Antibacterial Agents 3: Protein Synthesis Inhibitors Flashcards
Macrolides Drug Types
Erythromycin, clathromycin, azithromycin
Macrolides MoA
Binding to 50S ribosome, blocking translocation of peptidyle RNA
Passive Diffusion
Bacteriostatic
Macrolide
Erythromycin
Absorption
Absorption varies depending on salt form
Estolate appears more bioavailable in children than ethyle succinate
Macrolides
Clarithromycin
Absorption
Can be taken without regards to food
Macrolides
Azithromycin
Absorption
Taken without food
Macrolides
Distribution
Wide distribution
except brain and CSF
Traverses placenta
Azi/Clathro= High tissue penentrance, low plasma levels
Macrolides
Erithromycin
Metabolism/Excretion
Liver and excreted in bile
Macrolides
Clarithromycin
Metabolism/excretion
Metabolized to active so renal excretion
Macrolides
Azithromycin
MEtabolism/Excretion
Not metabolized, high tissue penetrance
Gram Positive Cocci
Streptococci and pneumococci
Macrolide Atbx uses
All
Gram Negative Cocci
Moraxella catarrhalis
Macrolide Atbx use
All
Bordetella pertussis
Macrolide Atbx uses
All
Heamophillus influenzae
Macrolide Atbx use
Azithromycin, Clathrithromycin
Helicobacter pylori
Marolide Atbx Use
Clarithromycin with PPI or H2 antagonist
Legionella
Macrolide atbx uses
Azithromycin
Mycobacterium avium
Macrolide atbx use
Clarithromycin and Azithromycin
Chlamydia
Macrolide atbx use
Azithromycin
Mycoplasma pneumoniae
Macrolide atbx use
All
Macrolides
Adverse Efects
Direct stimulation of gut motility, increasing activity
with erithro
Hepatotoxic
Prolongs QT interval
E and C inhibits p450
Telithromycin
Erithromycin derivative
Use only for community-acquired pneumonia that is atbx resistant
Tetracyclines
Drugs
Tetracycline, Doxycycline, Minocycline
Tetracyclines
MoA
Bacteriostatic
Reversible binding to bacterial 30S ribo subunit
Resistance: Change influx, block binding