Mechanism

Mechanism
Spectrum
of Activity
Pharmacology Indications
Indications
Mechanism
of Actionof Action
Mechanism
of of Spectrum
of Activity
Pharmacology
for Usefor Use
ToxicityToxicity
Mechanism
Mechanism
Action
of Action
Mechanism
Mechanism
Spectrum
Spectrum
of Activity
Activity
of ActivityPharmacology
Pharmacology
Indications
Indications
for for
Use
Toxicity
Resistance
Mechanism
of ofAction
Mechanism
ofof of
Spectrum
of
Pharmacology
Indications
for Use
Use Toxicity
Toxicity
Resistance
Mechanism of Action
Mechanism of
Spectrum of Activity Pharmacology
Indications for Use
Toxicity
Resistance
Resistance
Resistance
sequential
Sulfa
Broad
spectrum
combo
antibiotic
1:5
UTIs
hypersensitivity
rxns
Trimethoprimbinds
penicillin
binding
beta-lactamase
bactericidal
some
oral
use
hypersensitivity
Penicillin
Resistancein
st
bactericidal
Beta-lactamase
high
targets
affinity
d-ala-d-ala
for
problem
parenteral
serious
Gram+
low
risk
of
interference
with
folic
decreased
bactericidal
ratio
of
TMP:Sulfa;
prostatitis
(rash,
fever),
rare
Sulfamethoxazole
bactericidal
like
penicillins,
inhibit
permeability

failure
hydrophilic
molecules
common
infections
hypersensitivity
(rash,
1 Vancomycin
Generation
proteins binds
(transpeptidases,
cleaves
beta-lactam
Gram+
metabolism
(rash; dose
anaphylaxis)
peptidyl
presence
of fecium
enzyme
bacteriostatic minor
higher
levels
with
NOT
drug of penicillin
choice
related
bone
Chloramphenicol
inhibitors
most
Gram+
plasmid-mediated
petapeptide;
blocks
beta- of
2 ring
enterococcus
Mostly
nephrotoxicity
wide
tissue
acid
synthesis
permeability
Gram+
serum
ratio 1:20
pneumocystis
carinii
Stevens
Johnson
(TMP-SMZ) carboxypeptidases);
Gram+
cocci
Cephalosporins
enzymatic
rxns
needed
cephalosporins
to(plasmid)
that by
achieve
excellent infections
urticaria,to
eosinophilia,
surgical in
prophylaxis
and
inactivates
streptococci,
excreted
act
as
haptens
transferase,
chloramphenicol
may
be bacteriocidal
ORAL
vs IV
forinfection
any infection;
used marrow
depression
steps
in cell
has
plasmid-mediated,
including
betapts(AIDS)
phlebitis
(frequent)
distribution
and
Sulfa
is in
aawall
structural
increased
PABA enterococci,
staphylococci,
oral
and
parenteral
syndrome
(mucosal
s. pneumoniae,
s. aureus,kidneys
forlactamases
stable
bacterial
wall
reach
receptor
sites
drugvialevels
in lung, allergic
fever,
anaphylaxis
skinin and
soft tissue
enzymes
involved
cell
drug
tubular
combine
withaplastic
human
component
of
the
50s
transacetylase
against
pneumococcus
well
distributed
more
developing
(rare)
anemia
Sulbactam
synergistic drug synthesis
Cefazolin,
synthesis
at
an
earlier
readily
transferable
lactamase
producers
due toproteins
infected
pleural,
analog
of PABA;
production
well
good infections
diarrheal
illness
due and
illness
red
man syndrome:
NOT streptococci,
enterococci listeria,secretion
by binding
to destroyed
kidney,distributed;
muscle, bone,
rare)cutaneous
by betainfections
wall (peptidoglycan)
(chromosomal
or
meningococci,
ribosome
(acetylates
the drug)
and
neisseria
throughout
body;
CSF world
inseen
neonates
get
gray
Clavulanic
acid
step
than
beta-lactams
resistance
(plasmids
and
methicillin
pericardial,
synovial,
resistant
s.
pneumoniae
combo
competes
for
enzyme
TMP
NOT
enterococci
levels
in
lungs,
to
salmonella,
shigella,
in
AIDS
pts)
Cephalothin,
when
given
in
toorarely
rapid
Gramrods
PBPs
placenta,
interstitial,
leukopenia and
lactamase
biosynthesis
plasmid mediated)
treponema
pallidum
(probenecid
will
major
determinant=
broad
spectrum
levels
30-50%
of
typhoid
fever
(s.
baby
syndrome
Tazobactam
have
been
shown
resistant
staph
aureus;
ascitic
fluids
and
or
MRstaph
dihydropteroate alteration
synthesis
of
Gramkidneys,
biliary
tree,
enterotoxigenic
e.
coli
GI

