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Penicillins, Carbapenems, Aztreonam
The bulk of it
123
Pharmacology
Graduate
08/21/2010

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Term
Do PCN's get into CSF or Cells
Definition
Not usually, CSF only with inflamed meninges
No Intracellular penetration, add azithro or doxycylcine to get into cells
Term
Eleimnation of PCN's
Definition
Renal T1/2B of Pen G is 30 min
Probenecid inhibits renal acid transport system which secretes pen G and increases t1/2B of Pen G
Term
Hypersensitivity
Definition
major det - penicilloic acid breakdown product + endogenous protein
minor det = penicillin or a metabolite + end protein
Term
Pen G administration and use
Definition
Always I.v. b/c it is acid labile
do not use of staph aureus
DOC for B-hemolytic strep
Term
Treatment for Strep pneumo
Definition
Pen G
Term
DOC for
Definition
B-hemoytic streps Groups a,b,c,f, and G
Term
Larger dosing of Pen G
Definition
used to cover strep pneumo
Term
Pen G Resistance cross
Definition
If Pen G Restistant, then also Cephalosporing Resistant. However at low levels of R use cefotaxime ceftriaxone and cefepime
Term
Treatment of Syphilis and Neis meningitides
Definition
Pen G
Term
Pen V
Definition
active by p.o acid stable however low bioavailability
Use Amoxicillin instead
Group A strep kille dquickly by Pen G and pen VK
Term
Depot PCN's
Definition
Procaine penicillin G and benzathine pen G -
Do NOT give I.V.
i.m. gives slow release
Term
used prophylactically to prevent group A strep in military recruits
Definition
Depot PCN's procain and benzathine
Term
Used to treat syphillus do to long duration
Definition
benzathine pen G
not used for neurosyphillus
Term
MSSA infection godl standard treatment
Definition
oxacillin and nafcillin which are resistant to B-lactamase - but are still susceptible to binding site changes like in MRSA
Term
methicillin
Definition
first B-lactamase resistant PCN, no longer available due to nephrotoxicity
Term
MRSA is also called
Definition
ORSA - oxacillin RSA
Term
Treatment of soft tissue infection by MSSA and susceptible strep infections SSTI's
Definition
oxacillin nafcillin I.V.
dicloxacillin p.o.
Term
Dosage of oxacillin, nafcillin, dicloxacillin
Definition
q4h or q6h due to short half life
Term
outpatient treatment of SSTI's cause by MRSA
Definition
clindamycin, trimeth-sulfa, or doxycycline
Term
current inpatient regimen or SSTI's at UH
Definition
doxycycline + cefazolin
cefazolin is added b/c doxycycline does not cover GBS
Term
Treatment of inpatient infections caused by MRSA
Definition
i.v. vancomycin
Term
Use of B-lactamase inhibitors
Definition
coadministration of an inhibitor of the B-lactamase protects these PCN's from inactiavtion
Term
B-lactamase inhibitors
Definition
clavulanate
sulbactam
tazobactam
Term
aminopenecillins
Definition
extended spectrum PCN's
ampicillin and amoxicillin
both destroyted by B-lactamase
Term
Aminopenicillin spectrum of activity
Definition
bactericidal activity comparable to pen G
spectrum is extended to cover the gram (-) bugs E. coli and H. flu b/c these PCNs are better able to penetrate the outer mem brane of gram (-) bacteria
Term
Aminopenicillins are used in combination with what? Why?
Definition
Used in combination with B-lac inh like clav, sul, tazo, b/c they are not resistant to B-lactamases
Term
DOC for infections with Listeria spp. and Enterococcus spp.
