Erdman - FQ Flashcards
all of the quinolones available today are structural derivatives of the original prototype agent of this class, ___ acid
nalidixic
MECHANISM OF ACTION
inhibition of ___ synthesis by binding to and inhibiting bacterial ___
- For many Gram ___ bacteria, DNA gyrase is the primary target
- For many Gram ___ bacteria (S. aureus), topoisomerase IV is the primary target of the FQs.
The FQs display ___ dependent bactericidal activity
DNA
topoisomerases
negative
positive
concentration
MECHANISMS OF RESISTANCE
- alteration in ___ sites (decreased affinity)
- expression of active ___
- alteration in cell wall ___
___ is usually observed between the FQs
- binding
- efflux
- permeability
- Cross-resistance
SOA
Gram-positive aerobes
- ciprofloxacin has ___ activity against Gram-positive bacteria
- Streptococcus pneumoniae: ___ – except ___
- MSSA
- (MRSA) – ONLY ___
Gram negative aerobes
- some FQs have excellent activity against Enterobacteriaceae (___ , ___ , ___ > gemifloxacin, moxifloxacin), H. influenzae, M. catarrhalis, and Neisseria species
- ____ (cipro≥levo>dela; NOT moxi or gemi)
- poor
- PRSP, ciprofloxacin
- delafloxacin
- ciprofloxacin, levofloxacin, delafloxacin
- Pseudomonas aeruginosa
SOA
___ – trovafloxacin had adequate activity against anaerobes including
Bacteroides fragilis; moxifloxacin has some activity but resistance is emerging
Atypical Bacteria – FQs are extremely active against ___ , Chlamydia,
Mycoplasma, and Ureaplasma
Other Organisms – Mycobacterium tuberculosis (cipro, levo, moxi, dela), Bacillus anthracis (cipro, levo
Anaerobes
Legionella
FQs exhibit rapid, ___ -dependent bactericidal activity
- FQs display a ___ against both Gram-positive (2 hours) and Gram-negative aerobic bacteria (2 to 4 hours)
concentration
PAE
Absorption
FQs are well absorbed after ___ administration
- Tmax is achieved within 1 to 2 hours; coingestion with food delays peak serum concentrations
oral
Distribution
- Most of the FQs display extensive tissue penetration obtaining therapeutic concentrations in the ___ , liver, ___ , ___ mucosa, ___ , bile, saliva, skin and soft tissue, ___ and into alveolar macrophages
- Some FQs achieve high urinary concentrations (not ___ and ___ ) making them useful for the treatment of UTIs and prostatitis
- FQs achieve ___ penetration into the CSF
- prostate, lung, bronchial, sputum, bone
- moxifloxacin, gemifloxacin
- minimal
Elimination
- Renal elimination – levofloxacin, ofloxacin, and gatifloxacin; dosage adjustments of these agents are necessary in the presence of renal insufficiency
- NONE of the FQs are removed during ___
- Hepatic metabolism elimination - trovafloxacin and moxifloxacin are primarily metabolized
- ___ , ___ , and gemifloxacin undergo both renal and hepatic elimination
- hemodialysis
- Ciprofloxacin, delafloxacin
CLINICAL USES
- Community-acquired pneumonia – levofloxacin, moxifloxacin, gemifloxacin and delafloxacin (new)
- Acute exacerbations of chronic bronchitis and sinusitis – ciprofloxacin, levofloxacin, moxifloxacin, and gemifloxacin
- Bacterial exacerbations in cystic fibrosis (P. aeruginosa) - ciprofloxacin
- Nosocomial pneumonia – ciprofloxacin and levofloxacin
- Urinary tract infections (cystitis, pyelonephritis) – ciprofloxacin, levofloxacin; norfloxacin (cystitis only)
- Chronic bacterial prostatitis – ciprofloxacin and levofloxacin
- Skin and skin structure infections – delafloxacin
- Osteomyelitis - ciprofloxacin and levofloxacin
- Other – intraabdominal infections (ciprofloxacin or levofloxacin with ___ , moxifloxacin alone); traveler’s diarrhea (ciprofloxacin, norfloxacin); tuberculosis (ciprofloxacin, levofloxacin, moxifloxacin); STDs; febrile neutropenia prophylaxis
and treatment (ciprofloxacin); eye infections
dont worry about these for the 2nd exam
- metronidazole
ADVERSE EFFECTS
GI
Neurologic
- ___
Hepatotoxicity
- ___ and ___
Phototoxicity
Cardiac
- ___ prolongation
- FQs should be used with
caution in patients with ___, concomitant use of class III
antiarrhythmics ( ___ and ___ ), preexisting QTc prolongation
Articular Damage
- contraindication in ___ , ___ , and ___ patients
Tendonitis and ___ Rupture
- peripheral neuropathy
- trovafloxacin, moxifloxacin
- QTc, hypokalemia, amiodarone, sotalol
- pediatric, pregnant, breastfeeding
- tendon
DRUG INTERACTIONS
- cations (Zn, Fe, Ca, Al, Mg) – including ___ , ddI, ___ , ___ feeds) impair the absorption of ANY ORAL FQ
- ___
- Theophylline and Cyclosporine - ___
- antacids, sucralfate, enteral
- warfarin
- ciprofloxacin
