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36 Cards in this Set
- Front
- Back
Clinically relevant antimicrobial activity: 1st Gen.
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+++ Gram +
+ Gram - 0 Pseudomonas 0/+ Anaerobes |
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Clinically relevant antimicrobial activity: 2nd Gen.
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++ Gram +
++ gram - 0 Pseudomonas ++ Anaerobes (cephamycins only) |
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Clinically relevant antimicrobial activity: 3rd Gen.
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+ Gram +
+++ Gram - +++ Pseudomonas (ceftazidime only) 0/+ Anaerobes |
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Clinically relevant antimicrobial activity: 4th Gen.
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++ Gram +
+++ Gram - +++ Pseudomonas 0/+ Anaerobes |
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progression of gram -/+ activity from 1st to 4th gen.
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2nd 3rd gen enhance gram - activity, but lost gram +
4th gen. retain gram - and improve gram + activity |
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What bacteria are cephalosporins NOT effective against?
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MRSA
enterococci Listeria Atypical: chlamydophila, mycoplasma, legionella |
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what are the atypicals?
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chlamydophila
mycoplasma legionella |
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Common 1st Gen. cephalosporins
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cephalexin (PO)
cefazolin (IV) |
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Spectrum of activity 1st Gen
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narrow, primarily Gram +
Gram + aerobes (staph, strep) Gram - aerobes (some enteric bacilli: Klebsiella, E. coli, Enterobacter, Proteus) Anaerobes: only PCN susceptible strains (oropharynx) |
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which Gram + aerobes do 1st gen. cephalosporins treat?
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primarily streptococci, staphylococci,
NOT MRSA, no enterococci |
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which gram - aerobes do 1st gen. cephalosporins treat?
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only certain enteri bacilli
(ex) Klebsiella, E. coli, Enterobacter, Proteus Poor Beta lactamase activity |
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which anaerobes do 1st gen. cephalosporins treat?
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limited to PCN susceptible strains such as those in oropharynx
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common 2nd gen. cephalosporins
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cefaclor (PO)
cefoxitin (IV) |
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which 2nd gen. cephalosporins are cephamycins?
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cefoxitin
cefotetan* defmetazole* *have NMTT side chain |
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unique feature of cephamycins (2nd gen)
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"anti aerobic"
enhanced anaerobic activity, enhanced gram - activity, decreased gram + activity compared to "true" 2nd gen cephalosporins |
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what is the NMTT side chain?
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increased PBP binding...
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undesired effects of NMTT side chain
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inhibit vit K epoxide reductase (bleeding)
inhibit aldehyde dehydrogenase (cant drink EtOH) |
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Spectrum of activity 2nd Gen cephalosporins
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broader in spectrum, improved gram - activity compared to 1st gen.
Gram + aerobes: Primarily streptococci and staphylococci, not quite as active as first-gen. agents Gram - aerobes: Improved Gram-negative activity against enteric bacilli (e.g. E. coli, Klebsiella, Enterobacter, Proteus) Also good activity against some selected β-lactamase producing organisms, e.g. Haemophilus influenzae, Moraxella catarrhalis Anaerobes: Limited overall Exception: cephamycins have best activity of cephalosporin class, including Bacteroides fragilis |
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what gram + aerobes do 2nd gen cephalosporins treat
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Primarily streptococci and staphylococci, not quite as active as first-gen. agents
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what gram - aerobes do 2nd gen. cephalosporins treat?
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Improved Gram-negative activity against enteric bacilli (e.g. E. coli, Klebsiella, Enterobacter, Proteus)
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what beta lactamase producing microbes to 2nd gen. cephalosporins treat?
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some selected β-lactamase producing organisms, e.g. Haemophilus influenzae, Moraxella catarrhalis
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what anaerobes do 2nd gen. cephalosporins treat?
