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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  acid labile hapten  Altered cell wall
 thiazolidine ring and Carboxypeptidases  narrow spectrum formation
-side chain radicals involved in cell wall synthesis  high potency  Tolerance
determine properties of  active autolytic enzymes  sometimes
different penicillian types  Bactericidal against  Penicillin V autolytic enzymes
growing bacteria  same but low not activated by
potency Penicillin
 results in:
 Low
MIC
 High
MBC
Semisynthetic various side chains added  stable in stomach
to nucleus to create various acid
effects  wider spectrum
 Beta lactamase
resistance
Cephalosporins  like Penecillin  same as Penicillin above Broad spectrum (gram+ -) Hypersensitivity same as Penicillin
except:  Bactericidal
Note:
 Dihydrothiazine  Parenterally admin.
Semisynthetic
ring  orally admin.
cephalosporins similar
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  Narrow spectrum Neurotoxic  alteration of cell wall
Sugars onto growing peptidoglycan  Bactericidal Nephrotoxic  Tolerant organisms

Bacitracin  same as above  Topical application Nephrotoxic


 Oral administration
Cycloserine  Blocks D-alanine  Narrow Spectrum: CNS toxicity
incorporation 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
Streptomycin mRNA misreading  Nephrotoxicity cell
 Alteration of biding site
Tobramycin
Amikacin
Tetracyclines Bacteriostatic Prevents  Broad Spectrum
Chlamydia
 Discoloration of 

Plasmid
less Permeable bacteria
Doxycycline and attachement of kids teeth
Borrelia burgdorferi  Resistant to All if
Minicycline (cleared in charged tRNA Rickettsiae (Board  Bone growth block resistant to one
feces.. use in renal Question!) in kids
failure) Acne  GI
Renal clearance
Mini dox feces Tularemia  Fanconi’s
except for mini dox
Cholera Syndrome
Ureaplasma
Mycoplasma  Photosensitivity
CB RAT CUM

Chloramphenical Bacteriostatic Blocks peptidyl Meningitis bugs  Marrow  Acetyltransferase


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

Erythromycin Bacteriostatic Blocks Gram (+) Cocci  Hepatotoxic  altered cell wall
Translocation Legionella decreasing permeabilty
 GI  alteration of 50S
Mycoplasma binding site
Neisseria  Cross resistance
Chlamydia between macrolides &
LMN lincosamides
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
1. Passive Diffusion into cell - Anaerobic bacteria/protazoa rxn
2. Reduction of drug - Amebiasis Vestibular
produces toxic - Giardia dysfunction
- Gardenella
intermediates - Trichomoniasis
3. breaks bacterial DNA I took the Metro and got dizzy
and vommitted (disulfarim-like)
vAGinA and
GuT
Rifampin  Blocks RNA  Anti-TB The 4 R’s for Rifampin
Polymerase resistance
 broad spectrum, but - RNA Polymerase
developes quickly so must be - Revs up P450
used in Combination with - Red/orange body
others fluid
- 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