nd gentamycin used to treat?
which is cheaper?
sepsis and pneumonia from gram - bacteria that are R to other drugs
used in combo with B-lactam (penicillin)
burns, wounds, skin lesions

what s amikacin used to treat?
resistant micro-organisms
it si R to many enzymes that inactivate gentamycin and tobramycin
what are neomycin adn kanamycin used to treat?
only topical (injected in to joints/pleural cavity,) and/or oral use (to cleanse large bowel for elective colorectal surgery)
Adverse effects of aminoglycosides
all are nephrotoxic
ototoxicity when used for >5 days --> auditory and vestibular damage (ototoxicity is irreversible)
which aminglycosides are the most nephrotoxic?
how is it made worse?
is it reversible?

concurrent use of loop diuretics

Which aminoglycosides are the most ototoxic?
for hearing:

for vestibular:
MOA chloramphenicol
binds to 50S ribosomal subunit, interferes with protein synth
spectrum of chloramphenicol?
aerobic and anaerobic gram +/- bacteria (esp gram -, in bacteremia and sepsis)
what is chloramphenicol commonly combined with?
(used to treat endocarditis and tb)
MOR to chloramphenicol?
production of chloramphenicol acetyltransferase (plasmid encoded enzzyme that inactivats the drug)
Pharmacokinetics of chloramphenicol
rapidly and completely absorbed after oral admin
widely distributed to all tissues and body fluids (incl CNS and CSF)
penetrates cell membrane readily
How is chloramphenicol cleared primarily from body?
Uses of chloramphenicol
don't use systemically, bad side effecs and widespread R
Rickettsial infections in children <8 yo
alt to B-lactam for bacterial meningitis caused by pen-R strianst of pneumococcus and meningococcus
eye infectiosn (penetrates ocular tissue and is broad-specrum)
Adverse rxns to chloramphenicol
GI probs (N/V/diarrhea in adults, not kids, candidiasis)
bone marrow probs (aplastic anemia and RBC suppression)
toxicity for neonates (lack liver enzymes to detox drug)
intearctions with other drugs (inhbiits liver enzymes)
what can happen to infants taking chloramphenicol
gray baby syndrome w vomiting, flaccidity, hypothermia, gray color, shock, colllapse
what drug interactinos are there w chloramphenicol
bacteriostatic protein synth inhibitors
antagonizes cidal drugs (like penicillin and aminoglycosides)
MOA of macrolides
bind 50S ribosomal subunit
spectrum of macrolides
gram +
strep, staph, pneumococci, corynebacteria
MOR of macrolides
reduced perm of cell membrane or active efflux
production of esterases that hydrolyze macrolides
modifications of ribosomal binding sites by chromosomal mutation or methylation
Pharmacokinetics of macrolides
widely distributed, except brain and CSF
traverse placenta and reach fetus
not a prob in pts with renal probs
What happens to macrolides in stomach
gets destroyed by acid, so must have enteric coating
which macrolide has longest t 1/2? how long/
3 days
Clinical uses of macrolides
corynebacterial infections
resp, neonatal, ocular, and genital chlamydial infections
community acquired pneumonia
adverse effects to macrolides
GI (anorexia, N/V/D, stim of gut motility)
liver toxicity --> acute cholestatic hepatitsi (hypersens rxn?)
Drug interactiosn
which macrolide drugs cause drug interactions? whihc ones don;t?
erythromycina nd clarithromycin metabolites inhbiit p450 increasesing serum [] of teophylline, oral anticoags, cyclosporine, methyprednisolone
azithromycin doesn't affecct p450
Antimicrobial activity of linezolid?
static or cidal?
gram + aerobes and anaerobic cocci
gram + rods (corynebacteria and listeria)
generally static except against streptococci (cidal)
MOA linezolid
inhibits protein synth by preveting formation of ribosome complex that initiates protein synth
MOR of linezolid
unique binding site on 23S ribosomal RNA of 50S subunit
so, no x-R with other drug classes
R from mutation of linezolid binding site on 23S ribosomal RNA
pharmacokinetics of linezolid
100% bioavailable after oral admin
doesn't affect p450
Clinical uses of linezolid
nosocomial pneumoania
strep/MRSA skin infections
reserved for tx of infections caused by MDR gram + bacteria
Adverse rxs to linezolid
GI, HA, rash
thrombocytopenia (esp if >2wks)
weak MAOI (watch out w tyramine)
peripheral and optic neuropathy
What is quniupristin-dalfoprisitn?
combo of 2 streptogramins
cidal for most organisms
gram +, MDR orgs and MRSA
R to streptogramins
modification of ribosomal binding site of quinupristin
inactivation of dalfopristin
drug efflux
are dose-adjustments needed for streptogramins in pts with renal probs
adverse rxns to streptogramins
painat infusion site
inhibit CYP3A4
MOA of tetracyclines
binds 30S ribosomal subunit, interferign with protein synth
spectrum of tetracyclines
gram +,-
MOR against tetracycline
decreased intracellular accumulation d/t impaired influx or increased efflux by active transport protein pump
ribosome protection d/t production of proteins that interfere with tetracycline ribosome interactions
enzymatic inactivations of tetracyclines
which tetracycline has best oral bioavailabity?
what affects oral bio?
doxy and minocycline
food decreases absorption (Ca, Mg, Fe, Al, dairy, antacids, and high pH)
distribution of tetracyclines
everywhere but CSF
tetra x placenta and enters breast milk
which tetracycline is best to use in renal failure
dosing of oral doxy?
1x day, absorption not affected by food
adverse rxns to tetracyclines
binds Ca so affects bone and tooth formation
deposited in fetal teeth
impar hepatic fxn (esp during preg)
RTA, N retention
DVT if given IV, IM is painful local irritiation
UV sensitization
vestibular rxns