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Limited overall
Exception: cephamycins have best activity of cephalosporin class, including Bacteroides fragilis |
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common 3rd gen. cephalosporins
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ceftazidime (IV)
cefpodoxime proxetil* (PO) cefditoren pivoxil* (PO) *prodrug |
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spectrum of activity 3rd gen. cephalosporins
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BROAD spectrum, excellent gram - activity
much more stable against beta lactamases produced by gram +/- Useful for broad range of community-acquired and nosocomial infections (IV agents) due to good Gram-positive and excellent Gram-negative activity Gram + aerobes: primarily streptococci and staphylococci, less active than other generations but still clinically useful Gram - aerobes: Active against wide range of organisms, but still subject to inactivation by many β-lactamases Excellent against Enterobacteriaceae Also excellent against H. influenzae, M. catarrhalis, Neisseria Ceftazidime has good activity against P. aeruginosa Anaerobes: Limited to oropharyngeal strains |
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which gram + aerobes do 3rd gen. cephalosporins treat?
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primarily streptococci and staphylococci, less active than other generations but still clinically useful
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which gram - aerobes do 3rd gen. cephalosporins treat?
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Gram - aerobes: Active against wide range of organisms, but still subject to inactivation by many β-lactamases
Excellent against Enterobacteriaceae Also excellent against H. influenzae, M. catarrhalis, Neisseria |
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what microbe is ceftazidime good against?
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Pseudomonas aerigunosa
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what anaerobes do 3rd gen. cephalosporins treat?
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limited to oropharyngeal strains
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what is the 4th gen. cephalosporin?
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cefepime (IV)
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spectrum of activity of 4th gen. cephalosporin cefepime
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Has good Gram-positive activity, similar to first- and second-generation agents
Has excellent Gram-negative activity, including P. aeruginosa More stable than third-generation agents to many β-lactamases, particularly those produced by Enterobacteriaceae |
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safety/side effects of cephalosporins
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Cephalosporins are considered to be among the safest of antimicrobial and are associated with few serious adverse effects
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side effect profile cephalosporins
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generally similar to penicillins
PCN SE: Gastrointestinal: nausea, vomiting, abdominal pain, diarrhea (20-30% incidence with ampicillin) Skin: rash most commonly reported with ampicillin and amoxicillin (5-10% vs. 1-2% with other penicillins) Rash during ampicillin administration does NOT necessarily signify a serious hypersensitivity reaction Hematologic: neutropenia, prolonged bleeding times, thrombocytopenia CNS: mental status changes, seizures in high-risk patients Electrolytes: hypokalemia, hypernatremia Hepatic: transaminase elevations Renal: interstitial nephritis, acute tubular necrosis Clostridium difficile-associated disease Caused by disruption of normal bowel flora Allows overgrowth of Clostridium difficile C. difficile causes infection of colon Toxin-mediated inflammation, diarrhea, mucosal injury Significant morbidity and mortality Associated with nearly all antibiotic classes, especially broad-spectrum agents with anaerobic activity Superinfection: Antibiotic-induced suppression of susceptible organisms allows growth of different and/or less susceptible organisms Leads to new infections with more resistant bacterial organisms as well as fungal organisms, e.g. Candida Most commonly associated with broad-spectrum antibiotics |
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hypersensitivity of cephalosporins
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Hypersensitivity reactions occur in 1-3% of patients
Reactions range from rash to anaphylactic reactions Approximately 7-10% of patients with true penicillin allergy will have cross-sensitivity to cephalosporins Many patients will develop rash to penicillins (e.g. ampicillin), does not necessarily contraindicate cephalosporin administration but care should be exercised |
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unique side effect of ceftriaxone
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billiary sludging
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unique side effect of NMTT side chain cephalosporins
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hypothrombinemia (increased bleed time)
disulfiram-like rxns when used in pts. w/ recent EtOH use |
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which cephalosporins have NMTT side chain? what is their generation?
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2nd Gen:
cefamandole cefotetan (cephomycin) cefmetazole (cephomycin) 3rd Gen: cefoperazone |