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Pharm 43
Beta-lactam and other cell wall-active antibiotics
116
Pharmacology
Professional
08/31/2011

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Term
Which classes of antibiotics prevent bacterial cell wall synthesis by binding to and and inhibiting cell wall transpeptidases?
Definition
penicillins, cephalosporins, carbapenems, monobactams
Term
Which drugs inhibit cell wall synthesis by binding to the D-ala D-ala terminus of nascent peptidoglycan?
Definition
glycopeptides
Term
Which drugs bind to cell membrane, causing depolarization and rapid cell death?
Definition
lipopeptides
Term
penicillin G: MOA?
Definition
prevent bacterial cell wall synthesis by binding to and and inhibiting cell wall transpeptidases
Term
What are the effects of penicillins, cephalosporins, carbapenems and monobactams?
Definition
rapid bactericidal activity against susceptible bacteria
Term
What are the clinical applications of Pcn G?
Definition
streptococcal infections, meningococcal infections, neurosyphilis
Term
What drug can be used for streptococcal infections, meningococcal infections, and neurosyphilis?
Definition
PCN G
Term
Name the drug: IV, rapid renal clearance (half life 30min) so requires frequent dosing every 4 hr, Tox: immediate hypersensitivity, rash seizures
Definition
PCN G
Term
Which drug can cause immediate hypersensitivity, rash and seizures?
Definition
PCN G
Term
How does PCN V compare to PCN G?
Definition
oral, low systemic levels limit widespread use
Term
which penicillin is taken orally and reaches low systemic levels which limit widespread use?
Definition
PCN V
Term
How do benzathine PCN and procaine PCN compare to PCN G?
Definition
intramuscular, long-acting formulations
Term
which PCNs can be given intramuscularly and have long-acting formulations?
Definition
benzathine and procaine PCN
Term
How do nafcillin and oxacillin compare to PCN G?
Definition
IV, added stability to staphylococcal B lactamase, biliary clearance
Term
Which PCNs are given IV, have added stability to staphylococcal B lactamase and biliary clearance?
Definition
nafcillin, oxacillin
Term
How do ampicillin, amoxicillin, ticaricillin and piperacillin compare to PCN G?
Definition
greater activity against gram-negative bacteria, addition of B-lactamase inhibitor restores activity against many B-lactamase-producing bacteria
Term
Which PCNs have greater activity against gram-negative bacteria, addition of B-lactamase inhibitor restores activity against many B-lactamase-producing bacteria
Definition
ampicillin, amoxicillin, ticarcillin, piperacillin
Term
What are the 1st gen cephalosporins?
Definition
cefazolin, cephalexin, etc
Term
cefazolin, cephalexin are which generation?
Definition
1st
Term
Which cephalosporins are 2nd gen?
Definition
Cefuroxime, cefotetan, cefoxitin
Term
Cefuroxime, cefoxitin, cefotetan are which generation?
Definition
2nd
Term
Ceftriaxone, cefotaxime, ceftazidime are which generation?
Definition
3rd
Term
Name the 3rd gen cephalosporins
Definition
Ceftriaxone, cefotaxime, ceftazidime
Term
Cefazolin: MOA?
Definition
prevents bacterial cell wall synthesis by binding to and inhibiting cell wall transpeptidases
Term
What are the clinical applications for cefazolin?
Definition
skin and soft tissue infections, urinary tract infections, surgical prophylaxis
Term
Which drug is used for skin and soft tissue infections, urinary tract infections, surgical prophylaxis
Definition
cefazolin
Term
name the drug: IV admin, renal clearance (half life 1.5 hr), dosed every 8h, poor penetration into CNS, tox: rash, drug fever
Definition
cefazolin
Term
Which drug can cause rash and drug fever?
Definition
cefazolin
Term
How does cephalexin compare to cefazolin?
