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133 Cards in this Set
- Front
- Back
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peripheral neuropathy
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fluoroquinolones
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greatest risk of long qt syndrome; least
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moxofloxacin; levofloxacin
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phototoxicity
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fluoroquinolones and tetracyclines
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tendon rupture
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fluoroquinolones
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cartilage erosion
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fluoroquinolones
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enters thru porins
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fluoroquinolones
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urinary excreted fluoroquinolones
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cipro and levo
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kidney excreted fluoroquinolones
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moxifloxacin
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antacids, calium, zinc not to be taken with
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fluoroquinolones
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anthrax tx
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cipro
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pneumonic plague tx
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levofloxacin
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complicated intra-abdominal anaerobic infections
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moxifloxacin
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moxifloxacin prescribed mostly for
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resp infections
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fluoroquinolone better for anaerobes
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moxi
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fluoroquinolone best for atypical organisms like mycoplasma, chlamydia, legionella
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levo
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enhanced activity against gram pos like strep pneumoniae
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levo
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best action against gram pos cocci and bacilli
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moxi
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effective against gram neg bacteria
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fluroquinolones
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2nd gen, 3rd gen, 4th gen fluoroquinolones
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cipro, levo, moxi
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bind replication fork (topisomerase II in gram neg) and topoisomerase IV in gram pos
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fluoroquinolones
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post antibiotic effect
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fluoroquinolones and aminoglycosides
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concentration dependent killing
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fluoroquinolones and aminoglycosides
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how to rectify anti folate toxicity
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folinic acid
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acute hemolytic anemia in ppl with G6PD deficiency
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sulfonamides
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kernicterus
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sulfonamides
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stevens johnson syndrome
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sulfonamides
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inadequate glucuronidations in enonates
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sulfonamides
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effective for pneumocystis jurovecii (carinii) in immunosuppressed pts
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SMX-TMP
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tx for toxoplasmosis in immunosuppressed pts
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SMX-TMP
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folic acid auxotrops naturally resistant to
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SMX-TMP
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mycobacterium tb resistant to
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SMX-TMP
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penicillin resistant pneumococci resistant to
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Smx-tmp
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p aeruginosa resistant to
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Smx-tmp
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specificitity for DHFR in prokaryotes
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trimethoprim
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effective against some h influenza
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smx-tmp
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sulfoniamide is competitive inhibitor of
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dihydropteroate synthase
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binds 30s ribosome
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aminoglycosides
tetracyclines |
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Aminoglycosides pneumonic
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MEAN GNATS caNNOT kill anerobes
gentamycin, neomycin, amikacin, tobramycin, streptomycin nephrotoxicity, neuromuscular blockade, ototoxicity, teratogen |
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for gentamicin resistant organisms in nosocomial gram neg infections
effective against mtb and atypical mycobacteria in AIDS pts |
amikacin
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most common used for gram neg aerobic
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gentamicin
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worst nephro and ototoxicity- only used for TB and topical
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kanamycin
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topical use, bowel sterilization
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neomycin
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for tb in hospital setting
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streptomycin
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p aeruginosa aminoglycoside tx
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tobramycin
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require O2 for uptake
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aminoglycosides
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therapy for brucellosis
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gentamycin + doxy
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tularemia tx
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gentamicin
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plague (yersinia) tx
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streptomycin + doxy
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psydeomonas aeruginosa tx
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tobramycin +pipericillin/ticarcillin
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klebsiella tx
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gentamicin +pip/ticarcillin
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clinical use of aminoglycosides
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severe gram neg rod infections; used with b lactam
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why are aminoglycosides ineffective against anaerobes
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they require o2 for uptake
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empiral tx of gram neg infections
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aminoglycosides
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MOA of aminoglycosides
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passive diffusion thru porins in outer membrane
o2 dependent active trans into cytosol via inner membrane binds 30s subunit disrupts protein synthesis and causes misreading of mRNA |
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Mech of resistance of aminoglycosides
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-depletion of porins (MDR)
-anaerobes -impaired binding to 30s via acetylation, phosphorylation, adenylation -mutation of 30s |
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anaerobes resistant to aminoglycosides
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gram + clostridia
gram - bacteroides, fusobacteria facultative bacteria in true anaerobic environment |
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3 modifications of amino or hydroxyl groups on aminoglycosides that resistant bacteria make to inhibit entry via porins or inhibit 30 s binding
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acetylation
phosphorylation adenylation |
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adverse effects of aminoglycosides
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nephotoxicity
ototoxicity neuromuscular blockade teratogen |
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one single dose vs multiple dose of aminoglycosides
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single dose is safer b/c with multiple dosing, drug accumulates
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highly polar, poorly absorbed by GI tract, accumulation in renal cortex and ear perilymph
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aminoglycosides
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nephrotoxicity risk increases with
ototoxicity risk increases with |
cephlosporins
loop diuretics |
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can cause deafness in children expose to drug during pregnancy
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aminoglycosides (streptomycin and tobramycin)
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may produce myasthenia gravis as side effect
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aminoglycoside
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first choice aminoglycoside for serious gram neg infection
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gentamycin
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aminoglycoside for endocarditis, peritonitis
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gentamycin
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tx of rickettsial infections
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doxy
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tx of borrelia burgdorgeri (spirochete), lyme dz
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doxy
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tx of chlamydia
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doxy
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tx of mycoplasma pneumonia of young adults in close quarters