Definition
Ampicillin I.V.
others active against enterococcis are vanc, pen G, peracillin, doxy, tigecylin, linezolid, and daptomycin
Term
Are Ampicillina and Amoxicillin active against MRSA
Definition
NO
Term
Administration of ampicillin
Definition
i.v. only b/c it causes diarrhea
Term
amoxicillin administaration
Definition
given po.o is not affected by the presence of food, often given with clavulanate which causes diarrhea
Term
antipseudomonal penicillins
Definition
designed to kill Pseudomonas aeruginosa, with activity against Enterobacter
Term
Antipseudomonal pnicillins given in combination with what? Why?
Definition
Given with aminoglycoside gentamicin due to resistance development
Term
Antipseudomonal treatement I.V. or P.O.?
Definition
IV only, no po equivalent
Term
What are teh anti-pseudomonal drugs?
Definition
ticarcillin + clavulanate(TImentin)
piperacillin - the best PCN vs. Pseudom
piperacillin + tazobactam (Zosyn/piptazo) - best anti-pseudomonal should be reserved for ICU
Term
DOC for B-emolytic strep (group A, B, C, F and G)
Definition
pen G and V
Term
DOC for susceptible Strep pneumo
Definition
amoxicillin/pen G
Term
DOC for meningococcal meningitis
Definition
use only pen G at higher doses
Term
DOC for MSSA - cellulities, abscesses, and other infectionsupt ot and including endocarditis and meningitis
Definition
oxacillin or naficillon i.v. or
dicloxacillin - p.o.
Term
DOC for otitis media in children
Definition
amoxicillin
Term
second line DOC for treatment of Otitis media
Definition
amoxicillin + clavulantate (Augmentin)
Term
DOC for inf cause by Pseudomonas and other nosocomial gram negatives
Definition
piperacillin +tazobactam
Term
Good MSSA and S. pneumo coverage
Definition
pip/tazo or ticarcillin + clavulanate
Term
DOC anaero
Definition
pip/tazo, or ticarcillin + clavulante
Term
Carbapenems
Definition
the same as PCN's but given I.v. only! and the broadset spectrum B-lactam ab drugs excetp for ertapenem
Term
ertapenem
Definition
Term
Carbapenems coverage
Definition
many nosocomial gram (-) rods, including Pseudomonas spp, anaerobes and gram (+) (very similar to spectrum of piptazo)
Term
Carbapenem problem
Definition
worst B-lactams for the treatment of Pseudomonas infetions 50% of isolates develop resistance during terapy. Mut eliminates porins.
Term
Carbapenem Resistance
Definition
Not hydrolyzed by most B-lactamases but are degraded by metallo B-lactamases. Klebsiella pneumo cabapenemase KPC enzyme is a huge problem.
Term
Carbapenem Drug names
Definition
Imipenem - given with renal DHP inhibitor cilastatin
meropenem - used for
ertapenem
doripenem
Term
side effect of imipenem
Definition
causes seizures in high doses in patients with poor renal function and neuro surgical patients
Term
side effect of imipenem
Definition
causes seizures in high doses in patients with poor renal function and neuro surgical patients
Term
meropenem use
Definition
used for meningitis b/c it is less likely to cause seizures. better for gram (-) bugs
Term
ertapenem coverage
Definition
does not cover Pseudomonas, Acinetobacter or enterococci
Term
Indications for cabapenems
Definition
good tissu penetration, drugs of last resort for MDR bugs, given to patients who have failed pip-tazo or cefepime
Term
Febrile neutropenic patients DOC
Definition
pipericillin tazo or cefepime
Term
Carbapenem cross reactivity
Definition
allergic reactions occur in 10-15% of patients with a Pen allergy
Term
Aztreonam spectrum of activity and MOA
Definition
MOA is same as PCNs
very good gram (-) activity including pseudomonas, comp to ceftazidime
NOT active against anaerobics and G+
Term
Aztreonam specturm of activity is similar to?
