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76 Cards in this Set

  • Front
  • Back
how do sulfonamides work (antimetabolites)
competitively inhibit folic acid and inhibit DNA synthesis

analog of PABA

bacteristatic (reversible)
inhibits the production of folic acid by competitive inhibition?

what infection is it used for

used for UTIs cause it is conc in urine
sulfonamides - bacteriocidal or static
some of these antibiotics are concentrated in urin and so their greates application is in treating UTIs
inhibits dihydrofolate reductase

an antimetabolite. often used in conjunction with sulfonamide (BACTRIM)
narrow spectrum antibiotic.
works against M. tuberculosis by interfering with the sythesis of mycolic acid (material unique to the cell walls of mycobacteria)

antimetabolite (inhibits enzyme termed InhA needed for fatty acid elongation)
isoniazid - cidal or static
cidal - penetrates well through human cell membrane to fight M. tuberculosis
how does penecillin work
inhibits cell wall synthesis

by binding PBPs (many are responsible for the terminal stages of cell wall synthesis e.g transpeptidazes)

inactivation of PBPs trigger autolytic enzymes to break down cell wall
this class of antibiotics inhibits peptidoglycan synthesis
cell wall inhibitors

uncouples the control of endogenous degradative activities (autolysins) which normally are synchronized with cell wall synthesis - cell lysis in hypotonic media
A Penicillin which is hydrolyzed by acidity of stomach, is sensitive to penecillinase and has benzyl side chain on 6-amino-penicillanic acid
penicillin G

works against G+, some G-
penicillin which is NOT sensitive to acid hydrolysis but IS sensitive to penicillinase and has a phenoxymethyl side chain
Penicilin V
not sensitive to acid hydrolysis but still sensitive to penicillinase with an aminobenzyl side chain

broader specturm the P G and V. works against G- enteric Bacilli, and G+
B lactam antibiotics are structural analogs of?
and bind what?
analogs of pepotidoglycan pentapeptide

bind penicillin-binding proteins (PBPs e.g transpeptidase)
sensitive to penicillinase - limited spectrum - highest activity against Gm+ bacteria and G- cocci; ineffective versus Gm- enterics
Penicilin G and V
sensitive to penicillinase - broader spectrum (active against G- enteric bacilli as well as retaining most activity against G+)
amoxiciillin (like ampicllin but higher serum levels)
semisynthetic penicillin - acid resistant - resistant to penicillinase - available oraly
like peniccilins but substitute a dihydrothiazine ring instead of the thiazolidine ring of the penicillins

cidal or static?
cephalosporins - bacteriocidal

good for people with penicillin allergies
cephalosporins work against what kind of bacteria
broad spectrum, gram + and some gm - bacilli
first generation cephalosporin cefazolin is good against
g+ cocci, some gm - bacilii but NOT P.aeruginosa
secod generation of cephalosporins (cefuroxime) is good against
g- enterics, less effective against gm +
NOT effective gainst P. aeruginosa
third generation cephalosporin called ceftriaxone are effective against
P. aeruginosa -
better CNS penetration
improved B-lactamase stability
clavulanic acid and sulbactam are
B-lactamase inhibitors
vancomycin targets
only gram + organisms
binds R D-Ala-D-Ala
inhibiting RNA synthesis
D-alanine analong which inhibits cell wall synthesis and is used to treat TB
Bacitracin (a cell wall inhibitor) treats what kind of bacteria
Gm + organism
restricted to topical (in neosporin)

a cell wall inhibitor
an inhibitor of protein synthesis -bacteriocidal but not lytic.
binds 30 S?

fights what kind of bacteria
enters through imperfections in growing membrane

gm -
streptomycin targets what kind of bacteria

note: stretpomycin and gentamicin are aminoglycosides and there fore are inhibited by anaerobic and acid conditions
group of drugs that are
used for treatment of immunocompromised patients because limited to serious infections
blocks the binding of aminoacyl-RNA to 30S
not to be give during pregnancy or kids (mottled anamel)
tetracycline or doxycycline
resistance to efflux pump
derivitive of tetracycline
blocks chain elongation
inhibits 50S

spectrum similar to penicillin but includes mycoplasma and chlamydia
like erythromycin but broader spectrum, high sustained tissue concentrations