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doxy
alternate-erythromycin |
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tx of cholera
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doxy
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binds 30s and inhibits attachment of aminoacyl tRNA to mRNA ribosome complex; bacteriostatic
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tetracylcines
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amphipathic (hydrophobic and hydrophilic sides) substances that can enter cytosol of bacteria, mitochondria in mammals
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tetracyclines
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mechanisms of resistance to tetracycline
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-tetracycline efflux pump
-ribosome protection via methylation |
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the tetracycline that can enter CNS and reach therapeutic levels to treat meningitis
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minocycline
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the only tetracycline safe to use in renal impairment b/c its cleared almost entirely by biliary excretion
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doxy
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excretion of tetracyclines
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biliary secretion
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adverse effects of tetracycline
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Gi disturbance-superinfection
-accumulation in teeth and bone -fatal hepatotoxicity -phototoxicity vestibular probs in minocycline -diabetes insipidus in demeclocycline |
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this drug class chelates Calcium and Mg and thus cannot be administered with antacids if GI distress is experienced b/c it then inhibits absorption of drug
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tetracyclines
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contraindicated in children less than 8
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tetracyclines
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fatty liver deposition leading to fatal hepatotoxicity during pregnancy b/c of accumulation in mitochondria
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tetracycline
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risk of c dif (pseudomemranous colitis) with this drug class
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tetracyclines
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initial tx for c dif
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metronidazole
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1st choice in recurrence of c dif
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vancomycin
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tx of c dif that is icu acquired
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fidaxomicin
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MOA: DNA damage via reductive metabolism
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metronidazole
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MOA: cell wall synthesis elongation step
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vancomycin
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what enzyme do anaerobic and microaerophilic pathogens not rely on
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pyruvate dehydrogenase
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what enzyme do anaerobics use
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PFOR (pyruvate ferrodoxin oxidoreductase complex, which activates metronidazole
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gives metallic taste
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metronidazole
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disulfram like reaction associated with intake of alcohol
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metronidazole
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safer improvement on tetracycline
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tigecycline
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decreased susceptibility to tet A efflux pumps and ribosomal protection
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tigecycline
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tetracycline that is effect against anaerobes
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tigecycline
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bind 50s ribosome
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macrolides and ketolides
clindamycin chloramphenicol linezolid |
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-romycins
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macrolides and ketolides
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use in pts w/ penicillin allergy for treponema pallidium (syphillis)
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erythromycin
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drug of choice for legionnaires
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azithromycin
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least drug interactiosn of macrolides
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azithromycin
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macrolide limited to activity against gram + cocci and treponema
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erythromycin
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macrolide with activity extended to gram -
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clarithromycin
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macrolide with greatest activity against gram neg
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azithromycin
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ketolide tx for multi drug resistant Strep pneumonia
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telithromycin
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major indication for macrolides
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Community acquired pneumonia
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macrolides not active against
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MRSA
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azithromycin dosing vs other macrolides
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once a day, 5 days as effective as 10 day course of other macrolides
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bind 50s and inhibit translocation step of protein synthesis
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macrolides (ECA)
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do macrolides irreversible bind or reversible bind
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irreversible but bacterostatic
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mech of resistant for macrolides
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-methylation of ribosomes (high level of resistance)
-macrolide efflux pumps (medium resistance) |
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bacteria that are intrinsically resistant to macrolides and why
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enterobacteria, pseudomonas, acinetobacter
-b/c they have decreases permeability of outer envelope |
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adverse effects of macrolides and telithromycin
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MACRO, cyp3A interaction, reversible hearing loss
-motility, arrhthymias caused by prolonged QT, cholestatic hepatitis, rash, eosinophilia |
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greatest risk for qt prolongation of macrolides
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e>c>a
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more dangerous macrolide (risk of sudden death)
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erythromycin
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safest macrolides for preggers
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category b, Erythromycin and azithromycin
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macrolides with cyp3a inhibition
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erythromycin and clarithromycin
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lincosamide
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clindamycin
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clindamycin has similar MOA and activity to
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erythromycin
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clindamycin vs erythromycin
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clindamycin primarily used against anaerobes
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main adverse effect of clindamycin
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C dif overgrowth
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wide spectrum, rare clinical use
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chloramphenicol
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clinical use restricted to life threatening infections like meningitis in developing countries
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chloramphenicol
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aplastic anemia
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chloramphenicol
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gray baby syndrome-
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chloramphenicol
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inhibits peptidyl transferase step of protein synthesis
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chloramphenicol
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blocks peptide transfer (transpeptidation)
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clindamycin
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resistance to this drug via acetyltransferase (CAT)- less binding to 50s
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chloramphenicol
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what makes chloramphenicol so toxic
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can enter mitochondria
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clinical use of linezolid
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VRSA and VRE
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is linezolid bacteriostatic or bacteriocidal
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static
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bacteriocidals
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aminoglycosides, fluoroquinolones, SMX-TMP, but not sulfonamides alone
vancomycin, b-lactams |
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interferes with bindng to intiation complex on 50S
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linezolid
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but AT 30, CCEL at 50
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aminoglycosides, tetracyclines
clindamycin, chloramphenicol, erythromycin, linezolid |
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example of resistance mech for b-lactams
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b-lactamases that enxymatically modify drugs
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PBPs affected by what type of mech of resistance
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mutation reducing drug affinity for target
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