Antibiotic Classification &

Mechanism
Author: Derek Moore
Topic updated on 02/17/15 12:52pm

Overview of By Mechanism

FLUOR
PENI CEPHA
AMINO MON CARB MAC
OQUIN
OTHE
CILLI LOSPO
GLYCO OBAC APEN ROLI
OLONE
NS RINS
SIDES TAMS EMS DES
S
Natru First Ciproflox Amikac Aztre Ertap Azithr Vanco
al genera acin
in
onam enem omyc mycin

tion

(Cipro) Gentam
Levoflox icin
Penic Cephal acin
Kanamy
illin G othin (Levagui cin
Penic Cefazol n)
Neomyc
illin- in
Moxiflox in
VK (Ancef, acin
Tobram
Kefzol) (Avelox) ycin
Cepha Norfloxa
pririn cin
Cephal
exin
(Keflex)
other
Penic Secon
illinas
d
e Genera
Resis tion
tant
Methi Cefaco
cillin r
Nafcil Cefotet
lin
an
Oxaci (Cefota
llin
n)
other other

Imien in
Rifam
em
Clarit pin
Merop hrom Doxyc
enem ycin ycline
Dirith Linezo
romy lid
cin Tetrac
Eryth ycline
romy Trimet
cin hopri
Clind m/
amyc sulfam
in
ethox
acole

Amin Third
openi Genera
cillins tion
Ampi Ceftriax
cillin one
(Rocep
hin)
other
Fourth
Genera
tion
Cefpiro
me

Cefepi
me
Antibiotic Grouping By Mechanism
Cell Wall Synthesis Penicillins
Cephalosporins
Vancomycin
Beta-lactamase
Inhibitors
Carbapenems
Aztreonam

Polymycin
Bacitracin
Protein Synthesis
Inhibit 30s Subunit
Inhibitors
Aminoglycosides
(gentamicin)
Tetracyclines
Inhibit 50s Subunit
Macrolides
Chloramphenicol
Clindamycin
Linezolid
Streptogramins
DNA Synthesis
Inhibitors
RNA synthesis
Inhibitors
Mycolic Acid
synthesis inhibitors
Folic Acid
synthesis inhibitors

Fluoroquinolones
Metronidazole
Rifampin
Isoniazid
Sulfonamides
Trimethoprim

Antibiotic Classification & Indications

Inhibits Cell Wall Synthesis
Penicillins
(bactericidal: blocks cross linking via
competitive inhibition of the transpeptidase
enzyme)
Class/Mech
Drugs
Indicatio Toxicity
anism
ns
(**Drug
of
Choice)
Penicillin Penicillin G
Hyperse
Strep.
Aqueous
nsitivity
pyogene
penicillin G
reaction
s
Procaine
Hemolyti
(Grp.A)**
penicillin G
c
Step.
Benzathine
anemia
agalacti
penicillin G
ae
Penicillin V
(Grp.B)*
*
C.

perfringe
ns(Bacill
i)**
Aminopeni Ampicillin
cillins
Amoxicillin

Penicillinas Methicillin
e-resistant- Nafcillin
penicillins Oxacillin
Cloxacillin
Dicloxacillin
Antipseudo Carbenicillin
monal
Ticarcillin
penicillins Piperacillin

Above +
Gramnegative:
E.
faecalis*
*
E. Coli**

Above

Above + Above
PCNase- +
producin Interstiti
gStaph. al
aureus nephritis
Above + Above
Pseudo
monas
aerugino
sa**

Cephalosporins
(bactericidal: inhibits bacterial cell wall
synthesis via competitive inhibition of the
transpeptidase enzyme)
1st
Cefazolin
Staph. Allergic
generation Cephalexin aureus** reaction
Staph. Coombs
epidermi -positive
dis**
anemia
Some
(3%)
Gramnegative
s:
E. Coli
Klebsiell
a
2nd
Cefoxitin
Above + Allergic
generation Cefaclor
Gram- Reactio
Cefuroxime negative n
ETOH
Disulfira
m

reaction
3rd
Ceftriaxone Above + Allergic
generation Cefotaxime Gram- Reactio
Ceftazidime negative n
Cefepime
Pseudo ETOH
(4th
monas Disulfira
generation)
m
reaction
Other Cell Wall Inhibitors
Vancomyci Vancomycin
Red
MRSA**
n
man
PCN/Ce
(bactericidal
syndrom
ph
: disrupts
e
allegies*
peptioglyca
Nephrot
*
n crossoxicity
S.
linkage)
Ototoxici
aureus
ty
S.
epidermi
dis
BetaClavulanic
lactamase Acid

Hyperse
nsitivity

Inhibitors Sulbactam
(bactericidal Tazobactam
: blocking
cross
linking)

Reactio
aureus**
n
S
Hemolyti
epidermi
c
s**
anemia
E.Coli**
Klebsiell
a**

Carbapene Imipenem (+
ms
cilastatin)
Meropenem
Doripenem
Ertapenem

Broadest
activity
of any
antibiotic
(except
MRSA,
Mycopla
sma)
Gramnegative
rods
Aerobes
Hospitalacquired

