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187 Cards in this Set
- Front
- Back
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What is the MOA of b-lactams?
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inhibition of cell wall synthesis (irreversible binding); prevents crosslinking of peptidoglycan
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B-lactams are bactericidal or bacteriostatic?
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bactericidal
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b-lactams are time dependent or concentration dependent?
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time dependent
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What are the requirements for susceptibility to b-lactams?
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actively growing and making a cell wall, not producing inactivating enzymes, lactams must be able to enter porin channels to reach peptidoglycan layer (gram -)
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What organisms do b-lactams offer no coverage for?
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atypicals, MRSA (except ceftaroline - 5th gen cephalosporin)
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What anti-hyperlipidemic drug has a beta-lactam ring?
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ezetimibe
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What structure do b-lactams bind to kill bacteria?
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penicillin binding proteins
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Who discovered penicillin?
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alexander flemming (1928)
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What are the two types of natural pcn?
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PCN G and PCN V (VK)
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What are the routes for PCN G?
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IM and IV (although does come oral but not in notes)
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What are the routes for penicillin V?
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PO`
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What does the short acting form of PCN G have?
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procaine
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What does the long acting form of PCN G have?
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benzathine
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What is the dosing unit for pcn?
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million units
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Gram stain for streptococci and PCN usage?
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Gram +, used frequently for streptococci
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Gram stain for staphylococci and PCN usage?
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gram +, has resistance issues to regular PCN
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Gram stain for enterococci and PCN usage?
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gram +, has resistance issues to regular PCN
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Gram stain for streptococcus pneumoniae and PCN usage?
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gram +, only used in highly susceptible strains
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Gram stain for N. meningitidis and PCN usage?
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gram - cocci and frequently used
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What anaerobes is natural PCN used for?
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Peptostreptococcus sp, and Actinomyces
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What spirochete is natural PCN used for?
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Treponema pallidum (syphillis)
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What are the common clinical uses for natural PCN?
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Upper respiratory tract infections *URI* (strep throat), meningitis, skin infections (S. pyogenes with clindamycin added), endocarditis (with gent), bone infections
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What is the drug of choice for syphillis?
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PCN (all stages of disease)
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What is the dosing frequency for PCN?
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q 4 to 6 h
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LA form of PCN contains?
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benzathine
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CR form of PCN contains?
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mix of benzathine and procaine
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What are the resistance mechanisms to b-lactams?
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-overproduction of PBPs,
-production of PBPs with reduced affinity to PCN or beta-lactams (usually gram +) -B-lactam inactivatin enzymes -inactivation of porins (gram -) -efflux pumps (gram -) |
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What are the anti-staphylococcal PCNs / penicillinase-resistant PCNs?
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Oxacillin, nafcillin, dicloxacillin, cloxacillin, methicillin (last two not on market anymore)
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What are the routes of admin for oxacillin?
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IV, PO
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What are the routes of admin for nafcillin?
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IV
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What are the routes of admin for Dicloxacillin?
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PO
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What addition was made to the anti-staphylococcal PCNs (chemically) to be reistant to b-lactamases?
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addition of large R group to sterically block b-lactamases
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What is the drug of choice for MSSA?
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anti-staphylococcal PCNs (oxacillin, nafcillin, dicloxacillin)
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What to treat Streptococci with, Oxacillin or PCN?
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PCN
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What is the antimicrobial spectrum for anti-staphylococcal pcns?
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staphylococci (as the majority are PCN resistant today), streptococci, limited anaerobic activity
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What organisms does anti-staphylococcal pcns not have coverage against?
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Enterococcus, gram - organisms
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What are the two aminopenicillins?
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Ampicillin, amoxicillin
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Route of admin for ampicillin?
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IV, PO
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Route of admin for amoxicillin?
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PO
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Greater stability in gastric acid, amox or amp?
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amox
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Advantage of aminopenicillins over anti-staphylococcal pcns?
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Gram - coverage with aminopenicillins
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Antimicrobial spectrum coverage of aminopenicillins?
