Fluoroquinolones Flashcards
What is the MOA of fluoroquinolone?
Inhibition of DNA synthesis via inhibition of DNA gyrase and topoisomerase IV
What is the main enzyme targeted by FQs in Gram (+)?
Topoisomerase IV
What is the main enzyme targeted by FQs in Gram (-)?
DNA Gyrase (Topoisomerase II)
Which of the FQs is used against Gram + aerobes?
Levofloxacin, Moxifloxacin, Gemifloxacin
Which of the FQs is used against Gram - aerobes?
Ciporfloxacin = Levofloxacin > Moxifloxacin
What FQs should NOT be used for Pseudomonas?
Moxifloxacin
Gemifloxacin
What FQ should be used for anaerobes?
Moxifloxacin
What FQs should be used for atypical bacteria?
All of the FQs
What are the pharmokinetics of FQs?
Concentration-dependent bactericidal activity
What are the mechanisms of resistance to FQs?
Altered target sites
Efflux of the drug
Change in cell wall permeability
What is the old FQ that is still in use?
Ciprofloxacin
What are the new FQs?
Levofloxaxin
Moxifloxacin
Gemifloxacin
What FQs have good Gram + activity?
The newer ones.
Levofloxaxin
Moxifloxacin
Gemifloxacin
What is the best FQ against anaerobes?
Moxifloxacin
Which of the FQs has good CSF penetration?
Moxifloxacin
What FQs are used for CA pneumonia?
Levofloxaxin
Moxifloxacin
Gemifloxacin
What FQs are used for HCA pneumonia?
Ciprofloxacin (add a Gram + antibiotic)
Levofloxacin
What FQs are used to treat UTIs and prostatitis?
Ciprofloxacin
Levofloxacin
What FQs are used to treat sinusitis and bronchitis?
All of them
What FQs are used to treat TB?
Levofloxacin
Moxifloxacin
How are intrabdominal infections treated?
Use of a FQ alongside metronidazole for anaerobe coverage
What is used to treat Pseudomonas?
Ciprofloxacin
What are the SE of FQs?
GI problems
QT elongation
Tendonitis
Tendon rupture
What population should FQs NOT be used in?
Pregnant women
What are the drug interactions of FQs?
Divalent and trivalent cations will impair oral absorption of FQs
Warfarin + FQ will cause prolonged bleeding
Theophylline/Cyclosporine + FQ will cause a buildup of the former and lead to toxicity
49 yo female was admitted with a UTI. Urine culture is positive for E.Coli >100,000 colonies sensitive to fluoroquinolones. Which of the following is NOT appropriate treatment.
• A. Ciprofloxacin
• B. Levofloxacin
• C. Moxifloxacin
• C. Moxifloxacin - it doesn’t enter into the urine
- 24yo male is admitted with community acquired pneumonia. CXR shows a right middle lobe infiltrate. Sputum cultures are positive for Streptococcus pneumoniae sensitive to FQ’s. Which of the following in NOT appropriate treatment.
- A. Ciprofloxacin
- B. Levofloxacin
- C. Moxifloxacin
- D Gemifloxacin
• A. Ciprofloxacin
What is the MOA of metronidazole?
Ultimately inhibits DNA synthesis
- Prodrug that is activated by a reductive process
- Selective toxicity against anaerobic and microaerophilic bacteria due to the presence of ferredoxins within these
bacteria
- Ferredoxins are proteins that donate electrons to form
highly reactive nitro anion that damages bacterial DNA,
inhibit DNA synthesis, and cause cell death
What are the pharmokinetics of metronidazole?
Metronidazole displays concentration-dependent bactericidal activity
What are the mechanisms of resistance to metronidazole?
- Altered growth requirements – organisms grows in higher local oxygen concentrations causing decreased activation of metronidazole
- Altered ferredoxin levels – reduced transcription of the ferredoxin gene; less activation of metronidazole
What is the spectrum of activity of metronidazole?
Anaerobes
Peptostreptococcus spp. Bacteroides spp. (ALL)* Fusobacterium Prevotella spp. Clostridium spp. (ALL)* Helicobacter pylori
What are the administration methods of metronidazole?
IV or oral
What is the main metabolism of metronidazole?
Liver
What is metronidazole the drug of choice for?
Moderate C. difficile infection
What are the main SEs of metronidazole?
GI problems - nausea/vomiting
Peripheral neuropathy
What is the interaction of metronidazole and warfarin?
It will increase the anticoagulant effect of warfarin
Are the FQs removed in hemodialysis?
No
Is metronidazole removed in hemodialysis?
Yes