Cephalosporins Flashcards
Stability, metabolism, adverse effects, drug interactions, protein binding, half life
R2
Oral agents have good or bad absorption?
Good
Oral cephalosporins available as __________ and _________ compounds
prodrug esters
nonesterified compounds
Prodrug esters hydrolyzed in ___________ to active drug
Food enhances or decrease absorption
intestines
enhances
Cefuroxime (2nd gen.) and cefpodoxime proxetil (3rd gen) are
Prodrug esters
Binds to _________ and inhibits crosslinking of peptidoglycan strands
PBPs
Well or poorly distributed to body tissues and fluids?
Well
CSF penetration?
Yes, especially with inflamed meninges
Good for meningitis
High or low dosage?
3rd generation
Ceftriaxone
High (4X normal)
All ___________ excretion except 2 agents
Renal
Ceftriaxone and cefoperazone have ________ elimination
hepatic
_____________ associated with n-methylthiotetrazole side chain (NMTT)
bleeding
Cefamandole and cefoperazone disturb _________ factors
vitamin K clotting dependent
Causes disulfiram-like intolerance with _______________ when agents have _________
alcohol
NMTT side chain
Causes serum sickness in children
cefaclor (2nd gen)
Prolongs excretion in cephalosporins that have tubular secretion
Probenecid
Use for community acquired pneumonia
3rd generations
Use ceftaz and cefepime for
nosocomial pneumonia
Use ceftriazone for
meningitis with higher dosage
Use for simple cellulitis skin infections with staph and strep
1st generation
Use for complicated skin infections or diabetic patients
3rd/4th generations with cephamycins
Used for surgical prophylaxis
Cefazolin
Use ceftazidime/van or cefepime/van for
febrile neutropenia
Spectrum activity, PBP affinity, Beta-lactamase susceptibility
R1
