Principles of antibiotic
and basic classification
16th /feb/2015
introduction
• Antibiotics are substances produced by
various microorganisms, or synthetic agents,
that suppress growth of other
microorganisms.
• Among the most prescribed drugs.
• Proper use can be life saving
• Indiscriminate use causes more:
– Cost of h/care,
– Side effects
– Drug interactions
– Foster emergence of drug resistance
Principle of antibiotic
• Selectivity
– Selectivty8 toxicity9
• Therapeutic index
– Toxic dose/ Effective dose
• Categories of antibiotics
– Bactericidal
• Usually antibiotic of choice
– Bacteriostatic
• Duration of treatment sufficient for host defenses
cont
• Antibiotic susceptibility testing (in vitro)
– Minimum inhibitory concentration (MIC)
• Lowest concentration that results in inhibition of visible
growth
– Minimum bactericidal concentration (MBC)
• Lowest concentration that kills 99.9% of the original
inoculum
cont
• Combination therapy
– Prevent emergence of resistant strains
– Temporary treatment until diagnosis is made
– Antibiotic synergism
• Penicillins and aminoglycosides
• CAUTION: Antibiotic antagonism
– Penicillins and bacteriostatic antibiotics
• Antibiotics vs chemotherapeutic agents vs
antimicrobials
Classification of antibiotic by
mechanism of action
• 1) Drugs that inhibit bacterial wall synthesis or
activate enzymes that disrupt the cell wall.
• 2) Drugs that increase cell membrane
permeability (causing leakage of intracellular
material)
• 3) Drugs that cause lethal inhibition of bacterial
protein synthesis.
• 4) Drugs that cause nonlethal inhibition of
protein synthesis (bacteriostatics).
• 5) Drugs that inhibit bacterial synthesis of nucleic
acids
CONT
• 6) Antimetabolites (disruption of specific
biochemichal reactions-->decrease in the
synthesis of essential cell constituents).
• 7) Inhibitors of viral enzymes.
• Acquired resistance to Antimicrobial drugs.
• Mechanisms:
• 1) Microbes may elaborate drug -metabolizing
enzymes (ie penicillinase).
CONT
• 2) Microbes may cease active uptake of
certain drugs
• 3) Microbial drug receptors may undergo
change resulting in decreased antibiotic
binding and action.
• 4) Microbes may synthesize compounds that
antagonize drug actions.
CONT
• How is resistance acquired?
• A) Spontaneous mutation
• B) Conjugation
• Use of antibiotics PROMOTES the emergence
of drug-resistant microbes.
• Suprainfection (or supeinfection) : a new
infection that appears through the course of
treatment for a primary infection.
CONT
• Delaying the emergence of resistance:
• 1) Use antimicrobial agents only when
needed.
• 2) Use narrow-spectrum antibiotics whenever
possible.
• 3) Newer antibiotics should be reserved for
situations in which older drus are dangerous
or no longer effective.
MODE OF ACTION
PROTEINS SYNTHESIS
30S
1 3
2 GTP
1 2 3 GTP
Initiation Factors
mRNA
3
1
2 GTP
30S
Initiation
Complex
f-met-tRNA
Spectinomycin
Aminoglycosides
1
2
GDP + Pi
50S
70S
Initiation
Complex
AP

Presentation1

  • 1.
    Principles of antibiotic andbasic classification 16th /feb/2015
  • 2.
    introduction • Antibiotics aresubstances produced by various microorganisms, or synthetic agents, that suppress growth of other microorganisms. • Among the most prescribed drugs. • Proper use can be life saving • Indiscriminate use causes more: – Cost of h/care, – Side effects – Drug interactions – Foster emergence of drug resistance
  • 3.
    Principle of antibiotic •Selectivity – Selectivty8 toxicity9 • Therapeutic index – Toxic dose/ Effective dose • Categories of antibiotics – Bactericidal • Usually antibiotic of choice – Bacteriostatic • Duration of treatment sufficient for host defenses
  • 4.
    cont • Antibiotic susceptibilitytesting (in vitro) – Minimum inhibitory concentration (MIC) • Lowest concentration that results in inhibition of visible growth – Minimum bactericidal concentration (MBC) • Lowest concentration that kills 99.9% of the original inoculum
  • 5.
    cont • Combination therapy –Prevent emergence of resistant strains – Temporary treatment until diagnosis is made – Antibiotic synergism • Penicillins and aminoglycosides • CAUTION: Antibiotic antagonism – Penicillins and bacteriostatic antibiotics • Antibiotics vs chemotherapeutic agents vs antimicrobials
  • 6.
    Classification of antibioticby mechanism of action • 1) Drugs that inhibit bacterial wall synthesis or activate enzymes that disrupt the cell wall. • 2) Drugs that increase cell membrane permeability (causing leakage of intracellular material) • 3) Drugs that cause lethal inhibition of bacterial protein synthesis. • 4) Drugs that cause nonlethal inhibition of protein synthesis (bacteriostatics). • 5) Drugs that inhibit bacterial synthesis of nucleic acids
  • 7.
    CONT • 6) Antimetabolites(disruption of specific biochemichal reactions-->decrease in the synthesis of essential cell constituents). • 7) Inhibitors of viral enzymes. • Acquired resistance to Antimicrobial drugs. • Mechanisms: • 1) Microbes may elaborate drug -metabolizing enzymes (ie penicillinase).
  • 8.
    CONT • 2) Microbesmay cease active uptake of certain drugs • 3) Microbial drug receptors may undergo change resulting in decreased antibiotic binding and action. • 4) Microbes may synthesize compounds that antagonize drug actions.
  • 9.
    CONT • How isresistance acquired? • A) Spontaneous mutation • B) Conjugation • Use of antibiotics PROMOTES the emergence of drug-resistant microbes. • Suprainfection (or supeinfection) : a new infection that appears through the course of treatment for a primary infection.
  • 10.
    CONT • Delaying theemergence of resistance: • 1) Use antimicrobial agents only when needed. • 2) Use narrow-spectrum antibiotics whenever possible. • 3) Newer antibiotics should be reserved for situations in which older drus are dangerous or no longer effective.
  • 11.
  • 12.
    PROTEINS SYNTHESIS 30S 1 3 2GTP 1 2 3 GTP Initiation Factors mRNA 3 1 2 GTP 30S Initiation Complex f-met-tRNA Spectinomycin Aminoglycosides 1 2 GDP + Pi 50S 70S Initiation Complex AP