Definition
Aminoglycosides such as gentamicin
Term
Cross Resistance of Aztreonam
Definition
cross resistance with many 3rd gen Cephalosporins especially ceftazidime and cefepime
Term
Clinical use of aztreonam
Definition
I.V. only
little allergic cross reactivity with other B-lactams thus can be used in a patient with a PCN allergy for G(-) infections
Term
MOA of cephalosporins
Definition
same as PCN's
inhibit PG crosss linking by binding to the active site of the PBP's
Term
Resistance mechanism to Cephalosporins
Definition
same as PCN's changes in the PBP site, and some make cephalosporinases
Term
Cephalosporin Sceptrum of activity
Definition
varies between generations
all are relatively resistant to hydrolysis by B-lactamases = broader spectrum
No activity against Enterococcus, Listeria, PCN R Strep Pneumo or MRSA
Term
DOC for surgical prophylaxis good tissue penetration and cheap, good for SSTI's
Definition
Cefazolin
Term
Treats SSTIs, safe to use in pregnant women
Definition
Cephalexin
Term
1st generation cephalosporins
Definition
cefazolin
cephalexin
cephradine
Term
2nd generation Cephalosportins
Definition
cefoxitin
cefotetan
cefuroxime
cefaclor
Term
The only two cephamycins which cover anaerobic bugs
Definition
cefoxitin and cefotetan I.V. ONLY
Term
Used to treat pedi and FP outpatients
Definition
P.O. cefuroxime and cefaclor
Term
I.V. 2nd gen cephalorins
Definition
cefoxitin and cefotetan
Term
P.O. 2nd gen Cephalosportins
Definition
Cefuroxime, and cefaclor
Term
3rd gen I.V. Cephalosporins
Definition
cefotaxime
cetriaxone
ceftzidime
Term
3rd gen P.O. cephalosporins
Definition
cefpodoxime
cefdinir
cefixime
Term
I.M. 3g Ceph
Definition
ceftriaxone
Term
3rd gen drug that kills Pseudomonas
Definition
ceftazidime
Term
Turns feces brick red in children
Definition
cefdinir
Term
3rd gen cef for gonorrhea
Definition
cefixime not a good drug for Strep pneumo or MRSA
Term
1st gen Ceph Spectrum
Definition
best against gram +
Proteus
E
coli
Klebsiella
Term
2nd gen Ceph spectrum
Definition
gram(+), but add some gram (-) and anaerobes(only cefoxitin and cefotetan
Hen Peck
Haemophilus
enteroBacter
Neiserria
+1st gen PEcK
Term
3rd gen Ceph spectrum
Definition
increased gram (-) at the expense of gram + coverage (esp. MRSA)
Term
Can you use a 3G Ceph to treat MRSA
Definition
NO
Term
4th gen Ceph Spectrum
Definition
moderate G+ and excellent G(-) activity
Term
Do cephalosporins enter cells?
Definition
NO
Term
Do Cephalosporins enter CNS
Definition
Yes, with ceftazidime, ceftriaxone, cefotaxime, and cefepime
Term
Elimination of cephalosporins is mostly by
Definition
renal so decrease the does with impaired renal fxn. and diabetes
Term
Cephalosporing cross reactivity in patients with allergy to PCN's
Definition
as the generation goes up, the allergic cross reactivity does down
significant cross reactivity btween 1st gen cephalosporins and PCNs, less between 3rd and 4th
Term
Thromobphelbities
Definition
uncommon but can occur when the drugs, esp ceoxitin are gien by i.v. push
Term
Is superinfection common in treatement with cephalosportins?
Definition
Yes, anything with a broad spectrum coverage will give superinfection
Term
The other Cephalosporin side effect
Definition
prolongs prothrombin time causing bleeding
inhibit vit k epoxid red, most likely occurs with cfotetan
Term
Do cephalosporing cover enterococci or MRSA
Definition
NO
Term
Coverage of 1st gen cephalosporing, i.v. cefazolin and p.o. cephalexin and cephadrine
Definition
cefaxolin is agreat gram + drug with little G(-) activity, better than vancomycin for MSSA
Term
cefazolin coverage
Definition
MSSA, streptococci except S. pneumo, and the gram (-) bugs E.coli, K pneumo, Proteus, and H. flu
Proteus
E.
coli
Klebsiella
Term
Only cephalosporin with significant activity against anaerobic bugs?
