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Antibiotic Classification and General Information

Protein synthesis inhibitors

Major groups: aminoglycosides, tetracyclines, macrolides
General mechanism of action: Protein synthesis inhibiting antibiotics primarily target the
bacterial ribosome (70S) which is made up of a small, 30S subunit and a large, 50S subunit.
A ribosome is an essential, complex molecule made up of proteins and RNA and is
responsible for synthesizing proteins. Aminoglycosides, macrolides, and other protein
synthesis inhibitors target and prevent specific stages of protein synthesis at specific
locations on 70S ribosomes. Bacterial death occurs because the cell cannot make proteins
required for essential cellular processes.
Effects on humans – Humans, and other eukaryotic cells synthesize proteins using a 80S
(not 70S) ribosome which is not targeted by these inhibitors. (other side effects are possible)

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tein Synthesis Inhibitors

 
 
 
Aminoglycosides
-mycin
 
(initiation inhibitors) Streptomycin
(Streptomyces) Dihydrostreptomycin
Neomycin
Paromomycin
Amikacin
Kanamycin
30S Subunit

Tobramycin
Spectinomycin
Hygromycin B
 
-micin 
 
Gentamicin
(Micromonospora)
Netilmicin
 
  Sisomicin
Tetracycline
Tetracyclines
 
antibiotics Doxycycline
(rRNA binding)
Chlortetracycline
Tetracycline
 Metacycline

Pr
Minocycline
Oxytetracyline
   
Glycylcyclines  
 
  Tigecycline
Peptidyl 
Amphenicols
 
transferase
Chloramphenicol
Thiamphenicol
Florfenicol
 
50S Subunit  
Pleuromutilins
Tiamulin
  Valnemulin
 
MLS 
Macrolides
 
(transpeptidation Azithromycin
/tranaslocation)
Clarithromycin
Oleandomycin
Erythromycin
Roxithromycin
Spiramycin
Telithromycin
  Tylosin

  Lincosamides
 
  Clindamycin
EF- Steroid Antibacterials   Lincomycin
G
Fusidic Acid

Nucleic acid synthesis inhibitors

Major groups: Antifolates, topoisomerase inhibitors (floroquinolones)

General mechanism of action: These antibiotics target different stages and pathways of nucleic acid (DNA,
RNA…) synthesis. In summary, antifolates (includes sulfonamides) inhibit enzymes involved in folate/folic acid
(vitamin B9) synthesis. Folate is an essential ingredient for the synthesis of pyrimidine and purines, two
molecules found in nucleotides, the building blocks of DNA and other nucleic acids. Topoisomerase
inhibitors prevent DNA replication by inhibiting topoisomerase activity. Toposiomerases are enzymes that
relieve DNA supercoil stress during DNA replication. By inhibiting topoisomerase activity, DNA replication is
greatly hindered and cell division rate is diminished.

Effects on humans – Humans acquire folate from dietary sources, they do not have a synthesis pathway for
folate and are not affected by antifolates in the same way bacteria are. Topoisomerases can be found in
human cells; however the molecular makeup of human topoisomerases differs from those found in
bacteria. (other side effects are possible)

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cleic Acid

 
 
DHFR inhibitor  
Trimethoprim
Antifolates

 
 
Sulfonamides Short-acting  
(DHPS inhibitor) Sulfathiazole
 Sulfamethoxazole
  Intermediate  
Sulfadiazine

N
 
  Long-acting Sulfamerazine
   
1 st generation

Topoisomerase Inhibitors and quinolones

Flumequine
  Nalidixic acid
Oxolinic acid
Pipemidic acid
 
Fluoroquinolones
Ciprofloxacin
  2nd generation  
Ofloxacin
Norfloxacin
Pefloxacin

Levofloxacin
  3rd generation   Sparfloxacin

Moxifloxacin
  4th generation   Gatifloxacin
Difloxacin
Enrofloxacin
Marbofloxacin

  Novobiocin
  Related(DG)
 
Anaerobic DNA  
inhibitors Nitro-imidazole derivatives  
Metronidazole
 
Nitrofuran derivatives  
Nitrofurantoin
  Furazolidone

RNA synthesis  
Rifamycins/RNA polymerase  
Rifampicin

Cell wall synthesis inhibitors

Major groups: Beta-lactams (cephalosporins, penicillins)

General mechanism of action: As the name implies, this group of antibiotics inhibits
certain stages in bacterial cell wall synthesis. A major structural component in the bacterial
cell wall (more so in Gram-positive bacteria) is an essential polymer called peptidoglycan.
Beta-lactam antibiotics bind to PBPs or penicillin binding proteins which are involved in the
final stages of peptidoglycan synthesis. By inhibiting PBP function, peptidoglycan cannot
be properly synthesized and the cell lyses.

Effects on humans – Human cells do not use nor synthesize peptidoglycan and are
therefore not susceptible to beta-lactam antibiotics. (other side effects are possible)

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i
   Fosfomycin

An
Intracellular   Cycloserine
Bacitracin

  Vancomycin
Glycopeptide   Teicoplanin

 
 
Penicillins  
(penams) Extended sp.  
Amoxicillin
Ampicillin
Carbenicillin
Ticarcillin
Temocillin
Azlocillin
Piperacillin
Mezlocillin
Mecillinam
 
Narrow sp.  
β-lactamase  
sensitive Benzylpenicillin
 
β-lactamase  
resistant Cloxacillin
Dicloxacillin
Flucloxacillin
Oxacillin
Methicillin
 
Nafcillin
Penems  
Faropenem
 
Carbapenems  
Ertapenem
Doripenem
Imipenem
Meropenem
 
B-lactams/ (inhibit PBP cross-links)

Cephalosporins/  
Cephamycins 1st  
(cephems) Cefazolin
Cefadroxil
Cefalexin
  Cefradine
2nd  
Cefaclor
Cefamandole
Cefminox
Cefotiam
Cefprozil
Cefuroxime
Cefoxitin
Cefotetan
  Cefmetazole
3rd  
Cefixime
 Ceftriaxone
Ceftazidime
Cefoperazone
Cefdinir
Cefditoren
Cefotaxime
Cefpodoxime
Cefsulodin
Cefteram
  Ceftibuten
4th   Ceftizoxime
Cefepime
Cefozopran
Cefpirome
 
Veterinary  
  Ceftiofur
Monobactams  
Aztreonam
 
β-lactamase  
inhibitors Sulbactam
Tazobactam
Clavulanic acid
Cefdinir
 
Combinations  
Amoxicillin/clavulanic
acid
Imipenem/cilastatin
Ampicillin/sulbactam
 
Other  
Colistin
Polymyxin B
Daptomycin
Gramicidin
Isonaizid

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