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87 Cards in this Set
- Front
- Back
where do tetracyclines prevent protein synthesis?
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30S ribosome
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Tigecycline is used for what
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MRSA
and really bad resistant stuff |
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tetracyclines are ___ spectrum
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broad
wide range of aerobic and anaerobic G+ & G- bacteria |
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Chlamydia, Rickettsia, mycoplasma p. can be readily treated with this broad spectrum drug
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Tetracycline
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2 most widely prescribed tetracyclines?
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Doxycycline & minocycline
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if a pt has poor renal function, what would be your tetracycline of choice?
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Doxycycline
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what tetracycline can enter the CSF?
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minocycline
for meningococcal carrier state |
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DOC or alternative for
Mycoplasma p |
Tetracyclines
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DOC or alternative for chlamydia
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Tetracyclines
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DOC or alternative for Rickettsiae
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Tetracyclines
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DOC or alternative for Lyme Disease
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Tetracyclines
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DOC or alternative for Anthrax
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Tetracyclines
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Tetracyclines are bacterio____
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STATIC
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tetracycline MOA
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Tetracyclines bind reversibly on 30S to interfere with charged tRNA and keep from binding to acceptor site
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what is the resistance to tetracycline at the ribosomal level?
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bug produces a protein to protect itself. this protein competes with the drug for binding and kick it off
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what are the 2 mechanisms of resistance to teteracyclines
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1. efflux pumps
2. ribosome protection proteins that interfere with tetracycline binding they dislodge drug from the ribosome & increase the apparent kd of drug binding to the ribosome |
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what are the bacteriocidals and statics?
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Bacteriocidals: Very Finely Proficient At Cell Murder- Vancomycin, Fluoroquinolones, Penecillins, Aminoglycosides, Cephalosporins, Metronidazole
Bacteriostatics: We're ECSTaTiC about bacteriostatics!- Erythromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Chloramphenicol |
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what drug chelates and messes with absorption of certain vitamins and the drug itself
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Tetracyclines
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pt says their stomach gets upset when they take this drug. So they want to take milk, or antacids with it. You know that this drug forms stable chelates, which messes with absorption. What is the drug?
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Tetracyclines
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pt has taken tetracycline since they were 3. what might this do to the mouth
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staining of mandiublar teeth
Chelates with calcium concentrates in bone & teeth |
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what tetracyclines are less dependent on kidneys for elimination?
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Doxycycline and minocycline are less dependent on kidneys for elimination
no dosage adjustment with compromised renal function excreted in bile |
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MRSA, Staph epidermis, penicillin-resistant streptococcus pneumoniae (PRSP), vancomycin-resistant enterococcus (VRE)... consider using
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Tigecycline
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how is tigecycline administered?
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IV
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why is tigecycline not useful for UTIs?
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biliary excretion!!
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tetracyclines should not be used in what populations due to tooth affects?
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Children (Readily bind in newly formed bone or teeth in young children)
preggo women, it can cross the placenta |
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just note that tetracyclines can cause
Liver Toxicity Rare but can be fatal Occurs more commonly with tetracycline and minocycline and less often with doxycycline Local Tissue Toxicity Directly irritating to tissues … IV: thrombophlebitis (frequent w/ prolonged use) IM: painful (avoid route) |
had to say this...it was just a rando slide that I couldn't think of a question
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pt comes in and has very bad sunburn from limited exposure to the sun..what caused this
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tetracyclines
photosensitive |
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Pt grabs an old bottle of tetracycline. They feel like they have an infection so they start popping it even though the expiration date is well past due. What can this cause?
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Fanconi syndrome
kidney tox! |
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Chloramphenicol acts where?
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Protein Synthesis Inhibitors acting at the 50S ribosome
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this is a drug of last resort, for life-threatening infections.
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Chloramphenicol
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what is the biggest tox of Chloramphenicol?
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bone marrow suppression
Anemia, leukopenia, thrombocytopenia Dose-dependent Reversible |
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what is an idiosyncratic response?
what drug has a tox that can act like this? |
just pops up out of nowhere
Chloramphenicol (remember it can wipe out bone marrow, so it could kill someone) |
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newborn baby was given a drug that causes Gray color, shock, hypothermia, vomiting, flaccidity
Can be fatal within 2 days of initial symptoms 40% mortality rate what was the drug? |
Chloramphenicol
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Erythromycin
Clarithromycin Azithromycin are what kind of drugs? |
macrolides
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what is a good substitute for penicillins?
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macrolides
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DOC for Campylobacter jejuni
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Macrolides
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DOC for H pylori
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Macrolides
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DOC for Shigella spp.
