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FUN 24 ANTIBIOTICS - PROTEIN SYNTHESIS INHIBITORS (linezolid (oxazolinone,…
FUN 24 ANTIBIOTICS - PROTEIN SYNTHESIS INHIBITORS
Bacteriostatic
target = prokaryotic ribosomes
30 + 50 subunits = 70S
different from mammalian ribosomes...
bigger
40 + 60 subunits = 80S
some bind to 30 subunit
macrolides, linezolid, streptogramins
some bind to 50 subunit
ahminoglycosides, tetracyclines
5 classes
aminoglycosides (elongated effect)
macrolides (elongated effect)
tetracyclines
amphenicols
oxazolidinones
aminoglycosides
amino sugars linked by glycosidic bonds
IV
enter cells via O2 dependent transporter
hence only work for aerobic bacteria
toxicology
mild, common, reversible nephrotoxicity
rare, permanent ototoxicity
resistance: less permeability + xenobiotic pump
macrolides
contain a multimembered lactone ring with deoxy sugars attached
not given with H1 antagonists (tachycardia)
resistance: xenobiotic pump + target mutation
lincosamides
same MOA as macrolides
orally active against gram +ve + anaerobes
resistance: target mutation
streptogramins
combination of quinupristin + dalfopristin
alone bacteriostatic, together bactericidal
bind to different sites on 50 subunit
multiple daily IV infusions
resistance: target mutation
linezolid
oxazolinone
blocks formation of initiation complex
admin: oral, IV, CSF
works against MRSA
SE = myelosuppression
resistance: target mutation
tetracyclines
4 fused cyclic rings
stain growing teeth!
resistance: xenobiotic pump
lipopeptide antibiotics
daptomycin
cyclic lipopeptide
lipid chain inserts into membrane + makes pore
causes depol + disrupts membrane potential
proteins can no longer be synthesised
bactericidal against gram +ve
resistance: bacteria increases its +ve charge
televancin