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Why was grepafloxacin withdrawn from the market?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Why was gatifloxacin withdrawn from the market?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