Antibacterials Flashcards
Four Mechanisms of Actions of Antibacterials
- inhibitors of cell wall synthesis
- inhibitors of translation and transcription
- inhibition of DNA syntheses and integrity
- inhibitors of folate synthesis and function
Inhibitors of Cell Wall Synthesis
beta lactams penicillins
cephalosporins
glycopeptides: vancomycin
TB medications
Inhibitors of Translation/Transcription
tetracyclines
macrolides
clindamycin
oxazolidinones: linezolid
aminoglycosides and spectinomycin
TB medications
Inhibition of DNA syntheses and integrity/inhibitors of folate synthesis and function
sulfonamides, trimethoprim
quinolones
Bactericidal
mechanism is generally inhibit cell wall synthesis
time dependent killing
concentration dependent killing
Time Dependent Killing
serum level above MIC
beta lactams, vancomycin
Concentration Dependent Killing
higher drug concentration determines rate and extent of killing
aminoglycosides, quinolones
Bacteriostatic
mechanism is generally inhibition of protein synthesis
tetracyclines, macrolides, sulfonamides
Postantibiotic Effect
persistent suppression of bacterial growth after limited exposure to an antimicrobial agent
antibiotic level falls below MIC
Postantibiotic Effect: Proposed Mechanisms
slow recovery after reversible non lethal damage to cell structures
persistence of the drug at the binding site
need to synthesize new enzymes before microorganism growth can resume
Penicillin: narrow spectrum
Penicillinase susceptible:
- PCN G
- PCN VK
Penicillinase resistant:
- nafcillin
- oxacillin
Penicillin: wider spectrum
+/- penicillinase inhibitor
- ampicillin
- amoxicillin
- piperacillin
- ticarcillin
What additional microorganisms are covered by amoxicillin but NOT penicillin?
H influenza
M catarrhalis
S aureus
Strept
Penicillin: PK
rapid renal elimination
some biliary clearance (ampicillin, nafcillin)
-concern for newborns
Penicillin: ADE
hypersensitivity rxn
maculopapular rash (ampicllin)
Penicillin: activity spectrum (narrow and wider)
Narrow:
- streptococcal infections
- staphlococcal infections
- meningococcal infections
- syphilis
Wider:
-gram negative bacteria
Cephalosporins: first generation
cephalexin
activity:
- skin
- soft tissue
- UTI
Cephalosporins: second generation
cefotetan
cefoxitin
cefuroxime
activity:
- S pneumoniae
- H influenza
- B fragilis (cefotetan)
Cephalosporins: third generation
ceftriaxone
cefixime
cefotaxime
ceftazidime
activity:
- pneumonia
- meningitis
- gonorrhea
- broad activity(beta lactamase stable)
Cephalosporins: fourth generation
cefipime
activity:
-pseudomonas
Cephalosporins: fifth generation
ceftaroline
activity:
- skin
- soft tissue
- CA pneumonia
Cephalosporins: PK
older: oral
newer: IV
renal elimination
THIRD GENERATION ENTER CNS
Cephalosporins: ADEs
hypersensitivity reactions
assume complete cross reactivity bt cephalosporins
1st generation: partial cross reactivity with PCNs
What cephalosporin is not given to newborns?
cetriaxone
-displaces bilirubin