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-Gram + (Streptococci and Enterococci, Listeria monocytogenes; DOES NOT cover Staph well)
- Gram - (E. coli, Proteus mirabilis, H. influenzae, Salmonella sp, Shigella sp) -Some anaerobic coverage |
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What is the drug of choice for Enterococci?
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Aminopenicillins
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What is the drug of choice for Listeria?
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aminopenicillins
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What is the drug of choice for otitis media?
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aminopenicillins (specifically high dose Amoxicillin)
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What caution should be taken with administration of ampicillin?
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ampicillin has a high level of sodium and should use caution with high dose and long term use or in selected populations
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What are the carboxypenicillins?
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Carbenicillin, Ticarcillin
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What are the urediopenicillins?
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Azloxillin, Mezocillin, Piperacillin
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What are the carboxypenicillins and ureodiopenicillins referred to as?
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extended spectrum penicillins
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What is the antimicrobial spectrum for the extended spectrum penicillins?
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increased gram - including pseudomonas, less activity with staph, strep and entero; excellent anaerobe activity
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What is more potent for Pseudomonas and Enterococci, Piperacillin or Ticarcillin?
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Piperacillin
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What is more potent for Stenotrophomonas maltophilia (gram -) , Piperacillin or Ticarcillin?
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Ticarcillin
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Name the b-lactamase inhibitors
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Clavulanic acid, sulbactam, tazobactam
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What organism is sulbactam have activity against?
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Acinetobacter sp
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What are the side effects of Clavulanic acid?
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Gi sides, cholestasis
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What is another name for amoxicillin/clavulanic acid? Route of admin?
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Augmentin, PO
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What is another name for ampicillin/sulbactam? Route of admin?
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Unasyn, IV
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What is another name for Ticarcillin/clavulanic acid? Route of admin?
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Timentin, IV
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What is another name for Piperacillin/Tazobactam? Route of admin?
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Zosyn, IV
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MOA of b-lactamase inhibitors?
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Suicide binding (irreversible)
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Does ampicillin cover MSSA?
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no
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Does amoxicillin cover MSSA?
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no
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Does Augmentin cover MSSA?
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yes
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Does Unasyn cover MSSA?
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yes
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What is the difference between the MOA in MRSA resistance compared to MSSA?
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MSSA uses b-lactamases but MRSA has a change in the PBP so b-lactamase inhibitors won't work
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Augmentin or Unasyn work for S. pneumoniae?
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no
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What is the antimicrobial spectrum coverage of Augmentin and Unasyn?
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-Expanded Gram + (MSSA)
-Expanded Gram - (Citrobacter, Enterobacter, Serratia, H influenzae, M catarrhalis - last two mislisted in the notes) -Better anaerobic coverage (Bacteroides sp) |
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"Clinical Pearl" type of infections that b-lactam/ b-lactamases augmenting and unasyn are used for?
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nosocomial acquired pneumonia, otitis media, sinusitis, skin and bone infections, ob/gyn, infections of (or near) mouth, intrabdominal infections
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Drug of choice for otitis media?
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Amox mono (not augmentin as clavulanic acid causes increased diarrhea and cholestasis)
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What is the antimicrobial spectrum for b-lactam/b-lactamase inhibitors timentin and zosyn?
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What augmentin or unasyn covers:
-Expanded Gram + (MSSA) -Expanded Gram - (Citrobacter, Enterobacter, Serratia, H influenzae, M catarrhalis - last two mislisted in the notes) -Better anaerobic coverage (Bacteroides sp) PLUS pseudomonas, serratia, acinetobacter |
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"Clinical Pearls" type of infections for zosyn?
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nosocomial infections +/- AG FQ, respiratory, intrabdominal, diabetic foot, ssti
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"Clinical Pearls" type of infections for timentin?
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-2nd line for Stenotrophomonas maltophilia (cf patients)
-rarely used due to Na overload, teratogenicity, decreased platelet aggregation (increased chance of bleeding) |
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What PCN has the best coverage against pseudomonas: oxacillin, ampicillin, piperacillin, penicillin?
