Term
what are the four steps in protein synthesis? |
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Definition
intiation
aa incorportation
peptide bond formation
translocation |
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Term
at which step of protein syn do each of the drugs act? |
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Definition
aminoglycosides act at the initiation step
tetracyclines act at the amino acid incorporation step
chloramphenical block peptide bond formation
macrolides and clindamycin inhibit translocation step |
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Term
how do aminoglycosides work? |
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Definition
they bind the 30s and cause misreading of bacterial DNA -> bactericidal
block the formation of mRNA
they ar etaken into the cells via and O2-dependent mech, so can't use w/ anaerobes |
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Term
what are the major aminoglycosides? |
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Definition
gentamicin, streptomicin, amikacin, neomycin, tobramycin |
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Term
the -glyco in aminoglycosides tells you what about these drugs? |
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Definition
these are like sugars, so they are polar.
they are not absorbed orally, they are excreted by the kidneys.
since they are excreted by the kidneys, you need to adjust the dose in renal failure. |
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Term
what are some of the major side effects of the aminoglycosides. |
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Definition
nephrotoxicity (6-7% incidence)
ototoxicity (2% incidence)
weird side effet = neuromuscular blockade, so don't give with muscle relaxants
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Term
aminoglycosides are useful against which bacteria? |
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Definition
gram - rods
streptomycin used in TB, DOC for bubonic plague and tularemia |
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Term
what kind of bacteria do you not want to tx with aminoglycosides? |
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Definition
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Term
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Definition
they inhibit amino-acid incorporation by blocking the attachment of tRNA to the acceptor (A) site.
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Term
some examples of tetracyclines include: |
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Definition
doxycycline, minocycline, demeclocycline, tetracycline |
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Term
are tetracyclines bactericidal? |
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Definition
no, are bacteriostatic.
ar ebroad spectrum antibiotics that can be used against chlamydia, mycoplasma, h pylori, rickettsia, borrelia, brucella, and vibrio |
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Term
tell me about doxycycline. |
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Definition
it is lipid soluble and more effective than tetracycline. unlike the other tetra's is metabolize din liver (lipid sol)
useful for rickettsia and borrelia (DOC)
concentrates in prostate, so good for prostatitis (gonorrhea or chlamydia) |
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Term
what are some of the major side effects of the tetracyclines? |
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Definition
tooth enamel dysplasia
decreased bone growth in kids
phototoxicity (esp doxy)
NVD
superinfections -> candidiasis or colitis
vestibular dys w minocycline
contraindicated in pregnancy and children |
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Term
most of the tetracyclines are eleminated by the... |
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Definition
kidneys!
except doxycycline, which is lipid sol and eliminated by the liver |
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Term
when do you need to adjust the dose of tetracyclines? |
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Definition
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Term
since tetracyclines are known to interact with tooth enamel and bone growth, it makes sense that they interact with divalent cations (esp Ca2+).
Knowing this, what would you want to avoid doing when you take these? |
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Definition
eating, esp anything with lots of Ca2+, or taking antacids.
these drugs make pt's feel ill, so the tendency is to eat something with them...but this will decrease the absorption |
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Term
minocycline concentrates where in the body? |
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Definition
in the saliva and tears. can be used to treat the meningococcal carrier state |
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Term
which step in proteins synthesis does chloramphenicol inhibit? |
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Definition
the peptide bond formation step by inhibiting the activity of peptidyltransferase
is bacteriostatic |
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Term
the -phen in chloramphenicol indicates what? |
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Definition
that the drug is lipid soluble, crosses BBB, and is met by the liver.
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Term
chloramphenicol has what spectrum of activity? |
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Definition
wide-spectrum
used as backup drug mostly
do get into the CNS, so can be used for sepsis and meningitis |
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Term
some of the major side effects of chloramphenicol are? |
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Definition
gray baby syndrome: babies have less glucuronosyl transferase, so the drug can saturate this sys -> displacement of bilirubin and kernicterus in infants.
dose-dependent bone marrow suppression common |
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Term
macrolides act on which step of proteins synthesis? |
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Definition
the translocation step.
they inhibit the translocation of tRNA form A site to the P site
are bacteriostatic |
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Term
give example sof macrolizes. |
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Definition
erythromycin, azithromycin, clarithromycin |
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Term
erythromycin is effective against which organisms? |
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Definition
gram + cocci
aypical organims (chlamydia, mycoplasma, and ureaplasma)
Legionella pneumophila
camplylobacter jejuni
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Term
for erythromycin, think of... |
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Definition
Gram P, soldier that died of atypical pneumonia (mycoplasma), kidney stones and chlamydia, all contracted from the camps |
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Term
Azithromycin is more effective against which types of infections? |
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Definition
respiratory infections
Azithromycin Air |
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Term
azithromycin often used for what? |
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Definition
mycobacterium avium-intracellulare in HIV pts |
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Term
since azithromycin is effective in the lungs, a wet environment, kind of makes sense that it is excreted by the... |
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Definition
kidneys, v the rest of the macrolides, which are metabolized by the liver and excreted in bile.
these also inhibit cytochrome P450's
(azithro does not)
and can cross the placenta (not safe in pregnancy)
azithro doesn't and so is safer in pregnancy |
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Term
what are the majore side effects associated with macrolides? |
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Definition
directly stimulate motilin receptors -> NVD
(used to prevent gut stasis after surgery)
cause reversible deafness at high doses
erythromycin can cause jaundice and cholestasis |
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Term
community acquired atypical pneumonia often caused by what and treated with what? |
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Definition
mycoplasma and chalmydia, treated with macrolides |
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Term
clindamycin acts at which step in protein synthesis? |
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Definition
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Term
clindamycin has the same MOA as which class? |
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Definition
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Term
clindamycin often used for what kind of infection? |
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Definition
osteomyelitis caused by G+ cocci (s aureus)
"clings to bones) |
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Term
osteomyelitis is often caused by which organisms according to poulation? |
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Definition
in healthy people, s aureus
iv drug users and diabetics, p aeruginosa
sickle cell patients, salmonella
clindamycin not useful for last 2, would use quinolones |
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