Antibiotics Flashcards
Mupirocin: Class? Action? Bacteriostatic/cidal? Species range? Applications?
Translation inhibitor
Binds isoleucyl-tRNA synthetase, so no charged ile-tRNA available
Bacteriostatic at low concentrations, cidal at higher (with topical administration)
Used in surgeons to prevent transmission of MRSA from nasal cavity
Ciprofloxacin: Class? Action? Bacteriostatic/cidal? Species range? Applications?
Fluoroquinolone (DNA replication inhibitor)
Inhibits DNA gyrase and thus DNA synthesis
Bacteriocidal
Broad spectrum: Gm- enterics, G+ cocci, Pseudomonas
Resistance emerging
Not for kids or pregnant women
Moxifloxacin: Class? Action? Bacteriostatic/cidal? Species range? Applications?
Fluoroquinolone (DNA replication inhibitor)
Inhibits DNA gyrase AND topoisomerase activity (less susceptible to resistance)
Bacteriocidal
Broad spectrum: Gm- enterics, G+ cocci, Pseudomonas, MRSA
Not for kids or pregnant women
Metronidazole: Class? Action? Bacteriostatic/cidal? Species range? Applications?
Nitroimidazole (DNA replication inhibitor)
Activated form (in anaerobic conditions) binds DNA and fragments it
Bacteriocidal
Useful against anaerobic bacterial, protozoa
Rifampin: Class? Action? Bacteriostatic/cidal? Species range? Applications?
RNA synthesis inhibitor
Binds beta subunit of RNA pol, inhibiting transcription
Bacteriocidal
Broad spectrum
Effective prophylactic against N. menigitidis b/c secreted in saliva
Resistance develops rapidly, used in combo
Example of antagonistic combined antibiotic action
Penicillin (requires growth) given with bacteriostatic agent (tetracycline)
Ethambutol and pyrazinamide: Class? Action? Bacteriostatic/cidal? Species range? Applications?
Anti TB drugs Unknown mechanism of action E- static, P- cidal once activated Narrow spectrum (TB)
Example of synergistic combined antibiotic action
Agent which damages cell wall/membrane with cidal agent taken up poorly by bacterium
Indications for combined use of antibiotics (5)
Synergistic activity expected Pathogen requires more than one agent Likelihood of resistance reduced Dosage of toxic drug can be reduced Polymicrobial infection requires use of more than one agent
Disadvantages of combined antibiotics (4)
Increased risk of side effects
Increased risk of superinfections
Possible antagonism
Increased cost
4 general reasons for antibiotic inactivity
- Enzyme inactivation: antibiotic is inactivated (extracellular, intracellular, both)
- Altered membrane permeability/antibiotic efflux: antibiotic can’t enter cell or is actively pumped out
- Alteration of ribosomal/cell wall precursor/enzyme targets: bacterial cell contains altered enzyme that resists action of antibiotic
- Bypass pathways: antibiotic enters cell but drug-binding target site is replaced
Mechanisms of resistance to trimethoprim
Plasmid-coded, trimethoprim-resistant dihydrofolate reductase
Mechanisms of resistance to penicillins (3)
Hydrolysis of beta-lactam ring by beta-lactamase
Decreased cephalosporins permeability of bacteria
Altered penicillin binding proteins
Mechanisms of resistance to methicillin
Altered penicillin binding proteins
Beta-lactamase resistant
Mechanisms of resistance to aminoglycosides (3)
Enzymatic modification of drug by plasmid-coded enzyme
Decreased permeability to antibiotic
Altered antibiotic binding site
Mechanisms of resistance to tetracyclines
Interference with transport of drug into cell
Mechanisms of resistance to chloramphenicol
Detoxification of drug by acetylation of hydroxyl
Mechanisms of resistance to erythromycin
Enzymatic methylation of 23S ribosomal RNA
Mechanisms of resistance to ciprofloxacin/rifampin
Altered target enzymes (gyrase, RNAP)
Mechanisms of resistance to vancomycin
Alteration of cell wall precursor target
Characteristics of an ideal antibiotic (4)
Target one or more bacterial species with no toxicity or allergy
Persist long enough to destroy target
Not lose effectiveness due to bacterial resistance
Achieve effective concentrations in sites of infection
Define bacteriostatic
Stops growth of bacteria for a time
Define bacteriocidal
Kills bacteria
What is the Kiby-Bauer disc diffusion method? How does it work?
Allows you to test the sensitivity of multiple antibiotics against a given strain
Plate purified bacteria on agar plate
-> Add filter paper discs with antibiotic onto the surface
-> Measure circular zones of inhibition of bacterial growth around each disc
(inhibition = sensitivity, growth = insensitivity)