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137 Cards in this Set

  • Front
  • Back
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