Beta lactams and cell wall inhibitors Flashcards
Penicillins- MOA
D-Ala-D-Ala analog –> inhibit the enzyme transpeptidase resulting in inhibition of the transpeptidation rxn. activating autolysis.
Penicillins- MOR
MRSA/PRSP- change PBP
Salmonella- efflux pump
Pseudomonas- change porin structure so drug cant penetrate
staph and gram neg- plasmid betalactamases.
Penicillin- classifications
Narrow spectrum- penicillinase susceptible
Very narrow spectrum- penicillinase resistant
Extended spectrum- penicillinase resistant
Narrow Spectrum penicillins- drugs
Penicillin G
Penicillin V
pehnoxyethyl penicillin
Narrow Spectrum penicillins- resistant strains
S. aureus
N. gonorrhea
Very narrow spectrum- drugs
Methicillin Nafcillin Oxacilin cloxacillin dicloxacillin
Very narrow spectrum- uses
Staph
Penicillinase resistant
Extended spectrum- drugs
amoxicillin
ampicillin
pipercillin
ticarcillin
extended spectrum- prenicillinase resistant?
No they are susceptible to penicillinase thus are used with beta lactamase inhibitors
extended spectrum + beta lactamase inhibitor pairings
amoxicillin- clavulonic acid
ampicillin- sublactam
pipercillin- tazobactam
ticarcillin- clavulonic acid
Cephalosporins- how many generations
4
Cephalosporins- What are the characteristics of the generations
Gram + coverage dec as you move up
Gram - coverage inc as you move up
resistance to beta-lactamases inc as you move up
CNS penetration- inc as you go up
Cephalosporins- MOR
inactivated by beta-lactamases esp staphylococci
Modificatino of PBP
MRSA / PRSP drug permeability
Cephalosporins- 1st generation - drug names
Cefazolin
Cephalexin
Cephalosporins- 2nd generation- drug names
Cetotetan
Cetoxitin
Cefuroxime
Cefaclor
Cephalosporins- 3rd generation - drug names
cetoxamine
ceftazadime
cetraixone
ceoperazone
Cephalosporins- 4th generation- drug names, characteristics and uses
Cerfepime
combines gram positive spectrum of 1st generation with the characteristics of the other generations
Monobactams- MOA
binds to PBP3
Monobactams- names
Aztreonam
Monobactams- uses
Aerobic Gram negative rods including pseudomonas
synergistic with aminoglycosides
Carbapenems- MOA
similar to other beta lactams
Carbapenems- Uses
Broad spectrum- So thy are used as a shotgun approach gram + cocci: Staph and strep Gram - rods: pseudomonas Anaerobes doesn't work agaisnt MRSA and listeria
Carbapenems- MOR
resistant to most beta lactamases
BUT is synthetic to metalo-beta-lactamases
Carbapenems- drugs
Imipenem
Meropenem
Ertapenem
Classes of beta- lactams
penicillins
cephalosporins
Monobactams
Carbapenems
Vancomycin- MOA
Binds to D-Ala-D-Ala inhibiting transglycosylase= inhibition of transglycosylation = elongation is blocked and damages membranes
Vancomycin- MOR
plasmid mediated changes of D-Ala-D-Ala to D-Ala-D-lactate.
