Nucleic acid
Inhibit the synthesis of nucleotides
Alteration of base pairing property of template
By inhibiting either DNA or RNA polymerase
Inhibition of DNA gyrase
Direct effect on DNA
Formed structures of the cells
Cell membrane
Antifungals
DNA
Bleomycin for cancer
Intracellular organelles
Microtubules:
Albendazole intestinal worm
vinca alkaloids for cancer
Food vacuoles
Chloroquine
Muscle fibres
Anthelmintics: piperazine, pyrantel
Antimicrobials
Infectious Microbes Are Living Entities
With a Nearly Unlimited Ability to Adapt
Microbes Tiny Organisms
Control symptoms
Destroy organisms
Eradicate diseases
Antimicrobials
Antimicrobials
The chemicals to kill or control the
growth of micro-organisms
Antibiotics
Chemicals obtained from living organism
to kill or control the growth of micro-
organisms
History of Antimicrobials
Time line of events
1980s,
1928, 1962,
1940s: Penicillin Fluorinated
Penicillin Quinolones
becomes commercially Quinolones
discovered discovered
available and available
Cephalosporins are
synthesized
How to choose an
antimicrobial
Antibiotic may be Proper?
diagnosis
chosen before results
of the culture are
available based on
some preliminary
information
Site of infection and
likely causative
organism
Gram-stain result
(does result
correlate with
potential organism
above)
Minimal inhibitory concentration
lowest level stopping growth
-lactam antibiotics
Penicillins
Cephalosporins
Cycloserine
Vancomycin
Bacitracin
Cell Membrane
Bacteriocidal
Kills bacteria, effective when host
immune system is compromised
Resistance to drugs
1. Alteration in membrane permeability
Membrane transport or pores
Antimicrobials cannot cross
tetracyclines, quinolones, aminoglycosides
2. Alteration of target
Bacterial ribosomes altered by DNA mutation
Antimicrobial agent no longer binds
erythromycin, rifamycin, antimetabolites
Resistance to drugs
3. Development of enzymes
lactamase which inactivates
penicillin & cephalosporins;
4. Enzyme alteration
Sulfonamide resistant bacteria have ability
to acquire needed PABA when drug is present
Resistance to drugs
5. Metabolic pathway alteration
By-pass reaction inhibited by antimicrobial
agent
Sulfonamide resistant bacteria can by-pass
production of Folic acid and use ready made
folic acid from environment
Factors contributing to
resistance
Widespread use of antibiotics