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54 Cards in this Set
- Front
- Back
Examples of aminoglycosides
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streptomycin
gentamycin tobramycin amikacin neomycin kanamycin |
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Examples of macrolide AB
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erythromycin
clarithromycin azithromycin |
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Examples of streptogramins
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quinupristin
dalfopristin |
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Examples of tetracyclines
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tetracycline
chlortetracycline oxytetracycline demeclocycline Methacycline Doxycycline minocycline |
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What is the basic mech behind broad spectrum abx
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inhibits bacterial protein synth
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MOA of aminoglycosides
cidal or static? |
Biinds 30s ribosomal subunit, irreversibly interfering with protein synth
cidal (w killing being [] dependent) also has post-abx effect, w antibacterial activity persisting beyond time that measurable amt of drug is present |
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What type of bacteria are aminoglycosides effective against?
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gram - enteric bacteria , esp in bacteremia and sepsis
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What can be combined with aminoglycosides to treat endocarditis? TB?
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vancomycin or penicillin for both
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MOR against aminoglycosides
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inactivation of aminoglycosides by plasmid encodied transferase enzymes
impaired entry of aminoglycoside into cell modification of ribosomal binding site **transferase mediated R is main type** |
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Absorption of aminoglycosidES
distribution |
poor from GI tract, give IM
highly polar that don't enter cells readily, largely excluded from CNS and eye usually only high levels are found in UTI |
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Uses of SM?
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2nd line agent for TB tx, used in combo with other agents to prevent R
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What are tobramycin a nd gentamycin used to treat?
which is cheaper? |
sepsis and pneumonia from gram - bacteria that are R to other drugs
used in combo with B-lactam (penicillin) burns, wounds, skin lesions gentamycin |
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what s amikacin used to treat?
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resistant micro-organisms
it si R to many enzymes that inactivate gentamycin and tobramycin |
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what are neomycin adn kanamycin used to treat?
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only topical (injected in to joints/pleural cavity,) and/or oral use (to cleanse large bowel for elective colorectal surgery)
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Adverse effects of aminoglycosides
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all are nephrotoxic
ototoxicity when used for >5 days --> auditory and vestibular damage (ototoxicity is irreversible) |
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which aminglycosides are the most nephrotoxic?
how is it made worse? is it reversible? |
neomycin
tobramycin gentamycin concurrent use of loop diuretics yes |
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Which aminoglycosides are the most ototoxic?
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for hearing:
neomycin kanamycin amikacin for vestibular: SM gentamycin |
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MOA chloramphenicol
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binds to 50S ribosomal subunit, interferes with protein synth
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spectrum of chloramphenicol?
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aerobic and anaerobic gram +/- bacteria (esp gram -, in bacteremia and sepsis)
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what is chloramphenicol commonly combined with?
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vanco
penicillin (used to treat endocarditis and tb) |
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MOR to chloramphenicol?
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production of chloramphenicol acetyltransferase (plasmid encoded enzzyme that inactivats the drug)
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Pharmacokinetics of chloramphenicol
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rapidly and completely absorbed after oral admin
widely distributed to all tissues and body fluids (incl CNS and CSF) penetrates cell membrane readily |
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How is chloramphenicol cleared primarily from body?
