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BIOL 3200 (54)
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BIOL 3200

1. Antibiotic resistance 2. How do they work 3. What produces them 4. Over-prescription 5. Allergies? 6. Affect on microflora 7. Mass production • Inhibition of protein synthesis o Proteins are synthesized on ribosome • Differences in prokaryotic (70s) and eukaryotic (80s) ribosomes are responsible for selective toxicity  Drugs of this class include • Aminoglycosides • Tetracyclines • Macrolides • Chloramphenicol • Lincosamides • Oxazolidinones • Streptogramins o Prokaryotic kill prokaryotes “are we so different?”  What are the possible targets and considerations • Peptidoglycan • Ribosome o Inside cell • Tetracyclines o Reversibly bind 30S ribosomal subunit  Blocks attachment of tRNA to ribosome • Prevents continuation of protein synthesis o Effective against certain gram + and gram – o Newer tetracyclines such as doxyxycline (derivative of tetracycline) have longer half-life o Resistance due to decreased accumulation by bacteria cells • Macrolides o Reversibly binds to 50S ribosome o Effective against variety of gram +organisms and those responsible for atypical pneumonia o Often drug of choice if allergic to penicillin o Macrolides include  Erythromycin, clarithromycin, and azithromycin o Resistance can occur via modification of RNA target  Also production of enzyme that chemically modifies drug as well as alterations that result in decreased uptake of drug • Prokaryotes kill prokaryotes o Possible targets and considerations  Peptidoglycan and ribosome  Access, access, and mechanism • Inhibition of nucleic acid synthesis o These include  Fluoroquinolones • Target ‘bacterial’ DNA replica0on enzyme  Rifamycins- RNA synthesis • Can sometimes damage DNA • Reason birth control may not work while taking antibiotics • Inhibition of metabolic pathways o Inhibit enzymes in metabolic pathways o Most useful are folate inhibitors  Mode of ac0ons to inhibit the produc0on of folic acid o An0microbials in this class include  Sulfonamides  Trimethoprim • Sulfonamides o Competitive inhibition of enzyme that aids in production of folic acid o Inhibit growth of gram + and gram- o Structurally similar to para-aminobenzoic acid o Human cells lack specific enzyme in folic acid pathway o Resistance can be acquired from a plasmid  Plasmid has gene that encodes an enzyme that has mutations that lower affinity to drug o • Cell membrane integrity o Damage cell membrane  Polymyxin B most com
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