Emaneini M. PhD.
The Spectrum of Antimicrobial Activity
Narrow spectrum (limited spectrum)
 Antimicrobials effective against a (limited spectrum)
of microbial types
 A drug effective on G+ or G- bacteria
Broad spectrum (extended spectrum)
 Antimicrobials effective against a (extended spectrum) wide
variety of microbial types
 A drug effective against both G+& G- bacteria
Emaneini M. PhD.
The Action of Antimicrobial Drugs
Bactericidal
Kill microbes directly
Bacteriostatic
Prevent microbes from growing
Emaneini M. PhD.
Mechanisms of Antibiotics Action
Emaneini M. PhD.
1- Inhibition of Cell Wall Synthesis
2- Injuring the Plasma Membrane
3- Inhibition of Protein Synthesis
4- Inhibition of Nucleic Acid Synthesis
5- Inhibiting the Synthesis of Essential Metabolites
Mechanisms of Antibiotics Action
Emaneini M. PhD.
Inhibition of Cell Wall Synthesis
Transpeptidases, Carboxypeptidases, Transglycosylases
Penicillin-binding proteins (PBPs(
β-Lactam antibiotics: generally are bactericidal agents
Emaneini M. PhD.
1- Beta-Lactam Antibiotics
 Penicillins
 Cephalosporins
2- Glycopeptides
 Vancomycin
3- Lipopeptides
 Daptomycin
4- Polypeptides
 Bacitracin
Inhibition of Cell Wall Synthesis
Emaneini M. PhD.
Inhibition of Cell Wall Synthesis
Isoniazid, Ethionamide, Ethambutol, & Cycloserine
Used for the treatment of mycobacterial infections
Isoniazid
Isonicotinic acid hydrazide [INH])
Bactericidal; Blocks mycolic acid synthesis
Ethionamide
Derivative of INH
Blocks mycolic acid synthesis
Ethambutol
Interferes with the synthesis of arabinogalactan in the cell wall
Cycloserine
Inhibits D-alanine-Dalanine synthetase & Alanine racemase
Emaneini M. PhD.
Injuring the Plasma Membrane
1- Lipopeptides
Daptomycin
2- Polypeptides
Polymyxins
Emaneini M. PhD.
Inhibition of Protein Synthesis
Emaneini M. PhD.
Chloramphenicol
 Broad spectrum
 Bacteriostatic
 Blocking peptide elongation
 Binding reversibly to the peptidyl transferase (50S)
 Only for the treatment of typhoid fever
 Can produce aplastic anemia (1 per 24,000 treated patients)
 Resistance: plasmid-encoded chloramphenicol acetyltransferase
Emaneini M. PhD.
Inhibition of Nucleic Acid Synthesis
1- Quinolones
2- Rifampin
3- Metronidazole
Emaneini M. PhD.
 Synthetic
 Inhibit bacterial DNA gyrases (II) or topoisomerases (IV)
Nalidixic acid
Fluoroquinolones:
Ciprofloxacin Levofloxacin Gatifloxacin
Resistance: mutations in chromosomal genes of DNA gyrases (II)
or topoisomerases (IV)
Quinolones
Emaneini M. PhD.
Antimetabolites
Sulfonamides
 Preventing the synthesis of the folic acid
 Compete with p-aminobenzoic acid
 Mammalian organisms do not synthesize folic acid
Treatment of Nocardia, Chlamydia, & some protozoa infections
Sulfacetamide Sulfadiazine Sulfisoxazole
R Group

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Antibiotics lecture

  • 1. Emaneini M. PhD. The Spectrum of Antimicrobial Activity Narrow spectrum (limited spectrum)  Antimicrobials effective against a (limited spectrum) of microbial types  A drug effective on G+ or G- bacteria Broad spectrum (extended spectrum)  Antimicrobials effective against a (extended spectrum) wide variety of microbial types  A drug effective against both G+& G- bacteria
  • 2. Emaneini M. PhD. The Action of Antimicrobial Drugs Bactericidal Kill microbes directly Bacteriostatic Prevent microbes from growing
  • 3. Emaneini M. PhD. Mechanisms of Antibiotics Action
  • 4. Emaneini M. PhD. 1- Inhibition of Cell Wall Synthesis 2- Injuring the Plasma Membrane 3- Inhibition of Protein Synthesis 4- Inhibition of Nucleic Acid Synthesis 5- Inhibiting the Synthesis of Essential Metabolites Mechanisms of Antibiotics Action
  • 5. Emaneini M. PhD. Inhibition of Cell Wall Synthesis Transpeptidases, Carboxypeptidases, Transglycosylases Penicillin-binding proteins (PBPs( β-Lactam antibiotics: generally are bactericidal agents
  • 6. Emaneini M. PhD. 1- Beta-Lactam Antibiotics  Penicillins  Cephalosporins 2- Glycopeptides  Vancomycin 3- Lipopeptides  Daptomycin 4- Polypeptides  Bacitracin Inhibition of Cell Wall Synthesis
  • 7. Emaneini M. PhD. Inhibition of Cell Wall Synthesis Isoniazid, Ethionamide, Ethambutol, & Cycloserine Used for the treatment of mycobacterial infections Isoniazid Isonicotinic acid hydrazide [INH]) Bactericidal; Blocks mycolic acid synthesis Ethionamide Derivative of INH Blocks mycolic acid synthesis Ethambutol Interferes with the synthesis of arabinogalactan in the cell wall Cycloserine Inhibits D-alanine-Dalanine synthetase & Alanine racemase
  • 8. Emaneini M. PhD. Injuring the Plasma Membrane 1- Lipopeptides Daptomycin 2- Polypeptides Polymyxins
  • 9. Emaneini M. PhD. Inhibition of Protein Synthesis
  • 10. Emaneini M. PhD. Chloramphenicol  Broad spectrum  Bacteriostatic  Blocking peptide elongation  Binding reversibly to the peptidyl transferase (50S)  Only for the treatment of typhoid fever  Can produce aplastic anemia (1 per 24,000 treated patients)  Resistance: plasmid-encoded chloramphenicol acetyltransferase
  • 11. Emaneini M. PhD. Inhibition of Nucleic Acid Synthesis 1- Quinolones 2- Rifampin 3- Metronidazole
  • 12. Emaneini M. PhD.  Synthetic  Inhibit bacterial DNA gyrases (II) or topoisomerases (IV) Nalidixic acid Fluoroquinolones: Ciprofloxacin Levofloxacin Gatifloxacin Resistance: mutations in chromosomal genes of DNA gyrases (II) or topoisomerases (IV) Quinolones
  • 13. Emaneini M. PhD. Antimetabolites Sulfonamides  Preventing the synthesis of the folic acid  Compete with p-aminobenzoic acid  Mammalian organisms do not synthesize folic acid Treatment of Nocardia, Chlamydia, & some protozoa infections Sulfacetamide Sulfadiazine Sulfisoxazole R Group