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liver
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Uses of chloramphenicol
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don't use systemically, bad side effecs and widespread R
Rickettsial infections in children <8 yo alt to B-lactam for bacterial meningitis caused by pen-R strianst of pneumococcus and meningococcus eye infectiosn (penetrates ocular tissue and is broad-specrum) |
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Adverse rxns to chloramphenicol
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GI probs (N/V/diarrhea in adults, not kids, candidiasis)
bone marrow probs (aplastic anemia and RBC suppression) toxicity for neonates (lack liver enzymes to detox drug) intearctions with other drugs (inhbiits liver enzymes) |
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what can happen to infants taking chloramphenicol
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gray baby syndrome w vomiting, flaccidity, hypothermia, gray color, shock, colllapse
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what drug interactinos are there w chloramphenicol
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bacteriostatic protein synth inhibitors
antagonizes cidal drugs (like penicillin and aminoglycosides) |
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MOA of macrolides
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bind 50S ribosomal subunit
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spectrum of macrolides
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gram +
strep, staph, pneumococci, corynebacteria |
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MOR of macrolides
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reduced perm of cell membrane or active efflux
production of esterases that hydrolyze macrolides modifications of ribosomal binding sites by chromosomal mutation or methylation |
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Pharmacokinetics of macrolides
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widely distributed, except brain and CSF
traverse placenta and reach fetus not a prob in pts with renal probs |
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What happens to macrolides in stomach
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gets destroyed by acid, so must have enteric coating
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which macrolide has longest t 1/2? how long/
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azithromycin
3 days |
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Clinical uses of macrolides
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corynebacterial infections
resp, neonatal, ocular, and genital chlamydial infections community acquired pneumonia |
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adverse effects to macrolides
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GI (anorexia, N/V/D, stim of gut motility)
liver toxicity --> acute cholestatic hepatitsi (hypersens rxn?) Drug interactiosn |
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which macrolide drugs cause drug interactions? whihc ones don;t?
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erythromycina nd clarithromycin metabolites inhbiit p450 increasesing serum [] of teophylline, oral anticoags, cyclosporine, methyprednisolone
azithromycin doesn't affecct p450 |
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Antimicrobial activity of linezolid?
static or cidal? |
gram + aerobes and anaerobic cocci
gram + rods (corynebacteria and listeria) MT generally static except against streptococci (cidal) |
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MOA linezolid
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inhibits protein synth by preveting formation of ribosome complex that initiates protein synth
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MOR of linezolid
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unique binding site on 23S ribosomal RNA of 50S subunit
so, no x-R with other drug classes R from mutation of linezolid binding site on 23S ribosomal RNA |
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pharmacokinetics of linezolid
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100% bioavailable after oral admin
doesn't affect p450 |
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Clinical uses of linezolid
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VRE
nosocomial pneumoania strep/MRSA skin infections reserved for tx of infections caused by MDR gram + bacteria |
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Adverse rxs to linezolid
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GI, HA, rash
thrombocytopenia (esp if >2wks) neutropenia weak MAOI (watch out w tyramine) peripheral and optic neuropathy |
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What is quniupristin-dalfoprisitn?
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combo of 2 streptogramins
cidal for most organisms gram +, MDR orgs and MRSA |
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R to streptogramins
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modification of ribosomal binding site of quinupristin
inactivation of dalfopristin drug efflux |
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are dose-adjustments needed for streptogramins in pts with renal probs
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no
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adverse rxns to streptogramins
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painat infusion site
arthralgia-myalgia inhibit CYP3A4 |
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MOA of tetracyclines
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binds 30S ribosomal subunit, interferign with protein synth
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spectrum of tetracyclines
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gram +,-
anaerobes rickettsiae chlamydiae mycoplasma protozoa |
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MOR against tetracycline
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decreased intracellular accumulation d/t impaired influx or increased efflux by active transport protein pump
ribosome protection d/t production of proteins that interfere with tetracycline ribosome interactions enzymatic inactivations of tetracyclines |
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which tetracycline has best oral bioavailabity?
what affects oral bio? |
doxy and minocycline
food decreases absorption (Ca, Mg, Fe, Al, dairy, antacids, and high pH) |
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distribution of tetracyclines
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everywhere but CSF
tetra x placenta and enters breast milk |
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which tetracycline is best to use in renal failure
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doxy
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dosing of oral doxy?
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1x day, absorption not affected by food
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adverse rxns to tetracyclines
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GI
binds Ca so affects bone and tooth formation deposited in fetal teeth impar hepatic fxn (esp during preg) RTA, N retention DVT if given IV, IM is painful local irritiation UV sensitization vestibular rxns |