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Flouroquinolones
agents, adverse reactions, therapeutics, pharmacokinetics
59
Pharmacology
Professional
10/28/2011

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Cards

Term
What is the cause of the flouroquinolone's "downfall"?
Definition
their ease of use
Term
What is the original quinolone?
Definition
Nalidixic acid
Term
What did the flourine group do to the quinolones?
Definition
enhanced their spectrum of activity
Term
When were quinolones discovered?
Definition
1960s
Term
What are the "2nd generation" agents?
Definition
Ofloxacin
Norfloxacin
Ciprofloxacin
Lomefloxacin
Enoxacin
Term
Which "second generation" flouroquinolone is still used today?
Definition
ciprofloxacin
Term
List the newer flouroquinolone agents
Definition
levofloxacin
trovafloxacin
sparfloxacin
grepafloxacin
gatifloxacin
moxifloxacin
gemifloxacin
Term
Why was trovafloxacin and alatrofloxacin taken off the market?
Definition
severe hepatic toxicity
Term
Why was sparfloxacin taken off the market?
Definition
bad photosensitivity
Term
Why was grepafloxacin withdrawn from the market?
Definition
caused arrhythmias
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Why was gatifloxacin withdrawn from the market?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
DNA gyrase
Term
Which flouroquinolone target site is more important for effecting gram + bacteria?
Definition
topoisomerase IV
Term
What ratio is important in predicting the flouroquinolone response?
Definition
AUC/MIC
Term
Which pathogen must have a flouroquinolone and a beta-lactam to treat?
Definition
pseudomonas
Term
Which flouroquinolone is the least potent against E.coli and enteric gram - bacteria?
Definition
gemifloxacin
Term
Should flouroquinolones be used as anti-staphlococcal drugs?
Definition
no
Term
What is the only flouroquinolone that is good against anaerobes?
Definition
moxifloxacin
Term
Are flouroquinolones good against atypical drugs?
Definition
yes
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
through urine
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
UTIs
Term
What respiratory tract infections are flouroquinolones used for?
Definition
CAP
HAP/VAP/HCAP
Term
What is the second "downfall" of the flouroquinolones?
Definition
CAP
Term
What bacteria are the flouroquinolones active against for CAP?
Definition
S. pneumoniae
Term
Which flouroquinolone doesn't cover S. pneumoniae?
Definition
Ciprofloxacin
Term
What bacteria are flouroquinolones good against for hospital acquired pneumonia/ventilatory acquired pneumonia/HCAP?
Definition
P. aeruginosa
Term
Which two flouroquinolones are used against P. aeruginosa in combination with another P. aeruginosa agent?
Definition
cipro or levo
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
<18 yrs
Term
What are the flouroquinolones glycemic abnormalities?
Definition
hypo/hyper glycemia
Term
What are the dermatologic adverse effects?
Definition
photosensitivity
rash
Term
Which flouroquinolone has the worst photosensitivity adverse effects?
Definition
sparfloxacin
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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