A ntimicrobial D rugs

Chapter 20
 Antimicrobial Drugs

‡ A ntimicrobial drugs: Interfere with the growth

of microbes within a host

‡ A ntibiotic: A substance produced by a microbe

that, in small amounts, inhibits another microbe
 Antimicrobial Drugs

‡ 1928: Fleming
discovered
penicillin,
produced by
Penicillium
‡ 1940: Howard
Florey and Ernst
Chain performed
first clinical trials
of penicillin
Figure 1.5
F eatures of A ntimicrobial D rugs
1. Selective toxicity
2. A ntimicrobial action:
Bacteriostatic vs. Bactericidal
3. Spectrum of activity:
B road-spectrum vs. Nar row-spectrum
4. A dverse effects: A llergies, Toxicity,
Suppression of the normal flora
 Mechanism of Action of
Antibacterial drugs
T argets :
Inhibition of cell wall synthesis
Inhibition of protein synthesis
Inhibition of nucleic acid synthesis
Inhibition of metabolic pathways
Inhibition of cell membrane integrity
The Action of Antimicrobial Drugs

Figure 20.2
 1. Inhibitors of Cell Wall Synthesis
‡ Penicillin
1. Natural penicillins
Penicillin G and Penicillin V

2. Semisynthetic penicillins
E xtended-spectrum penicillins
Resistant to Penicillinase/ ȕ-L actamase
Figure 20.6
2. T he Inhibition of Protein Synthesis by A ntibiotics

Figure 20.4
 Antibiotic Resistance
‡ A variety of mutations can lead to antibiotic
resistance

‡ Resistance genes are often on plasmids or

transposons that can be transfer red between
bacteria
Resistance to Antibiotics

Figure 20.20
Selective advantage

Figure 21.13
 Antibiotic Resistance
‡ M isuse of antibiotics selects for resistance
mutants. M isuse includes
± Using outdated or weakened antibiotics
± Using antibiotics for the common cold and other
inappropriate conditions
± Using antibiotics in animal feed
± F ailing to complete the prescribed regimen
± Using someone else's leftover prescription
E xamples of emerging resistance

1. E nterococci (vancomycin ± resistant

enterococci)
2. Staphylococcus aureus (methicillin ±
resistant Staphylococcus aureus)
3. Streptococcus pneumoniae (penicillin
resistant)
4. Mycobacterium tuberculosis
 Effects of Combinations of Drugs
‡ Synergism occurs when the effect of two
drugs together is greater than the effect of
either alone
‡ A ntagonism occurs when the effect of two
drugs together is less than the effect of either
alone
‡ Antibiotic Safety
Therapeutic index: risk vs. benefit
 Anti-viral drugs
‡ Selective toxicity difficult to achieve
‡ A ntibiotics (antibacterials) have no effect
on viruses
‡ Relatively few
‡ None can eliminate latent viruses
 Targets
‡ Uncoating
± A mantadine & rimantidine ± influenza
‡ Nucleic acid synthesis
± Nucleoside analogs ± H erpesvirus & H I V
± polymerase inhibitors
‡ Assembly and release
± Protease inhibitors ± H I V
± Neuraminidase inhibitors - influenza
Nucleoside and Nucleotide Analogs

Figure 20.16b ,c