Antibiotic Grouping By Mechanism

Cell Wall Synthesis

Penicillins
Cephalosporins
Vancomycin
Beta-lactamase Inhibitors
Carbapenems
Aztreonam
Polymycin
Bacitracin

Protein Synthesis Inhibitors

Inhibit 30s Subunit

Aminoglycosides (gentamicin)
Tetracyclines
Inhibit 50s Subunit
Macrolides
Chloramphenicol
Clindamycin
Linezolid
Streptogramins

DNA Synthesis Inhibitors

Fluoroquinolones
Metronidazole

RNA synthesis Inhibitors

Rifampin

Mycolic Acid synthesis inhibitors

Isoniazid

Folic Acid synthesis inhibitors

Sulfonamides
Trimethoprim

Antibiotic Classification & Indications

Inhibits Cell Wall Synthesis

Penicillins
(bactericidal: blocks cross linking via competitive inhibition of the transpeptidase enzyme)
Class/Mechanism

Drugs

Indications (**Drug
of Choice)

Toxicity

Penicillin

Penicillin G
Aqueous penicillin G
Procaine penicillin G
Benzathine penicillin G
Penicillin V

Strep. pyogenes
(Grp.A)**
Step. agalactiae
(Grp.B)**
C.
perfringens(Bacilli)
**

Hypersensitivity
reaction
Hemolytic
anemia

Aminopenicillins

Ampicillin
Amoxicillin

Above +
Gram-negative:
E. faecalis**
E. Coli**

Above

Penicillinase-resistantpenicillins

Methicillin
Nafcillin
Oxacillin
Cloxacillin
Dicloxacillin

Above +
PCNaseproducingStaph.
aureus

Above +
Interstitial
nephritis

Antipseudomonal
penicillins

Carbenicillin
Ticarcillin
Piperacillin

Above +
Pseudomonas
aeruginosa**

Above

Cephalosporins
(bactericidal: inhibits bacterial cell wall synthesis via competitive inhibition of the
transpeptidase enzyme)
1st generation

Cefazolin
Cephalexin

Staph. aureus**
Staph.
epidermidis**
Some Gramnegatives:
E. Coli
Klebsiella

Allergic reaction
Coombs-positive
anemia (3%)

2nd generation

Cefoxitin
Cefaclor
Cefuroxime

Above +
Gram-negative

Allergic Reaction
ETOH Disulfiram
reaction

3rd generation

Ceftriaxone
Cefotaxime
Cef

azidime
Cefepime (4th
generation)
Above +
Gram-negative

Allergic Reaction
ETOH Disulfiram
reaction

Pseudomonas
Other Cell Wall Inhibitors
Vancomycin
(bactericidal: disrupts
peptioglycan crosslinkage)

Vancomycin

MRSA**
PCN/Ceph
allegies**
S. aureus
S. epidermidis

Red man
syndrome
Nephrotoxicity
Ototoxicity

Beta-lactamase
Inhibitors
(bactericidal: blocking
cross linking)

Clavulanic Acid
Sulbactam
Tazobactam

S aureus**
S epidermis**
E.Coli**
Klebsiella**

Hypersensitivity
Reaction
Hemolytic
anemia

Carbapenems

Imipenem (+ cilastatin)
Meropenem
Doripenem
Ertapenem

Broadest activity of
any antibiotic
(except MRSA,
Mycoplasma)

Aztreonam

Aztreonam

Gram-negative rods
Aerobes
Hospital-acquired
infections

Polymyxins

Polymyxin B
Polymyxin E

Topical Gramnegative infections

Bacitracin

Bacitracin

Topical Grampositive infections

Protein Synthesis Inhibition

Anti-30S ribosomal subunit
Aminoglycosides
(bactericidal: irreversible
binding to 30S)

Gentamicin
Neomycin
Amikacin
Tobramycin
Streptomycin

Aerobic GramNephrotoxicity
negatives
Ototoxicity
Enterobacteriaceae
Pseudomonas

Tetracyclines
(bacteriostatic: blocks
tRNA)

Tetracycline
Doxycycline
Minocycline
Demeclocycline

Rickettsia
Mycoplasma
Spirochetes (Lyme's
disease)

Hepatotoxicity
Tooth
discoloration
Impaired growth
Avoid in children
< 12 years of age

Anti-50S ribosomal subunit

Macrolides
Erythromycin
(bacteriostatic: reversibly Azithromycin
binds 50S)
Clarithromycin

Streptococcus
H. influenzae
Mycoplamsa
pneumonia

Coumadin
Interaction
(cytochrome
P450)

Chloramphenicol
(bacteriostatic)

Chloramphenicol

H influenzae
Aplastic Anemia
Bacterial Meningitis Gray Baby
Brain absces
Syndrome

Lincosamide
(bacteriostatic: inhibits
peptidyl transferase by
interfering with amino
acyl-tRNA complex)

