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52 Cards in this Set

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What are the major antibiotics that inhibit bacterial cell wall synthesis?

Penicillins and Cephalosporins, which are beta-lactams
What type of drug are beta-lactams?
Bactericidial drugs
What are the steps of beta-lactams?
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.
What is a major form of resistance to beta-lactams?
Beta-lactamses (penicillinases) by most staphylococci and many gram-negatives.
Pencillin G is useful for what and is the DOC for?
Gram-positive cocci, and DOC for spirochetes (Treponema pallidum), Neisseria meningococcal (but NOT N. gonorrhoeae).

Activity against enterococci is enhanced with aminoglycoside.
Penicillin G is not useful for?
Staphyloccous aureus, Neisseria gonorrhoeae and many strains of pneumonococci.
What drugs are used to treat known or suspected staph infections?
I MET a NAsty OX (beta-lactamase resistant penicillins: METHicillin, NAFcillin, and OXacillin)
Ampicillin and amoxicillin (wide spectrum penicillinase-susceptible drugs) are used for?
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
TCP: Ticarcillin, Carbenicillin, Piperacillin (wide spectrum penicillinase-susceptible drugs) are useful for?
TCP: Takes Care of Pseudomonas

Pseudomonas, Enterobacter, and Klebsiella
What drug can be used with penicillin/ampicillin to have a synergistic effect against enterococcal and listerial infections (and broader gram negative coverage)?
Aminoglycosides
What are some allergic reactions with penicillin?
Drug-indcued Coombs' positive hemolytic anemia; urticaria, severe prutirtius, fever, joint swelling, nephritis, and anaphylaxis
What drug can result in pseudomembranous colitis?
Clindamycin, cephalosporins, or any penicillin (amoxicillin)
Oral penicillins can cause what GI upset?
Nausea and diarrhea, which may be caused by overgrowth of gram-positive organisms or yeast.
Cephalosporins bind with what?
Penicillin-binding protein
What type of drug is cephalosporins?
Bactericidal
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
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.
What is the third generation of cephalosporins and what are they effective against?
Ceftazidime, ceftriaxone, cefotaxime:

Most penetrate the BBB: meningitis.

Gram-negative, and pneumoniae, meningitis, and gonorrhea
What is the fourth generation of cephalosporins and what are they effective against?
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)
What is the allergic reaction against cephalosporins?
From skin rash to anaphylactic shock. Disulfiram-like reaction with ethanol, and nephrotoxicity
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?
NO
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?
Aztreonam. It is only effective against Gram-negative (including Pseudomonas) and NOT gram-positive
How does aztreonam work?
Binds to PBP and blocks peptidoglycan cross-linking.
What drug does not have a cross-allergen of penicillin?
Aztreonam.

Note: for penicillin-allergic PTs and those with renal insufficiency who cannot tolerate aminoglycosides.
What drug belongs to the class monobactam?
Aztreonam
Carbapenems are effective against?
Broad spectrum includes PRSP strains (not MRSA), gram-negatie rods, gram-positive cocci, and anaerobes.
What are the SE of carbapenems?
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.
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?
Clavulanic acid, sulbactam, tazobactam.

NOT against Enterobacter, Pseudomonas, and Serratia.
What inactivates bacterial beta-lactamases and added to piperacillin to broaden the spectrum against gram-negative and S. aureus infections?
Tazobactam
What drug inhibits transglycosylase (by binding to D-Ala-D-Ala terminal) an enzyme involved in peptidoglycan elongation and cross-linking?
Vancomycin
What is vancomycin used for?
Serious gram-positive resistant organisms, including S. aureus and Clostridium difficile (pseudomembranous colitis, but metronidazole is the DOC)
SE of vancomycin?
Nephrotoxicity, ototoxicity, thrombophlebitis, diffuse flushing--"red main syndrome"(due to histamine release) (can largely be prevented by pretreatment with antihistamines and slow infusion rate).
MOA of cephalosporins involves inhibition of?
Reactions involving transpeptidation; therefore, inhibiting peptidoglycan cross-linking.
Vancomycin inhibits?
Transglycoslase, preventing elongation of peptidoglycan by binding to D-alanine D-alanine to inhibit transpeptidation.
What is the DOC for gonorrhea?
Ceftriaxone
What is the DOC for Treponema pallidum?
Penicilling G.

If allergic, than doxycycline or tetracycline.
A debilitated PT has a fever from a skin infection, which yields gram-positive cocci. DOC is?
Nafcillin, which is resistant to penicillinases and S. aureus (but not MRSA) and common strep. Bacterial lesions are most likely staph or strep
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?
Aztreonam, which has no cross-reactivity between penicillins.
PT presents with S. pneumoniae, but is penicillin G resistant. What is the treatment?
Cefotaxime or ceftriaxone, which are the most active cephalosporins against penicillin-resistant pneumococci, and the addition of vancomycin or rifampin is recommended.
What is the reason for resistance to penicillin G?
Changes to penicillin binding protein.
Diptheroid-like gram-positive rods in the CSF in an elderly PT are indicative of what? What is the DOC?
Listeria monocytogenes. Ampicillin.

Listeria are common in neonates, the elderly PTs, and those who are immunocompromised.
PT with severe anaphylactic reaction to penicillin G, has enterococcal endocarditis. What is the DOC?
Vancomyin. Aminoglycoside may be added for synergistic effect.
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)
Piperacillin
Vancomycin is not susceptible to?
Penicillinase
Transpeptidase AKA?
penicillin-binding protein
What can be given with imipenem to increase its duration of action. It is the DOC for?
Cilastain, which inhibits renal dihydropeptidase I (inactivates imipenem in the renal tubules)

DOC for Enterobacter.

Note: cilastatin is ALWAYS given with imipenem.
What is similar to methicillin, in the sense that it is resistant to beta-lactamases?
Aztreonam
What are peptidoglycan and transpeptidases?
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.
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?
Very narrow spectrum penicillinase-resistant drugs. Treatment of staph infections.

Methicillin is hardly used due to nephrotoxic potential
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?
Imipenem, meropenem, and ertapenem.
What drug is less likely to cause seizures in the carbapenem class?
Meropenem. It is not metabolized by renal dehydropeptidases.
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.