Antibiotics Flashcards
bactericidal
Kill
Bacteriostatic
slow/stop replication
Ideal Antibiotic
- broad spectrum
- not induce resistance
- high therapeutic index
- –ratio of 1 means effective dose would be toxic
- selective toxicity
Selective Toxity
Cell wall is unique in microbes
Enzymes for replicaiton, transcription, and translation can be unique in microbes
Microbes have some unique essential metabolites
Ribosome structure unique in microbes
Penicillin
Disrupts cell wall synthesis
- cleaves off D-ala needed for synthesis
- after cleavage becomes toxic for bacterial cell
Inhibition of DNA replication problem
these inhibitors can attach to host dna
- metronidazole is inactive in aerobic conditons
- -only becomes active in anaerobic bacterial conditions
DNA gyrase
unique in bacteria
-attacked by nalidixic acid and quinolones
rifamycin
inhibit RNA polymerase
Steps in the action of antibiotics
- Drug penetrates the envelope
- Transport into the cell
- Drug binds to target
Mechanism of Drug Resistance
Synthesis of enzymes that inactivate the drug
Prevention of access to the target site
1. Inhibiting uptake 2. Increasing secretion of the drug
Modification of the target site
Preventing access to target site
Many antibiotics enter the cell through porins (proteins that extend across the lipid bilayer and create channels or pores)
Resistance to tetracyclines and quinolones
Some bacteria develop efflux pumps to pump the antibiotics out of them (resistance to tetracycline)
All classes of bacteria have been shown to have drug efflux transporters
Modification of target site
- Modify enzyme affinity
2. Alteration of metabolic pathway