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52 Cards in this Set
- Front
- Back
What are the major antibiotics that inhibit bacterial cell wall synthesis? |
Penicillins and Cephalosporins, which are beta-lactams
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What type of drug are beta-lactams?
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Bactericidial drugs
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What are the steps of beta-lactams?
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1) binding to penicillin-binding proteins in the bacterial cytoplasmic mm; 2) inhibition of transpeptidation reaction (cross-links the peptidoglycan chain of the cell wall); 3) activation of autolytic enzyme that cause lesions in the bacterial cell wall.
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What is a major form of resistance to beta-lactams?
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Beta-lactamses (penicillinases) by most staphylococci and many gram-negatives.
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Pencillin G is useful for what and is the DOC for?
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Gram-positive cocci, and DOC for spirochetes (Treponema pallidum), Neisseria meningococcal (but NOT N. gonorrhoeae).
Activity against enterococci is enhanced with aminoglycoside. |
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Penicillin G is not useful for?
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Staphyloccous aureus, Neisseria gonorrhoeae and many strains of pneumonococci.
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What drugs are used to treat known or suspected staph infections?
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I MET a NAsty OX (beta-lactamase resistant penicillins: METHicillin, NAFcillin, and OXacillin)
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Ampicillin and amoxicillin (wide spectrum penicillinase-susceptible drugs) are used for?
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Similar to penicillin G but also:
HELPS: (Haemophilus influenzae, E. coli, Listeria monocytogenes, Proteus mirabilis, Salmonella) (Enterococci, and these drugs are amongst the few effective against this bug!) Gram-negative cocci and rods, gram-positive cocci |
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TCP: Ticarcillin, Carbenicillin, Piperacillin (wide spectrum penicillinase-susceptible drugs) are useful for?
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TCP: Takes Care of Pseudomonas
Pseudomonas, Enterobacter, and Klebsiella |
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What drug can be used with penicillin/ampicillin to have a synergistic effect against enterococcal and listerial infections (and broader gram negative coverage)?
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Aminoglycosides
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What are some allergic reactions with penicillin?
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Drug-indcued Coombs' positive hemolytic anemia; urticaria, severe prutirtius, fever, joint swelling, nephritis, and anaphylaxis
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What drug can result in pseudomembranous colitis?
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Clindamycin, cephalosporins, or any penicillin (amoxicillin)
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Oral penicillins can cause what GI upset?
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Nausea and diarrhea, which may be caused by overgrowth of gram-positive organisms or yeast.
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Cephalosporins bind with what?
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Penicillin-binding protein
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What type of drug is cephalosporins?
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Bactericidal
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What is the first generation of cephalosporins and what are they effective against?
PEcK |
Cefazolin and cephalexin:
Proteus mirabilis, E. coli, Klebsiella pneumoniae. Effective against gram-positive cocci |
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What is the second generation of cephalosporins and what are they effective against?
HEN PEcKS |
Cefoxitin, cefaclor, cefuroxime
H. influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens. Less effective against Gram-positive cocci compared to the first generation, but more effective against gram-negative such as anaerobe (e.g., bacteroides fragilis) and sinus, ear, and respiratory infections caused by H. influenzae or M. catarrhalis. |
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What is the third generation of cephalosporins and what are they effective against?
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Ceftazidime, ceftriaxone, cefotaxime:
Most penetrate the BBB: meningitis. Gram-negative, and pneumoniae, meningitis, and gonorrhea |
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What is the fourth generation of cephalosporins and what are they effective against?
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Cefepime
Broad activity, beta-lactamase-stable. Combines gram-positive activity of first-generation with wider gram-negative spectrum of 3rd generation. Against beta-lactamases (Enterobacter, Haemophilus, Neisseria, and some penicillin-resistant pneumococci) |
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What is the allergic reaction against cephalosporins?
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From skin rash to anaphylactic shock. Disulfiram-like reaction with ethanol, and nephrotoxicity
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Although, there is a cross reactivity between penicillins and cephalosporins, and those who are allergic to penicillin can sometimes be treated with cephalosporin; however, if the PT has had a history of anaphylaxis to penicillin, can they be treated with cephalosporin?
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NO
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What drug is resistant to beta-lactamases produced by gram-negative rods (Klebsiella, Pseudomonas, and Serratia); and therefore can be used to treat against those infections?
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Aztreonam. It is only effective against Gram-negative (including Pseudomonas) and NOT gram-positive
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How does aztreonam work?
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Binds to PBP and blocks peptidoglycan cross-linking.
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What drug does not have a cross-allergen of penicillin?
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Aztreonam.
Note: for penicillin-allergic PTs and those with renal insufficiency who cannot tolerate aminoglycosides. |
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What drug belongs to the class monobactam?
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Aztreonam
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Carbapenems are effective against?
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Broad spectrum includes PRSP strains (not MRSA), gram-negatie rods, gram-positive cocci, and anaerobes.
