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137 Cards in this Set
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protein synthesis inhibitors
|
aminoglycosides
tetracyclines glycylycycline macrolides lincosamides chloramphenicol streptogramins oxazolidinones mupirocin |
|
protein synthesis inibitors interact w/ -- to inhibit protein synthesis
|
ribosome
|
|
bac cell walls have -- and --- subunits of ribosome
|
30's
50's |
|
mammalian cells have ---- and --- subunits
|
40s
50s |
|
most bacterio----- except aminoglycosides and mupirocin
|
bacteriostatic
|
|
aminoglycosdides bind to both -- and --- subunits
|
30
50 |
|
tetracycline and spectinomycin bind to -- subunits
|
30
|
|
macrolides, chloramphenicol, streptogramins, and lincosamide bind the --subunit
|
50s
|
|
-- prevent formation of the 70s
|
linezolid
|
|
mupirocin binds --- ---
|
transfer RNA
|
|
protein synthesis:
meth --- --- initiates synthesis by binding to p-site |
t-RNA
|
|
protein synthesis:
tRNA binds to the -- site and a peptide bond is formed |
A
|
|
after the tRNA leaves the P site what occurs
|
peptide shifts from A to P site
new t-RNA binds |
|
when the stop codon binds waht occurs
|
peptide released and ribosome dissociates
|
|
amino prevents initiation of --- --- from binding
|
meth-t-RNA
|
|
amino binds to interfere btw -- and -- subunits
|
30
50 |
|
amino distorts ---
|
codons
|
|
amino enchanes early breakdown of --- unit
|
ribosomal
|
|
tetracycline binds 30s subunit to prevent t-RNA from binding to the -- site
|
A
|
|
tetra prevents elongation of ----
|
peptide
|
|
tetra binding reversible/irreversible
|
reversible
when drug gone synthesis resumes |
|
macrolides binds to the 50 subunits to interfere w/ the --- ---
|
initiation complex
|
|
macrolides interfere w/ transfer of :
|
peptide t-RNa complex from site A to P site
|
|
macrolides prevents ---
|
elongation
|
|
ketolides binds to 50's subunits and interferes w/ --- ----
|
initiation complex
|
|
ketolides interferes w/ transfer of ------ complex from site A to P site
|
peptide t-RNA
|
|
ketolides prevents ---
|
elongation
|
|
lincosamide binds to -- subunit
and interferes w/ -- ---- |
50's
initiation complex |
|
lincosamide site very close to -- and ---
|
macrolides
chlorampehnicol |
|
lincosamides prevents ----
|
elongation
|
|
chloramphenicol binds 50s subnits and inhibits bond formation btw -- adn new ----
|
peptide
amino acid |
|
t/f
chlorampehnicol bindind is irreversible |
f
reversible |
|
streptogramins binds to -- subunits
|
50s
|
|
dalfopristin prevents ---- bond formation
|
peptide (inhibits peptidyltranserase, early termination)
|
|
quinupristin inhibits ---- -----
|
t-RNA synthesis
(inhibits elongation, early termination) |
|
linezolid binds specific ---- ribosomal dna on -- subunit
prevents formation of functional --- ribosomal unit |
23s
50s 70s |
|
mupirocin inibits -------
|
isoleucyl-t-RNA synthase
|
|
mupirocin prevents incorporation of --- into proteins
|
isoleucine
|
|
t/f
mupirocin has no x tolerance w/other abx |
t
|
|
ex of amino's
|
amikacin
gentamicin kenamycin neomycin netilmicin tobramycin streptomycin (plague) |
|
amino's used to tx gram -- bacilli, and aerobic/anaerobic bacteria
|
negative
aerobic |
|
amino's are bacteri---
|
bactericidal
|
|
amino is --- dependent killing
|
concentration
|
|
amino are --- in body fluids
|
ionized
|
|
t/f
amino are readily absorbed |
f
(ionized in bodily fluids) |
|
amino eliminated by
|
glomerular filtration
so modify dose w/ kidney fx |
|
amino used in combo in ----- ---- - -
|
serious infections
sepsis pneumonia endocarditis |
|
why combine amino w/ b lactam
|
