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110 Cards in this Set
- Front
- Back
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the 4 types of beta-lactams
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-penicillins
-cephalosporins -aztreonam -carbapenems |
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MOA of penicillin
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-bind to penicillin binding proteins and inhibit cell wall synth
-activate endogenous autolytic system of bact.-->cell lysis and death -bactericidal and time-dependent killing |
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MOR to penicillin
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-inactivation by b-lactamase enzymes
-alteration of PBP -decreased cell wall permeability/no porin channels |
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structure of penicillins
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house with a garage
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classification of penicillins
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-Natural
-Penicillinase-Resistant -AMINOpenicillins -UReidopenicillins -Beta-lactam/BLase inhibitors -Carboxypenicillins? |
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penicillins have _____ tissue penetration
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good; except eye, prostate and CNS (better w/ inflamed meninges)
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oral penicillin agents are ____ by gastric acid
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destroyed
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food ____ absorption of penicillins
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delays
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the most acid stable penicillin is... and the other two are
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amoxicillin, dicloxacillin and ampicillin
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benzathine is used to treat...and levels are ____ MIC and last for ___
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syphillis; below; weeks
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procaine is used to treat...and levels are... and last for ...
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neurosyphillis; high; 12-24 hrs.
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protein binding of penicillin is ....
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widely variable between agents 15-97%
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metabolism of penicillins is....
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minimal to none
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penicillin is eliminated by...except for ... and ... which are elimnated by..
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kidney; nafcillin and oxcillin; liver
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does pen. require renal dose adjusting?
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YES!
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pen. half lives are ... and require...daily dosing
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short; multiple
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name all the natural penicillins
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G - IV, benzathine, procain
VK (oral) |
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spectrum of natural penicillins
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G+ - strep (B&G always susc.), staph (mostly resistant now), enterococci, l. monocytogenes
G- - n. meningitides Anaerobes - fair (not B. fragilis) other - trep. pallidum (syphillis) |
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name the penicillinase-resistant pens.
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oxacillin
nafcillin dicloxacillin (PO) cloxacillin (PO) |
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what is the drug of choice for staph. aureus that is not MRSA
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oxacillin/nafcillin
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name the aminopenicillins
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-ampicillin (PO and IV)
-amoxicillin (PO) |
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what is the most preferred aminopenicillin and why?
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amoxicillin b/c of better bioavailability
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name the carboxypenicillins
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ticarcillin
carbenicillin (PO) |
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what was the first class of drugs to treat pseudomonas aur.?
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carboxypenicillins
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name the ureidopenicillins
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-piperacillin
-mezlocillin (not available?) |
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are there any ureidopenicillins available orally?
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nope
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T/F ureidopenicillins are not effective against pseudomonas?
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False, they are very effective
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name the beta-lactam/Blactamase inhibitors
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-ampicillin/sulbactam
-ticarcillin/clavulanate -piperacillin/tazobactam -amoxicillin/clavulanate (PO) |
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what coverage does BL/BLase inhibitors have that other BLs don't?
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anaerobes!
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what is the most dangerous hypersensitivity rxn associated w/ BLs?
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immediate (anaphylaxis) - IgE mediated
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what BLs can cause an hepatic ADRs
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ox and naf (metabolized by liver)
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serum sickness is mediated by ____ and has what symptoms and when is the onset
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IgG; rash, fever, leukopenia, arthralgia, pupura, lymphadenopathy; 1-2 weeks
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the delayed IgG mediated hypersensitivity is seen with _____ and has what symtpoms/onset
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beta-lactams; maculopapular rash; after several days of therapy
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what beta-lactam can cause electrolyte abnormalities?
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carboxypenicillins
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the GI ADRs seen in beta-lactams could be caused by a ____ infxn
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C. diff
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what BL is prone to causing diarrhea as an ADR
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clavulanate from augmentin (ticarcillin and clavulanate)
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Drug interactions of BLs
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-Oral contraceptives
-warfarin -probenicid |
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structure of cephalosporins
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'house with a basement'
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cephalosporins do not cover...
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-MRSA
-Enterococci |
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t/f oral absorption is good for cephs
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t
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what gens of ceph penetrate CSF
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3 and 4
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the distribution of ceph is similar to ...
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pen
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what cephs are partially metabolized
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-ceftriaxone
-cefoperazone |
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1st gen cephs
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-cefazolin
-cephalexin (po versrion of cefazolin) -cefadroxil -cefeclor |
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half lives of cephs are generally ____ than PCN an require ____ frequent dosing
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longer;
less |
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most cephs are eliminated by the ____ and require ____
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kidneys
renal dose adjustment |
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what drugs are cephamycins, what group are they in, what extra coverage do they have and what are they commonly used for
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-cefotetan and cefoxitin
-2nd gen ceph -G- anaerobes -GI surgery propylaxis |
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name the 2nd gen cephs
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-cefuroxime
-cefotetan -cefoxitin |
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what extra coverage to 2nd gen cephs have"?
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h. influenzae and m. catarrhalis
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name the 3rd gen cephs
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-ceftriaxone
-cefotaxime -ceftazidime |
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name the 4th gen ceph
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cefepime
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what special coverage do ceftriaxone and cofotaxime have?