Definition
oral, 1st gen, skin and soft tissue infections and UTI
Term
name the cephalosporin: oral, 1st gen, skin and soft tissue infections and UTI
Definition
cephalexin
Term
Describe cefuroxime
Definition
oral and IV, 2nd gen, improved activity for pneumococcus and H flu
Term
Name the cephalosporin: oral and IV, 2nd gen, improved activity for pneumococcus and H flu
Definition
cefuroxime
Term
Describe cefotetan / cefoxitin
Definition
IV, 2nd gen, activity against Bacteroides fragilis allows for use in abdominal/pelvic infections
Term
Name the cephalosporin: IV, 2nd gen, activity against Bacteroides fragilis allows for use in abdominal/pelvic infections
Definition
cefotetan, cefoxitin
Term
Describe ceftriaxone
Definition
IV, 3rd gen, mixed clearance with long half life (6hrs), good CNS penetration, many uses including pneumonia, meningitis, pyelonephritis, and gonorrhea
Term
name the cephalosporin: IV, 3rd gen, mixed clearance with long half life (6hrs), good CNS penetration, many uses including pneumonia, meningitis, pyelonephritis, and gonorrhea
Definition
ceftriaxone
Term
Describe cefotaxime
Definition
IV, 3rd gen, similar to ceftriaxone but clearance is renal and half life is one hour
Term
name the cephalosporin: IV, 3rd gen, similar to ceftriaxone but clearance is renal and half life is one hour
Definition
cefotaxime
Term
Describe ceftazidime
Definition
IV, 3rd gen, poor gram-positive activity, good activity against pseudomonas
Term
name the cephalosporin: IV, 3rd gen, poor gram-positive activity, good activity against pseudomonas
Definition
caftazidime
Term
Name a 4th gen cephalosporin
Definition
cefepime
Term
Describe cefepime
Definition
IV, 4th gen, broad activity with improved stability to chromosomal B-lactamase
Term
name the cephalosporin: IV, 4th gen, broad activity with improved stability to chromosomal B-lactamase
Definition
cefepime
Term
What are the investigational cephalosporins that are administered IV, are active against methicillin resistant staphylococci, and have broad gram-negative activity?
Definition
ceftobiprole, ceftaroline
Term
What type of drug is imipenem-cilastatin?
Definition
carbapenem
Term
imipenem-cilastatin: MOA?
Definition
prevents cell wall synthesis by binding and inhibiting transpeptidases
Term
What are the applications for imipenem-cilastatin?
Definition
serious infections such as pneumonia and sepsis
Term
Name the drug: IV, renal clearance (half life 1 hr), dosed every 6-8hr, component of drug prevents hydrolysis by renal dehydropeptidase, tox: seizures especially in renal failure or with high doses
Definition
imipenem-cilastatin
Term
Why is cilastatin added to imipenem-cilastatin?
Definition
to prevent hydrolysis by renal dehydropeptidase
Term
which drug can cause seizures especially in high doses?
Definition
imipenem-cilastatin
Term
What drug is used for serious infections such as pneumonia and sepsis?
Definition
imipenem-cilastatin
Term
Describe meropenem / doripenem
Definition
IV, similar activity to imipenem, stable to renal dehydropeptidase, lower incidence of seizures
Term
name the drug: IV, similar activity to imipenem, stable to renal dehydropeptidase, lower incidence of seizures
Definition
meropenem / doripenem
Term
describe ertapenem
Definition
IV, longer half life allows for once-daily dosing, lacks activity versus pseudomonas and acinetobacter
Term
name the drug: IV, longer half life allows for once-daily dosing, lacks activity versus pseudomonas and acinetobacter
Definition
ertapenem
Term
What type of drug is aztreonam?
Definition
monobactam
Term
name a monobactam
Definition
aztreonam
Term
aztreonam: MOA?
Definition
binds and inhibits cell wall transpeptidases
Term
What are the clinical applications for aztreonam?
Definition
infections caused by aerobic, gram negative bacteria in pts with immediate hypersensitivity to PCNs
Term
Which drug is used for infections caused by aerobic, gram negative bacteria in pts with immediate hypersensitivity to PCNs
Definition
aztreonam
Term
How is aztreonam given? How is it cleared? Is there cross allergenicity with PCNs?
Definition
IV, renally, no
Term
Vancomycin: MOA?
