Chapter 9 Structures Flashcards
(8 cards)
Ciprofloxacin
2nd gen
lipophilic and amphoteric
distributes in to human cells
Admin: otic, opthalmic, oral, IV
DDI: theophylline, caffeine
Use: acinetobacter (but treat with combo of drugs), M. Catarrhalis, H. Influ, pasturella, eikenella, E. Coli, Salmonella, Shigella, Proteus Mirabilis, Proteus Vulgaris, providencia stuartii, citrobacter, enterobacter, P. aeruginosa (cipro works best), serratia (cipro works best), legionella, chlamydia, rickettsia, mycoplasma, ureaplasma, mycobacteria
Can also be used for anthrax, plague, and tularemia
Works best for UTI
DDI: CYP
mech of resistance: AAC(6’) acetylase - bind nitrogen which causes nitrogen to become unionizable which decreases affnity
undergo gluc (and recycling - all)
The piperazine ring and F help with extended spectrum and distribution
half life increased in renal impairment
Norfloxacin
2nd gen
lipophilic and amphoteric
admin: oral
DDI: CYP, theophylline, caffeine
undergo gluc (and recycling - all)
mech of resistance: AAC(6’) acetylase - bind nitrogen which causes nitrogen to become unionizable which decreases affnity
Use: acinetobacter (but treat with combo of drugs), M. Catarrhalis, H. Influ, pasturella, eikenella, E. Coli, Salmonella, Shigella, Proteus Mirabilis, Proteus Vulgaris, providencia stuartii, citrobacter, enterobacter, P. aeruginosa (cipro works best), serratia (cipro works best), legionella, chlamydia, rickettsia, mycoplasma, ureaplasma, mycobacteria
half life increased in renal impairment
Gatifloxacin
3rd gen
admin: otic, opthalmic
minimal CYP = blocked by substituents
half life increased in renal impairment
undergo gluc
block potassium channel in pancreatic tissue which blocks insulin release and causes hyperglycemia. This is particularly seen in pt with DM already
use: MSSA/MSSE (not best choice drug to use), PSSP, PRSP, other strep, listeria, acinetobacter (but treat with combo of drugs), M. Catarrhalis, H. Influ, pasturella, eikenella, E. Coli, Salmonella, Shigella, Proteus Mirabilis, Proteus Vulgaris, Klebsiella, providencia stuartii, citrobacter, enterobacter, P. aeruginosa, serratia, legionella, chlamydia, rickettsia, mycoplasma, ureaplasma, mycobacteria
Ofloxacin
- 5 gen
admin: otic, opthalmic, oral
Bridge = inc activity, dec DDI
chiral center
Levofloxacin has lower MIC value and can treat strep!
undergo gluc
Use: MSSA/MSSE (not best choice drug to use), PSSP, PRSP, other strep, acinetobacter (but treat with combo of drugs), M. Catarrhalis, H. Influ, pasturella, eikenella, E. Coli, Salmonella, Shigella, Proteus Mirabilis, Proteus Vulgaris, Klebsiella, providencia stuartii, citrobacter, enterobacter, P. aeruginosa, serratia, legionella, chlamydia, rickettsia, mycoplasma, ureaplasma, mycobacteria
Trovafloxacin
4th gen
too hepatoxic
metabolite is retained = inc high life
Moxifloxacin
4th gen
admin: oral
Long t1/2, more lipophilic, renal impairment inc t1/2
balanced excretion (R + biliary)
CYP blocked
undergo gluc
has activity for B. Fragilis, can be used for surgery prophylaxis
use: MSSA/MSSE (not best choice drug to use), PSSP, PRSP, other strep, listeria, acinetobacter (but treat with combo of drugs), M. Catarrhalis, H. Influ, pasturella, eikenella, E. Coli, Salmonella, Shigella, Proteus Mirabilis, Proteus Vulgaris, Klebsiella, providencia stuartii, citrobacter, enterobacter, P. aeruginosa, serratia, legionella (moxi works best), campylobacter, B. Fragilis, Prevotella, Clostridium, peptostrep, propionibacterium
chlamydia, rickettsia, mycoplasma, ureaplasma, mycobacteria (moxi works best)
Gemifloxacin
3rd gen
admin: oral
Nalidixic acid
1st gen FQ
Use: acinetobacter (but treat with combo of drugs), M. Catarrhalis, H. Influ, pasturella, eikenella, E. Coli, Salmonella, Shigella, Proteus Mirabilis, Proteus Vulgaris, Klebsiella, providencia stuartii, citrobacter, enterobacter, P. aeruginosa
short half life, highly PPB
