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168 Cards in this Set

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Name the antibiotics that target cell wall synthesis?
cycloserine
vancomycin
bacitracin
fosfomycin
penicillins
cephalosporins
monobactems
carbapenems
Name the antibiotics that target folic acid metabolism.
trimethoprim (DHF A to THF A)
sulfonamide (PABA to DHF A)
Name antibiotics that target the cell membrane.
polymyxins
Name the antiobiotics that target DNA replication/ DNA gyrase.
nalidixic acid
quinolones
Name the antibiotics that target the DNA-dependent RNA polymerase.
rifampin
Name the antiobiotics that target the 50s ribosome of protein synthesis.
erythromycin
chloramphenicol
clindamycin
Name the antibiotics that target the 30s ribosome of protein synthesis.
tetracycline
spectinomycin
streptomycin
gentamicin
tobramycin
amikacin
Name the mold that produces penicillin.
penicillium chrysogenum
Name the bacteria that produces vancomycin.
amycolatopsis orientalis, from soil in Borneo
Name the bacteria that produces tetracycline antibiotics.
streptomyces aurefaciens
Name the three types of antimicrobial therapy.
empiric
specific
prophylactic
What is the MIC?
mininum inhibitory concentration- lowest concentration required to prevent visible growth
What is the AUC/ MIC ratio?
amount of time that the area under the curve (AUC) of the antibiotic remains above the MIC- will the antibiotic be effective against a given pathogen
What is the MBC?
minimum bactericidal concentration, lowest conc required to sterilize or kill 99.9% of bacterial count
What is bacteriostatic?
drugs that reversibly impair replicating ability- no growth
requires innate immune system to eradicate org.s
What is bactericidal?
drugs that irreversibly destroy the ability of a microorg to replicate, kill bacteria w/o outside assistance
What is PAE?
postantibiotic effect- persistant effect of antimicrobial growth after exposure
What is selective toxicity?
inhibition or destruction of infecting organism w/o damage to host cells
What are the two main ways antibiotics work?
concentration-dependent
concentration-independent (aka time dependent)
What is the mechanism of action of beta lactams?
irreversibly bind to penicillin-binding proteins (PBPs), inactivating an autolytic enzyme in cell wall
What is the end result of beta lactam binding to PBPs?
rupture of peptidoglycan framework
osmotic rupture
cell death
What is the key component for beta-lactam acitivty?
the beta lactam ring
What are the resistance issues to beta lactams?
beta lactamases
alterations in PBP
efflux pumps
porin channels
beta-lactams
bacteriocidal
time dependent
what are beta-lactamases?
enzymes produced by bacteria to destroy beta-lactam ring
How does porin channel alteration affect beta lactam effectiveness?
entry sites fo antibiotics
alterations reduce ability to enter
Name the categories of penicillins.
penicillin
aminopenicillin
penicillinase resistan
aminopcn w/ beta-lactamase inhibitor
extended spetrum
Name the aminopcns.
ampicillin
amoxicillin
Name the penicillinase resistant pcns.
dicloxacillin
oxacillin
nafcillin
methicillin
Name the aminopcns w/ beta-lactamase inhibitor.
ampicillin/ sulbactam
amoxicillin/ clavulanic acid
Name the extended-spectrum pcns.
piperacillin/ tazobactam
icarcillin/ clavulanate
What is the spectrum of use for penicilin G, VK?
very narrow
some gram (+)
*drug of choice for GAS pharyngitis
What is the spectrum of use for aminopcns?
narrow, improved gram (-) coverage relative to pcns
What is the spectrum of use for penicillinase resistant pcns?
gram (+) coverage
*drug of choice for MRSA
What is the spectrum of use of aminopcns w/ beta-lactamase inhibitors?
inc gram (-) coverage, good anaerobe coverage
What type of drug are cephalosporins?
beta-lactams
same mechanism
What is the difference btwn cephalosporins and other beta-lactams?
divided into generations, inc gram (-) coverage w/ each generation
more stable around beta-lactamases
Name the first generation cephalosporins.
cefazolin
cephalexin
What is the spectrum of use of first generation cephalosporins?
great gram (+), esp MRSA
some gram (-)
Name the respiratory second generation cephalosporins.