Aztreonam Aztreonam

infection
s
PolymyxinsPolymyxin B Topical
Polymyxin E Gramnegative
infection
s
Bacitracin Bacitracin
Topical
Grampositive
infection
s
Protein Synthesis Inhibition
Anti-30S ribosomal subunit
Aminoglyc Gentamicin Aerobic Nephrot
osides
Neomycin
Gram- oxicity
(bactericidal Amikacin
negative Ototoxici
: irreversible Tobramycin s
ty
binding to Streptomycin Enterob
30S)
acteriac
eae
Pseudo

monas
Tetracyclin Tetracycline
Hepatot
Rickettsi
es
Doxycycline
oxicity
a
(bacteriostat Minocycline
Tooth
Mycopla
ic: blocks
Demeclocycli
discolor
sma
tRNA)
ne
ation
Spiroche
Impaired
tes (Lym
growth
e's
Avoid in
disease)
children
< 12
years of
age
Anti-50S ribosomal subunit
Macrolides Erythromycin Streptoc
Coumad
(bacteriostat Azithromycin occus
in
ic: reversibly Clarithromyci H.
Interacti
binds 50S) n
influenz
on
ae
(cytochr
Mycopla
ome
msa
P450)
pneumo

nia
Chloramph Chloramphe H
Aplastic
enicol
nicol
influenz Anemia
(bacteriostat
ae
Gray
ic)
Bacterial Baby
Meningiti Syndro
s
me
Brain
absces
Lincosamid Clindamycin
Bacteroi Pseudo
e
des
membra
(bacteriostat
fragilis nous
ic: inhibits
S
colitis
peptidyl
aureus Hyperse
transferase
Coagula nsitivity
by
seReactio
interfering
negative n
with amino
Staph &
acyl-tRNA
Strep
complex)
Excellent
Bone
Penetrati

on
Linezolid
(variable)

Linezolid

Resistan
t Grampositives
Streptogra Quinupristin VRE
mins
Dalfopristin GAS and
S.
aureus
skin
infection
s
DNA Synthesis Inhibitors
Fluoroquinolones
(bactericidal: inhibit DNA gyrase enzyme,
inhibiting DNA synthesis)
1st
Nalidixic acid Steptoco
Phototo
generation
ccus
xicity
Mycopla
Achilles
sma
tendon
Aerobic
rupture
Gram +

Impaired
fracture
healing
2nd
Ciprofloxacin As
as
generation Norfloxacin Above above
Enoxacin
+Pseudo
Ofloxacin
monas
Levofloxacin
3rd
Gatifloxacin As
as
generation
above + above
Grampositives
4th
Moxifloxacin As
as
generation Gemifloxacin above + above
Grampositives
+
anaerob
es
Other DNA Inhibitors
Metronidaz Metronidazol Anaerobic Seizures

s
ole
e (Flagyl)
Crebelar
(bacteridical
dysfunct
: metabolic
ion
biproducts
ETOH di
disrupt
sulfram
DNA)
reaction
RNA Synthesis Inhibitors
Rifampin Rifampin
Staphylo Body
(bactericidal
coccus fluid
: inhibits
Mycoba discolor
RNA
cterium ( ation
transcription
TB)
Hepatox
by inhibiting
icity
RNA
(with
polymerase)
INH)
Mycolic Acids Synthesis Inhibitors
Isoniazid Isoniazidz
TB
Latent
TB
Folic acid Synthesis Inhibitors
Trimethopri Trimethoprim UTI
Thromb
m/Sulfona /Sulfamethox organis

mides
azole (SMX) ms
ocytope
(bacteriostat Sulfisoxazole Proteus
nia
ic: inhibition Sulfadiazine Enterob
Avoid in
with PABA)
acter
third
trimester
of
pregnan
cy
Pyrimetha Pyrimethami Malaria
mine
ne
T. gondii
Bacteria Overview
Gram Postive Cocci
Staphylococcus Staph. aureus
MSSA
MRSA
Staph. epidermis
Staph saprophyticus
Streptococcus
Strep pneumoniae
Strep pyogenes (Group

A)
Strep agalacticae (Group
B)
Strep viridans
Strep Bovis (Group D)
Enterococci
E. faecalis (Group D
strep)
Gram Positive Bacilli
Spore Forming
Bacillus anthracis
Bacillus cereus
Clostridium tetani
Clostridium botulinum
Clostridium perfringens
Clostridium difficile
Non-Spore
Forming

Corynebacterium
diphtheriae
Listeria monocytogenes
Gram Negative Cocci
Neisseria
Neisseria meningitidis
Neisseria gonorrhoeae
Gram Negative Bacilli

Enterics

Respiratory
bacilli
Zoonotic bacilli

Escherichia coli
Salmonella typhi
Salmonella enteridis
Shigella dysenteriae
Klebsiella pneumoniae
Serratia
Proteus
Campylobacter jejuni
Vibrio cholerae
Vibrio
parahaemolyticus/vulnific
us
Helicobacter pylori
Pseudomonas
aeruginosa
Bacteroides fragilis
Haemophilus influenzae
Haemophilius ducreyi
Bordatella pertussis
Yersinia enterocolitica
Yersinia pestis
Brucella

