Aminoglycosides Flashcards
Aminoglycoside Examples
Streptomycin
Gentamicin
Tobramycin
Amikacin
Aminoglycoside MOA
inhibit protein synthesis by inhibiting 30S subunit of bacterial ribosome
inhibit protein synthesis
Resistance to Aminoglycosides
Mutation or methylation of 16S rRNA-binding site
Enzymatic destruction of the drug
Lack of permeability to the drug molecule –> drug cannot get into the organism
Active efflux (or lack of active transport)
CHANGE to BINDING SITE
Aminoglycoside Spectrum
aerobic gnb bacilli
Aminoglycosides are synergistic with….
penicillins for enterococci and streptococci
Streptomycin can be used for…
- TB
Aminoglycoside Route of Admin
- IV/IM
Aminoglycosides absorbtion
Penetrate tissues relatively poorly; not CNS
Aminoglycoside Adverse Effects
Nephrotoxicity
Ototoxicity
Neuromuscular blockade
Allergies rare
Aminoglycosides Drug Interactions
Other nephrotoxic drugs
Other ototoxic drugs
Neuromuscular blocking agents
Fluoroquinolone Examples
- Ciprofloxacin
- Levofloxacin
- Moxifloxacin
Fluoroquinone MOA
- inhibit DNA gyrase or topoisomerase II & IV
Bacteriocidal; concentration dependent killing
Inhibit DNA replication
Fluoroquinone Resistance
alteration of the A or B subunit of DNA gyrase
-
Mutation in ParC or ParE of topoisomerase IV
Change in outer membrane permeability –> cannot get in to act at DNA
Efflux pumps
In general, fluoroquinones spectrum is
highly active against gnb, Haemophilus sp, neisseriae, chlamydiae, etc
Ciprofloxacin Spectrum
most active against .P aeruginosa
Levofloxacin Spectrum
activity against S. pneumoniae –> gram positive cocci