to increase bacterial uptake
|
|
amino's can accumulate in -- tubule
inhibits ----synthesis |
proximal
prostaglandins |
|
amino damages -- ---cells
|
brush border
|
|
incidence of amino toxicity r/t
|
age
total dose females >males duration of tx |
|
what can increase amino toxicity
|
cisplatin
cyclosporine other nephrotoxins |
|
what can increase ototoxicity w/ amino's
|
cisplatin
|
|
t/f
ototoxicity is not permanent |
f
can be permanent |
|
ototoxicity affects -- and ---
|
auditory
vestibular |
|
ototoxicity occurs due to ---- administration, --- dose
|
prolonged
increase |
|
continued loss of hearing w/ amino w/
|
repeated doses
|
|
what can potentiate ototoxicity
|
ethacryni acid
furosemide cisplatin other ototoxins |
|
3 hypothesis that play in role in amino toxicity
|
ca hypothesis
free radical nmda hypothesis |
|
ca hypothesis:
amino's interfere w/ ca and --polarize/-- polarize |
over/hyper
|
|
free radical hypothesis w/ amino toxicity: interact w/ --- to form ---- and ---- ---- ---
|
Fe
superoxide hydroxyl free radicals |
|
nmda hypothesis of amino tox:
-- causes excitatory |
glutamate
|
|
amino blocsk --- release of ca
|
presynaptic
|
|
amino's ci in
|
myasthenia gravis
|
|
amino enchane --- ---- in sx
|
neuromuscular blockade
|
|
amino resistance due to -- acquired, aminoglycoside --- enzyme
|
plasmid
modifying |
|
amino resisance due to altered -- into bacteria
altered ---- |
transport
ribosome |
|
tetracyclines tx gram ---
anaerobes/aerobes -- --- --- |
gram pos and neg
anaerobes aerobes rikettsia chlamydia lyme's disease |
|
tetrac bacterio---
|
bacteriostatic
|
|
route of tetra
|
oral
parenteral |
|
tetracycline enter bacteria by -- and ---- ---
|
diffusion
active transport (prevent this and u have resistence) |
|
tetracyclines used for
|
acne
|
|
what impairs tetracyc absorption
|
mild
antacids chelate divalent cations (tetra bind to ca) |
|
tetrac
enters the --- crosses ---- found in |
x: CNS
placenta breast milk |
|
tetra is eliminated by
|
glomerular filtration
biliary excretion (some) |
|
doxycycline mainly excreted in ---; some ---
|
feces
renal |
|
toxicity of tetra:
-- disturbances -- sensitivity -- infections effects -- and ------ ----/--- toxicity --- disturbances --- rxns |
GI
photsensitivity super-infections stains bones and teeths renal/hepatic toxicity vestibular disturbances hypersensitivity |
|
resistance to tetra:
-- mediated: addition of active -- transporters |
plasmid
efflux |
|
resistance to tetra:
--- produced protection protein displaces tetrac |
ribosomal
|
|
resistance to tetra:
increased --- activity |
enzymatic
|
|
cross-resistance of tetra depends on mechanism of -----
|
resistnace
|
|
ex of glycylcycline
|
tigecycline
|
|
tigecycline r/t
|
minocycline
|
|
tigecycline route
|
iv
|
|
tigecycline mainly excreted in
|
bile
urine (unchanged) |
|
tigecycline used in complicated --- structure and --- infections
effective in other ---- resistant organisms |
skin
intraabd tetracycyline |
|
tox to tigecycline
|
similar to other tetra's
|
|
macrolides tx gram ---
cocci/bacilli --- ---- |
gram positive
cocci bacilli chylamidia legionella |
|
ex of macrolides
|
erythomycin
clarithomycin azithromycin |
|
clarithromycin has ----
azithromycins has what sturutural feature |
clari: OCH3
Azit: N-CH3 |
|
macrolides inactived by
|
acid. . . enteric coated tabs
|
|
macrolides excreted via
|
biliary
|
|
t/f
marolides x bbb |
f
crosses placenta NOT xBBB |
|
toxicity of macrolides:
--- hepatitis --- rxn -- disturbances -----, -- loss, reversible/irreversible |
cholestatic
sensitivity GI tinnitus hearing reversible |
|
Erythromicin can cuase QT prolongation w/ ---, --------
