Major Antibiotics--mxn & resistance Flashcards
Macrolides
Mechanism: (bacteriostatic)
-50s, inhibit translocation
Resistance:
-methytransferases alter the binding site
Chloramphenicol
Mechanism: (bacteriostatic)
-50s, inhibit transpeptidation
Resistance:
-inactivating acetyltransferases
*bactericidal → pneumococci, meningococci, haemophilus
Aminoglycosides
Mechanism: (bactericidal– concentration dependent)
- 30s, blocks initiation
- elicit premature termination
- incorporate incorrect AA
Resistance:
-acetyl, phosphoryl, or adenylyl conjugation
-long PAE (esp. against Gram Negative)
Tetracycline
Mechanism: (bacteriostatic)
-30s, prevent binding the incoming charged tRNA
Resistance:
-pump out
Fluoroquinolones
Mechanism: (bactericidal– concentration dependent)
-inhibit topoisomerase
Resistance:
- change in sensitivity of TE
- pump out
-long PAE (esp. against Gram Negative)
Rifampin
Mechanism: (bactericidal)
-inhibits DNA dependent RNA polymerase
Resistance:
-change in enzyme
Sulfonamides
Mechanism: (bacteriostatic)
- inhibits folic acid synthesis
- -bacteria must make folic acid
Resistance:
- ↓ sensitivity of the target enzymes
- ↑ formation of PABA
- use of exogenous folate
Beta lactams
Mechanism: (bactericidal– time dependent)
-inhibit bacterial cell wall synthesis
Resistance:
- penicillinase
- modification of PBP’s
- change of porins
Vancomycin
Mechanism: (bactericidal– time dependent)
-inhibition of peptidoglycan chain elongation
Resistance:
-change in pentapeptide, D-ala → D-lactate