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Author: Derek Moore Topic updated on 10/23/13 2:20am
Antibiotic Classification & Mechanism
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 (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
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Penicillin V C. perfringens(Bacilli)**
Aminopenicillins Ampicillin
Amoxicillin
Above +
Gram-negative:
E. faecalis**
E. Coli**
Above
Penicillinase-resistant-
penicillins
Methicillin
Nafcillin
Oxacillin
Cloxacillin
Dicloxacillin
Above +
PCNase-
producingStaph.
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 Gram-negatives:
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
Ceftazidime
Cefepime (4th generation)
Above +
Gram-negative
Pseudomonas
Allergic Reaction
ETOH Disulfiram
reaction
Other Cell Wall Inhibitors
Vancomycin
(bactericidal: disrupts
peptioglycan cross-linkage)
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 Gram-negative
infections

Bacitracin Bacitracin Topical Gram-positive
infections

Protein Synthesis Inhibition
Anti-30S ribosomal subunit
Aminoglycosides
(bactericidal: irreversible
binding to 30S)
Gentamicin
Neomycin
Amikacin
Tobramycin
Streptomycin
Aerobic Gram-
negatives
Enterobacteriaceae
Pseudomonas
Nephrotoxicity
Ototoxicity
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
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12 years of age
Anti-50S ribosomal subunit
Macrolides
(bacteriostatic: reversibly
binds 50S)
Erythromycin
Azithromycin
Clarithromycin
Streptococcus
H. influenzae
Mycoplamsa
pneumonia
Coumadin
Interaction
(cytochrome P450)
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
Coagulase-negative
Staph & Strep
Excellent Bone
Penetration
Pseudomembranous
colitis
Hypersensitivity
Reaction
Linezolid
(variable)
Linezolid Resistant Gram-
positives

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 +
Phototoxicity
Achilles tendon
rupture
Impaired fracture
healing
2nd generation Ciprofloxacin
Norfloxacin
Enoxacin
Ofloxacin
Levofloxacin
As Above
+Pseudomonas
as above
3rd generation Gatifloxacin As above + Gram-
positives
as above
4th generation Moxifloxacin
Gemifloxacin
As above + Gram-
positives + anaerobes
as above
Other DNA Inhibitors
Metronidazole
(bacteridical: metabolic
biproducts disrupt DNA)
Metronidazole (Flagyl)
Anaerobi cs
Seizures
Crebelar dysfunction
ETOH disulfram
reaction
RNA Synthesis Inhibitors
Rifampin
(bactericidal: inhibits RNA
transcription by inhibiting RNA
polymerase)
Rifampin Staphylococcus
Mycobacterium (TB)
Body fluid
discoloration
Hepatoxicity (with
INH)
Mycolic Acids Synthesis Inhibitors
Isoniazid Isoniazidz TB
Latent TB

Folic acid Synthesis Inhibitors
Trimethoprim/Sulfonamides
(bacteriostatic: inhibition with
PABA)
Trimethoprim/Sulfamethoxazole
(SMX)
Sulfisoxazole
Sulfadiazine
UTI organisms
Proteus
Enterobacter
Thrombocytopenia
Avoid in third
trimester of
pregnancy
Pyrimethamine Pyrimethamine Malaria
T. gondii


Bacteria Overview

Gram Postive Cocci
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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 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
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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
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
confers resistance to tetracyclines, quinolones, trimethoprim and lactam antibiotics
Creation of biofilm barrier
provides an environment where offending bacteria can multiply safe from the hoste immune
system
Salmonella
Staph epidermidis
Active efflux pumps
confers resistance to erythromycin and tetracycline
e.g. msrA gene in Staph
Altered peptidoglycan subunit (altered D-alanyl-D-alanine of NAM/NAG-peptide)
confers resistance to vancomycin
e.g. vancomycin resistant enterococcus (VRE)
Ribosome alteration
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
interfer with bacterial cell wall synthesis
Subclassification and tested examples
natural
penicillin G
penicillinase-resistant
methicillin (Staphcillin)
aminopenicillins
ampicillin (Omnipen, Polycillin)

Cephalosporins
Overview
bactericidal
Mechanism
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
first generation
cefazolin (Ancef, Kefzol)
second generation
cefaclor (Ceclor)
third generation
cefriazone (Rocephin)
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cefriazone (Rocephin)
fourth generation
cefepime (Maxipime)
Fluoroquinolones
Mechanism
blocks DNA replication via inhibition of DNA gyrase
Side effects
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
ciprofloxacin (Cipro)
levofloxacin (Levaquin)
Aminoglycosides
Mechanism
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
gentamicin (Garamycin)
Vancomycin
Coverage
gram-positive bacteria
Mechanism
bactericidal
an inhibitor of cell wall synthesis
Resistance
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
Pneumococcal immunization
Haemophilus influenza type B vaccine
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Haemophilus influenza type B vaccine
Meningococcal group C conjugate vaccine
Influenza immunization
Lifelong prophylactic antibiotics (oral phenoxymethylpenicillin or erythromycin)