|
antihistamines
ketoconazole |
|
ketolides interferes w/ transfer of ------ complex from site A to P site
|
peptide t-RNA
|
|
ketolides prevents ---
|
elongation
|
|
lincosamide binds to -- subunit
and interferes w/ -- ---- |
50's
initiation complex |
|
lincosamide site very close to -- and ---
|
macrolides
chlorampehnicol |
|
lincosamides prevents ----
|
elongation
|
|
what macrolides inihbit cyp3A4
|
Eryth
claritho (affects thophylline, warfarin, digoxin) |
|
clarit is used for
|
H pylori
|
|
azith is usedfor
|
h influ
|
|
cwhich macrolides used to tx mycobacterium avium-intracellulare
|
clarithromycin
azithromycin |
|
reisistance of macrolides due to
--- --- out of bacteria decreased binding of ---- increased --- 50s ribosomal --- |
active transport
ribosome metabolism mutations |
|
ex of ketolide
|
telithromycin
|
|
telithromycin is a semi-synthetic derrivated of ---
|
erythromycin
|
|
ketolide similear abx activity to --
|
macrolides
|
|
telithromycin has less --- and ----- mediated resistance
|
metabolic
efflux |
|
telithromycin used for -- --- --
|
community acquired pneumonia
|
|
telithromycin not used for bronchitis and sinusitus due to:
|
hepatic toxicity
|
|
telithromycin causes visual disturbances due to --- ---
|
slow accomadation
|
|
telithromycin can cause --- coliitis
--- prolongation -- inhibitor |
pseudomembranous
Qt cyp3A4 |
|
lincosamides used to tx gram ---
aerobic/anaerobic -- resistant -- and ----- |
gram positive
anaertoci pcn resistant staph and strep |
|
lincosamide doc for
|
lung abscess
anaerobic lung pleural space infection |
|
lincosamides used for --- ---
|
streptococcus pyogenes:
necrotizineg fascilitis. . . inhibits toxin production |
|
lincosamide is highly -- ---
|
protein bound
|
|
toxicity of lincoasamide:
|
diarrhea: c diff. . . pseudomembranous colitis
steven's john's |
|
resistance of lincosamide due to altered ---
|
metabolism
|
|
chloramphenicol bacteriacidal for
|
h influenza
strep penumoniae neisseria miningitidis (bacteriostatic) |
|
what limits the sued of chloramphenicol
|
toxicity
|
|
resistance of chlorampehnicol due to -- encoded acetlytransferase prevents binding to -----
|
plasmid
ribosome |
|
chlorampehnicol causes ---- glucorinidation
|
hepatic . . .gray baby syndrome
|
|
chlorampehnicol x the:
|
cns
breast mild placenta |
|
toxicity of chlorampehnicol:
--- --- suppression altered --- maturation peripheral ------- inhibits --- enzymes -- rxns inhibits --- enzymes |
bone marrow
rbc peripheral micorsomal hypersensitivity cyp |
|
streptogramins is a combo of
|
dalfopristin
quinupristin |
|
resistance of streptogramins due to
altered ---- binding increased ---- |
ribosmal (quinupristin)
metabolism (dalfoprisitin) |
|
streptocgramins used for:
|
vanco reisistant e faecium, not acitve against faecalis
methcililn resisitant s aureus and s pyogenenes |
|
stretogramins route
|
iv infusion
|
|
streptogramins toxicity:
inflammation of --- muscle ---- --/---- interacts w/ cyp --- elevates serum --- |
veins, muscle aches
diarrhea/nausea cyp3A4 transaminase |
|
oxazolidonones used for
|
vanco resistant e faecium
nosocomial pneumonia (mrsa, s aureus, s pneumonia) multi drug resistance |
|
route of oxazolidines
|
oral
iv |
|
toxicity to oxazolidinones
|
nausea
thrombocytopenia itiching nonselective maoi (worry about di) peripheral neuropath |
|
when is mupirocin bacteriostatic
|
at low conc
bacterialcidal at high conc |
|
mupirocin route
|
topical cream or ointment
|
|
mupirocin used for traumatic --- ---- or --- ----
|
traumatic skin lesionns
nasal colonizations w/ meth resistant s aureus |
|
ae of mupirocin
|
skin irritation
sensitization |