nausea,
Cephalexin (oral),
an
infusion
get
e.
coli,
klebsiella,
proteus
synovial,
and
hemolytic
anemia
of
PBPs
Gram- can change (syphilis),
most
block)
penicilloyl
aerobic
serum
w/o
typhi)
(vasomotor
collapse,
Combination:
binds synthetase
PBPs; enzymes Gramcan ofchange
bactericidal
; klebsiella,
broad
capable
replicating
streptococcus,
meninges
dihydrofolate
e. coli,Gram+
and
CNS
diarrhea
Cefaclor (oral)
generalized
rash, with
mirabilis
peritoneal
fluids,
and inupper and lower(uticariavomiting,
superinfection
porin
channel
anaerobes
well
distributed
to
and latedistention,
most
Graminflammation
meningitis
in
abdominal
(penicillin + betainvolved
in cell
porin
channel
spectrum
in
s.
aureus)
clostridia,
listeria,
TMP
is a wall
competitive
reductase
with
proteus,
salmonella,
excreted
partially
by
metabolized
kidneys
respiratory
infections
(rare)
hepatitis,
uticaria
(due
to
urine
fungi
or
resistant
permeability
poor most
activity
against
lungs,
liver,
kidney,
rxns)
anaerobes
metabolized
to
allergic
ptsby cyanosis)
lactamase inhibitor
biosynthesis
permeability
Gram+
bacillus
transposable
element
inhibitor of
decreased
for
shigella,
vibrio,
in
liver,
excreted
in penicillin
infections
causedminor
megoblastic
anemia,
histamine
release)
eliminated
via kidney
Gramorganisms
preventing
drugaffinity
Gramrods
muscle,
bone
and
determinant=
inactive
metabolite in (pneumococcus,
drug organism
from streptococci,
beta-lactamase
that
allows
to ricksettsia
dihydropteroic acidpreventing
TMP
neisseria, h influenzae
urine
p. cepacia, nocardia
increased
serum
(?)
ototoxicity
(probenecid blocks
phlebitis,
false+ tests
from
reaching
placenta
benzylpenicilloate
liver
hemophilus, neisseria)
Piperacilin +
reaching
receptor
site of
enterococci,
sense
vancomycin
and
inhibitors
overproduction
misc.
creatinine
of some
(Coombs,
glucose)
receptor
site
high secretion
urinary and
(anaphylaxis
and
rickettsial
infections
pumps
Tazobactam
activate
transcription meningococci,
dihydrofolate
pneumocystis,
(tazobactam) high efflux
compounds)
efflux
pumps
bilewell
concentrations
accelerated
rxns)
bind DNA-DNA alteration
mutations
in
bactericidal
absorbed orally empiric therapy for
well-tolerated
nd Quinolones
of
PBPs
treponema
pallidum
leading
to
replacement
reductase
affinity
for
plasmid
bactericidal
like penicillins,
inhibit
permeability

