Antibacterial Agents Overview Flashcards
Cell Wall Synthesis Inhibitors
Penicillins, cephalosporins, carbapenems, and miscellaneous drugs
Active on cell walls, inhibiting transpeptidase and promoting cross-linking for a stronger wall
Penicillins
Penicillins are ________ on cell walls, inhibiting _____________ and promoting cross-linking for a stronger wall
active; transpeptidase
Defense mechanisms of Cell Wall Synthesis Inhibitors
Beta-lactamase enzymes countered by inhibitors like clavulanic acid
Resistance mechanisms of Penicillins:
Beta-lactamase, structural changes in proteins, or alterations in the outer wall.
Cell walls have sites that are amenable to ___________
transpeptidation
Cross-linking is facilitated by proteins acting on _____________ of the cell wall, linking them together
peptidoglycans
Penicillins have a ________ ring that binds to the protein
B-lactam
By inhibiting the penicillin binding protein, __________ of the cell wall will occur.
autocatalysis
B-lactamases (penicillinases) ___________ the B-lactam ring
break down
mechanism of most types of resistance
B-lactamases (penicillinases) break down the B-lactam ring
The breaking down of the B-lactam rings are countered by inhibitors of these enzymes
Clavulanic acid (i.e. amoxicillin-clavulanate)
Sulbactam (ampicillin sulbactam)
Tazobactam (i.e. piperacillin-tazobactam)
amoxicillin-clavulanate
Clavulanic acid
ampicillin sulbactam
Sulbactam
piperacillin-tazobactam
Tazobactam
Changes in the porin structures in the outer wall (i.e. pseudomonas aeruginosa are seen in __________ resistance
methicillin resistance
Penicillins that have very narrow spectrum
Methicillin, nafcillin, oxacillin
__________________ are resistant to all penicillins
methicilin resistant staphylococcus aureus
Penicillin linked to interstitial nephritis
Methicillin
Penicillin associated with neutropenia
Nafcillin
Penicillins that have wider spectrum but are still susceptible to B-lactamases
Ampicillin, amoxicillin
Ampicillin, amoxicillin are enhanced when used with ____________
clavulanate
In ______________ infections, ampicillin is complementary with ________
eneterococcal; aminoglycosides
Penicillins that have strong activity against gram-negative organisms
Piperacillin, ticarcillin
Penicillins that have compelmetary actions with aminoglycosides
Piperacillin, ticarcillin
These are susceptible to penicillinases, used with tazobactam to limit resistance
Piperacillin, ticarcillin
Piperacillin, ticarcillin are susceptible to penicillinases, used with _________ to limit resistance
tazobactam
First generation cephalosporins
Cefalozin, cephalexin
Used in surgical infections
First generation cephalosporins (Cefalozin, cephalexin)
Minimal effectiveness against gram-negative bacteria
First generation cephalosporins (Cefalozin, cephalexin)
Second generation cephalosporins
Cefotetan, cefoxitina, cefamandole, cefuroxime, cefactor
More active against gram-negative
Second generation cephalosporins (Cefotetan, cefoxitina, cefamandole, cefuroxime, cefactor)
Will also work against Haemophilus influenzae
Second generation cephalosporins (Cefotetan, cefoxitina, cefamandole, cefuroxime, cefactor)
Third generation cephalosporins
Ceftazidime, cefoperazone, cefotaxime, ceftriaxone
Even more active against gram-negative
Third generation cephalosporins (Ceftazidime, cefoperazone, cefotaxime, ceftriaxone)
Will often work against organisms that are resistant to penicillin
Third generation cephalosporins (Ceftazidime, cefoperazone, cefotaxime, ceftriaxone)
We only use these drugs in serious infections
Third generation cephalosporins (Ceftazidime, cefoperazone, cefotaxime, ceftriaxone)
Fourth generation cephalosporins
Cefepime,
More resistant to B-lactamases
Fourth generation cephalosporins (Cefepime, ceftaroline)
Eneterobacter, Haemophilus, Neisseria
has activity in infections caused by methicillin resistant staphylococci
Ceftaroline
less likely to cause rashes and allergic reactions than penicillins
Cephalosporins
Anti-infectives
Ceftaroline, ceftobiprole
Ceftaroline
Ceftobiprole
Community acquired pneumonia
Ceftaroline
Skin/soft tissue infections, inlucidng MRSA
Ceftaroline
Hospital acquired pneumonia
Ceftobiprole
Resistant to B-lactamases
Aztreonam
No activity against gtam-positive drugs
Aztreonam
Binds to penicillin-binding protein 3 (PBP3)
Aztreonam
Half-life is prolonged in renal failure
Aztreonam
Aztreonam ADE
GI upset
Vertigo, headache
No cross allergy with penicillins
Broad-spectrum activity against gram positives, gram negatives, anaerobes, and Pseudomonas.
Carbapenems
Carbapenems that are chemically unique, but still containing a B-lactam ring
Imipenem, doripenem, meropenem
Low susceptibility to penicillinases
Imipenem, doripenem, meropenem
Very susceptible to renal dehydropeptidases
Imipenem, doripenem, meropenem
Imipenem, doripenem, meropenem are very susceptible to renal dehydropeptidases, thus Administered with ______________
silastatin
Imipenem, doripenem, meropenem are wide ranging activity against:
gram -positive cocci
Gram-negative rods
Anaerobes
Pseudomonas and acinetobacter species
Used for severe infections, especially against resistant strains.
Vancomycin
Binds to a bacterial glycoprotein, causing “red man syndrome” (histamine release-induced severe cutaneous flushing).
Vancomycin
histamine release-induced severe cutaneous flushing
Red man syndrome
Bactericidal glycoprotein that binds to the alanine terminal of the peptidoglycan
Vancomycin
Resistant organisms have an altered terminal - decreased affinity for vancomycin
Vancomycin
Used for serious infections only
Vancomycin
Vancomycin does not cross the blood brain barrier - used ____________
intrathecally
Used orally for luminal infections of the gut
Vancomycin
Toxicity of Vancomycin
Red man syndrome
Phlebitis, otototxicity, nephrotoxicity
Topical treatment and decontamination for Staphylococcus colonization.
Bacitracin
Bacitracin is used in caution due to potential __________.
nephrotoxicity
Used in topical treatment and decontamination syndromes
Bacitracin
Used in staphylococcus colonization of the skin
Bacitracin
Marked nephrotoxicity - not used parenterally
Bacitracin
Cyclic lipopeptide for vancomycin-resistant strains.
Daptomycin
Requires close monitoring of creatinine kinase levels due to potential muscle disease.
Daptomycin
Cyclic lipopeptide
Daptomycin
For the treatment of VRE and VRSA
Daptomycin
During treatment of Daptomycin, creatinine kinase during treatment must be monitored because it is _____________
myopathic