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piperacillin
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Which b-lactam group does not require renal adjustments?
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anti-staphylococcal; mostly excreted in bile
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Which pcn groups have rash associated with them?
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all
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Which pcn groups have allergic reactions associated with them?
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all
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Which pcn groups have diarrhea associated with them?
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All, natural pcn sometimes not though; ampicillin has higher than normal
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Which pcn groups have increased liver enzymes associated with them?
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pcn, amino-pcn, anti-staph pcn
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Which pcn groups have interstitial nephritis associated with them?
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pcn and anti-staph pcn (methicillin)
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Which pcn groups have extravasation associated with them?
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Nafcillin
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Which pcn groups have seizure associated with them?
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PCN, amino-pcn
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What are the b-lactams that have a decrease in absorption when ingested with food?
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PCN V, amox, dicloxacillin, cloxacillin
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PCNs that strongly interact with warfarin?
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Nafcillin/dicloxacillin (strong cyp3a4 inducers)
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PCNs that interact with birth control?
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PCN and aminopenicillins (but really all PCNs)
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What is the drug interaction with probenecid and PCN?
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inhibits tubular secretion of PCN and increases half life
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PCN anaphylaxis is mediated by which immunoglobulin?
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IgE
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PCN allergy crossreactivity with 1st gen cephalosporins?
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10%
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PCN allergy crossreactivity with 2nd and 3rd gen cephalosporins?
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1-5%
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PCN allergy crossreactivity with carbapenems?
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5%
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PCN allergy crossreactivity with monobactams?
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Rare
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What constitutes an immediate PCN allergy?
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- <1h
-anaphylaxis, wheezing, bronchospasm, angioedema, hypotension, urticaria -IgE mediated |
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What constitutes an accelerated PCN allergy?
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- 1-72h
-urticaria, fever, laryngospasm, angioedema -IgE mediated |
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What constitutes a delayed PCN allergy?
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-rash, interstitial nephritis, hemolytic anemia, stephens-jonson syndrome, drug fever, neutropenia, thrombocytopenia
-IgG and IgM mediated |
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What agent does not beed to be renally adjusted: ampicillin, nafcillin, piperacillin/tazobactam, tazobactam?
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nafcillin
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What organisms in our notes do cephalosporins have no activity against?
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enterococcus, lsteria, atypicals
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Only 5th gen cephalosporin?
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ceftaroline
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What are the 1st gen cephalosporins?
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IV
-Cefazolin, cephalothin, cephadrine PO -Cephalexin, cefadroxil (only generation to have ceph instead of all "cef") |
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What is another name for ancef? what gen?
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cefazolin, 1st gen
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What is another name for cephalexin? what gen?
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keflex, 1st gen
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what is another name for duricef? what gen?
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cefadroxil, 1st gen
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What is the spectrum of activity for the first gen cephalosporins?
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-Staph (MSSA and some coag-neg staph
-Streptococci, but not S/ pneumoniae -Limited gram - (only enterobacteriaceae that don't make b-lactamases) -no anaerobic (except peptostreptococcus) |
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"clinical pearl" infections treated with 1st gen cephalosporins?
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-SSTI
-uncomplicated UTI -surgical prophylaxis -Lack of coverage for S. pneumoiae, H influenzae, and M catarrhalis limits use in respiratory tract infections, sinusitis, and otitis media |
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What are the 2nd gen cephalosporins?
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IV
-Cefuroxime (zinacef), cefmetazole PO -Cefuuroxime (ceftin, zinacef), cefprozil (cefzil), cefaxlor (ceclor), loracarbef (lorabid) |
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What is the spectrum of activity for the second gen cephalosporins?
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-increased gram - activity compared to 1st gen
-decreased gram + compared to first gen -limited anaerobic |
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What are the cephamycins?
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special 2nd gen cephs, Cefoxitin (mefoxin) and Cefotetam(cefotan); jave anaerobic coverage
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What is the spectrum of activity for cephamycins?
