Flashcards in Pharm antimicrobials 2 Deck (57)
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1
vancomycin class
glycopeptide - cell wall synthesis inhibitor
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vancomycin mechanism
binds rapidly and irreversibly to the D-alanyl-D-alanine group on the peptide side-chain of the membrane-bound precurosr; glycan chain extension, transpeptidation inhibited
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vancomycin spectrum - why?
gram + only - molecule is HUUUUGGGGGEEEEE!!! can't get into gram -
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vancomycin clinical uses
serious, multidrug-resistant organisms including MRSA, s epidermidis, enterococcus, clostridium difficile
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vancomycin adverse effects
well tolerated in general but NOT trouble free (Nephrotoxicity, Ototoxicity, Thrombophlebitis and red man syndrome)
Red man driving a van down the intestine getting c diff
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vancomycin administration
IV only - not absorbed orally
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what is the advantage of vancomycin not being absorbed orally?
c difficile is in gut - it doesn't need to be absorbed to treat this
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daptomycin class
cell wall TOXIN - lipopetide
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daptomycin mechanism
penetrates gram + cell wall forming a channel for subsequent leakage of intracellular ions
-insertion into the gram + cell membrane causing depolarization and ultimate cell death
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daptomycin spectrum
gram + cocci only - used for VRE and VRSA (vancomycin resistant organisms)
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what is daptomycin not used for? why?
pneumonia because it avidly binds to and is inactivated by surfactant
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daptomycin side effects
myopathy and rabdomyolysis,
also eosinophilic pneumonia
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what are the lipoglycopeptides (analogs of vancomycin)
-vancins
dalbavancin, telavancin, oritavancin
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-vancins mechanism
binds to same target as vancomycin (D-alanyl-D-alanine group on peptide side-chain of the membrane-bound precursor)--> cell wall precursor and inhibits transglycosylation
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-vancins spectrum
similar to vancomycin (gram + only) but active against VRE and more anaerobe coverage
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-vancins side effects
metallic taste, nausea, HA, nephrotoxicity, teratogenic (don't take if preggers)
also very very expensive
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what is the half life of the -vancins? what is the longer half life due to?
telavancin - 7.5 hr
dalbavancin and oritavancin long (100+ hrs)
-due to lipophilic side chain that prolongs half life
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are protein synthesis inhibitors bacteriocidal or bacteriostatic?
bacteriostatic EXCEPT aminoglycosides
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30 S ribosomal subunit protein synthesis inhibitors
ATG = DNA = small
aminoglycosides, tetracyclines, glycylcyclines
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50S ribosomal subunti protein synthesis inhibitors
COM = bigger and better!
clindamycin, oxazolidinones, macrolides
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what are the aminoglycosides?
gentamicin, tobramycin, amikacin, streptomycin
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aminoglycoside mechanism
bactericidal: irreversible inhibition of initiation complex through binding of the 30S subunti - can cause misreading of mRNA - also inhibits initiation
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aminoglycoside spectrum
extremely effective against G- rods (esp enterics)
covers pseudomonas aeruginosa!!
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what are aminoglycosides ineffective against? why?
anaerobes!! have O2 dependent uptake mechanism!!!
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clinical use of aminoglycosides - what is it given with? why?
synergistic with cell-wall active agents for enterococcus infections (esp penicillins because they facilitate entry), cystic fibrosis (pseudomonas common infection)
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aminoglycosides side effects
the MEAN GUY! (bacteriocidal)
-punch to the ear (ototoxicity)
-punch to the kidney (nephortoxicity)
-punch a pregnant woman (teratogen)
-knock them out (neuromuscular blockade)
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which aminoglycoside is toxic and is typically only used topically for skin infections?
neomycin
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which aminoglycoside has the broadest spectrum?
amikacin
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what are the tetracyclines?
-cycline
doxycycline, minocycline, tetracycline
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