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Pharm 3
Inhibitors of Cell Wall Syn II
67
Accounting
Pre-School
04/18/2009

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Term
Penicillin G: Spectrum
Definition
narrow spectrum, B-lactamase susceptible,: Group A streptococci (pyogenes), T pallidum, enterococci, pneumococci, meningococci (Neisseria meningitidis ), anaerobes.
Can't kill staph because of penicillinase.
Term
To treat staphylococci
Definition
Nafcillin, oxacillin: very narrow spectrum, penicillinase-resistant (Can't treat MRSA).
Term
Methicillin
Definition
Oxacillin used instead of methicillin to treat staphylococci(renal toxicity)
Term
Aminopenicillins:
Definition
ampicillin, amoxicillin. Like G (strep pyogenes, strep pneumonia, neisseria meningitidis, enterococci, T Pallidum, anaerobes), + Gram negatives (E. coli, H influenza, L monocytogenes, P mirabilis)
Term
Broad spectrum, B-lactamase susceptible penicilins
Definition
aminopenicillins (ampicillin, amoxicillin), Carboxypenicillins (ticarcillin), Ureidopenicillins (piperacillin). Can be combined with a B-lactamase inhibitor to extend spectrum
Term
Carboxypenicillins
Definition
Ticarcillin. BROAD SPECTRUM. gram - spectrum extends to pseudomonas and proteus
Term
Ureidopenicillin
Definition
Piperacillin: gram neg is similar to ticarcillin but extends to K pneumonia, B fragilis
Term
B lactamase inhibitors: structure
Definition
contain a B-lactam ring that acts as a suicide substrate. Synergism with amoxicillin, ampicillin, ticarcillin, piperacillin
Term
Cephalosporin: spectrum
Definition
BROADER, less susceptible to B-lactamases
Term
Cephalosporin: bactericidal/static
Definition
cidal
Term
Cephalosporin: target
Definition
PBP; less susceptible to B-lactamase
Term
Cephalosporin: substituents
Definition
affect porin penetration, B-lactamase susceptibility, target binding
Term
Cephalosporin: resistance
Definition
B-lactamase production, altered target, impaired access
Term
Cephalosporin: adverse effects
Definition
hypersenstivity: limited cross allergenicity w penicillins but do NOT use in pts with anaphylaxis; GI like penicillins
Term
Cephalosporin: pharmacokinetics
Definition
parenteral; do not enter the CNS
Term
Cephalosporin: elimination
Definition
renal excretion
Term
Cephalosporin: 1st generation spectrum
Definition
Not penicillins so they can kill bugs that produce penicillinases: gram + cocci prophylaxis, + E. coli, k pneumonia, p mirabilis
Term
Cephalosporin: 2nd generation spectrum
Definition
increased activity against gram - (H influenza, B fragilis), anaerobe prophylaxis
Term
Cephalosporin: 3rd and 4th generation spectrum
Definition
enteric gram - bacilli : hospital acquired strains that exhibit mulitdrug res
Term
Cephalosporin: 1st generation uses
Definition
surgical prophylaxis, skin infections
Term
Cephalosporin: 2nd generation uses
Definition
respiratory and mixed anaerobic infections
Term
Cephalosporin: 3rd/4th generation uses
Definition
empirical therapy of serious infections-meningitis, sepsis
Term
Cephalosporin: 3rd generation uses
Definition
gonorrhea
Term
Monobactam (aztreonam): target
Definition
PBP 3 of GRAM NEGATIVE
Term
Monobactam (aztreonam): cidal/static
Definition
cidal
Term
Monobactam (aztreonam): spectrum
Definition
gram -. Not susceptible to B-lactamases
Term
Monobactam (aztreonam): resistant organisms
Definition
gram + and anaerobes are intrinsically resistant.
