L33 - Drugs Flashcards
Explain beta-lactamases resistance
Hydrolyze beta lacatam ring
Inactivates the drug
= penicillinases
What are 2 common alterations to the binding site that confer resistance
PBP2a from mecA
vanA (B, C)
= lives with the threat by changing the drug’s target site
Adverse event for penicillin
HST
Adverse event for vanco
Red Man
Nephro-oto-toxicity
Adverse event for daptomycin
Rhabdomyolysis
Eosinophilic pneumonia
Which drugs work ONLY on g+
Nafcillin
Vanco
Dapto
Bacitracin
Which drugs work ONLY on g-
Aztreonam
Polymyxins
Drugs active against MRSA
Ceftaroline
Vanco
Dapto
4 beta lactam agents
Penicillins
Cephalosporins
Carbapenems
Monobactams
Explain B lactam activity
Mimics d-ala-d-ala terminal end of peptidoglycan monomer NAM
Can’t cross link NAG and NAMs via transpeptidases
ALSO no remodeling after autolysins come in and cut bonds
Net = cell lysis from osmotic pressure as cell wall (peptidoglycan layer) is weakened
Penicillin bacteriocidal or static
Cidal
Explain the reasons penicillin is a good drug of choice vs bad
Good: - High therapeutic index - Good tissue penetration Bad: - Renally excreted --> dosing - Short 1/2 life --> frequent dosing - Bugs can be resistant easily via beta lactamases
What bugs does penicillin work against - draw the parallel to the clinical usage
GN cocci only - N.meningitis
GP broad - strep –> dental abscesses/human bites
Spirochetes - syphilis
IV & PO forms of the semi-synthetic penicillins (penicillinase resistant)
IV = Nafcillin PO = Dicloxacillin
What kinds of bacteria do Nafcillin & Dicloxacillin target?
G+ ONLY
How do bugs become resistant to semi-synthetic penicillin?
mecA gene –> PBP2a
What are the IV & PO aminopenicillins?
IV = Ampicillin PO = Amoxicillin
Which bacteria do aminopenicillins target?
G+ cocci & anaerobes
G- b/c R group is more polar allowing entry through porins
What is unique about Piperacillin? Downside?
G- w/ PSEUDO
G+
Limited use b/c of resistance (beta-lactamase) –> almost always used in combo (beta-lactamase inhibitor)
When do you give B lactamase inhibitors?
Give w/ resistant infections b/c extends the activity of penicillins
Ampicillin-sulbactam
IV
Conquers:
- Penicillinase S.aureus
- B-lactamase G- & anaerobes
Amoxicillin-clavulanic acid
PO
Conquers:
- Penicillinase S.aureus
- B-lactamase G- & anaerobes
Piperacillin-tazobactam
Conquers:
- Penicillinase S.aureus
- B-lactamase G- & anaerobes including PSEUDO!!