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50 Cards in this Set
- Front
- Back
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Hydrolysis of the B-lactam ring yields?
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Penicilloic acid:
lacks antibacterial activity |
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substituents attached to what biological group, yield modified penicillins?
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amino group
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basic structure of penicillin
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Thiazolidine ring attached to a B-lactam ring that carries a secondary amino group.
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Penicillins have activity against what organisms?
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Gram +
Gram - cocci Non B-lactamase anaerobes |
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Penicillin has little activity against
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Gram - rods
B-lactamase producers |
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Resistant to staphylococcal B lactamase
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Nafcillin
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Similiar to ampicillin but better absorbed
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Amoxicillin
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Ampicillin
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Similar to penicillin but with greater activity against gram - and its also acid-stable
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MOA of penicillin
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Inhibit bacterial growth by interfering with transpeptidation of the bacterial cell wall synthesis. B-lactams bind to the PCP of the D-ALA-D-ALA peptide that is attached to NAM and stops it from binding to another D-ALA-D-ALA peptide of another NAM.
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B-lactam antibiotics only work when the bacteria is actively
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growing and synthesizing cell wall
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Mos common resistance to B-lactams
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beta-lactamases
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Basis of resistance to B-lactams in MRSA and penicillin resistance in pneumococci and enterococci
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Altered target PBP's
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Resistance due to impaired penetration of antibitotic to target PBP's occurs only in gram- species because?
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they have an impenetrable outer wall that is absent in gram+
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How do B-lactams work against gram- bacteria?
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They cross the outer cell wall via porin channels
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B-lactam that is highly bound to proteins
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Nafcillin
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Penicillin is rapidly cleared via? Nafcillin?
Ampicillin? |
tubular excretion in the kidneys. Thus, the dose must be adjusted in those with renal failure.
Biliary excretion Kidney |
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Should penicillins be given with food?
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Except for amoxicillin, no, because they may bind to food proteins, and may also be inactivated in a highly acidic environment.
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Effective in the txmt of syphilis
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Benzathine penicillin G:
IM penicillinG |
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Adverse effect of methicillin. Nafcillin?
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interstitial nephritis
Neutropenia |
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Implicated in pseudomembranous colitis
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Ampicillin:
may also cause Nausea and diarrhea |
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B-lactams that are resistant to beta-lactamase producing staphylococci
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Methicillin and nafcillin
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Active against staphylococci and streptococci, but not against enterococci, anaerobes, or gram- rods/cocci
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Antistaph penicillins:
Methicillin and nafcillin |
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Broad-spectrum penicillins. Are they resistant to b-lactamases?
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Ampicillin
Amoxicillin Piperacillin Ticarcillin They are not resistant, even though they are effective against L. monocytogenes, E. coli, H. influenzae and others. |
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DOC for infections of streptococci, staphylococci, enterococci, meningococci
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Penicillin
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Ampicillin is synergistic with aminoglycosides in what type of infections?
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Listeria or enterococcal
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given orally to treat UTI's, sinusitis, otitis, and lower respiratory tract infections
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Amoxicillin or ampicillin
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B-Lactams that have activity against gram- rods including pseudomonas, enterobacter, and Klebsiella. What if you have anaphylatic allergic rxn to penicillins?
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Piperacillin and ticarcillin
Wide spectrum b-lactamase susceptible drugs Carbanapems: Imanapem |
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Nucleus of cephalosporins
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7-aminocephalosporanic acid
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1st generation cephalosporins
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cephazolin, Cephalexin
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Cephalosporin used as prophylaxis txmt before surgery
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cefazolin
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MOA of cephalosporins
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Bind to PBP's and inhibit bacterial wall synthesis
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Excretion of cephalosporins
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Via tubular cells of kidney
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Alternative to antistaphylococcal penicillin for pts allergic to penicillin
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Cefazolin:
Good activity against gram+ organisms and is resistant to some beta-lactamases |
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B-lactam DOC for penicillin-resistant pneumococci
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ampicillin or amoxicillin
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Ampicillin, ticarcillin, and piperacillin are usually combined with what to increase their activity
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B-lactamase inhibitors:
clavulanic acid, sulbactam, or tazobactam. |
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DOC for gonnorhea
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3rd generation cephalosporins:
Ceftriaxone Cefixime |
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Most active cephalosporins against penicillin resistant pneumocci
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Ceftriaxone and cefotaxime...used in meningitis. 3rd gen cephs.
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3rd generation cephalosporins should be avoided in txmt of?
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enterobacter infections due to emergence of resistance. Instead use 4th gen cefipime.
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Used in txmt of sepsis of unkown cause in pts who are immunocompromised
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3rd generation cephalosporins:
Cefdinir(Omnicef) Ceftriaxone(rocephin) Cefotaxamine |
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Useful characteristics of of 3rd generation cephalosporins
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Expanded gram- coverage and cross the blood brain barrier
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Cephalosporin useful in the txmt of enterobacter
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4th gen:
Cefipime |
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Should pts with a hx of anaphylaxis after penicillin administration be given cephalosporins
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No
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Carbapenems
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Imipenem, Meropinem, and ertapenam
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Only monobactam available in the US. What is it used for?
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Aztreonam:
Aerobic gram+ bacteria such as Pseudomomas |
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Beta-Lactamase Inhibitors are most active against bacteria with?
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Class A beta lactamases:
Plasma encoded Not useful for inducible chromosomal beta-lactamases |
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Inhibits transglycolase, thus preventing elongation of petidoglycan chains
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vancomycin
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Antimetabolite that blocks the incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan. When is it used?
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Cycloserine:
Used during resistant tuberculosis strains, when the 1st line txmt did not work. Causes neurotoxicity. |
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Bacitracin is active against? MOA
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Gram+
Stops dephosphorylation of lipid carrier that transfers peptidoglycan units to cell wall. Highly nephrotixic, so its used only topically. |
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Used in vanc resistant strains of enterococci and staphylococci
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Daptomycin:
causes K+ efflux |
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SE of daptomycin use
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May cause myopathy, so levels of CPK should be checked
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