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Macrolides
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Macrolides are a go to for what groups (alt to tetra)
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children & pregnant females (alternative to tetracyclines)
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what drug class is best used for URIs
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macrolides
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DOC for Mycoplasma pneumoniae
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Macrolides
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DOC for Chlamydia
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Macrolides
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DOC for Bordetella p. (Whooping cough)
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Macrolides
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DOC for Campylobacter (enteritis)
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Macrolides
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Macrolides are bacterio____
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static
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MOA for Macrolides
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reversibly binds 50 ribosome
inhibits peptide chain elongation inhibits translocation of peptidyl tRNA from A to P site |
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2 resistance against Macrolides
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efflux pump
ribosome modification |
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what is the ribosome modification in macrolides that provide resistance?
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Methylation alters the macrolide binding site on bacterial ribosome
(note this is different than the tetracyclines!) |
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erythromycin is less ____ than the newer macrolides?
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acid-stable
aka it has worse oral absorption |
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this marcolide is taken once a day and has a long half-life. good for pt compliance
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Azithromycin
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macrolides can inhibit what?
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CYP3A4
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what GI effects do macrolides have?
** |
Directly stimulates GI motility
can cause anorexia, NVD, epigastric distress |
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number one reason for stopping erythromycin?
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Directly stimulates GI motility-->epigastric distress
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Cholestatic hepatitis can be a side effect of?
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erythromycin
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Clindamycin acts where
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Protein Synthesis Inhibitors acting at the 50S ribosome
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Clindamycin is bacterio_____
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static
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spectrum of use for Clindamycin
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Treatment of anaerobic and streptococcal & staphylococcal infections (skin/soft tissue)
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DOC for C. perfringens
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Clindamycin
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primary resistance to clindamycin?
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Alteration of ribosomal binding site
primarily by methylation (like the macrolides) Cross resistance may be seen with erythromycin |
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what drug can penetrate well into bones?
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Clindamycin
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what drug can be actively transported into polymorphonuclear leukocytes and macrophages?
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Clindamycin
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diarrhea and pseudomembranous colitis can be adverse effects of?
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Clindamycin
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what drug is most likely to cause pseudomembranous colitis (not based on % of time the drug is used, just by how it works)
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Clindamycin
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where do quinupristin + dalfopristin
work? |
Protein Synthesis Inhibitors acting at the 50S ribosome
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effective against G+ bacteria
staphylococci resistant to Methicillin (MRSA) (alt) Quinolones Vancomycin you would use? |
quinupristin + dalfopristin
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DOC for Vancomycin-resistant Enterococcus faecium (VRE)
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quinupristin + dalfopristin
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principle use of quinupristin + dalfopristin?
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drug resistant G+ cocci infections
bacteremia and soft tissue infections |
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quinupristin + dalfopristin are bacteri_____
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cidal
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MOA for quinupristin + dalfopristin
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Quinupristin:
binds at same site as macrolides (prevent peptide chain elongation, can't move A to P) Dalfopristin directly interferes with polypeptide chain formation binds near quinupristin; synergistically enhances binding of quinupristin |
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resistance to dalfopristin?
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Enzymatic inactivation
Efflux pump |
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resistance to quinupristin??
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Binding site modification by methylase
Enzymatic inactivation |
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Quinupristin & dalfopristin do what to P450 enzymes?
** |
Potent CYP3A4 inhibitor
Appropriate caution and monitoring recommended for drugs in which the therapeutic index is narrow |
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what can cause severe arthralgias and myalgias?
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Quinupristin & dalfopristin
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Linezolid works where
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Protein Synthesis Inhibitors acting at the 50S ribosome
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spectrum of Linezolid?
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Similar to quinupristin & dalfopristin (G+ bacteria) plus E. faecalis
Should be reserved for MDR G+ bacteria |
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DOC for pen resistant strep pneumo, and MRSA?
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Linezolid
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DOC for enterococcus faecium AND faecalis
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Linezolid
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MOA for Linezolid
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Binds to 50S to block formation of initiation complex
Mostly ‘static’ (cidal for streptococci) |
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resistance to Linezolid
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Mutation of rRNA binding site
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you should avoid tyramine rich food with use of what?
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Linezolid
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this drug should be avoided with use of adrenergic or serotonergic drugs (SSRIs)
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Linezolid
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VRE, MRSA, serious G+... use?
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Daptomycin
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MOA for Daptomycin
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causes loss of gradient of the ions needed for DNA and RNA for protein synthesis
pokes holes in the membrane |
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Daptomycin is bacteri_____
time or conc depend? |
cidal
conc dependet |
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clearance of daptomycin?
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renal
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one thing daptomycin doesn't really work for?
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pneumonia
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this drug can cause Skeletal muscle damage (myopathy)
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Daptomycin
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