Francisella tularensis
Pasteurella multocida
Bartonella henselae
Other
Gardnerella vaginalis
Other Bacteria
Mycobacteria
Mycobacterium
tuberculosis
Mycobacterium leprae
MOTTS
Spirochetes
Borrelia burgdorferi
Leptospira interrogans
Treponema pallidum
Chlamydiaceae Chlamydia trachomatis
Chlamydophila
Rickettsia
Ehrlichia
Mycoplasmatace Mycoplasma
ae
pneumoniae
Ureaplasma urealyticum
Fungus-like
Actinomyces israelii
Bacteria
Nocardia

Antibiotic Resistance Mechanisms

Bacteria develop ability to hydrolyze
these drugs using lactamase
o confers resistance to penicillin
o e.g. E. coli, Staph epidermidis,
Pseudomonas aeruginosa, Klebsiella
pneumoniae
o add lactamase inhibitor e.g.
clavulanic acid in amoxicillinclavulanate (Augmentin)
Genetic mutation of mecA
o a bacterial gene encoding a
penicillin-binding protein. New PBP
has reduced affinity for antibiotics
o confers resistance to methicillin,
oxacillin, nafcillin
o e.g. MRSA

 Altered cell wall permeability

o confers resistance to tetracyclines,
quinolones, trimethoprim and
lactam antibiotics
Creation of biofilm barrier
o provides an environment where
offending bacteria can multiply safe
from the hoste immune system
Salmonella
Staph epidermidis
Active efflux pumps
o confers resistance to erythromycin
and tetracycline
o e.g. msrA gene in Staph
Altered peptidoglycan subunit
(altered D-alanyl-D-alanine

of NAM/NAG-peptide)
o confers resistance to vancomycin
o e.g. vancomycin resistant
enterococcus (VRE)
Ribosome alteration
o erm gene confer inducible resistance
to MLS (macrolide lincosamide
streptogranin) agents via methylation
of 23s rRNA
o demonstrate using D zone test
for inducible clindamycin
resistance in Staph and beta
hemolytic Strep
Penicillins
Mechanism
o interfer with bacterial cell wall
synthesis

 Subclassification and tested examples

o natural
penicillin G
o penicillinase-resistant
methicillin (Staphcillin)
o aminopenicillins
ampicillin (Omnipen, Polycillin)
Cephalosporins
Overview
o bactericidal
Mechanism
o disrupts the synthesis of
the peptidoglycan layer of
bacterial cell walls

 does so through competitive

inhibition on PCB (penicllin
binding proteins)
peptidoglycan layer is important
for cell wall structural integrity.
o same mechanicsm of action as betalactam antibiotics (such
as penicillins)
Subclassification and tested examples
o first generation
cefazolin (Ancef, Kefzol)
o second generation
cefaclor (Ceclor)
o third generation
cefriazone (Rocephin)
o fourth generation

 cefepime (Maxipime)
Fluoroquinolones
Mechanism
o blocks DNA replication via inhibition
of DNA gyrase
Side effects
o inhibit early fracture healing through
toxic effects on chondrocytes
o increased rates of tendinitis, with
special predilection for the Achilles
tendon.
tenocytes in the Achilles tendon
have exhibited degenerative
changes when viewed
microscopically after
fluoroquinolone administration.
recent clinical studies have
shown an increased relative risk

of Achilles tendon rupture of 3.7.

Subclassification and tested examples
o ciprofloxacin (Cipro)
o levofloxacin (Levaquin)
Aminoglycosides
Mechanism
o bactericidal
o inhibition of bacterial protein
synthesis
work by binding to the 30s
ribosome subunit, leading to the
misreading of mRNA. This
misreading results in the
synthesis of abnormal peptides
that accumulate intracellularly
and eventually lead to cell death.
These antibiotics arebactericidal.

 Subclassification and tested examples

o gentamicin (Garamycin)
Vancomycin
Coverage
o gram-positive bacteria
Mechanism
o bactericidal
o an inhibitor of cell wall synthesis
Resistance
o increasing emergence of
vancomycin-resistant enterococci ha
s resulted in the development of
guidelines for use by the (CDC)
o indications for vancomycin
serious allergies to penicillins

or beta-lactam antimicrobials
serious infections caused by
susceptible organisms resistant
to penicillins (MRSA, MRSE)
surgical prophylaxis for major
procedures involving implantation
of prostheses in institutions with a
high rate of MRSA or MRSE
Rifampin
Most effective against intracellular
phagocytized Staphylococcus aureus in
macrophages
Linezolid
Linezolid binds to the 23S portion of the
50S subunit and acts by preventing the
formation of the initiation
complex between
the the 30S and 50S subunits of the

ribosome.
Splenectomy
Splenectomy patients or patients with
functional hyposplenism require the
following vaccines and/or antibiotics
o Pneumococcal immunization
o Haemophilus influenza type B
vaccine
o Meningococcal group C conjugate
vaccine
o Influenza immunization
o Lifelong prophylactic antibiotics (oral
phenoxymethylpenicillin or
erythromycin)