is a macrolide (binds 503) like erthromycin
blocks chain elongation
is aminoglycoside
bacteriostatic (sometimes bacteriocidal)

used against B.fragilis
a derivitive of lincomycin. has activity against Gm+ and moderate activity against anaerobes.
inhibits peptidyl transfer
two drugs that inhibit translation by interactions with ribosome and have potential for treating VREF, MRSA
oxazolidinones and streptogramins
binds tRNA synthetase inhibits translation
treatment of MRSA
topical treatment of impetigo caused by s.aureaus and s.pyogenes
inhibitors of DNA replication
e.g Nalidixic Acid
and Nitroamidazoles
group of drugs that inhibit DNA gyrase and are bacteriocidal
e.g nalidixic acid

works against Gm- enterics and good for treating UTI
not for pregant women or children due to growing bone
should not be prescribed for pregnant women or children because they damage growing bone
an anaerobic drug which binds DNA and fragments it
good for Bacteriodes species
action requires anaerobic conditions
broad spectrum
inhibits RNA synthesis by binding B subunit of bacterial RNA polymerase, inhibiting specific binding to DNA
efficeintly secreted in saliva - so useful as prophylactic against infectious bacteria (N. menigitidis!)

used in combo with other drugs cause resistance develops rapidly
ethambutol and pyrazinamide are used
etham - static
pyrazin - cidal
using penicillin and tetracycline would not work why
penicillin requires growth and tetracycline is static
penicillin and aminoglycosides work well together because
one damages the cell wall and one is taken up poorly by bacterium

e.g streptomycin (aminoglycoside) enters through growing membrane
aminoglycosides are inhibited by
acid, and anaerobic conditions
hydrolyzes the lactone ring of erythromycin
erythromycin esterase
antibiotic efflux from cell is an issue for what two antibiotics
tetracycline and fluconazole (an antifungal - inhibitor of membrane synthesis)
alteration of ribosomal targets occur frequently for
erythromycin and streptomycin
mode of bacterial resistance of vancomycin
alteration of cell wall precursor targets
methicillin resistance is via
altered affinity PBPs

(Neisseria, HiB, P. aeruginosa)
altered dihydropteroate synthetase
four classes of drugs which inhibit protein synthesis
aminoglysides (streptomycin)
macrolides (erythromycin)
mechanisma of resistance is an interference with transport of drug into cell / efflux pumps
mechanism of resistance is detoxificaiton of drug by acetylation of hydroxyl
mechanism of resistance is enzymatic methylation o 23S ribosomal RNA
altered target enzyme (gyrase, RNAP) affects what two drugs
ciprofloxacin (a fluoroquinolone) and rifampin
inhibits ergosterol synthesis (anti-fungal)
topical or oral fungal infections
"swish and swallow"

is not absorbed by GI tract which is good cause it would be toxic systemically

nystatin works by increase membrane permeability -by binding sterols in the CM.
fungal drug that affects membrae permeability, is fungicidal
it is polyene compounds so it binds sterols in cell membrane
amphotericin B

(is only injectable)
amphotericin B - cidal or static

Nystatin is static
inhibits cell membrane synthesis in fungus - used to treat thrush
inhibitors of glucan synthesis
echniocandins (Caspofungin)

dont get confused with Azoles which inhibit ergosterol synthesis. glucan is in fungal wall and ergosterol is in the CM
antimetabolite anti-fungal drugs which works by replacing uracil with 5-fluroururicil in fungal RNA
therefore interferes with DNA synthesis and is
cidal or static
therapeutic index
dose toxic to host/ dose therapeutic
how does toatl cell count and viable cell count differ with bacteriostatic and bactericidal
1. bacteriostatic: no change in total count, decrease viable
2. decrease total and viable
Quinolones work against what kind of bacteria and are therefore used to treat what
work against Gm- enterics - used to treat UTI
quinolones - cidal or static

inhibitors of DNA replication

e.g nalidixic acid - used against Gm - enterics
treatment of anthrax
Ciprofoloxacin - a fluorquinolones
inhibits gyrase AND topoisomerase so theoretically resistance will not develop rapidly due ot multiple DNA targets
fourth generaion fluroquinolones

activated under anaerobic conditions
polymyxin B and polyumyxin E (colisin) are cidal or static

they affect cell how

affect membrane permeability
Streptomycin is not used except for treating
tb -