L22: Penicillins Flashcards
True or False: Penicillin G and Penicillin V/K are natural penicillins
True
Which four drugs are anti-staphylococcals?
1) Nafcillin
2) Oxacillin
3) Cloxacillin
4) Dicloxacillin
Ampicillin and Amoxicillin belong to which class?
A. Natural Penicillins
B. Anti-Staphylococcals
C. Anti-pseudomonals
D. Aminopenicillins
D. Aminopenicillins
Clavulanate, Tazobactam, and Avibactam belong to which group?
A. Natural Penicillins
B. Anti-Staphylococcals
C. Anti-pseudomonals
D. Aminopenicillins
E. Beta-lactamase Inhibitors
E. Beta-lactamase Inhibitors
True or False: Amoxicillin-clavulanate and Piperacillin-tazobactam are combination drugs
True
β-lactams antibiotics include which 4 major subgroups?
- Penicillins
- Cephalosporins
- Monobactams
- Carbapenems
Features shared by: 1) Penicillins, 2) Cephalosporins, 3) Monobactams, and 4) Carbapenems??
1) four membered lactam ring
2) can cause SJS
3) commonly used during pregnancy
What are two reasons for major resistance of β-lactams antibiotics?
1) Resistance to bacterial lactamase enzymes
2) Altered penicillin binding proteins
True or False: Lactamase inhibitors are co-formulated with penicillinsand other beta-lactams, to protect against degradation by lactamase enzymes
True
β-lactams inhibit _____ peptidoglycan cross-linking
transpeptidase-mediated
True or False: Transpeptidase reaction
site centers are found on D-alanyl-D-alanine, which β-lactam resembles
True
With β-lactam, transpeptidase mistakenly uses ___ as substrate, results in
irreversible inhibition
lactam
β-lactams inhibit transpeptidase-mediated peptidoglycan crosslinking.
Inhibition of peptidoglycan synthesis weakens ___, making it vulnerable to osmotic stress and rupture
cell well
β-lactams inhibit transpeptidase-mediated peptidoglycan crosslinking.
In this case, only ___ cells die – mechanism of cell death not completely understood
replicating
____: bacterial proteins that bind to penicillins & cephalosporins
penicillin binding proteins (PBP’s)
True or False: Only some bacteria with cell walls contain PBPs (penicillin binding proteins)
False - ALL bacteria with cell walls
contain PBPs (penicillin binding proteins)
True or False: Gram (-) strains contain B-lactamase while Gram (+) strains contain PBP
False –
Both Gram (+)/(-) contain PBP and B-lactamase
- However, B-lactamase is more externally located in Gram (+) while it is in more internal in Gram (-)
Structural differences & mutations in PBPs mean…?
They do not bind β-lactam drugs
- 4 of 5 PBPs in highly resistant Strep
pneumoniae have lower affinity for
penicillins
Alterations of PBP’s result in resistance typical of ___
MRSA
_____ commonly describes
organisms resistant to many beta-lactams
“Methicillin-resistant”
MRSA/ORSA refers to resistance to virtually all β-
lactams, including nearly all cephalosporins except 5th
gen agent ____
ceftaroline
___ is the leading cause of surgical site infection in
both tertiary and community hospitals
A. MRSA
B. ORSA
B. ORSA
____ is a β-lactamase with spectrum limited to
penicillins
Penicillinase
____ can hydrolyze a wide
variety of β-lactams; exclusive to gram(-) nosocomials
Extended Spectrum β-lactamases (ESBLs)
____: A few lactamase-producing individuals can protect an
entire community; this effect is commonly seen in Gram (+) microbes
Inoculum Effect
Which test uses substrate that changes color when degraded by lactamase?
Nitrocefin
Penicillins are more effective in ___ vs.
stationary growth phase
Logarithmic
Which four factors influence antibiotic efficacy?
1) Growth Phase
2) Population
3) Extracellular Biofilms
4) Location
True or False: Resistant minority microbes secrete lots of lactamase, which can protect neighbors
True
True or False: Bacteria persisting inside host cells are inaccessible to β-lactams + Adherent bacteria secrete polysaccharide
substrate
True
True or False: Penicillins are concentration-dependent, bacterialstatic agents
False - penicillins are TIME-DEPENDENT, BACTERICIDAL AGENTS
True or False: Penicillins kill power generally unaffected by low pH, low O2, or presence of proteins/constituents of pus
True
Where do penicillins distribute to? Where do they not distribute to?
Does: Joint, pleural, pericardial & bile fluids
Does NOT: Intraocular space, prostate, phagocytes, or CSF
when meninges are normal
When penicillins are used and meninges are inflamed, the drugs get into __
CNS