Definition
inhibits cell wall synthesis by binding D-ala D-ala terminus of nascent peptidoglycan
Term
How do the effects of vancomycin compare to B-lactam abx?
Definition
slower kill
Term
What are the clinical applications for vancomycin?
Definition
infections caused by gram positive bacteria including sepsis, endocarditis and meningitis, C difficile colitis (oral formulation)
Term
which drug is used for infections caused by gram positive bacteria including sepsis, endocarditis and meningitis, C difficile colitis (oral formulation)
Definition
vancomycin
Term
Name the drug: Oral and IV, renal clearance (6 hr half life), tox: red man syndrome, nephrotoxicity uncommon
Definition
vancomycin
Term
Describe teicoplanin
Definition
IV, similar to vanco except long half life permits once daily dosing
Term
Name the drug: IV, similar to vanco except long half life permits once daily dosing
Definition
teicoplanin
Term
describe dalbavancin
Definition
IV, very long half life 6-11d, once weekly dosing, more active than vanco
Term
name the drug: IV, very long half life 6-11d, once weekly dosing, more active than vanco
Definition
dalbavancin
Term
describe telavancin
Definition
IV, dual MOA results in improved activity against bacteria with reduced susceptibility to vancomycin
Term
name the drug: IV, dual MOA results in improved activity against bacteria with reduced susceptibility to vancomycin
Definition
telavancin
Term
What type of drug is daptomycin?
Definition
lipopeptide
Term
daptomycin: MOA?
Definition
binds cell membrane, causing depolarization and rapid cell death
Term
what are the effects of daptomycin compared to vanco
Definition
more rapidly bactericidal
Term
What are the clinical applications for daptomycin?
Definition
infections caused by gram positive bacteria including sepsis and endocarditis
Term
Name the drug: IV, renal clearance (half life 8hr), once daily dosing, inactivated by pulmonary surfactant so cannot be used to treat pneumonia, tox: myopathy, should monitor CK levels
Definition
deptomycin
Term
which drug is inactivated by pulmonary surfactant?
Definition
daptomycin
Term
which drug causes myopathy?
Definition
daptomycin
Term
Aminopenicillins offer better coverage of...
Definition
gram negative bacteria
Term
penicillinase-resistant PCNs are also called...
Definition
staphylococcal PCNs
Term
Anti-pseudomonal PCNs include which groups?
Definition
carboxy and ureidopenicillins and monobactams
Term
describe the coverage for cephalosporins
Definition
Resistant to beta-lactamase, broad spectrum of G+ and G-
Term
PCN G is acid ____, so it can be given ____.
Definition
labile, IM or IV
Term
PCN V is the oral form of ...
Definition
PCN G
Term
Name the aminopenicillins. How does their spectrum compare to PCN G? Why? Are they sensitive to b-lactamases?
Definition
ampicillin and amoxicillin, broader spectrum with better killing of G-, they can penetrate the outer membrane better and bind transpeptidases better, yes they are still sensitive to b-lactamase
Term
The G- bacteria killed by aminoPCNs include ______ and other enterics. However, resistance has developed and many enteric G- bacteria have acquired _____ and are resistant.
Definition
E coli, b-lactamases
Term
Both ampicillin and amoxacillin can be taken ____, but amoxicillin better absorbed this way.
Definition
orally
Term
IV ampicillin is commonly used with other ABX like aminoglycosides (gentamicin) for broad gram-_____ coverage
Definition
negative
Term
What are the penicillinase-resistant penicillins? What do they kill? How are they given?
Definition
methicillin, nafcillin, oxacillin, Staph aureus, only IV
Term
Naficillin is the DOC for...
Definition
serious staph aureus infections, like cellulitis, endocarditis, sepsis
Term
The clocks were ticking. It was only a matter of time before the ORAL beta-lactamase resistant PCNs were discovered. They are...
