Antibiotic Classification & Mechanism

Author: Derek Moore MD

Topic updated on 07/05/12 8:13pm
Overview of By Mechanism

Antibiotic Grouping By Mechanism

Cell Wall Synthesis

Penicillins
Cephalosporins
Vancomycin
Beta-lactamase Inhibitors
Carbapenems
Aztreonam
Polymycin
Bacitracin

Protein Synthesis Inhibitors

Inhibit 30s Subunit
Aminoglycosides (gentamycin)

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

Penicillin

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

Aminopenicillins

Ampicillin
Amoxicillin

Penicillinaseresistant-penicillins

Methicillin
Nafcillin
Oxacillin

Indications
(**Drug of Choice)

Toxicity

Hypersensitivity
Strep. pyogenes reaction
Hemolytic
(Grp.A)**
Step. agalactiae anemia
(Grp.B)**
C.
perfringens(Bacilli
)**
Above
Above +
Gram-negative:
E. faecalis**
E. Coli**
Above +
Above +
PCNase-producing Interstitial
Staph. aureus
nephritis

Cloxacillin
Dicloxacillin
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
Above +
Cefotaxime
Gram-negative
Ceftazidime
Pseudomonas
Cefepime (4th generation)

Allergic
Reaction
ETOH
Disulfiram
reaction

Other Cell Wall Inhibitors

Vancomycin
(bactericidal: disrupts
peptioglycan crosslinkage)

Vancomycin

Beta-lactamase
Inhibitors
(bactericidal: blocking
cross linking)

Clavulanic Acid
Sulbactam
Tazobactam

Carbapenems

Imipenem (+ cilastatin)
Meropenem
Doripenem
Ertapenem

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

S aureus**
S epidermis**
E.Coli**
Klebsiella**
Broadest activity of
any antibiotic
(except MRSA,
Mycoplasma)

Red man
syndrome
Nephrotoxicity
Ototoxicity

Hypersensitivity
Reaction
Hemolytic
anemia

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
Gentamicin
(bactericidal: irreversible Neomycin
binding to 30S)
Amikacin
Tobramycin
Streptomycin

Aerobic GramNephrotoxicity
negatives
Ototoxicity
Enterobacteriaceae
Pseudomonas

Tetracyclines
(bacteriostatic: blocks
tRNA)

Hepatotoxicity
Tooth
Rickettsia
discoloration
Mycoplasma
Spirochetes (Lyme's Impaired growth
Avoid in
disease)
children < 12
years of age

Tetracycline
Doxycycline
Minocycline
Demeclocycline

Anti-50S ribosomal subunit

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

Streptococcus
H. influenzae
Mycoplamsa
pneumonia

Chloramphenicol
(bacteriostatic)

Chloramphenicol

H influenzae
Bacterial
Meningitis
Brain absces

Aplastic Anemia
Gray Baby
Syndrome

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

Clindamycin
Bacteroides
fragilis
S aureus
Coagulasenegative Staph &
Strep
Excellent Bone

Pseudomembran
ous colitis
Hypersensitivity
Reaction

Coumadin
Interaction
(cytochrome
P450)

Penetration
Linezolid
(variable)

Linezolid

Resistant Grampositives

Streptogramins

Quinupristin
Dalfopristin

VRE
GAS and S. aureus
skin infections

DNA Synthesis Inhibitors

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

Nalidixic acid

Steptococcus
Mycoplasma
Aerobic Gram +

2nd generation

Ciprofloxacin
Norfloxacin
Enoxacin
Ofloxacin
Levofloxacin

As Above +
Pseudomonas

3rd generation

Gatifloxacin

As above + Gram- as above

positives

4th generation

Moxifloxacin
Gemifloxacin

As above + Gram- as above

positives +
anaerobes

Phototoxicity
Achilles tendon
rupture
Impaired
fracture
healing
as above

Other DNA Inhibitors

Metronidazole
Metronidazole (Flagyl)
(bacteridical: metabolic
biproducts disrupt DNA)

Anaerobics

Seizures
Crebelar
dysfunction
ETOH disulfram
reaction

RNA Synthesis Inhibitors

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

Rifampin

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

Mycolic Acids Synthesis Inhibitors

Isoniazid

Isoniazidz

TB
Latent TB

Folic acid Synthesis Inhibitors

Trimethoprim/Sulfona
mides
(bacteriostatic: inhibition
with PABA)

Trimethoprim/Sulfamethox UTI organisms

azole (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

Neisseria

Neisseria meningitidis

Thrombocytope
nia
Avoid in third
trimester of
pregnancy

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

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 beta-lactam 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 are bactericidal.

Subclassification and tested examples

o gentamicin (Garamycin)

Vancomycin

Covergage
o gram-positive bacteria

Mechanism
o bactericidal
o an inhibitor of cell wall synthesis

Resistence
o increasing emergence of vancomycin-resistant enterococci has resulted in the
development of guidelines for use by the (CDC)

indications for vancomycin include but are not limited to

serious allergies to penicillins or beta-lactam antimicrobials

serious infections caused by susceptible organisms resistant

to penicillins (MRSA, MRSE)

mecA is a bacterial gene which encodes for a penicillin-binding

protein that alters the efficacy of penicillin-like antibiotics in
certain bacteria like MRSA

surgical prophylaxis for major procedures involving implantation

of prostheses in institutions with a high rate of MRSA or MRSE

Other antibiotics/issues
Rifampin
o most effective against intracellular phagocytized Staphylococcus
aureus in macrophages
Linezolid
o 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 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)