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Anaerobic coverage, especially gram - Bacteroides
decreased gram + coverage esp MSSA |
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What are the general uses for 2nd gen cephalosporins today?
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mild to moderate community acquired infections
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What are the uses for cephamycins?
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surgical prophylaxis, intrabdominal, pelvic, ob.gyn infections
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What are the 3rd gen cephalosporins?
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IV
-ceftriaxone (rocephin), cefotaxime (claforan), ceftizoxime (ceftizox), ceftazidime (fortaz), cefoperazone |
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What is the spectrum of activity for 3rd gen cephalosporins?
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-Enhanced gram - activity (enterobacteriaecae, Enterobacter, Citrobacter, Providencia)
-increased activity against H influenzae and M catarrhalis -!!Pseudomonas activity: Ceftazidime only -Limited gram + activity S. Pneumoniae (ceftriaxone and cefotaxime only - have identical coverage) |
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Dosing schedule for ceftiaxone?
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once daily due to protein binding
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Drug of choice for inpatient community acquired pneumonia?
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ceftriaxone/cefotaxime (3rd gen) +/- macrolide
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Which 3rd gen cephalosporin should not be used in neonates? Why? Which should be used?
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Ceftriaxone should not be used due to kernicterus in less than 3 months old; should use Cefotaxime instead
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Drug of choice for gonorrheal infections?
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ceftriaxone/cefotaxime
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Which cephalosporin should be used for S. pneumoniae meningitis?
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Ceftriaxone/cefotaxime
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What are the oral 3rd gen cephalosporins?
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Cefixime(suprax), cefpodoxime(vantin), ceftibuten(cedax), cefdinir(omnicef)
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What is the microbial spectrum for 3rd gen ceph orals?
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same as 3rd gen iv but no pseudomonas; cefixime and ceftibuten lack Staph activity
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Primary use for 3rd gen ceph orals?
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URI or Otitis media; can be used for STDs (gonorrhea with cefixime)
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What are the 4th gen cephalosporins?
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cefepime (maxipime)
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What is the microbial spectrum for the 4th gen cephs?
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-broadest of cephs (zqitterions)
-increased gram neg including pseudomonas -increased gram + including S pneumoniae -stable aginst many b-lactamases (can be used on Enterobacter, Citrobacter, Proteus vulgaris) -Minimal anaerobic coverage |
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What is the drug of choice in febrile neutropenia?
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cefepime(maxipime) (4th gen ceph)
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Possible uses of cefepime other than febrile neutropenia?
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meningitis, nosocomial infections (still need anaerobe coverage)
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What are the 5th gen cephalosporins?
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ceftaroline (teflaro) IV
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FDA indications for ceftaroline?
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-SSTI caused by MSSA, MRSA, Streps, E coli, Klebsiella
-CAP caused by MSSA, not MRSA, Streps, H flu, Klebsiella |
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What is ceftobiprole?
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unapproved cephalosporin with MRSA, pseudomonas, enterococcus, and increased S. pneumoniae coverage
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1st gen ceph absorption?
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90%
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2ng gen ceph absorption?
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90%
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3rd gen ceph absoprtion?
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poor, 25-40%
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4th gen ceph absorption?
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iv only
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5th gen ceph absorption?
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iv only
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what is the distribution of 1st gen ceph?
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well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
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what is the distribution of 5th gen ceph?
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well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
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what is the distribution of 4th gen ceph?
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well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
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what is the distribution of 3rd gen ceph?
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well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
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what is the distribution of 2nd gen ceph?
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well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
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2nd gen ceph dist into meningitis?
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some with cefuroxime
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3rd gen ceph dist into meningitis?
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high
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4th gen ceph dist into meningitis?
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high
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5th gen ceph dist into meningitis?
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high
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1st gen ceph excretion?
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renal
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2nd gen ceph excretion?
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tubular secretion
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3rd gen ceph excretion?
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renal except ceftriaxone which is biliary and thus no renal adjustment
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4th/5th gen ceph excretion?
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tubular secretion
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All ceph % metabolized?