failure
hypersensitivity
(rash,
parenteral
drugs
upper
respiratory
alteration
of
PBPs
stnocardia, chlamydia
2 Generation
gyrase (topoisomerase
topoisomerase
II or (syphilis),
IV 1 generation
andparenterally
community-acquired
GI symptoms
ind-ala-d-ala
most
of
mediated
Gram+
cocci
Cephalosporins
enzymatic
rxnsenzymes
needed
of(esp.
cephalosporins
towith durticaria,
eosinophilia,
(esp.
in Gram+)
Gram+)
hydrophilic
molecules pneumonia
tract infections (h.CNS
II) complex
and blocks
resistance
is
excellent
tissue
symptoms
(nalidixic
acid)
ala-d-lactate
s.anaerobes
pneumoniae, less s. oral that
for stable
bacterial
wall reach
receptor sites(rather
anaphylaxis
excellent
beta-lactamase
bactericidal
and achieve
IV bone
is fever,
common
Ampicillin
influenzae)
binds
pencillin
binding
further
DNA
chromosomal
Gram- enterics
distribution;
and complicated
UTI rash
or allergic
rxns
(rash,
Gramaureus,
NOT enterococci
synthesis
by
binding
to
rare) drug fever)
destroyed
by
betadrug< levels
in lung, respiratory
(aminopenicillins)
cleaves
beta-lactam
Gram+
GI tracttract
flora
proteins
replication
than
plasmid)
(UTIs)
CSF
serum
uticaria,
pseudomonas
Cefuroxime
GramPBPs blocks topoisomerase
leukopenia and
rarely
lactamase
kidney,
muscle, bone, infections
nd rodsenterococci
ringcan
and(cefuroxime
inactivates
streptococci,
infections
(transpeptidases,
emerge
quickly
high
intracellular
photosensitivity
(esp.
2 generation
aeruginosa,
Cefoxitin
e.
coli,
klebsiella,
proteus
placenta,
interstitial,
is
STABLE
to
plasmid
hemolytic
anemia
drug
(unless
they
express
carboxypeptidases);
IV inteferes with
during therapy esp. bacteroides,
concentration (PMNs) serious infections like with additional F or Cl
(norfloxacin,
proteus
Cefotetan
mirabilis
synovial,
and by
(chromosomal
or or beta-lactamases)
with
enzymes
involved
cel
separation
of in mediated
with penicillinases)
s.toaureus,
p.
ciprofloxacin)
most
eliminated
osteomyelitis,
at superinfection
position
8similar
of drug
bactericidal;
HUGE
Carbapenems
binds
PBP-2
STABLE
betaallergic
rxns
to
cefuroxime
covers
h.
peritoneal
fluids,
and
in
plasmid
mediated)
Gramalteration
of
PBPs
fungi
or
resistant
l permeability
interlockedthrough
replicatedlactamase;
aeruginosa;
a single spectrum
better Gramkidneys (trovofloxin
pneumonia, soft tissuepenicillin
structure)
butchange
alternate
rdurine
influenzae
Gramcan
hemophilus,
e.coli,
Gramorganisms
DNA
molecules
mutation
p.
liver
function
wall
biosynthesis
Imipenem
3 gen. eliminated by STDs: gonorrhea,
killscoverage,
most
enzymes
that leads
can to salmonella,
porin
channels
Imipenem
may
porin
channel
shigella
eliminated via kidneychancroid, chlamydial (?)
cefoxitin
andGram+,
cefotetan
phlebitis,
false+
other
sites
of
action
resistance
aeruginosa
liver)
abnormalities
rare tests
better
penetration
Meropenem
hydrolyze
Gram-,
and
lower
seizure
permeability
(but
many
Gramhave
(probenecid
increased
anaerobe
coverage,
(Coombs,
glucose)
(?) outer
RNA and
active of
efflux
Gram+
s. aureus
and decreased
oralblocks
urethritis
fatalities
following
through
mb protein
of alteration
porinsystem
anaerobic
bacteria
threshold
preventing
drug
plasmid
mediated
secretion following
of some
bacteroides
synthesis
(?)
in
Gram+
and
Gramb.
anthracis
absorption
empiric
therapy
for
trovafloxacin
Gram- than penicillin Gchannels
including
from reaching
resistance)
rd
compounds)
coadministration
of
travelers diarrhea
joint arthralgias or
3 generation
and better binding to receptor site
rd
pseudomonas
like penicillins, inhibit permeability failure bactericidal
cefotaxime=
drug of swelling
hypersensitivity
(rash,
cefotaxime
3 Generation
metal
cations and
(infectious
diarrhea)
in kids
(levofloxacin)
PBPs
aeruginosa;
pumps to
Cephalosporins
cefotaxime:
highly
enzymatic rxns needed of efflux
cephalosporins
choice forresistant
meningitis urticaria, eosinophilia,
ceftriaxone achievemulti-drug
improved Gram+
(antacids)
does
NOTenteric
kill:
alteration
PBPs
for stable bacterial wall reach
receptorof sites
fever, anaphylaxis
active
against
s. and
good CSF levels; TBceftriaxone=
Gram(esp. in toGram+)
MRSA,
enterococcus,
synthesis by binding to STABLE
plasma
ceftazidime adequateoutpatient coverage of rare)
pseudomonas
pneumoniae;
n.
cefotaxime
binds
Semisynthetic
c. mycoplasma,
difficile h.
bulk prevents
Methicillin
least serious septic pneumococcal
PBPs penicillin binding mediated
leukopenia and rarely
beta- them bactericidal
CSF levels
meningitides,
proteins
penicillinaseceftriaxone
primarily
for protein
from getting
bactericidal;
bound of longer
the staphylococcus
Monobactams
can pts,
use n.in gonorrhea,
place of an
only (transpeptidases,
binds Gram- lactamases
STABLE
to beta- used
and
hemolytic anemia
legionella,
anaerobes
ceftriaxone
influenzae, e. coli,
resistant
penicillins carboxypeptidases);
ceftazidime
through Gramgrouphalf-life and more
NARROW spectrum
staphylococci
aminoglycoside
CNS
lyme disease
aureus
infections
PBPs
lactamase
alteration
of PBPs
superinfection with
klebsiella,
NOT Gramp.
AztreonamOxacillin, enzymes involved in cell porins
(Nafcillin,
ONLY aerobic
Nafcillin
high
Gram+
can use in penicillin
fungi or resistant
(cellulites,
active
than
aeruginosa
Methicillin)
wall (peptidoglycan)
rods; including p.
biliarycefotaxime;
excretion
allergic pts (little
crossGram- organisms
pneumococci,
sepsis)
aendocarditis,
single
biosynthesis
ceftriaxone:
aeruginosa s. pneumoniae,
Isoxazolyl
phlebitis, false+ tests
streptococci,
IM does can kill reactivity)
for
bulky side chains inhibit
n. gonorrhea,
b. burgdorferi
penicillins
(Coombs, glucose)
NOT
enterococci
12-24 hrs
action of staph betaceftazidime: less Gram+(parenteral and IV
lactamases
activity but can kill p. forms)
aeruginosa
Drug

Drug