Fluoroquinolones Flashcards
Name the fluoroquinolones by class
1st generation - Norfloxacin
2nd generation - Ciprofloxacin, Ofloxacin
3rd generation - Levofloxacin
4th generation - Moxifloxacin, Gemifloxacin
Increasing Gram + activity with increasing generations
How do fluoroquinolones work?
DNA gyrase inhibition in gram - bacteria
(Gyrase clips DNA to allow it to supercoil)
Topoisomerase type 4 in gram +
(Topo clips DNA to allow daughter cells to uncoil)
What enzyme is targeted as an anticancer agent with fluoroquinolones?
Topoisomerase type 2
True or false: Fluoroquinolones require minimum concentrations to work
True, they’re concentration dependent
How are fluoroquinolones administered?
Orally available
How are fluoroquinolones excreted?
Renal excretion; dose adjusted in renal insufficiency
What is Norfloxacin used for?
UTI’s, prostatitis
What is Ciprofloxacin used for?
Sexually transmitted diseases (Chlamydia)
Anthrax
Intra-abdominal infections
What is Ofloxacin used for?
STD’s (Chlamydia)
Intra-abdominal infections
What is Gemifloxacin used for?
Community acquired pneumonia
What agents are fluoroquinolones against when treating infectious diarrhea?
Salmonella
Shigella
E. coli
What causes resistance with fluoroquinolones?
Mutations in topoisomerase IV or DNA gyrase
What toxicities do you have to worry about with fluoroquinolones?
GI disturbances (nausea, vomiting, pain)
CNS (Dizziness, headache, insomnia, hallucinations, seizures, photosensitivity)
Cartilage damage - children and pregnant women (rare)
QT prolongation, use with caution with type 1A and 3 anti-arrhythmics (esp moxfloxacin)
What drug do you have to worry about with arrhythmias?
Moxfloxacin
True or False: Fluoroquinolones cross the CNS
True
