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Drug Family

Cell wall synthesis

Drug name

Penicillins
Natural Penicillins

Penicillin V
Penicillin G

Aminopenicillins

Amoxicillin
Ampicillin

Amoxicillin + Clavulanate
Aminopenicillins plus lactamase inhibitors

Penicillinase resistant
penicillins

Ampicillin+Sulbactam
Nafcillin
Oxacillin
Dicloxacillin

Extended spectrum penicillin Piperacillin+Tazobactam


plus B-lactamase inhibitor Ticarcicillin+Clavulanate
Cephalosporins

1st Generation

Cefazolin
Cephalexin
Cefadroxil

2A Generation

Cefuroxime
Cefaclor
Cefprozil

2B Generation

Cefoxitin
Ceftibuten
Cefdinir
Cefpodoxime

Ceftriaxone
Cefotaxime
Cefixime
Ceftazidime
3rd Generation

Ceftaroline

4th Generation

Cefepime

Monobactam

Aztreonam

Carbapenems

Imipenem/Cliastatin
Meropenem
Doripenem
Ertapenem

Glycopeptides

Vancomycin

Fosfomycins

Fosfomycin

Inhibitors of DNA/RNA
Synthesis

Sulfa Drugs

Trimethoprim+Sulfamethoxazole

Rifampin

Rifampin

Fidaxomicin

Fidaxomicin
Ciprofloxacin

Fluoroquinolones

Levofloxacin

Moxifloxacin
Inhibitors of Protein Synthesis
Aminoglycosides

Gentamicin
Tobramycin
Amikacin
Azithromycin

Macrolides
Clarithromycin
Tetracycline
Tetracyclines

Doxycycline
Minocycline

Glycylcycline

Tigecycline

Lincosamide

Clindamycin

Oxazolidinone
DNA Damaging Agents

Linezolid

Nitrofurantoin

Metronidazole
Cell Membrane Damaging
Agents

Lipopeptides
Polymyxins

Daptomycin
Polymyxin B
Colistin

Routes of administration

Mechanism of action

PO
IM, IV

inhibition of peptidoglycan
cross linking

PO
IV

inhibition of peptidoglycan
cross linking

IV

the B lactamase inhibitor


allows the aminopenicillin to
block peptidoglycan cross
linking

IV
IV
PO

resistant to a particular beta


lactamase

PO

IV- used more often than Tic/Clav


IV

IV
PO
PO

IV, PO
PO
PO

IV

same as other cillins

inhibition of peptidoglycan
cross linking
inhibition of peptidoglycan
cross linking

same

PO
PO
PO

same

same

IV
IV
PO
IV
IV
IV

same

IV

same as other B-lactams

IV
IV
IV

same as other B-lactams

IV

primarily IV, PO for C dif

binds to D-Ala and blocks


peptidoglycan synthesis

PO - suspension

inhibits the first step in


peptidoglycan synthesis by
binding to the enzyme that
catalyzes the formation of Nacetylmuramic acid

IV and PO

in combination act
synergistically to inhibit
nucleic acid synthesis,
inhibition of 2 enzymes in
DNA synthesis pathway

IV and PO

inhibits DNA-dependent RNA


polymerase-> RNA synth

PO only

inhibits transcription of
bacterial RNA polymerase

IV and PO

IV and PO

block function of DNA gyrase

IV only

bind 16S rRNA component of


30S ribosome, leads to tln
inhibition

inhibit elongation of peptide


chain at 50S ribosome

PO
PO
IV and PO

block access of tRNAs to 30S


ribosome

PO

IV

block access of tRNAs to 30S


ribosome

IV and PO

inhibits elongation of peptide


chain at 50S ribosome

IV and PO

blocks initiation of
translation at 50S ribosome

PO

forms DNA damaging ROS

IV and PO

anaerobic nitro-reduction to
radicals that damage DNA

IV

inserts into the cytoplasmic


membrane in a calcium
dependent manner, results
in membrane depolarization
and loss of intracellular
components

IV
IV

act as cationic detergent in


Gram - membranes

Gram +

Gram -

most streptococci, some enterococci minimal

most streptococci, some enterococci, E. coli, P. mirabilis, some strains


Listeria monocytogenes
of H. influenzae

most streptococci, some enterococci, E. coli, P. mirabilis, more strains


Listeria monocytogenes, methicillin- of H. influenzae, some Klebsiella
sensitive S. aureus
spp.

