Brenner and Stevens, Pharmacology 3rd edition, page 413, copyright
2010
Principles of Antimicrobial Chemotherapy
Mechanism of Action
Antimicrobial Agents
Inhibition of bacterial cell-wall synthesis
Penicillins, cephalosporins,
imipenem/meropenem, aztreonam,
vancomycin
Inhibition of bacterial protein synthesis
Aminoglycosides, chloramphenicol,
macrolides, tetracyclines,
streptogramins, linezolid
DNA topoisomerase II (DNA gyrase) and
IV inhibitors
Fluoroquinolones
Inhibition of nucleic acid synthesis
Rifampin
Inhibition of folic acid synthesis
Sulfonamides, trimethoprim,
pyrimethamine (Txs. toxoplasmosis)
Disruption of cell membrane function
Azole and polyene antifungal agents
Principles of Antimicrobial Chemotherapy
Antimicrobial Agents
Primary Mechanisms of Resistance
Penicillins and
Cephalosporins
Production of beta-lactamases, which
cleave the beta-lactam ring structure;
change in penicillin-binding proteins;
change in porins
Aminoglycosides
(gentamicin, streptomycin,
amikacin, etc.)
Formation of enzymes that inactivate drugs
via conjugation reactions that transfer
acetyl, phosphoryl, or adenylyl groups
Macrolides (erythromycin,
azithromycin,
clarithromycin, etc.) and
clindamycin
Formation of methyltransferases that alter
drug binding sites on the 50S ribosomal
unit
Primary Mechanisms of Resistance
Antimicrobial Agents
Mechanisms of Resistance
Tetracyclines
Increased activity of transport systems that
pump drugs out of the cell
Sulfonamides
Change in sensitivity to inhibition of target
enzyme; increased formation of PABA; use
of exogenous folic acid
Fluoroquinolones
Change in sensitivity to inhibition of target
enzymes; increased activity of transport
systems that promote drug efflux
Chloramphenicol
Formation of inactivating acetyltransferases
A 37-week gestation infant male presents with respiratory distress.
Six hours after a normal vaginal delivery the infant had slightly
increased body temperature, and displayed jaundice and lethargy.
In order to provide effective coverage for suspected bacterial
meningitis, what would be the most appropriate empiric therapy?
A. Nafcillin + cephalexin
B. Ampicillin + cefotaxime
C. Penicillin G + gentamicin
D. Ceftriaxone
E. Vancomycin
Causative organisms = Strep pneumo, N. meningitidis, H. influenza
Typical empiric meningitis therapy =3rd-gen cephs
Causative organisms in neonates =Group B Strep, E. coli, Listeria
Correct Answer: B