cefaclor
cefdinir
cefuroxime
What is the spectrum of use of respiratory second generation cephalosporins?
good gram (+)
expanded gram (-)
no anaerobes
Name the abdominal second generation cephalosporins.
cefotetan
cefoxitin
What is the spectrum of use of abdominal second generation cephalosporins?
anaerobes, abd surgery prophylaxis
Name the third generation cephalosporins.
cefixime
cefotaxime
ceftriaxone
ceftazidime
What is the spectrum of use of cefixime and cefotaxime? Difference?
less gram (+)
extended gram (-)
poor anaerobe
cefotaxime is for peds
What is the spectrum of use of ceftriaxone?
good strep coverage
extended gram (-)
What is the spectrum of use of ceftazidime?
only 3rd gen w/ pseudomanas coverage
Name the fourth generation cephalosporins.
cefepime
loracarbef
What is the spectrum of use of cefepime?
broadest spectrum
good pseudomonas coverage
What is the spectrum of use of loracarbef?
sim to 2nd gen respiratory agents
Name a monobactam antibiotic.
aztreonam
What type of drug is aztreonam?
beta-lactam but can be used in pcn/ cephalosprin allergy pts
What is the spectrum of use of aztreonam?
gram (-) only
including pseudomonas
What are carbapenems?
broadest spectrum in beta-lactam class
Name the carbapenems?
ertapenem
imipenem-cilastaten
meropenem
doripenem
What is the spectrum of use of ceftriaxone?
good strep coverage
extended gram (-)
What is the spectrum of use of ceftazidime?
only 3rd gen w/ pseudomanas coverage
Name the fourth generation cephalosporins.
cefepime
loracarbef
What is the spectrum of use of cefepime?
broadest spectrum
good pseudomonas coverage
What is the spectrum of use of loracarbef?
sim to 2nd gen respiratory agents
Name a monobactam antibiotic.
aztreonam
What type of drug is aztreonam?
beta-lactam but can be used in pcn/ cephalosprin allergy pts
What is the spectrum of use of aztreonam?
gram (-) only
including pseudomonas
What are carbapenems?
broadest spectrum in beta-lactam class
Name the carbapenems?
ertapenem
imipenem-cilastaten
meropenem
doripenem
What is the spectrum of use of ceftriaxone?
good strep coverage
extended gram (-)
What is the spectrum of use of ceftazidime?
only 3rd gen w/ pseudomanas coverage
Name the fourth generation cephalosporins.
cefepime
loracarbef
What is the spectrum of use of cefepime?
broadest spectrum
good pseudomonas coverage
What is the spectrum of use of loracarbef?
sim to 2nd gen respiratory agents
Name a monobactam antibiotic.
aztreonam
What type of drug is aztreonam?
beta-lactam but can be used in pcn/ cephalosprin allergy pts
What is the spectrum of use of aztreonam?
gram (-) only
including pseudomonas
What are carbapenems?
broadest spectrum in beta-lactam class
Name the carbapenems?
ertapenem
imipenem-cilastaten
meropenem
doripenem
What is the spectrum of use of ertapenem?
no coverage of pseudomonas, acinetobacter or enterococcus
Wht is the spectrum of use of imipenem-cilastaten, meropenem, and doripenem?
very broad, gram (+) and (-)
covers pseudomonas
dori is most potent against pseudomonas
What is the mechanism of action of vancomycin?
interferes w/ cell wall synthesis by inhibiting transglycosylase, preventing elongation & cross-linking of peptidoglycan
What is Red-Man's Syndrome?
administering vanc too quickly, causing a histamine-mediated rxn
What are the best indictor of vancomycin monitoring?
troughs
What is the limitation of oral vancomycin? IV?
oral- not systemically absorbed, only for C. diff
IV- only for systemic, not for C. diff
What is daptomycin?
lipopeptide antibiotic
What is the spectrum of use of daptomycin?
gram (+) skin/soft tissue, abd infections, and endocarditis
Why can't daptomycin be used to treat pneumonia?
surfactant inactivates
What is the mechanism of action of daptomycin?
binds to bacterial membranes, causing rapid depol and interuption of cell wall synthesis
How is daptomycin dosed?
weight based
renally adjusted
Name the topical polypeptide antibiotics.
