FA fluoroquinolones Flashcards
1st generation?
1st generation: nalidixic acid (oral)
2nd generation?
2nd generation: norfloxacin, ciprofloxacin, ofloxacin (oral), enoxacin (oral or IV)
3rd generation?
3rd generation: levofloxacin (oral or IV)
4th generation?
4th generation: moxifloxacin, gemifloxacin, gatifloxacin (oral)
respiratory fluoroquinolones?
Levofloxacin, moxifloxacin, and gemifloxacin are respiratory fluoroquinolones.
non-respiratory fluoroquinolones?
ciprofloxacin, enoxacin, norfloxacin, ofloxacin
fluoroquinolones mechanism?
inhibition of prokaryotic topoisomerase II (DNA gyrase) and topoisomerase IV→ DNA supercoiling → formation of double-stranded breaks → inhibition of DNA replication and transcription (bactericidal effect)
fluoroquinolones static or cidal?
cidal
fluoroquinolones must not be taken with what?
antacids
fluoroquinolones inhibits what 2 enzymes?
prokaryotic topoisomerase II (DNA gyrase) and topoisomerase IV
fluoroquinolones cns penetration?
good
fluoroquinolones route of ellimination?
Primarily renal (via glomerular filtration and tubular secretion)
Moxifloxacin undergoes biliary excretion.
Absorption is reduced when coadministered with polyvalent cations (e.g., magnesium, calcium, iron).
Norfloxacin, ciprofloxacin, and ofloxacin indications?
Norfloxacin, ciprofloxacin, and ofloxacin:
a) Gram-negative rods causing urinary and gastrointestinal infections
b) Some gram-positive pathogens
c) Genitourinary infections caused by Neisseria gonorrhoeae, Chlamydia trachomatis, and/or Ureaplasma urealyticum
c) Ciprofloxacin: Pseudomonas aeruginosa (e.g., malignant otitis externa)
ciprofloxacin special indication?
Ciprofloxacin: Pseudomonas aeruginosa (e.g., malignant otitis externa)
Levofloxacin, moxifloxacin, and gemifloxacin indications?
Levofloxacin, moxifloxacin, and gemifloxacin:
a) Atypical bacteria (e.g., Legionella spp., Mycoplasma spp., Chlamydophila pneumoniae)
b) Also effective against anaerobes
c) Gemifloxacin is highly potent against penicillin-resistant pneumococci.
d) Moxifloxacin: 2nd-line treatment of tuberculosis in patients who cannot tolerate antitubercular drugs and in multidrug resistant tuberculosis
fluoroquinolones adverse? dahuja cia
GI upset
Neurological symptoms
Mild headache
Dizziness
Mood changes
Peripheral neuropathy
Can lower seizure threshold (increased risk in patients taking NSAIDs and those with a previous history of epilepsy)
!!Hyperglycemia/hypoglycemia
!!QT prolongation
Photosensitivity
Skin rash
Superinfection (most commonly with gram-positive pathogens)
Potentially life-threatening exacerbations in patients with myasthenia gravis
In children: potential damage to growing cartilage → reversible arthropathy
!!!!!!Muscle ache, leg cramps, tendinitis, tendon rupture, especially of the Achilles tendon (the risk of tendon rupture is higher for individuals over 60 years of age and for individuals on steroid therapy)
fluoroquinolones special considerations?
Special considerations: increased risk for drug interactions as ciprofloxacin inhibits cytochrome P450
fluoroquinolones contraindications? dahuja
!!!Children and teenagers < 18 years of age
Patients > 60 years of age and those taking cortisol
!!!!!Pregnant women
!!!!Breastfeeding women
Epilepsy, stroke, CNS lesions/inflammation
QT prolongation
Myasthenia gravis
Cautious use in patients with:
Renal failure
Hepatic failure
Antacid use [61]
Known aortic aneurysm or increased risk of aneurysms (e.g., Marfan syndrome, Ehlers-Danlos syndrome, advanced age, peripheral atherosclerotic disease, hypertension)
fluoroquinolones resistance?
Mechanism of resistance
Chromosome-encoded mutation in DNA gyrase and topoisomerase IV enzymes
Altered cell wall permeability
Plasmid-encoded mutations in efflux pump proteins
