Antibiotics Flashcards
(93 cards)
Penicillin G,V
Mechanism?
D-Ala-D-Ala structural analog. Bind penicillin-binding proteins (transpeptidases).
Block transpeptidase cross-linking of peptidoglycan in cell wall.
Activate autolytic enzymes.
Penicillin G,V
Clinical Use?
Mostly used for gram ⊕ organisms (S pneumoniae, S pyogenes, Actinomyces). Also used for gram ⊝
cocci (mainly N meningitidis) and spirochetes (mainly T pallidum). Bactericidal for gram ⊕ cocci,
gram ⊕ rods, gram ⊝ cocci, and spirochetes. β-lactamase sensitive.
Penicillin G,V
Adverse Effects
Hypersensitivity reactions, direct Coombs ⊕ hemolytic anemia, drug-induced interstitial nephritis.
Penicillin G,V
Resistance
β-lactamase cleaves the β-lactam ring. Mutations in PBPs.
Penicillinase-sensitive
penicillins
Examples?
Amoxicillin, ampicillin; aminopenicillins
Penicillinase-sensitive
penicillins
Mechanisms?
Same as penicillin. Wider spectrum;
penicillinase sensitive. Also combine with
clavulanic acid to protect against destruction
by β-lactamase.
AMinoPenicillins are AMPed-up penicillin.
AmOxicillin has greater Oral bioavailability
than ampicillin.
Penicillinase-sensitive
penicillins
Clinical Use?
Extended-spectrum penicillin—H influenzae,
H pylori, E coli, Listeria monocytogenes,
Proteus mirabilis, Salmonella, Shigella,
enterococci.
Coverage: ampicillin/amoxicillin HHELPSS
kill enterococci.
Penicillinase-sensitive
penicillins
Adverse Effects?
Hypersensitivity reactions, rash,
pseudomembranous colitis.
Penicillinase-sensitive
penicillins
Resistance?
Penicillinase (a type of β-lactamase) cleaves
β-lactam ring
Penicillinase-resistant
penicillins
Examples
Dicloxacillin, nafcillin, oxacillin.
Penicillinase-resistant
penicillins
Mechanisms
Same as penicillin. Narrow spectrum;
penicillinase resistant because bulky R group
blocks access of β-lactamase to β-lactam ring.
Penicillinase-resistant
penicillins
Clinical Use
S aureus (except MRSA).
“Use naf (nafcillin) for staph.”
Penicillinase-resistant
penicillins
Adverse Effects
Hypersensitivity reactions, interstitial nephritis
Penicillinase-resistant
penicillins
Resistance
MRSA has altered penicillin-binding protein
target site.
Antipseudomonal
penicillins
Examples?
Piperacillin, ticarcillin.
Antipseudomonal
penicillins
Mechanism?
Same as penicillin. Extended spectrum. Penicillinase sensitive; use with β-lactamase inhibitors.
Antipseudomonal
penicillins
Clinical Use?
Pseudomonas spp. and gram ⊝ rods.
Antipseudomonal
penicillins
Adverse Effects
Hypersensitivity reactions.
Cephalosporins
Mechanism
β-lactam drugs that inhibit cell wall synthesis
but are less susceptible to penicillinases.
Bactericidal
Cephalosporins
What organisms are not covered by 1st-4th generation cephalosporins?
Listeria, Atypicals (Chlamydia, Mycoplasma),
MRSA, and Enterococci
Clinical Use and examples
1st generation Cephalosporins
1st generation (cefazolin, cephalexin)—gram ⊕
cocci, Proteus mirabilis, E coli, Klebsiella
pneumoniae. Cefazolin used prior to surgery to
prevent S aureus wound infections.
1st generation—⊕ PEcK
Clinical Use and examples
2nd generation Cephalosporins
2nd generation (cefaclor, cefoxitin, cefuroxime,
cefotetan)—gram ⊕ cocci, H influenzae,
Enterobacter aerogenes, Neisseria spp., Serratia
marcescens, Proteus mirabilis, E coli, Klebsiella
pneumoniae.
2nd graders wear fake fox fur to tea parties.
2nd generation—⊕ HENS PEcK
Clinical Use and examples
3rd generation Cephalosporins
3rd generation (ceftriaxone, cefotaxime, cefpodoxime, ceftazidime)—serious gram ⊝ infections resistant to other β-lactams.
Can cross blood-brain barrier.
Ceftriaxone—meningitis, gonorrhea,
disseminated Lyme disease.
Ceftazidime—Pseudomonas.
Clinical Use and examples
4th generation Cephalosporins
4th generation (cefepime)—gram ⊝ organisms, with increased activity against Pseudomonas and gram ⊕ organisms.