Flashcards in antibiotics for osteomyelitis and skin infections med chem Deck (42)
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tetracycline drugs
tetracycline
monocycline
doxycycline
tigecycline
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tetracycline MoA
interacts with 30S subunit of ribosome and sits in A site to prevent elongation (bacteriostatic)
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tetracycline general pharmacophore
4 rings and dimethylamine pointing into the board
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ways to inactivate tetracyclines
-make dimethylamine come out of the board
-dehydration of OH on north side
-breaking C ring through intramolecular reaction
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avoid taking tetracyclines with what
multivitamins and milk because of chelation with ions
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tetracyclines clinical use
-Gm+
-MRSA
-limited Gm-
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tetracycline resistance
widespread in forms of
-efflux
-mutations in ribosome
-cell wall variation
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side effects of tetracyclines
-light sensitivity
-severe kidney damage
-incorporation into bones and teeth
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tigecycline unique structure feature
the claw on the tetracycline ring that prevents efflux based resistance
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tigecycline clinical use
broad spectrum, typically saved for instances of resistance
*hits basically everything but pseudomonas*
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clindamycin MoA
sits in 50S peptidyltransferase to inhibit the enzyme
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clindamycin clinical use
-Gm+ (staph, strep)
-used w/ aminoglycosides for Gm-
-some anaerobes
-used if PCN allergy
-PO/IV
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clindamycin side effects
-GI
-pseudomembranous colitis caused by C.difficile
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linezolid MoA
prevents formation of 70S subunit complex by binding w/ 50S subunit
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linezolid clinical use
-Gm+
-MRSA
-VRE
-IV/PO
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linezolid resistance
still rare but can be seen as:
-point mutation of ribosome
-efflux pump in Gm-
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linezolid side effects
-monoamine oxidase inhibitor, so avoid w/ tyramine foods and serotonergic drugs
-bone marrow suppression
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linezolid monitoring
weekly blood counts
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synercid
-IV only
-combo of dalfopristin and quinupristin
-30:70 ratio quinupristin:dalfopristin because dalfo binding first increases affinity for quinupristin
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synercid MoA
binds to A and P sites to interfere with tRNA binding and misalignment of P site
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mupirocin MoA
binds to Ile-tRNA synthetase to prevent incorporation of Ile into proteins
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mupirocin clinical use
-used topically or nasally because it is hydrolyzed in vivo
-broad spectrum activity, good against staph and strep
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mupirocin resistance
mutations in synthetase enzyme prevents binding
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vancomycin MoA
"hugs" cross link area of peptidoglycan to prevent transpeptidase cross link AND prevents sugars from cross linking
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vancomycin clinical use
-narrow spectrum Gm+
-used for C.diff and enterococci
-last resort for MRSA
-PO/IV
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vancomycin resistance
D-Ala D-Ala becomes D-Ala D-Lactate to reduce hydrogen bonding
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vancomycin resistant enterococci background
-2nd most common Gm+ in hospitals
-high moretality
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treatments for VRE
synercid
linezolid
cubicin (daptomycin)
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linezolid route
oral and IV
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