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40 Cards in this Set
- Front
- Back
Explain the mechanism of cross-linking in the formation of the peptidogylcan cell wall
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The enzyme transpeptidase links adjacent strands by combining the string of 5 glycines at the D-ala D-ala terminal end of the adjacent glycopeptide
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What is the function of beta-lactam antibiotics and what must the organism be doing in order for the drugs to work?
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Beta-lactams act on growing bacteria by binding and irreversibly inhibiting penicillin binding proteins such as transpeptidase
They also activate autolysins which degrade cell walls |
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What are penicillin binding proteins?
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Proteins in the plasma membrane of the bacteria which are responsible for the synthesis and maintenance of the cell wall
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What are the three mechanisms by which resistance to beta-lactam antibiotics occurs?
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1) beta lactamase production
2) decreased pores for diffusion of the drug into the cell 3) alteration of penicillin binding proteins conferring low affinity for beta lactams |
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What organisms alter their penicillin binding proteins as means of resistance?
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staph aureus (MRSA) and penicillin resistant strept pneumo (MDRSP)
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Describe the important pharmacokinetic parameters of penicillin G
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It is destroyed by the acid in the stomach and only 30% of an oral dose is absorbed
Food interferes with its absorption 99% of an IM dose is eliminated in the kidney |
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What drug is given with penicillin G and why?
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Probenecid is given to to prolong the duration of action by blocking penicillin's active transport in the proximal tubule
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What is the repository form of penicillin G?
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It is a salt that includes procaine and benzathine, given IM which slows absorption from the injection site
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What are the differences between penicillin G and V
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V - resistant to acid and preferred oral form
G - inactivated by acid, given in salt form as IV or IM administration |
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What are the penicillinase resistant penicillins and what are they used to treat?
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They are used to treat penicillinase producing staphylocci
1) Methicillin 2) Oxacillin 3) cloxacillin 4) Dicloxicillin 5) nafcillin |
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What are the extended spectrum penicillins and what organisms can they cover?
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They cover gram positives and some strains of e. coli, H. influenza, salmonella, shigella, and proteus
1) ampicillin 2) bacampicillin 3) amoxicillin |
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Describe the differences in the extended spectrum penicillins
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ampicillin causes diarrhea due to incomplete absorption, but bacampicillin doesn't
Amoxicillin is better absorbed but can't cover shigella |
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What are the anti-pseudomonal penicillins?
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1) carbenicillin
2) ticarcillin 3) piperacillin |
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Describe the spectrum of ticarcillin
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Similar to ampicillin and also effective against proteus, enterobacter, and pseudomonas
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What antibiotic is the most potent anti pseudomonal and can also be used against klebsiella?
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piperacillin
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What are the beta-lactamase inhibitors and with what drugs are they commonly given?
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1) clavulanic acid
2) sulbactam 3) tazobactam They are commonly given with amoxicillin, ampicillin, piperacillin, and ticarcillin |
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Describe the hypersensitivity reactions that can occur with penicillins
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1) Reactions range from mild rash to anaphylaxis
2) immune complexes producing serum sickness 3) hemolytic anemia 4) convulsions at high doses |
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What adverse effects associated with carbenicillin and ticarcillin?
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They bind to the ADP receptor on platelets and inhibit aggregation and coagulation
They have a high salt content and can cause electrolyte disturbances |
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What happens in patients with mononucleosis who receive amp/amoxicillin?
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They develop a rash that is not immune mediated
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What is the mechanism of cephalosporin killing?
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They inhibit cell wall synthesis and are bacterocidal
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What enzymes are effective against cephalosporins? Which are not?
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They are resistant to gram positive penicillinase
They are hydrolyzed by cephalosporinase and broad spectrum beta lactamases |
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Which cephalosporins do not penetrate the blood brain barrier?
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1st and 2nd generation
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What are the first generation cephalosporins and what organisms can they be used to kill?
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1) cephalexin
2) cefazolin They are used to kill E. coli, K. pneumonia, proteus, gram positive cocci Cannot kill: MRSA, listeria, enterococci, penicillin resistance strep |
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What are the second generation cephalosporins and what are they used to kill?
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1) cefuroxime
2) cefaclor 3) cefoxitin They are active against E. coli, Klebsiella, proteus, H. influenza, and morexella 4) cefotetan - also can kill bacteroides and is more resistant to beta lactamase |
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What are the third generation cephalosporins and for what are they used?
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1) cefotaxime
2) ceftazidine 3) ceftriaxone They have expanded gram negative spectrum and some penetration into the CNS |
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What are the fourth generation cephalosporins and for what are they used?
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1) cefepime
Comparable to third generation but more resistant to beta lactamases |
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As you proceed from 1st to 4th generation cephalosporins, what patterns emerge?
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They are able to move across the outer membrane of gram negatives better and stability towards gram negative beta lactamases increases
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In whom are cephalosporins contraindicated?
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In those who have experienced an immediate or other serious allergic reaction to penicillin
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The methylthiotetrazole side chain of some cephalosporins can lead to what adverse effects?
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1) blood coagulation problems (interferes with Vit K)
2) disulfuram-like effects in people who consume alcohol |
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What are the drugs in the carbepenem class of antibiotics?
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1) imipenem
2) meropenem 3) ertapenem |
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What is always administered with imipenem and why?
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Cilistatin is given to prevent metabolic inactivation of imipenem by the enzyme dehydropeptidase in the kidney
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What drug has the widest spectrum of any beta-lactam?
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imipenem
However, MRSA and enterococcus are resistant |
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What are the side effects of imipenem?
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The main side effect is seizures
they are also cross-resistant to cephalosporins and penicillins |
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What is the drug in the monobactam class and for what is it used?
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Aztreonam is only useful against aerobic gram negatives and has excellent stability against beta lactamase
Main use is nosocomial gram negatives |
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What drug is a non-beta-lactam cell wall synthesis inhibitor and how does it work?
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Vancomycin binds to the terminal D-ala D-ala portion of the peptidoglycan wall, inhibiting transglycosylase and preventing elongation of the cell wall or cross-linking
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How is enterococci resistance against vancomycin mediated?
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They substitute D-lac for the terminal D-ala and vancomycin cannot find its binding site
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What is observed in patients who are rapidly infused with Vancomycin?
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Flushing of the upper body or neck (red neck syndrome), caused by histamine release from mast cells
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What are the uses of vancomycin?
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MRSA, antibiotic induced C-diff, streptococcal endocarditis
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What are adverse effects of vancomycin?
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1) nephrotoxicity
2) ototoxicity 3) thrombophlebitis 4) red neck syndrome |
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What are the miscellaneous inhibitors of cell wall synthesis?
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1) bacitracin
2) cycloserine 3) fosfomycin |