Term
| What is the cause of the flouroquinolone's "downfall"? |
|
Definition
|
|
Term
| What is the original quinolone? |
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Definition
|
|
Term
| What did the flourine group do to the quinolones? |
|
Definition
| enhanced their spectrum of activity |
|
|
Term
| When were quinolones discovered? |
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Definition
|
|
Term
| What are the "2nd generation" agents? |
|
Definition
Ofloxacin
Norfloxacin
Ciprofloxacin
Lomefloxacin
Enoxacin |
|
|
Term
| Which "second generation" flouroquinolone is still used today? |
|
Definition
|
|
Term
| List the newer flouroquinolone agents |
|
Definition
levofloxacin
trovafloxacin
sparfloxacin
grepafloxacin
gatifloxacin
moxifloxacin
gemifloxacin |
|
|
Term
| Why was trovafloxacin and alatrofloxacin taken off the market? |
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Definition
|
|
Term
| Why was sparfloxacin taken off the market? |
|
Definition
|
|
Term
| Why was grepafloxacin withdrawn from the market? |
|
Definition
|
|
Term
| Why was gatifloxacin withdrawn from the market? |
|
Definition
| blood glucose abnormalities (hypo or hyper glucose) |
|
|
Term
| Which four quinolones are still used? |
|
Definition
ciprofloxacin
levofloxacin
moxifloxacin
gemifloxacin |
|
|
Term
| Are flouroquinolones bacteriostatic or bacteriacidal? |
|
Definition
| bactericidal under most circumstances |
|
|
Term
| What are the main target sites of flouroquinolones? |
|
Definition
DNA gyrase
topoisomerase IV |
|
|
Term
| What are DNA gyrase and topoisomerase IV essential for? |
|
Definition
| DNA duplication, transcription, repair |
|
|
Term
| Which flouroquinolone target site is more important for effecting gram - bacteria? |
|
Definition
|
|
Term
| Which flouroquinolone target site is more important for effecting gram + bacteria? |
|
Definition
|
|
Term
| What ratio is important in predicting the flouroquinolone response? |
|
Definition
|
|
Term
| Which pathogen must have a flouroquinolone and a beta-lactam to treat? |
|
Definition
|
|
Term
| Which flouroquinolone is the least potent against E.coli and enteric gram - bacteria? |
|
Definition
|
|
Term
| Should flouroquinolones be used as anti-staphlococcal drugs? |
|
Definition
|
|
Term
| What is the only flouroquinolone that is good against anaerobes? |
|
Definition
|
|
Term
| Are flouroquinolones good against atypical drugs? |
|
Definition
|
|
Term
| What are the three flouroquinolone mechanisms of resistance? |
|
Definition
decreased affinity for DNA gyrase and topoisomerase IV
decreased cell membrane permeability
efflux pumps |
|
|
Term
| What is the percent absorption of the flouroquinolones? |
|
Definition
excellent oral bioavailability
cipro 80%
all others close to/around 100% |
|
|
Term
| How are flouroquinolones distributed? |
|
Definition
| wide volume of distribution into most body sites |
|
|
Term
| How is ciprofloxacin metabolized? |
|
Definition
| partially metabolized by liver |
|
|
Term
| How is levofloxacin metabolized? |
|
Definition
no significant metabolism
basically 100% eliminated by kidney as unchanged drug |
|
|
Term
| How is moxifloxacin metabolized? |
|
Definition
| significant hepatic metabolism |
|
|
Term
| How is gemifloxacin metabolized? |
|
Definition
very limited hepatic metabolism
eliminated by kidney |
|
|
Term
| How is ciprofloxacin eliminated? |
|
Definition
| parent and metabolites through urine |
|
|
Term
| How is levofloxacin eliminated? |
|
Definition
|
|
Term
| How is moxifloxacin eliminated? |
|
Definition
| parent (minor) and metabolites (major) through feces and urine |
|
|
Term
| How is gemifloxacin eliminated? |
|
Definition
| parent (major) and metabolites (minor) through urine |
|
|
Term
| What is gemifloxacin's niche? |
|
Definition
| respiratory tract infections |
|
|
Term
| What are flouroquinolones therapeutic uses? |
|
Definition
genitourinary infections
respiratory tract infections
sexually transmitted diseases
bacterial gastroenteritis
osteomyelitis
skin and soft tissue infections |
|
|
Term
| What genitourinary infections are flouroquinolones used for? |
|
Definition
cystitis/pyelonephritis
prostatitis |
|
|
Term
| What is the most common use of flouroquinolones? |
|
Definition
|
|
Term
| What respiratory tract infections are flouroquinolones used for? |
|
Definition
|
|
Term
| What is the second "downfall" of the flouroquinolones? |
|
Definition
|
|
Term
| What bacteria are the flouroquinolones active against for CAP? |
|
Definition
|
|
Term
| Which flouroquinolone doesn't cover S. pneumoniae? |
|
Definition
|
|
Term
| What bacteria are flouroquinolones good against for hospital acquired pneumonia/ventilatory acquired pneumonia/HCAP? |
|
Definition
|
|
Term
| Which two flouroquinolones are used against P. aeruginosa in combination with another P. aeruginosa agent? |
|
Definition
|
|
Term
| What is levofloxacin structurally? |
|
Definition
| the L isomer of oxifloxacin |
|
|
Term
| What sexually transmitted disease are flouroquinolones used against? |
|
Definition
| gonococcal infections (alternative treatment) |
|
|
Term
| Which bacterial gastroenteritis species are flouroquinolones good against? |
|
Definition
| Salmonella, shigella, campylobacter |
|
|
Term
| What are the flouroquinolones adverse effects? |
|
Definition
GI toxicity
CNS problems
cardiac toxicity
tendon toxicity
cartilage malformation
glycemic abnormalities
dermatologic
hepatic toxicity |
|
|
Term
| What adverse GI effects occur with flouroquinolones? |
|
Definition
| N/V, diarrhea, abdominal discomfort |
|
|
Term
| What adverse CNS effects occur with flouroquinolones? |
|
Definition
headache, dizziness, insomnia, alteration in mood
seizures reported, but rare |
|
|
Term
| What cardiac toxicity do flouroquinolones have? |
|
Definition
QT prolongation of heart contraction
can lead to arrhythmia |
|
|
Term
| What tendon toxicity do flouroquinolones have? |
|
Definition
tendinities
Achilles tendon rupture |
|
|
Term
| What cartilage malformation adverse effects do flouroquinolones have? |
|
Definition
originally seen in juvinile dogs
never proven in humans |
|
|
Term
| In what population are flouroquinolones contraindicated? |
|
Definition
|
|
Term
| What are the flouroquinolones glycemic abnormalities? |
|
Definition
|
|
Term
| What are the dermatologic adverse effects? |
|
Definition
|
|
Term
| Which flouroquinolone has the worst photosensitivity adverse effects? |
|
Definition
|
|
Term
| Whih two flouroquinolones appear to not cause photosensitivity? |
|
Definition
| gatifloxacin and moxifloxacin |
|
|
Term
| What are the drug interactions for flouroquinolones? |
|
Definition
antacids, iron, and zinc reduce absorption
sucralfate
theophylline and caffeine (increased concentrations)
warfarin (increased anticoagulant effect)
also avoid drugs known to prolong QT interval including antiarrhythmic agents, phenothiazines, and TCAs |
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