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<10%
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Half life on all cephs?
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1-2 h except ceftriaxone which is 6h
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What are the common adverse rxns to cephs?
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rash, diarrhea, allergic rxns, c. diff (decreased rxns in general compared to pcns with trend being 1st gen > 2nd>3rd>4th/5th)
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What are the rare adverse rxn to cephs?
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seizures, hematologic issues interstitial nephritis
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Which cephs have a methylthiotetrazole side chain? what is the significance?
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Cefotan, Cefmandole, cefoperazone, cefmetazole (It apPERs the MAN has a TAN, or is it a METAZtasis? -melanoma) Causes vit k antagonism and disulfiram type rxns
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Cephs and food interactions?
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food can delay the rate of absorption
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Cephs and drug interactions?
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MMT-side chain = warfarin &eoth; probenecid causes decrease in tubular secretions
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What is the broadest abx spectrum beta lactams?
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carbapenems
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What coverage is included in general with carbapenems?
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Gram - including MDR organisms (Pseudomonas, Acinetobacter, ESBLs), Gram + except MRSA and E. faecium (VRE usually), and anaerobes (except C. diff)
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What are the four carbapenems?
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ertapenem, imipenem/cilastin, meropenem, doripenem
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What organisms does ertapenem not cover?
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Acinetobacter, Pseudomonas, Enterococci (but it is highly protein bound and only needs qd dosing)
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What is the Drug of choice for extended spectrum beta lactamases?
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carbapenems
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What type of excretion are the carbapenems?
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renal and need renal adjust.
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What is the purpose of cilastin?
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protects imipenem from inactivation by renal dehydropeptidase 1 and protects kidney from metabolites
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What is the half life for the carbapenems?
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1h for all except ertapenem which is 4h (and gets 1g IV qd)
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What are the drug interactions for carbapenems?
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decreases levels of valproic acid
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What are the adverse rxns associated with carbapenems?
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seizures (imipenem>meropenem/ertapenem>doripenem), and have issues with superinfections due to lack of coverage for VRE, stenotropomonas maltophilia, MRSA, Candida (but has a lower propensity for C diff infections than other agents)
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What is the coverage with aztreonam?
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gram - aerobes only; limited acitivity against Pseudomonas, enterobacter, citrobacter; inactive against acinetobacter and stenotrophomonas
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What class is aztreonam?
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monobactam
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What is the common use for aztreonam?
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usually when pt has PCN allergy. Can be used in menigitis, but requires renal adj
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Cross resistance with aztreonam?
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ceph resistance (inactive against ESBL_
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What is the brand name for aztreonam?
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azactam
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What is the brand name for ertapenem?
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invanz
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what is the brand name for inipenem/cilastin?
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primaxin
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what is the brand name for meropenem?
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merrem
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what is the brand name for doripenem?
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doribax
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what is the brand name for ceftaroline? gen?
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teflaro; 5th
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what is the brand name for cefepime? gen?
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maxipime; 4th
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what is the brand name for cefixime? gen?
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suprax; 3rd
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what is the brand name for cefpodoxime? gen?
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vantin; 3rd
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what is the brand name for ceftibuten? gen?
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cedax; 3rd
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what is the brand name for cefdinir? gen?
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omnicef; 3rd
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what is the brand name for ceftriaxone? gen?
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rocephin; 3rd
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what is the brand name for cefotaxime? gen?
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claforan; 3rd
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what is the brand name for ceftizoxime? gen?
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ceftizox, 3rd
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what is the brand name for ceftazidime? gen?
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fortaz, 3rd
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what is the gen for cefoperazone?
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3rd
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What is the brand name for cefuroxime? gen?
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zinacef, 2nd
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what is the gen for cefmetazole?
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2nd
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what is the brand name for cefazolin, gen?
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ancef, 1st
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what is the brand name for cephalexin, gen?
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1st, keflex
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what is the brand name for cefadroxil, gen?
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duricef, 1st
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what is the gen for cephalothin?
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1st
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what is the gen for cephadrine?
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1st
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