macrolides, vanco, and metronidazole med chem/pharmacology Flashcards
(28 cards)
coverage of macrolides
- strep
- Gm- bacteria
macrolide side effects
GI (erythromycin most)
macrolides MoA
binds 50s subunit of ribosome at E site (static)
important part of ribosome for macrolide binding
Adenine 2058
*major mutation site in resistance)
forms of resistance to macrolides
- mutation at A2058
- esterases
- efflux
specific compound in erythromycin degradation responsible for GI effects
the spiroketal
what makes clarithromycin and azithromycin have less GI effects
structures prevent the formation of the ketal
unique side effect of clarithromycin
metallic taste
clindamycin MoA
blocks peptidyltransferase in 50S subunit
clindamycin coverage
- Gm+
- anaerobes
side effects of clindamycin
- skin rash
- psedomembranous colitis from C.diff
C.diff features
- Gm+ anaerobe
- produces spores that are hard to get rid of
- shed in feces and contaminates anything it touches
antibiotics that can treat C.diff
- metronidazole
- PO vanco
- fidaxomicin
Metronidazole MoA
generates a nitro radical and interferes with RNA and DNA
metronidazole coverage
- anaerobes
- C.diff
- protozoans
metronidazole side effects
- diarrhea
- dizziness
- neuropathy
- metallic taste
DDIs with metronidazole
- warfarin (increased bleeding)
- alcohol (disulfiram-like reaction)
Fidaxomicin MoA
binds to DNA template to inhibit RNA polymerase complex and transcription
fidaxomicin coverage
- Gm+ anaerobes
- C.diff
how are bacterial susceptibilities determined
calculating minimum inhibitory concentration
how can we estimate the MIC
zone diameters on agar plate cultures
what pharmacodynamic parameter best predicts vancomycin efficacy
AUC/MIC ratio
minimum vanco trough concentration to avoid resistance
- for no MIC 10 mg/L
- for MIC of 1, 15 mg/L
target trough concentration of AUC:MIC
at least 400