Definition
cloxacillin, dicloxacillin, flucloxacillin
Term
cloxacillin, dicloxacillin and flucoxacillin are not good against gram-_____ bacteria, they are used for gram-____ bacteria, especially those that produce _______, like _______
Definition
negative, positive, penicillinase, staph aureus
Term
Pt has infected skin wound. He most likely has _____ or _______. Would treating with PCN G, V or ampicillin work? Why or why not?
Definition
staph aureus or group A beta-hemolytic strep, those would not cover penicillinase-producing Staph. Treating with a penicillinase-resistant agent (meth, ox, naf) would, and if you give an oral abx (clox, diclox, fluclox) you can send him home with an Rx and don't have to care for him around the clock
Term
CarboxyPCNs and ureidoPCNs are what type of PCN? What are they good for?
Definition
anti-pseudomonal PCN, expanded G- rod coverage especially against pseudomonas, also active against anaerobes and G+ bacteria
Term
Pseudomonas was so tricky we needed James Bond to help. His tools include a special CAR, a trained TICK, and a PIPE bomb. What are the anti-pseudomonal PCNs?
Definition
carbenicillin and ticaricillin (carboxyPCNs), piperacillin, mezlocillin, azlocillin (ureidoPCNs)
Term
Like ampicillin, the anti-pseudomonal penicillins are frequently combined with ______ to double up the pseudomonas killing
Definition
aminoglycoside
Term
anti-pseudomonal ABX are sensitive to ________, and thus most _______ infections are resistant
Definition
penicillinases, staph
Term
What are the b-lactamase inhibitors?
Definition
clavulonic acid, sulbactam, tazobactam
Term
The generations of cephalosporins are based on...
Definition
activity against gram+ and gram-
Term
With each generation of cephalosporins, the drugs get better in which ways?
Definition
Increasingly able to kill G-, increasingly resistant to b-lactamases, increasingly potent
Term
The newer (3rd gen) cephalosporins are less effective against...
Definition
gram + organisms like staph and strep
Term
MRSA is resistant to all cephalosprorins because it has changed...
Definition
the structure of its PBP (transpeptidase). The enterococci are also resistant to cephalosporins
Term
FA, FAM, FUR, FOX, TEA - what is this?
Definition
2nd gen cephs - cefamandole, cefaclor, cefuroxime, cefoxitin, cefotetan
Term
around 10% of pts with allergy to PCN will also have allergy to...
Definition
cephalosporins
Term
How are first gen cephs used?
Definition
Excellent G+ coverage, so used as alternative to PCN for staph and strep infections. Surgeons love to use them before surgery to prevent infection from skin
Term
2nd gen cephalosporins cover more gram-____ rods. Cefuroxime is a good agent for CAP because it has good coverage against ____ and ____.
Definition
strep pneumo and H flu
Term
3 second gen cephalosporins have good coverage against anaerobes, making them good for abd/pelvic infections, aspiration pneumonia, and colorectal surgery prophylaxis. Which are they?
Definition
cefotetan, cefoxitin, cefmetazole - the fox met the anaerobic bug for tea
Term
In general, what are 3rd gen cephalosporins good for?
Definition
Multi-drug resistant aerobic G- organisms that cause nosocomial pneumonia, meningitis, sepsis and UTIs
Term
Which is the only cephalosporin that's good against pseudomonas?
Definition
ceftazidine
Term
What is special about ceftriaxone?
Definition
best CSF penetration, first line drug for meningitis in neonates, kids and adults. Also given IM for gonorrhea as more of these bugs have been resistant to tetracycline and PCN, pneumonia and pyelonephritis
Term
What bugs are still resistant to imipenem?
Definition
MRSA, some pseudomonas, mycoplasma
Term
Imipenem is ____ to beta-lactamases. It is very small and can pass through porin channels to the _____ space. There, it can interact with _____.
Definition
stable, periplasmic, transpeptidase
Term
inipenem can cause what types of reactions? It also lowers the threshold for what?
Definition
allergic, seizures
Term
Aztreonam - what's it good for?
Definition
it is a monobactam, good for AEROBIC GRAM NEGATIVE only, kills the tough ones like Pseudomonas
Term
can you use aztreoname in PCN-allergic pts?
Definition
Yes!
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