polymyxins
bacitracin
mupirocin
chlorhexidine
What is the spectrum of use of polymyxins?
topically for gram (+) bacillilary infections
What is the mechanism of action of polymyxins?
attach to bacterial cell membranes rich in phosphatidylethanolamine and disrupt osmotic properties & transport mechanisms
What inhibits the action of polymyxins?
cations
What is the spectrum of use of bacitracin?
gram (+) cocci and bacilli
generally topical
What is the mechanism of action of bacitracin?
inhibits biosynthesis of bacterial cell wall by altering membrane permiability and preventing formation of peptidoglycan chains
What is the systemic toxicity of bacitracin?
nephrotoxic- causes proteinuria, hematuria, and nitrogen retention
What is the spectrum of action of mupirocin?
greater gram (+) coverage
skin infection d/t staph aureus & strep pyogenes
MRSA decontam
What is the mechanism of action of mupirocin?
blocks protein synthesis by reversibly & specifically binding isoleucyl transfer-RNA synthetase
What are the uses of chlorhexidine?
oral rinse
prevention of vent assoc pneumonia
skin sterilization
What is the mechanism of action of chlorhexidine?
cation
bind to bacterial wall altering osmotic equilibrium, causing lysis & death
Name the anti-folate drugs.
sulfonamids
trimethoprim
What is the spectrum of use of sulfonamides?
gram (+) and some (-)
What is the mechanism of action of sulfonamides?
inhibits dihydropteroate synthetase (PABA to DHF A)
What are the mechanisms of bacterial resistance to sulfonamides?
dec permiability to drug
inc PBA production
altered dihydropteroate synthetase
What are the pharmokinetics of sulfonamides?
penetrate CNS
metabolized by acetylation
metabolites have toxicity potential
renal excretion
variable oral absorption
What are the potential toxicities of sulfonamides?
renal
hypersensitivity
hematopoietic problemes
prenatal (kernicterus)
What are the clinical uses of sulfonamides?
UTI
otitis media
pneumocystitis carinii
nocardiosis
toxoplasmosis
prophylaxix
What is the spectrum of use of trimethoprim?
most aerobic gram (+) and (-);
adjunct to sulfonamides
What is the mechanism of action of trimethoprim?
inhibits dihydrofolate reductase (DHF A to THF A)
What are the mechanisms of bacterial resistance to trimethoprim?
dec cell permiability
inc production fo dihydrofolate reductase
mutation of reductase
What are the pharmokinetics of trimethoprim?
well abs from GI
good distribution, 70% bound
hepatic acetylation
renal excretion
What is the dosing of trimethoprim with sulfamethoxazole?
5:1 yields 20:1 in plasma (T:S)
What is the potential toxicity of trimethoprim?
nausea, vomitting, diarrhea
hematological problems rare
What are the clinical uses of trimethoprim?
UTI
pulmonary bacteria
otitis media
AIDS pt w/ pneumocyctitis carinii
What is the prototypical quinolone?
ciprofloxacin
What are fluoroquinolones?
synthetic analogue of nalodixic acid capable of achieving effective systemic antibacterial levels
What is the spectrum of use of fluoroquinolones?
variety of gram (+) and gram (-)
What is the mechanism of action of fluoroquinolones?
block bacterial DNA synthesis by inhibiting DNA gyrase (II) and topoisomerase (IV)
What causes resistance to fluoroquinolones?
one or more point mutations at binding region
What are the pharmokinetics of fluorquinolones?
well abs by oral admin
bioavailability of 80-95%
oral abs impaired by divalent ions (antacids)
well-distrib (but not eff for CNS)
renal elimination
How are fluorquinolones eliminated by the kidneys?
glomerular filtration
tubule secretion
Name the urinary tract antiseptics.
methenamine
nitrofurantoin
phenazopyridine
What is the active moiety of methenamine?
formaldehyde
To what is production of formaldehyde from methenamine sensitive?
pH
What is the risk of methenamine?