plasmid mediated changes in permeability
Vancomycin- uses
Gram +’s- MRSA and PRSP
Endocarditis
beta-lactamase producers in people with a penicillin allergy- E. Faecalis
Oral is used to tx pseudomembranous colitis b/c it gets to colon unchanged
Daptomycin- clearance and monitoring
cleared by kidney
monitor CPK levels b/c can cause myopathy
Daptomycin- uses
VRE
VRSA
Fosfomycin- MOA
inhibits enolpyruvate transferase- prevents formation of N-Acetylmuramic acid
Fosfomycin- uses
Concentrates well in the Urinary tract system, and is excreted at levels greater than MIC therefore is good for UTI
fosfomycin- MOR
dec in intracellular concentration
Cefazolin- class
1st generation Cephlosporin
Cefazolin method of admin
IV
Cefazolin Uses
Clean surgical prophylaxis
UTI- Staph Saprophyticus, strep, or E.Coli
PEcK- Proteus, E Coli, Klebsiella
Cephalexin- class
1st generation Cephalosporin
Cephalexin- administration
Oral
Cephalexin- uses
skin & soft tissue infections
oral Cephalosporins- excretion, how well are they absorbed, AE
renal excretion
Absorbed well
superinfection, pseudomembranous colitis
Narrow Spectrum Penicillins- Uses
Strep Penumo- pharyngitis and meningitis non penicillinase staph anaerobes- closridia, actinomycosis niserria menigitidis treponemes GAS
narrow spectrum penicillins- which organ failure prompts dose change
Renal
penicillin G- class
narrow spectrum penicillin
penicillin G- how well is it absorbed, route of admin
IV
poorly absorbed
Types of Penicillin G- repository forms
Have additive that helps them hang around in muscle and last longer
Procaine
Benzocaine
Penicillin V- route of admin
Oral
Penicillin V- AE
Neurologic changes and acting funny
Pehnoxyethyl Penicillin- admin
Oral
Very narrow spectrum metabolism, exception
All are metabolized by the liver except for Methicillin,
Methicillin- what organ failure requires dose decrease
Renal
Methicillin- AE
Interstial nephritis= eosinophiluria, rash, arthralgias, eosinophilia, fever
NO LONGER USED
Nafcillin- Excretion
Bile
Nafcillin- AE
Neutropenia
Phlebitis
Oxacillin- AE
Neutropenia
LFT’s
Extended Specrum Penicillins- what organ has to fail to change dose
Kidney
Amoxicillin- admin
Oral
Ampicillin- uses
DOC for listeria when paired with an aminoglycoside (Amp Gent)
Amoxicillin/ Ampicillin uses
Infections of:Ear, Nose, Throat, and Lungs
Pen G sensitive organisms- H flu, proteus, Ecoli
What drug is always including when treating an elderly person for meningitis
Ampicillin b/c Listeria meningitis is a common cause of meningitis in this age group
Amoxicillin- AE
#1 cause of pseudomembranous colitis b/c it is broad spectrum and kills off natural flora- thus C. diff is no longer contained this is b/c is the most commonly prescribed penicillin
Pipercillin- route of admin
IV
Ticarcillin- route of admin
IV
Pipercilin/ Ticarcillin- uses
Use with aminoglycosides for- serious gram negatives- E. Faecalis, Pseudomonas
bacteroides fragilis, proteus
Extended spectrum penicillins + beta lactamases- uses
bacteroides
moraxella
beta lactamase producing strains of - staph auerus and H. Flu
Amoxicillin + Clavulanic acid- route of admin
Oral
Amoxicillin + Clavulanic acid- uses
upper and lower respiratory infections
Amoxicillin and Clavulonic Acid- AE
diarrhea, more than amoxicillin alone
Ampicillin + Sublactam- route of admin
IV
Ampicillin + Sublactam- uses
mixed non resistant aerobe/ anaerobe ie. dirty surgical infection, aspiration pneumonia
Pipercillin + Tazobactam- route of admin
IV
Ticarcillin + Clavulanic acid- route of admin
IV
Pipercillin + Tazobactam
Ticarcillin + Clavulanic acid- uses
VERY BROAD SPECTRUM- esp for gram negative
used for shotgun therapy
use with aminoglycosides for spectrum and synergy
switch to something different when you can
2nd generation Cephalosporins- Uses
Surgical prophylaxis
