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FIU - Antibiotics
cell wall inhibitors
41
Pharmacology
Graduate
01/12/2012

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Cards

Term
what is the difference between Gram+ and Gram- bacteria? what color do they stain?
Definition
Gram+ have peptidoglycan cell wall outside of cell membrane; purple
Gram- have peptidoglycan layer between plasma membrane and outer cell wall; pink
Term
what are atypical bacteria? eg?
Definition
don't have a peptidoglycan cell wall
Mycoplasma and chlamydia
Term
Steps in cell wall synthesis
Definition
1. Nam-Nag precursors formed in cytoplasm, transported to cell wall
2. Transglycosylation - polymerization of Nam-Nag complexes
3. Transpeptidation - PBP cross link aa chains of Nam-Nag
Term
types of B-Lactams
Definition
Penicillin, Cephalosporin, Carbapenems, Monobactams
Term
what do all B-lactams have in common?
Definition
Structure (B-lactam ring)
mechanism of action - inhibition of transpeptidation
Synergism w/ aminoglycosides and antagonism w/ tetracyclines
Term
mechanisms of resistance to penicilin?
Definition
-B-lactamase production - attacks C-N bond and inactivates drug
-Structural changes in PBP - won't allow drug to bind
-Changes in porin structure - won't allow drug to enter bacteria
Term
how are penicilins eliminated
Definition
Renally through PSOASS
EXCEPT: Nafcilin and Oxacilin - more lipid soluble, secreted via bile
Term
ADR of penicilins
Definition
hypersensitivity - ranging from; simple rash, bronchospasm, urticaria, anaphalctic shock
Term
categories of penicillins
Definition
Natural, Anti-staphylococcal(Oxipenicillins), Extended spectrum (aminopenicillins), and Anti-pseudomonal
Term
DOC for syphilis
Definition
Penicillin G
Term
what penicillins are resistant to B-lactamase
Definition
Anti-staphylococcal (oxipenicillins)
Term
DOC for MRSA
Definition
Vancomycin
Term
MOA of Aminopenicillins
Definition
water solublility from amine group allows them to pass through porin channels in gram- bacteria
Term
depot forms of Penicillin G
Definition
combinations to extend halflife
Pen G Procaine or Pen G benzathine
Term
Anti-pseudomonal use? MOA? examples?
Definition
gram- bacteria, mainly pseudomonas aeruginosa (green toe infection)
structure allows access through pseudomonal bacteria that don't have porin structure
Carbenicillin, Piperacillin, Ticarcillin
Term
what are "suicidal inhibitors"? examples?
Definition
B-lactamase inhibitors; have similar structure to B-Lactams, administered w/ B-lactams, bind to B-lactamase to inactivate and protect the B-lactam
Sublactam, Clavulonate, Tazobactam
Term
B-lactamase inhibitor administered with - ampicillin, amoxicillin, piperacillin, ticarcillin
Definition
ampicillin + sublactam
amoxicillin + clavulonate
Piperacillin + tazobactam
Ticarcillin + clavulonate
Term
cephalosporin similarities to penicillins
Definition
structure/function, excretion, cross-allergenicity, resistance
Term
DOC for bacterial meningitis
Definition
3rd generation cephalosporins, Ceftriaxone, Cefotaxime, Ceftazidime
Term
cephalosporins w/ NMTT side chain
Definition
PMT
Cefoperazone
Cefamandole
Cefotetan
Term
unique side effects of NMTT cephalosporins
Definition
- hypoprothrombinemia -> prolonged bleeding from inhibitions of Vitamin K depenedent factors
-disulfiram-like reaction (hangover symptoms)
Term
what B-lactams have the broadest spectrum?
Definition
Carbapenems
Term
Imipenem, class? what is it commonly administered w/ and why?
Definition
Carbapenem
Administered with cilastatin
Cilastatin inhibits renal dehydropeptidase I which normally cleaves Imipenem to an inactive metabolite that is nephrotoxic
Term
Aztreonam
Definition
Monobactam
Term
what are monobactams used for
Definition
gram- rods
Term
2 non-B-Lactams
Definition
Vancomycin and Bacitracin
Term
B-Lactams MOA
Definition
block transpeptidation via binding to PBP, leads to weakening of cell wall, upon exposure to hypotonic environment causes cell swelling -> lysis
Term
Vancomycin MOA
Definition
inhibition of transglycosylation
binds to D-ala-D-ala terminal end of Nam preventing binding to next Nam-Nag complex
Term
Bacitracin MOA
Definition
block transport of Nam-Nag precursors from cytoplasm to cell wall
Term
Vancomycin, ADRs? mode of resistance?
Definition
glycopeptide
Red man syndrome, Ototoxicity and Nephrotoxicity
Replacement of D-Ala with D-Lactate -> vancomycin cannot cap this end
Term
Teicoplanin
Definition
glycopeptide
similar spectrum, less toxic and longer t1/2 version of Vancomycin
equally as efficacious in pseudomembranous colitis
Term
Daptomycin
Definition
cyclic lipopeptide
bacteriocidal
bind to membrane causing rapid depolarization, loss of membrane potential, inhibition of DNA, RNA and protein synthesis
used for Gram+ and complicated skin and skin structure infections (cSSSI) from S. Aureus bactermia
Term
Carbenicillin
Definition
Anti-pseudomonal penicillin
Term
Piperacillin
Definition
Anti-pseudomonal, penicillin
Term
Nafcillin
Definition
Oxipenicilin (anti-staph), penicillin
Term
Ticarcillin
Definition
Anti-pseudomonal, penicillin
Term
Methicillin
Definition
Oxipenicillin (anti-staph), penicillin
*highly hepatotoxic, only used to determine if MRSA
Term
What makes MRSA resistant
Definition
additional PBP - PBP2A which has low affinity for most B-lactams, so bacteria will still produce a cell wall, just more slowly
Term
which generation cephalosporins, are more sensitive to lactamases? more specific to gram+, gram-? can cross BBB?
Definition
1st generation
gram+ = 1st generation
gram- = 3rd generation
BBB = 3rd generation
Term
which B-Lactams are renally excreted but not probenacid sensitive?
Definition
Carbapenems and Monobactams
Term
DOC for pseudomembranous colitis? alternative?
Definition
DOC: Metroniazol
Alternative: Vancomycin
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