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PCN resistant pneumococci
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what extra coverage do the 3rd gen cephs have
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n. gonorrheae and enterobacteriaceae and pcn resistant pneumococci
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what is special about ceftazidime
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pseudomonal coverage
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what does cefepime cover
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everything but anaerobes
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hypersensitivities of cephs
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cross react w/ pcn -- serious IgE rxns
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ADRs of ceph
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hypoprothrombinemia and bleeding
-agents with MTT inhibit vit. K clotting factors -->disulfram (antabuse) rxns -other rxns like pcn |
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t/f cephs have few drug interactions
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t
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name the carbapenems
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-imipenem/cilastatin
-meropenem -ertapenem |
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what 3rd gen cef has p. aureginosa coverage?
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ceftazidime
|
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spectrum of 3rd gen ceph
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G+ staph, strep (*esp pcn resistant pneumococci***)
G- same as 2nd gen + neis. gonorrhea + enterobactericeae Ana - None |
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name the 4th gen cef
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cefepime
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spectrum of cefepime
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G+ cocci
G- PEcK + Hi + McNgEb ana - none |
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hypersensitivity of cefs
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x-reactive w/ pcn - create serious IgE rxns in 7%
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ADRs of cefs
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-Hypoprothrombinemia/Bleeding from agents w/ MTT side chain
-disulfram like rxns |
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t/f cefs have lots of drug interactions
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false
|
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name the carbapenems
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-imipenem/cilastatin
-meropenem -ertapenem |
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wtf is cilastatin
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-not a beta-lactamase inhibitor and has no antimicro action
-prevents degradation of imipenem in brush border of kidney |
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carbapenem dist. and absorption
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-poor oral absorption
-good distribution |
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where is imipenem metabolized
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by dihydropeptidase in brush border of kidney
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carbs are eliminated how?
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renally
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carbs have ____ spectrum
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broad
|
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carbs cover MRSA t/f
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false
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carb spectrum
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imi-/meropenem - very good G+, excellent G-, Excellent ana
erta- same but no pseudomonas or enterococcus |
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carb. hypersensitivity
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x-react with pcn
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ADRs of carb.
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-seizures (renally dose adjust)
-hypersensitivity |
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name the monobactam
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aztreonam
|
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spectrum of aztreonam
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Gram - ONLY!!
|
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structure of aztreonam
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garage w/ no house
|
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t/f aztreonam has x-reactivity w/ pcn allergies
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false - aztreonam has a different structure than pcn
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t/f aztreonam distributes into eyes/prostate/CNS
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false but has otherwise good distribution
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the activity of sulfonamide is due to it's _____ ring in it's structure
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benzene
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folic acid is necessary for making _____
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thymidine, purines and AAs
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where do bact. get their folic acid derivatives and where do we get them from
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bact. must synthesize them
we get them from our diet |
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what does PABA stand for
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para-aminobenzoic acid
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what is the activity of sulfonamide drugs linked to?
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the benzene ring
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sulfa drugs are bacterio____
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static
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t/f sulfa drugs affect mammalian cells
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f - we get folate from our diets
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t/f sulfa drugs are good for treating serious infxns such as bacteremias
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false, they are bacteriostatic
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MOA for sulfonamide
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competitive inhibitor of dihydropteroate synthetase
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MOA for trimethoprim
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competitive inhibitor of dihydrofolate reductase (takes dihydrofolic acid to tetrahydrofolic acid)
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Mech of resistance to sulfa
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-overproduction of PABA
-use of alternate metabolic pathway (ie. exogenous FA intake -mutations of dihydropteroate synthase ->poor affinity for sulfa -losss of cell wall permeability |
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sulfasalazine is ____ absorbed and therefore used to treat...
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poorly
ulcerative colitis/Crohn's DZ |
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sulfamethoxazole is used for...
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UTI
nocardiosis toxoplasmosis malaria |
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what is co-trimoxazole
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trimethoprim-sulfamethoxazole
Bactrim Septra TMP-SMX (TMP-SMZ) |
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why is tmp paired with smx?
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synergism baby
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what is the most effective ratio of SMX to TMP
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20 parts SMX to 1 part TMP
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TQ*** what is the dosing of SMP-TMX based on?
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the TMP component!!!
|
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tmp-smx is ____ absorbed
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well
|
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tmp is ____ lipid soluble than smx and has a ____Vd
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more
larger |
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t/f tmp-smx distribute well into tissues including lung, CSF, urine
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t
|
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tmp is ___metabolized and is ____ excreted in urine and _____ renal dose adjustment
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not
totally requires |
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TQ**** t/f TMP-smx does not require renal dose adjustment
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FFFFF
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TQ**** T/F tmp-smx should be used to treat serious infxns such as bacteremias
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F
|
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smx is _____ metabolized and ____% is excreted unchanged in urine
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acetylated
30 |
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1/2 life of smx/tmp
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8-10 hours
|
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spectrum of tmp/smx
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G+
staph (sometimes MRSA) strep A,B,C and pneumonia (highly resistant L. monocytogenes (2nd DOC) G- Hi, m. catarrhalis, enterobactericeae (resist.) Misc. -pneumocystis carinii -nocardia -GI pathogens (salmonella, shigella, v. cholera) |
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ADRs of tmp/smx
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-hypersens.
-crytalluria ->stones -hematologic -G6PD deficiency*** -->hemolytic anemia -bone marrow suppression -hyperkalemia -NVD |
|
what ADRs are specific to tmp/smx
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-hyperkalemia from tmp blocking K+ from being secreted
-NVD from large doses |
|
drug intrxns of tmp-smx
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-WARFARIN****TQ*** inc. INR and inc. risk of bleeding
-displace highly protein bound drugs phenytoin - seizures gyburide - oral hypoglycemic -kernicterus in preggos -> displaces bilirubin from albumin ->newborn encephalopathy |