Class

Penicillins

Cephalosporins
BetaLactams
Carbapenems
Monobactams
Beta-lactamase
inhibitors
Other cell wall synthesis inhibitors

Class

Drug
Penicillin G
Ampicillin
Cephalexin
Cefuroxime
Ceftriaxone
Cefepime
Imipenem (plus
cilastatin)
Aztreonam

Gentamicin

Macrolides

Erythromycin

Lincosamides

Clindamycin

Tetracyclines

Doxycycline

Vancomycin

Chloramphenicol
Linezolid

Class

Drug

Sulfonamides

Sulfamethoxazol
e

Diaminopyrimidine
s

Trimethoprim

Inhibits transglycosylase from elongating PG chain

Antibiotics
MOA

- Ultimate effect of MOA 1

+ 2: bactericidal
- Ultimate effect of MAO 1
only: bacteriostatic
- Time-dependent

- Natural resistance in bacteria that: lack PG, have impermeable

cell walls, are beta-lactamase producing, or have PBPs with low
affinity
- Acquired resistance mediated by a plasmid
- Cross-resistance
- Mechanisms: production of beta-lactamase enzymes,
development of PBPs with affinity, permeability, active
efflux pump

Ultimate effect: bactericidal

Inhibitors of Bacterial Protein Synthesis

Features

1) Penetration through cell envelope by diffusion

through aqueous channels or by active transport
2) Irreversible inhibition of 30S ribosomal subunit
through blockade of initiation complex, misreading
of mRNA template, & blockade of translocation

Quinupristin/Dalfopristi
n
Others

1) Bind PBPs on cytoplasmic membrane to inhibit

transpeptidases from catalyzing cross-linking
2) Activate autolytic enzymes to degrade
peptidoglycan

Resistance

Clavulanate

Drug

Aminoglycosides

Inhibitors of Bacterial Cell Wall Synthesis

MOA
Features

1) Reversible inhibition of 50S ribosomal subunit

2) Blockade of translocation (main)
3) Blockage of transpeptidation
1) Penetration through cell envelope by diffusion
through aqueous channels or by active transport
2) Reversible inhibition of 30S ribosomal subunit
preventing access of aminoacyl tRNA to acceptor site
1) Quinupristin binds 50S ribosomal subunit to inhibit
translocation
2) Dalfopristin binds 50S ribosomal subunit to induce
conformational change in 50S ribosome
Reversible inhibition of 50S ribosomal subunit
preventing transpeptidation reaction
Binds 50S ribosomal subunit to inhibit formation of
initiation complex

- Ultimate effect: bactericidal

- Concentration-dependent
- Postantibiotic effect

Resistance
- Natural resistance in bacteria that: have impermeable cell walls, produce
inactivating enzymes, are anaerobic, or lack receptor on ribosomal subunit
- Acquired resistance mediated by a plasmid
- Cross-resistance
- Mechanisms: plasmid-mediated production of transferases, mutation
induced change of receptor on 30S ribosome, permeability of cell wall

Ultimate effect: bacteriostatic

Ultimate effect: bacteriostatic

- Drugs used in combination
mostly with MethicillinVancomycin-Staph infection
- Ultimate effect: bactericidal
Ultimate effect: bacteriostatic
Ultimate effect: bacteriostatic

Inhibition of Bacterial Nucleic Acid Synthesis or Function

MOA
Features
- Folate antagonists
- Sulfonamides block dihydropteroate synthase
- Trimethoprim blocks dihydrofolate synthase

Fluoroquinolones

Ciprofloxacin

1) Penetration through cell envelope by diffusion through aqueous channels

2) Inhibition of DNA function by blocking topoisomerase II (DNA gyrase blocks
relaxation of supercoiled DNA) and topoisomerase IV (blocks separation)

Nitroimidazoles

Metronidazole

- Prodrug activated by anaerobic pathogens containing e- transport components

that donate e- to metronidazole
- Reduction of nitro group of metronidazole forms radical which damages DNA

- Ultimate effect alone:

bacteriostatic
- Ultimate effect together:
bactericidal
- Ultimate effect:
bactericidal
- Concentrationdependent
- Postantibiotic effect
Ultimate effect:
bactericidal

Resistance
- Cross-resistance
- Acquired resistance mediated by plasmids
- Mechanisms: PABA, sensitivity of dihydropteroate
synthase, cell wall permeability
Plasmid coding for altered dihydrofolate reductase
- Plasmid mediated
- Cross-resistance
- Mechanisms: change in DNA gyrapse, permeability,
efflux pump activity