Definition
Cefoxitin and cefotetan 2nd gen cephs
Term
Used to trat pelvic inflammatory disease and intra-abdominal infections
Definition
cefoxitin and cefotetan
Term
DOC for prophylaxis for intra-abdominal surgery
Definition
cefoxitin and cefotetan
Term
Ceftazidime coverage
Definition
gram (-) bugs including Pseudomonas aer. and bugs which end in bacter, but it has very little G+ activity
Term
DOC for treatement of strep pneumo infections including meningitis
Definition
Cefotaxime and ceftriaxone, b/c they are effective against low level Pen G R strep pneumo and are very potent with low MIC
Term
What is the difference between cefotaxime and ceftriaxone
Definition
t1/2 of ceftriaxone is 8h versus 1 hour for cefotaxime
Term
given in a single large I.M. dose for cervical, urethral, oropharyngeal or rectal gonorrhea
Definition
Ceftriaxone
Term
CDC recommended oral alternative for uncomplicated gonorrhea
Definition
Cefixime
Term
Used to treat meningities caused by strep pneumo and Neisseria spp.
Definition
Cefotaxime and ceftriaxone
Term
Good for the treatment of otitis media after tow failures with amoxacillin or augmentin(amox + clav)
Definition
Cefdinir
Term
Use of 4th gen cefepime
Definition
I.V. in the ICU esp in neutropenic patients
Term
4th gen ceph, cefepime spectrum of activity
Definition
moderate G+ and excellent gram (-) activity, active against Pseudomonas aer
Term
Improved activity over ceftazidime
Definition
cefepime 4th gen
Term
only ceph active against MRSA
Definition
ceftaroline
Term
#1 drug for surgical proph
Definition
cefazolin 1st gen cephalosporin
Term
Used to treat MSSA SSTI's but not MRSA
Definition
1st gen cephs
Term
along with oxacillin and nafcillin, better than vancomycin for MSSA
Definition
1st gen ceph,
Term
First line agent for patients with mild PCN allergy and MSSA infection
Definition
1st gen ceph
cefaxolin, cephalexin, cephradine
Term
#1 drugs for intra-abdominal surgical prophylaxis
Definition
2nd gen cephs cefoxitin and cefotetan
Term
used with gentamicin until the antibiotic suscept of the isolate is known
Definition
ceftazidime, i.v. for Pseudomonas aer
Term
Has No gram + activity
Definition
ceftazidime 3rd gen ceph
Term
Used for strep pneumo infections including meningitis and B-hemolytic strep
Definition
cefotaxime and cetriaxone i.v.
Term
used for community acquired meningities, H. flu, strep pneumo and Neisseria
Definition
cefotaxime 3rd gen cephalosporin
Term
Used for inpatient community acquired pneumonia = H. flu, strep pneumo, and Moraxella
Definition
cefotaxime and cetriaxone i.v.
a macrolide like clarithromycin can be added to cover the atypical bugs
Term
Used to treat uncomplicated gonorrhea with a single dose of
Definition
i.m. ceftriaxone or a single p.o. dose of cefixime
Term
febrile neutropenic patients where gram (-) bugs can kill in two hours so you need a bactericidal drug with stron gram (-) coverage
Definition
cefepime 4th gen ceph
Term
Treat inpatient strep pneumo, pseudomonas, ICU patients, mixed infections, unknown infections
Definition
cefepime
Term
Do cephalosporins cover enterococci or MRSA?
Definition
NO
Term
Gram + cephalosporin activity trend
Definition
1>2>3
Term
Gram (-) ceph activity trend
Definition
3>2>1
Term
Cephs with good anaerobic activity
Definition
Cefoxitin and cefotetan 2nd gen cephs
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