***drug of choice for MSSA, also


covers most streptococci

none

MSSA, most streptococci, enterococci

**Pseudomonas, plus many


others

MSSA, streptococci

E. coli, some Klebsiella

MSSA, streptococci

poor MSSA, some streptococci

MSSA, streptococci

E. coli, some Klebsiella, H.


influenzae, Cefuroxime, Cefaclor
cover Moraxella catarrhalis and
more H. influenzae

same as 2A

moderate spectrum, NOT


Pseudomonas

MSSA, streptococci

moderate spectrum, NOT


Pseudomonas

poor

broad spectrum, ***Pseudomonas


coverage

**MRSA, MSSA, Streptococcus

moderate spectrum, NOT


Pseudomonas

MSSA, streptococci

broad spectrum, ***Pseudomonas


coverage

none

broad spectrum, ***Pseudomonas


coverage

MSSA and strep, some enterococcus

broad spectrum, ***Pseudomonas


coverage

MSSA, strep

moderate spectrum, NOT


Pseudomonas

very good gram + coverage,


including MRSA and all strep, nonVRE E. faecium and E. faecalis

NONE

good spectrum against


Staphylococcus spp, Streptococcus
spp and Enterococcus spp

>95% of E. coli susceptible and a


few others but NOT Pseudomonas

most strains of Staph aureus and


Staph epidermidis including most
MRSA and MRSE

good spectrum including


Stenotrophomonas maltophiliaNOT including Pseudomonas

can be used in combinations for


staph and strep

limited, prophylaxis for N.


meningitidis

some activity against Staph, strep,


enterococci

none

not much, some strep but not S.


pneumoniae

broad spectrum, ***Pseudomonas


coverage

good for S. pneumoniae

broad spectrum, ***Pseudomonas


coverage

good for S. pneumoniae

moderate spectrum, NOT


Pseudomonas

used in combination with a cell wall broad spectrum, ***Pseudomonas


inhibitor- good for Enterococcus,
coverage, amikacin best for
some staph and strep
Pseudomonas
decent activity for S. pneumoniae,
some other strep and MSSA, not first
line except pen/ceph allergies

H. influenzae, N. gonorrhea, M.
catarrhalis, Campylobacter, H.
pylori

H. influenzae, M. catarrhalis,
S. pneumoniae, Enterococcus, MRSA
Campylobacter, E. coli, Klebsiella,
and MSSA
some N. gonorrheae

broad spectrum, MRSA, VRE

moderate spectrum, NOT


Pseudomonas

good against MRSA, MRSE, some


strep but not first line

none

broad spectrum, including MRSA,


most VRE

none

most E. coli, some Klebsiella,


good for most Gram + including VRE some Enterobacter

none

H. pylori

extensive G+ activity, MRSA, MRSE,


MSSA, drug resistant strep and most
VRE
none

none

broad spectum, ***Pseudomonas


coverage

Anaerobes

Atypicals

Renal adjustment

mouth anaerobes

Treponema pallidum yes

mouth anaerobes

T. pallidum, B.
burgdorferi

yes

good anaerobic
coverage including B.
fragilis

T. pallidum, B.
burgdorferi

yes

none

none

NO**

good anaerobic
coverage including B.
fragilis

T. pallidum

yes

mouth anaerobes

none

yes

none

yes

mouth anaerobes

moderate B. fragilis

none

yes
none

mouth anaerobes
only

yes

mouth anaerobes
only

CA-meningitis, N.
gonorrhea, B.
burgdorferi

NO***

yes

none

mouth anaerobes
only

none

yes

none

none

yes

broad spectrum, good


B. fragilis

yes
none

PO used for C. difficile none

yes

none

none

yes

none

Nocardia,
Pneumocystis
jiroveci, Toxoplasma
gondii
yes

none

M. tuberculosis

**NO

Primary use is to
treat C. dif, active
against Gram +
anaerobes

none

yes
yes

poor anaerobic
activity

Chlamydia,
Mycoplasma,
Legionella

better anaerobic
coverage, incl. B.
fragilis

**NO

none

none

some anaerobes but


not B. fragilis

Legionella,
Mycoplasma,
Chlamydia, M.
avium (MAC)