Term
Monobactam (aztreonam): resistance
Definition
not susceptible to B-lactamases of gram - aerobes
Term
Monobactam (aztreonam): synergistic co-drugs
Definition
aminoglycosides; similar spectrum to aminoglycosides as well
Term
Monobactam (aztreonam): adverse effects
Definition
NO cross allergenicity with penicillins or cephalosporins
Term
Monobactam (aztreonam): pharmacokinetics
Definition
parenteral
Term
Monobactam (aztreonam): clearance
Definition
renal
Term
Monobactam (aztreonam): uses
Definition
Serious infections with drug resistant gram - aerobes
Term
Carbapenems: drug names
Definition
imipenem/cilastatin, meropenem, eratepenem
Term
Carbapenems: target
Definition
PBP
Term
Carbapenems: cidal/static
Definition
cidal
Term
Carbapenems: spectrum
Definition
Very broad spectrum: kill many gram - and gram + organisms as well as PRSP (but not MRSA). Includes anaerobes
Term
Carbapenems: resistance
Definition
low susceptibility to B-lactamases
Term
Carbapenems: resistant organisms
Definition
Ps. Aeruginosa, deliberately limiting drug use reduces selection pressure
Term
Carbapenems: uses
Definition
Mixed infections (aspiration pneumonia, ruptured appendix, empirical therapy in immunocomromised hosts). As a last resort if 3rd generation cephalosporins don't work.
Term
Carbapenems: pharmacokinetics
Definition
parenteral
Term
Carbapenems: clearance
Definition
renal elimination. Renal dehydropeptidase I cleaves B-lactam ring of imipenem. cilastatic dehydropeptidase
Term
Carbapenems: adverse effects
Definition
hypersenstivity (cross sensitivity w Penicillins), GI, CNS (seizures w renal failure)
Term
Glycopeptides: target
Definition
Binds D-ala-D-ala to inhibit polyermization of the cell wall precursor. inhibits polymerization of the monomer
Term
Glycopeptides: drug names
Definition
Vancomycin, teicoplanin
Term
Glycopeptides: cidal/static
Definition
cidal
Term
Glycopeptides: spectrum
Definition
gram + (gram - are intrinsically resistant because vancomycin is too large to fit thru porins)
Term
Glycopeptides: resistance mechanisms
Definition
D-ala-D-ala is replaced by D-ala-D-lactate. loss of 1 hydrogen bond leads to a 1000x decrease in drug binding affinity.
Term
Glycopeptides: adverse effects
Definition
vasodilation (histamine induces red man syndrome), ototoxicity (hearing loss), nephrotoxicity.
Term
Glycopeptides: pharm
Definition
parenteral
Term
Glycopeptides: clearance
Definition
renal
Term
Glycopeptides: uses
Definition
Serious infections with B-lactam resistant gram +: MRSA, PRSP
Term
Bacitracin: target
Definition
blocks dephosphorylation of the lipid II carrier transfers peptidoglycan subunits across the plasma membrane
Term
Bacitracin: spectrum
Definition
gram +
Term
Bacitracin: uses
Definition
nephrotoxic, only used topically
Term
Cycloserine: target
Definition
structural analog of D-ala
Term
Cycloserine: uses
Definition
second tier drug for TB
Term
Cycloserine: toxicity
Definition
CNS: headaches, tremors, convulsions
Term
Fosfomycin: target
Definition
inhibits enolpyruvate
Term
Fosfomycin: spectrum
Definition
gram + and -
Term
Fosfomycin: uses
Definition
UTIs, safe for pregnant, expensive
Term
Daptomycin: target
Definition
cell membrane: Ca++ dependent insertion of lipid tail causes depolarization, disrupts macromolecular synthesis
Term
Daptomycin: spectrum
Definition
gram +
Term
Daptomycin: pharmacokinetics
Definition
Concentration dependent, PAE, parenteral
Term
Daptomycin: clearance
Definition
urinary (adjust for renal disease)
Term
Daptomycin: uses
Definition
endocarditis and complex skin infections due to MRSA, VRSA, VRE (vancomycin resistanct enterococcus)
Term
Daptomycin: toxicity
Definition
GI, myopathy
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