ANTIBIOTICS QUICK REVIEW

Agents That Inhibit Peptidoglycan Synthesis

Drug Structure Mech. of Action Pharmacology Side Effects Resistance

Penicillins Nucleus  blocks peptidoglycan Natural Penicillins Hypersensitivity  Beta Lactamase
6-aminopenicillanic acid synthesis  Penicillin G  penicilloyl can act as - breaks lactam ring
Natural  beta lactam ring  blocks Transpeptidases and  acid labile hapten  Altered cell wall
 thiazolidine ring Carboxypeptidases involved  narrow spectrum formation
-side chain radicals in cell wall synthesis  high potency  Tolerance
determine properties of  active autolytic enzymes  sometimes autolytic
different penicillian types  Bactericidal against growing  Penicillin V enzymes not activated
bacteria  same but low potency by Penicillin
 results in:
 Low MIC
 High MBC
Semisynthetic various side chains added  stable in stomach acid
to nucleus to create various  wider spectrum
effects  Beta lactamase
resistance
Cephalosporins  like Penecillin except:  same as Penicillin above  Broad spectrum (gram+ Hypersensitivity same as Penicillin
 Dihydrothiazine ring -)
Note:
 Bactericidal
Semisynthetic
 Parenterally admin.
cephalosporins similar
 orally admin.
to Penicillin’s
Beta Lactamase  Little antimicrobial activity Examples: Augmentin = Clavulanic Acid + Amoxycillin
 given in combination with beta lactam sensitive drugs Timentin = Clavulanic Acid + Ticarcillin
Inhibitor Unasym = Sulbactam + Ampicilin
Zosyn = Tazobactam + Piperacillin
Vancomycin  Blocks transfer of Amino Sugars  Narrow spectrum Neurotoxic  alteration of cell wall
onto growing peptidoglycan  Bactericidal Nephrotoxic  Tolerant organisms

Bacitracin  same as above  Topical application Nephrotoxic

 Oral administration
Cycloserine  Blocks D-alanine incorporation  Narrow Spectrum: CNS toxicity
into Peptidoglycan Mycobacterium tuberculosis
 Agents That Block Protein Synthesis by Binding Ribosomal Subunits
Drug Category Specific MOA Bugs Side Effects Resistance
Aminoglcosides Bactericidal Blocks formation of  Narrow spectrum  Ototoxicity  Enzymatic modification
initiation complex - gram (-) rods - especially in combo with - Acetyltransferase
Gentamicin loop diuretics  Blocks transport into cell
Streptomycin mRNA misreading  Nephrotoxicity  Alteration of biding site
Tobramycin
Amikacin
Tetracyclines Bacteriostatic Prevents  Broad Spectrum
Chlamydia
 Discoloration of kids 

Plasmid
less Permeable bacteria
Doxycycline and attachement of teeth
Borrelia burgdorferi  Resistant to All if resistant
Minicycline (cleared in charged tRNA Rickettsiae (Board
 Bone growth block in to one
feces.. use in renal Question!) kids
failure) Acne  GI
Renal clearance
Mini dox feces Tularemia  Fanconi’s Syndrome
except for mini dox
Cholera  Photosensitivity
Ureaplasma
Mycoplasma
CB RAT CUM

Chloramphenical Bacteriostatic peptidyl

Blocks Meningitis bugs  Marrow depression 

Acetyltransferase
altered cell wall decreasing
transferase H influenza  Aplastic Anemia
N meningitidis permeability
Strep Pneumonia
 Gray baby
(premies with low liver UDP-
glucuronyl transferase)

Erythromycin Bacteriostatic Blocks Gram (+) Cocci  Hepatotoxic  altered cell wall decreasing
Translocation Legionella permeabilty
 GI  alteration of 50S binding site
Mycoplasma  Cross resistance between
Neisseria macrolides & lincosamides
Chlamydia
LMN
C+
(C+ is as easy as LMN) (not
ABC)

Lincosamides Bacteriostatic

Lincomycin
 Clindomycin

Agents Inhibiting Nucleic Acid Function

Drug Category Specific MOA Bugs Side Effects Other
Metronidazole Bactericidal Steps  Narrow spectrum Disulfiram – like rxn
1. Passive Diffusion into cell - Anaerobic bacteria/protazoa Vestibular dysfunction
2. Reduction of drug - Amebiasis
produces toxic - Giardia I took the Metro and got dizzy
- Gardenella and vommitted (disulfarim-like)
intermediates - Trichomoniasis
3. breaks bacterial DNA
vAGinA and
GuT
Rifampin  Blocks RNA  Anti-TB The 4 R’s for Rifampin
Polymerase  broad spectrum, but - RNA Polymerase
resistance - Revs up P450
developes quickly so must be - Red/orange body
used in Combination with fluid
others - Resistance is rapid
Nalidixic Acid Bactericidal  Blocks DNA  UTI Cartilage and Tendon
Gyrase damage in animal studies
CI
- Pregnancy
- Kids
Quinolones “ “ “

Mechanism of action not exactly clear:

Drug Structure Mech. of Action Pharmacology Side Effects Resistance
Isoniazid (INH) Pyridoxine 
(B6) Analog
? Antagonizes
Pyridoxine catalyzed


Anti-TB
quick resistance so combine with
reactions other anti-TB drugs
 Narrow spectrum
Nitrofurans  ? oxidation of Pyruvic
Acid


Bacteriostatic
Broad Spectrum
Nitrofurantoin
Ethambutol ? 

Anti-TB
quick resistance so combine with
rare retinal damage
 other anti-TB drugs

Agents Blocking Folic Acid Synthesis

Drug Structure Mech. of Action Pharmacology Side Effects Resistance

Sulfonimides various side 
chains 
PABA Analogs
tie up


Urinary tract infections
Bacteriostatic
 Hypersensitivity 

PABA Overproduction
Structural alteration of
Sulfanilamide Tetrahydropteroic acid  Broad Spectrum Tetrahydropteroic acid
Sulfamethoxazole synthetase  Folic Acid dependency
 Purine synthesis  Decreased permeability
inhibited
Sulfones  unknown, but probably
like above


Leprosy treatment
Narrow Spectrum
 unknown mechanism

DDS
Trimethoprim  Blocks dihydrofolate
reductase
 mixture of Trimethoprim and 
Sulfamethoxazole will inhibit 2
same as
sulfonimides
 same as sulfonimides but based
on Dihydrofolate reductase
 prevents folic acid steps in folic acid synthesis thereby
synthesis increasing spectrum of activity
 Purine synthesis
inhibited

Agents that Damage Cell Membrane

Drug Structure Mech. of Action Pharmacology Side Effects Resistance

Polymixin Polypeptide  Cationic Detergent  Bactericidal against Resting
and Dividing bacteria
 Neurotoxic
- dose related / reversible
 Altered cell wall to protect
inner membrane
Polymixin B  Narrow Spectrum  Nephrotoxic
Polymixin E  Topical Ointments - dose related
(Colistin)
 Agents with Unknown Mechanisms of Inhibition

Drug Structure Mech. of Action Pharmacology Side Effects Resistance

Isoniazid (INH) Pyridoxine 
(B6) Analog
? Antagonizes
Pyridoxine catalyzed


Anti-TB
quick resistance so combine with
reactions other anti-TB drugs
 Narrow spectrum
Nitrofurans  ? oxidation of Pyruvic
Acid


Bacteriostatic
Broad Spectrum
Nitrofurantoin
Ethambutol ? 

Anti-TB
quick resistance so combine with
rare retinal damage

other anti-TB drugs