good anaerobic
coverage

B. burgdorferi,
Rickettsia

good anaerobic
coverage, including
B. fragilis

yes

good anaerobic
coverage but some B.
fragilis are resistant none

yes

**NO
yes

***NO

no but needs
hepatic
adjustment

***NO

none

none

yes

none

none

yes

Extensive anaerobic
activity including C.
diff, B.fragilis

Trichomonas,
Giardia

yes

none

none

yes

none

none

yes

Toxicities

Pharmacodynamics

Cidal/Static

hypersensitivities common,
seizures at high doses

Time Dependent

Cidal

hypersensitivity, seizures

time dependent

cidal

hypersensitivity, seizures,
diarrhea

Time Dependent

cidal

hypersensitivity, seizures,
hepatotoxicity, interstitial
nephritis

time dependent

cidal

hypersensitivity, seizures,
diarrhea

Time Dependent

cidal

hypersensitivities common,
seizures at high doses

Time Dependent

cidal

hypersensitivity, seizures

Time Dependent

cidal

hypersensitivity, seizures

Time Dependent

cidal

hypersensitivity, seizures

time dependent

cidal

biliary sludging at high doses

time dependent

cidal

hypersensitivity, seizures

hypersensitivity, seizures

Time Dependent

cidal

can be used safely in pts with


allergies to pens, cephs

time dependent

cidal

increased risk of seizures - only


Imipenem

time dependent

cidal

Red Man's syndrome,


nephrotoxicity, neutropenia, rare
allergies
exposure dependent

cidal

well tolerated

exposure dependent

cidal

skin rash- mild to Stevens


Johnson syndrome, TMP-Sulfa
also inhibits secretion of
creatinine and may lead to
increased serum levels,
hyperkalemia, acute tubular
necrosis, acute interstitial
nephritis

time dependent

components static
but together cidal

orange-red discoloration of tears,


sweat, urine, PO formulation
causes GI symptoms,
hepatotoxicity ranging from mild
to fulminant hepatitis
exposure dependent

cidal

well tolerated

cidal

concentration dependent

cidal

reversible nephrotoxicity, rare


irreversible ototoxicity

concentration dependent

cidal

some GI symptoms,
Clarithromycin - drug interactions
common, also torsades de
pointes (V-Tach)

exposure dependent

static

exposure dependent

static

headache, dizziness, imsomnia,


mood change, seizures, tendinitis
- important concern for elderly
pts, high risk of C. diff

GI symptoms including
esophageal ulceration,
photosensitivity, in childrendiscoloration of teeth

same as tetracyclines, plus 25%


of pts nausea and vomiting

exposure dependent

static

NVD, very high risk of C. diff

exposure dependent

static

myelosuppression,
thrombocytopenia, serotonin
syndrome

time dependent

static

GI, pulmonary- cough, dyspnea,


chronic use can lead to pulm
fibrosis

GI, metallic taste, peripheral


neuropathy

concentration dependent cidal (?)

muscle pain, weakness, need to


monitor CPK levels, rash

concentration dependent cidal

nephrotoxicity, neuromuscular
blockade, paresthesias

cidal (?)

Other notes

used for skin, soft tissue


infections, prophylaxis.
Cefadroxil has a longer half
life than cephalexin

can be used for sinusitis,


otitis media
can be used for
intraabdominal and pelvic
infections

ceftaroline = cetriaxone +
MRSA coverage

ceftaroline = cetriaxone +
MRSA coverage

Cliastatin inhibits enzyme


that hydrolyzes imipenem

80% of E. faecium and 20%


of E. faecalis are resistant

only used for cystitis in


females in USA

drug interaction with


warfarin, monitor for
increase in INR

many drug interactions,


needs to be used in
combination due to
emergence of resistance,
fairly toxic, can be used to
break apart biofilms
only clinical use is to treat C.
difficile, does less to disrupt
the normal flora of gut than
other antibiotics

lots of resistance emerging,


use carefully

require careful monitoring


for toxicity, often used in
combination with other
antibiotics

good for CA-pneumonias

can't use for bacteremia due


to low serum levels

rarely used due to C. diff


risk, primary role is for
skin/soft tissue infections for
pt w/pen allergy, also part of
combo therapy for
necrotizing fasciitis

used for resistant Gram +


infections

very low serum levels, only


used for cystitis
first line treatment for C dif,
extensively used for
anaerobic infections

used for resistant Gram +


bloodstream infections, does
not efectively treat
pneumonia
drug of last resort for highly
resistant Gram negatives