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