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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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Aminoglycosides
-mycin
 
(initiation inhibitors) Streptomycin
(Streptomyces) Dihydrostreptomycin
Neomycin
Paromomycin
Amikacin
Kanamycin
otein Synthesis Inhibitors

30S Subunit

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

Tigecycline
 
Peptidyl
Amphenicols
 
transferase
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Thiamphenicol
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50S
Florfenicol
  Pleuromutilins  
Tiamulin
  Valnemulin
MLS
(transpeptidation   Macrolides  
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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DHFR inhibitor  
Trimethoprim
Antifolates

 
 
Sulfonamides Short-acting  
(DHPS inhibitor) Sulfathiazole
 
cleic Acid Inhibitors

 
Intermediate Sulfamethoxazole
Sulfadiazine
 
  Long-acting  
  Sulfamerazine
 
isomerase Inhibitors and quinolones

1 st generation Flumequine
Nalidixic acid
Oxolinic acid
Pipemidic acid
 
 
Fluoroquinolones
 
2nd generation Ciprofloxacin
Ofloxacin
Norfloxacin
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Pefloxacin
 
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3rd generation Levofloxacin
Sparfloxacin
 Nu
Topo
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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Intracellular  
Fosfomycin
Cycloserine
tibacterials:cell envelope antibiotics

Bacitracin
 
Glycopeptide  
Vancomycin
Teicoplanin
 
 
Penicillins  
(penams) Extended sp.  
Amoxicillin
Ampicillin
Carbenicillin
Ticarcillin
ctams/ (inhibit PBP cross-links)

Temocillin
Azlocillin
Piperacillin
Mezlocillin
Mecillinam
 
Narrow sp.  
β-lactamase  
sensitive Benzylpenicillin
 
 
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β-lactamase
resistant Cloxacillin
Dicloxacillin
Settings Accept All Cookies Flucloxacillin
Oxacillin
 Ant

B-la
Methicillin
Penems  
  Faropenem Nafcillin

Carbapenems  
  Ertapenem
Doripenem
Imipenem
Meropenem
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
  Ceftizoxime
4th  
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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