Community acquired adult pneumonia
Gram -: HENPEcK- H.Flu, Enetrobacter, Nisseria, Proteus, E.Coli, Klebsiella
Cefotetan- Class
2nd Generation Cephalosporin
Cefotetan- Uses
bacteroides
mixed intraabdominal/ pelvic infxns
Cefotetan- AE
Antabuse type rxn w/ EtOH
Cefoxitin- Use
BACTEROIDES
mixed intraabdominal/ pelvic infxns
Cefoxitin- Class
2nd Gen Cephalosporin
Cefuroxime- ROA and uses
IV= CNS- staph, strep, gram -, and serious pediactric pneumonia (b/c protects from meningitis)- ONLY 2ND GEN CEPHALOSPORIN W/ CNS COVERAGE
Oral- RTI, UTI
Cefaclor- class
2nd gen Cephalosporin
Cefaclor- ROA
Oral
Cefaclor- AE
Serum Sickness
3rd generation Cephalosporin- Uses
CNS INFXNS Hospital acquired Gram negatives gram negative infections- PS HEN PEcK Pseudomonas, Serratia H.Flu, Enterobacter, Niseeria Proteus, Ecoli, Klebsiella
Cefotaxime- Class
3rd Gen Cephalosporin
Cefotaxime- metabolism
Hepatic
Ceftazidime- uses
ONLY 3RD GEN WITH AXN AGAINST Pseudomonas when used synergistically with Aminoglycosides
Ceftriaxone- excretion
billary
Ceftriaxone- Use
DOC in Gonorrhea and MENINGITIS
community acquired infxns for coverage against strep pneumo
Why is Ceftriaxone used for meningitis
Good CNS penetration and good activity agaisnt meningococcus and strep pneumo
Ceftriaxone- Class
3rd Gen Cephalosporin
Cefoperazone- class
3rd Gen Cephalosporin
Cefoperazone- AE
antabuse like rxn w/ EtoH
4th gen Cephalosporin- uses
good for pretty much everything EXCEPT- Listeria, Enterococcus VRE, and MRSA
Cefepime- class
4th gen Cephalosporin
Cefepime- use
Pseudomonas
H.Flu
Can you use monobactams if the person had a penicillin allergy
Yes it should be fine
Imipenem- class
Carbepenems
Imipenem- what drug is it given with
Cilstatin- blocks its breakdown by dipeptidase in the renal tubules–> effective urinary concentrations of the drug
Imipenem- AE
seizures if there is impaired renal function that interferes with clearance
Procaine AE
Procaine Brain- when Procaine is injected into a muscle but accidentally hits a vein so it goes to the brain
Nafcillin/ Oxacillin ROA
Mostly IV
Cefotetan- t1/2
longest t1/2 of 2nd gen cephalosporins
Cefoxitn - t1/2
shortest t1/2 of the 2nd gen cephalosporins
Cefotaxime and Cefriaxone- use
Meningitis
Pneumonia
How is Cefoperazone different than other 3rd gen cephalosporins as far as distribution
NO CNS penetration
5th gen cephalosporin
Cefteroline
Ceftarroline- ROA
IV
Ceftaroline- CNS coverage
Maybe
Ceftaroline- clearance
Renal
Ceftaroline- Use
MRSA- ONLY CEPHALOSPORIN THAT CAN ATTACK MRSA
enterococcus, listeria, staph/ strep. comm aq pneumonia
Ertapenem
long t1/2
Cephalosporin, monobactam, carbepenem- AE
N/D- Antibiotic assoc Colitis Allergey- IgE cross reactivity with penicillin drugs EXCEPT MONOBACTAMS neutropenia, hemolytic anemia interstial nephritis SUPER INFXN
Vancomycin - distribution
distributed everywhere except- CNS, eye, prostate
vancomycin- AE
dose related nephrotoxicity- when combined with aminoglycosides
ototoxicity
narrow therapeutic range
red neck syndrome- due to histamine release- red, itchy, hypotension- give with an antihistamine. Occurs when you infuse vanco to rapidly
vancomycin- what levels should be measured when giving vanco
peak and trough levels
renal fxn
Telavancin- type of drug
derivative of vancomycin
telavancin- use
inc activity against MRSA
Telavancin- AE
more nephrotoxicity than vanco
nausea
taste perversion
Telavancin- pregnancy
CI in pregnancy
Telavancin vs vanco t1/2
telavancin has a longer t 1/2
Daptomycin- effect in the body
concentration dependent killing
long post antibiotic effect
Daptomycin- inactivated by what endogenous compound
good test question
Surfactant- thus is not active against lung infections
good test question
Daptomycin- AE
skeletal muscle toxicity= myalgias, weakness, elevated enzymes
synergisitc effect with statins