GI toxicity
How is nitrofurantoin cleared?
rapid clearance to urine
turns urine brown
What is phenazopyridine?
urinary tract analgesis
What is the primary agent used in the treatment of TB?
isoniazid
What is the only agent used in the prophylaxis of TB?
isoniazid
What type of drug is isonizid?
bateriocidal
What does isoniazid require for effectiveness?
requires uptake by bacteria
Describe the pharmacokinetics of isoniazid.
well absorbed after oral
distributed to all fluid compartments
acylated
What is the toxicity of isoniazid?
hepatic most significant
inc w/ age
peripheral neuritis
pyridoxine
allergies
What is the MOA of rifampin?
inhibits RNA synthesis
forms stable complex w/ RNA polymerase
What type of drug is rifampin?
bacteriocidal
What are the pharmacokintetics of rifampin?
well abs after oral admin
highly bound (85%)
distributes to all fluids (red/orange)
active deacelylated metabolite
induces liver microsomal enzymes
What is the toxicity of rifampin?
GI
flu-like symptoms
hepatitis
What type of drug is ethambutol?
water soluble, heat stable, bacteriostatic antitubercular
What is the MOA of ethambutol?
inhibits arabinosyl transferase enzyems in cell wall synthesis
What RIPE drugs are only effective intracellularly?
ethambutol
pyrazinamide
What are the pharmacokinetics of ethambutol?
good abs after oral admin
depot effect in RBCs
distributes in most tissues & fluids, inc CNS
some liver metabolism
renal excretion
What is the toxicity of ethambutol?
visual problems: dec acuity, color discrim, peripheral vis
inc plasma urate levels
mild GI, allergic, CNS
What type of drug is pyrazinamide?
bactericidal, inhibits cell wall synthesis
What is required for pyrazinamide effectiveness?
acidic pH intracellular
What is the first line drug in RIPE?
pyrazinamide
What are the pharmacokinetics of pyrazinamide?
well abs after oral admin
good distributiton
hepatic metabolism, renal excretion
What is the toxicity of pyrazinamide?
hepatic- major
inc plasma urate
What type of drug is streptomycin?
bactericidal in vitro
suppressive agent extracell
What is the duration for streptomycin treatment?
effective w/ short duration only
What are the second line antimycotic drugs?
para-amino salicylic acid, ethionamide, cycloserine, amikacin, kanamycin, capreomycin
What are the pharmacokinetics of the antimycotic second-line drugs?
well abs after oral admin (ex amioglycosides)
good distribution (cycloserine esp in CNF)
metabolized by liver (ex cycloserine- exc unchanged)
Which second line antimycotics cause GI toxicity?
PAS
ethionamide
Which second line antimycotics cause CNS toxicity?
*cycloserine
ethionamide
What type of toxicity is seen with aminoglycosides?
ex. amikacin, kanamycin
ototoxicity
nephrotoxicity
What drugs are used in chemotherapy of mycobacterium aviam?
rifabutin
macrolides
quinolones
clofazimine
What is the MOA of rifabutin?
inhibits RNA polymerase
What is the clinical use of rifabutin?
prevents MAC infections in HIV pts
treats both HIV & non-HIV MAC pts
Resistance to what drug w/ also cause resistance to rifabutin?
rifampin
What are the pharmacokinetics of rifabutin?
well abs after oral admin
biphasic elimination (t1/2= 45hr)
lipophilic
eliminated in urine & bile
What are the adverse effects of rifabutin?
rash, GI, neutropenia
colors body fluids
uveitis, arthralgias (esp w/ fluconazole or clarithromycin)
hepatitis
drug interactions at CYP450
What is the therapy for leprosy?
sulfones
rifampin
clofazimine
What sulfone is used for the tx of leprosy?
dapsone
What are sulfones?
bacteriostatic agents
What is the MOA of sulfones?
blockade of folic acid synthesis
What are the pharmacokinetics of sulfones?
complete but SLOW abs
wide distribution & good retention in skin, muscle, liver, & kidney
70% bound
enterohepatic circ & reabs
metabolized by liver, acetylation, glucuronidation
What is used in combination w/ dapsone for treating leprosy?
rifampin
What is the use of clofazimine in treating leprosy?
for pts resistant to dapsone tx
How should clofazimine be used?
multidrug tx
What type of drug is clofazimine?
bactericidal
What is the MOA of clofazimine?
inhibits DNA template function, maybe by binding to mycobacterial DNA
anti-inflammatory
What are the pharmacokinetics of clofazimine?
GI abs variable
wide distribution w/ long half-life (2mo)
exc in bile