Clindamycin

Bacteroides fragilis
S aureus
Coagulase-negative
Staph & Strep
Excellent Bone
Penetration

Linezolid
(variable)

Linezolid

Resistant Grampositives

Streptogramins

Quinupristin
Dalfopristin

VRE
GAS and S. aureus
skin infections

Pseudomembrano
us colitis
Hypersensitivity
Reaction

DNA Synthesis Inhibitors

Fluoroquinolones
(bactericidal: inhibit DNA gyrase enzyme, inhibiting DNA synthesis)
1st generation

Nalidixic acid

Steptococcus
Mycoplasma
Aerobic Gram +

Phototoxicity
Achilles tendon
rupture
Impaired fracture
healing

2nd generation

Ciprofloxacin
Norfloxacin
Enoxacin
Ofloxacin
Levofloxacin

As Above
+Pseudomonas

as above

3rd generation

Gatifloxacin

As above + Grampositives

as above

4th generation

Moxifloxacin
Gemifloxacin

As above + Grampositives +
anaerobes

as above

Other DNA Inhibitors

Metronidazole
(bacteridical: metabolic
biproducts disrupt DNA)

Metronidazole (Flagyl)

Anaerobics

RNA Synthesis Inhibitors

Seizures
Crebelar
dysfunction
ETOH disulfram
reaction

Rifampin
Rifampin
(bactericidal: inhibits RNA
transcription by inhibiting
RNA polymerase)

Staphylococcus
Body fluid
Mycobacterium (TB discoloration
)
Hepatoxicity
(with INH)

Mycolic Acids Synthesis Inhibitors

Isoniazid

Isoniazidz

TB
Latent TB

Folic acid Synthesis Inhibitors

Trimethoprim/Sulfonami
des
(bacteriostatic: inhibition
with PABA)

Trimethoprim/Sulfamethoxa UTI organisms

zole (SMX)
Proteus
Sulfisoxazole
Enterobacter
Sulfadiazine

Pyrimethamine

Pyrimethamine

Malaria
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

Thrombocytopeni
a
Avoid in third
trimester of
pregnancy

Neisseria

Neisseria meningitidis
Neisseria gonorrhoeae
Gram Negative Bacilli

Enterics

Escherichia coli
Salmonella typhi
Salmonella enteridis
Shigella dysenteriae
Klebsiella pneumoniae
Serratia
Proteus
Campylobacter jejuni
Vibrio cholerae
Vibrio parahaemolyticus/vulnificus
Helicobacter pylori
Pseudomonas aeruginosa
Bacteroides fragilis

Respiratory bacilli

Haemophilus influenzae
Haemophilius ducreyi
Bordatella pertussis

Zoonotic bacilli

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

Mycoplasmataceae

Mycoplasma pneumoniae
Ureaplasma urealyticum

Fungus-like Bacteria

Actinomyces israelii
Nocardia

Antibiotic Resistance Mechanisms

Bacteria develop ability to hydrolyze these drugs using lactamase

confers resistance to penicillin

e.g. E. coli, Staph epidermidis, Pseudomonas aeruginosa, Klebsiella

pneumoniae

add lactamase inhibitor e.g. clavulanic acid in amoxicillin-clavulanate

(Augmentin)

Genetic mutation of mecA

o

a bacterial gene encoding a penicillin-binding protein. New PBP has

reduced affinity for antibiotics

confers resistance to methicillin, oxacillin, nafcillin

e.g. MRSA

Altered cell wall permeability

o

Creation of biofilm barrier

o

confers resistance to tetracyclines, quinolones, trimethoprim and

lactam antibiotics

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

e.g. msrA gene in Staph

Altered peptidoglycan subunit (altered D-alanyl-D-alanine of NAM/NAGpeptide)

o

confers resistance to vancomycin

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

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

penicillinase-resistant

penicillin G

methicillin (Staphcillin)

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.

same mechanicsm of action as beta-lactam antibiotics (such

as penicillins)

Subclassification and tested examples

o

first generation

second generation

cefaclor (Ceclor)

third generation

cefazolin (Ancef, Kefzol)

cefriazone (Rocephin)

fourth generation

cefepime (Maxipime)
Fluoroquinolones
Mechanism

blocks DNA replication via inhibition of DNA gyrase

Side effects
o

inhibit early fracture healing through toxic effects on chondrocytes

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)

levofloxacin (Levaquin)
Aminoglycosides
Mechanism
o

bactericidal

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

an inhibitor of cell wall synthesis

Resistance
o

increasing emergence of vancomycin-resistant enterococci has resulted in the

development of guidelines for use by the (CDC)

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

Haemophilus influenza type B vaccine

Meningococcal group C conjugate vaccine

Influenza immunization

Lifelong prophylactic antibiotics (oral phenoxymethylpenicillin or

erythromycin)