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What are the SE of carbapenems?
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CNS toxicity (Confusion, encephalopathy, seizures). Seizures can be reduced by reducing dosage in PTs with renal impairment. Partial cross-reactivity with penicillins.
Note: the significant SE limits its use to being the DOC for Enterobacter. |
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What inactivates bacterial beta-lactamases, and added to amoxicillin or ampicillin to broaden the spectrum of coverage against gonococci, streptococci, E. coli, and H. influenzae?
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Clavulanic acid, sulbactam, tazobactam.
NOT against Enterobacter, Pseudomonas, and Serratia. |
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What inactivates bacterial beta-lactamases and added to piperacillin to broaden the spectrum against gram-negative and S. aureus infections?
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Tazobactam
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What drug inhibits transglycosylase (by binding to D-Ala-D-Ala terminal) an enzyme involved in peptidoglycan elongation and cross-linking?
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Vancomycin
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What is vancomycin used for?
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Serious gram-positive resistant organisms, including S. aureus and Clostridium difficile (pseudomembranous colitis, but metronidazole is the DOC)
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SE of vancomycin?
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Nephrotoxicity, ototoxicity, thrombophlebitis, diffuse flushing--"red main syndrome"(due to histamine release) (can largely be prevented by pretreatment with antihistamines and slow infusion rate).
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MOA of cephalosporins involves inhibition of?
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Reactions involving transpeptidation; therefore, inhibiting peptidoglycan cross-linking.
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Vancomycin inhibits?
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Transglycoslase, preventing elongation of peptidoglycan by binding to D-alanine D-alanine to inhibit transpeptidation.
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What is the DOC for gonorrhea?
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Ceftriaxone
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What is the DOC for Treponema pallidum?
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Penicilling G.
If allergic, than doxycycline or tetracycline. |
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A debilitated PT has a fever from a skin infection, which yields gram-positive cocci. DOC is?
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Nafcillin, which is resistant to penicillinases and S. aureus (but not MRSA) and common strep. Bacterial lesions are most likely staph or strep
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A women is treated for bacteremia with gram-negative bacilli. Records show that she has had severe rash, hypotension, and respiratory distress after penicillin V. What is the drug regimen?
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Aztreonam, which has no cross-reactivity between penicillins.
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PT presents with S. pneumoniae, but is penicillin G resistant. What is the treatment?
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Cefotaxime or ceftriaxone, which are the most active cephalosporins against penicillin-resistant pneumococci, and the addition of vancomycin or rifampin is recommended.
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What is the reason for resistance to penicillin G?
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Changes to penicillin binding protein.
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Diptheroid-like gram-positive rods in the CSF in an elderly PT are indicative of what? What is the DOC?
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Listeria monocytogenes. Ampicillin.
Listeria are common in neonates, the elderly PTs, and those who are immunocompromised. |
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PT with severe anaphylactic reaction to penicillin G, has enterococcal endocarditis. What is the DOC?
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Vancomyin. Aminoglycoside may be added for synergistic effect.
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This drug has activity against Pseudomonas; however, when used alone, resistance emerges. The drug should not be used in penicillin-allergic PTs. Its activity against gram-negative rods is enhanced if used in combination with tazobactam. It is also effective against anaerobes (Bacteroides fragilis)
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Piperacillin
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Vancomycin is not susceptible to?
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Penicillinase
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Transpeptidase AKA?
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penicillin-binding protein
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What can be given with imipenem to increase its duration of action. It is the DOC for?
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Cilastain, which inhibits renal dihydropeptidase I (inactivates imipenem in the renal tubules)
DOC for Enterobacter. Note: cilastatin is ALWAYS given with imipenem. |
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What is similar to methicillin, in the sense that it is resistant to beta-lactamases?
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Aztreonam
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What are peptidoglycan and transpeptidases?
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Peptidoglycan are chains of polysaccharides and polypeptides that are cross-linked to form the bacterial cell wall.
Transpeptidases are bacterial enzymes involved in the cross-linking of linear peptidoglycan chains, the final step in cell wall synthesis. |
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What spectrum do methicillin, nafcillin, and oxacillin fall under, and what is their main use? Which one is hardly used due to its nephrotoxic potential?
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Very narrow spectrum penicillinase-resistant drugs. Treatment of staph infections.
Methicillin is hardly used due to nephrotoxic potential |
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What drugs belong to the class carbapenems, that have a low susceptibility to beta-lactamases, and structurally different than penicillin but retains the beta-lactam ring structure?
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Imipenem, meropenem, and ertapenem.
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What drug is less likely to cause seizures in the carbapenem class?
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Meropenem. It is not metabolized by renal dehydropeptidases.
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What drug has a spectrum similar to vancomycin and active against vancomycin-resistant strains of enterococci and staph?
What should be monitor with this drug and why? |
Daptomycin
Creatinine phosphokinase, since daptomycin may cause myopathy. |